JP2006517199A5 - - Google Patents
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- 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
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- 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 (https=) | 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 (https=) |
| EP (1) | EP1590319A1 (https=) |
| JP (1) | JP2006517199A (https=) |
| CN (1) | CN100586927C (https=) |
| AR (1) | AR043355A1 (https=) |
| BR (1) | BRPI0406938A (https=) |
| CA (1) | CA2513349A1 (https=) |
| PE (1) | PE20041040A1 (https=) |
| TW (1) | TW200503994A (https=) |
| WO (1) | WO2004065351A1 (https=) |
Families Citing this family (151)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE467616T1 (de) * | 2003-04-11 | 2010-05-15 | High Point Pharmaceuticals Llc | Verbindungen mit aktivität an der 11beta- hydroxasteroiddehydrogenase |
| NZ544784A (en) * | 2003-07-28 | 2009-11-27 | Reddys Lab Inc Dr | Treatment and prevention of cardiovascular events using a beta-adrenergic receptor antagonist, a diuretic, an inhibitor of HMG CoA reductase, an inhibitor of the rennin-angiotensin system and asprin; wherein acidic and basic components are separated. |
| SI1663185T1 (sl) | 2003-09-22 | 2009-04-30 | Onepharm Res & Dev Gmbh | Preprečevanje in zdravljenje z vnetjem inducirane in/ali imunsko posredovane izgube kosti |
| PT1761497E (pt) | 2004-01-09 | 2008-09-25 | Corcept Therapeutics Inc | Azadecalinas moduladoras do receptor de glucocorticóides |
| 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 |
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| JP7789561B2 (ja) | 2019-02-22 | 2025-12-22 | コーセプト セラピューティクス， インコーポレイテッド | レラコリラント、ヘテロアリール－ケトン縮合アザデカリングルココルチコイド受容体調節物質の治療用途 |
| JP7569492B2 (ja) | 2019-12-11 | 2024-10-18 | コーセプト セラピューティクス， インコーポレイテッド | 抗精神病薬誘発性体重増加のミリコリラントによる治療方法 |
| PH12022552021A1 (en) * | 2020-02-07 | 2024-02-05 | Cytokinetics Inc | Nampt modulators |
| EP4153303A1 (en) | 2020-05-18 | 2023-03-29 | GEN1E Lifesciences Inc. | P38alpha mitogen-activated protein kinase inhibitors |
| WO2021242912A1 (en) | 2020-05-27 | 2021-12-02 | Corcept Therapeutics Incorporated | Concomitant administration of glucocorticoid receptor modulator relacorilant and paclitaxel, a dual substrate of cyp2c8 and cyp3a4 |
| 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 |
| US12433882B2 (en) | 2022-10-28 | 2025-10-07 | Corcept Therapeutics Incorporated | Treatments for amyotrophic lateral sclerosis using dazucorilant |
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| 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 |
| DK48575A (https=) * | 1974-02-19 | 1975-10-20 | 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 |
| AU657424B2 (en) * | 1992-07-02 | 1995-03-09 | Otsuka Pharmaceutical Co., Ltd. | 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 |
| AP1542A (en) * | 1999-04-30 | 2006-01-31 | Pfizer Prod 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 |
| JP2005515176A (ja) * | 2001-11-03 | 2005-05-26 | アストラゼネカ アクチボラグ | 抗腫瘍剤としてのキナゾリン誘導体 |
| RS44204A (sr) * | 2001-11-22 | 2007-06-04 | Biovitrum Ab., | Inhibitori 11-beta- hidroksistereoidne dehidrogenaze tipa 1 |
| BR0308162A (pt) * | 2002-03-01 | 2004-12-07 | Pfizer | Derivados de indolil-uréia de tienopiridinas úteis como agentes antiangiogênicos e métodos para o seu uso |
-
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 EP EP04704554A patent/EP1590319A1/en not_active Withdrawn
- 2004-01-23 US US10/542,759 patent/US20060205772A1/en not_active Abandoned
- 2004-01-23 JP JP2006500009A patent/JP2006517199A/ja active Pending
- 2004-01-23 CN CN200480002540A patent/CN100586927C/zh not_active Expired - Fee Related
- 2004-01-23 BR BR0406938-2A patent/BRPI0406938A/pt not_active IP Right Cessation
- 2004-01-23 CA CA002513349A patent/CA2513349A1/en not_active Abandoned
- 2004-01-23 WO PCT/EP2004/000571 patent/WO2004065351A1/en not_active Ceased
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