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31. 发明申请

US20100189773A1 5-CYANO-4- (PYRROLO [2,3] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS 失效
标题翻译：用作蛋白激酶抑制剂的5-氰基-4-（吡咯并[2,3]吡啶-3-基） - 吡啶衍生物
公开(公告)号：US20100189773A1
公开(公告)日：2010-07-29
申请号：US12448489
申请日：2007-12-21
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： A61K9/127 , C07D487/04 , A61K31/506 , A61K31/5377 , A61K31/551 , A61P35/00 , A61P3/10 , A61P7/00 , A61P19/02 , A61P37/00 , A61P35/02 , A61K38/50 , A61K31/565 , A61K38/19 , A61K39/395 , A61K31/7088 , A61K31/661 , A61K33/24 , A61K31/7008 , A61K31/704 , A61K31/7068 , A61K31/69 , A61K38/21 , A61K38/20 , C12N5/00
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。

32. 发明授权

US07829561B2 Caspase inhibitors and uses thereof 失效
标题翻译：胱天蛋白酶抑制剂及其用途
公开(公告)号：US07829561B2
公开(公告)日：2010-11-09
申请号：US12165952
申请日：2008-07-01
申请人： Jean-Damien Charrier , Guy Brenchley
发明人： Jean-Damien Charrier , Guy Brenchley
IPC分类号： C07D487/04 , C07D487/14 , A61K31/5025 , A61K31/4985 , A61P19/02 , A61P39/00
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N═C, C(R3)═C, C(═O)—N, or C(═O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ═O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
摘要翻译：本发明提供了式I的新型胱天蛋白酶抑制剂：其中R1是氢，CHN2，R或-CH2Y; R是脂族基，芳基，芳烷基，杂环基或杂环基烷基; Y是电负离子团; R2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; X2-X1是N（R3）-C（R3），C（R3）2-C（R3），C（R3）2-N，N = C，C（R3）= C，C（= N或C（= O）-C（R3）; 每个R 3独立地选自氢或C 1-6脂族基; 环C是稠合芳环; n为0,1或2; 并且环A中的每个亚甲基任选且独立地被-O或 - 一个或多个卤素，C 1-4烷基或C 1-4烷氧基取代。这些化合物可用于治疗半胱天冬酶介导的疾病。

33. 发明申请

US20110003824A1 Caspase Inhibitors and Uses Thereof 失效
标题翻译：胱天蛋白酶抑制剂及其用途
公开(公告)号：US20110003824A1
公开(公告)日：2011-01-06
申请号：US12883424
申请日：2010-09-16
申请人： Jean-Damien Charrier , Guy Brenchley
发明人： Jean-Damien Charrier , Guy Brenchley
IPC分类号： A61K31/5025 , A01N1/02 , C12N5/071 , A61K31/519 , A61K31/437 , C07D487/04 , C07D471/04 , A61P19/02
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2-X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N═C, C(R3)═C, C(═O)—N, or C(═O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ═O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
摘要翻译：本发明提供了式I的新型胱天蛋白酶抑制剂：其中R1是氢，CHN2，R或-CH2Y; R是脂族基，芳基，芳烷基，杂环基或杂环基烷基; Y是电负离子团; R2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; X2-X1是N（R3）-C（R3），C（R3）2-C（R3），C（R3）2-N，N = C，C（R3）= C，C（= N或C（= O）-C（R3）; 每个R 3独立地选自氢或C 1-6脂族基; 环C是稠合芳环; n为0,1或2; 并且环A中的每个亚甲基任选且独立地被-O或 - 一个或多个卤素，C 1-4烷基或C 1-4烷氧基取代。这些化合物可用于治疗半胱天冬酶介导的疾病。

