MXPA06009895A

MXPA06009895A - Fused heterocycle derivative, medicinal composition containing the same, and medicinal use thereof

Info

Publication number: MXPA06009895A
Application number: MXPA/A/2006/009895A
Authority: MX
Inventors: Fujikura Hideki; Fushimi Nobuhiko; Isaji Masayuki
Original assignee: Kissei Pharmaceutical Co Ltd
Priority date: 2004-03-04
Filing date: 2006-08-31
Publication date: 2007-04-20

Abstract

A fused heterocycle derivative represented by the following general formula (I), a pharmacologically acceptable salt thereof, or a prodrug of either [in the formula, R1 to R4 each is hydrogen, OH, amino, etc.;R5 and R6 each is hydrogen, OH, halogeno, optionally substituted alkyl, etc.;Q is alkylene, alkenylene, etc.;ring A is aryl or heteroaryl;the ring (R1) shown below is any of the rings (R2) shown below;and G is a group represented by the following general formula (G-1) or (G-2) (wherein E1 is hydrogen, fluorine, or OH;and E2 is hydrogen, fluorine, methyl, etc.)]. They have human SGLT inhibitory activity and are useful as a preventive or therapeutic agent for diseases attributable to hyperglycemia, such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, complications of diabetes, and obesity.

Description

DERIVATIVE OF FUSED HETEROC1CLO. MEDICAL COMPOSITION CONTAINING THE SAME. AND MEDICAL USE OF THE SAME Technical Field The present invention relates to fused heterocyclic derivatives, pharmaceutically acceptable salts thereof or prodrugs thereof, which are useful as medicaments, pharmaceutical compositions comprising the same and pharmaceutical uses thereof. More particularly, the present invention relates to fused heterocyclic derivatives having an inhibitory activity in human SGLT, pharmaceutically acceptable salts thereof or prodrugs thereof which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes , impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising same and pharmaceutical uses thereof.

Previous Technique Diabetes is one of the diseases related to the lifestyle with the antecedent of change of the alimentary habit and lack of exercise. Therefore, exercise and diet therapies are performed in patients with diabetes. In addition, when sufficient control and continuous performance are difficult, drug treatment is performed simultaneously. In addition, it has been confirmed by the large-scale clinical trial that it is necessary to practice a strict long-term control of blood sugar levels in order to prevent diabetic complications from occurring in patients with diabetes when receiving treatment (for example, see the following references 1 and 2). In addition, many epidemiological studies on impaired glucose tolerance and macroangiopathy show that impaired glucose tolerance as the limit type is also a risk factor in macroangiopathy as well as diabetes. In this way, needs have been found to improve postprandial hyperglycemia (for example, see the following reference 3). In recent years, the development of several antidiabetic agents has progressed with the history of a rapid increase in patients with diabetes. For example, antidiabetic agents such as biguanides, sulfonylureas, insulin sensitivity enhancers, a-glucosidase inhibitors and the like have been employed. However, biguanides and sulfonylureas occasionally show adverse effects such as lactic acidosis and hypoglycemia, respectively. Insulin sensitivity enhancers occasionally show adverse effects such as edema, and advancement of obesity is concerned. In addition, a-glucosidase inhibitors, which delay the digestion and absorption of carbohydrates in the small intestine, are used to improve postprandial hyperglycemia. It has also been reported that acarbose, one of the α-glucosidase inhibitors, has an effect in preventing or delaying the incidence of diabetes when applied to patients with impaired glucose tolerance (for example, see the following reference 4). However, since α-glucosidase inhibitors do not affect high glucose levels by ingesting a glucose monosaccharide (e.g., see the following reference 5), with freshly changing compositions of sugars in meals, a wider range of activities inhibiting the absorption of carbohydrates has been desired. In recent years, the search and development of new types of antidiabetic agents has been in progress, promoting urinary glucose excretion and lower blood glucose level by preventing excess glucose reabsorption in the kidney (for example, see following reference 6). In addition, it is reported that SGLT2 (sodium-dependent glucose transporter 2) is present in the S1 segment of the proximal tubule of the kidney and participates mainly in the reabsorption of glucose filtered through glomerular (for example, see the following reference 7). According to the above, the inhibition of human SGLT2 activity prevents the reabsorption of excess glucose in the kidney, subsequently promotes the excretion of excess glucose through the urine, and normalizes the level of glucose in the blood. In addition, since such agents to promote the excretion of urinary glucose excrete excess glucose through the urine and consequently the accumulation in the body is decreased, it is also expected to have an effect of prevention or alleviation in obesity and a diuretic effect. In addition, the agents are considered useful for several related diseases that occur accompanying the progress of diabetes or obesity due to hyperglycemia. In addition, it has been known that SGLT1, a sodium-dependent glucose transporter 1, exists in the small intestine that controls the absorption of carbohydrates. It has also been reported that the insufficiency of galactose and glucose absorption originates in patients with dysfunction due to congenital abnormalities of human SGLT1 (for example, see the following references 8-10). In addition, it has been confirmed that SGLT1 is included in galactose and glucose uptake (for example, see the following references 1 1 and 12). Furthermore, it is confirmed that the increase in mRNA and SGLT1 protein and glucose absorption are accelerated in OLETF rats and rats with diabetic symptoms induced by streptozotocin (for example, see the following references 13 and 14). Generally in patients with diabetes, the digestion and absorption of carbohydrates increase. For example, it is confirmed that mRNA and SGLT1 protein are highly increased in the human small intestine (for example, see the following reference 15). Therefore, blocking a human SGLT1 activity inhibits the absorption of carbohydrates such as glucose in the small intestine, subsequently preventing the increase of the blood sugar level. Especially, it is considered that the delay of the absorption of glucose based on the mechanism mentioned above is effective to normalize the postprandial hyperglycemia. Therefore, the rapid development of antidiabetic agents with a new mechanism of action, which has an inhibitory activity in human SGLT, has been desired to improve or solve the aforementioned problems. The fused heterocyclic derivatives provided in the present invention are completely new compounds. It has not been reported that these derivatives have inhibitory activities in SGLT1 and / or SGLT2 and inhibit the absorption of glucose and galactose in the small intestine, or are useful as agents to inhibit the reabsorption of excess glucose in the kidney. Reference 1: The Diabetes Control and Complications Trial Research Group, N. Engl. J. Med. , 1993.9, Vol. 329, No. 14, pp. 977-986; Reference 2: UK Prospective Diabetes Study Group, Lancet, 1998.9, Vol. 352, No. 9131, p. 837-853; Reference 3: Makoto TOMINGA, Endocrinology & Diabetology, 2001 .1 1, Vol. 13, No. 5, pp. 534-542; Reference 4: Jean-Louis Chiasson and 5 persons, Lancet, 2002.6, Vol. 359, No. 9323, p. 2072-2077; Reference 5: Hiroyuki ODAKA and 3 persons, Journal of Japanese Society of Nutrition and Food Science, 1992, Vol. 45, p. 27; Reference 6: Luciano Rossetti and 4 persons, J. Clin. Invest., 1987.5, Vol. 79, pp. 1510-1515; Reference 7: Yoshikatsu Kanai and 4 persons, J. Clin. Invest., 1994.1, Vol.93, pp.397-404; Reference 8: Tadao BABA and 1 person, Supplementary volume of Nippon Rinsho, Ryoikibetsu Shokogun, 1998, No. 19, pp.552-554; Reference 9: Michihiro KASAHARA and 2 persons, Saishin Igaku, 1996.1, Vol.51, No. 1, pp.84-90; Reference 10: Tomofusa TSUCHIYA and 1 person, Nippon Rinsho, 1997. 8, Vol.55, No.8, pp.2131-2139; Reference 11: Yoshikatsu KANAI, Kidney and Dialysis, 1998.12, Vol. 45, extra edition, pp.232-237; Reference 12: E. Turk and 4 persons, Nature, 1991.3, Vol. 350, pp. 354-356; Reference 13: Y. Fujita and 5 persons, Diabetologia, 1998, Vol. 41, pp. 1459-1466; Reference 14: J. Dyer and 5 Persons, Biochemical Society Transactions, 1997, Vol.25, p.479S; Reference 15: J. Dyer and 4 persons, American Journal of Physiology, 2002.2, Vol.282, No.2, pp. G241-G248.

Brief Description of the Invention The present inventors have previously studied finding compounds having an inhibitory activity in human SGLT. As a result, it was found that certain heterocyclic derivatives represented by the following general formula (I) show an inhibitory activity in human SGLT1 and / or SGLT2 and are excellent agents having inhibitory activity in increasing blood glucose level or decreasing the level of blood glucose as shown below, thus forming the basis of the present invention. The present invention is to provide novel compounds that show inhibitory activity in human SGLT, pharmaceutical compositions comprising same and pharmaceutical uses thereof. That is, the present invention relates to [1] a fused heterocyclic derivative represented by the following general formula (I): wherein R1 to R4 independently represent a hydrogen atom, a hydroxy group, an amino group, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a cyano group, a carboxy group, an alkoxycarbonyl group C2-7, a carbamoyl group, a mono- or di- (C? -6) amino group, a halo group (C? -6 alkyl), a hydroxy group (C1-6 alkyl), a cyano group (C1-6 alkyl) 6), a carboxy group (C 1-6 alkyl), a C 2-7 alkoxycarbonyl group (C 1-6 alkyl), a carbamoyl group (C 1-6 alkyl), an amino group (C 1-6 alkyl), a mono group or di (C 1-6 alkyl) amino (C 1-6 alkyl), a halo group (C 1-6 alkoxy), a hydroxy group (C 1-6 alkoxy), a carboxy group (C 1-6 alkoxy), a C 2 alkoxycarbonyl group -7 (C6-alkoxy), a carbamoyl group (C1-6 alkoxy), an amino group (C6-alkoxy), a mono- or di (C1-6 alkyl) group (alkoxy d6), a group C3-7 cycloalkyl, a C3-7 cycloalkyl group, a C3-7 cycloalkyl group (C1-6 alkyl), or a C3-7 cycloalkyl group (C1-6 alkoxy); R5 and R6 independently represent a hydrogen atom, a hydroxy group, a halogen atom, a C-? 6 alkyl group, a C2-6 alkenyl group, a C2.6 alkynyl group, a C1-6 alkoxy group, a C 2-6 alkenyloxy group, a C 1-6 alkylthio group, a C 2-6 alkenylthio group, a halo (C 1-6 alkyl) group, a halo (C 1-6 alkoxy) group, a halo (C 1-6 alkylthio) group , a hydroxy group (C? -6 alkyl), a hydroxy group (C2-6 alkenyl), a hydroxy group (C1-6 alkoxy), a hydroxy group (C -6 alkylthio), a carboxy group, a carboxy group ( alkyl d 6), a carboxy group (C 2-6 alkenyl), a carboxy group (C 1-6 alkoxy), a carboxy group (C 1-6 alkylthio), a C 2-7 alkoxycarbonyl group, a C 2-7 alkoxycarbonyl group (C 1 -6 alkyl) -6), a C2-7 alkoxycarbonyl group (C2-6 alkenyl), a C2-7 alkoxycarbonyl group (C1-6 alkoxy), a C2-7 alkoxycarbonyl group (C1-6 alkylthio), a C1-6 alkylsulfonyl group, an alkylsulfonyl group C? -6, -UVWN (R7) -Z or any of the following substituents (i) ) to (xxviii) which may have any of 1 to 3 groups selected from the following substituent group a on the ring; (i) a C6-10 aryl group, (ü) aryl-O-C6-10, (iii) aryl-S-C6-? o, (iv) a C6-? o aryl group (C1-6 alkyl), (v) a C6-? or (C6-6 alkoxy) aryl group, (vi) a C6-? 0 aryl group (C6-6 alkylthio), (vii) a heteroaryl group, (viii) heteroaryl-O-, ( ix) heteroaryl-S-, (x) a heteroaryl group (C 1-6 alkyl), (xi) a heteroaryl group (C 1-6 alkoxy), (xi i) a heteroaryl group (C 1-6 alkylthio), (xiii) a C 3-7 cycloalkyl group, (xiv) cycloalkyl-O-C 3-7, ( xv) cycloalkyl-S-C3-7, (xvi) a C3- (C6-6 alkyl) cycloalkyl group, (xvii) a C3-7 cycloalkyl group (C6-alkoxy), (xviii) a C3-7 cycloalkyl group (C 1-6 alkylthio), (xix) a heterocycloalkyl group, (xx) heterocycloalkyl-O-, (xxi) heterocycloalkyl-S-, (xxii) a heterocycloalkyl group (C 1-6 alkyl), (xxiii) a heterocycloalkyl group ( C 1-6 alkoxy), (xxiv) a heterocycloalkyl group (C 1-6 alkylthio), (xxv) an aromatic cyclic amino group, (xxvi) an aromatic cyclic amino group (C 1-6 alkyl), (xxvii) a cyclic amino group aromatic (C 1-6 alkoxy), or (xxviii) an aromatic cyclic amino group (alkylthio Ci. 6), U represents -O-, -S- or a single bond and with the proviso that at least one of V and W is not a single bond, when U is -O- or -S-); V represents a C1-6 alkylene group which may have a hydroxy group, a C2-6 alkenylene group or a single bond; W represents -CO-, -S02-, -C (= NH) - or a single bond; Z represents a hydrogen atom, a C2.7 alkoxycarbonyl group, a C6-10 aryl group (C2-7 alkoxycarbonyl), a formyl group, -RA, -CORB, -SO2RB, -CON (Rc) RD, -CSN ( RC) RD, -SO2NHRA or -C (= NRE) N (RF) RG; R7, RA, Rc and RD independently represent a hydrogen atom, a C1-6 alkyl group which may have any of 1 to 5 groups selected from the following substituent group β, or any of the following substituents (xxix) to (xxxii) which they may have any of 1 to 3 groups selected from the following substituent group a; (xxix) a C6-? or aryl group, (xxx) a heteroaryl group, (xxxi) a C3-7 cycloalkyl group or (xxxii) a heterocycloalkyl group or Z and R7 together with the next nitrogen atom to form a aliphatic cyclic amino group which may have any of 1 to 3 groups selected from the following substituent group a; or Rc and RD are joined together with the next nitrogen atom to form an aliphatic cyclic amino group which may have any of 1 to 3 g selected from the following substituent group a; RB represents a C2-7 alkoxycarbonyl group, a C1-6 alkylsulfonylamino group, a C6-6alkylsulfonylamino group. a C1-6 alkyl group which may have any of 1 to 5 g groups selected from the following substituent group β, or any of the following substituents (xxxiii) to (xxxvi) which may have any of 1 to 3 groups selected from the following substituent group to; (xxxiii) a g arpo aryl C6-? or, (xxxiv) a heteroaryl group, (xxxv) a C3-7 cycloalkyl group or (xxxvi) a heterocycloalkyl group RE, RF and RG independently represent a hydrogen atom, a cyano group, a carbamoyl group, an acyl group C2 -7, a C2-7 alkoxycarbonyl group, a C6- or C2- (C2.7 alkoxycarbonyl) group, a nitro group, a C1-6 alkylsulfonyl group, a sulfamide group, a carbamimidoyl group, or a C1-6 alkyl group which may have any of 1 to 5 groups selected from the following substituent group ß; or RE and RF join to form an ethylene group; or RF and RG are joined with the next nitrogen atom to form an aliphatic cyclic amino group which may have any group selected from the following substituent group a; Q represents -C1-6alkylene-, -C2-6alkenylene-, -alkynylene C2.6-, -C1-6alkylene-O-, -C1-6alkylene-S-, -O-C1-6alkylene-, -S- C1-6alkylene-, -C1-6alkylene-O-alkylene C1-6-, -C1-6alkylene-S- C1-6alkylene-, -CON (R8) -, -N (R8) CO-, -C1-6alkylene-CON (R8) - or - CON (R8) ) -C1-6alkylene-; R8 represents a hydrogen atom or a C1-6 alkyl group; ring A represents a C6.10 aryl group or a heteroaryl group; ring: It represents R9 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group (C6 alkyl), a C3-7 cycloalkyl group or a C3-7 cycloalkyl group (C1-6 alkyl); G represents a group represented by a formula: or a formula: E1 represents a hydrogen atom, a fluorine atom or a hydroxy group; E2 represents a hydrogen atom, a fluorine atom, a methyl group or a hydroxymethyl group; [substituent group a] a halogen atom, a hydroxy group, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group, a halo (C1-6 alkyl) group, a halo (C1-6 alkoxy) group ), a hydroxy group (C 1-6 alkyl), a C 2-7 alkoxycarbonyl group (C 1-6 alkyl), a hydroxy group (C 1-6 alkoxy), an amino group (C 1-6 alkyl), an amino group (alkoxy) C1-6), a mono- or di (C6-alkyl) amino group, a mono- or di-hydroxy (C1-6 alkyl) amino group, a C1-6 alkylsulfonyl group, an alkylsulfonylamino group C -? - 6, a C1-6 alkylsulfonylamino group (C6 alkyl), a carboxy group, a C 2-7 alkoxycarbonyl group, a sulfamoyl group and -CON (RH) R '[substituent group β] a halogen atom, a hydroxy group, an amino group, a C 1-6 alkoxy group, an alkylthio group C 1-6, a halo (C 1-6 alkoxy) group, a halo (C 1-6 alkylthio) group, a hydroxy group (C 1-6 -alkoxy), a hydroxy group (C 1-6 alkyl), an amino group (C 1-6 alkoxy), an amino group (C 1-6 alkylthio), a mono- or di- (C 1-6 alkyl) amino group, a mono- or di-hydroxy (C 1-6) alkyl] amino group, a ureido group, a sulphonamide group, a mono- or di- (C6-6) ureido group, a mono- or di-hydroxy (C1-6 alkyl)] ureido group, a mono- or di- (C1-6 alkyl) group; Sulfonamide, a mono- or di-hydroxy (C 1-6 alkyl) - suifamide group, a C 2-7 acylamino group, an amino group (C 2-7 acylamino), a C 1-6 alkylsulfonyl group, a C 1-7 alkylsulfonylamino group 6, a carbamoyl (C 1-6 alkylsulfonylamino) group, a carboxy group, a C 2 - alkoxycarbonyl group, -CON (RH) R ', and any of the following substituents (x xxvii) a (xxxxviii) which may have any of 1 to 3 groups selected from the substituent group a above in the ring; (xxxvii) an aryl group C6-? o, (xxxviii) aryl C6- oO-, (xxxix) an aryl group C6-? o (C6-alkoxy), (xxxx) a C6-? o aryl group (C1- alkylthio) 6), (xxxxi) a heteroaryl group, (xxxxii) heteroaryl-O-, (xxxxiii) a C3-7 cycloalkyl group, (xxxxiv) C3-7-O- cycloalkyl, (xxxxv) a heterocycloalkyl group, (xxxxvi) heterocycloalkyl-O-, (xxxxvii) an aliphatic cyclic amino group or (xxxxviii) an aromatic cyclic amino group RH and R1 independently represent a hydrogen atom or a C1-6 alkyl group which may have any of 1 to 3 groups selected from the following substituent group? or both of RH and R1 are joined together with the next nitrogen atom to form an aliphatic cyclic amino group which may have any of 1 to 3 groups selected from the following substituent group d; [substituent group?] a halogen atom, a hydroxy group, an amino group, a C? -6 alkoxy group, a halo (C1-6 alkoxy) group, a hydroxy (alkoxy) group C-uß), an amino group (C 1-6 alkoxy), a mono- or di- (C 1-6 alkyl) group, a mono- or di-hydroxy (C 1-6) alkyl] amino group, a ureido group, a sulfamide group , a mono- or di- (C1-6 alkyl) ureido group, a mono- or di-hydroxy (C-? 6-alkyl)] ureido group, a mono- or di- (Ci- 6 alkyl) sulfamide group, a mono- or di- [hydroxy (C6 alkyl)] - sulfamide, a C2-7 acylamino group, an amino group (C2-7 acylamino), a C6 alkylsulfonyl group, a C6 alkylsulfonylamino group, a carbamoyl (C1-7 alkylsulfonylamino group) 6), a carboxy group, a C2-7 alkoxycarbonyl group, a sulfamoyl group and -CON (RJ) R? [substituent group d] a halogen atom, a hydroxy group, an amino group, a C1-6 alkyl group, a C6 alkoxy group, a halo (C1-6 alkyl) group, a halo (C1-6 alkoxy) group ), a hydroxy group (C 1-6 alkyl), a C 2-7 alkoxycarbonyl group (C 1-6 alkyl), a hydroxy group (C 1-6 alkoxy), an amino group (C 1-6 alkyl), an amino group (C 1-6 alkoxy), a mono- or di (C 1-6 -alkyl) amino group, a mono- or di-hydroxy (C 1-6) alkyl amino group, an alkylsulfonyl group Ci.β, a C 1-6 alkylsulfonylamino group , a C 1-6 alkylsulfonylamino group (C 1-6 alkyl), a carboxy group, a C 2-7 alkoxycarbonyl group, a sulfamoyl group and -CON (RJ) RR and R? independently represent a hydrogen atom or a C1-6 alkyl group which may have any of 1 to 3 groups selected from a hydroxy group, an amino group, a mono- or di (C1-6 alkyl) group, a C2-7 alkoxycarbonyl group and a carbamoyl group; or both of RJ and R? they are joined together with the next nitrogen atom to form an aliphatic cyclic amino group which may have any of 1 to 3 groups selected from a hydroxy group, an amino group, a mono or di (C1-6 alkyl) group, a group Cf_6 alkyl, a hydroxy group (C 1-6 alkyl), a C 2-7 alkoxycarbonyl group, a C 2-7 alkoxycarbonyl group (C 1-6 alkyl) and a carbamoyl group, or a pharmaceutically acceptable salt thereof, or a prodrug of them; [2] a heterocyclic derivative fused as described above in [1], wherein Q represents a methylene group, an ethylene group, -OCH2-, -CH2O-, -SCH2- or -CH2S-, or a pharmaceutically acceptable salt of the same, or a prodrug thereof; [3] a heterocyclic derivative fused as described above in [2], wherein Q represents an ethylene group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof; [4] a heterocyclic derivative fused as described above in [2], wherein Q represents a methylene group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof; [5] heterocyclic derivative fused as described above in any of [1] to [4], wherein the ring: A ^ A1 It represents or a pharmaceutically acceptable salt thereof, or a prodrug thereof; [6] a heterocyclic derivative fused as described above in any of [1] to [4], wherein the ring: A-A1 Xf • represents or a pharmaceutically acceptable salt thereof, or a prodrug thereof; [7] a heterocyclic derivative fused as described above in [1], wherein R5 and R6 independently represent a hydrogen atom, a hydroxy group, a halogen atom, an alkylene group C -? - 6, an alkenyl group C2-6, a C2-6 alkynyl group, a C6-6 alkoxy group, a C2-6 alkenyloxy group, a C1-6 alkylthio group, a C2-6 alkenylthio group, a halo (C1-6 alkyl) group , a halo group (C 1-6 alkoxy), a halo group (C 1-6 alkylthio), a hydroxy group (C? -6 alkyl) > a hydroxy group (C2-6 alkenyl), a hydroxy group (C6 alkoxy) or a hydroxy group (C1-6 alkylthio), or a pharmaceutically acceptable salt thereof, or a prodrug thereof; [8] a heterocyclic derivative fused as described above in any of [1], [5], [6] and [7], wherein ring A represents a benzene ring or a pyridine ring, or a pharmaceutically salt acceptable thereof, or a prodrug thereof; [9] a heterocyclic derivative fused as described above in any of [1] to [8], wherein G represents a group represented by the formula: or a pharmaceutically acceptable salt thereof, or a prodrug thereof; [10] a pharmaceutical composition comprising as an active ingredient a fused heterocyclic derivative as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof, or a prodrug thereof; [1 1] a human SGLT inhibitor comprising as an active ingredient a fused heterocyclic derivative as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof, or a prodrug thereof; [12] a human SGLT inhibitor as described above in

