WO2003026661A1 - Insulin secretion accelerator and novel pyrimidine derivative - Google Patents

Insulin secretion accelerator and novel pyrimidine derivative Download PDF

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Publication number
WO2003026661A1
WO2003026661A1 PCT/JP2002/009350 JP0209350W WO03026661A1 WO 2003026661 A1 WO2003026661 A1 WO 2003026661A1 JP 0209350 W JP0209350 W JP 0209350W WO 03026661 A1 WO03026661 A1 WO 03026661A1
Authority
WO
WIPO (PCT)
Prior art keywords
pyrimidine derivative
insulin secretion
insulin
novel pyrimidine
secretion accelerator
Prior art date
Application number
PCT/JP2002/009350
Other languages
French (fr)
Japanese (ja)
Inventor
Yasuhiro Yonetoku
Tatsuya Maruyama
Kenji Negoro
Hiroyuki Moritomo
Naoki Imanishi
Itsuro Shimada
Ayako Moritomo
Wataru Hamaguchi
Hana Misawa
Shigeru Yoshida
Takahide Ohishi
Original Assignee
Yamanouchi Pharmaceutical Co., Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Yamanouchi Pharmaceutical Co., Ltd. filed Critical Yamanouchi Pharmaceutical Co., Ltd.
Priority to JP2003530296A priority Critical patent/JPWO2003026661A1/en
Publication of WO2003026661A1 publication Critical patent/WO2003026661A1/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A pyrimidine derivative which is highly effective in promoting insulin secretion, increasing insulin content, and inhibiting blood sugar level from increasing and is usable for treatments for insulin-dependent diabetes, noninsulin-dependent diabetes, insulin-resistant diseases, and obesity.
PCT/JP2002/009350 2001-09-14 2002-09-12 Insulin secretion accelerator and novel pyrimidine derivative WO2003026661A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2003530296A JPWO2003026661A1 (en) 2001-09-14 2002-09-12 Insulin secretion promoter and novel pyrimidine derivatives

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2001-279671 2001-09-14
JP2001279671 2001-09-14
JP2002121012 2002-04-23
JP2002-121012 2002-04-23

Publications (1)

Publication Number Publication Date
WO2003026661A1 true WO2003026661A1 (en) 2003-04-03

Family

ID=26622233

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2002/009350 WO2003026661A1 (en) 2001-09-14 2002-09-12 Insulin secretion accelerator and novel pyrimidine derivative

Country Status (2)

Country Link
JP (1) JPWO2003026661A1 (en)
WO (1) WO2003026661A1 (en)

Cited By (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005047268A2 (en) * 2003-11-10 2005-05-26 X-Ceptor Therapeutics, Inc. Substituted pyrimidine compositions and methods of use
WO2005054199A1 (en) 2003-12-03 2005-06-16 Cytopia Research Pty Ltd Tubulin inhibitors
EP1549316A1 (en) * 2002-09-10 2005-07-06 Scios Inc. INHIBITORS OF TFG&bgr;
JP2005520821A (en) * 2002-03-15 2005-07-14 チバ　スペシャルティ　ケミカルズ　ホールディング　インコーポレーテッド 4-Aminopyrimidine and its use for antimicrobial treatment of surfaces
EP1610774A2 (en) * 2003-04-09 2006-01-04 Exelixis, Inc. Tie-2 modulators and methods of use
WO2006076231A2 (en) * 2005-01-10 2006-07-20 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2007120702A2 (en) 2006-04-11 2007-10-25 Arena Pharmaceuticals, Inc. Use of gpr119 receptor agonists for increasing bone mass and for treating osteoporosis, and combination therapy relating thereto
WO2008128984A1 (en) * 2007-04-20 2008-10-30 Probiodrug Ag Aminopyrimidine derivatives as glutaminyl cyclase inhibitors
JP2009526868A (en) * 2006-02-15 2009-07-23 アボット・ラボラトリーズ Novel acetyl-CoA carboxylase (ACC) inhibitors and their use in diabetes, obesity and metabolic syndrome
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
JP2010195834A (en) * 2001-12-07 2010-09-09 Vertex Pharmaceuticals Inc Compound based on pyrimidine which is useful as gsk-3 inhibitor
US20100298143A1 (en) * 2009-05-19 2010-11-25 Dow Agrosciences Llc Compounds and methods for controlling fungi
EP2107908A4 (en) * 2007-02-02 2011-07-20 Redpoint Bio Corp Use of a trpm5 inhibitor to regulate insulin and glp-1 release
EP2402750A1 (en) 2006-04-11 2012-01-04 Arena Pharmaceuticals, Inc. Methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual
CN103896856A (en) * 2012-12-25 2014-07-02 叶龙 Multi-substituted monocyclopyrimidine JNK (Jun N Terminal) kinase inhibitor as well as preparation method and use thereof
WO2014105952A3 (en) * 2012-12-28 2014-10-09 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
US8933083B2 (en) 2003-01-14 2015-01-13 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
US10894787B2 (en) 2010-09-22 2021-01-19 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
US11534424B2 (en) 2017-02-16 2022-12-27 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
US11884626B2 (en) 2015-06-22 2024-01-30 Arena Pharmaceuticals, Inc. Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1P1 receptor-associated disorders

