JP2006517199A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2006517199A5 JP2006517199A5 JP2006500009A JP2006500009A JP2006517199A5 JP 2006517199 A5 JP2006517199 A5 JP 2006517199A5 JP 2006500009 A JP2006500009 A JP 2006500009A JP 2006500009 A JP2006500009 A JP 2006500009A JP 2006517199 A5 JP2006517199 A5 JP 2006517199A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- hydrogen
- aralkyl
- heteroaralkyl
- alkyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims description 113
- 239000001257 hydrogen Substances 0.000 claims description 113
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 76
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 74
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 74
- 125000003118 aryl group Chemical group 0.000 claims description 67
- 150000002431 hydrogen Chemical class 0.000 claims description 57
- 125000001072 heteroaryl group Chemical group 0.000 claims description 51
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 50
- 125000000217 alkyl group Chemical group 0.000 claims description 47
- 150000001875 compounds Chemical class 0.000 claims description 46
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 33
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 29
- 229910052757 nitrogen Inorganic materials 0.000 claims description 27
- 150000003839 salts Chemical class 0.000 claims description 25
- 229910052799 carbon Inorganic materials 0.000 claims description 23
- 125000005843 halogen group Chemical group 0.000 claims description 22
- 125000001589 carboacyl group Chemical group 0.000 claims description 19
- 125000003545 alkoxy group Chemical group 0.000 claims description 18
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 14
- 229910052760 oxygen Inorganic materials 0.000 claims description 14
- 239000001301 oxygen Substances 0.000 claims description 14
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 13
- 239000011593 sulfur Chemical group 0.000 claims description 13
- 229910052717 sulfur Chemical group 0.000 claims description 13
- 125000000623 heterocyclic group Chemical group 0.000 claims description 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 10
- 230000000694 effects Effects 0.000 claims description 8
- 238000011282 treatment Methods 0.000 claims description 8
- 125000002947 alkylene group Chemical group 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 150000001408 amides Chemical class 0.000 claims description 5
- 125000003368 amide group Chemical group 0.000 claims description 4
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims description 3
- 125000002619 bicyclic group Chemical group 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 125000003435 aroyl group Chemical group 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 35
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 18
- 150000001721 carbon Chemical group 0.000 claims 16
- 241000124008 Mammalia Species 0.000 claims 10
- 238000000034 method Methods 0.000 claims 9
- -1 1-adamantyl Chemical group 0.000 claims 7
- 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 6
- 102000008645 11-beta-Hydroxysteroid Dehydrogenase Type 1 Human genes 0.000 claims 5
- 108010088011 11-beta-Hydroxysteroid Dehydrogenase Type 1 Proteins 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 208000004611 Abdominal Obesity Diseases 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 206010065941 Central obesity Diseases 0.000 claims 3
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 3
- 208000002705 Glucose Intolerance Diseases 0.000 claims 3
- 239000003862 glucocorticoid Substances 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 201000009104 prediabetes syndrome Diseases 0.000 claims 3
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 2
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims 2
- 229940123208 Biguanide Drugs 0.000 claims 2
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 2
- 229920001268 Cholestyramine Polymers 0.000 claims 2
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 2
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 claims 2
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 206010022489 Insulin Resistance Diseases 0.000 claims 2
- 229940122199 Insulin secretagogue Drugs 0.000 claims 2