34. 发明授权

US07968716B2 Caspase inhibitors and uses thereof 失效
标题翻译：胱天蛋白酶抑制剂及其用途
公开(公告)号：US07968716B2
公开(公告)日：2011-06-28
申请号：US12883424
申请日：2010-09-16
申请人： Jean-Damien Charrier , Guy Brenchley
发明人： Jean-Damien Charrier , Guy Brenchley
IPC分类号： C07D487/04 , C07D487/14 , A61K31/5025 , A61K31/4985 , A61P19/02 , A61P39/00
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N═C, C(R3)═C, C(═O)—N, or C(═O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ═O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
摘要翻译：本发明提供了式I的新型胱天蛋白酶抑制剂：其中R1是氢，CHN2，R或-CH2Y; R是脂族基，芳基，芳烷基，杂环基或杂环基烷基; Y是电负离子团; R2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; X2-X1是N（R3）-C（R3），C（R3）2-C（R3），C（R3）2-N，N = C，C（R3）= C，C（= N或C（= O）-C（R3）; 每个R 3独立地选自氢或C 1-6脂族基; 环C是稠合芳环; n为0,1或2; 并且环A中的每个亚甲基任选且独立地被-O或 - 一个或多个卤素，C 1-4烷基或C 1-4烷氧基取代。这些化合物可用于治疗半胱天冬酶介导的疾病。

35. 发明申请

US20090023739A1 CAPASE INHIBITORS AND USES THEREOF 失效
标题翻译：容量抑制剂及其用途
公开(公告)号：US20090023739A1
公开(公告)日：2009-01-22
申请号：US12165952
申请日：2008-07-01
申请人： Jean-Damien Charrier , Guy Brenchley
发明人： Jean-Damien Charrier , Guy Brenchley
IPC分类号： A61K31/5025 , C07D471/04 , A61K31/4985 , C12N5/02 , A61P35/04 , A01N1/02 , A61K31/4375 , C07D471/14
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N═C, C(R3)═C, C(═O)—N, or C(═O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ═O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
摘要翻译：本发明提供了式I的新型胱天蛋白酶抑制剂：其中R1是氢，CHN2，R或-CH2Y; R是脂族基，芳基，芳烷基，杂环基或杂环基烷基; Y是电负离子团; R2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; X2-X1是N（R3）-C（R3），C（R3）2-C（R3），C（R3）2-N，NC，C（R3）-C，C（-O）或C（-O）-C（R 3）; 每个R 3独立地选自氢或C 1-6脂族基; 环C是稠合芳环; n为0,1或2; 环A中的每个亚甲基任选和独立地被-O，或一个或多个卤素，C 1-4烷基或C 1-4烷氧基取代。这些化合物可用于治疗半胱天冬酶介导的疾病。

36. 发明授权

US07407964B2 Caspase inhibitors and uses thereof 失效
标题翻译：胱天蛋白酶抑制剂及其用途
公开(公告)号：US07407964B2
公开(公告)日：2008-08-05
申请号：US09877832
申请日：2001-06-07
申请人： Jean-Damien Charrier , Guy Brenchley
发明人： Jean-Damien Charrier , Guy Brenchley
IPC分类号： C07D487/04 , A61K31/5365 , A61P19/02 , A61P39/06 , A61K31/5025
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N═C, C(R3)═C, C(═O)—N, or C(═O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ═O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
摘要翻译：本发明提供了式I的新型半胱天冬酶抑制剂：其中R 1是氢，CH 2 N 2，R 3或-CH 2 Y; R是脂族基，芳基，芳烷基，杂环基或杂环基烷基; Y是电负离子团; R 2是CO 2 H，CH 2 CO 2 H，或它们的酯，酰胺或等体醇; X 2 -X 1是N（R 3）-C（R 3），C（R 3） C（R 3）2 N 2，-C（R 3）2，C（R 3） -N，NC，C（R 3）C，C（= O）-N或C（-O）-C（R 3））。每个R 3独立地选自氢或C 1-6烷基; 环C是稠合芳环; n为0,1或2; 环A中的每个亚甲基任选且独立地被-O，或一个或多个卤素C 1-4烷基或C 1-4烷氧基取代。这些化合物可用于治疗半胱天冬酶介导的疾病。