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH1087492A (en) * 1996-06-25 1998-04-07 Ono Pharmaceut Co Ltd Nitrogen monoxide production inhibitor
WO1998037079A1 (en) * 1997-02-19 1998-08-27 Berlex Laboratories, Inc. N-heterocyclic derivatives as nos inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH1087492A (en) * 1996-06-25 1998-04-07 Ono Pharmaceut Co Ltd Nitrogen monoxide production inhibitor
WO1998037079A1 (en) * 1997-02-19 1998-08-27 Berlex Laboratories, Inc. N-heterocyclic derivatives as nos inhibitors

Cited By (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010195834A (en) * 2001-12-07 2010-09-09 Vertex Pharmaceuticals Inc Compound based on pyrimidine which is useful as gsk-3 inhibitor
JP2005520821A (en) * 2002-03-15 2005-07-14 チバ　スペシャルティ　ケミカルズ　ホールディング　インコーポレーテッド 4-Aminopyrimidine and its use for antimicrobial treatment of surfaces
EP1549316A1 (en) * 2002-09-10 2005-07-06 Scios Inc. INHIBITORS OF TFG&bgr;
EP1549316A4 (en) * 2002-09-10 2008-04-09 Scios Inc INHIBITORS OF TFGbeta
US8933083B2 (en) 2003-01-14 2015-01-13 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
JP4895806B2 (en) * 2003-04-09 2012-03-14 エクセリクシス， インク． TIE-2 modulator and usage
JP2006523238A (en) * 2003-04-09 2006-10-12 エクセリクシス， インク． TIE-2 modulator and usage
EP1610774A4 (en) * 2003-04-09 2008-07-16 Exelixis Inc Tie-2 modulators and methods of use
EP1610774A2 (en) * 2003-04-09 2006-01-04 Exelixis, Inc. Tie-2 modulators and methods of use
US8410119B2 (en) 2003-07-14 2013-04-02 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US7625906B2 (en) 2003-07-14 2009-12-01 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2005047268A2 (en) * 2003-11-10 2005-05-26 X-Ceptor Therapeutics, Inc. Substituted pyrimidine compositions and methods of use
WO2005047268A3 (en) * 2003-11-10 2005-07-21 X Ceptor Therapeutics Inc Substituted pyrimidine compositions and methods of use
JP2011093930A (en) * 2003-12-03 2011-05-12 Ym Biosciences Australia Pty Ltd Tubulin inhibitor
JP2007513093A (en) * 2003-12-03 2007-05-24 サイトピア・リサーチ・ピーティーワイ・リミテッド Tubulin inhibitor
AU2004294354B2 (en) * 2003-12-03 2009-02-19 Ym Biosciences Australia Pty Ltd Tubulin inhibitors
US7981900B2 (en) 2003-12-03 2011-07-19 Ym Biosciences Australia Pty Ltd 2-phenyl pyrimidines which are tubulin inhibitors
JP4772690B2 (en) * 2003-12-03 2011-09-14 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド Tubulin inhibitor
US9732046B2 (en) 2003-12-03 2017-08-15 Ym Biosciences Australia Pty Ltd. Substituted 1,2,4-triazines as tubulin inhibitors
EP2277865A1 (en) * 2003-12-03 2011-01-26 YM BioSciences Australia Pty Ltd Phenyl-substituted 6-ring nitrogen-heterocycles as microtubule polymerisation inhibitors
US9139560B2 (en) 2003-12-03 2015-09-22 Ym Biosciences Australia Pty Ltd. Substituted pyrazines as tubulin inhibitors
WO2005054199A1 (en) 2003-12-03 2005-06-16 Cytopia Research Pty Ltd Tubulin inhibitors
US8394806B2 (en) 2003-12-03 2013-03-12 Ym Biosciences Australia Pty Ltd 2-phenyl pyrazines as tubulin inhibitors
WO2006076231A2 (en) * 2005-01-10 2006-07-20 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level
EP1808168A1 (en) * 2005-01-10 2007-07-18 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
EP2116235A1 (en) 2005-01-10 2009-11-11 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