- 229940122355 Insulin sensitizer Drugs 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 102000018692 Sulfonylurea Receptors Human genes 0.000 claims 2
- 108010091821 Sulfonylurea Receptors Proteins 0.000 claims 2
- 229960001138 acetylsalicylic acid Drugs 0.000 claims 2
- 210000000577 adipose tissue Anatomy 0.000 claims 2
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 2
- 239000000883 anti-obesity agent Substances 0.000 claims 2
- 239000003524 antilipemic agent Substances 0.000 claims 2
- 229940125710 antiobesity agent Drugs 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 229940125753 fibrate Drugs 0.000 claims 2
- 230000002440 hepatic effect Effects 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 239000004026 insulin derivative Substances 0.000 claims 2
- 230000002473 insulinotropic effect Effects 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 229960003512 nicotinic acid Drugs 0.000 claims 2
- 235000001968 nicotinic acid Nutrition 0.000 claims 2
- 239000011664 nicotinic acid Substances 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- NENLYAQPNATJSU-UHFFFAOYSA-N 1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline Chemical class C1NCCC2CCCCC21 NENLYAQPNATJSU-UHFFFAOYSA-N 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 201000010390 abdominal obesity-metabolic syndrome 1 Diseases 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000005110 aryl thio group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 1
- 125000004856 decahydroquinolinyl group Chemical class N1(CCCC2CCCCC12)* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 235000021588 free fatty acids Nutrition 0.000 claims 1
- 230000004110 gluconeogenesis Effects 0.000 claims 1
- 125000004470 heterocyclooxy group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 230000004130 lipolysis Effects 0.000 claims 1
- 208000011661 metabolic syndrome X Diseases 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 9
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 9
- 0 CC(C(C)=C(**1)C(N(*)*)=O)=C1C=C Chemical compound CC(C(C)=C(**1)C(N(*)*)=O)=C1C=C 0.000 description 8
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 7
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 6
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 4
- 125000004432 carbon atom Chemical group C* 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- GIDDWUIWEVRLPQ-UHFFFAOYSA-N 4-methoxycarbonylnaphthalene-1-carboxylic acid Chemical compound C1=CC=C2C(C(=O)OC)=CC=C(C(O)=O)C2=C1 GIDDWUIWEVRLPQ-UHFFFAOYSA-N 0.000 description 3
- 235000019439 ethyl acetate Nutrition 0.000 description 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- FUFLCEKSBBHCMO-KJQYFISQSA-N 11-dehydrocorticosterone Chemical compound O=C1CC[C@]2(C)[C@H]3C(=O)C[C@](C)([C@H](CC4)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 FUFLCEKSBBHCMO-KJQYFISQSA-N 0.000 description 2
- FUFLCEKSBBHCMO-UHFFFAOYSA-N 11-dehydrocorticosterone Natural products O=C1CCC2(C)C3C(=O)CC(C)(C(CC4)C(=O)CO)C4C3CCC2=C1 FUFLCEKSBBHCMO-UHFFFAOYSA-N 0.000 description 2
- CEOCVKWBUWKBKA-UHFFFAOYSA-N 2,4-dichlorobenzoyl chloride Chemical compound ClC(=O)C1=CC=C(Cl)C=C1Cl CEOCVKWBUWKBKA-UHFFFAOYSA-N 0.000 description 2
- BBRVEUKQSXUATK-UHFFFAOYSA-N 2h-quinoline-1-carbaldehyde Chemical compound C1=CC=C2N(C=O)CC=CC2=C1 BBRVEUKQSXUATK-UHFFFAOYSA-N 0.000 description 2
- VHYFNPMBLIVWCW-UHFFFAOYSA-N 4-Dimethylaminopyridine Chemical compound CN(C)C1=CC=NC=C1 VHYFNPMBLIVWCW-UHFFFAOYSA-N 0.000 description 2
- UKWUOTZGXIZAJC-UHFFFAOYSA-N 4-nitrosalicylic acid Chemical compound OC(=O)C1=CC=C([N+]([O-])=O)C=C1O UKWUOTZGXIZAJC-UHFFFAOYSA-N 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 2
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 239000010410 layer Substances 0.000 description 2
- 239000002609 medium Substances 0.000 description 2
- 239000012074 organic phase Substances 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 2
- 239000011541 reaction mixture Substances 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- NGNBDVOYPDDBFK-UHFFFAOYSA-N 2-[2,4-di(pentan-2-yl)phenoxy]acetyl chloride Chemical compound CCCC(C)C1=CC=C(OCC(Cl)=O)C(C(C)CCC)=C1 NGNBDVOYPDDBFK-UHFFFAOYSA-N 0.000 description 1
- KPJXEWJRJKEOCD-UHFFFAOYSA-N 2-methoxy-4-nitrobenzoic acid Chemical compound COC1=CC([N+]([O-])=O)=CC=C1C(O)=O KPJXEWJRJKEOCD-UHFFFAOYSA-N 0.000 description 1
- 229960000549 4-dimethylaminophenol Drugs 0.000 description 1
- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 description 1
- WJSAQQLOLUNFKE-IJSCHUJVSA-N CCCNC(/C=C/C=C(\C(C)(C)COC)/N[C@@](C)([C@H](C)CCl)O)O Chemical compound CCCNC(/C=C/C=C(\C(C)(C)COC)/N[C@@](C)([C@H](C)CCl)O)O WJSAQQLOLUNFKE-IJSCHUJVSA-N 0.000 description 1
- OMFXVFTZEKFJBZ-UHFFFAOYSA-N Corticosterone Natural products O=C1CCC2(C)C3C(O)CC(C)(C(CC4)C(=O)CO)C4C3CCC2=C1 OMFXVFTZEKFJBZ-UHFFFAOYSA-N 0.000 description 1
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical class [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 229960000583 acetic acid Drugs 0.000 description 1
- 150000003927 aminopyridines Chemical class 0.000 description 1
- 239000000908 ammonium hydroxide Substances 0.000 description 1
- 239000000538 analytical sample Substances 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- WORJEOGGNQDSOE-UHFFFAOYSA-N chloroform;methanol Chemical compound OC.ClC(Cl)Cl WORJEOGGNQDSOE-UHFFFAOYSA-N 0.000 description 1
- OMFXVFTZEKFJBZ-HJTSIMOOSA-N corticosterone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@H](CC4)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OMFXVFTZEKFJBZ-HJTSIMOOSA-N 0.000 description 1
- UKJLNMAFNRKWGR-UHFFFAOYSA-N cyclohexatrienamine Chemical group NC1=CC=C=C[CH]1 UKJLNMAFNRKWGR-UHFFFAOYSA-N 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 238000003818 flash chromatography Methods 0.000 description 1
- 239000012362 glacial acetic acid Substances 0.000 description 1
- 239000001963 growth medium Substances 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 239000005457 ice water Substances 0.000 description 1
- 238000003384 imaging method Methods 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000012044 organic layer Substances 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 239000002953 phosphate buffered saline Substances 0.000 description 1
- 238000007747 plating Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 238000003828 vacuum filtration Methods 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US44253203P | 2003-01-24 | 2003-01-24 | |
| PCT/EP2004/000571 WO2004065351A1 (en) | 2003-01-24 | 2004-01-23 | Amide derivatives and their use as inhibitors of 11-beta-hydroxysteroid dehydrogenase type 1 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006517199A JP2006517199A (ja) | 2006-07-20 |
| JP2006517199A5 true JP2006517199A5 (OSRAM) | 2007-03-08 |
Family
ID=32772048
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006500009A Pending JP2006517199A (ja) | 2003-01-24 | 2004-01-23 | アミド誘導体およびそれらの１１−ベータ−ヒドロキシステロイドデヒドロゲナーゼ・タイプ１の阻害剤としての使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20060205772A1 (OSRAM) |
| EP (1) | EP1590319A1 (OSRAM) |
| JP (1) | JP2006517199A (OSRAM) |
| CN (1) | CN100586927C (OSRAM) |
| AR (1) | AR043355A1 (OSRAM) |
| BR (1) | BRPI0406938A (OSRAM) |
| CA (1) | CA2513349A1 (OSRAM) |
| PE (1) | PE20041040A1 (OSRAM) |
| TW (1) | TW200503994A (OSRAM) |
| WO (1) | WO2004065351A1 (OSRAM) |
Families Citing this family (148)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602004027171D1 (de) * | 2003-04-11 | 2010-06-24 | High Point Pharmaceuticals Llc | Verbindungen mit Aktivität an der 11Beta-Hydroxasteroiddehydrogenase |
| CN1822820A (zh) * | 2003-07-28 | 2006-08-23 | 雷迪实验室有限公司 | 心血管疾病的治疗和预防 |
| DE602004018338D1 (de) | 2003-09-22 | 2009-01-22 | Onepharm Res And Dev Gmbh | Prävention und behandlung von durch entzündung ausgelöstem und/oder immunvermitteltem knochenschwund |
| DE602005009530D1 (de) | 2004-01-09 | 2008-10-16 | Corcept Therapeutics Inc | Azadecalinmodulatoren des glucocorticoidrezeptors |
| US7880001B2 (en) | 2004-04-29 | 2011-02-01 | Abbott Laboratories | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme |
| US20100222316A1 (en) | 2004-04-29 | 2010-09-02 | Abbott Laboratories | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme |
| US8415354B2 (en) | 2004-04-29 | 2013-04-09 | Abbott Laboratories | Methods of use of inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme |
| TWI350168B (en) | 2004-05-07 | 2011-10-11 | Incyte Corp | Amido compounds and their use as pharmaceuticals |
| NZ551077A (en) | 2004-05-07 | 2009-05-31 | Janssen Pharmaceutica Nv | Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors |
| SI1753512T1 (sl) | 2004-05-28 | 2008-12-31 | 4Sc Ag | Tetrahidropiridotiofeni |
