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公开(公告)号：WO2004087699A2
公开(公告)日：2004-10-14
申请号：PCT/US2004/009166
申请日：2004-03-25
Applicant: VERTEX PHARMACEUTICALS INCORPORATED , BRENCHLEY, Guy , FARMER, Luc, J. , HARRINGTON, Edmund, Martin , KNEGTEL, Ronald , O'DONNELL, Michael , SALITURO, Francesco, G. , STUDLEY, John, R. , WANG, Jian
Inventor： BRENCHLEY, Guy , FARMER, Luc, J. , HARRINGTON, Edmund, Martin , KNEGTEL, Ronald , O'DONNELL, Michael , SALITURO, Francesco, G. , STUDLEY, John, R. , WANG, Jian
IPC: C07D417/00
CPC classification number: C07D417/14 , C07D417/04
Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Abstract translation: 本发明涉及可用于蛋白激酶抑制剂的化合物。 本发明还提供了包含所述化合物的药学上可接受的组合物以及使用该组合物治疗各种疾病，病症或障碍的方法。
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2.发明申请4-OXO-3-(1-OXO-1H-ISOQUINOLIN-2-YLACETYLAMINO)-PENTANOIC ACID ESTER AND AMIDE DERIVATIVES AND THEIR USE AS CASPASE INHIBITORS 审中-公开4-OXO-3-（1-OXO-1H-异喹啉-2-基乙酰胺基） - 戊酸酯和酰胺衍生物及其作为CASPASE抑制剂的用途
公开(公告)号：WO2004058718A1
公开(公告)日：2004-07-15
申请号：PCT/US2003/040870
申请日：2003-12-22
Applicant: VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , MORTIMORE, Michael , STUDLEY, John, R.
Inventor： CHARRIER, Jean-Damien , MORTIMORE, Michael , STUDLEY, John, R.
IPC: C07D217/24
CPC classification number: C07D401/12 , C07D217/24 , C07D405/12 , C07D417/12
Abstract: The present invention provides a compound of formula (I):, wherein: X i s -OR 1 or -N (R 5 ) 2 , Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R 1 is: C 1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or alkynyl is optionally substituted with optionally substituted aryl, CF 3 , C1, F, OMe, OEt, OCF 3 , CN, or NMe 2 ; C 1-6 cycloalkyl, wherein 1-2 carbon atoms in the cycloalkyl is optionally replaced with -0- or -NR 5 -; R 2 is C 1-6 straight chained or branched alkyl; R 3 is hydrogen, halo, OCF 3 , CN, or CF 3 ; R 4 is hydrogen, halo, OCF 3 , CN, or CF 3 ; and each R 5 is independently H, C 1-6 straight chained or branched alkyl, aryl, -O-C 1-6 straight chained or branched alkyl, or -O-aryl. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated disease, particularly in the central nervous system.
Abstract translation: 本发明提供式（I）的化合物：其中：X 1 -OR 1或-N（R 5）2，Y是卤素，三氟苯氧基或四氟苯氧基; R 1是：C 1-6直链或支链烷基，烯基或炔基，其中烷基，烯基或炔基任选被任选取代的芳基CF 3，C 1，F，OMe，OEt，OCF 3，CN， 或NMe2; C 1-6环烷基，其中环烷基中的1-2个碳原子任选被-O-或-NR 5 - 取代; R 2是C 1-6直链或支链烷基; R 3是氢，卤素，OCF 3，CN或CF 3; R 4是氢，卤素，OCF 3，CN或CF 3; 并且每个R 5独立地为H，C 1-6直链或支链烷基，芳基，-O-C 1-6直链或支链烷基或-O-芳基。 本发明还提供了使用这种组合物治疗半胱天冬酶介导的疾病，特别是中枢神经系统的药物组合物和方法。
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3.发明申请3-[2-(3-ACYLAMINO-2-OXO-2H-PYRIDIN-1-YL)-ACETYLAMINO]-4-OXO-PENTANOIC ACID DERIVATIVES AND THEIR USE AS CASPASE INHIBITORS 审中-公开3- [2-（3-氨基亚氨基-2-氧代-2H-吡啶-1-基） - 乙酰氨基] -4-氧代戊酸衍生物及其作为CASPASE抑制剂的用途
公开(公告)号：WO2006057961A1
公开(公告)日：2006-06-01
申请号：PCT/US2005/042139
申请日：2005-11-21
Applicant: VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , KNEGTEL, Ronald , MORTIMORE, Michael , STUDLEY, John, R.
