JP2006528637A5 - - Google Patents
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- Publication number
- JP2006528637A5 JP2006528637A5 JP2006521272A JP2006521272A JP2006528637A5 JP 2006528637 A5 JP2006528637 A5 JP 2006528637A5 JP 2006521272 A JP2006521272 A JP 2006521272A JP 2006521272 A JP2006521272 A JP 2006521272A JP 2006528637 A5 JP2006528637 A5 JP 2006528637A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- heterocyclyl
- alkyl
- heteroaryl
- cycloalkyl
- 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.)
- Granted
Links
- 125000000623 heterocyclic group Chemical group 0.000 claims 131
- 125000001072 heteroaryl group Chemical group 0.000 claims 124
- 229910052739 hydrogen Inorganic materials 0.000 claims 95
- 239000001257 hydrogen Substances 0.000 claims 95
- 125000003710 aryl alkyl group Chemical group 0.000 claims 88
- 125000000547 substituted alkyl group Chemical group 0.000 claims 81
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 78
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 76
- 150000002431 hydrogen Chemical class 0.000 claims 70
- 150000001875 compounds Chemical class 0.000 claims 63
- 125000003107 substituted aryl group Chemical group 0.000 claims 59
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 51
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 50
- 125000005843 halogen group Chemical group 0.000 claims 48
- -1 R 21 Chemical compound 0.000 claims 40
- 125000000217 alkyl group Chemical group 0.000 claims 39
- 229910052799 carbon Inorganic materials 0.000 claims 38
- 125000000753 cycloalkyl group Chemical group 0.000 claims 37
- 125000003118 aryl group Chemical group 0.000 claims 36
- 125000003342 alkenyl group Chemical group 0.000 claims 33
- 150000001721 carbon Chemical group 0.000 claims 33
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 33
- 229910052757 nitrogen Inorganic materials 0.000 claims 26
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 26
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 24
- 125000000304 alkynyl group Chemical group 0.000 claims 23
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 20
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 13
- WMFYOYKPJLRMJI-UHFFFAOYSA-N Lercanidipine hydrochloride Chemical compound Cl.COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)(C)CN(C)CCC(C=2C=CC=CC=2)C=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 WMFYOYKPJLRMJI-UHFFFAOYSA-N 0.000 claims 12
- 125000001188 haloalkyl group Chemical group 0.000 claims 12
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 11
- 125000004043 oxo group Chemical group O=* 0.000 claims 11
- 125000000464 thioxo group Chemical group S=* 0.000 claims 11
- 125000004429 atom Chemical group 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 9
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 125000001118 alkylidene group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 6
- 125000002462 isocyano group Chemical group *[N+]#[C-] 0.000 claims 6
- DYMRYCZRMAHYKE-UHFFFAOYSA-N n-diazonitramide Chemical compound [O-][N+](=O)N=[N+]=[N-] DYMRYCZRMAHYKE-UHFFFAOYSA-N 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000002577 pseudohalo group Chemical group 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 5
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 5
- 150000002923 oximes Chemical class 0.000 claims 5
- 201000001320 Atherosclerosis Diseases 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 230000003143 atherosclerotic effect Effects 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 201000001421 hyperglycemia Diseases 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
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 150000007857 hydrazones Chemical class 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 102100038495 Bile acid receptor Human genes 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010008635 Cholestasis Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 206010049287 Lipodystrophy acquired Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 230000007870 cholestasis Effects 0.000 claims 2