[11], wherein SGLT is SGLT1 and / or SGLT2; [13] an inhibitor of human SGLT as described above in [1 1], which is an agent for the inhibition of postprandial hyperglycaemia; [14] a human SGLT inhibitor as described above in [1 1], which is an agent for the prevention or treatment of a disease associated with hyperglycemia; [15] a human SGLT inhibitor as described above in

[14], wherein the disease associated with hyperglycemia is a disease selected from the group consisting of diabetes, impaired glucose tolerance, diabetic complications, obesity, hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, lipid metabolism disorder, atherosclerosis, hypertension, heart failure congestive, edema, hyperuricemia and gout; [16] an inhibitor of human SGLT as described above in [1 1], which is an agent for the inhibition of impaired glucose tolerance in progress in diabetes in a subject; [17] a pharmaceutical composition as described above in

[10], wherein the dosage form is sustained release formulation; [18] a human SGLT inhibitor as described above in [1 1], wherein the dosage form is sustained release formulation; [19] a method for the inhibition of postprandial hyperglycemia, which comprises administering an effective amount of a fused heterocyclic derivative as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof, or a prodrug thereof. same;

[20] a method for the prevention or treatment of a disease associated with hyperglycemia, comprising administering an effective amount of a fused heterocyclic derivative as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof , or a prodrug thereof; [21] a method for prevention or treatment as described above in [20], wherein the disease associated with hyperglycemia is a disease selected from the group consisting of diabetes, impaired glucose tolerance, diabetic complications, obesity, hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, dyslipidemia, atherosclerosis, hypertension, congestive heart failure, edema, hyperuricaemia and gout; [22] a method for inhibiting impaired glucose tolerance in progress in diabetes in a subject, comprising administering an effective amount of a fused heterocyclic derivative as described above in either [1] to [9], or a salt pharmaceutically acceptable thereof, or a prodrug thereof; [23] a use of a fused heterocyclic derivative as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof, or a prodrug thereof for the manufacture of a pharmaceutical composition for the inhibition of postprandial hyperglycaemia; [24] a use of a fused heterocyclic derivative as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof, or a prodrug thereof for the manufacture of a pharmaceutical composition for the prevention or treatment of a disease associated with hyperglycemia; [25] a use as described above in [24], wherein the disease associated with hyperglycemia is a disease selected from the group consisting of diabetes, impaired glucose tolerance, diabetic complications, obesity, hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, disorder of lipid metabolism, atherosclerosis, hypertension, congestive heart failure, edema, hyperuricemia and gout; [26] a use of a fused heterocyclic derivative as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof, or a prodrug thereof for the manufacture of a pharmaceutical composition for the inhibition of tolerance to impaired glucose in progress in diabetes in a subject; [27] a pharmaceutical composition as described above in [10], which comprises combination with at least one member selected from the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, a secretory enhancer, insulin, an SGLT2 inhibitor, an insulin or insulin analog, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, a dipeptidyl peptidase inhibitor IV, a phosphatase inhibitor -1 B protein tyrosine, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, an inhibitor of glycogen synthase kinase-3, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist , amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an α-aminobutyric acid receptor antagonist, a sodium channel antagonist, an NF-? B inhibitor of the transcription factor, a lipid peroxidase inhibitor, an N-acetylated linked acid dipeptidase inhibitor, an insulin-like growth factor I,. platelet-derived growth factor, an analogue of platelet-derived growth factor, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1-methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrheal, cathartic, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a β3-adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer , a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter inhibitor / bile acid, an inhibitor of cholesterol ester transfer protein, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, a receptor antagonist of endothelin, a diuretic agent, a calcium antagonist, an antihypertensive vasodilator agent, a sympathetic blocking agent, a centrally acting antihypertensive agent, an adrenoceptor agonist 2, an antiplatelet agent, a uric acid synthesis inhibitor, an uricosuric agent and a urinal alkalizer; [28] a human SGLT inhibitor as described above in

[11], which comprises combination with at least one member selected from the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an analogue of insulin or insulin, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, an inhibitor of glycogen phosphorylase, a gIucosa-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, an inhibitor of glycogen synthase kinase-3, an inhibitor of glycogen Glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an α-aminobutyric acid receptor antagonist, a sodium channel antagonist, an N F-? B inhibitor of the transcription factor, a lipid peroxidase inhibitor, an N-acetylated acid dipeptidase inhibitor, an insulin-like growth factor I, platelet-derived growth factor, a platelet-derived growth factor analog, factor of epidermal growth, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1-methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrheal, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl , a fibrate, a β 3 adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a thyroid hormone receptor agonist, an absorption inhibitor, n of cholesterol, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a palmitoyltransferase inhibitor of carnitine, an inhibitor of squalene synthase, a low density lipoprotein receptor enhancer, a derivative of nicotinic acid, a bile acid sequestrant, a sodium cotransporter inhibitor / bile acid, a cholesterol ester transfer protein inhibitor, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor , an angiotensin II receptor antagonist, an endothelin conversion enzyme inhibitor, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, a vasodilator antihypertensive agent, a sympathetic blocking agent, an antihypertensive agent acting centrally , an a2 adrenoceptor agonist, an antiplatelet agent, an inhibitor of synthesis of uric acid, an uricosuric agent and a urinary alkalizer; [29] a method for the inhibition of postprandial hyperglycemia as described above in [19], which comprises administering in combination with at least one member selected from the group consisting of an insulin sensitivity enhancer, a glucose uptake inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, a peptidase inhibitor of dipeptidyl IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor , D-chiro-initol, a glycogen synthase kinase-3 inhibitor, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analog, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an α-aminobutyric acid receptor antagonist, a sodium channel antagonist, a NF-β B inhibitor of the transcription factor, a lipid peroxidase inhibitor, an N-acetylated acid dipeptidase inhibitor, a factor I of insulin-like growth, platelet-derived growth factor, a platelet-derived growth factor analog, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1-methylhydatoin, EGB-761 , bimoclomol, sulodoxide, Y-128, an antidiarrheal, cathartic, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a beta3-adrenoceptor agonist, an acyltransferase inhibitor of acyl-coenzyme A cholesterol, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a carnitine palmitoyltransferase inhibitor , a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter / bile acid inhibitor, an inhibitor of cholesterol ester transfer protein , an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, a vasodilator antihypertensive agent, a sympathetic blocking agent, an agent centrally acting hypertension, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, an uricosuric agent and a urinary alkalinizer; [30] a method for the prevention or treatment of a disease associated with hyperglycemia as described above in [20], which comprises administering in combination with at least one member selected from the group consisting of an insulin sensitivity enhancer, an inhibitor of absorption of glucose, a biguanide, an insulin secretion enhancer, an inhibitor of SGLT2, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, a dipeptidyl peptidase inhibitor IV, a tyrosine phosphtase-1 B inhibitor of protein, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a kinase-3 inhibitor, glycogen synthase, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, a reductase inhibitor of aldose, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an α-aminobutyric acid receptor antagonist, a sodium channel antagonist, an inhibitor N F-? B of the transcription factor, a lipid peroxidase inhibitor, an N-acetylated acid dipeptidase inhibitor, an insulin-like growth factor I, a platelet-derived growth factor, a growth factor analog platelet derivative, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1-methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrheal, cathartics, a reductase inhibitor of coenzyme A of hydroxymethylglutaryl, a fibrate, a β 3 adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a palmitoyltransferase inhibitor of carnitine, a squalene synthase inhibitor, an inhibitor of low density lipoprotein receptor, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter / bile acid inhibitor, a cholesterol ester transfer protein inhibitor, an appetite suppressant, an enzyme inhibitor, conversion of angiotensin, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin conversion enzyme inhibitor, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, an antihypertensive vasodilator agent, an agent of sympathetic blockade, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, a uricosuric agent and a urinary alkalizer; [31] a method for inhibiting impaired glucose tolerance in progress in diabetes in a subject as described above in [21], which comprises administering in combination with at least one member selected from the group consisting of an insulin sensitivity enhancer , a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a peptidase inhibitor of tripeptidyl II, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a gIucosa-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, an inhibitor of pyruvate dehydrogenase, an inhibitor of hepatic gluconeogenesis, D-chiroiinsitol, a glycogen synthase kinase-3 inhibitor, a glucagon-like peptide-1, an an logo-1 peptide glucagon antagonist, a peptide-1 glucagon, amylin, an amylin analogue, an amylin agonist, an inhibitor of aldose reductase inhibitor, a formation of advanced glycation end-products, a protein kinase C inhibitor, a? -aminobutyric acid receptor antagonist, a sodium channel antagonist, an NF-? B inhibitor of transcription factor, a lipid peroxidase inhibitor, a linked acid dipeptidase inhibitor to N-acetylated, an insulin-like growth factor I, platelet-derived growth factor, an analogue of platelet-derived growth factor, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, hydroxy-1-methyhidatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrhoeal, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a β3-adrenoceptor agonist, an acyl cholesterol acyltransferase inhibitor -coenzyme A, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a micro-triglyceride transfer protein inhibitor somal, a lipoxygenase inhibitor, a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter inhibitor / bile acid, an inhibitor of cholesterol ester transfer protein, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral enptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor , an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, an antihypertensive vasodilator agent, a sympathetic blocking agent, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, an acid synthesis inhibitor uric acid, an uricosuric agent and a urinary alkalinizer; [32] a use of (A) a fused heterocycle derivative as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof, or a prodrug thereof and (B) at least one member selected from the group consisting of insulin sensitivity enhancer, a glucose uptake inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, a stimulant insulin receptor kinase, a peptide inhibitor of tripeptidyl II, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a glycogen-synthase kinase-3 inhibitor, a glucagon-like peptide-1, an an Glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of advanced glycation end-product formation, a protein kinase C inhibitor, a? -aminobutyric acid receptor antagonist, a sodium channel antagonist, an NF-? B inhibitor of the transcription factor, a lipid peroxidase inhibitor, a dipeptidase inhibitor of acid bound to N-acetylated, an insulin-like growth factor I, platelet-derived growth factor, a platelet-derived growth factor analog, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy -1-methylishidatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrheal, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, an adrenoceptor agonist 3, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor , a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium / bilious acid cotransporter inhibitor, an inhibitor of cholesterol ester transfer protein, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, a receptor antagonist, endothelin, a diuretic agent, a calcium antagonist, an antihypertensive vasodilator, an agent of sympathetic blockade, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, a uricosuric agent and a urinary alkalizer, for the manufacture of a pharmaceutical composition for the inhibition of postprandial hyperglycemia; [33] a use of (A) a heterocyclic derivative fused as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof, or a prodrug thereof and (B) at least one selected member of the group consisting of insulin sensitivity enhancer, a glucose uptake inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, a kinase stimulant of the insulin receptor, a peptide inhibitor of tripeptidyl II, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a glycogen-synthase kinase-3 inhibitor, a similar peptide-1 to glucagon, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of end-product formation of advanced glycation, a protein kinase C inhibitor, a? -aminobutyric acid receptor antagonist, a sodium channel antagonist, an NF-? B inhibitor of the transcription factor, a peroxidase lipid inhibitor, a dipeptidase inhibitor of acid bound to N-acetylated, an insulin-like growth factor I, platelet-derived growth factor, a platelet-derived growth factor analog, epidermal growth factor, or of nerve growth, a derivative of carnitine, uridine, 5-hydroxy-1-methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarreic, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a β3-adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter / bile acid inhibitor , an inhibitor of cholesterol ester transfer protein, an appetite suppressant, an angiotensin-converting enzyme inhibitor, an inhibitor or of neutral endopeptidase, an angiotensin II receptor antagonist, an endothelin conversion enzyme inhibitor, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, a vasodilator antihypertensive agent, a sympathetic blocking agent, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, a uricosuric agent and a urinary alkalizer, for the manufacture of a pharmaceutical composition for the prevention or treatment of a disease associated with hyperglycemia; [34] a use of (A) a heterocyclic derivative fused as described above in any of [1] to [9], or a pharmaceutically acceptable salt thereof, or a prodrug thereof and (B) at least one selected member of the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, a stimulant insulin receptor kinase, a peptide inhibitor of tripeptidyl II, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a glycogen synthase kinase-3 inhibitor, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of advanced glycation end-product formation, a protein kinase C inhibitor, a? -aminobutyric acid receptor antagonist, a sodium channel antagonist, a NF-? B inhibitor of the transcription factor, a lipid peroxidase inhibitor, a dipeptidase inhibitor of acid bound to N-acetylated, an insulin-like growth factor I, platelet-derived growth factor, a platelet-derived growth factor analog, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy -1-methylishidatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrhoeal, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, an adrenoceptor agonist r ß3, an acyl-coenzyme A cholesterol acyl transferase inhibitor, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, an inhibitor of lipoxygenase, a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium / bile acid cotransporter inhibitor, an inhibitor of cholesterol ester transfer protein, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, a receptor antagonist of endothelin, a diuretic agent, a calcium antagonist, a vasodilator antihypertensive agent, an sympathetic blocking agent, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, a uricosuric agent and a urinary alkalizer, for the manufacture of a pharmaceutical composition for the inhibition of tolerance to impaired glucose in progress in diabetes in a subject; and the similar. In the present invention, the term "C 1-6 alkyl group" means a branched or straight chain alkyl group having 1 to 6 carbon atoms such as a methyl group, an ethyl group, a propyl group, an isopropyl group, a group butyl, an isobutyl group, a sec-butyl group, a tert-butyl group, a pentyl group, an isopentyl group, a neopentyl group, a tert-pentyl group, a hexyl group, or the like; the term "C-6 alkylene group" or "-C1-6 alkylene-" means a branched or straight-chain alkylene group having 1 to 6 carbon atoms such as a methylene group, an ethylene group, a trimethylene group, a tetramethylene group, a propylene group, a 1, 1 -dimethylene group or similar; the term "-C1-5alkylene-" means a branched or straight-chain alkylene group having 1 to 5 carbon atoms such as a methylene group, an ethylene group, a trimethylene group, a tetramethylene group, a group of propylene, a group of 1,1-dimethylethiione or the like; and the term "-C1- - alkylene" means a branched or straight-chain alkylene group having 1 to 4 carbon atoms such as a methylene group, an ethylene group, a trimethylene group, a tetramethylene group, a propylene group, a group 1, 1-dimethyethylene or the like. The term "hydroxy group (C-6 alkyl)" means the above C-6 alkyl group substituted by a hydroxy group; the term "amino group (C 1-6 alkyl)" means the above C 1-6 alkyl group substituted by an amino group such as an aminomethyl group, a 2-aminoethyl group or the like; the term "cyano group (C 1-6 alkyl)" means the above C 1-6 alkyl group substituted by a cyano group; the term "carbamoyl group (C? -6 alkyl)" means the above C-6 alkyl group substituted by a carbamoyl group; and the term "carboxy group (C 1-6 alkyl)" means the above C 1-6 alkyl group substituted by a carboxy group. The term "C 1-6 alkoxy group" means a branched or straight-chain alkoxy group having 1 to 6 carbon atoms such as a methoxy group, an ethoxy group, a propoxy group, an isopropoxy group, a butoxy group, an isobutoxy group , a sec-butoxy group, a tert-butoxy group, a pentyloxy group, an isopentyloxy group, a neopentyloxy group, a tert-pentyloxy group, a hexyloxy group, or the like; the term "hydroxy group (C 1-6 alkoxy)" means the above alkoxy d-e group substituted by a hydroxy group; the term "carboxy group (C 1-6 alkoxy)" means the above C 1-6 alkoxy group substituted by a carboxy group; the term "amino group (C 1-6 alkoxy)" means the above alkoxy d-6 group substituted by an amino group; and the term "carbamoyl group (C 1-6 alkoxy)" means the above C 1-6 akoxy group substituted by a carbamoyl group. The term "C1-6 alkylthio group" means a branched or straight chain alkylthio group having 1 to 6 carbon atoms such as a methylthio group, an ethylthio group, a propylthio group, an isopropylthio group, a butylthio group, an isobutylthio group , a sec-butylthio group, a tert-butylthio group, a pentthylthio group, an isopentylthio group, a neopentylthio group, a tert-pentthylthio group, a hexylthio group, or the like; the term "hydroxy group (C-6 alkylthio)" means the above C-6 alkylthio group substituted by a hydroxy group; the term "carboxy group (C 1-6 alkylthio)" means the above C 1-6 alkylthio group substituted by a carboxy group; the term "amino group (C 1-6 alkylthio)" means the above C 1-6 alkylthio group substituted by an amino group. The term "C2-6 alkenyl group" means a branched or straight-chain alkenyl group having 2 to 6 carbon atoms such as a vinyl group, an allyl group, a 1 -propenyl group, an isopropenyl group, a 1 -butenyl group , a 2-butenyl group, a 2-methylallyl group or the like; the term "C2-6 alkenylene group" or "-C2-6 alkenylene-" means a straight or branched chain alkenylene group having 2 to 6 carbon atoms such as a vinylene group, a propenylene group or the like; the term "-C2-5 alkenylene-" means a branched or straight chain alkenylene group having 2 to 5 carbon atoms such as a vinylene group, a propenylene group or the like; the term "-C2-4 alkenylene-" means a branched or straight chain alkenylene group having 2 to 4 carbon atoms such as a vinylene group, a propenylene group or the like; the term "hydroxy (C2-6 alkenyl) group" means the above C2-6 alkenyl group substituted by a hydroxy group; the term "carboxy group (C 2-6 alkenyl)" means the above C 2-6 alkenyl group substituted by a carboxy group; the term "C2-6 alkenyloxy group" means a branched or straight chain alkenyloxy group having 2 to 6 carbon atoms such as a vinyloxy group, an allyloxy group, a 1-propenyloxy group, an isopropenyloxy group, a 1-butenyloxy group, a 2-butenyloxy group, a 2-methylalkyloxy group or the like; the term "C2-6 alkenylthio group" means a branched or straight-chain alkenylthio group having 2 to 6 carbon atoms such as a vinyl group, an allylthio group, a 1 -propenylthio group, a isopropenylthio group, a group 1 - butenylthio, a 2-butenylthio group, a 2-methyalkylthio group or the like; the term "C2-6 alkynyl group" means a branched or straight-chain alkynyl group having 2 to 6 carbon atoms such as an ethynyl group, a 2-propynyl group or the like; the term "-alkynylene C2-6-" means a branched or straight-chain alkylene group having 2 to 6 carbon atoms such as an ethynylene group, a propynylene group or the like; the term "-alkynylene C2-5-" means a branched or straight-chain alkynylene group having 2 to 5 carbon atoms such as an ethynylene group, a propynylene group or the like; and the term "-C2-4alkynylene-" means a branched or straight-chain alkynylene group having 2 to 4 carbon atoms such as a ethynylene group, a propynylene group or the like. The term "mono- or di (C1-6 alkyloxy) amino" means an amino group mono-substituted by the C1-6 alkyl group above or disubstituted by the same C1-6 alkyl group or different as defined above; the term "mono or di (alkyl d-6) amino (C 1-6 alkyl)" means the above C 6 -6 alkyl group substituted by the above mono- or di (C 1-6 alkyl) group; the term "mono- or di (C1-6 alkyl) amino (C1-6 alkoxy)" means the above alkoxy group "6" substituted by the above mono- or di (alkaline C-6) group; the term "mono or di [hyd roxy (alkyl d-6)] amino" means an amino group mono- substituted by the hydroxy group (C1-6 alkyl) above or di-substituted by any of the hydroxy groups (alkyl C) -6) previous; the term "mono- or di- (C 1-6 alkyl) ureido" means a monomeric group substituted by the C 1-6 alkyl group above or di-substituted by any of the above C 1-6 alkyl groups; the term "mono- or di [hyd roxy (C6-alkyl)] u" means a ureido group mono-substituted by the hydroxy group (C1-C6 alkyl) above or di-substituted by any of the hydroxy groups ( C1 -6 alkyl) above; the term "mono or di (alkyl d-6) sulfamide" means a sulfamide group mono-substituted by the group C1-6 alkyl above or di-substituted by any of the above C1-6 alkyl groups; the term "mono or di [hydroxy (C 1-6 alkyl)] sulfamide" means a sulphamide group mono-substituted by the hydroxy group (C 1-6 alkyl) above or di-substituted by any of the hydroxy groups (alkyl d). -6) previous; the term "C2-7 acyl group" means a branched or straight chain acyl group having 2 to 7 carbon atoms such as an acetyl group, a propionyl group, a butyryl group, an isobutyryl group, a valeryl group, ungroup pivaloyl, a hexanoyl group or the like; the term "g" acylamino C2-7"means an amino group substituted by the above C2-7 acyl group; and the term "amino group (C2-7 acylamino)" means the C2-7 acylamino group substituted by an amino group, such as a 2-aminoacetylamino group, or a 3-aminopropionylamino group or the like. The term "C 1-6 alkylsulfinyl group" means a branched or straight chain alkyl-sulfinyl group having 1 to 6 carbon atoms such as a methylsulfinyl group, an ethylsulfinyl group or the like; the term "C 1-6 alkylsulfonyl group" means a branched or straight-chain alkylsulfonyl group having 1 to 6 carbon atoms such as a methanesulfonyl group, an ethanesulfonyl group or the like; the term "C 1-6 alkyl sulfonylamino group" means an amino group substituted by the above C 1-6 alkylsulfonyl group; the term "carbamoyl (d6-sulfonylamino) group means the above alkylsulfonylamino group d_6 substituted by a carbamoyl group, such as a carbamoylmethanesulphonylamino group or the like, and the term" C-6 alkylsulfonylamino group (C1-6 alkyl) "means the above C-6 alkyl group substituted by the above alkylsulfonylamino d-6 group The term "halogen atom" means a fluorine atom, a chlorine atom, a bromine atom or an iodine atom, the term "halo group ( (d) "alkyl" means the above d.6 alkyl group substituted by any of 1 to 3 halogen atoms as defined above, the term "halo group (C1-6 alkoxy)" means the C6 alkoxy group above substituted by any of 1 to 3 halogen atoms as defined above, and the term "halo (alkylthio d.6) group" means the above C-6 alkylthio group substituted by any of 1 to 3 halogen atoms as defined The term "group alc "C2-7 oxycarbonyl" means a branched or straight-chain alkoxycarbonyl group having 2 to 7 carbon atoms such as a methoxycarbonyl group, an ethoxycarbonyl group, a propoxycarbonyl group, an isopropoxycarbonyl group, a butoxycarbonyl group, an isobutyloxycarbonyl group, a sec group -butoxycarbonyl, a tert-butoxycarbonyl group, a pentyloxycarbonyl group, an isopentyloxycarbonyl group, a neopentyloxycarbonyl group, a tert-pentyloxycarboyl group, a hexyloxycarbonyl group or the like; the term "C2-7 alkoxycarbonyl group (d-6 alkyl)" means the alkyl group d. 6 above replaced by the above C2-7 alkoxycarbonyl group; the term "C2-7 alkoxycarbonyl group (C6-alkoxy)" means the above C6-6 alkoxy group substituted by the above C2-7 alkoxycarbonyl group; the term "C 2-7 alkoxycarbonyl (C 1-6 alkylthio)" means the above C 1-6 alkylthio group substituted by the above C 2-7 alkoxycarbonyl group; and the term "C2-7 alkoxycarbonyl group (C2-6 alkenyl)" means the above C2-6 alkenyl group substituted by the above C2-7 alkoxycarbonyl group. The term "C3-7 cycloalkyl group" or "C3-7 cycloalkyl-" means a cyclopropyl group, a cyclobutyl group, a cyclopentyl group, a cyclohexyl group or a cycloheptyl group; the term "C3-7 cycloalkyl group (C? -6 alkyl)" means the above d.sub.3 alkyl group substituted by the above C3-7 cycloalkyl group; the term "C3-7 cycloalkyl group (C1-6 alkoxy)" means the above alkoxy d-6 group substituted by the above C3-7 cycloalkyl group; the term "C 3-7 cycloalkyl group (C 1-6 alkylthio)" means the above C 1-6 alkylthio group substituted by the above C 3-7 cycloalkyl group; and the term "C3-7 cycloalkyloxy group" means a hydroxy group substituted by the above C3-7 cycloalkyl group. The term "heterocycloalkyl group" or "heterocycloalkyl-" means an aliphatic heterocyclic group of 3 to 7 members containing any of 1 or 2 heteroatoms other than the selected bonding position of an oxygen atom, a sulfur atom and a nitrogen atom in the ring, which is derived from morpholine, thiomorpholine, tetrahydrofuran, tetrahydropyran, aziridine, azetidine, pyrrolidine, imidazoline, oxazoline, piperidine, piperazine, pyrazolidine, pyrroline, imidazoline or the like, or a 5- or 6-membered aliphatic heterocyclic group with a 6-membered ring containing any of 1 or 2 heteroatoms other than the selected binding position of an oxygen atom, a sulfur atom, and a nitrogen atom in the ring, which is derived from indoline, isoindole, tetrahydroindoline, tetrahydroisoindoline, hexahydroindoline, hexahydroisoindoline or the like. The term "heterocycloalkyl (C 1-6 alkyl)" group means the above C 1-6 alkyl group substituted by the above heterocycloalkyl group; the term "heterocycloalkyl group (d-6-alkoxy) means the above C1-C6 alkoxy group substituted by the above heterocycloalkyl group, and the term" heterocycloalkyl group (C -6 alkylthio) "means the above C1-6 alkylthio group substituted by the above heterocycloalkyl group The term "C6-10 aryl group" or "C6 aryl- or o-" means an aromatic cyclic hydrocarbon group having 6 or 10 carbon atoms such as a phenyl group, a naphthyl group or the like; "Cß-10 aryl group (C?-6 alkyl)" means the d-6 alkyl group substituted by the above C 6-10 aryl group, the term "C 6-10 aryl group (C 1-6 alkoxy)" means the alkoxy group Former C1-6 substituted by the above C6-10 aryl group, and the term "C6-aryl group or (C1-6 alkylthio)" means the above C1-6 alkylthio group substituted by the above C6-10 aryl group. term "C6-10 arylsulfonylamino group" means a sulfonylamino group having the aryl group C6-10 above, such as a benzenesulfonylamino group or the like; the term "aryl group C6.o (C2-7 alkoxycarbonyl)" means the above C2.7 alkoxycarbonyl group substituted by the aryl group C6-? or above; and the term "heteroaryl group" or "heteroaryl-" means a 5- or 6-membered aromatic heterocyclic group containing any of 1 to 4 heteroatoms other than the selected bonding position of an oxygen atom, a sulfur atom and a hydrogen atom. nitrogen in the ring, which is derived from thiazole, oxazole, isothiazole, isooxazole, pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, thiophene, imidazole, pyrazole, oxadiazole, thiodiazole, tetrazole, furazan or the like, or an aromatic heterocyclic group of 5 or 6 members fused with a 6-membered aromatic ring containing any of 1 to 4 heteroatoms other than the selected binding position of an oxygen atom, a sulfur atom and a nitrogen atom in the ring, which is derived from indole , Soindola, benzofuran, isobenzofuran, benzothiophene, benzooxazole, benzothiazole, indazole, benzoimidazole, quinoline, isoquinoline, eftalazine, quinoxaline, quinazoline, cinnoline, indolizine, na ftiridine, pteridine or similar. The term "heteroaryl group (C 1-6 alkyl)" means the group C 1-6 alkyl above substituted by the above heteroaryl group; the term "heteroaryl group (C 1-6 alkoxy)" means the above C 1-6 alkoxy group substituted by the above heteroaryl group; and the term "heteroaryl group (C 1-6 alkylthio)" means the above C 1-6 alkylthio group substituted by the above heteroaryl group. The term "aliphatic cyclic amino group" means a 5- or 6-membered aliphatic cyclic amino group which may contain a heteroatom different from the nitrogen atom at the selected binding position of an oxygen atom, a sulfur atom and a nitrogen atom in the ring, such as a morpholino group, a thiomorpholino group, a 1-aziridinyl group, a 1-azetidinyl group, a 1-pyrrolidinyl group, a piperidino group, a 1-imidazolidinyl group, a 1-piperazinyl group, a group pyrazolidinyl or the like; the term "aromatic cyclic amino group" means a 5-membered aromatic cyclic amino group which may contain 1 to 3 nitrogen atoms in the ring other than the nitrogen atom in the position of a nion, such as a 1-imidazolyl group, a 1-pyrrolyl group, a pyrazolyl group, a 1-tetrazoyl group or the like; the term "aromatic cyclic amino moiety (alkyl d-6)" means the above C1-6 alkyl group substituted by the above cyclic aromatic amino group; the term "aromatic cyclic amino group (C 1-6 alkoxy)" means the above C 1-6 alkoxy group substituted by the above cyclic aromatic amino group; and the term "aromatic cyclic amino group (alkylthio C? -6)" means the above C1-C6 alkylthio group substituted by the above cyclic aromatic amino group. The term "hydroxy protecting group" means a hydroxy protecting group used in general organic synthesis such as a methyl group, a benzyl group, a methoxymethyl group, an acetyl group, a pivaloyl group, a benzoyl group, a tert-butyldimethylsilyl group, a tert-butyldiphenylsilyl group, an allyl group or similar; the term "amino protecting group" means an amino protecting group used in general organic synthesis such as a benzyloxycarbonyl group, a tert-butoxycarbonyl group, a benzyl group, an acetyl group, a trifluoroacetyl group or the like; the term "carboxy protective group" means a carboxy protecting group used in general organic synthesis such as a methyl group, an ethyl group, a benzyl group, a tert-butyldimethylsilyl group, an allyl group or the like. In addition, in the substituent Q, the left-hand bond means a bond attached to a fused ring containing nitrogen and the right-hand bond means a bond attached to a ring A. The compounds represented by the above general formula (I) of the present invention can be prepared according to the following analogous methods or procedures thereof, or other methods described in the literatures or analogous processes thereof or the like.