| AU2005251485A1 (en) | 2004-06-11 | 2005-12-22 | 4Sc Ag | Tetrahydropyridothiophenes for treating hyperproliferative disorders |
| US8071624B2 (en) | 2004-06-24 | 2011-12-06 | Incyte Corporation | N-substituted piperidines and their use as pharmaceuticals |
| US7572805B2 (en) | 2004-07-14 | 2009-08-11 | Bristol-Myers Squibb Company | Pyrrolo(oxo)isoquinolines as 5HT ligands |
| US7618980B2 (en) | 2004-07-14 | 2009-11-17 | Bristol-Myers Squibb Company | Pyrrolo(oxo)quinolines as 5HT ligands |
| DE602005017159D1 (de) | 2004-08-30 | 2009-11-26 | Janssen Pharmaceutica Nv | Oxysteroid-dehydrogenase-inhibitoren |
| CN101039908B (zh) * | 2004-08-30 | 2010-06-23 | 詹森药业有限公司 | 作为11-β羟甾类脱氢酶抑制剂的三环内酰胺衍生物 |
| KR101197674B1 (ko) | 2004-08-30 | 2012-11-07 | 얀센 파마슈티카 엔.브이. | １１-베타 하이드록시스테로이드 탈수소효소 저해제로서의 ｎ-2 아다만타닐-２-페녹시-아세트아미드 유도체 |
| CN101035762B (zh) * | 2004-10-04 | 2010-09-29 | 霍夫曼-拉罗奇有限公司 | 用于糖尿病的作为11-β抑制剂的烷基(alkil)-吡啶类 |
| US8110581B2 (en) | 2004-11-10 | 2012-02-07 | Incyte Corporation | Lactam compounds and their use as pharmaceuticals |
| AU2006203918B2 (en) | 2005-01-05 | 2011-05-19 | Abbvie Inc. | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme |
| US8198331B2 (en) | 2005-01-05 | 2012-06-12 | Abbott Laboratories | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme |
| US20090192198A1 (en) | 2005-01-05 | 2009-07-30 | Abbott Laboratories | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme |
| CA2594098C (en) | 2005-01-05 | 2014-04-01 | Abbott Laboratories | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme |
| WO2006084869A1 (en) | 2005-02-09 | 2006-08-17 | Nycomed Gmbh | Tetrahydropyridothiophenes for the treatment of proliferative diseases such as cancer |
| US7741488B2 (en) | 2005-02-11 | 2010-06-22 | 4Sc Ag | Tetrahydropyridothiophenes as antiproliferative agents for the treatment of cancer |
| JP5140577B2 (ja) * | 2005-03-31 | 2013-02-06 | タケダ カリフォルニア インコーポレイテッド | ヒドロキシステロイドデヒドロゲナーゼ阻害剤 |
| BRPI0610459A2 (pt) | 2005-04-05 | 2010-06-22 | Hoffmann La Roche | composto, processo para a sua preparação, composições farmacêuticas que o compreendem, método para o tratamento terapêutico e/ou profilático de enfermidades que são moduladas por inibidores de deidrogenase de hidroxiesteróides-11b e utilização do composto |
| EP2527337A1 (en) * | 2005-04-14 | 2012-11-28 | Bristol-Myers Squibb Company | Inhibitors of 11-beta hydroxysteroid dehydrogenase type I |
| CA2609004A1 (en) | 2005-05-25 | 2006-11-30 | Nycomed Gmbh | Tetrahydropyridothiophenes for use in the treatment of cancer |
| AU2006251167A1 (en) | 2005-05-25 | 2006-11-30 | 4Sc Ag | Tetrahydropyridothiophenes for use in the treatment of cancer |
| US8952176B2 (en) | 2005-06-07 | 2015-02-10 | Shionogi & Co., Ltd. | Heterocyclic compound having type I 11 β hydroxysteroid dehydrogenase inhibitory activity |
| US7579360B2 (en) * | 2005-06-09 | 2009-08-25 | Bristol-Myers Squibb Company | Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| US7572807B2 (en) | 2005-06-09 | 2009-08-11 | Bristol-Myers Squibb Company | Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors |
| US7605289B2 (en) | 2005-06-17 | 2009-10-20 | Amgen, Inc. | Benzamide derivatives and uses related thereto |
| EP1904455B1 (en) | 2005-07-05 | 2011-08-17 | F. Hoffmann-La Roche AG | Pyridazine derivatives |
| AU2006272922A1 (en) | 2005-07-22 | 2007-02-01 | Amgen Inc. | Aniline sulfonamide derivatives and their uses |
| US20100152188A1 (en) * | 2005-08-05 | 2010-06-17 | Akella Satya Surya Visweswara Srinivas | Novel Heterocyclic Compounds |
| US7622492B2 (en) | 2005-08-31 | 2009-11-24 | Hoffmann-La Roche Inc. | Pyrazolones as inhibitors of 11β-hydroxysteroid dehydrogenase |
| CA2621255A1 (en) * | 2005-09-21 | 2007-04-05 | Incyte Corporation | Amido compounds and their use as pharmaceuticals |
| GB0521716D0 (en) * | 2005-10-25 | 2005-11-30 | Genomica Sau | Modulation of 11beta-hydroxysteriod dehydrogenase 1 expression for the treatment of ocular diseases |
| US20090124598A1 (en) * | 2005-11-01 | 2009-05-14 | Henrik Sune Andersen | Pharmaceutical use of substituted amides |
| US20070116756A1 (en) * | 2005-11-23 | 2007-05-24 | Dr. Reddy's Laboratories Limited | Stable pharmaceutical compositions |
| WO2007067504A2 (en) | 2005-12-05 | 2007-06-14 | Incyte Corporation | Lactam compounds and methods of using the same |
| EP1801098A1 (en) | 2005-12-16 | 2007-06-27 | Merck Sante | 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors |
| WO2007084314A2 (en) | 2006-01-12 | 2007-07-26 | Incyte Corporation | MODULATORS OF 11-ß HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME |
| AU2007207055B2 (en) | 2006-01-18 | 2011-06-02 | F. Hoffmann-La Roche Ag | Thiazoles as 11 beta-HSD1 inhibitors |
| EP1981848A2 (en) | 2006-02-07 | 2008-10-22 | Wyeth | 11-beta hsd1 inhibitors |
| RU2407740C2 (ru) * | 2006-02-13 | 2010-12-27 | Ф.Хоффманн-Ля Рош Аг | Гетеробициклические сульфонамидные производные для лечения диабета |
| JP5240775B2 (ja) | 2006-03-30 | 2013-07-17 | 塩野義製薬株式会社 | Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有するイソキサゾール誘導体およびイソチアゾール誘導体 |
| EP2013163A1 (en) | 2006-05-01 | 2009-01-14 | Incyte Corporation | Tetrasubstituted ureas as modulators of 11-beta hydroxyl steroid dehydrogenase type 1 |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| EP2018378A2 (en) | 2006-05-17 | 2009-01-28 | Incyte Corporation | Heterocyclic inhibitors of 11-b hydroxyl steroid dehydrogenase type i and methods of using the same |
| TW200808695A (en) * | 2006-06-08 | 2008-02-16 | Amgen Inc | Benzamide derivatives and uses related thereto |
| DE602007008237D1 (de) * | 2006-06-08 | 2010-09-16 | Amgen Inc | Benzamidderivate und assoziierte verwendungen |
| MX2008016426A (es) | 2006-07-05 | 2009-01-19 | Hoffmann La Roche | Derivados de alquilpiridazina como inhibidores de 11 beta hidroxiesteroide deshidrogenasa tipo 1(11b-hsd 1). |
| AU2007283113A1 (en) | 2006-08-08 | 2008-02-14 | Sanofi-Aventis | Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, processes for preparing them, medicaments comprising these compounds, and their use |
| US7727978B2 (en) | 2006-08-24 | 2010-06-01 | Bristol-Myers Squibb Company | Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| TW200827346A (en) * | 2006-11-03 | 2008-07-01 | Astrazeneca Ab | Chemical compounds |
| DE102006058207A1 (de) * | 2006-12-11 | 2008-06-19 | Universitätsklinikum Schleswig-Holstein | Verfahren zur Herstellung spezifischer Inhibitoren der 11beta-Hydroxysteroid-Dehydrogenase Typ 1 mit Nor-Oleanan- oder Nor-Ursan-Grundgerüsten |
| EP1935420A1 (en) | 2006-12-21 | 2008-06-25 | Merck Sante | 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors |
| ES2627221T3 (es) | 2006-12-28 | 2017-07-27 | Rigel Pharmaceuticals, Inc. | Compuestos de heterocicloalquiloxibenzamida N-sustituidos y métodos de uso |
| DE102007005045B4 (de) | 2007-01-26 | 2008-12-18 | Sanofi-Aventis | Phenothiazin Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| TW200836719A (en) | 2007-02-12 | 2008-09-16 | Astrazeneca Ab | Chemical compounds |
| CA2675669C (en) * | 2007-02-23 | 2015-05-26 | High Point Pharmaceuticals, Llc | Novel compounds |
| CN101686680B (zh) | 2007-03-09 | 2015-12-09 | 伊沃泰克美国股份有限公司 | 作为p2x7调节剂的双环杂芳基化合物及其用途 |
| RU2342361C1 (ru) * | 2007-04-16 | 2008-12-27 | Государственное образовательное учреждение высшего профессионального образования "Пермская государственная фармацевтическая академия Федерального агентства по здравоохранению и социальному развитию" (ГОУ ВПО ПГФА Росздрава) | Метиламид и бензиламид n-ацетил-3,5-дибромантраниловой кислоты, проявляющие противовоспалительную и анальгетическую активности |
| CL2008001839A1 (es) | 2007-06-21 | 2009-01-16 | Incyte Holdings Corp | Compuestos derivados de 2,7-diazaespirociclos, inhibidores de 11-beta hidroxil esteroide deshidrogenasa tipo 1; composicion farmaceutica que comprende a dichos compuestos; utiles para tratar la obesidad, diabetes, intolerancia a la glucosa, diabetes tipo ii, entre otras enfermedades. |
| JP2009035513A (ja) * | 2007-08-02 | 2009-02-19 | Ube Ind Ltd | ４−ｎ−（メチルベンゾイル）アミノ−２−メチル安息香酸の製法 |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| JP5736098B2 (ja) | 2007-08-21 | 2015-06-17 | アッヴィ・インコーポレイテッド | 中枢神経系障害を治療するための医薬組成物 |
| US8119658B2 (en) | 2007-10-01 | 2012-02-21 | Bristol-Myers Squibb Company | Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| US8304539B2 (en) * | 2008-02-07 | 2012-11-06 | Bristol-Myers Squibb Company | Fused heteroaryl modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof |
| EP2276761B1 (en) | 2008-04-23 | 2015-07-29 | Rigel Pharmaceuticals, Inc. | Carboxamide compounds for the treatment of metabolic disorders |
| UY31968A (es) | 2008-07-09 | 2010-01-29 | Sanofi Aventis | Nuevos derivados heterocíclicos, sus procesos para su preparación, y sus usos terapéuticos |
