HRP20120829T1 - Karboksilne kiseline supstituirane fenilaminobenzoksazolom, postupak njihovog dobivanja i njihova upotreba kao medikamenata - Google Patents
Karboksilne kiseline supstituirane fenilaminobenzoksazolom, postupak njihovog dobivanja i njihova upotreba kao medikamenata Download PDFInfo
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- HRP20120829T1 HRP20120829T1 HRP20120829TT HRP20120829T HRP20120829T1 HR P20120829 T1 HRP20120829 T1 HR P20120829T1 HR P20120829T T HRP20120829T T HR P20120829TT HR P20120829 T HRP20120829 T HR P20120829T HR P20120829 T1 HRP20120829 T1 HR P20120829T1
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- inhibitor
- agonist
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- alkyl
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- 239000003814 drug Substances 0.000 title claims 6
- 238000004519 manufacturing process Methods 0.000 title claims 4
- 238000000034 method Methods 0.000 title claims 2
- 150000001735 carboxylic acids Chemical class 0.000 title 1
- BFLIOKCEGCUTNH-UHFFFAOYSA-N n-phenyl-1,3-benzoxazol-2-amine Chemical group N=1C2=CC=CC=C2OC=1NC1=CC=CC=C1 BFLIOKCEGCUTNH-UHFFFAOYSA-N 0.000 title 1
- 239000000556 agonist Substances 0.000 claims 17
- 239000003112 inhibitor Substances 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 229940079593 drug Drugs 0.000 claims 4
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 4
- 229940086609 Lipase inhibitor Drugs 0.000 claims 3
- 102100038831 Peroxisome proliferator-activated receptor alpha Human genes 0.000 claims 3
- 239000013543 active substance Substances 0.000 claims 3
- 239000005557 antagonist Substances 0.000 claims 3
- 229940126601 medicinal product Drugs 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 2
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 2
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 239000000637 Melanocyte-Stimulating Hormone Substances 0.000 claims 2
- 108010007013 Melanocyte-Stimulating Hormones Proteins 0.000 claims 2
- -1 SCF3 Chemical group 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 239000003613 bile acid Substances 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 238000002483 medication Methods 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 claims 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- YYGNTYWPHWGJRM-UHFFFAOYSA-N (6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene Chemical compound CC(C)=CCCC(C)=CCCC(C)=CCCC=C(C)CCC=C(C)CCC=C(C)C YYGNTYWPHWGJRM-UHFFFAOYSA-N 0.000 claims 1
- ZOBPZXTWZATXDG-UHFFFAOYSA-N 1,3-thiazolidine-2,4-dione Chemical compound O=C1CSC(=O)N1 ZOBPZXTWZATXDG-UHFFFAOYSA-N 0.000 claims 1
- 102100036506 11-beta-hydroxysteroid dehydrogenase 1 Human genes 0.000 claims 1
- 101710186107 11-beta-hydroxysteroid dehydrogenase 1 Proteins 0.000 claims 1
- DWEQEAULNYFVCY-UHFFFAOYSA-N 3-[2-(2-methylanilino)-1,3-benzoxazol-6-yl]propanoic acid Chemical compound CC1=CC=CC=C1NC1=NC2=CC=C(CCC(O)=O)C=C2O1 DWEQEAULNYFVCY-UHFFFAOYSA-N 0.000 claims 1
- SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 claims 1
- 102000004146 ATP citrate synthases Human genes 0.000 claims 1
- 108090000662 ATP citrate synthases Proteins 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 1
- 229940123208 Biguanide Drugs 0.000 claims 1
- 102000013585 Bombesin Human genes 0.000 claims 1
- 108010051479 Bombesin Proteins 0.000 claims 1
- 229940123158 Cannabinoid CB1 receptor antagonist Drugs 0.000 claims 1
- 229940121889 Endothelin A receptor antagonist Drugs 0.000 claims 1
- 102000027487 Fructose-Bisphosphatase Human genes 0.000 claims 1
- 108010017464 Fructose-Bisphosphatase Proteins 0.000 claims 1