In the formula, E 1 a represents a hydrogen atom, a fluorine atom or a benzyloxy group; E2a represents a hydrogen atom, a fluorine atom, a methyl group or a benzyloxymethyl group; L1 represents a chlorine atom, a bromine atom or an iodine atom; L2 represents a lithium atom, MgCl, MgBr or Mgl; M represents a benzyl group; G1 represents a group represented by a formula: or a formula: wherein M, E1 a and E2a have the same meanings as defined above; G2 represents the previous G with a hydroxy group protected by a benzyl group; R1 to R6, G, Q, ring A and a ring: J have the same meanings above, and with the proviso that in the case that there is a hydroxy group, an amino group and / or a carboxy group in each compound, a compound having a protecting group can be used suitably. Process 1 A compound represented by the general formula (III) above can be prepared by subjecting a compound represented by the general formula (II) above 1) to lithiation using a lithiation reagent such as n-butyllithium, sec-butyllithium, tert-butyllithium. or the like in an inert solvent, or 2) to the preparation of a Grignard reagent in the presence of an additive such as iodine, 1,2-dibromoethane or the like using magnesium in an inert solvent. As the solvent is used in the lithiation reaction, for example, tetrahydrofuran, diethyl ether, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually -100 ° C to 0 ° C, and the reaction time is usually from 1 minute to 3 hours, varying based on a starting material used, solvent and reaction temperature. As the solvent is used in the preparation of the Grignard reagent, for example, tetrahydrofuran, diethyl ether, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually from 30 minutes to 5 hours, varying based on a used starting material, solvent and reaction temperature. Process 2 A compound represented by the above general formula (IV) can be prepared by subjecting a compound represented by the general formula (III) above to condensation with a sugar lactone represented by the general formula (Ga) or (Gb) above in a inert solvent. As the solvent is used, for example, tetrahydrofuran, diethyl ether, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually -100 ° C at room temperature, and the reaction time is usually from 5 minutes to 5 hours, varying based on a used starting material, solvent and reaction temperature. Process 3 A compound represented by the general formula (V) above can be prepared by subjecting a compound represented by the general formula (IV) above to reduction to remove a hydroxy group at the anomeric position in the presence of boron trifluoride ether complex diethyl using a reagent such as triethylne, triisopropylne or the like as an inert solvent. As the solvent is used, for example, acetonitrile, dichloromethane, 1,2-dichloroethane, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually -20 ° C at room temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a starting material used, solvent and reaction temperature. Process 4 A compound represented by the above general formula (I) of the present invention can be prepared by subjecting a compound represented by the general formula (V) above 1) to catalytic hydrogenation using a palladium catalyst such as palladium-carbon powder or the like in an inert solvent or 2) to treatment using a reagent such as ethanethiol in the presence of an acid such as boron trifluoride-diethyl ether complex to remove the benzyl group in an inert solvent. As the solvent is used in catalytic hydrogenation, for example, methanol, ethanol, ethyl acetate, tetrahydrofuran, acetic acid, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually from 0 ° C to reflux temperature, and the reaction time is usually from 1 hour to 2 days, varying based on a used starting material, solvent and reaction temperature. As the solvent is used in the acid treatment, for example, dichloromethane, 1,2-dichloroethane, acetonitrile, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a used starting material, solvent and reaction temperature. Of the compounds represented by the general formula (I) above of the present invention, a benzofuran compound wherein Q represents -C6 -alkylene-, -C2-6alkenylene-, -C2-6alkynylene-, -C1- alkylene- 6-O-,-C1-6-S-alkylene, -C1-6-O-C1-6 alkylene- or C1-6-S-C1-6 alkylene- alkylene can also be prepared according to the following 5 to 10 processes using the following compound (Vi l) which can be prepared from the following compound (VI): according to the previous procedures.

Process 7 '"^ COOR10 (XI) In the formula, R represents a methyl group or an ethyl group; G3 represents G above with a hydroxy group protected by an acyl group such as an acetyl group, a pivaloyl group, a benzoyl group; L3 represents a chlorine atom or a bromine atom; Q1 represents -C1-6alkylene-, -alkylene C2-6-, -C2-6alkynylene-, -C1-6alkylene- O-, -C1-6alkylene- S-, -6-O- alkylene. C1-6alkylene- or C1-6alkylene-S-alkylene C1-6alkyl-; R1 to R3, R5, R6, G and ring A have the same meanings as defined above, and with the proviso that in the case that there is a hydroxy group, an amino group and / or a carboxy group in each compound, a compound having a proteg group can be used appropriately. Process 5 A compound represented by the general formula (VII) above can be prepared by subjeg a compound represented by the above general formula (VI I) to O-acylation in the presence of a base such as pyridine, triethylamine, N, N- diisopropylethylamine or the like in the presence or absence of an additive such as 4-dimethylaminopyridine or the like using an acylating agent such as acetyl chloride, pivaloyl chloride, benzoyl chloride, or the like in an inert solvent. As the solvent is used in the rean, for example, pyridine, triethylamine, N, N-diisopropylethylamine, dichloromethane, 1,2-dichloroethane, tetrahydrofuran, acetonitrile, ethyl acetate, a mixed solvent thereof and the like can illustrate The rean temperature is usually 0 ° C at reflux temperature, and the rean time is usually from 1 hour to 5 days, varying based on a starting material used, solvent and rean temperature.

Process 6 A compound represented by the general formula (X) above can be prepared by subjeg a compound represented by the general formula (VI II) above to Friedel-Crafts rean to acylate and demethylate in the presence of a Lewis acid such as aluminum chloride or the like using a compound represented by the general formula (IX) above in an inert solvent. As the solvent is used, for example, dichloromethane, 1,2-dichloroethane, carbon disulfide, chlorobenzene, a mixed solvent thereof and the like can be illustrated. The rean temperature is usually 0 ° C at reflux temperature, and the rean time is usually from 1 hour to 5 days, varying based on a starting material used, solvent and rean temperature. Process 7 A compound represented by the general formula (Xl l) above can be prepared by subjeg a compound represented by the general formula (X) above to O-alkylation in the presence of a base such as potassium carbonate, calcium carbonate or the like. similar using a haloacetic acid ester represented by the general formula (XI) above in an inert solvent. As the solvent is used, for example, N, N-dimethylformamide, acetone, a mixed solvent thereof and the like can be illustrated. The rean temperature is usually from room temperature to reflux temperature, and the rean time is usually from 1 hour to 5 days, varying based on a used starting material, solvent and rean temperature. Process 8 A phenoxyacetic acid derivative represented by the above general formula (XII) can be prepared by subjeg a compound represented by the general formula (Xl 1) above to hydrolysis in the presence of a basic substance such as sodium hydroxide, potassium hydroxide or the similar. As the solvent is used, for example, methanol, ethanol, 2-propanol, tetrahydrofuran, water, a mixed solvent thereof and the like can be illustrated. The rean temperature is usually from room temperature to reflux temperature, and the rean time is usually from 1 hour to 1 day, varying based on a starting material used, solvent and rean temperature. Process 9 A benzofluor derivative represented by the general formula (Va) above can be prepared by subjecting a compound represented by the general formula (Xl l l) above to cyclization in the presence of sodium acetate and acetic anhydride in an inert solvent. As the solvent is used, for example, acetic acid and the like can be illustrated. The reaction temperature is usually 50 ° C at reflux temperature, and the reaction time is usually from 1 hour to 3 days, varying based on a starting material used, solvent and reaction temperature. Process 1 0 A compound represented by the above general formula (Ia) of the present invention can be prepared by subjecting a compound represented by the general formula (Va) above to hydrolysis in the presence of a basic substance such as sodium hydroxide, methoxide of sodium, sodium ethoxide or similar. As the solvent is used, for example, methanol, ethanol, tetrahydrofuran, water, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a used starting material, solvent and reaction temperature. The initial materials used in the above manufacturing methods can be prepared according to the procedures described in the literature or analogous processes thereof or the like. In addition, of the compounds represented by the general formula (I I) above, a compound represented by the following general formula (lia), (llb) or (llc) can also be prepared according to the following processes 1 to 17.

Process 16 In the formula, A3 represents an oxygen atom, a n sulfur atom or a nitrogen atom attached to R9; L4 represents a lithium atom, MgCl, MgBr or Mg l; L5 represents -P (= O) (OR1 1) 2 or -P + (PPh3) 3X ", R1 represents a g alkyl group d-6, Ph represents a phenyl group, X represents a chlorine atom, a bromine atom or an iodine atom, Q2 represents a single bond, -C5 alkylene-, -C2-5alkenylene-, -C2-5alkynylene-, -C1-5alkylene- O-, -alkylene d- 5-S-, -C 1 -5-O-C 1-6 -alkylene- or-C-5-S-C-6-alkylene-C-6-alkylene represents a single bond, -Cal-Cal-alkylene, -C 2-4 -alkenylene-, - C 2-4 alkynylene, C 4 -4 O-, C 4 -4 S-, C 1-4 alkylene-O-alkylene d-6- or C 1-4 alkylene-C alkylene ? -6-; R1 to R6, R9, L1 and ring A have the same meanings as defined above Process 1 1 A compound represented by the above general formula (XVI) can be prepared by subjecting a compound represented by the general formula ( XIV) prior to Friedel-Crafts reaction to acylate in the presence of a Lewis acid such as aluminum chloride or the like using a compound represented by r the general formula (XV) above in an inert solvent. As the solvent is used, for example, dichloromethane, 1,2-dichloroethane, carbon disulfide, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a used starting material, solvent and reaction temperature. Process 12 A compound represented by the general formula (Ha) above can be prepared by subjecting a compound represented by the above general formula (XVI) to reduction in the presence of an acid such as trifluoroacetic acid or the like using a reagent such as triethylsilan or the similar in an inert solvent. As the solvent is used, for example, trifluoroacetic acid, dichloromethane, 1,2-dicyoroethane, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually 30 minutes to 3 days, varying based on a starting material used, solvent and reaction temperature. Process 13 A compound represented by the general formula (XVII) above can be prepared by subjecting a compound represented by the general formula (XIV) above to Vilsmeier reaction using phosphorus oxychloride and N, N-dimethylformamide in an inert solvent.

As the solvent is used in the reaction, for example, N, N-dimethylformamide, acetonitrile, dichloromethane, 1,2-dichloroethane, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a used starting material, solvent and reaction temperature. Process 14 A compound represented by the above general formula (XIX) can be prepared by subjecting a compound represented by the general formula (XVII) above to condensation using a lithium organ reagent or a Grignard reagent represented by the general formula (XVIII) above. As the solvent is used, for example, tetrahydrofuran, diethyl ether and what is simulated can be illustrated. The reaction temperature is usually -78 ° C at room temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a used starting material, solvent and reaction temperature. Process 1 A compound represented by the general formula (Na) above can be prepared by subjecting a compound represented by the general formula (XIX) above 1) to reduction in the presence of N, N-dimethylaminopyridine using a boran reagent such as complex of boran-tetrahydrofuran, boran-dimethylsulfide complex or the like in an inert solvent or 2) to reduction in the presence of an acid such as trifluoroacetic acid, boron trifluoride-diethyl ether complex or the like using a reagent such as triethylsilan in an inert solvent. As the solvent is used in reduction 1), for example, tetrahydrofuran, diethyl ether, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually 30 minutes to 5 days, varying based on a starting material used, solvent and reaction temperature. As the solvent is used in reduction 2), for example, triflu roacetic acid, dichloromethane, 1,2-dichloroethane, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually from 30 minutes to 5 days, varying based on a used starting material, solvent and reaction temperature. Process 1 6 A compound represented in general formula (I lb) above can be prepared by subjecting a compound represented by general formula (XVII) above to Wittig reaction or Horner-Emmons reaction in the presence of a base such as sodium hydride , sodium hydroxide, potassium tert-butoxide, n-butyllithium, tert-butyllithium or the like using a compound represented by the general formula (XX) above in an inert solvent. As the solvent is used in the reaction, for example, tetrahydrofuran, N, N-dimethylformamide, dimethyl sulfoxide, methanol, ethanol, acetonitrile, water, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a used starting material, solvent and reaction temperature. Process 17 A compound represented by the general formula (Ie) above can be prepared by subjecting a compound represented by the general formula (Ib) above 1) to catalytic hydrogenation using a palladium catalyst such as palladium-carbon powder or the like in an inert solvent, or 2) a reduction of diimide in the presence or absence of a base such as triethylamine, N, N-diisopropyl-ethylamine or the like using a reagent such as 2,4,6-triisopropyl-benzenesulfonyl hydrazide or similar in an inert solvent. As the solvent is used in catalytic hydrogenation, for example, methanol, ethanol, ethyl acetate, tetrahydrofuran, acetic acid, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually from 1 hour to 2 days, varying based on a starting material used, solvent and reaction temperature. As the solvent is used in the reduction of diimide, for example, tetrahydrofuran, diethyl ether, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually from room temperature to reflux temperature, and the reaction time is usually from 1 hour to 3 days, varying based on a used starting material, solvent and reaction temperature. Of the compounds represented by the general formula (XIV) above, a compound wherein A3 represents a sulfur atom can also be prepared according to the following Processes 18 and 19.

