JP2005517006A5 - - Google Patents
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- Publication number
- JP2005517006A5 JP2005517006A5 JP2003565952A JP2003565952A JP2005517006A5 JP 2005517006 A5 JP2005517006 A5 JP 2005517006A5 JP 2003565952 A JP2003565952 A JP 2003565952A JP 2003565952 A JP2003565952 A JP 2003565952A JP 2005517006 A5 JP2005517006 A5 JP 2005517006A5
- Authority
- JP
- Japan
- Prior art keywords
- halogen
- alkyl
- optionally substituted
- cyano
- independently
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 229910052736 halogen Inorganic materials 0.000 claims 21
- 150000002367 halogens Chemical class 0.000 claims 21
- -1 3,4-methylenedioxyphenyl Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims 15
- 125000005843 halogen group Chemical group 0.000 claims 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 208000002193 Pain Diseases 0.000 claims 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 3
- 150000001204 N-oxides Chemical class 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000000842 isoxazolyl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 229910052801 chlorine Chemical group 0.000 claims 2
- 239000000460 chlorine Chemical group 0.000 claims 2
- AIMMVWOEOZMVMS-UHFFFAOYSA-N cyclopropanecarboxamide Chemical compound NC(=O)C1CC1 AIMMVWOEOZMVMS-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000003349 osteoarthritic effect Effects 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 230000002980 postoperative effect Effects 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000004371 toothache Diseases 0.000 claims 2
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 2
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 1
- GYPLSWLUTVLVRT-CYBMUJFWSA-N 2-fluoro-n-methoxy-6-[4-[(1r)-1-[[1-(3,3,3-trifluoropropanoylamino)cyclopropanecarbonyl]amino]ethyl]phenyl]benzamide Chemical compound CONC(=O)C1=C(F)C=CC=C1C1=CC=C([C@@H](C)NC(=O)C2(CC2)NC(=O)CC(F)(F)F)C=C1 GYPLSWLUTVLVRT-CYBMUJFWSA-N 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- ZNZGNKLGRXUQOI-UHFFFAOYSA-N methyl 2-fluoro-6-[4-[2-[[1-[(2,2,2-trifluoroacetyl)amino]cyclopropanecarbonyl]amino]propan-2-yl]phenyl]benzoate Chemical compound COC(=O)C1=C(F)C=CC=C1C1=CC=C(C(C)(C)NC(=O)C2(CC2)NC(=O)C(F)(F)F)C=C1 ZNZGNKLGRXUQOI-UHFFFAOYSA-N 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35506202P | 2002-02-08 | 2002-02-08 | |
| US41017202P | 2002-09-12 | 2002-09-12 | |
| PCT/US2003/003338 WO2003066577A1 (en) | 2002-02-08 | 2003-02-04 | N-biphenylmethyl aminocycloalkanecarboxamide derivatives with a substiituent on the methyl useful as bradykinin antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005517006A JP2005517006A (ja) | 2005-06-09 |
| JP2005517006A5 true JP2005517006A5 (https=) | 2005-12-22 |
| JP4098249B2 JP4098249B2 (ja) | 2008-06-11 |
Family
ID=27737481
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003565952A Expired - Fee Related JP4098249B2 (ja) | 2002-02-08 | 2003-02-04 | ブラジキニン拮抗薬として有用なメチル上に置換基を有するｎ−ビフェニルメチルアミノシクロアルカンカルボキサミド誘導体 |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US6919343B2 (https=) |
| EP (1) | EP1501787B1 (https=) |
| JP (1) | JP4098249B2 (https=) |
| KR (1) | KR20040083440A (https=) |
| CN (1) | CN1328247C (https=) |
| AR (1) | AR038377A1 (https=) |
| AT (1) | ATE309202T1 (https=) |
| AU (1) | AU2003216169B2 (https=) |
| BR (1) | BR0307508A (https=) |
| CA (1) | CA2474373C (https=) |
| DE (1) | DE60302240T2 (https=) |
| DK (1) | DK1501787T3 (https=) |
| EA (1) | EA007297B1 (https=) |
| EC (1) | ECSP045217A (https=) |
| ES (1) | ES2250899T3 (https=) |
| HR (1) | HRP20040677A2 (https=) |
| IS (1) | IS7372A (https=) |
| JO (1) | JO2356B1 (https=) |
| MA (1) | MA27108A1 (https=) |
| MX (1) | MXPA04007660A (https=) |
| NO (1) | NO20043739L (https=) |
| NZ (1) | NZ534062A (https=) |
| PE (1) | PE20030986A1 (https=) |
| PL (1) | PL371664A1 (https=) |
| RS (1) | RS65404A (https=) |