- 231100000359 cholestasis Toxicity 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 208000006132 lipodystrophy Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 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 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 0 *C1(*)C(***2)=C2C(*)=C(*)N(*)C1(*)* Chemical compound *C1(*)C(***2)=C2C(*)=C(*)N(*)C1(*)* 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US48985403P | 2003-07-23 | 2003-07-23 | |
| PCT/US2004/023745 WO2005009387A2 (en) | 2003-07-23 | 2004-07-23 | Azepine derivatives as pharmaceutical agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006528637A JP2006528637A (ja) | 2006-12-21 |
| JP2006528637A5 true JP2006528637A5 (https=) | 2007-10-04 |
| JP4679517B2 JP4679517B2 (ja) | 2011-04-27 |
Family
ID=34102943
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006521272A Expired - Fee Related JP4679517B2 (ja) | 2003-07-23 | 2004-07-23 | 薬剤としてのアゼピン誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8466143B2 (https=) |
| EP (1) | EP1648408A4 (https=) |
| JP (1) | JP4679517B2 (https=) |
| KR (1) | KR20060052867A (https=) |
| CN (1) | CN1852748A (https=) |
| AU (1) | AU2004259009A1 (https=) |
| BR (1) | BRPI0412262A (https=) |
| CA (1) | CA2532798C (https=) |
| CR (1) | CR8258A (https=) |
| EC (1) | ECSP066392A (https=) |
| IL (1) | IL173287A0 (https=) |
| NO (1) | NO20060871L (https=) |
| RU (1) | RU2006105646A (https=) |
| WO (1) | WO2005009387A2 (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7595311B2 (en) * | 2002-05-24 | 2009-09-29 | Exelixis, Inc. | Azepinoindole derivatives as pharmaceutical agents |
| ES2319539T3 (es) | 2003-09-17 | 2009-05-08 | Janssen Pharmaceutica Nv | Compuestos heterociclicos condensados como moduladores del receptor de serotonina. |
| ATE420091T1 (de) | 2005-03-14 | 2009-01-15 | Glaxo Group Ltd | Kondensierte thiazolderivate mit affinität für den histamin-h3-rezeptor |
| EP1963331A1 (en) * | 2005-12-15 | 2008-09-03 | Exelixis, Inc. | Azepinoindole derivatives as pharmaceutical agents |
| US20080299118A1 (en) * | 2007-06-01 | 2008-12-04 | Wyeth | FXR Agonists for the Treatment of Malignancies |
| US20080300235A1 (en) * | 2007-06-01 | 2008-12-04 | Wyeth | FXR Agonists for Reducing LOX-1 Expression |
| US20090163474A1 (en) * | 2007-10-19 | 2009-06-25 | Wyeth | FXR Agonists for the Treatment of Nonalcoholic Fatty Liver and Cholesterol Gallstone Diseases |
| US20090215748A1 (en) * | 2007-12-20 | 2009-08-27 | Wyeth | FXR agonists for treating vitamin D associated diseases |
| AU2009308708B2 (en) | 2008-10-31 | 2015-11-19 | Medivation Technologies, Inc. | Azepino [4, 5-b] indoles and methods of use |
| TWI477503B (zh) * | 2008-10-31 | 2015-03-21 | Medivation Technologies Inc | 含有剛性部分之吡啶并〔４，３－ｂ〕吲哚 |
| CN101875627B (zh) * | 2009-04-30 | 2014-01-15 | 凯惠科技发展(上海)有限公司 | 一种1-烷氧羰基-2h-异吲哚衍生物及其制备方法和中间体 |
| RU2542103C2 (ru) * | 2009-05-22 | 2015-02-20 | Эббви Инк. | Модуляторы рецепторов 5-нт и способы их применения |
| US9040519B2 (en) | 2010-02-18 | 2015-05-26 | Medivation Technologies, Inc. | Fused tetracyclic pyrido [4,3-B] indole and pyrido [3,4-B] indole derivatives and methods of use |
| WO2011103460A1 (en) | 2010-02-18 | 2011-08-25 | Medivation Technologies, Inc. | Fused tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]ondole derivatives and methods of use |
| WO2011103433A1 (en) | 2010-02-18 | 2011-08-25 | Medivation Technologies, Inc. | Pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives and methods of use |
| WO2011146089A1 (en) * | 2010-05-21 | 2011-11-24 | Abbott Laboratories | Modulators of 5-ht receptors and methods of use thereof |
| US8791132B2 (en) * | 2011-02-18 | 2014-07-29 | Medivation Technologies, Inc. | Compounds and methods for treatment of hypertension |
| US9434747B2 (en) | 2011-02-18 | 2016-09-06 | Medivation Technologies, Inc. | Methods of treating diabetes |
| WO2014031165A1 (en) * | 2012-08-22 | 2014-02-27 | Medivation Technologies, Inc. | Compounds and methods of treating diabetes |
| CN111662297A (zh) * | 2014-11-21 | 2020-09-15 | 阿卡纳治疗学有限公司 | 用于治疗疾病的稠合双环化合物 |