EP2322157A1 (en) 2005-01-10 2011-05-18 Arena Pharmaceuticals, Inc. Composition for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
EA011883B1 (en) * 2005-01-10 2009-06-30 Арена Фармасьютикалз, Инк. Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level
WO2006076231A3 (en) * 2005-01-10 2007-01-18 Arena Pharm Inc Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level
JP2009526868A (en) * 2006-02-15 2009-07-23 アボット・ラボラトリーズ Novel acetyl-CoA carboxylase (ACC) inhibitors and their use in diabetes, obesity and metabolic syndrome
EP2253311A2 (en) 2006-04-11 2010-11-24 Arena Pharmaceuticals, Inc. Use of GPR119 receptor agonists for increasing bone mass and for treating osteoporosis, as well as combination therapy relating thereto
WO2007120702A2 (en) 2006-04-11 2007-10-25 Arena Pharmaceuticals, Inc. Use of gpr119 receptor agonists for increasing bone mass and for treating osteoporosis, and combination therapy relating thereto
EP2402750A1 (en) 2006-04-11 2012-01-04 Arena Pharmaceuticals, Inc. Methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual
EP2107908A4 (en) * 2007-02-02 2011-07-20 Redpoint Bio Corp Use of a trpm5 inhibitor to regulate insulin and glp-1 release
US8188094B2 (en) 2007-04-20 2012-05-29 Probiodrug Ag Inhibitors of glutaminyl cyclase
WO2008128984A1 (en) * 2007-04-20 2008-10-30 Probiodrug Ag Aminopyrimidine derivatives as glutaminyl cyclase inhibitors
JP2010524896A (en) * 2007-04-20 2010-07-22 プロビオドルグ エージー Aminopyridine derivatives as glutaminyl cyclase inhibitors
US8883714B2 (en) 2008-04-07 2014-11-11 Arena Pharmaceuticals, Inc. Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
US20100298143A1 (en) * 2009-05-19 2010-11-25 Dow Agrosciences Llc Compounds and methods for controlling fungi
JP2012527461A (en) * 2009-05-19 2012-11-08 ダウ アグロサイエンシィズ エルエルシー Compounds and methods for controlling fungi
CN102438993A (en) * 2009-05-19 2012-05-02 陶氏益农公司 Compounds and methods for controlling fungi
US8759356B2 (en) * 2009-05-19 2014-06-24 Dow Agrosciences, Llc. Compounds and methods for controlling fungi
US10894787B2 (en) 2010-09-22 2021-01-19 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
CN103896856B (en) * 2012-12-25 2016-06-08 叶龙 A kind of polysubstituted monocycle miazines JNK kinase inhibitor and its production and use
CN103896856A (en) * 2012-12-25 2014-07-02 叶龙 Multi-substituted monocyclopyrimidine JNK (Jun N Terminal) kinase inhibitor as well as preparation method and use thereof
US20150344443A1 (en) * 2012-12-28 2015-12-03 The United States Of America, As Represented By The Secretary, Department Of Health And Human Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
JP2016504365A (en) * 2012-12-28 2016-02-12 アメリカ合衆国 USP1 / UAF1 deubiquitinase complex inhibitor and use thereof
US9802904B2 (en) * 2012-12-28 2017-10-31 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof
WO2014105952A3 (en) * 2012-12-28 2014-10-09 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
US11884626B2 (en) 2015-06-22 2024-01-30 Arena Pharmaceuticals, Inc. Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1P1 receptor-associated disorders
US11534424B2 (en) 2017-02-16 2022-12-27 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis

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