- 102000019432 Galanin Human genes 0.000 claims 1
- 101800002068 Galanin Proteins 0.000 claims 1
- 229940122904 Glucagon receptor antagonist Drugs 0.000 claims 1
- 229940117965 Glucocorticoid receptor modulator Drugs 0.000 claims 1
- 229940121931 Gluconeogenesis inhibitor Drugs 0.000 claims 1
- 229920002527 Glycogen Polymers 0.000 claims 1
- 108010051975 Glycogen Synthase Kinase 3 beta Proteins 0.000 claims 1
- 102100038104 Glycogen synthase kinase-3 beta Human genes 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 101000843809 Homo sapiens Hydroxycarboxylic acid receptor 2 Proteins 0.000 claims 1
- 102100030643 Hydroxycarboxylic acid receptor 2 Human genes 0.000 claims 1
- 239000003458 I kappa b kinase inhibitor Substances 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 102000000853 LDL receptors Human genes 0.000 claims 1
- 108010001831 LDL receptors Proteins 0.000 claims 1
- 102000016267 Leptin Human genes 0.000 claims 1
- 108010092277 Leptin Proteins 0.000 claims 1
- 102000004882 Lipase Human genes 0.000 claims 1
- 108090001060 Lipase Proteins 0.000 claims 1
- 239000004367 Lipase Substances 0.000 claims 1
- 108010013563 Lipoprotein Lipase Proteins 0.000 claims 1
- 102100022119 Lipoprotein lipase Human genes 0.000 claims 1
- 102000057248 Lipoprotein(a) Human genes 0.000 claims 1
- 108010033266 Lipoprotein(a) Proteins 0.000 claims 1
- 229940122014 Lyase inhibitor Drugs 0.000 claims 1
- 102100031545 Microsomal triglyceride transfer protein large subunit Human genes 0.000 claims 1
- 108010015847 Non-Receptor Type 1 Protein Tyrosine Phosphatase Proteins 0.000 claims 1
- 102000002512 Orexin Human genes 0.000 claims 1
- 108010016731 PPAR gamma Proteins 0.000 claims 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 1
- 229940122054 Peroxisome proliferator-activated receptor delta agonist Drugs 0.000 claims 1
- 102100038825 Peroxisome proliferator-activated receptor gamma Human genes 0.000 claims 1
- 229940086543 Phosphoenol pyruvate carboxykinase inhibitor Drugs 0.000 claims 1
- 102000004257 Potassium Channel Human genes 0.000 claims 1
- 229940123866 Protein kinase C beta inhibitor Drugs 0.000 claims 1
- 108091006296 SLC2A1 Proteins 0.000 claims 1
- 108091006299 SLC2A2 Proteins 0.000 claims 1
- 102000000019 Sterol Esterase Human genes 0.000 claims 1
- 108010055297 Sterol Esterase Proteins 0.000 claims 1
- 101100054666 Streptomyces halstedii sch3 gene Proteins 0.000 claims 1
- 229940100389 Sulfonylurea Drugs 0.000 claims 1
- BHEOSNUKNHRBNM-UHFFFAOYSA-N Tetramethylsqualene Natural products CC(=C)C(C)CCC(=C)C(C)CCC(C)=CCCC=C(C)CCC(C)C(=C)CCC(C)C(C)=C BHEOSNUKNHRBNM-UHFFFAOYSA-N 0.000 claims 1
- 229940123464 Thiazolidinedione Drugs 0.000 claims 1
- 102100031241 Thioredoxin reductase 2, mitochondrial Human genes 0.000 claims 1
- 108010071769 Thyroid Hormone Receptors beta Proteins 0.000 claims 1
- 102100033001 Tyrosine-protein phosphatase non-receptor type 1 Human genes 0.000 claims 1
- 102000008219 Uncoupling Protein 2 Human genes 0.000 claims 1
- 108010021111 Uncoupling Protein 2 Proteins 0.000 claims 1
- 102000008200 Uncoupling Protein 3 Human genes 0.000 claims 1
- 108010021098 Uncoupling Protein 3 Proteins 0.000 claims 1
- 102000005630 Urocortins Human genes 0.000 claims 1
- 108010059705 Urocortins Proteins 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 claims 1
- 229940121373 acetyl-coa carboxylase inhibitor Drugs 0.000 claims 1
- 239000003463 adsorbent Substances 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 239000003392 amylase inhibitor Substances 0.000 claims 1