Inventor： CHARRIER, Jean-Damien , KNEGTEL, Ronald , MORTIMORE, Michael , STUDLEY, John, R.
IPC: C07D213/75 , A61K31/4412 , A61K31/4436 , A61K31/4439 , C07D401/06 , C07D409/06
CPC classification number: C07D213/75 , C07D211/72 , C07D401/02 , C07D401/06 , C07D409/06
Abstract: The present invention provides a compound of formula (I): wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.
Abstract translation: 本发明提供式（I）化合物：其中R 1，R 2，R 3，R 3， > 4 ，＆lt; SUP＆gt;和R＆lt; 5＆gt;如本文所定义。 本发明还提供了使用这种组合物治疗半胱天冬酶介导的疾病的药物组合物和方法以及制备本发明化合物的方法。
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Patent Agency Ranking
公开(公告)号：WO2005085236A3
公开(公告)日：2005-10-20
申请号：PCT/US2005006540
申请日：2005-02-28
Applicant: VERTEX PHARMA , CHARRIER JEAN-DAMIEN , DURRANT STEVEN , MORTIMORE MICHAEL , O'DONNELL MICHAEL , RUTHERFORD ALISTAIR , RAMAYA SHARN , STUDLEY JOHN R , TRUDEAU MARTIN , LOOKER ADAM
Inventor： CHARRIER JEAN-DAMIEN , DURRANT STEVEN , MORTIMORE MICHAEL , O'DONNELL MICHAEL , RUTHERFORD ALISTAIR , RAMAYA SHARN , STUDLEY JOHN R , TRUDEAU MARTIN , LOOKER ADAM
IPC: A61K38/04 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/04 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/443 , A61P37/00
CPC classification number: C07D405/12 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/12 , C07K5/0202
Abstract: The present invention provides a compound of formula (I): wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula (I), and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.
Abstract translation: 本发明提供式（I）的化合物：其中变量如本文所定义。 本发明还提供制备式（I）化合物及其中间体，包含那些化合物的药物组合物的方法，以及使用该化合物和组合物的方法。
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公开(公告)号：WO2004087699A3
公开(公告)日：2004-12-09
申请号：PCT/US2004009166
申请日：2004-03-25
Applicant: VERTEX PHARMA , BRENCHLEY GUY , FARMER LUC J , HARRINGTON EDMUND MARTIN , KNEGTEL RONALD , O'DONNELL MICHAEL , SALITURO FRANCESCO G , STUDLEY JOHN R , WANG JIAN
Inventor： BRENCHLEY GUY , FARMER LUC J , HARRINGTON EDMUND MARTIN , KNEGTEL RONALD , O'DONNELL MICHAEL , SALITURO FRANCESCO G , STUDLEY JOHN R , WANG JIAN
IPC: A61K31/506 , A61P29/00 , A61P35/00 , A61P37/00 , C07D417/00 , C07D417/04 , C07D417/14
CPC classification number: C07D417/14 , C07D417/04
Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. These compounds have the general formula I: Or a pharmaceutically acceptable salt thereof, wherein R , R , R , R , and Ar are as defined in the present claims.
