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1.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：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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公开(公告)号：AU2005309776B2
公开(公告)日：2011-12-22
申请号：AU2005309776
申请日：2005-11-21
Applicant: VERTEX PHARMA
Inventor： JEAN-DAMIEN CHARRIER , MICHAEL MORTIMORE , STUDLEY JOHN R , RONALD KNEGTEL
IPC: C07D213/75 , A61K31/4412 , A61K31/4436 , A61K31/4439 , C07D401/06 , C07D409/06
Abstract: The present invention provides a compound of formula (I): wherein R, R, R,R,and Rare 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.
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公开(公告)号：AU2005219861B2
公开(公告)日：2011-08-11
申请号：AU2005219861
申请日：2005-02-28
Applicant: VERTEX PHARMA
Inventor： STUDLEY JOHN R , MICHAEL MORTIMORE , JEAN-DAMIEN CHARRIER , ALISTAIR RUTHERFORD , ADAM LOOKER , MICHAEL O'DONNELL , MARTIN TRUDEAU , SHARN RAMAYA , STEVEN DURRANT
IPC: C07D207/16 , A61K38/04 , A61K38/06 , C07D209/52 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/04
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.
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Patent Agency Ranking
公开(公告)号：NZ544156A
公开(公告)日：2009-05-31
申请号：NZ54415604
申请日：2004-05-27
Applicant: VERTEX PHARMA
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
Abstract: Disclosed is a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed is the use of the above compound in the manufacture of a medicament for inhibiting a caspase-mediated function in a patient or for decreasing IGIF or IFN-gamma production in a patient.
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公开(公告)号：BRPI0508102A
公开(公告)日：2007-07-17
申请号：BRPI0508102
申请日：2005-02-28
Applicant: VERTEX PHARMA
Inventor： CHARRIER JEAN-DAMIEN , DURRANT STEVEN , MORTIMORE MICHAEL , O'DONNELL MICHAEL , RUTHERFORD ALISTAIR , RAMAYA SHARN , STUDLEY JOHN R , TRUDEAU MARTIN , LOOKER ADAM
IPC: C07D405/12 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/443 , A61K38/04 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/04
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.
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公开(公告)号：NO20073170A
公开(公告)日：2007-06-22
申请号：NO20073170
申请日：2007-06-22
Applicant: VERTEX PHARMA
Inventor： MORTIMORE MICHAEL , KNEGTEL RONALD , CHARRIER JEAN-DAMIEN , STUDLEY JOHN R
IPC: C07D213/75
CPC classification number: C07D213/75 , C07D211/72 , C07D401/02 , C07D401/06 , C07D409/06
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公开(公告)号：NO20064344L
公开(公告)日：2006-10-19
申请号：NO20064344
申请日：2006-09-26
Applicant: VERTEX PHARMA
Inventor： CHARRIER JEAN-DAMIEN , MORTIMORE MICHAEL , DURRANT STEVEN , STUDLEY JOHN R , O'DONNELL MICHAEL , RUTHERFORD ALISTAIR , RAMAYA SHARN , TRUDEAU MARTIN , LOOKER ADAM
IPC: C07D207/16 , A61K38/04 , A61K38/06 , C07D209/52 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/04
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.
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公开(公告)号：NO20056192A
公开(公告)日：2005-12-27
申请号：NO20056192
申请日：2005-12-27
Applicant: VERTEX PHARMA
Inventor： CHARRIER JEAN-DAMIEN , KNEGTEL RONALD , BRENCHLEY GUY , MORTIMORE MICHAEL , DURRANT STEVEN , STUDLEY JOHN R
IPC: C07D213/74 , A61K31/4412 , C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12
CPC classification number: C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12
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