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公开(公告)号：US20070155718A1
公开(公告)日：2007-07-05
申请号：US11489939
申请日：2006-07-20
IPC分类号： A61K31/55 , A61K31/5513 , A61K31/503 , A61K31/517 , A61K31/513 , A61K31/4745 , A61K31/424 , C07D491/04
CPC分类号： C07D498/04
摘要： This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.
摘要翻译： 本发明涉及包含呋喃并[3,2-d]恶唑啉-5-酮部分的胱天蛋白酶抑制剂的前体药物，其在特定条件下可转化为生物活性化合物，特别是胱天蛋白酶抑制剂。 本发明还涉及制备这些半胱天冬酶抑制剂前药的方法。 本发明还涉及包含所述前药的药物组合物及其用于治疗与炎性或退行性疾病相关的疾病的用途。
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公开(公告)号：US07960415B2
公开(公告)日：2011-06-14
申请号：US12140497
申请日：2008-06-17
申请人： Guy Brenchley , Jean-Damien Charrier , Steven Durrant , Ronald Knegtel , Michael Mortimore , John Studley
发明人： Guy Brenchley , Jean-Damien Charrier , Steven Durrant , Ronald Knegtel , Michael Mortimore , John Studley
IPC分类号： A61K31/44 , C07D211/72
CPC分类号： C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12
摘要： The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 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.
摘要翻译： 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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公开(公告)号：US08168798B2
公开(公告)日：2012-05-01
申请号：US12971649
申请日：2010-12-17
IPC分类号： C07D498/14
CPC分类号： C07D498/04
摘要： This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors.This invention also relates to the processes for preparing these prodrugs of caspase inhibitors.This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.
摘要翻译： 本发明涉及包含呋喃并[3,2-d]恶唑啉-5-酮部分的胱天蛋白酶抑制剂的前体药物，其在特定条件下可转化为生物活性化合物，特别是胱天蛋白酶抑制剂。 本发明还涉及制备这些半胱天冬酶抑制剂前药的方法。 本发明还涉及包含所述前药的药物组合物及其用于治疗与炎性或退行性疾病相关的疾病的用途。
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公开(公告)号：US20110137037A1
公开(公告)日：2011-06-09
申请号：US12971649
申请日：2010-12-17
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors.This invention also relates to the processes for preparing these prodrugs of caspase inhibitors.This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.
摘要翻译： 本发明涉及包含呋喃并[3,2-d]恶唑啉-5-酮部分的胱天蛋白酶抑制剂的前体药物，其在特定条件下可转化为生物活性化合物，特别是胱天蛋白酶抑制剂。 本发明还涉及制备这些半胱天冬酶抑制剂前药的方法。 本发明还涉及包含所述前药的药物组合物及其用于治疗与炎性或退行性疾病相关的疾病的用途。
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公开(公告)号：US07879891B2
公开(公告)日：2011-02-01
申请号：US11489939
申请日：2006-07-20
IPC分类号： C07D498/14 , A61K31/4725 , A61K31/4439 , A61K31/424
CPC分类号： C07D498/04
摘要： This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors.This invention also relates to the processes for preparing these prodrugs of caspase inhibitors.This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.
摘要翻译： 本发明涉及包含呋喃并[3,2-d]恶唑啉-5-酮部分的胱天蛋白酶抑制剂的前体药物，其在特定条件下可转化为生物活性化合物，特别是胱天蛋白酶抑制剂。 本发明还涉及制备这些半胱天冬酶抑制剂前药的方法。 本发明还涉及包含所述前药的药物组合物及其用于治疗与炎性或退行性疾病相关的疾病的用途。
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公开(公告)号：US20050233979A1
公开(公告)日：2005-10-20
申请号：US11069895
申请日：2005-02-28
申请人： Jean-Damien Charrier , Steven Durrant , Michael Mortimore , Michael O'Donnell , Alistair Rutherford , Sharn Ramaya , John Studley , Martin Trudeau , Adam Looker
发明人： Jean-Damien Charrier , Steven Durrant , Michael Mortimore , Michael O'Donnell , Alistair Rutherford , Sharn Ramaya , John Studley , Martin Trudeau , Adam Looker
IPC分类号： A61K38/04 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/04 , C07D45/14
CPC分类号： C07D405/12 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/12 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： The present invention provides a compound of formula 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.