- 230000003178 anti-diabetic effect Effects 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 claims 1
- 229940125388 beta agonist Drugs 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- DNDCVAGJPBKION-DOPDSADYSA-N bombesin Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC=1NC2=CC=CC=C2C=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1NC(=O)CC1)C(C)C)C1=CN=CN1 DNDCVAGJPBKION-DOPDSADYSA-N 0.000 claims 1
- 239000003555 cannabinoid 1 receptor antagonist Substances 0.000 claims 1
- 230000001906 cholesterol absorption Effects 0.000 claims 1
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims 1
- 229940125881 cholesteryl ester transfer protein inhibitor Drugs 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 1
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N dodecahydrosqualene Natural products CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 claims 1
- 239000003062 endothelin A receptor antagonist Substances 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- 229940125753 fibrate Drugs 0.000 claims 1
- 229940124828 glucokinase activator Drugs 0.000 claims 1
- 229940096919 glycogen Drugs 0.000 claims 1
- 239000000122 growth hormone Substances 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- 239000000411 inducer Substances 0.000 claims 1
- 229940039781 leptin Drugs 0.000 claims 1
- NRYBAZVQPHGZNS-ZSOCWYAHSA-N leptin Chemical compound O=C([C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(C)C)CCSC)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CS)C(O)=O NRYBAZVQPHGZNS-ZSOCWYAHSA-N 0.000 claims 1
- 235000019421 lipase Nutrition 0.000 claims 1
- 239000002697 lyase inhibitor Substances 0.000 claims 1
- 229950004994 meglitinide Drugs 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- SLZIZIJTGAYEKK-CIJSCKBQSA-N molport-023-220-247 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)CN)[C@@H](C)O)C1=CNC=N1 SLZIZIJTGAYEKK-CIJSCKBQSA-N 0.000 claims 1
- 239000002658 neuropeptide Y receptor agonist Substances 0.000 claims 1
- 230000002474 noradrenergic effect Effects 0.000 claims 1
- 108060005714 orexin Proteins 0.000 claims 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 108020001213 potassium channel Proteins 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229940076279 serotonin Drugs 0.000 claims 1
- 239000000952 serotonin receptor agonist Substances 0.000 claims 1
- 230000002295 serotoninergic effect Effects 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 229940031439 squalene Drugs 0.000 claims 1
- TUHBEKDERLKLEC-UHFFFAOYSA-N squalene Natural products CC(=CCCC(=CCCC(=CCCC=C(/C)CCC=C(/C)CC=C(C)C)C)C)C TUHBEKDERLKLEC-UHFFFAOYSA-N 0.000 claims 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 1
- 239000000777 urocortin Substances 0.000 claims 1
Classifications
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (9)
1. Spoj formule I,
[image]
naznačen time što
R1 je H;
R6, R7, R8, R9 i R10 su međusobno neovisno H, F, Cl, Br, CF3, OCH3, OCF3, OCHF2, SCH3, SCF3, fenil, (C1-C6)-alkil, O-(C1-C6)-alkil ili NR3R4, gdje alkil i fenil mogu biti supstituirani s jednim ili više R2, te gdje u svakom slučaju dva od radikala R6, R7, R8, R9, R10 na susjednim položajima u fenilnom prstenu zajedno mogu tvoriti radikal -CH=CH-CH=CH-;
m je 0, 1, 2 ili 3;
X je -(CH2)2-;
R2 je F, Cl, Br, CN, OCH3, OCF3, CH3, CF3, (C1-C6)-alkil ili O-(C1-C6)-alkil, gdje alkil može biti supstituiran s jednim ili više OH, F, Cl, Br ili CN;
R3, R4 su međusobno neovisno H ili (C1-C6)-alkil;
izuzevši 3-(2-o-tolilaminobenzoksazol-6-il)propansku kiselinu;
i njihove fiziološki prihvatljive soli.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen upotrebi u obliku medikamenta.