(XXII) In the formula, L6 represents a chlorine atom, a bromine atom or an iodine atom; R12 represents a methyl group or an ethyl group, or both R12 join to form an ethylene group or a trimethylene group; R1 to R4 and L1 have the same meanings as defined above.

Process 1 8 A compound represented by the general formula (XXI II) above can be prepared by subjecting a compound represented by the general formula (XXI) above to S-alkylation in the presence of a base such as potassium carbonate, cesium carbonate, triethylamine, N, N-diisopropylethylamine or the like using a compound represented by the general formula (XXI I) above in an inert solvent. As the solvent is used, for example, N, N-dimethylformamide, acetone, dichloromethane, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a used starting material, solvent and reaction temperature. Process 1 9 A benzothiophene derivative represented by the general formula (XlVa) above can be prepared by subjecting a compound represented by the general formula (XXI I I) above to cyclization in the presence of polyphosphoric acid in an inert solvent. As the solvent is used, for example, benzene, chlorobenzene, toluene and the like can be illustrated. The reaction temperature is usually from room temperature to reflux temperature, and the reaction time is usually from 1 hour to 1 day, varying based on a used starting material, solvent and reaction temperature. Of the compounds represented by the general formula (XIV) above, a compound wherein A3 represents a sulfur atom; and R4 represents a hydrogen atom can also be prepared according to the following Processes 20 to 23.

(XlVb) (XXVIII) In the formula, R 13 represents a methyl group or an ethyl group; R1 to R3 and L1 have the same meanings as defined above. Process 20 A compound represented by the general formula (XXV) above can be prepared by subjecting a compound represented by the general formula (XXIV) above 1) to lithiation in the presence or absence of an additive such as N, N, N \ N ' -tetramethylenediamine, hexamethylphosphoramide or the like using a base such as n-butyllithium, sec-butyllithium, tert-butyllithium, lithium diisopropylamide or the like in an inert solvent, and then 2) to formylation using N, N-dimethylformamide. As the solvent is used, for example, tetrahydrofuran, diethyl ether, a mixed solvent thereof and the like can be illustrated. The reaction temperatures are usually from -100 ° C to 0 ° C in reaction 1) and usually from -100 ° C to room temperature in reaction 2), and the reaction times are usually from 5 minutes to 5 hours in the reaction. reaction 1) and usually from 5 minutes to 1 day in reaction 2), varying based on a starting material used, solvent and reaction temperature. Process 21 A benzothiopene derivative represented by the general formula (XXVII) above can be prepared by subjecting a compound represented by the above general formula (XXV) to cyclization in the presence of a base such as triethylamine, N, N-diisopropyethylamine, carbonate potassium, cesium carbonate, potassium tert-butoxide, sodium hydride or the like using a mercaptoacetic acid ester represented by the general formula (XXVI) above in an inert solvent. As the solvent is used, for example, N, N-dimethylformamide, dimethyl sulfoxide, tetrahydrofuran, methanol, ethanol, n-butanol and the like can be illustrated. The reaction temperature is usually from room temperature to reflux temperature, and the reaction time is usually from 5 minutes to 1 day, varying based on a starting material used, solvent and reaction temperature. Process 22 A carboxylic acid derivative represented by the general formula (XXVI I I) can be prepared by subjecting a compound represented by the general formula (XXVII) above to hydrolysis in the presence of a basic substance such as sodium hydroxide, potassium hydroxide or similar. As the solvent is used, for example, methanol, ethanol, 2-propanol, tetrahydrofuran, water, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually from room temperature to reflux temperature, and the reaction time is usually from 1 hour to 1 day, varying based on a used starting material, solvent and reaction temperature. Process 23 A compound represented by the general formula (XlVb) above can be prepared by subjecting a compound represented by the above general formula (XXVIII) to decarboxylation using a catalyst such as copper powder or the like in an inert solvent. As the solvent is used, for example, quinoline and the like can be illustrated. The reaction temperature is usually 100 ° C at reflux temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a starting material used, solvent and reaction temperature. Of the compounds represented by the general formula (I) above of the present invention, a compound represented by the general formula (Ib) above can also be prepared according to the following Processes 24 to 30.

In the formula, P represents a protective group such as a tosyl group, a benzenesulfonyl group or the like; L7 represents a chlorine atom, a bromine atom, an iodine atom, a mesyloxy group or a tosyloxy group; Q3 represents -C6 -6- alkylene, -C2-6alkenylene-, -C2-6alkynylene-, -C1-6alkylene-O-, -alkylene d. 6-S-, -alkylene d-6-O-alkylene C? -6- or -alkylene C? _6-S-alkylene C? -6-; -CO N (R8) -, -alkylene C? -6-CON (R8) - or -CON (R8) -alkylene C? -6-; R1 to R6, L1, L2, G, G1, G2 and ring A have the same meanings as defined above. Process 24 A compound represented by the above general formula (XXX) can be prepared by protecting a nitrogen atom of a compound represented by the above general formula (XXIX) in the presence of a base such as hydride, sodium, potassium hydroxide or the like using a protective reagent such as toluenesulfonyl chloride, benzenesulfonyl chloride or the like in an inert solvent. As the solvent is used in the reaction, for example, N. N-dimethylformamide, dimethylsulfoxide, tetrahydrofuran, toluene, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually from 0 ° C to reflux temperature, and the reaction time is usually from 1 hour to 1 day, varying based on a used starting material, solvent and reaction temperature. Process 25 A compound represented by the above general formula (XXXI) can be prepared by subjecting a compound represented by the general formula (XXX) above 1) to lithiation using a lithiation reagent such as n-butyllithium, sec-butyllithium, tert-butyllithium. or the like in an inert solvent, or 2) to the preparation of a Grignard reagent in the presence of an additive such as iodine, 1,2-dibromoethane or the like using magnesium in an inert solvent. As the solvent is used in the lithiation reaction, for example, tetrahydrofuran, diethyl ether, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually from -100 ° C to 0 ° C, and the reaction time is usually from 1 minute to 3 hours, varying based on a used starting material, solvent and reaction temperature. As the solvent is used in the reaction of the Grignard reagent, for example, tetrahydrofuran, diethyl ether, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually from 30 minutes to 5 hours, varying based on a used starting material, solvent and reaction temperature. Process 26 A compound represented by the general formula (XXXI I) can be prepared by subjecting a compound represented by the general formula (XXXI) above to condensation with a sugar lactone represented by the general formula (Ga) or (Gb) above in a inert solvent. As the solvent is used, for example, tetrahydrofuran, diethyl ether, or a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually -100 ° C at room temperature, and the reaction time is usually from 5 minutes to 5 hours, varying based on a starting material used, solvent and reaction temperature. Process 27 A compound represented by the above general formula (XXXI II) can be prepared by subjecting a compound represented by the general formula (XXXI I) above to reduction to remove a hydroxy group at the anomeric position in the presence of boron trifluoride complex Diethyl ether using a reagent such as triethylsilane, triisopropylsilane or the like in an inert solvent. As the solvent is used, for example, acetonitrile, dichloromethane, 1,2-dichloroethane, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually -20 ° C at room temperature, and the reaction time is usually 30 minutes to 1 day, varying based on an initial material used, solvent and reaction temperature. Process 28 A deprotected compound represented by the above general formula (XXXIV) can be prepared by subjecting a compound represented by the general formula (XXXI II) above to hydrolysis using a base such as potassium hydroxide, sodium hydroxide or the like in an inert solvent. As the solvent is used, for example, ethanol, methanol, water, tetrahydrofuran, N, N-dimethylformamide, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually from 1 hour to 2 days, varying based on a used starting material, solvent and reaction temperature. Process 29 A compound represented by the general formula (Vb) above can be prepared by subjecting a compound represented by the above general formula (XXXIV) to N-alkylation or N-acylation in the presence of a base such as sodium hydride, hydride of potassium, potassium hydroxide, n-butyllithium, potassium tert-butoxide or the like using a compound represented by the general formula (XXXV) above in an inert solvent. As the solvent is used, for example, N, N-dimethylformamide, tetrahydrofuran, dimethyl sulfoxide, toluene, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually from 0 ° C to reflux temperature, and the reaction time is usually from 1 hour to 1 day, varying based on a used starting material, solvent and reaction temperature. Process 30 A compound represented by the above general formula (Ib) of the present invention can be prepared by subjecting a compound represented by the general formula (Vb) above 1) to catalytic hydrogenation using a palladium catalyst such as palladium-carbon or the like in an inert solvent, or 2) to treatment to remove the benzyl group using a reagent such as ethanethiol or the like in the presence of an acid such as boron trifluoro-diethyl ether complex or the like in an inert solvent. As the solvent is used in the hydrogenation, for example, methanol, ethanol, ethyl acetate, tetrahydrofuran, acetic acid, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually from 0 ° C to reflux temperature, and the reaction time is usually from 1 hour to 2 days, varying based on a used starting material, solvent and reaction temperature. As the solvent is used in the acid treatment, for example, dichloromethane, 1,2-dichloroethane, acetonitrile, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually 0 ° C at reflux temperature, and the reaction time is usually 30 minutes to 1 day, varying based on a used starting material, solvent and reaction temperature. Of the compounds represented by the general formula (ll) above, a compound represented by the above general formula (lid) can also be prepared according to the following Process 31.

In the formula, Q4 represents an oxygen atom or a sulfur atom; Q5 represents -alkylene C? _6-; A3 represents an oxygen atom, a sulfur atom or NR9; L8 represents a chlorine atom, a bromine atom, an iodine atom, a mesyloxy group or a tosyloxy group, R1 to R6, R9, L1 and ring A have the same meanings as defined above. Process 31 A compound represented by the general formula (I id) above can be prepared by subjecting a compound represented by the general formula (XXXVI) above to condensation with a compound represented by the above general formula (XXXVII) in the presence of such a base such as sodium hydride, potassium hydroxide, potassium tert-butoxide, cesium carbonate or the like in an inert solvent. As the solvent is used in the condensation reaction, for example, tetrahydrofuran, N, N-dimethylformamide, dimethyl sulfoxide, acetone, methanol, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually from 0 ° C to reflux temperature, and the reaction time is usually from 1 hour to 1 day, varying based on a used starting material, solvent and reaction temperature. Of the compounds represented by the general formula (I I) above, a compound represented by the general formula (Ie) above can also be prepared according to the following Process 32.

(XXXVIII) (XXXIX) In the formula, Q6 represents an oxygen atom or a sulfur atom; Q7 represents a single bond or -C1-6alkylene-; L9 represents a chlorine atom, a bromine atom, an iodine atom, a mesyloxy group or a tosyloxy group; R1 to R6, L1, A3 and ring A have the same meanings as defined above. Process 32 A compound represented by the general formula (Me) above can be prepared by subjecting a compound represented by the general formula (XXXIX) above to condensation with a compound represented by the general formula (XXXVIII) above in the presence of such a base such as sodium hydride, potassium hydroxide, potassium tert-butoxide, cesium carbonate or the like in an inert solvent. As the solvent is used in the condensation reaction, for example, tetrahydrofuran, N, N-dimethylformamide, dimethyl sulfoxide, acetone, methanol, a mixed solvent thereof and the like can be illustrated. The reaction temperature is usually from 0 ° C to reflux temperature, and the reaction time is usually from 1 hour to 1 day, varying based on a used starting material, solvent and reaction temperature. In case of compounds having a hydroxy group, an amino group and / or a carboxy group in the above processes, they can also be used in each reaction after introducing any protecting group in the usual manner as the occasion demands. The protecting group can optionally be removed in any subsequent reaction in the usual manner. The compounds represented by the above general formula (I) of the present invention obtained by the above production processes can also be isolated and purified by conventional separation means such as fractional recrystallization, purification using chromatography, solvent extraction and solid phase extraction.

The fused heterocyclic derivatives represented by the general formula (I) above of the present invention can be converted to its pharmaceutically acceptable salts in the usual manner. Examples of such salts include acid addition salts with mineral acids such as hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, nitric acid, phosphoric acid, and the like, acid addition salts with organic acids such as formic acid, acid acetic, methanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, propionic acid, citric acid, succinic acid, tartaric acid, fumaric acid, butyric acid, oxalic acidmalonic acid, maleic acid, lactic acid, malic acid, carbonic acid, guthamic acid, aspartic acid and the like, salts with inorganic bases such as a sodium salt, a potassium salt and the like, and salts with organic bases such as N-methyl-D-glucamine, N, N'-dibenzylethylenediamine, 2-aminoethanol, tris (hydroxymethyl) aminomethane, arginine, lysine and the like. The compounds represented by the general formula (I) above of the present invention include their solvates with pharmaceutically acceptable solvents such as ethanol and water. Of the fused heterocyclic derivatives represented by the general formula (I) above of the present invention and the prodrugs thereof, there are two geometric isomers, cis (Z) -isomer and trans (E) -isomer, in each compound having one bond unsaturated In the present invention, any of the isomers can be employed.

Of the fused heterocyclic derivatives represented by the general formula (I) above of the present invention and the prodrugs thereof, there are two optical isomers, R isomer and S isomer, in each compound having an asymmetric carbon atom excluding the sugar portion . In the present invention, any of the optical isomers may also be employed, and a mixture of both optical isomers may also be employed. A prodrug of a compound represented by the above general formula (I) of the present invention can be prepared by introducing an appropriate group to form a prodrug in any one or more groups selected from a hydroxy group, an amino group and a cyclic amino group such as a pyrazole ring, a piperazine ring or the like of the compound represented by the general formula (I) above using a corresponding reagent to produce a prodrug such as a halide compound or the like in the usual manner, and then upon isolating adequately and purify in the usual way as the occasion demands. As a group forming a prodrug used in a hydroxy group or an amino group, for example, a C2-7 acyl group, a C1-6 alkoxy group (C2-7 acyl), a C2-7 alkoxycarbonyl group (C2-7 acyl), a C2-7 alkoxycarbonyl group, a C6- [alpha] aryl group (C2-7 alkoxycarbonyl), a C6 alkoxy group (C2 alkoxycarbonyl -7) or similar can be illustrated.