| TW (1) | TWI259079B (https=) |
| WO (1) | WO2003066577A1 (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1466904A4 (en) * | 2001-12-28 | 2005-12-14 | Takeda Pharmaceutical | BIARYL CONNECTION AND ITS USE |
| US7091380B2 (en) * | 2002-02-08 | 2006-08-15 | Merck & Co., Inc. | N-biphenylmethyl aminocycloalkanecarboxamide derivatives |
| WO2004019868A2 (en) * | 2002-08-29 | 2004-03-11 | Merck & Co., Inc. | N-biarylmethyl aminocycloalkanecarboxamide derivatives |
| AU2003299757A1 (en) * | 2002-12-19 | 2004-07-14 | Elan Pharmaceuticals Inc. | Substituted n-phenyl sulfonamide bradykinin antagonists |
| EP1654232A4 (en) * | 2003-08-07 | 2008-11-12 | Merck & Co Inc | SULPHONYL SUBSTITUTED N- (BIARYLMETHYL) AMINOCYCLOPROPANCARBOXYLIC ACID AMIDE |
| US7790754B2 (en) * | 2003-12-22 | 2010-09-07 | Merck Sharp & Dohme Corp. | Alpha-hydroxy amides as bradykinin antagonists or inverse agonists |
| ATE423114T1 (de) * | 2004-03-02 | 2009-03-15 | Merck & Co Inc | Aminocyclopropancarbonsäureamidderivate als bradykininantagonisten |
| US20050245543A1 (en) * | 2004-04-30 | 2005-11-03 | Pfizer Inc | Histamine-3 receptor antagonists |
| MX2007001348A (es) * | 2004-08-02 | 2008-03-11 | Bebaas Inc | Composiciones de vitamina b12. |
| DE102004060542A1 (de) * | 2004-12-16 | 2006-07-06 | Sanofi-Aventis Deutschland Gmbh | Hydroxybiphenyl-Carbonsäuren und Derivate, Verfahren zu deren Herstellung und deren Verwendung |
| PT1830869E (pt) | 2004-12-24 | 2013-08-22 | Spinifex Pharm Pty Ltd | Método de tratamento ou profilaxia |
| US20070178141A1 (en) * | 2005-09-07 | 2007-08-02 | Bebaas, Inc. | Vitamin B12 compositions |
| US20130131007A1 (en) | 2005-09-07 | 2013-05-23 | Bebaas, Inc. | Vitamin b12 compositions |
| CA2646379C (en) * | 2006-03-20 | 2014-12-23 | The University Of Queensland | Method of treatment or prophylaxis inflammatory pain |
| US8945505B2 (en) * | 2007-02-02 | 2015-02-03 | Panaphix, Inc. | Use of arsenic compounds for treatment of pain and inflammation |
| EP2520561B1 (en) | 2007-06-08 | 2016-02-10 | MannKind Corporation | IRE-1A Inhibitors |
| AR070750A1 (es) | 2007-08-29 | 2010-05-05 | Boehringer Ingelheim Int | Compuestos b1-antagonistas, sus sales farmaceuticamente compatibles, medicamentos que contienen dichos compuestos, uso de los mismos para preparar medicamentos y procedimientoo de preparacion de un medicamento |
| CA2722704A1 (en) * | 2008-04-28 | 2009-11-05 | Zalicus Pharmaceuticals Ltd. | Cyclylamine derivatives as calcium channel blockers |
| JP5629274B2 (ja) * | 2009-02-26 | 2014-11-19 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ブラジキニンｂ１アンタゴニストとしての化合物 |
| WO2010097374A1 (de) * | 2009-02-26 | 2010-09-02 | Boehringer Ingelheim International Gmbh | Verbindungen als bradykinin-b1-antagonisten |
| WO2010097373A1 (de) * | 2009-02-26 | 2010-09-02 | Boehringer Ingelheim International Gmbh | Verbindungen als bradykinin b1 antagonisten |
| US10457810B2 (en) | 2009-08-24 | 2019-10-29 | Board Of Trustees Of Michigan State University | Densified biomass products containing pretreated biomass fibers |
| CN102781916B (zh) | 2010-02-23 | 2014-06-25 | 贝林格尔.英格海姆国际有限公司 | 作为缓激肽b1拮抗剂的化合物 |
| BR112012026710B8 (pt) | 2010-04-19 | 2020-06-23 | Univ Michigan State | método para produzir um produto extraído a partir de biomassa lignocelulósica e método para produzir um produto digerido a partir de biomassa lignocelulósica |
| US8937073B2 (en) * | 2010-08-20 | 2015-01-20 | Boehringer Ingelheim International Gmbh | Disubstituted tetrahydrofuranyl compounds and their use as B1-receptor antagonists |
| HUP1000598A2 (en) * | 2010-11-05 | 2012-09-28 | Richter Gedeon Nyrt | Indole derivatives |
| US8912221B2 (en) * | 2010-12-27 | 2014-12-16 | Hoffmann-La Roche Inc. | Biaryl amide derivatives |
| US8592426B2 (en) * | 2011-01-24 | 2013-11-26 | Hoffmann—La Roche Inc. | Aryl-benzocycloalkyl amide derivatives |