37. 发明申请

US20120136000A1 TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS 有权
公开(公告)号：US20120136000A1
公开(公告)日：2012-05-31
申请号：US12670989
申请日：2010-01-27
申请人： Juan-Miguel Jimenez , John Studley , Ronald Knegtel , Luca Settimo , Damien Fraysse , Philip N. Collier , Guy Brenchley , Dean Boyall , Andrew Miller , Heather Twin , Stephen Young
发明人： Juan-Miguel Jimenez , John Studley , Ronald Knegtel , Luca Settimo , Damien Fraysse , Philip N. Collier , Guy Brenchley , Dean Boyall , Andrew Miller , Heather Twin , Stephen Young
IPC分类号： A61K31/496 , A61K31/497 , A61K31/437 , A61K31/506 , A61P37/00 , A61P29/00 , A61P35/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P3/10 , A61P1/00 , A61P37/06 , A61P35/02 , A61P19/04 , C07D471/04
CPC分类号： C07D471/04 , A61K31/496 , A61K31/506 , C07D239/24 , C07D241/10 , C07D519/00
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.

38. 发明授权

US08017619B2 Compositions useful as inhibitors of protein kinases 失效
标题翻译：可用作蛋白激酶抑制剂的组合物
公开(公告)号：US08017619B2
公开(公告)日：2011-09-13
申请号：US12713811
申请日：2010-02-26
申请人： Juan-Miguel Jimenez , Jeremy Green , Huai Gao , Young-Choon Moon , Guy Brenchley , Ronald Knegtel , Francoise Pierard
发明人： Juan-Miguel Jimenez , Jeremy Green , Huai Gao , Young-Choon Moon , Guy Brenchley , Ronald Knegtel , Francoise Pierard
IPC分类号： A01N43/54 , A61K31/505 , C07D491/00
CPC分类号： A61K31/496 , C07D239/70 , C07D239/84 , C07D333/22 , C07D333/38 , C07D333/54 , C07D333/70 , C07D471/04 , C07D487/04 , C07D495/04 , C07D495/14 , C07D513/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供了制备化合物的方法，包含该化合物的药学上可接受的组合物，以及使用该化合物和组合物治疗各种疾病，病症或病症的方法。

39. 发明申请

US20060122213A1 Azaindoles useful as inhibitors of protein kinases 审中-公开
标题翻译：可用作蛋白激酶抑制剂的吖啶酮
公开(公告)号：US20060122213A1
公开(公告)日：2006-06-08
申请号：US11170779
申请日：2005-06-29
申请人： Francoise Pierard , Juan-Miguel Jimenez , Ronald Knegtel , Guy Brenchley , Michael Mortimore , Francesca Mazzei
发明人： Francoise Pierard , Juan-Miguel Jimenez , Ronald Knegtel , Guy Brenchley , Michael Mortimore , Francesca Mazzei
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D471/04
摘要： The present invention relates to compounds useful as 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. The invention also provides processes for preparing the compounds of the invention.
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。

40. 发明申请

US20120183577A1 COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES 失效
标题翻译：作为蛋白激酶抑制剂的组合物
公开(公告)号：US20120183577A1
公开(公告)日：2012-07-19
申请号：US13205291
申请日：2011-08-08
申请人： Juan-Miguel Jimenez , Jeremy Green , Huai Gao , Young-Choon Moon , Guy Brenchley , Ronald Knegtel , Francoise Pierard
发明人： Juan-Miguel Jimenez , Jeremy Green , Huai Gao , Young-Choon Moon , Guy Brenchley , Ronald Knegtel , Francoise Pierard
IPC分类号： A61K39/00 , A61K31/519 , C07D513/04 , A61P7/00 , A61P1/16 , A61P29/00 , A61P19/00 , A61P3/10 , A61P37/00 , A61P37/02 , A61P37/06 , A61K31/5377 , A61P31/12
CPC分类号： A61K31/496 , C07D239/70 , C07D239/84 , C07D333/22 , C07D333/38 , C07D333/54 , C07D333/70 , C07D471/04 , C07D487/04 , C07D495/04 , C07D495/14 , C07D513/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供了制备化合物的方法，包含该化合物的药学上可接受的组合物，以及使用该化合物和组合物治疗各种疾病，病症或病症的方法。

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