As a group forming a prodrug used in a cyclic amino group, for example, a C2-7 acyl group, a C1-6 alkoxy group (C2.7 acyl), a C2-7 alkoxycarbonyl group (C2-7 acyl), a C2-7 alkoxycarbonyl group, a C6-? aryl group or (C2-7 alkoxycarbonyl), a C6-6 alkoxy group (C2-7 alkoxycarbonyl), a C2-7 acyloxymethyl group, a 1 - (C2-7 acyloxy) ethyl group, a (C2 alkoxycarbonyl group. 7) - Oxymethyl, a group 1 - [(C 2-7 alkoxy) oxy] ethyl, a group (C 3-7 cycloalkyl) oxycarbonyloxymethyl, a group 1 - [(C 3-7 cycloalkyl) oxycarbonyloxy] ethyl or the like Shine The term "C1-6 alkoxy group (C2-7 acyl)" means the above C2-7 acyl group substituted by the above C6-6 alkoxy group; the term "C2-7 alkoxycarbonyl group (C2- acyl)" means the above C2-7 acyl group substituted by the C2-7 alkoxycarbonyl group; the term "C 1-6 alkoxy group (C 2-7 alkoxycarbonyl)" means the above C 2-7 alkoxycarbonyl group substituted by the above C 1-6 alkoxy group. The term "(C2-7 acyloxy) methyl group" means an O-hydroxymethyl group substituted by the above C2-7 acyl group; the term "group 1 - (C2-7 acyloxy) ethyl" means a 1-hydroxyethyl group O-substituted by the above C2-7 acyl group; the term "(C2-7 alkoxycarbonyl) oxymethyl group" means an O-substituted hydroxymethyl group by the above C2-7 alkoxycarbonyl group; the term "group 1 - [(C2-7 alkoxy) oxy] ethyl" means a 1-hydroxyethyl group O-substituted by the C2-7 alkoxycarbonyl group; the term "(C3-7 cycloalkyl) oxycarbonyl group" means a cyclic alkoxycarbonyl group having the above C3-7 cycloalkyl group; the term "(C3-7 cycloalkyl) oxycarbonyl-oxymethyl group" means a hydroxymethyl group O-substituted by the group (C3-7 cycloalkyl) oxycarbonyl above; and the term "group 1 - [(C3-7 cycloalkyl) oxycarbonyloxy] ethyl" means a 1-hydroxyethyl group O-substituted by the above group (C3-7 cycloalkyl) oxycarbonyl. In addition, as a group forming a prodrug, a glucopyranosyl group or a galactopyranosyl group can be illustrated. For example, these groups are preferably introduced into the hydroxy group in the 4 or 6 position of the glucopyranosyloxy group or the galactopyranosyloxy group, and are more preferably introduced into the hydroxy group in the 4 or 6 position of the glucopyranosyloxy group. The fused heterocyclic derivatives represented by the general formula (I) above of the present invention, for example, showed potent inhibitory activity in human SGLT1 or SGLT2 in a confirmatory test of human SGLT1 or SGLT2 inhibitory activity as described below. Thus, a fused heterocyclic derivative represented by the above general formula (I) of the present invention can exert an excellent inhibitory activity of SGLT1 in the small intestine or an excellent inhibitory activity of SGLT2 in the kidney, and significantly inhibits the increase in glucose level in the blood or significantly decreases the level of glucose in the blood. Therefore, a fused heterocyclic derivative represented by the above general formula (I) of the present invention, a pharmaceutically acceptable salt thereof and a prodrug thereof are extremely useful as an agent for the inhibition of postprandial hyperglycemia, the inhibition of advancing in diabetes in a subject with impaired glucose tolerance and the prevention or treatment of a disease associated with hyperglycemia such as diabetes, impaired glucose tolerance (IGT), diabetic complications (eg, retinopathy, neuropathy, nephropathy, ulcer, macroangiopathy), obesity, hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, lipid metabolism disorder, atherosclerosis, hypertension, congestive heart failure, edema, hyperuricemia, gout or the like, which is related to SGLT1 activity in the small intestine and SGLT2 activity in the kidney . In addition, the compounds of the present invention can be used suitably in combination with at least one member selected from the following drugs. Examples of drugs that can be used in combination with the compounds of the present invention include an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin analogue or insulin, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, an inhibitor of glycogen phosphorylase, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a glycogen-synthase kinase-3 inhibitor, a peptide -1 similar to glucagon, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an agonist amylin, an inhibitor of aldose reductase, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an α-aminobutyric acid receptor antagonist, a sodium channel antagonist, an inhibitor NF-? B of the transcription factor, a lipid peroxidase inhibitor, an N-acetylated acid dipeptidase inhibitor, an insulin-like growth factor I, a platelet-derived growth factor (PDGF), a factor analogue of platelet-derived growth (PDGF) (eg, PDGF-AA, PDGF-BB, PDGF-AB), epidermal growth factor (EGF), nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1 -methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrhoeal, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a β3-adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor , probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a palmitoyltransferase inhibitor of carnitine, an inhibitor of squalene synthase , a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter / bile acid inhibitor, an inhibitor of cholesterol ester transfer protein, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, a vasodilator antihypertensive agent, a sympathetic blocking agent, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, an uricosuric agent and a urinary alkalinizer. In case of uses of the compound of the present invention in combination with one or more prior drugs, the present invention includes either simultaneous administration dosage forms as a single preparation or separate preparations in the same or different administration route mode, and administration at different dosage intervals as separate preparations in the same or different administration route mode. A pharmaceutical combination comprising the compound of the present invention and the above drug (s) includes both dosage forms as a single preparation and separate preparations for combination as mentioned above. The compounds of the present invention can obtain more advantageous effects than additive effects in the prevention or treatment of the above diseases when they are suitably used in combination with one or more prior drugs. Also, the administration dose can be decreased compared to administration of either the drug alone, or adverse effects of co-administered drugs can be avoided or declined. Concrete compounds such as drugs used for combination and preferable diseases to be treated are exemplified as follows. However, the present invention is not limited thereto, and the particular compounds include their free compounds, and their pharmaceutically acceptable salts. As insulin sensitivity enhancers, receptor agonists? peroxisome proliferator-activated such as troglitazone, pioglitazone hydrochloride, rosiglitazone maleate, sodium darglitazone, GI-262570, isaglitazone, LG-100641, NC-2100, T-174, DRF-2189, CLX-0921, CS-01 1, GW-1929, ciglitazone, sodium englitazone and NI P-221, peroxisome proliferator-activated receptor agonists such as GW-9578 and BM-170744, a /? Receptor agonists. peroxisome proliferator-activated such as GW-409544, KRP-297, N-622, CLX-0940, LR-90, SB-219994, DRF-4158 and DRF-MDX8, retinoid X receptor agonists such as ALRT-268 , AGN-4204, MX-6054, AGN-194204, LG-100754 and bexarotene, and other insulin sensitivity enhancers such as reglixan, ONO-5816, MBX-102, CRE-1625, FK-614, CLX-0901, CRE-1633, NN-2344, BM-13125, BM-501050, HQL-975, CLX-0900, MBX-668, MBX-675, S-15261, GW-544, AZ-242, LY-510929, AR- H049020 and GW-501516 are illustrated. Insulin sensitivity enhancers are preferably used for diabetes, impaired glucose tolerance, diabetic complications, obesity, hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, lipid metabolism disorder or atherosclerosis, and more preferably for diabetes, impaired glucose tolerance or hyperinsulinemia due to the improvement of the disturbance of insulin signal transduction in peripheral tissues and increase of glucose uptake in the blood tissues, leading to a decrease in the level of glucose in the blood. As inhibitors of glucose uptake, for example, α-glucosidase inhibitors such as acarbose, voglibose, miglitol, CKD-71 1, emiglitate, MDL-25, 637, camiglibose and MDL-73, 945, amylase inhibitors a as AZM-127, inhibitors of SGLT1 described in pamphlets of International Publications Nos. WO02 / 098893, WO2004 / 014932 and the like are illustrated. The glucose absorption inhibitors are preferably used for diabetes, impaired glucose tolerance, diabetic complications, obesity or hyperinsulinemia, and more preferably for impaired glucose tolerance due to inhibition of the gastrointestinal enzymatic digestion of carbohydrates contained in foods, and inhibition or delay of the absorption of glucose in the body. As biguanides, phenformin, buformin hydrochloride, metformin hydrochloride or the like are illustrated. Biguanides are preferably used for diabetes, impaired glucose tolerance, diabetic complications or hyperinsulinemia, and more preferably for diabetes, impaired glucose tolerance or hyperinsulinemia due to decreased blood glucose level by inhibitory effects on hepatic gluconeogenesis, accelerating the effects on Anaerobic glycolysis in tissues or improving the effects of insulin resistance in peripheral tissues. As insulin secretion enhancers, tolbutamide, chlorpropamide, tolazamide, acetohexamide, glycopyramide, glyburide (glibenclamide), gliclazide, 1-butyl-3-methanylyl-urea, carbutamide, glibornuride, glipizide, gliquidone, glisoxapide, glibutiazole, glibuzole, glihexamide, Sodium glimidine, glipinamide, fenbutamide, tolciclamide, glimepiride, nateglinide, calcium hydrate of mitiglinide, repaglinide or the like are illustrated. In addition, insulin secretion enhancers include glucokinase activators such as RO-28-1675. Insulin secretion enhancers are preferably used for diabetes, impaired glucose tolerance or diabetic complications, and more preferably for diabetes or impaired glucose tolerance due to decreased blood glucose level by acting on pancreatic β cells and increasing secretion of insulin. As inhibitors SGLT2, T-1095 and compounds described in Japanese Patent Publication Nos. HeM O-237089 and 2001-288178, and International Publications Nos. WO01 / 16147, WO01 / 271 28, WO01 / 68660, WO01 / 74834, WO01 / 74853, WO02 / 28872, WO02 / 36602, WO02 / 44192, WO02 / 53573, WO03 / 000712, WO03 / 020737 and the like are illustrated. The SGLT2 inhibitors are preferably used for diabetes, impaired glucose tolerance, diabetic complications, obesity or hyperinsulinemia, and more preferably for diabetes, impaired glucose tolerance, obesity or hyperinsulinemia due to the decrease in the level of glucose in the blood by inhibiting the glucose reabsorption in the proximal tubule of the kidney. As insulin or insulin analogues, human insulin, insulin derived from animal, insulin analogs derived from animal or human or the like are illustrated. These preparations are preferably used for diabetes, impaired glucose tolerance or diabetic complications, and more preferably for diabetes or impaired glucose tolerance. As antagonists of the glucagon receptor, BAY-27-9955, NNC-92-1687 or similar are illustrated; as stimulants of insulin receptor kinase, TER-1741 1, L-783281, KRK-613 or the like are illustrated; as inhibitors of tripeptidyl peptidase I I, UCL-1397 or the like are illustrated; as inhibitors of dipeptidyl peptidase IV, NVP-DPP728A, TSL-225, P-32/98 or the like are illustrated; as inhibitors of protein tyrosine phosphatase 1 B, PTP-1 12, OC-86839, PNU-177496 or the like are illustrated; as inhibitors of glycogen phosphorylase, NN-4201, CP-368296 or the like are illustrated; as fructose-biphosphatase inhibitors, R-132917 or the like are illustrated; as inhibitors of pyruvate dehydrogenase, AZD-7545 or the like are illustrated; as inhibitors of hepatic gluconeogenesis, FR-225659 or similar are illustrated; as analogs of glucagon-like peptide-1, exendin-4, CJC-1 131 or the like are illustrated; as agonists of glucagon-like peptide-1; AZ -134, LY-315902 or similar are illustrated; and as amylin, amylin analogs or amylin agonists, pramlintide acetate or the like are illustrated. These drugs, glucose-6-phosphatase inhibitors, D-chiro-initol, inhibitors of glycogen-synthase kinase-3 and glucagon-like peptide-1 are preferably used for diabetes, impaired glucose tolerance, diabetic complications or hyperinsulinemia, and more preferably for diabetes or impaired glucose tolerance. As inhibitors of aldose reductase, ascorbyl gamolenate, tolrestate, epalrestate, DNA-138, BAL-ARI8, ZD-5522, DNA-31 1, GP-1447, IDD-598, fidarestate, sorbinil, ponalrestate, risarestate, zenarestate, minalrestate, metosorbonil, AL-1567, imitostat, M-16209, TAT, AD-5467, zopolrestate, AS-3201, NZ-314, SG-210, JTT-81 1, Lindolrestate or the like are illustrated. Aldose reductase inhibitors are preferably used for diabetic complications due to the inhibition of aldose reductase and reduction of excessive intracellular accumulation of sorbitol in accelerated polyol trajectory that are in hyperglycemic condition continues in the tissues in diabetic complications. As inhibitors of the formation of advanced glycation end products, pyridoxamine, OPB-9195, ALT-946, ALT-71 1, pimagedine hydrochloride or the like are illustrated. Inhibitors of the formation of advanced glycation end products are preferably used for diabetic complications due to the inhibition of formation of advanced glycation end products that are accelerated in continuous hyperglycemic condition in diabetes and decline in cell damage. As inhibitors of protein kinase C, LY-333531, midostaurin or the like are illustrated. Protein kinase C inhibitors are preferably used for diabetic complications due to the inhibition of protein kinase C activity that is accelerated in hyperglycemic condition continues in diabetes. Antagonist of the α-aminobutyric acid receptor, topiramate or the like are illustrated; as antagonists of the sodium channel, mexiletin hydrochloride, oxcarbazepine or the like are illustrated; as NF-? B inhibitors of the transcription factor, dexlipotam or the like are illustrated; as inhibitors of peroxidase lipid, mesylate of tirilizad or the like are illustrated; as inhibitors of N-acetylated acid dipeptidase bound, GPI-5693 or the like are illustrated; and as derivatives of carnitine, carnitine, levacecarnine hydrochloride, levocarnitine chloride, levocarnitine, ST-261 or the like are illustrated. These drugs, insulin-like growth factor I, platelet-derived growth factor, analogues of platelet-derived growth factor, epidermal growth factor, nerve growth factor, uridine, 5-hydroxy-1-methylhydatoin, EGB-761 , bimoclomol, sulodoxide and Y-128 are preferably used for diabetic complications. As antidiarrheal or cathartic, polycarbophilic calcium, albumin tannate, bismuth subnitrate or similar are illustrated. These drugs are preferably used for diarrhea, constipation or the like accompanying diabetes or similar. As inhibitors of coenzyme A reductase of hydroxymethylglutaryl, sodium cerivastatin, pravastatin sodium, lovastatin, simvastatin, fluvastatin sodium, calcium hydrate of atorvastatin, SC-45355, SQ-33600, CP-83101, BB-476, L- 669262, S-2468, DMP-565, U-20685, BAY-x-2678, BAY-10-2987, calcium pitavastatin, calcium rosuvastatin, colestolone, dalvastatin, acitemate, mevastatin, crilvastatin, BMS-180431, BMY- 21950, glenvastatin, carvastatin, BMY-22089, bervastatin or the like are illustrated. Coenzyme A reductase inhibitors of hydroxymethylglutaryl are preferably used for hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, lipid metabolism disorder or atherosclerosis, and more preferably for hyperlipidemia, hypercholesterolemia or atherosclerosis due to the decrease in blood cholesterol level by inhibiting reductase of Coenzyme A hydroxymethylglutaryl. As fibrates, bezafibrate, beclobrate, binifibrate, ciprofibrate, clinofibrate, clofibrate, aluminum clofibrate, clofibric acid, etofibrate, fenofibrate, gemfibrozil, nicofibrate, pirifibrate, ronifibrate, simfibrate, theofibrate, AHL-157 or the like are illustrated. Fibers are preferably used for hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, lipid metabolism disorder or atherosclerosis, and more preferably for hyperlipidemia, hypertriglyceridemia or atherosclerosis due to the activation of hepatic lipoprotein lipase and increased oxidation of the fatty acid, leading to decrease in the triglyceride level in the blood. As β3-adrenoceptor agonists, BRL-28410, SR-5861 1 A, ICI-198157, ZD-2079, BMS-194449, BRL-37344, CP-331679, CP-1 14271, L-750355, BMS-187413, SR -59062A, BMS-210285, LY-377604, SWR-0342SA, AZ-40140, SB-226552, D-71 14, BRL-35135, FR-149175, BRL-26830A, CL-316243, AJ-9677, GW- 427353, N-5984, GW-2696, YM 178 or the like are illustrated. Β3-adrenoceptor agonists are preferably used for obesity, hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia or lipid metabolism disorder, and more preferably for obesity or hyperinsulinemia due to the stimulation of the adrenoceptor β3 in adipose tissue and increased oxidation of fatty acid, leading to to induction of energy expenditure. As acyl-coenzyme A cholesterol acyltransferase inhibitors, NTE-122, MCC-147, PD-132301 -2, DUP-129, U-73482, U-76807, RP-70676, P-06139, CP-1 13818 , RP-73163, FR-129169, FY-038, EAB-309, KY-455, LS-31 15, FR-145237, T-2591, J-104127, R-755, FCE-28654, YIC-C8- 434, avasimiba, CI-976, RP-64477, F-1394, eldacimiba, CS-505, CL-283546, YM-17E, lecimibide, 447C88, Y -750, E-5324, KW-3033, HL-004, eflucimiba or similar are illustrated. Acyl-Coenzyme A cholesterol acyltransferase inhibitors are preferably used for hyperlipidemia, hypercholesterolemia, hypertriglyceridemia or lipid metabolism disorder, and more preferably for hyperlipidemia or hypercholesterolemia due to a decrease in the level of cholesterol in the blood by inhibiting acyltransferase of acyl cholesterol. Coenzyme A. As agonists of the thyroid hormone receptor, sodium liothyronine, sodium levothyroxine, KB-261 1 or the like are illustrated; as inhibitors of cholesterol absorption, ezetimibe, SCH-48461 or the like are illustrated; as inhibitors of lipase, orlistat, ATL-962, AZM-131, RED-103004 or the like are illustrated; as carnitine palmitoyltransferase inhibitors, etomoxir or the like are illustrated; as inhibitors of squalene synthase, SDZ-268-198, BMS-188494, A-87049, RPR-101821, ZD-9720, RPR-107393, ER-27856, TAK-475 or the like are illustrated; as nicotinic acid derivatives, nicotinic acid, nicotinamide, nicomol, niceritrol, acipimox, nicorandil or the like are illustrated; as bile acid sequestrants, cholestyramine, cholestylan, colesevelam hydrochloride, GT-102-279 or the like are illustrated; as sodium cotransporter / bile acid inhibitors, 264W94, S-8921, SD-5613 or the like are illustrated; and as inhibitors of cholesterol ester transfer protein, PNU-107368E, SC-795, JTT-705, CP-529414 or the like are illustrated. These drugs, probcol, inhibitors of microsomal triglyceride transfer protein, lipoxygenase inhibitors and low density lipoprotein receptor enhancers are preferably used for hyperlipidemia, hypercholesterolemia, hypertriglyceridemia or lipid metabolism disorder. As appetite suppressants, monoamine retake inhibitors, serotonin reuptake inhibitors, serotonin release stimulants, serotonin agonists (especially 5HT2C agonists), noradrenaline reuptake inhibitors, noradrenaline release stimulants, a1-adrenoceptor agonists, agonists of β2-adrenoceptor, dopamine agonists, cannabinoid receptor agonists, α-aminobutyric acid receptor antagonists, histamine H3 antagonists, L-histidine, leptin, leptin analogues, leptin receptor agonists, melanocortin receptor agonists ( especially, MC3-R agonists, MC4-R agonists), a-melanocyte-stimulating hormone, amphetamine and cocaine-regulated transcription, mahogany protein, entero-statin agonists, calcitonin, calcitonin gene-related peptide, cholecystokinin agonists (especially agonists CCK-A), corticotropin releasing hormone, hormone analogs released corticotrophin, corticotrophin releasing hormone agonists, urocortin, somatostatin, somatostatin analogues, somatostatin receptor agonists, pituitary adenylate cyclase activation peptide, brain derived neurotrophic factor, ciliary neurotropic factor, thyrotropin releasing hormone , neurotensin, sauvagine, neuropeptide Y antagonists, opioid peptide antagonists, galanin antagonists, hormone antagonists concentrating melanin, agouti-related protein inhibitors and orexin receptor antagonists are illustrated. Specifically, as inhibitors of monoamine resumes, mazindol or the like are illustrated; as inhibitors of serotonin reuptake, dexfenfluramine hydrochloride, fenfluramine, sibutramine hydrochloride, fluvoxamine maleate, sertraline hydrochloride or the like are illustrated; as serotonin agonists, inotriptan, (-f -) - nofenfluramine or the like are illustrated; as norepinephrine retake inhibitors, bupropion, GW-320659 or the like are illustrated; as stimulants of release of noradrenaline, rolipram, YM-992 or the like are illustrated, as agonists of β2-adrenoceptor, amphetamine, dextroamphetamine, phentermine, benzfetamine, methamphetamine, phendimetrazine, fenmetrazine, diethylpropion, phenylpropanolamine, clobenzorex or the like are illustrated; as dopamine agonists, ER-230, doprexin, bromocriptine mesylate or the like are illustrated; as cannabinoid receptor antagonists, rimonobant or the like are illustrated; as α-aminobutyric acid receptor antagonists, topiramate or the like are illustrated; as histamine H3 antagonists, GT-2394 or the like are illustrated; such as leptin, leptin analogs or leptin receptor agonists, LY-355101 or similar are illustrated; as cholecystokinin agonists (especially CCK-A agonists), SR-146131, SSR-125180, BP-3,200, A-71623, FPL-15849, GI-248573M, GW-7178, GI-181771, GW-7854, A- 71378 or similar are illustrated; and as neuropeptide Y antagonists, SR-120819-A, PD-160170, NGD-95-1, BIBP-3226, 1229-U-91, CGP-71683, BIBO-3304, CP-671906-01, J-1 15814 or similar are illustrated. As appetite suppressants are preferably used for diabetes, impaired glucose tolerance, diabetic complications, obesity, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, lipid metabolism disorder, atherosclerosis, hypertension, congestive heart failure, edema, hyperuricemia or gout, and more preferably for obesity due to the stimulation or inhibition of the activities of intracerebral monoamines or bioactive peptides in central appetite regulating system and suppression of appetite, leading to the reduction of energy intake. As inhibitors of angiotensin converting enzyme, captopril, enalaprimaleate, alacepril, delapril hydrochloride, ramipril, lisinopril, imidapril hydrochloride, benazepril hydrochloride, ceronapril monohydrate, cilazapril, sodium fosinopril, perindopril erbumin, calcium moveltipril, hydrochloride of quinapril, spirapril hydrochloride, temocapril hydrochloride, trandolapril, calcium zofenopril, moexipril hydrochloride, rentiapril or the like are illustrated. As angiotensin-converting enzyme inhibitors, they are preferably used for diabetic complications or hypertension. As inhibitors of neutral endopeptidase, omapatrilat, MDL-100240, fasidotril, sampatrilat, GW-66051 1 X, mixanpril, SA-7060, E-4030, SLV-306, ecadotril or the like are illustrated. Neutral endopeptidase inhibitors are preferably used for diabetic complications or hypertension.

As angiotensin II receptor antagonists, cilexetil candesartan, cilexetil candesartan / hydroclortiazide, potassium losartan, eprosartan mesylate, valsartan, telmisartan, irbesartan, EXP-3174, L-158809, EXP-3312, olmesartan, tasosartan, KT-3- 671, GA-01 13, RU-64276, E D-90423, BR-9701 or the like are illustrated. Angiotensin receptor antagonists I I are preferably used for diabetic complications or hypertension. As inhibitors of endothelin conversion enzyme, CGS-31447, CGS-35066, SM-19712 or the like are illustrated; as antagonists of the endothelin receptor, L-749805, TBC-3214, BMS-182874, BQ-610, TA-0201, SB-215355, PD-180988, sodium sitaxsentan, BMS-193884, darusentan, TBC-371 1, bosentan, sodium tezosentan, J-104132, YM-598, S-0139, SB-234551, RPR-1 18031 A, ATZ-1993, RO-61 -1790, ABT-546, enlasetan, BMS-207940 or similar they are illustrated. These drugs are preferably used for diabetic complications or hypertension, and more preferably for hypertension. As diuretic agents, chlorthalidone, metolazone, cyclopentiazide, trichlorometiazide, hydrochlorothiazide, hydroflumethiazide, benzylhydrochlorothiazide, penflutizide, methiclothiazide, indapamide, tripamide, mefruside, azosemide, ethacrynic acid, toresamide, piretanide, furosemide, bumetanide, methicrane, potassium canrenoate, spironolactone, triamterene , aminophylline, cyclintanin hydrochloride, LLU-a, PNU-80873A, isosorbide, D-mannitol, D-sorbitol, fructose, glycerin, acetazolamide, methazolamide, FR-179544, OPC-31260, lixivaptan, conivaptan hydrochloride or the like illustrate As diuretic drugs are used preferably for diabetic complications, hypertension, congestive heart failure or edema, and more preferably for hypertension, congestive heart failure or edema due to the reduction of blood pressure or improvement of edema by increasing urinary excretion. As calcium antagonists, aranidipine, efonidipine hydrochloride, nicardipine hydrochloride, barnidipine hydrochloride, benidipine hydrochloride, manidipine hydrochloride, cilnidipine, nisoldipine, nitrendipine, nifedipine, nilvadipine, felodipine, amlodipine besilate, pranidipine, lercanidipine hydrochloride, isradipine , eldipidine, azelnidipine, lacidipine, vatanidipine hydrochloride, lemildipine, diltiazem hydrochloride, clentiazem maleate, verapamil hydrochloride, S-verapamil, fasudil hydrochloride, bepridil hydrochloride, gallopamil hydrochloride or the like are illustrated; as vasodilating antihypertensive agents, indapamide, todralazine hydrochloride, hiralazine hydrochloride, cadralazine, budralazine or the like are illustrated; as sympathetic blocking agents, amosulalol hydrochloride, terazosin hydrochloride, bunazosin hydrochloride, prazosin hydrochloride, doxazosin mesylate, propranolol hydrochloride, atenolol, metoprolol tartrate, carvedilol, nipradilol, celiprolol hydrochloride, nebivolol, betaxolol hydrochloride, pindolol , tertatolol hydrochloride, bevantolol hydrochloride, timolol maleate, carteolol hydrochloride, bisoprolol hemifumarate, bopindolol malonate, nipradilol, penbutolol sulfate, acebutolol hydrochloride, tilisolol hydrochloride, nadolol, urapidil, indoramine or the like are illustrated; as centrally acting antihypertensive agents, resperpina or the like are illustrated; and as agonists of cc2 adrenoceptor, clonidine hydrochloride, methyldopa, CHF-1035, guanabenz acetate, guanfacine hydrochloride, mexonidine, lofexidine, talipexole hydrochloride or the like are illustrated. These drugs are preferably used for hypertension. As antiplatelet agents, ticlopidine hydrochloride, dipyridamole, cilostazol, ethyl icosapentate, sarpogrelate hydrochloride, dilazep dihydrochloride, trapidil, beraprost sodium, aspirin or the like are illustrated. Antiplatelet agents are preferably used for atherosclerosis or congestive heart failure. As inhibitors of uric acid synthesis, allopurinol, oxipurinol or the like are illustrated; as uricosuric agents, benzbromarone, probenecid or the like are illustrated; and as urinary alkalizers, sodium hydrogen carbonate, potassium citrate, sodium citrate or the like are illustrated. These drugs are preferably used for hyperuricemia or gout. In cases of uses in combination with a compound of the present invention, for example, in use for diabetes, the combination with at least one member of the group consisting of an insulin sensitivity enhancer, a glucose uptake inhibitor, a biguanide , an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, a dipeptidyl peptidase inhibitor IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiroesitol, a glycogen synthase kinase-3 inhibitor, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a peptide-1 agonist similar to glucagon, amylin, an amylin analogue, an amylin agonist and appetite suppressant is preferable; the combination with at least one member of the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, an antagonist of the glucagon receptor, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, an inhibitor of dipeptidyl IV peptidase, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, an inhibitor of glucose-6-phosphatase, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a glycogen-synthase kinase-3 inhibitor, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analog and an amylin agonist is more preferable; and the combination with at least one member of the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin analog or insulin is more preferable . Similarly in the use for diabetic complications, the combination with at least one member of the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, a dipeptidyl peptidase inhibitor IV, a protein tyrosine phosphatase-1 B inhibitor , a glycogen phosphorylase inhibitor, a gIucosa-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, an inhibitor of glycogen, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analog, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an α-aminobutyric acid receptor antagonist, a sodium channel antagonist, an NF-? B inhibitor of transcription factor, an inhibitor of peroxidase lipid, an inhibitor of dipeptidase of acid bound to N-acetylated, an insulin-like growth factor I, platelet-derived growth factor, an analogue of platelet-derived growth factor, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1 - methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, a receptor antagonist of endothelin and a diuretic agent is preferable; and the combination with at least one member of the group consisting of an aldose reductase inhibitor, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor and an angiotensin receptor antagonist I I is more preferable. In addition, in the use for obesity, the combination with at least one member of the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an analogue of insulin or insulin, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a glycogen-synthase kinase-3 inhibitor, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an β3-adrenoceptor agonist, and an appetite suppressant is preferable; and the combination with at least one member of the group consisting of a glucose absorption inhibitor, an SGLT2 inhibitor, a β3-adrenoceptor agonist and an appetite suppressant is more preferable. When the pharmaceutical compositions of the present invention are employed in the practical treatment, various dosage forms are used depending on their uses. As examples of the dosage forms, powders, granules, fine granules, echo syrups, tablets, capsules, injections, solutions, ointments, suppositories, cataplasms and the like are illustrated, which are administered orally or parenterally. The pharmaceutical compositions of the present invention also include sustained release formulation including gastrointestinal mucoadhesive formulation (eg, international publications Nos. WO99 / 10010, WO99 / 26606, and Japanese Patent Publication No. 2001 -2567). These pharmaceutical compositions can be prepared by mixing with or by diluting and dissolving with an appropriate pharmaceutical additive such as excipients, disintegrants, binders, lubricants, diluents, regulators, isotonicities, antiseptics, wetting agents, emulsifiers, dispersing agents, stabilizing agents, dissolving aids. and the like, and formulate the mixture according to conventional methods. In case of the uses of the compound of the present invention in combination with another drug (s), they can be prepared by formulating each active ingredient together or individually in a similar manner as defined above. When the pharmaceutical compositions of the present invention are used in the practical treatment, the dosage of a compound represented by the above general formula (I), a pharmaceutically acceptable salt thereof or a prodrug thereof as the active ingredient is decided in a manner appropriate depending on the age, sex, body weight and degree of symptoms and treatment of each patient, which is approximately within the range of 0.1 to 1,000 mg per day per adult human in the case of oral administration and approximately within the range from 0.01 to 300 mg per day per adult human in the case of parenteral administration, and the daily dose can be divided into one to several doses per day and administered in an adequate manner. Also, in the case of the uses of the compound of the present invention in combination with another drug (s), the dosage of the compound of the present invention can be decreased, depending on the dosage of the drug (s). . EXAMPLES The present invention is further illustrated in more detail by way of the following Examples and Test Examples. Nevertheless, the present invention is not limited thereto. Example 1 Process 1 1 - (5-Bromobenzofbltiophen-3-M) -2-phenyletanone To a solution of 5-bromobenzothiophene (1 g) and phenylacetyl chloride (1.1 g) in dichloromethane (50 mL) is added aluminum chloride (1.9 g) at 0 ° C and the mixture is stirred at the same temperature for 2 hours. The reaction mixture is poured into an aqueous solution of cold hydrochloric acid (2 mol / L) and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate, and the solvent is removed under reduced pressure. The residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 8/1). After the solvent is removed, the residual solid is rinsed with hexane to give the title compound (1.1 g). 1 HN MR (CDCl 3) d ppm: 4.28 (2H, s), 7.20-7.40 (5H, m), 7.52 (1 H, dd, J = 1 .9, 8.7Hz), 7.69 (1 H, d, J = 8.7Hz), 8.37 (1H, s), 8.98 (1H, d, J = 1 .9Hz) Process 2 5-Bromo-3- (2-phenylethyl) benzorb1tiophene To a mixture of 1 - (5 -bromobenzo [b] thiophen-3-yl) -2-phenylethanone (1.1 g) and triethylsilane (1.5 g) add trifluoroacetic acid (10 mL) at room temperature, and the mixture is stirred at room temperature for 2 hours . The reaction mixture is poured into an aqueous solution of cold saturated potassium carbonate, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate, and the solvent is removed under reduced pressure. The residue is purified by column chromatography on silica gel (eluent: n-hexane) to give the title compound (0.94 g). 1 H-NMR (CDCl 3) d ppm: 3.00-3.15 (4H, m), 7.07 (1 H, s), 7.15-7.35 (5H, m), 7.44 (1 H, dd, J = 2.1, 8.5Hz) , 7.71 (1 H, d, J = 8.5 Hz), 7.86 (1 H, d, J = 2.1 Hz) Process 3 2.3.4.6-Tetra-Q-benzyl-1 - [3- (2-phenylethyl) benzo [bltiofen-5-α-D-qlucopyranose To a solution of 5-bromo-3- (2-phenylethyl) benzo [b] -thiophene (0.94 g) in tetrahydrofuran (25 mL) is added n-butyllithium (2.44) mol / L in n-hexane solution, 1.24 mL) at -78 ° C under an argon atmosphere, and the mixture is stirred at the same temperature for 5 minutes. To the reaction mixture is added a solution of 2,3,4,6-tetra-O-benzyl-D-glucono-1,5-Iactone (0.80 g) in tetrahydrofuran (4 mL), and the mixture is heated to 0 ° C and shake for 30 minutes. The reaction mixture is poured into saturated aqueous ammonium chloride solution, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate and the solvent is removed under reduced pressure. The residue is purified by column chromatography on silica gel (euent: n-hexane / ethyl acetate = 4/1 - 3/1) to give the title compound (1.1 g).