| WO2019090088A1 (en) * | 2017-11-02 | 2019-05-09 | Calico Life Sciences Llc | Modulators of the integrated stress pathway |
| TW202545902A (zh) | 2018-10-11 | 2025-12-01 | 美商嘉來克生命科學有限責任公司 | 整合應激路徑之前藥調節劑 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5270317A (en) | 1990-03-20 | 1993-12-14 | Elf Sanofi | N-substituted heterocyclic derivatives, their preparation and the pharmaceutical compositions in which they are present |
| IL99372A0 (en) | 1990-09-10 | 1992-08-18 | Ciba Geigy Ag | Azacyclic compounds |
| US5208236A (en) | 1992-09-23 | 1993-05-04 | Schering Corporation | N-(acylaminomethyl)glutaryl amino acids and use |
| DK0655461T3 (da) | 1993-11-16 | 2000-10-02 | Novartis Ag | Cykliske aminosyrederivater med ACE- og NEP-inhiberende aktivitet |
| WO1997011717A1 (en) | 1995-09-27 | 1997-04-03 | Novartis Ag | Treatment of chronic progressive renal failure |
| FR2743562B1 (fr) | 1996-01-11 | 1998-04-03 | Sanofi Sa | Derives de n-(arylsulfonyl) aminoacides, leur preparation, les compositions pharmaceutiques en contenant |
| US6433185B1 (en) | 1996-01-11 | 2002-08-13 | Sanofi-Synthelabo | N-(arylsulphonyl) amino acid derivatives, process for their preparation and pharmaceutical compositions containing them |
| JP4350306B2 (ja) | 1998-04-23 | 2009-10-21 | ノバルティス アクチエンゲゼルシャフト | エンドセリン変換酵素のチオール型阻害剤 |
| EP1080104B1 (en) | 1998-04-23 | 2005-02-09 | Novartis AG | Certain heteroaryl substituted thiol inhibitors of endothelin-converting enzyme |
| US20020052370A1 (en) | 2000-07-06 | 2002-05-02 | Barber Christopher Gordon | Cyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase |
| DE10036121A1 (de) | 2000-07-25 | 2002-02-07 | Merck Patent Gmbh | N-Substituierte-1-amino-1,1-dialkyl-carbonsäurederivate |
| US7091380B2 (en) | 2002-02-08 | 2006-08-15 | Merck & Co., Inc. | N-biphenylmethyl aminocycloalkanecarboxamide derivatives |
-
2003
- 2003-01-30 TW TW092102107A patent/TWI259079B/zh not_active IP Right Cessation
- 2003-01-30 AR ARP030100276A patent/AR038377A1/es not_active Application Discontinuation
- 2003-01-30 US US10/354,674 patent/US6919343B2/en not_active Expired - Lifetime
- 2003-02-04 PE PE2003000132A patent/PE20030986A1/es not_active Application Discontinuation
- 2003-02-04 CN CNB03803560XA patent/CN1328247C/zh not_active Expired - Fee Related
- 2003-02-04 DK DK03737624T patent/DK1501787T3/da active
- 2003-02-04 CA CA002474373A patent/CA2474373C/en not_active Expired - Fee Related
- 2003-02-04 RS YUP-654/04A patent/RS65404A/sr unknown
- 2003-02-04 DE DE60302240T patent/DE60302240T2/de not_active Expired - Lifetime
- 2003-02-04 NZ NZ534062A patent/NZ534062A/en unknown
- 2003-02-04 US US10/503,501 patent/US20050084463A1/en not_active Abandoned
- 2003-02-04 BR BR0307508-7A patent/BR0307508A/pt not_active IP Right Cessation
- 2003-02-04 HR HR20040677A patent/HRP20040677A2/hr not_active Application Discontinuation
- 2003-02-04 EP EP03737624A patent/EP1501787B1/en not_active Expired - Lifetime
- 2003-02-04 KR KR10-2004-7012238A patent/KR20040083440A/ko not_active Withdrawn
- 2003-02-04 PL PL03371664A patent/PL371664A1/xx unknown
- 2003-02-04 AU AU2003216169A patent/AU2003216169B2/en not_active Ceased
- 2003-02-04 ES ES03737624T patent/ES2250899T3/es not_active Expired - Lifetime
- 2003-02-04 EA EA200401054A patent/EA007297B1/ru not_active IP Right Cessation
- 2003-02-04 AT AT03737624T patent/ATE309202T1/de not_active IP Right Cessation
- 2003-02-04 JP JP2003565952A patent/JP4098249B2/ja not_active Expired - Fee Related
- 2003-02-04 WO PCT/US2003/003338 patent/WO2003066577A1/en not_active Ceased
- 2003-02-04 MX MXPA04007660A patent/MXPA04007660A/es unknown
- 2003-02-06 JO JO200315A patent/JO2356B1/en active
-
2004
- 2004-07-26 IS IS7372A patent/IS7372A/is unknown
- 2004-08-02 EC EC2004005217A patent/ECSP045217A/es unknown
- 2004-08-10 MA MA27820A patent/MA27108A1/fr unknown
- 2004-09-07 NO NO20043739A patent/NO20043739L/no not_active Application Discontinuation