Abstract translation: 本发明涉及可用于蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 这些化合物具有通式I：或其药学上可接受的盐，其中R 1，R 2，R 3，R 4和Ar 1如本权利要求中所定义。
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6.发明申请3 - [2- (3-AMINO-2-OXO-2H-PYRIDIN-1-YL) - ACETYLAMINO] - 4- OXO-PENTANOIC ACID DERIVATIVES AND THEIR USE AS CASPASE INHIBITORS 审中-公开3- [2-（3-氨基-2-氧代-2H-吡啶-1-基） - 乙酰氨基] -4-氧代戊酸衍生物及其作为CASPASE抑制剂的用途
公开(公告)号：WO2004106304A3
公开(公告)日：2005-11-03
申请号：PCT/US2004016706
申请日：2004-05-27
Applicant: VERTEX PHARMA , BRENCHLEY GUY , CHARRIER JEAN-DAMIEN , DURRANT STEVEN , KNEGTEL RONALD , MORTIMORE MICHAEL , STUDLEY JOHN R
Inventor： BRENCHLEY GUY , CHARRIER JEAN-DAMIEN , DURRANT STEVEN , KNEGTEL RONALD , MORTIMORE MICHAEL , STUDLEY JOHN R
IPC: C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12 , C07D213/74 , A61K31/4412 , C07D213/76 , C07D213/81
CPC classification number: C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12
Abstract: The present invention provides a compound of formula (I), wherein R , R C(O)-, HC(O)-, R SO2-, R OC(O)-, (R )2NC(O)-, (R ) (H) NC (O)-, R C (O) C (O) -, R -, (R ) 2NC (O) C (O)-, R (H) NC (O) C (O)-, or R OC (O) C (O)-; R is hydrogen, CF3, -halo, -OR , -NO2, -OCF3, -CN, or R ; R is hydrogen or (C1-C4) -aliphatic-; R is -COOH or -COOR ; R is -CH2F or -CH2O-2, 3, 5, 6-tetrafluorophenyl. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.
Abstract translation: 本发明提供式（I）化合物，其中R 1，R 6 C（O） - ，HC（O） - ，R 6 SO 2 - ，R 6 OC（O） ，（R 6）2 NC（O） - ，（R 6）（H）NC（O） - ，R 6 C（O）C（O） - ，R 6 - ，（R （O）C（O） - ，R 6（H）NC（O）C（O） - 或R 6 OC（O）C（O） - ; R 2是氢，CF 3， - 卤素，-OR 7，-NO 2，-OCF 3，-CN或R 8; R 3是氢或（C 1 -C 4） - 脂族 - R 4是-COOH或-COOR 8; R 5是-CH 2 F或-CH 2 O-2,3,5,6-四氟苯基。 本发明还提供了使用这种组合物治疗半胱天冬酶介导的疾病的药物组合物和方法以及制备本发明化合物的方法。
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公开(公告)号：WO2005085236A2
公开(公告)日：2005-09-15
申请号：PCT/US2005/006540
申请日：2005-02-28
Applicant: VERTEX PHARMACEUTICALS INCORPORATED , CHARRIER, Jean-Damien , DURRANT, Steven , MORTIMORE, Michael , O'DONNELL, Michael , RUTHERFORD, Alistair , RAMAYA, Sharn , STUDLEY, John, R. , TRUDEAU, Martin , LOOKER, Adam
Inventor： CHARRIER, Jean-Damien , DURRANT, Steven , MORTIMORE, Michael , O'DONNELL, Michael , RUTHERFORD, Alistair , RAMAYA, Sharn , STUDLEY, John, R. , TRUDEAU, Martin , LOOKER, Adam
IPC: C07D405/00
CPC classification number: C07D405/12 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/12 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389
Abstract: The present invention provides a compound of formula (I): wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula (I), and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.
Abstract translation: 本发明提供了式（I）化合物：其中变量如本文所定义。 本发明还提供了制备式（I）化合物及其中间体的方法，包含这些化合物的药物组合物，以及使用该化合物和组合物的方法。
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公开(公告)号：WO2004106304A2
公开(公告)日：2004-12-09
申请号：PCT/US2004/016706
申请日：2004-05-27
Applicant: VERTEX PHARMACEUTICALS INCORPORATED , BRENCHLEY, Guy , CHARRIER, Jean-Damien , DURRANT, Steven , KNEGTEL, Ronald , MORTIMORE, Michael , STUDLEY, John, R.
Inventor： BRENCHLEY, Guy , CHARRIER, Jean-Damien , DURRANT, Steven , KNEGTEL, Ronald , MORTIMORE, Michael , STUDLEY, John, R.
IPC: C07D213/00
CPC classification number: C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12
Abstract: The present invention provides a compound of formula (I), wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.
Abstract translation: 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和R 5如本文所定义。 本发明还提供了使用这种组合物治疗半胱天冬酶介导的疾病的药物组合物和方法以及制备本发明化合物的方法。
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