Process 4 5- (2,3,4,6-Tetra-O-benzyl-β-D-glucopyranosyl-3- (2-phenylethylbenzofbltiofen) To a solution of 2,3,4,6-tetra-O-benzyl-1 - [3- (2-phenylethyl) benzo [b] thiophen-5-yl] -D-glucose (1.1 g) and triethylsilane (0.34 g) in acetonitrile (15 mL) is added diethyl ether-boron trifluoride complex (0.23 g) ) under cooling with ice, and the reaction mixture is warmed to room temperature and stirred overnight.An aqueous solution of saturated potassium carbonate is added to the reaction mixture, and the mixture is stirred for 30 minutes. Pour into water, and the mixture is extracted with diethyl ether.The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate, and the solvent is removed under reduced pressure.

The residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 6/1). The solid obtained is rinsed with hexane and dried under reduced pressure to give the title compound (0.5 g). 1 H-NMR (CDCl 3) d ppm: 3.00-3.15 (4H, m), 3.50-3.60 (1 H, m), 3.60-3.70 (1 H, m), 3.72 (1 H, d, J = 10Hz) , 3.75-3.90 (4H, m), 4.35-4.45 (2H, m), 4.55-4.60 (1 H, m), 4. 60-4.70 (2H, m), 4.85-5.00 (3H, m), 6.75-6.85 (2H, m), 7.00-7.40 (24H, m), 7.48 (1H, dd, J = 1.5, 8.4Hz), 7.78 (1H, d, J = 1.5Hz), 7.86 (1 H, d, J = 8.4Hz). Process 5 1 - [3- (2-Phenyletipbenzo [bltiophen-5-yl] -1-deoxy-β-D-glucopyranose To a mixture of 5- (2,3,4,6-tetra-O-benzyl) -β-D-gIucopyranosyl) -3- (2-phenylethyl) benzo [b] thiophene (0.1 g) and ethanethiol (0.16 g) in dichloromethane (6 mL) is added diethyl ether-boron trifluoride complex (0.28 g) at room temperature, and the mixture is stirred at room temperature for 3 hours.An aqueous solution of saturated potassium carbonate is added to the reaction mixture, and the mixture is extracted with ethyl acetate.The organic layer is rinsed with brine and dry over anhydrous magnesium sulfate, and the solvent is removed under reduced pressure.The residue is purified by column chromatography on silica gel (eluent: dichloromethane / methanol = 10 / 1-5 / 1) to give the title compound ( 0.034 g) .1H-NMR (CD3OD) d ppm: 3.00-3.10 (2H, m), 3.10-3.20 (2H, m), 3.40-3.60 (4H, m), 3.74 (1H, dd, J = 5.3, 11.8Hz), 3.91 (1H, dd, J = 1.7, 11.8Hz), 4.29 (1H, d, J = 9.2Hz), 7.10-7.30 (6H, m), 7.40-7.50 (1H, m) , 7.80-7.90 (2H, m) Example 2 Process 1 1- (2,4-Dimethoxyphenyl) -2,3,4,6-tetra-O-benzyl D-glucopyranose To a solution of 2,4-bromobenzene ( 1.6 g) in tetrahydrofuran (40 mL) n-butyllithium (2.44 mol / L solution of n-hexane, 3.1 mL) is added at -78 ° C under an argon atmosphere, and the mixture is stirred at the same temperature for 5 minutes. To the reaction mixture is added a solution of 2,3,4,6-tetra-O-benzyl-D-glucono-1,5-lactone (2.0 g) in tetrahydrofuran (6 mL), and the reaction mixture heat to 0 ° C and stir for 1 hour. The reaction mixture is poured into an aqueous solution of saturated ammonium chloride, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate, and the solvent is removed under reduced pressure. The residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 4/1 - 3/1 - 2/1 - 1/1) to give the title compound (1.7 g). ). Process 2 1-Deoxy-2,3,4,6-tetra-O-benzyl-1- (2,4-dimethoxy-phenyl) -β-D-glucopyranose To a solution of 1- (2,4-dimethoxyphenyl) ) -2,3,4,6-tetra-O-benzyl-D-glucopyranose (1.7 g) and triethylsilane (0.59 g) in acetonitrile (20 mL) is added diethyl ether-boron trifluoride complex (0.40 g) ) under cooling with ice, and the mixture is warmed to room temperature and stirred overnight. An aqueous solution of saturated potassium carbonate is added to the reaction mixture, and the mixture is stirred for 30 minutes. The mixture is poured into water, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate, and the solvent is removed under reduced pressure. The residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 6/1 to give the title compound (1.1 g). 1 H-NMR (CDCl 3) d ppm: 3.55-3.62 ( 1 HOUR, m), 3.62-3.71 (1 H, m), 3.71 -3.90 (4H, m), 3.75 (3H, s), 3.82 (3H, s), 3.95 (1H, d, J = 10.7Hz), 4.43 (1H, d, J = 10.4Hz), 4.53 (1H, d, J = 12.1Hz), 4.60-4.80 (3H, m), 4.85-4.92 (2H, m), 4.95 (1H, d, J = 11.0 Hz), 6.46 (1H, d, J = 2.6Hz), 6.53 (1H, dd, 2.6, 8.5Hz), 6.90-6.95 (1H, m), 7.10-7.40 (20H, m) Process 3 1-Deoxy- 1- (2,4-d¡methoxyphenol) -β-D-glucopyranose To a solution of 1-deoxy-2,3,4,6-tetra-O-benzyl-1- (2,4- dimethoxyphenyl) -β-D-glucopyranose (1.1 g) in methanol (10 mL) and tetrahydrofuran (5 mL) is added 10% palladium-carbon powder (0.50 g), and the mixture is stirred at room temperature for 5 hours under an atmosphere of nitrogen. The insoluble material is removed by filtration, and the solvent of the filtrate is removed under reduced pressure to give the title compound (0.47 g). 1H-NMR (CD3OD) d ppm: 3.30-3.42 (2H, m), 3.44-3.50 (1H, m), 3.50-3.60 (1H, m), 3.65 (1H, dd, J = 5.6, 11.9Hz), 3.78 (3H, s), 3.80 (3H, s), 3.84 (1H, dd, J = 2.0, 11.9Hz), 4.60 (1H, d, J = 9.7Hz), 6.50-6.55 (2H, m), 7.25 -7.35 (1H, m) Process 4 1-Deoxy-2.3.4.6-tetra-O-pivaloyl-1- (2,4-dimethoxyphenyl-β-D-glucopyranose To a solution of 1-deoxy-1- (2,4- dimethoxyphenyl) -β-D-glucopyranose (0.47 g) in pyridine (10 mL) is added pivaloyl chloride (1.1 g) at room temperature, and the mixture is stirred at room temperature overnight.The reaction mixture is poured into The organic layer is rinsed with water, 1 mol / L aqueous hydrochloric acid solution, water and brine and dried over anhydrous magnesium sulfate.The solvent is removed under reduced pressure, and the mixture is extracted with diethyl ether. The residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 3/1 -1 / 1) The compound obtained (0.51 g) is dissolved in pyridine (6 mL), Pivaloyl chloride (0.23 g) and 4- (N, N-dimethylamino) pyridine (0.079 g) are added to the solution, and then the mixture is stirred at 50 ° C overnight. Pivaloyl chloride (0.12 mL) is added to the reaction mixture, and the mixture is stirred at 80 ° C overnight. The reaction mixture is poured into water, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water, 1 mol / L aqueous hydrochloric acid solution, water and brine and dried over anhydrous magnesium sulfate, and the solvent is removed under reduced pressure. The residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 4/1 -2/1) to give the title compound (0.58 g). 1 HN MR (CDCl 3) d ppm: 0.86 (9H, s), 1.12 (9H, s), 1.16 (9H, s), 1.22 (9H, s), 3.77 (3H, s), 3.78 (3H, s) , 3.80-3.90 (1 H, m), 4.09 (1 H, dd, J = 4.2, 12.4Hz), 4.19 (1 H, dd, J = 1 .9, 12.4Hz), 4.85-5.00 (1 H, m), 5.25-5.50 (3H, m), 6.37 (1 H, d, J = 2.6Hz), 6.47 (1 H, dd, J = 2.6y8.5Hz), 7.10-7.30 (1 H, m) Process 5 2-Phenyl-2'-hydroxy-4'-methoxy-5 '- (2,3,4,6-tetra-O-pivaloyl-β-Dg luco pyra nos i I) Propiophenone To a solution of 1 -deoxi-2,3,4,6-tetra-O-pivaloyl-1 - (2,4-dimethoxyphenyl) -β-D-gIucopyranose (0.58 g) in diethyl ether (9 mL) is added aluminum chloride (1 .5 g) under cooling with a cloud, and the mixture is stirred for 5 minutes. To the mixture is added 3-phenylpropionyl chloride (0.46 g) at room temperature, and the mixture is stirred for 4 days after the mixture is warmed to room temperature. The reaction mixture is poured into 2 mol / L cold aqueous hydrochloric acid solution, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate, and the solvent is removed under eluted pressure. The residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 6/1 -3/1) to give the title compound (0.35 g). 1H-N MR (CDCl 3) d ppm: 0.87 (9H, s), 1.12 (9H, s), 1.14 (9H, s), 1.16 (9H, s), 3.00-3.10 (2H, m), 3.15-3.40 (2H, m), 3.8-3.9 (4H, m), 4.05 (1H, dd, J = 4.4, 12.4Hz), 4.18 (1H, dd, J = 1 .9, 12.4 Hz), 4.80-5.00 (1 H, m), 5.20-5.50 (3H, m), 6.37 (1 H, s), 7.20-7.35 (5H, m), 7.73 (1 H, s), 12.82 (1 H, s) Process 6 2-Phenyl-2 '- (methoxycarbonylmethyloxy) -4'-methoxy-5' - (2.3.4.6-tetra-O-pivaloyl-β-Dg I ucopyranosyl I) propiophenone To one solution of 2-phenyl-2'-hydroxy-4'-methoxy-5 '- (2,3,4,6-tetra-O-pivaloyl-β-D-glucopyranosyl) propiophenone (0.35 g) in N, N-dimethylformamide (6 mL) add potassium carbonate (0.096 g) and methyl 2-bromoacetate (0.085 g) at room temperature, and the mixture is stirred at room temperature for 8 hours. The reaction mixture is poured into 0.5 mol / L aqueous hydrochloric acid solution, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water twice and brine and dried over anhydrous magnesium sulfate, and the solvent is removed under reduced pressure to give the title compound (0.38 g). 1H-N MR (CDCl 3) d ppm: 0.85 (9H, s), 1.12 (9H, s), 1.17 (9H, s), 1.22 (9H, s), 2.95-3.05 (2H, m), 3.30 -3.40 (2H, m), 3.70 (3H, s), 3.75-3.85 (1H, m), 3.86 (3H, s), 4.08 (1H, dd, J = 4.1, 12.4Hz), 4.20 (1 H, dd, J = 1 .7, 12.4Hz), 4.60-4.80 (3H, m), 5.20-5.60 (3H, m), 6.25 (1 H, s), 7.15-7.35 (5H, m), 7.85 (1 H, s) Process 7 2-Phenyl-2 '- (carboxymethyl) Loxi) -4'-methoxy-5 '- (2,3,4,6-tetra-O-pivaloyl-ß-Dg I ucopy ra nos) propiophenone To a solution of 2-phenyl-2' - (methoxycarbonyl-methyloxy) ) -4'-methoxy-5 '- (2, 3, 4,6-tetra-O-pivaloiI-ß-Dg I ucopiranos i I) propiophenone (0.15 g) in tetrahydrofuran (5 mL) is added 2 mol / L aqueous sodium hydroxide solution (0.18 mL) at room temperature, and the mixture is stirred at room temperature overnight. To the reaction mixture is added 2 ml / l additional aqueous sodium hydroxide solution (0.36 mL), and the mixture is stirred at room temperature for 5 hours. To the reaction mixture is added 5 mol / L additional aqueous sodium hydroxide solution (0.073 mL), and the mixture is stirred for 5 hours. After the reaction mixture is acidified by adding 1 mol / L aqueous hydrochloric acid solution, the mixture is extracted with diethyl ether. The organic layer is rinsed with brine and dried over anhydrous magnesium sulfate, and the solvent is removed under reduced pressure to give the title compound (0.15 g). 1 H-NMR (CDCl 3) d ppm: 0.87 (9H, s), 1.12 (9H, s), 1.15 (9H, s), 1.17 (9H, s), 3.00-3.10 (2H, m), 3.20-3.40 (2H, m), 3.80-3.95 (4H, m), 3.89 (3H, m), 4.05 (1 H, dd, J = 4.4, 12.5 Hz), 4.18 (1 H, dd, J = 1 .9, 12.5 Hz), 4.74 (2H, s), 4.80-5.00 (1 H, m), 5.20-5.50 (3H, m), 6.38 (1 H, s), 7.15-7.35 (5H, m), 7.80 (1 H, s) Process 8 1-r6-Methoxy-3- (2-phenylethyl) benzorbfuran-5-yl-1-deoxy-2.3.4.6-tetra-O-pivaloyl-β- D-glucopyranose To a mixture of 2-phenyl-2 '- (carboxymethyloxy) -4'-methoxy-5' - (2,3,4,6-tetra-O-pivaloyl-β-D-glucopyranosyl) -propiophenone ( 0.15 g), acetic acid (4.3 g) and sodium acetate (0.37 g) is added acetic anhydride (0.40 g), and the mixture is heated to reflux at 1 15 ° C overnight. The reaction mixture is cooled to room temperature and poured into water, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water twice, an aqueous solution of sodium hydrogen carbonate, water and brine and dried over anhydrous magnesium sulfate and the solvent is removed under reduced pressure. The residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 8/1) to give the title compound (0.03 g). 0. 81 (9H, s), 1.13 (9H, s), 1.18 (9H, s), 1.21 (9H, s), 2.85-3.05 (4H, m), 3.85 (3H, s), 3.85-3.95 (1H, m), 4.10 (1H, dd, J = 4.6.12.6 Hz), 4.23 (1H, dd, J = 1.8.12.6 Hz), 5.00-5.25 (1H, m), 5.30-5.40 (1H, m), 5.40 -5.60 (2H, m), 6.93 (1H, s), 7.10-7.75 (4H, m), 7.25-7.35 (2H, m), 7.53 (1H, s) Process 9 1-r6-Methoxy-3- ( 2-phenylethyl) benzorb1furan-5-yl-1-deoxy-β-D-glucopyranose To a suspension of 1- [6-methoxy-3- (2-phenylethyl) -benzo [b] furan-5- iI] -1-deoxy-2,3,4,6-tetra-O-pivaloyl-β-D-glucopyranose (0.03 g), in methanol (4 mL) is added sodium methoxide (28% methanol solution, 0.038) mL), and the mixture is stirred at 50 ° C for 6 hours. The reaction mixture is purified directly by column chromatography on silica gel (eluent: dichloromethane / methanol = 10 / 1-5 / 1) to give the title compound (0.015 g). 1H-NMR (CD3OD) d ppm: 2.90-3.05 (4H, m), 3.30-3.55 (3H, m), 3.55-3.65 (1H, m), 3.70 (1H, dd, J = 5.6.12.0 Hz), 3.80-3.95 (1H, m), 4.70-4.90 (1H, m), 7.07 (1H, s), 7.10-7.30 (5H, m), 7.32 (1H, s), 7.57 (1H, s) Example 3 1 -r3- (2-Phenylethyl) benzorb1thiophen-5-ill-1-deoxy-6-O-ethoxycarbonyl-β-D-glucopyranose To a solution of 1- [3- (2-phenylethyl) Benzo [b] -thiophen-5-yl] -1-deoxy-β-D-glucopyranose (0.19 g) in 2,4,6-trimethylpyridine (2 mL) is added ethyl chloroformate (1.1 mL) at 0 ° C , and the mixture is stirred at room temperature for 7 hours. The reaction mixture is poured into 10% aqueous citric acid solution, and the mixture is extracted with ethyl acetate. The organic layer is rinsed with brine and dried over anhydrous magnesium sulfate. The solvent is removed, and the residue is purified by column chromatography on silica gel (eluent: dichloromethane / methanol = 20/1) to give the title compound (0.16 g). 1H-NMR (CD3OD) d ppm: 1.20 (3H, t, J = 7.0Hz), 2.95-3.10 (2H, m), 3.10-3.20 (2H, m), 3.35-3.45 (1H, m), 3.45- 3.57 (2H, m), 3.60-3.70 (1H, m), 4.11 (2H, q, J = 7.0Hz), 4.29 (1H, d, J = 9.4Hz), 4.34 (1H, dd, J = 5.6, 11.7Hz), 4.48 (1H, d, J = 1.9, 11.7Hz), 7.10-7.30 (6H, m), 7.35-7.45 (1H, m), 7.75-7.85 (2H, m) Examples 4-14 The compounds described in Table 1 or 2 are prepared in a manner similar to that described in Example 1 using corresponding starting materials.