3. Medikament, naznačen time što sadrži jedan ili više spojeva u skladu s patentnim zahtjevom 1.
4. Medikament, naznačen time što sadrži jedan ili više spojeva u skladu s patentnim zahtjevom 1 i najmanje jedan dodatni aktivni sastojak.
5. Medikament u skladu s patentnim zahtjevom 4, naznačen time što kao dodatnu aktivnu tvar sadrži jedan ili više antidijabetika, hipoglikemijskih aktivnih sastojaka, inhibitora HMGCoA-reduktaze, inhibitora apsorpcije kolesterola, agonista PPAR-γ, agonista PPAR-α, agonista PPAR-α/γ, agonista PPAR-δ, fibrata, inhibitora MTP, inhibitora apsorpcije žučnih kiselina, inhibitora CETP, polimernih adsorbensa žučnih kiselina, induktora receptora za LDL, inhibitora ACAT, antioksidansa, inhibitora lipoprotein-lipaze, inhibitora ATP-citrat-lijaze, inhibitora skvalen-sintetaze, antagonista lipoproteina(a), agonista receptora HM74A, inhibitora lipaze, inzulina, sulfonilurea, bigvanida, meglitinida, tiazolidindiona, inhibitora α-glukozidaze, aktivnih tvari koje djeluju na kalijski kanal ovisan o ATP-u u beta-stanicama, inhibitora glikogen-fosforilaze, antagonisti glukagonskog receptora, aktivatora glukokinaze, inhibitora glukoneogeneze, inhibitora fruktoza-1,6-bisfosfataze, modulatora glukoznog transportera 4 (GLUT4), inhibitora glutamin-fruktoza-6-fosfat-amidotransferaze, inhibitora dipeptidilpeptidaze IV (DPP-IV), inhibitora 11β-hidroksisteroid-dehidrogenaze 1, inhibitora protein-tirozin-fosfataze 1B, modulatora glukoznog transportera 1 ili 2 ovisnog o natriju, inhibitora lipaze osjetljive na hormone, inhibitora acetil-CoA-karboksilaze, inhibitora fosfoenolpiruvat-karboksikinaze, inhibitora glikogen-sintaza-kinaze-3β, inhibitora protein-kinaze Cβ, antagonista receptora za endotelin-A, inhibitora IκB-kinaze, modulatora glukokortikoidnog receptora, agonista CART, agonista NPY, agonista MC4, oreksinskih agonista, agonista H3, agonista TNF, agonista CRF, CRF BP antagonisti, urokortinskih agonista, agonista β3, antagonista receptora CB1, agonista MSH (hormon stimulacije melanocita), agonista CCK, inhibitora povratnog unosa serotonin, miješanih serotoninergičkih i noradrenergičkih spojeva, agonista 5-HT, bombezinskih agonista, galaninskih antagonista, hormona rasta, liberatora hormona rasta, agonista TRH, modulatora rasprežućeg proteina 2 ili 3, leptinskih agonista, agonista DA, inhibitora lipaze/amilaze, modulatora PPAR, modulatora RXR ili agonista TR-β ili amfetamina.