摘要翻译： 本发明提供了式的化合物，其中变量如本文所定义。 本发明还提供制备式I化合物的方法及其中间体，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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![5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors](/abs-image/US/2013/09/10/US08530489B2/abs.jpg.150x150.jpg)
7.发明授权5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors 有权可用作蛋白激酶抑制剂的5-氰基-4-（吡咯并[2,3B]吡啶-3-基） - 嘧啶衍生物公开(公告)号：US08530489B2
公开(公告)日：2013-09-10
申请号：US13477663
申请日：2012-05-22
申请人： Michael Mortimore , Stephen Clinton Young , Simon Robert Lorrie Everitt , Ronald Knegtel , Joanne Louise Pinder , Alistair Peter Rutherford , Steven Durrant , Guy Brenchley , Jean-Damien Charrier , Michael O'Donnell
发明人： Michael Mortimore , Stephen Clinton Young , Simon Robert Lorrie Everitt , Ronald Knegtel , Joanne Louise Pinder , Alistair Peter Rutherford , Steven Durrant , Guy Brenchley , Jean-Damien Charrier , Michael O'Donnell
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.
摘要翻译： 本发明涉及可用作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。 本发明还提供了制备本发明化合物的方法。
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![5-CYANO-4- (PYRROLO [2,3B] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS](/abs-image/US/2012/12/06/US20120309963A1/abs.jpg.150x150.jpg)
8.发明申请5-CYANO-4- (PYRROLO [2,3B] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS 有权5-氰基-4-（吡咯并[2,3B]吡啶-3-基） - 吡啶衍生物，用作蛋白激酶抑制剂公开(公告)号：US20120309963A1
公开(公告)日：2012-12-06
申请号：US13477663
申请日：2012-05-22
申请人： Michael Mortimore , Stephen Clinton Young , Simon Robert Lorrie Everitt , Ronald Knegtel , Joanne Louise Pinder , Alistair Peter Rutherford , Steven Durrant , Guy Brenchley , Jean-Damien Charrier , Michael O'Donnell
发明人： Michael Mortimore , Stephen Clinton Young , Simon Robert Lorrie Everitt , Ronald Knegtel , Joanne Louise Pinder , Alistair Peter Rutherford , Steven Durrant , Guy Brenchley , Jean-Damien Charrier , Michael O'Donnell
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.
摘要翻译： 本发明涉及可用作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。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US07915305B2
公开(公告)日：2011-03-29
申请号：US11656876
申请日：2007-01-23
申请人： Guy Brenchley , Jean-Damien Charrier , Steven Durrant , David Kay , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
发明人： Guy Brenchley , Jean-Damien Charrier , Steven Durrant , David Kay , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
IPC分类号： A61K31/38
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinase represented by formula (I): or a pharmaceutically acceptable salt thereof. 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. The invention also provides processes for preparing compounds of the inventions.
摘要翻译： 本发明涉及可用作由式（I）表示的蛋白激酶抑制剂的化合物或其药学上可接受的盐。 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。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US20090286840A1
公开(公告)日：2009-11-19
申请号：US11786579
申请日：2007-04-12
申请人： Guy Brenchley , Steven Durrant , Jean-Damien Charrier , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
发明人： Guy Brenchley , Steven Durrant , Jean-Damien Charrier , Ronald Knegtel , Sharn Ramaya , Shazia Sadiq
IPC分类号： A61K31/4178 , C07D409/04 , A61K31/4155 , A61P35/00 , A61P25/00 , A61P29/00 , A61P3/10
CPC分类号： C07D409/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.
摘要翻译： 本发明涉及可用作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。 本发明还提供了制备本发明化合物的方法。
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