[Table 1] m), m), (3H, m), [Table 2] EXAMPLE 15 Process 1 6- B romo- 1 -toluen os or Ifon il- 1 H-indole To a solution of 6-bromo-1 H-indole (1.0 g) in N, N-dimethylformamide (10 mL) was add sodium hydride (55%, 0.23 g) at 0 ° C, and the mixture is stirred for 5 minutes. Toluenesulfonyl chloride (0.97 g) is added to the reaction mixture, and the mixture is stirred at room temperature for 2 hours. The reaction mixture is poured into water, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate. The solvent is removed under reduced pressure, and to the residue are added n-hexane and diethyl ether in a ratio of 2: 1. The solid is collected by filtration and dried under reduced pressure to give the title compound (1.2 g). Process 2 1 - (1-Toluenesulfonyl-1 H-indol-6-yl) -1-deoxy-2,3,4,6-tetra-O-benzyl-β-D-glucopyranose To a solution of 6-bromo-1 - toluenesuIfonil-1 H-indole (0.25 g) in tetrahydrofuran (8 mL) is added n-butyllithium (2.71 mol / L tetrahydrofuran solution, 0.26 mL) at -78 ° C, and the mixture is stirred for 5 minutes. To the mixture is added a solution of 2,3,4,6-tetra-O-benzyl-D-glucono-1,5-lactone (0.39 g) in tetrahydrofuran (2 mL) at -78 ° C, and the mixture stir at 0 ° C for 30 minutes. The reaction mixture is poured into an aqueous solution of saturated ammonium chloride, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate. The solvent is removed under reduced pressure, and the residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 3/1) to give the title compound (0.28 g). Process 3 1 - (1 -Toluenesulfonyl-1 H-indol-6-yl) -2,3,4,6-tetra-O-benzyl-D-glucopyranose To a solution of 1- (1-toluenesulfonyl-1 H-indole -6-il) -1-deoxy- 2, 3,4,6-tetra-O-benzyl-β-D-glucopyranose (0.28 g) and triethylsilane (0.68 g) in acetonitrile (4 mL) is added diethyl ether-boron trifluoride complex (0.053 g) to - 20 ° C and the mixture is stirred at room temperature for 30 minutes. An aqueous solution of saturated potassium carbonate is added to the reaction mixture, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate. The solvent is removed under reduced pressure, and the residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = .6 / 1-4 / 1) to give the title compound (0.19 g. ). 1 H-NMR (CDCl 3) d ppm: 2.21 (3H, s), 3.50-3.60 (1H, m), 3.60-3.70 (2H, m), 3.75-3.90 (4H, m), 4.26 (1H, d, J = 10.5Hz), 4.36 (1H, d, J = 9.4Hz), 4.59 (1H, d, J = 12.2Hz), 4.67 (1H, d, J = 10.8Hz), 4.69 (1H, d, J = 12.2 Hz), 4.90 (1H, d, J = 10.7Hz), 4.90 (1H, d, J = 11.1Hz), 4.94 (1H, d, J = 11.0Hz), 6.60-6.70 (1H, m), 6.80- 6.85 (2H, m), 7.00-7.18 (5H, m), 7.20-7.45 (16H, m), 7.54-7.55 (1H, m), 7.55-7.60 (1H, m), 7.65-7.75 (2H, m ), 8.10-8.15 (1H, m) Process 4 1- (1 H- 1 nd or l-6-i I) - 1-deoxy-2, 3.4, 6-tetra-O-be nci I- ß-D -glucopyranose To a solution of 1- (1-toluenesulfonyl-1 H-indol-6-yl) -1-deoxy-2,3,4,6-tetra-O-benzyl-β-D-glucopyranose (0.19 g) in ethanol (4 mL) and tetrahydrofuran (1 mL) is added potassium hydroxide (0.27 g), and the mixture is stirred at 50 ° C overnight. An aqueous solution of hydrochloric acid (2 mol / L, 6 mL) is added to the reaction mixture, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate. The solvent is removed under reduced pressure, and the residue is purified by column chromatography on silica gel (eluent: n-hexane / ethyl acetate = 3 / 1-3 / 2) to give the title compound (0.13 g) . 1 H-NMR (CDCl 3) d ppm: 3.55-3.68 (2H, m), 3.70 (1H, d, J = 10.6Hz), 3.75-3.90 (4H, m), 4.30 (1H, d, J = 10.6Hz) , 4.35 (1H, d, J = 9.4Hz), 4.57 (1H, d, J = 12.4Hz), 4.66 (1H, d, J = 10.7Hz), 4.68 (1H, d, J = 12.4Hz), 4.89 (1H, d, J = 10.7Hz), 4.90 (1H, d, J = 11.1Hz), 4.97 (1H, d, J = 11.1Hz), 6.64-6.60 (1H, m), 6.80-6.90 (2H, m), 7.05-7.40 (19H, m), 7.45-7.50 (1H, m), 7.60-7.70 (1H, m), 8.10-8.20 (1H, m) Process 5 1-ri- (4-Methylbenzyl) ) -1H-indol-6-n-1-deoxy-2,3,4,6-tetra-O-benzyl-β-D-glucopyranose To a solution of 1- (1 H -indol-6-yl) -1-deoxy -2,3,4,6-tetra-O-benzyl-β-D-glucopyranose (0.13 g) in N, N-dimethylformamide (2 mL) is added sodium hydride (60%, 0.01 g) at 0 ° C , and the mixture is stirred for 10 minutes. To the mixture is added 4-methylbenzylchloride (0.032 g) and the mixture is stirred at room temperature for 2 hours. The reaction mixture is poured into water, and the mixture is extracted with diethyl ether. The organic layer is rinsed with water and brine and dried over anhydrous magnesium sulfate. The solvent is removed under reduced pressure, and the residue is purified by column chromatography on silica gel (eluent. N-hexane / ethyl acetate = 5/1) to give the title compound (0.12 g). 1 H-NMR (CDCl 3) d ppm: 2.27 (3H, s), 3.50-3.65 (3H, m), 3.70-7.90 (4H, m), 4.22 (1H, d, J = 10.2Hz), 4.31 (1H, d, J = 9.5Hz), 4.54 (1H, d, J = 12.3Hz), 4.60-4.70 (2H, m), 4.88 (1H, d, 10.6Hz), 4.94 (1H, d, J = 10.7Hz) , 5.23 (2H, s), 6.50-6.55 (1H, m), 6.75-6.85 (2H, m), 6.90-7.00 (2H, m), 7.00-7.05 (2H, m), 7.05-7.40 (31H, m), 7.64-7.68 (1H, m) Process 6 1-H- (4-ethylbenzyl) -1 H -i nd or l-6-yl-1-deoxy-β-D-glucopyranose A solution of 1- [1- (4-methylbenzyl) -1H-indoI-6-yl] -1-deoxy-2,3,4,6-tetra-O-benzyl-β-D-glucopyranose and 10% palladium powder -carbon (0.12 g) in tetrahydrofuran (3 mL) and methanol (3 mL) is stirred at room temperature for 1 hour under a hydrogen atmosphere. The insoluble material is removed by filtration, and the filtrate is concentrated under reduced pressure. The residue is purified by column chromatography on silica gel (eluent: dichloromethane / methanol = 10/1) to give the title compound (0.035 g). 1H-NR (CD3OD) d ppm: 2.27 (3H, s), 3.30-3.55 (4H, m), 3.69 (1H, dd, J = 5.3, 12.0Hz), 3.87 (1H, dd, J = 1.7, 12.0Hz), 4.12 (1H, d, J = 8.9Hz), 5.34 (2H, s), 6.44-6.47 (1H, m), 7.00-7.05 (2H, m), 7.05-7.10 (2H, m), 7.13 (1H, dd, J = 1.2.8.Hz), 7.22 (1H, d, J = 3.2Hz), 7.42 (1H, m), 7.53 (1H, d, J = 8.1 Hz) The compounds described in Table 3 can be prepared in a manner similar to that described in the above Examples. [Table 3] Test Example 1 Test for inhibitory effects on human SGLT1 activity 1) Cloning and construction of the vector expressing human SGLT1 The cDNA library is prepared for PCR amplification by reverse transcription of total RNA deprived of human small intestine (Ori gene) using oligo-dT as a starter Using this cDNA library as a template, the DNA fragment encoding 1 to 2005 bp of human SGLT1 (ACCESS: M24847), which is reported by hyediger et al., Is amplified by PCR method and inserted into the multi-cloning site of pcDNA3.1 (-) (Invitrogen). The inserted DNA sequence fits perfectly to the sequence previously reported. 2) Establishment of cell line stably expressing human SGLT1 The expression vector of human SGLT1 is digested by Sea I in a linear DNA. Linear DNA is transfected into CHO-K1 cells by means of lipofection (Efectene Transfection Reagent: QIAGEN). Line strains resistant to neomycin are selected by culture in medium containing G418 (1 mg / ml, LIFE TECHNOLOGIES), and then the activity against the uptake of methyl-a-D-glucopyranoside is measured by the method described below. The cell line, which showed the highest capture activity, is selected and designated as CS1 -5-1 1 D. The CS1 -5-1 1 D cells are cultured in the presence of G418 at 200 μg / mL. 3) Measurement of inhibitory activity against methyl-aD-glucopyranoside (a-MG) capture CS1 -5-1 1 D cells are seeded in a 96-well culture plate at a density of 3x104 cells / well and cultured for 2 days, and are used in the intake test. A mixture of 14C labeled and unlabeled (Sigma) (Amersham Pharmacia Biotech) is added to the intake buffer (pH 7.4; containing 140 mM sodium chloride, 2 mM potassium chloride, 1 mM calcium chloride, 1 mM magnesium chloride, 10 mM 2- [4- (2-hydroxyethyl) -1-piperazinyl] ethane sulfonic acid and 5 mM tris (hydroxymethyl) aminomethane) in the final concentration of 1 mM. A test compound is dissolved in dimethyl sulfoxide, and then appropriately diluted with distilled water. The test compound solution is added to the intake regulator containing 1 mM a-MG, and designated as a measuring regulator. For the control group, the measurement regulator without compound test is prepared. To measure the basic intake, a basic intake measurement regulator containing 140 mM chorus chloride instead of sodium chloride is prepared. After removing the cell culture medium CS1 -5-1 1 D, 180 μL of the pre-treatment buffer (the basic intake regulator without a-MG) is added to each well and incubated at 37 ° C for 10 minutes . After repeating the same treatment, the pre-treatment regulator is removed. To each cavity 75 μL of the measuring regulator is added or the basic intake regulator is added and incubated at 37 ° C for 1 hour. After removing the measuring regulator, the cells are rinsed twice with 180 μL per rinsing regulator cavity (the basic intake regulator containing 10 mM non-labeled MG). The cells are solubilized by 75 μL per cavity of 0.2 mol / L sodium hydroxide. The cell lysates are transferred into PicoPlates (Packard), and then 150 μL of MicroScint-40 (Packard) are added and mixed. Radioactivity is measured by means of the TopCount micro-sampling counter (Packard). One hundred% is established in the difference between the intake in the control group and the baseline intake, and the intake of methyl a-D-glucopyranoside in each drug concentration is calculated. The concentration of drug, in which 50% methyl a-D-glucopyranoside intake is inhibited (IC50 value), is calculated using logit diagram. The results are shown in Table 4. [Table 4] Test example 2 Test for inhibitory effects on human SGLT2 activity 1) Cloning and construction of the vector expressing human SGLT2 The cDNA library is prepared for PCR amplification by reverse transcription of total RNA deprived of kidney (Ori gene) using oligo-dT as a primer. Using this cDNA library as a template, the DNA fragment encoding 2 to 2039 bp of human SGLT2 (ACCESS: M95549, M95299), which is reported by RG Wells et al., Is amplified by PCR method and inserted into the site Multi-cloning of pcDNA3.1 (-) (Invitrogen). The inserted DNA sequence fits perfectly to the sequence previously reported. 2) Establishment of cell line stably expressing human SGLT2 The expression vector of human SGLT2 is digested by Sea I in a linear DNA. Linear DNA is transfected into CHO-K1 cells by means of lipofection (Efectene Transfection Reagent: QIAGEN). Line strains resistant to neomycin are selected by culture in medium containing G418 (1 mg / ml, LI FE TECHNOLOGIES), and then the activity against the uptake of methyl-α-D-glucopyranoside is measured by the method described below. The cell line, which showed the highest capture activity, is selected and designated as CS2-5E. The CS2-5E cells are cultured in the presence of G418 at 200 μg / mL. 3) Measurement of the inhibitory activity against the intake of methyl-aD-glucopyranoside (a-MG) The CS2-5E cells are seeded in a 96-well culture plate at a density of 3x104 cells / well and cultured for 2 days, and they are used in the intake test. A mixture of 14C labeled and unlabeled (Sigma) (Amersham Pharmacia Biotech) is added to the intake buffer (pH 7.4; containing 140 mM sodium chloride, 2 mM potassium chloride, 1 mM calcium chloride, 1 mM magnesium chloride, 10 mM 2- [4- (2-hydroxyethyl) -1-piperazinyl-sulphonic acid sulfonic acid and 5 mM tris (hydroxymethyl) aminomethane) in the final concentration of 1 mM. A test compound is dissolved in dimethyl sulfoxide, and then appropriately diluted with distilled water. The test compound solution is added to the intake regulator containing 1 mM a-MG, and designated as a measuring regulator. For the control group, the measurement regulator without compound test is prepared. To measure the basic intake, a basic intake measurement regulator containing 140 mM chorus chloride instead of sodium chloride is prepared. After removing the cell culture medium CS1 -5-1 1 D, 180 μL of the pre-treatment buffer (the basic intake regulator without a-MG) is added to each well and incubated at 37 ° C for 10 minutes . After repeating the same treatment, the pre-treatment regulator is removed. To each cavity 75 μL of the measuring regulator is added or the basic intake regulator is added and incubated at 37 ° C for 1 hour. After removing the measuring regulator, the cells are rinsed twice with 180 μL per rinsing regulator cavity (the basic intake regulator containing 10 mM non-labeled MG). The cells are solubilized by 75 μL per cavity of 0.2 mol / L sodium hydroxide. The cell lysates are transferred into PicoPlates (Packard), and then 150 μL of MicroScint-40 (Packard) are added and mixed. Radioactivity is measured by means of the TopCount micro-sampling counter (Packard). One hundred% is established in the difference between the intake in the control group and the baseline intake, and the intake of methyl a-D-glucopyranoside in each drug concentration is calculated. The concentration of drug, in which 50% methyl a-D-glucopyranoside intake is inhibited (IC50 value), is calculated using logit diagram. The results are shown in Table 5.

[Table 5] Industrial Applicability The fused heterocyclic derivatives represented by the above general formula (I) of the present invention, pharmaceutically acceptable salts thereof and prodrugs thereof exert an inhibitory activity in human SGLT and can suppress the increase in glucose level in the blood or decrease the level of glucose in the blood by inhibiting the absorption of carbohydrate such as glucose in the small intestine or by inhibiting the reabsorption of glucose in the kidney. Thus, the present invention can provide excellent agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like.