6. Upotreba spojeva u skladu s patentnim zahtjevom 1, naznačena time što su navedeni spojevi namijenjeni proizvodnji medikamenta za snižavanje razine glukoze u krvi.
7. Upotreba spojeva u skladu s patentnim zahtjevom 1, naznačena time što su navedeni spojevi namijenjeni proizvodnji medikamenta za liječenje dijabetesa.
8. Upotreba spojeva u skladu s patentnim zahtjevom 1, naznačena time što su navedeni spojevi namijenjeni proizvodnji medikamenta za pojačavanje otpuštanja inzulina.
9. Postupak proizvodnje medikamenta koji sadrži jedan ili više spojeva u skladu s patentnim zahtjevom 1, naznačen time što se sastoji u miješanju aktivne tvari s farmaceutski prihvatljivom podlogom i prevođenju te smjese u oblik pogodan za primjenu.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102006021878A DE102006021878A1 (de) | 2006-05-11 | 2006-05-11 | Phenylamino-benzoxazol substituierte Carbonsäuren, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| PCT/EP2007/003806 WO2007131622A1 (de) | 2006-05-11 | 2007-04-30 | Phenylamino-benzoxazol substituierte carbonsäuren, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel |
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| HRP20120829T1 true HRP20120829T1 (hr) | 2012-11-30 |
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| HRP20120829TT HRP20120829T1 (hr) | 2006-05-11 | 2012-10-15 | Karboksilne kiseline supstituirane fenilaminobenzoksazolom, postupak njihovog dobivanja i njihova upotreba kao medikamenata |
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| BR (1) | BRPI0711448A2 (hr) |
| CA (1) | CA2651660A1 (hr) |
| CO (1) | CO6241107A2 (hr) |
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| ZA (1) | ZA200808490B (hr) |
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| US7572934B2 (en) | 2007-04-16 | 2009-08-11 | Amgen Inc. | Substituted biphenyl GPR40 modulators |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| JP5591706B2 (ja) | 2007-10-10 | 2014-09-17 | アムジエン・インコーポレーテツド | 置換ビフェニルｇｐｒ４０調節因子 |
| US8716283B2 (en) | 2007-11-07 | 2014-05-06 | University Of Massachusetts | Type III secretion inhibitors, analogs and uses thereof |
| EP2260017A1 (en) | 2008-03-06 | 2010-12-15 | Amgen, Inc | Conformationally constrained carboxylic acid derivatives useful for treating metabolic disorders |
| EP2358656B1 (en) | 2008-10-15 | 2014-01-01 | Amgen, Inc | Spirocyclic gpr40 modulators |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2011140296A1 (en) | 2010-05-05 | 2011-11-10 | Infinity Pharmaceuticals | Triazoles as inhibitors of fatty acid synthase |
| EP2566853B1 (en) | 2010-05-05 | 2017-01-25 | Infinity Pharmaceuticals, Inc. | Tetrazolones as inhibitors of fatty acid synthase |
| WO2011157827A1 (de) | 2010-06-18 | 2011-12-22 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
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| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| KR101898610B1 (ko) | 2010-08-31 | 2018-09-14 | 서울대학교산학협력단 | ＰＰＡＲδ 활성물질의 태자 재프로그래밍 용도 |
| EP2683700B1 (de) | 2011-03-08 | 2015-02-18 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683699B1 (de) | 2011-03-08 | 2015-06-24 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683705B1 (de) | 2011-03-08 | 2015-04-22 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| WO2012120053A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| WO2012120052A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
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| EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| CN105142621A (zh) | 2012-10-24 | 2015-12-09 | 国家健康科学研究所 | 用于预防或治疗糖尿病和促进β-细胞存活的TPL2激酶抑制剂 |