| GB0815784D0 (en) | 2008-08-29 | 2008-10-08 | Xention Ltd | Novel potassium channel blockers |
| GB0815781D0 (en) | 2008-08-29 | 2008-10-08 | Xention Ltd | Novel potassium channel blockers |
| GB0815782D0 (en) | 2008-08-29 | 2008-10-08 | Xention Ltd | Novel potassium channel blockers |
| MX2011004258A (es) | 2008-10-22 | 2011-06-01 | Merck Sharp & Dohme | Derivados de bencimidazol ciclicos novedosos utiles como agentes anti-diabeticos. |
| JP5645834B2 (ja) | 2008-10-23 | 2014-12-24 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | 嚢胞性線維症膜コンダクタンス制御因子の修飾因子 |
| AR074060A1 (es) | 2008-10-23 | 2010-12-22 | Vertex Pharma | Moduladores del regulador de conductancia transmembrana de la fibrosis quistica |
| CA2741672A1 (en) | 2008-10-31 | 2010-05-06 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| EA020496B1 (ru) | 2008-11-21 | 2014-11-28 | ХАЙ ПОЙНТ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Производное адамантилбензамида, фармацевтическая композиция, включающая его, и его применение |
| WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
| TW201028421A (en) * | 2009-01-15 | 2010-08-01 | Abbott Lab | Novel benzenesulfonamides as calcium channel blockers |
| JP5658688B2 (ja) * | 2009-01-28 | 2015-01-28 | ライジェル ファーマシューティカルズ， インコーポレイテッド | カルボキサミド化合物およびその使用方法 |
| GB0909672D0 (en) | 2009-06-04 | 2009-07-22 | Xention Discovery Ltd | Compounds |
| ES2350077B1 (es) | 2009-06-04 | 2011-11-04 | Laboratorios Salvat, S.A. | Compuestos inhibidores de 11beta-hidroxiesteroide deshidrogenasa de tipo 1. |
| GB0909671D0 (en) | 2009-06-04 | 2009-07-22 | Xention Discovery Ltd | Compounds |
| BR112012003973A2 (pt) | 2009-08-26 | 2015-09-08 | Sanofi Sa | hidratos de fluoroglicosídeo heteroaromático cristalinos, produtos farmacêuticos compreendendo estes compostos e seu uso |
| CA2786314A1 (en) | 2010-02-25 | 2011-09-01 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| US8933024B2 (en) | 2010-06-18 | 2015-01-13 | Sanofi | Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases |
| 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 |
| 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 |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process 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 |
| WO2012015715A1 (en) | 2010-07-27 | 2012-02-02 | High Point Pharmaceuticals, Llc | Substituted thiazol-2-ylamine derivatives, pharmaceutical compositions, and methods of use as 11-beta hsd1 modulators |
| SG192941A1 (en) | 2011-02-25 | 2013-09-30 | Merck Sharp & Dohme | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
| 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 |
| EP2683701B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8809325B2 (en) | 2011-03-08 | 2014-08-19 | Sanofi | Benzyl-oxathiazine derivatives substituted with adamantane and noradamantane, medicaments containing said compounds and use thereof |
| 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 |
| WO2012120056A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| WO2012120050A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende 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 |
| US8895547B2 (en) | 2011-03-08 | 2014-11-25 | Sanofi | Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof |
| US8710050B2 (en) | 2011-03-08 | 2014-04-29 | Sanofi | Di and tri- substituted oxathiazine derivatives, method for the production, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| WO2012124744A1 (ja) * | 2011-03-14 | 2012-09-20 | 大正製薬株式会社 | 含窒素縮合複素環化合物 |
| KR101332805B1 (ko) | 2011-03-31 | 2013-11-27 | 한국화학연구원 | 아다만틸기를 갖는 설파마이드 유도체 및 이의 약제학적으로 허용 가능한 염 |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| CN106957282B (zh) * | 2011-12-21 | 2019-08-30 | 诺维拉治疗公司 | B型肝炎抗病毒剂 |
| WO2013147026A1 (ja) | 2012-03-29 | 2013-10-03 | 武田薬品工業株式会社 | 芳香環化合物 |
| KR20150036245A (ko) | 2012-08-02 | 2015-04-07 | 머크 샤프 앤드 돔 코포레이션 | 항당뇨병 트리시클릭 화합물 |
| MX2015010935A (es) | 2013-02-22 | 2015-10-29 | Merck Sharp & Dohme | Compuestos biciclicos antidiabeticos. |
| EP2970119B1 (en) | 2013-03-14 | 2021-11-03 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| CA2929194A1 (en) * | 2013-11-05 | 2015-05-14 | F. Hoffmann-La Roche Ag | 5,6,7,8-tetrahydro-5,8-methanocinnoline derivatives as rorc modulators for the treatment of autoimmune diseases |