| WO2016103037A1 (en) * | 2014-12-22 | 2016-06-30 | Akarna Therapeutics, Ltd. | Fused bicyclic compounds for the treatment of disease |
| TWI698430B (zh) | 2015-02-13 | 2020-07-11 | 南北兄弟藥業投資有限公司 | 三環化合物及其在藥物中的應用 |
| EP3715348A1 (en) * | 2015-03-26 | 2020-09-30 | Akarna Therapeutics, Ltd. | Fused bicyclic compounds for the treatment of disease |
| WO2017143134A1 (en) * | 2016-02-19 | 2017-08-24 | Alios Biopharma, Inc. | Fxr modulators and methods of their use |
| BR112018073460A2 (pt) * | 2016-05-25 | 2019-07-09 | Akarna Therapeutics Ltd | terapias combinadas usando moduladores do receptor farnesoide x (fxr) |
| KR20190040140A (ko) * | 2016-05-25 | 2019-04-17 | 아카나 테라퓨틱스, 엘티디. | 질환의 치료를 위한 융합된 비시클릭 화합물 |
| RU2019144064A (ru) * | 2017-06-02 | 2021-07-13 | Акарна Терапьютикс, Лтд. | Конденсированные бициклические соединения |
| CR20250117A (es) | 2018-01-26 | 2025-05-09 | Exelixis Inc | COMPUESTOS PARA EL TRATAMIENTO DE TRASTORNOS DEPENDIENTES DE CINASAS (Divisional 2020-0355) |
| CA3088198A1 (en) | 2018-01-26 | 2019-08-01 | Exelixis, Inc. | Compounds for the treatment of kinase-dependent disorders |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GR35044B (el) * | 1966-05-10 | 1968-07-31 | The Upjohn Company | Μεθοδος παρασκευης οργανικων ενωσεων. |
| US4362739A (en) * | 1981-05-04 | 1982-12-07 | S.A. Omnichem | Pyrrolo(2,3-d)carbazole derivatives, compositions and use |
| IL101851A (en) * | 1991-06-13 | 1996-05-14 | Janssen Pharmaceutica Nv | 10-(4-piperidinyl- and piperidinylidene)-imidazo [1,2-a] (pyrrolo thieno or furano) [2,3] azepine derivatives their preparation and pharmaceutical compositions containing them and certain novel intermediates therefor |
| JPH09221475A (ja) * | 1996-02-13 | 1997-08-26 | Yamanouchi Pharmaceut Co Ltd | 新規なオキシム誘導体 |
| EP1003751A1 (en) * | 1997-08-04 | 2000-05-31 | Amgen Inc. | Hydroxamic acid substituted fused heterocyclic metalloproteinase inhibitors |
| CN100513570C (zh) | 1999-06-18 | 2009-07-15 | Cv治疗公司 | 结合框运输蛋白abc1的调节作用 |
| FR2796070B1 (fr) * | 1999-07-06 | 2003-02-21 | Lipha | Derives de benzodiazepines utilisables dans le traitement de dyslipidemies, de l'atherosclerose et du diabete, compositions pharmaceutiques les contenant et procedes de preparation |
| MY122278A (en) | 1999-07-19 | 2006-04-29 | Upjohn Co | 1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles containing arylsulfones at the 9-position |
| US20020013334A1 (en) * | 2000-06-15 | 2002-01-31 | Robl Jeffrey A. | HMG-CoA reductase inhibitors and method |
| US7595311B2 (en) * | 2002-05-24 | 2009-09-29 | Exelixis, Inc. | Azepinoindole derivatives as pharmaceutical agents |
| TWI329111B (en) * | 2002-05-24 | 2010-08-21 | X Ceptor Therapeutics Inc | Azepinoindole and pyridoindole derivatives as pharmaceutical agents |
| EP1963331A1 (en) * | 2005-12-15 | 2008-09-03 | Exelixis, Inc. | Azepinoindole derivatives as pharmaceutical agents |
-
2004
- 2004-07-23 US US10/565,702 patent/US8466143B2/en active Active
- 2004-07-23 AU AU2004259009A patent/AU2004259009A1/en not_active Abandoned
- 2004-07-23 EP EP04779004A patent/EP1648408A4/en not_active Withdrawn
- 2004-07-23 CA CA2532798A patent/CA2532798C/en not_active Expired - Fee Related
- 2004-07-23 RU RU2006105646/04A patent/RU2006105646A/ru not_active Application Discontinuation
- 2004-07-23 JP JP2006521272A patent/JP4679517B2/ja not_active Expired - Fee Related
- 2004-07-23 BR BRPI0412262-3A patent/BRPI0412262A/pt not_active IP Right Cessation
- 2004-07-23 KR KR1020067001566A patent/KR20060052867A/ko not_active Withdrawn
- 2004-07-23 WO PCT/US2004/023745 patent/WO2005009387A2/en not_active Ceased
- 2004-07-23 CN CNA2004800270768A patent/CN1852748A/zh active Pending
-
2006
- 2006-01-22 IL IL173287A patent/IL173287A0/en unknown
- 2006-02-22 NO NO20060871A patent/NO20060871L/no not_active Application Discontinuation
- 2006-02-23 EC EC2006006392A patent/ECSP066392A/es unknown
- 2006-02-23 CR CR8258A patent/CR8258A/es not_active Application Discontinuation
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