| US9957219B2 (en) | 2013-12-04 | 2018-05-01 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| WO2015119899A1 (en) | 2014-02-06 | 2015-08-13 | Merck Sharp & Dohme Corp. | Antidiabetic compounds |
| ES2805743T3 (es) | 2015-03-24 | 2021-02-15 | Inst Nat Sante Rech Med | Método y composición farmacéutica para uso en el tratamiento de la diabetes |
| AU2019222644B2 (en) | 2018-02-13 | 2021-04-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
| KR102591947B1 (ko) | 2018-04-19 | 2023-10-25 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| BR112020026746A2 (pt) | 2018-07-13 | 2021-03-30 | Gilead Sciences, Inc. | Composto, composição farmacêutica, métodos para inibir pd-1, pd-l1 e/ou a interação de pd-1/pd-l1 e para tratar câncer, e, kit para tratar ou prevenir câncer ou uma doença ou condição. |
| KR102635333B1 (ko) | 2018-10-24 | 2024-02-15 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
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-
2006
- 2006-05-11 DE DE102006021878A patent/DE102006021878A1/de not_active Withdrawn
-
2007
- 2007-04-30 JP JP2009508193A patent/JP2009536629A/ja active Pending
- 2007-04-30 SI SI200731028T patent/SI2024347T1/sl unknown
- 2007-04-30 RU RU2008148838/04A patent/RU2434003C2/ru not_active IP Right Cessation
- 2007-04-30 MX MX2008014102A patent/MX2008014102A/es active IP Right Grant
- 2007-04-30 AU AU2007250213A patent/AU2007250213B2/en not_active Expired - Fee Related
- 2007-04-30 NZ NZ572692A patent/NZ572692A/en not_active IP Right Cessation
- 2007-04-30 RS RS20120395A patent/RS52450B/en unknown
- 2007-04-30 EP EP07724733A patent/EP2024347B1/de active Active
- 2007-04-30 MY MYPI20084472A patent/MY148258A/en unknown
- 2007-04-30 WO PCT/EP2007/003806 patent/WO2007131622A1/de active Application Filing
- 2007-04-30 BR BRPI0711448-6A patent/BRPI0711448A2/pt not_active IP Right Cessation
- 2007-04-30 CN CN2007800162659A patent/CN101437805B/zh not_active Expired - Fee Related
- 2007-04-30 PT PT07724733T patent/PT2024347E/pt unknown
- 2007-04-30 CA CA002651660A patent/CA2651660A1/en not_active Abandoned
- 2007-04-30 PL PL07724733T patent/PL2024347T3/pl unknown
- 2007-04-30 DK DK07724733.6T patent/DK2024347T3/da active
- 2007-04-30 KR KR1020087027644A patent/KR20090006846A/ko not_active Application Discontinuation
- 2007-04-30 ES ES07724733T patent/ES2391203T3/es active Active
- 2007-05-09 AR ARP070102008A patent/AR060990A1/es not_active Application Discontinuation
- 2007-05-09 TW TW096116362A patent/TW200812987A/zh unknown
- 2007-05-10 UY UY30338A patent/UY30338A1/es not_active Application Discontinuation
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2008
- 2008-10-06 ZA ZA200808490A patent/ZA200808490B/xx unknown
- 2008-10-30 CO CO08116211A patent/CO6241107A2/es not_active Application Discontinuation
- 2008-11-05 MA MA31362A patent/MA30402B1/fr unknown
- 2008-11-09 IL IL195179A patent/IL195179A0/en unknown
- 2008-11-10 US US12/267,896 patent/US20090149519A1/en not_active Abandoned
- 2008-12-04 NO NO20085068A patent/NO20085068L/no not_active Application Discontinuation
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2009
- 2009-10-28 HK HK09110016.0A patent/HK1131978A1/xx not_active IP Right Cessation
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2012
- 2012-10-12 CY CY20121100941T patent/CY1113177T1/el unknown
- 2012-10-15 HR HRP20120829TT patent/HRP20120829T1/hr unknown
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2013
- 2013-07-10 US US13/938,627 patent/US8748465B2/en not_active Expired - Fee Related
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