| US10047082B2 (en) | 2013-11-25 | 2018-08-14 | Corcept Therapeutics, Inc. | Octahydro fused azadecalin glucocorticoid receptor modulators |
| UA121309C2 (uk) | 2014-02-03 | 2020-05-12 | Вітае Фармасьютікалс, Ллс | Дигідропіролопіридинові інгібітори ror-гамма |
| US9255096B1 (en) | 2014-10-07 | 2016-02-09 | Allergan, Inc. | Substituted 1,2,3,4-tetrahydrobenzo[C][2,7] naphthyridines and derivatives thereof as kinase inhibitors |
| BR112017007460A2 (pt) | 2014-10-14 | 2017-12-19 | Vitae Pharmaceuticals Inc | inibidores de di-hidropirrolopiridina de ror-gama |
| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline inhibitors of ROR-gamma |
| GB2532990A (en) | 2014-12-05 | 2016-06-08 | Schlumberger Holdings | Corrosion inhibition |
| WO2016095205A1 (en) | 2014-12-19 | 2016-06-23 | Merck Sharp & Dohme Corp. | Heteroaryl orexin receptor antagonists |
| ES2856931T3 (es) | 2015-08-05 | 2021-09-28 | Vitae Pharmaceuticals Llc | Moduladores de ROR-gamma |
| GB2543498A (en) * | 2015-10-19 | 2017-04-26 | Schlumberger Holdings | Corrosion inhibition |
| MX385332B (es) | 2015-11-20 | 2025-03-18 | Vitae Pharmaceuticals Llc | Moduladores de ror-gamma. |
| TW202220968A (zh) | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ＲＯＲ－γ調節劑 |
| US9481674B1 (en) | 2016-06-10 | 2016-11-01 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| AU2017281222B2 (en) | 2016-06-23 | 2022-06-16 | The Usa As Represented By The Department Of Veterans Affairs; Dept. Of Veterans Affairs Office Of General Counsel - Pag Iv (024) | Non-catalytic substrate-selective P38α-specific MAPK inhibitors with endothelial-stabilizing and anti-inflammatory activity, and methods of use thereof |
| EP3508474B1 (en) * | 2016-08-31 | 2023-05-17 | JCR Pharmaceuticals Co., Ltd. | Novel therapeutic agent for diabetes |
| EP3551176A4 (en) | 2016-12-06 | 2020-06-24 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| EP3558298A4 (en) | 2016-12-20 | 2020-08-05 | Merck Sharp & Dohme Corp. | ANTIDIABETIC SPIROCHROMAN COMPOUNDS |
| RU2771166C2 (ru) | 2016-12-21 | 2022-04-27 | Биотерикс, Инк. | Производные тиенопиррола для применения для нацеливания на белки, композиции с указанными производными, способы и применения |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| CN111225914B (zh) | 2017-07-24 | 2022-10-11 | 生命医药有限责任公司 | RORγ的抑制剂 |
| ES3025468T3 (en) | 2018-12-07 | 2025-06-09 | Univ Maryland | Non-atp/catalytic site p38 mitogen activated protein kinase inhibitors |
| WO2020132046A1 (en) | 2018-12-19 | 2020-06-25 | Corcept Therapeutics Incorporated | Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent |
| US11234971B2 (en) | 2018-12-19 | 2022-02-01 | Corcept Therapeutics Incorporated | Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent |
| CN113490496A (zh) | 2019-02-22 | 2021-10-08 | 科赛普特治疗学股份有限公司 | 一种杂芳基-酮稠合氮杂萘烷糖皮质激素受体调节剂瑞拉可兰的治疗用途 |
| WO2021119432A1 (en) | 2019-12-11 | 2021-06-17 | Corcept Therapeutics Incorporated | Methods of treating antipsychotic-induced weight gain with miricorilant |
| KR20220152537A (ko) * | 2020-02-07 | 2022-11-16 | 싸이토키네틱스, 인코포레이티드 | Nampt 조절제 |
| EP4153303A1 (en) | 2020-05-18 | 2023-03-29 | GEN1E Lifesciences Inc. | P38alpha mitogen-activated protein kinase inhibitors |
| EP4237415A1 (en) | 2020-10-29 | 2023-09-06 | GEN1E Lifesciences Inc. | Crystalline 5-(dimethylamino)-n-(4-(morpholinomethyl)phenyl) naphthalene-1-sulfonamide di-hydrochloride di-hydrate |
| WO2022204046A1 (en) | 2021-03-23 | 2022-09-29 | Gen1E Lifesciences Inc. | Substituted naphthyl p38alpha mitogen-activated protein kinase inhibitors |
| EP4608402A1 (en) | 2022-10-28 | 2025-09-03 | Corcept Therapeutics Incorporated | Treatments for amyotrophic lateral sclerosis using dazucorilant |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH242949A (de) * | 1942-12-11 | 1946-06-15 | Ag J R Geigy | Verfahren zur Herstellung von N-Cyclohexyl-6-pyridon-3-carbonsäurediäthylamid. |
| DE817911C (de) * | 1947-12-16 | 1951-10-22 | Chem Fab Tempelhof Preuss & Te | Verfahren zur Darstellung von in 6-Stellung basisch substituierten Pyridin-3-carbonsaeureamiden |
| US3646048A (en) * | 1970-02-02 | 1972-02-29 | American Cyanamid Co | N-(tert-aminoalkyl)-2-indenecarboxamides |
| US3963745A (en) * | 1972-04-03 | 1976-06-15 | A. H. Robins Company, Incorporated | Method for controlling emesis with N-(1-substituted-3-pyrrolidinyl)benzamides and thiobenzamides |