Claims

CLAIMS 1. A fused heterocyclic derivative represented by the following general formula (I): wherein R1 to R4 independently represent a hydrogen atom, a hydroxy group, an amino group, a halogen atom, a C1-6 alkyl group, a C6_6 alkoxy group, a cyano group, a carboxy group, an alkoxycarbonyl group C2-7, a carbamoyl group, a mono- or di- (C1-6) alkyl amino group, a halo (d-6 alkyl) group, a hydroxy (d-6 alkyl) group, a cyano (d- alkyl) group 6), a carboxy group (C-6 alkyl), a C 2-7 alkoxycarbonyl group (C 1-6 alkyl), a carbamoyl group (C 1-6 alkyl), an amino group (d-6 alkyl), a mono group or di (C-6 alkyl) amino (d.6 alkyl), a halo (C 1-6 alkoxy) group, a hydroxy (d 6 alkoxy), a carboxy (d) alkoxy group, a C 2-7 alkoxycarbonyl group (C6-C6 alkoxy), a carbamoyl group (d6 alkoxy), an amino group (C1-6 alkoxy), a mono- or di (C6-6 alkyl) group (d6-alkoxy), a C3- cycloalkyl group 7, a C3-7 cycloalkyl group, a C3-7 cycloalkyl group (C6-6 alkyl), or a C3-7 cycloalkyl group (C1-6 alkoxy); R5 and R6 independently represent a hydrogen atom, a hydroxy group, a halogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C6-6 alkoxy group, an alkenyloxy group C2-6, a C-6 alkylthio group, a C2-6 alkenylthio group, a halo group (d-6 alkyl), a halo (C6-6 alkoxy) group, a halo (C1-6 alkylthio) group, a hydroxy group (C-6 alkyl), a hydroxy group (C 2-6 alkenyl), a hydroxy group (C 1-6 alkoxy), a hydroxy group (C 1-6 alkylthio), a carboxy group, a carboxy group (alkyl d. 6), a carboxy group (C 2-6 alkenyl), a carboxy group (C 1-6 alkoxy), a carboxy group (C 1-6 alkylthio), a C 2-7 alkoxycarbonyl group, a C 2-7 alkoxycarbonyl group (C 1-6 alkyl) 6), a C2-7 alkoxycarbonyl group (C2-6 alkenyl), a C2-7 alkoxycarbonyl group (C6-6 alkoxy), a C2-7 alkoxycarbonyl group (C1-6 alkylthio), a C1-6 alkylsulfonyl group, an alkylsulfonyl group of, -UVWN (R7) -Z or any of the following substituents (i) a (xxviii) which may have any of 1 to 3 groups selected from the following substituent group a on the ring; (i) an aryl group C6-? or > (0) aryl-O-C6-? Or> (i1) aryl-S- C6-? O, (iv) a C6-? O aryl group (C? 6 alkyl), (v) a group C6-10 aryl (C6 alkoxy), (vi) a C6- or C2-6 alkyl group, (vii) a heteroaryl group, (viii) heteroaryl-O-, (ix) heteroaryl-S- , (x) a heteroaryl group (C 1-6 alkyl), (xi) a heteroaryl group (d 6 alkoxy), (xii) a heteroaryl group (C 1-6 alkylthio), (xiii) a C 3-7 cycloalkyl group, (xiv) cycloalkyl-O-C3-7, (xv) cycloalkyl-S-C3-7, (xvi) a C3.7 cycloalkyl group (C6-6 alkyl), (xvii) a C3-7 cycloalkyl group (alkoxy) C1-6), (xviii) a C3-7 cycloalkyl (C1-6 alkylthio), (xix) a heterocycloalkyl group, (xx) heterocycloalkyl-O-, (xxi) heterocycloalkyl-S-, (xxii) a heterocycloalkyl group ( alkyl d-6), (xxiii) a heterocycloalkyl group (alkoxy d.6), (xxiv) a heterocycloalkyl group (C1 -6 alkylthio), (xxv) an aromatic cyclic amino group, (xxvi) an aromatic cyclic amino group ( C1 -6 alkyl), (xxvii) an aromatic cyclic amino group (alco xi C1 -6), or (xxviii) an aromatic cyclic amino group (alkylthio d-β). U represents -O-, -S- or a single bond and with the proviso that at least u of V and W is not a single bond, when U is -O- or -S-); V represents an alkylene group d-6 which may have a hydroxy group, a C2-6 alkenylene group or a single bond; W represents -CO-, -SO2-, -C (= N H) - or a single bond; Z represents a hydrogen atom, a C 2-7 alkoxycarbonyl group, a C 6 - aryl group or (C 2-7 alkoxycarbonyl), a formyl group, -RA, -CORB, -SO 2 RB, -CON (Rc) RD, -CSN (RC) RD, -SO2N H RA or -C (= N RE) N (RF) RG; R7, RA, Rc, and RD independently represent a hydrogen atom, a C-6 alkoyl group which may have any of 1 to 5 groups selected from the following substituent group β, or any of the following substituents (xxix) a (xxxii) which may have any of 1 to 3 groups selected from the following substituent group at; (xxix) a C6-10 aryl group, (xxx) a heteroaryl group, (xxxi) a C3.7 cycloalkyl group or (xxxii) a heterocycloalkyl group or Z and R7 together with the next nitrogen atom to form a aliphatic cyclic amino group which may have any of 1 to 3 groups selected from the following substituent group a; or Rc and RD are joined together with the next nitrogen atom to form an aliphatic cyclic amino group which may have any of 1 to 3 groups selected from the following substituent group a; RB represents a C2-7 alkoxycarbonyl group, an alkylsulfonylamino C6-6 group, a C6-6 alkylsulfonylamino group, a C6-6 alkyl group which may have any of 1 to 5 groups selected from the following substituent group β, or any of the following substituents (xxxiii) to (xxxvi) which may have any of 1 to 3 groups selected from the following substituent group a; (xxxiii) a C6-aryl group, (xxxiv) a heteroaryl group, (xxxv) a C3.7 cycloalkyl group or (xxxvi) a heterocycloalkyl group RE, RF and RG independently represent a hydrogen atom, a cyano group, a carbamoyl group, a C2-7 acyl group, a C2-7 alkoxycarbonyl group, a C6-? or (C2-7 alkoxycarbonyl) aryl group, a nitro group, an alkylsulfonyl group d-6, a sulfamide group, a carbamimidoyl group , or a C? _6 alkyl group which may have any of 1 to 5 groups selected from the following substituent group?; or both ER and RF join to form an ethylene group; or both RF and RG are bonded with the next nitrogen atom to form an aliphatic cyclic amino group which may have any substituent selected from the following substituent group a; Q represents -alkylene d.6-, -alkenylene C2-6-, -alkynylene C2-6-, -alkylene C1.6-O-, -alkylene C? -6-S-, -O-alkylene C? -6 -, -S- C 1-6 -alkylene-, -C 1-6 -alkylene-O-C 1-6 -alkylene-, -alkylene-6-S-alkylene C? .6-, -CON (R 8) -, -N ( R8) CO-, -C1-6alkylene-CON (R8) - or - CON (R8) -alkylene-β-; R8 represents a hydrogen atom or a C6 alkyl group; ring A represents a C6-? o aryl group or a heteroaryl group; ring: It represents R9 represents a hydrogen atom, a C? -6 alkyl group, a hydroxy (C1-6 alkyl) group, a C7 cycloalkyl group or a C3-7 cycloalkyl group (C? -6 alkyl); G represents a group represented by a formula: or a formula: E1 represents a hydrogen atom, a fluorine atom or a hydroxy group; E2 represents a hydrogen atom, a fluorine atom, a methyl group or a hydroxymethyl group; [substituent group a] a halogen atom, a hydroxy group, an amino group, a d.6 alkyl group, a C6.6 alkoxy group, a halo (d6 alkyl), a halo (C1-6 alkoxy) group , a hydroxy group (alkyl d.6), a C2-7 alkoxycarbonyl group (C1-6 alkyl), a hydroxy group (C6-coxy), an amino group (d6 alkyl), an amino group ( alkoxy d-6), a mono- or di- (d6-alkyl) amino group, a mono- or di-hydroxy (C6-6 alkyl) amino group, a C6-alkylsulfonyl group, an alkylsulfonylamino group d.6, an alkylsulfonylamino group d.6 (alkyl d-6), a carboxy group, a C 2-7 alkoxycarbonyl group, a sulfamoyl group and -CON (RH) R '[substituent group β] a halogen atom, a hydroxy group, an amino group, a alkoxy group d-6, an alkylthio group C? 6, a halo group (C? -6 alkoxy), a halo (alkylthio d.6) group, a hydroxy group (C? -6 alkoxy), a hydroxy group ( alkyldio d-6), an amino group (d6 alkoxy), an amino group (alkylthio d.6), a mono- or di (C1-6 alkyl) amino group, a moiety no or di [hydroxy (C6-alkyl)] amino, a ureido group, a sulfamide group, a mono- or di- (C1-6 alkyl) ureido group, a mono- or di-hydroxy (C1-6 alkyl)] ureido group , a mono or di (alkyl d. 6) Sulfonamide, a mono- or di-hydroxy (C6-6 alkyl) - sulfamide group, a C2-7 acylamino group, an amino group (C2-7 acylamino), a C6-6 alkylsulfonyl group, an alkylsulfonylamino group C? .6, a carbamoyl (alkylsulfonylamino C? _6) group, a carboxy group, a C2-7 alkoxycarbonyl group, -CON (RH) R ', and any of the following substituents (xxxvii) to (xxxxviii) which may have any of 1 to 3 groups selected from the substituent group a above in the ring; (xxxvii) an aryl group C6-to, (xxxviii) aryl C6-? oO-, (xxxix) an aryl group C6- or (alkoxy d_6), (xxxx) a C6-10 aryl group (alkylthio d.6) , (xxxxi) a heteroaryl group, (xxxxii) heteroaryl-O-, (xxxxiii) a C3-7 cycloalkyl group, (xxxxiv) C3.7-O- cycloalkyl, (xxxxv) a heterocycloalkyl group, (xxxxvi) heterocycloalkyl-O -, (xxxxvii) an aliphatic cyclic amino group or (xxxxviii) an aromatic cyclic amino group RH and R1 independently represent a hydrogen atom or a d-6 alkyl group which may have any of 1 to 3 groups selected from the following substituent group?; or both of RH and R1 are joined together with the next nitrogen atom to form an aliphatic cyclic amino group which may have any of 1 to 3 groups selected from the following substituent group d; [substituent group?] a halogen atom, a hydroxy group, an amino group, a d6 alkoxy group, a halo (alkoxy) group, a hydroxy (C6-6 alkoxy) group, an amino group (C1-6 alkoxy) ), a mono- or di (alkyl d.6) group, a mono- or di-hydroxy (C6-6) alkyl] amino group, a ureido group, a sulfamide group, a mono or di (alkyl d-6) group ureido, a mono- or di-hydroxy (d6-alkyl)] ureido group, a mono- or di- (d6-alkyl) sulphonamide group, a mono- or di-hydroxy (alkyll.6)] -sulfonamide group, an acylamino C2 group -7, an amino group (C2-7 acylamino), a C6 alkylsulfonyl group, an alkylsulfonylamino C6-6 group, a carbamoyl (alkylsulfonylamino d-6) group, a carboxy group, a C2-7 alkoxycarbonyl group, an sulfamoyl group and -CON (RJ) R? [substituent group d] a halogen atom, a hydroxy group, an amino group, a C1-6 alkyl group, an alkoxy d-6 group, a halo group (C6_6 alkyl), a halo group (C1_6 alkoxy) ), a hydroxy group (alkyl d_6), a C2_7 alkoxycarbonyl group (C1_6 alkyl), a hydroxy group (C_6 alkoxy), an amino group (C6_6 alkyl), an amino group (C alkoxy? -6), a mono- or di (alkyl d-6) amino group, a mono- or di-hydroxy (d6-alkyl) amino group, an alkylsulfonyl group C6-6, a C1-6 alkylsulfonylamino group, an alkylsulfonylamino group d- 6 (C6 alkyl), a carboxy group, a C2-7 alkoxycarbonyl group, a sulfamoyl group and -CON (RJ) R? RJ and R? independently represent a hydrogen atom or a C?-6 alkyl group which may have any of 1 to 3 groups selected from a hydroxy group, an amino group, a mono or di (C-6 alkyl) group, a C 2 - alkoxycarbonyl group 7 and a carbamoyl group; or both of RJ and R? they are joined together with the next nitrogen atom to form an aliphatic cyclic amino group which may have any of 1 to 3 groups selected from a hydroxy group, an amino group, a mono or di (C1-6 alkyl) group, an alkyl group C .6, a hydroxy group (alkyl d.6), a C2-7 alkoxycarbonyl group, a C2.7 alkoxycarbonyl group (C6 alkyl) and a carbamoyl group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof.
2. A fused heterocyclic derivative according to claim 1, characterized in that Q represents a methylene group, an ethylene group, -OCH2-, -CH2O-, -SCH2- or -CH2S-, or a pharmaceutically acceptable salt thereof, or a prodrug of the same. 3. A fused heterocyclic derivative according to claim 2, characterized in that Q represents an ethylene group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. 4. A fused heterocyclic derivative according to claim 2, characterized in that Q represents a methylene group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. 5. A fused heterocyclic derivative according to any of claims 1 to 4, characterized in that the ring: -A1 A ^ A1 represents , * d or a pharmaceutically acceptable salt thereof, or a prodrug thereof. 6. A heterocyclic derivative fused according to any of claims 1 to 4, characterized in that the ring: It represents or a pharmaceutically acceptable salt thereof, or a prodrug thereof. 7. A fused heterocyclic derivative according to claim 1, characterized in that R5 and R6 independently represent a hydrogen atom, a hydroxy group, a halogen atom, an alkylene group d-6, a C2.6 alkenyl group, a C2-6 alkynyl group, a d6 alkoxy group, a C2.6 alkenyloxy group, an alkylthio d-6 group, a C2-6 alkenylthio group, a halo group (C6_6 alkyl), a halo group ( alkoxy d-6), a halo (C 1 6 alkylthio) group, a hydroxy group (a! q uilo d-6), a hydroxy group (C 2-6 alkenyl), a hydroxy group (C-6 alkoxy) ) or a hydroxy (C1-C6 alkylthio) group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. 8. A fused heterocyclic derivative according to any of claims 1, 5, 6 and 7, characterized in that the ring A represents a benzene ring or a pyridine ring, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. 9. A fused heterocyclic derivative according to any of claims 1 to 8, characterized in that G represents a group represented by the formula: or a pharmaceutically acceptable salt thereof, or a prodrug thereof. 10. A pharmaceutical composition comprising as an active ingredient a fused heterocyclic derivative according to any one of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. eleven . A human SGLT inhibitor comprising as an active ingredient a fused heterocyclic derivative according to any one of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. 1 2. A human SG LT inhibitor according to claim 1, characterized in that SGLT is SGLT1 and / or SG LT2.
3. A human SG LT inhibitor according to claim 11, which is an agent for the inhibition of postprandial hyperglycaemia. 14. A human SGLT inhibitor according to claim 1 which is an agent for the prevention or treatment of a disease associated with hyperglycemia. 15. A human SGLT inhibitor according to claim 14, characterized in that the disease associated with hyperglycemia is a disease selected from the group consisting of diabetes, impaired glucose tolerance, diabetic complications, obesity, hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, metabolic disorder lipid, atherosclerosis, hypertension, congestive heart failure, edema, hyperuricemia and gout. 16. A human SGLT inhibitor according to claim 1 which is an agent for the inhibition of impaired glucose tolerance in progress in diabetes in a subject. 17. A pharmaceutical composition according to claim 10, characterized in that the dosage form is sustained release formulation. 18. A human SGLT inhibitor according to claim 1, characterized in that the dosage form is sustained release formulation. 19. A method for the inhibition of postprandial hyperglycemia, comprising administering an effective amount of a fused heterocyclic derivative according to any of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. A method for the prevention or treatment of a disease associated with hyperglycemia, comprising administering an effective amount of a fused heterocyclic derivative according to any of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. twenty-one . A method for the prevention or treatment according to claim 20, characterized in that the disease associated with hyperglycemia is a disease selected from the group consisting of diabetes, impaired glucose tolerance, diabetic complications, obesity, hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, metabolism disorder lipid, atherosclerosis, hypertension, congestive heart failure, edema, hyperuricemia and gout. 22. A method for inhibiting impaired glucose tolerance in progress in diabetes in a subject, comprising administering an effective amount of a fused heterocyclic derivative according to any one of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug of it. 23. A use of a fused heterocyclic derivative according to any one of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof for the manufacture of a pharmaceutical composition for the inhibition of postprandial hyperglycemia. 24. A use of a fused heterocyclic derivative according to any of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof for the manufacture of a pharmaceutical composition for the prevention or treatment of a disease associated with hyperglycemia. 25. A use according to claim 24, characterized in that the disease associated with hyperglycemia is a disease selected from the group consisting of diabetes, impaired glucose tolerance, diabetic complications, obesity, hyperinsulinemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, lipid metabolism disorder, atherosclerosis , hypertension, congestive heart failure, edema, hyperuricemia and gout. 26. A use of a fused heterocyclic derivative according to any one of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof for the manufacture of a pharmaceutical composition for the inhibition of impaired glucose tolerance in progress in diabetes in a subject. A pharmaceutical composition according to claim 10, comprising combination with at least one member selected from the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an insulin inhibitor, SGLT2, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, a dipeptidyl peptidase inhibitor IV, a tyrosine phosphatase-1 B inhibitor of protein, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a kinase-3 inhibitor, glycogen synthase, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, a? -aminobutyric acid receptor antagonist, a sodium channel antagonist, an NF-? B inhibitor of the transcription factor, a peroxidase inhibitor lipid, a N-acetylated linked acid dipeptidase inhibitor, an insulin-like growth factor I, platelet-derived growth factor, a platelet-derived growth factor analog, epidermal growth factor, nerve growth factor, a derivative of carnitine, uridine, 5-hydroxy-1-methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrhoeal, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a β3-adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a protein transfer inhibitor, microsomal triglyceride, a lipoxygenase inhibitor, a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter inhibitor / bile acid, an inhibitor of cholesterol ester transfer protein, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an enzyme-converting enzyme inhibitor, endothelin, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, an agent and antihypertensive vasodilator, a sympathetic blocking agent, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, an uricosuric agent and a urinary alkalizer. 28. A human SGLT inhibitor according to claim 1, comprising combination with at least one member selected from the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an inhibitor of SGLT2, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, a dipeptidyl peptidase inhibitor IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiroesitol, a glycogen synthase kinase-3 inhibitor, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analog, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an α-aminobutyric acid receptor antagonist, a sodium channel antagonist, an NF-? B inhibitor of the transcription factor, a lipid peroxidase inhibitor, an N-acetylated acid dipeptidase inhibitor, an insulin-like growth factor l, platelet-derived growth factor, an analogue of platelet-derived growth factor, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1-methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, a antidiarrheic, cathartic, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a beta3-adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a thyroid hormone receptor agonist, an absorption inhibitor of cholesterol, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, an acid derivative nicotinic acid, a bile acid sequestrant, a sodium cotransporter / bile acid inhibitor, an ester transfer inhibitor lesterol, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, a vasodilator antihypertensive agent, a sympathetic blocking agent, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, an uricosuric agent and a urinary alkalizer. A method for the inhibition of postprandial hyperglycemia according to claim 19, which comprises administering in combination with at least one member selected from the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an enhancer of insulin secretion, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, an inhibitor of dipeptidyl peptidase IV, an inhibitor of protein tyrosine phosphatase-1 B, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, an inhibitor of glycogen synthase kinase-3, a glucagon-like peptide-1, a glucagon-like peptide-1 analog, a Glycagon-like peptide-1 nystatin, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an antagonist of the α-aminobutyric acid receptor, a sodium channel antagonist, an NF-? B inhibitor of the transcription factor, a lipid peroxidase inhibitor, an N-acetylated acid dipeptidase inhibitor, an insulin-like growth factor I, platelet-derived growth factor, an analogue of platelet-derived growth factor, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1 -methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrheal, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a β3-adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor , probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a carnitine palmitoyltransferase inhibitor, an inhibitor of squalene, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a cotra inhibitor sodium / bile acid carrier, a cholesterol ester transfer protein inhibitor, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an enzyme inhibitor of endothelin conversion, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, an antihypertensive vasodilator agent, a sympathetic blocking agent, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, an inhibitor of synthesis of uric acid, an uricosuric agent and a urinary alkalizer. A method for the prevention or treatment of a disease associated with hyperglycemia according to claim 20, which comprises administering in combination with at least one member selected from the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, a peptidase inhibitor of dipeptidyl IV, a protein tyrosine phosphtase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor , D-chiro-initol, a glycogen synthase kinase-3 inhibitor, a glucagon-like peptide-1, a peptide-1 analogue similar to glucagon, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of advanced glycation end products, a kinase C inhibitor of protein, an α-aminobutyric acid receptor antagonist, a sodium channel antagonist, a NF- [beta] B inhibitor of the transcription factor, a peroxidase lipid inhibitor, an N-acetylated acid dipeptidase inhibitor, a insulin-like growth factor I, platelet-derived growth factor, a platelet-derived growth factor analog, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1-methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrheal, cathartic, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a beta3-adrenoceptor agonist, an inhibitor of acyl-coenzyme A cholesterol acyltransferase, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a palmitoyltransferase inhibitor of carnitine, an inhibitor of squalene synthase, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter inhibitor / bile acid, a cholesterol ester transfer protein inhibitor, an appetite suppressant, an angiotensin conversion enzyme inhibitor, an inhibitor of neutral endopeptidase, an angiotensin II receptor antagonist, an endothelin conversion enzyme inhibitor, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, an antihypertensive vasodilator agent, a sympathetic blocking agent, an agent centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, a uricosuric agent and a urinary alkalizer. 31 A method for the inhibition of impaired glucose tolerance in progress in diabetes in a subject according to claim 21, comprising administering in combination with at least one member selected from the group consisting of an insulin sensitivity enhancer, a glucose absorption inhibitor , a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a tripeptidyl II peptidase inhibitor, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, an inhibitor of hepatic gluconeogenesis, D-chiro-initol, a glycogen synthase kinase-3 inhibitor, a glucagon-like peptide-1, a p-analogue glucagon-like eptid-1, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of advanced glycation end products, an inhibitor protein kinase C, a? -aminobutyric acid receptor antagonist, a sodium channel antagonist, an NF-? B inhibitor of the transcription factor, a lipid peroxidase inhibitor, an inhibitor of acid dipeptidase linked to N-? acetylated, an insulin-like growth factor I, platelet-derived growth factor, a platelet-derived growth factor analog, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1 -methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrhoeal, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a beta3-adrenoceptor agonist, an inhi acyl-coenzyme A cholesterol acyltransferase bimer, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, an inhibitor of carnitine palmitoyltransferase, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter / bile acid inhibitor, a transfer protein inhibitor of cholesterol ester, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, an endothelin receptor antagonist, an diuretic agent, a calcium antagonist, an antihypertensive agent vasodilator, a blocking agent sympathetic, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, an uricosuric agent and a urinary alkalizer. 32. A use of (A) a fused heterocycle derivative according to any of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof and (B) at least one member selected from the group consisting of insulin sensitivity, a glucose uptake inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a inhibitor of tripeptidyl peptidase II, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a glycogen-synthase kinase-3 inhibitor, a glucagon-like peptide-1, a glucagon-like peptide-1 analogue, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an α-aminobutyric acid receptor antagonist, an sodium channel antagonist, an NF-? B inhibitor of the transcription factor, a lipid peroxidase inhibitor, an N-acetylated acid dipeptidase inhibitor, an insulin-like growth factor I, platelet-derived growth factor , an analogue of platelet-derived growth factor, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1-methylhydatoin, EGB-761, bimoclomol, sul odexide, Y-128, an antidiarrhoeal, cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a β3-adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a hormone receptor agonist thyroid, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a lipoprotein receptor low density, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter inhibitor / bile acid, a cholesterol ester transfer protein inhibitor, an appetite suppressant, an angiotensin conversion enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an enzyme-converting enzyme inhibitor, endothelin, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, a vasodilator antihypertensive agent, a sympathetic blocking agent, a centrally acting antihypertensive agent, an a2-adrenoceptor agonist, an antiplatelet agent, a synthetic synthesis inhibitor, uric acid, a uricosuric agent and a urinary alkalizer, for the manufacture of a pharmaceutical composition for the inhibition of postprandial hyperglycemia. 33. A use of (A) a fused heterocyclic derivative according to any of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof and (B) at least one member selected from the group consisting of a sensitivity enhancer. of insulin, a glucose absorption inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, an inhibitor of tripeptidyl peptidase II, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, an inhibitor of inhibitor of pyruvate dehydrogenase, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a glycogen-synthase kinase-3 inhibitor, a glucagon-like peptide-1, an analogue of glucagon-like peptide-1, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, an α-aminobutyric acid receptor antagonist, a sodium channel antagonist, a NF-β B inhibitor of the transcription factor, a lipid peroxidase inhibitor, an N-linked acid dipeptidase inhibitor -acetylated, insulin-like growth factor I, platelet-derived growth factor, an analogue of platelet-derived growth factor, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy-1-methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarrheal , cathartics, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a β3 adrenoceptor agonist, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor , a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor, a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, a nicotinic acid derivative , a bile acid sequestrant, a sodium / bilious acid cotransporter inhibitor, an ester transfer inhibitor of cholesterol, an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, a vasodilator antihypertensive agent, a sympathetic blocking agent, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, an uricosuric agent and a urinary alkalizer, for manufacture of a pharmaceutical composition for the prevention or treatment of a disease associated with hyperglycemia. 34. A use of (A) a fused heterocyclic derivative according to any of claims 1 to 9, or a pharmaceutically acceptable salt thereof, or a prodrug thereof and (B) at least one member selected from the group consisting of an enhancer of insulin sensitivity, a glucose uptake inhibitor, a biguanide, an insulin secretion enhancer, an SGLT2 inhibitor, an insulin or insulin analogue, a glucagon receptor antagonist, an insulin receptor kinase stimulant, a inhibitor of tripeptidyl peptidase II, an inhibitor of dipeptidyl peptidase IV, a protein tyrosine phosphatase-1 B inhibitor, a glycogen phosphorylase inhibitor, a glucose-6-phosphatase inhibitor, a fructose-biphosphatase inhibitor, a pyruvate dehydrogenase inhibitor, a hepatic gluconeogenesis inhibitor, D-chiro-initol, a glycogen synthase kinase-3 inhibitor, a glucagon-like peptide-1, an an Glucagon-like peptide-1 logo, a glucagon-like peptide-1 agonist, amylin, an amylin analogue, an amylin agonist, an aldose reductase inhibitor, an inhibitor of the formation of advanced glycation end products, a protein kinase C inhibitor, a? -aminobutyric acid receptor antagonist, a sodium channel antagonist, an NF-? B inhibitor of the transcription factor, a lipid peroxidase inhibitor, a dipeptidase inhibitor of acid bound to N-acetylated, an insulin-like growth factor I, platelet-derived growth factor, a platelet-derived growth factor analog, epidermal growth factor, nerve growth factor, a carnitine derivative, uridine, 5-hydroxy -1-methylhydatoin, EGB-761, bimoclomol, sulodoxide, Y-128, an antidiarreic, cathartic, a coenzyme A reductase inhibitor of hydroxymethylglutaryl, a fibrate, a beta-adrenoceptor agonist 3, an acyl-coenzyme A cholesterol acyltransferase inhibitor, probcol, a thyroid hormone receptor agonist, a cholesterol absorption inhibitor, a lipase inhibitor, a microsomal triglyceride transfer protein inhibitor, a lipoxygenase inhibitor , a carnitine palmitoyltransferase inhibitor, a squalene synthase inhibitor, a low density lipoprotein receptor enhancer, a nicotinic acid derivative, a bile acid sequestrant, a sodium cotransporter / bile acid inhibitor, an inhibitor of cholesterol ester transfer protein , an appetite suppressant, an angiotensin-converting enzyme inhibitor, a neutral endopeptidase inhibitor, an angiotensin II receptor antagonist, an endothelin-converting enzyme inhibitor, an endothelin receptor antagonist, a diuretic agent, a calcium antagonist, a vasodilator antihypertensive agent, a sympathetic blocking agent, a centrally acting antihypertensive agent, an a2 adrenoceptor agonist, an antiplatelet agent, a uric acid synthesis inhibitor, an uricosuric agent and a urinary alkalinizer, for the manufacture of a pharmaceutical composition for the inhibition of impaired glucose tolerance and n advance in diabetes in a subject.