| DE2242007A1 (de) * | 1972-08-26 | 1974-03-14 | Basf Ag | Verfahren zur herstellung von phthalimidinen |
| GB1497536A (en) * | 1973-12-17 | 1978-01-12 | Lilly Industries Ltd | 2-acylaminooxazoles methods for their preparation and their use |
| FI750355A7 (OSRAM) * | 1974-02-19 | 1975-08-20 | Sandoz Ag | |
| GB1551735A (en) * | 1975-06-05 | 1979-09-12 | Lilly Industries Ltd | Acylated aminothiazoles and aminooxadiazoles |
| ZA775350B (en) * | 1976-12-23 | 1978-07-26 | Ciba Geigy Ag | Substituted 5-amino-2-pyridinecarboxylic acids |
| CA2116334A1 (en) * | 1992-07-02 | 1994-01-20 | Hidenori Ogawa | Oxytocin antagonist |
| GB9408185D0 (en) * | 1994-04-25 | 1994-06-15 | Fujisawa Pharmaceutical Co | New benzamide derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same |
| GB9511694D0 (en) * | 1995-06-09 | 1995-08-02 | Fujisawa Pharmaceutical Co | Benzamide derivatives |
| HRP20010804B1 (en) * | 1999-04-30 | 2006-05-31 | Pfizer Products Inc. | Glucocorticoid receptor modulators |
| SE0001899D0 (sv) * | 2000-05-22 | 2000-05-22 | Pharmacia & Upjohn Ab | New compounds |
| WO2003029199A1 (en) * | 2001-09-28 | 2003-04-10 | Takeda Chemical Industries, Ltd. | Benzene derivatives, process for preparing the same and use thereof |
| BR0213842A (pt) * | 2001-11-03 | 2004-08-31 | Astrazeneca Ab | Derivado de quinazolina ou um sal deste farmaceuticamente aceitável, processo para a preparação do mesmo, composição farmacêutica, e, uso do derivado de quinazolina ou de um sal deste farmaceuticamente aceitável |
| US7074788B2 (en) * | 2001-11-22 | 2006-07-11 | Biovitrum Ab | Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 |
| CA2478050A1 (en) * | 2002-03-01 | 2003-09-12 | Pfizer Inc. | Indolyl-urea derivatives of thienopyridines useful as anti-angiogenic agents |
-
2004
- 2004-01-20 TW TW093101445A patent/TW200503994A/zh unknown
- 2004-01-21 PE PE2004000085A patent/PE20041040A1/es not_active Application Discontinuation
- 2004-01-22 AR ARP040100172A patent/AR043355A1/es unknown
- 2004-01-23 WO PCT/EP2004/000571 patent/WO2004065351A1/en not_active Ceased
- 2004-01-23 JP JP2006500009A patent/JP2006517199A/ja active Pending
- 2004-01-23 EP EP04704554A patent/EP1590319A1/en not_active Withdrawn
- 2004-01-23 CN CN200480002540A patent/CN100586927C/zh not_active Expired - Fee Related
- 2004-01-23 CA CA002513349A patent/CA2513349A1/en not_active Abandoned
- 2004-01-23 US US10/542,759 patent/US20060205772A1/en not_active Abandoned
- 2004-01-23 BR BR0406938-2A patent/BRPI0406938A/pt not_active IP Right Cessation
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2006517199A5 (OSRAM) | ||
| GB2210368A (en) | 2-aryl substituted heterocyclic compounds as antiallergic and anti-inflammatory agents | |
| PL171933B1 (pl) | Sposób wytwarzania nowych amidów PL PL PL | |
| JPH0236163A (ja) | 新規なヒドロキサメート誘導体 | |
| IE861952L (en) | Pyrimidines | |
| HRP20020072A2 (en) | Carboxylic acid amides, medicaments containing these compounds and the use and production thereof | |
| BRPI0715872A2 (pt) | Composto; composição farmacêutica; método de preparação do composto; composto preparado pelo método; e método de tratamento de um transtorno em um mamífero necessitado | |
| CN116262736B (zh) | 新型氧代吡啶类化合物及其制备方法和用途 | |
| JP2016128465A (ja) | インダノン誘導体、その薬学的に許容される塩又は光学異性体、その調製方法及びそれを活性成分として含有するウイルス疾患の予防又は治療用の医薬組成物 | |
| AU2014224614A1 (en) | Novel sulfonamide TRPA1 receptor antagonists | |
| JPWO2016148114A1 (ja) | 酸化ストレス誘導神経細胞死抑制化合物 | |
| JP2004517100A (ja) | ｈＰＰＡＲアルファアゴニストとしての置換オキサゾールおよびチアゾール | |
| JP6143877B2 (ja) | ２−アリールセレナゾール化合物及びその薬剤組成物 | |
| CA2016665C (en) | Rhodanine derivatives and pharmaceutical compositions | |
| TW201843135A (zh) | 胺基-芳基-苯甲醯胺化合物及其使用方法 | |
| CA2451452C (en) | Cyclic diamine compound with condensed-ring groups | |
| US20070161697A1 (en) | Hydrazide type compounds and the use thereof in pharmaceutical compositions for the treatment of cardiovascular diseases | |
| JP3140494B2 (ja) | 置換されたフエニルアセチレン、これを含有する薬剤、この化合物及び薬剤を製造する方法 | |
| NO169648B (no) | Analogifremgangsmaate for fremstilling av terapeutisk aktive arakidonsyre-derivater | |
| CN109748914A (zh) | 吡啶并嘧啶类化合物及其应用 | |
| JP2018039733A (ja) | 新規複素環誘導体 | |
| EP0735029B1 (en) | Benzothiazole derivatives | |
| JP4823397B1 (ja) | フェナントレノン化合物、組成物および方法 | |
| US5310744A (en) | Quinolylmethoxyphenyl-acetamides | |
| WO2018223122A1 (en) | Hdac3-selective inhibitors |