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1. 发明授权

US07960415B2 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：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。

2. 发明申请

US20060160862A1 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：US20060160862A1
公开(公告)日：2006-07-20
申请号：US11284366
申请日：2005-11-21
申请人： Jean-Damien Charrier , Ronald Knegtel , Michael Mortimore , John Studley
发明人： Jean-Damien Charrier , Ronald Knegtel , Michael Mortimore , John Studley
IPC分类号： A61K31/4439 , A61K31/4412 , C07D401/02 , C07D211/72
CPC分类号： C07D213/75 , C07D211/72 , C07D401/02 , C07D401/06 , C07D409/06
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 preparting 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， R 5和R 5如本文所定义。本发明还提供了使用这样的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用于制备本发明化合物的方法。

3. 发明授权

US08071618B2 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：US08071618B2
公开(公告)日：2011-12-06
申请号：US12562277
申请日：2009-09-18
申请人： Jean Damien Charrier , Michael Mortimore , John Studley
发明人： Jean Damien Charrier , Michael Mortimore , John Studley
IPC分类号： C07D217/24 , A61K31/472
CPC分类号： C07D401/12 , C07D217/24 , C07D405/12 , C07D417/12
摘要： The present invention provides a compound of formula I: wherein: X is —OR1 or —N(R5)2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R1 is: C1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or alkynyl is optionally substituted with optionally substituted aryl, CF3, CI, F, OMe, OEt, OCF3, CN, or NMe2;C1-6 cycloalkyl, wherein 1-2 carbon atoms in the cycloalkyl is optionally replaced with —O— or —NR5—; R2 is C1-6 straight chained or branched alkyl; Art Unit 1625 R3 is hydrogen, halo, OCF3, CN, or CF3; R4 is hydrogen, halo, OCF3, CN, or CF3; and each R5 is independently H, C1-6 straight chained or branched alkyl, aryl, —O—C1-6 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.
摘要翻译：本发明提供式I化合物：其中：X为-OR1或-N（R5）2，Y为卤素，三氟苯氧基或四氟苯氧基; R 1为：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，Cl，F，OMe，OEt，OCF 3，CN或NMe 2取代; 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; R2是C1-6直链或支链烷基; Art Unit 1625 R3是氢，卤素，OCF 3，CN或CF 3; R4是氢，卤素，OCF3，CN或CF3; 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。

4. 发明授权

US07875712B2 Caspase inhibitors and uses thereof 有权
标题翻译：胱天蛋白酶抑制剂及其用途
公开(公告)号：US07875712B2
公开(公告)日：2011-01-25
申请号：US12235820
申请日：2008-09-23
申请人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
发明人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
IPC分类号： C07J43/00
CPC分类号： A61K31/55 , A61K31/4015 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/45 , A61K31/498 , A61K31/5025 , A61K31/538 , A61K31/54 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
摘要翻译：本发明提供了式I的半胱天冬酶抑制剂：其中Z是氧或硫; R1是氢，-CHN2，R，CH2OR，CH2SR或-CH2Y; R3和R4之间代表单键或双键; 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; R3是能够适应胱天蛋白酶的S2亚位点的基团; R4是氢或C1-6烷基或R3和R4一起形成环; 环A和环B各自为杂环，R和R 5如说明书所述。这些化合物是有效的凋亡抑制剂和IL-1和bgr; 分泌。

5. 发明授权

US07442790B2 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：US07442790B2
公开(公告)日：2008-10-28
申请号：US11770093
申请日：2007-06-28
申请人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
发明人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
IPC分类号： C07J43/00
CPC分类号： A61K31/55 , A61K31/4015 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/45 , A61K31/498 , A61K31/5025 , A61K31/538 , A61K31/54 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
摘要翻译：本发明提供了式I的半胱天冬酶抑制剂：其中Z是氧或硫; R 1是氢，-CHN 2，R 2，CH 2 OR，CH 2 SR或-CH 2 Y; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”6.35mm“file =”US07442790-20081028-P00001.TIF“alt =”custom character“img-content =”character“img-format R 3和R 4之间的=“tif”/>表示单键或双键; 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; R 3是能够适应半胱天冬酶的S2亚位点的基团; R 4是氢或C 1-6烷基或R 3和R 4合在一起形成环 ; 环A和环B各自是杂环，R和R 5如说明书中所述。这些化合物是凋亡和IL-1β分泌的有效抑制剂。

6. 发明申请

US20110144074A1 CASPASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译： CASPASE抑制剂及其用途
公开(公告)号：US20110144074A1
公开(公告)日：2011-06-16
申请号：US13012180
申请日：2011-01-24
申请人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
发明人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
IPC分类号： A61K31/58 , A61K31/405 , A61K31/5415 , A61K31/473 , A61K31/55 , A61K31/496 , A61K31/437 , A61K31/5025 , A61K31/538 , A61K31/498 , A61K31/45 , A61K31/4015 , A61P29/00 , A61P31/00 , A61P19/02 , A61P3/10 , A61P37/06 , A61P35/00 , A61P25/28 , A01N1/02 , C12N5/071
CPC分类号： A61K31/55 , A61K31/4015 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/45 , A61K31/498 , A61K31/5025 , A61K31/538 , A61K31/54 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
摘要翻译：本发明提供了式I的半胱天冬酶抑制剂：其中Z是氧或硫; R1是氢，-CHN2，R，CH2OR，CH2SR或-CH2Y; R3和R4之间代表单键或双键; 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; R3是能够适应胱天蛋白酶的S2亚位点的基团; R4是氢或C1-6烷基或R3和R4一起形成环; 环A和环B各自为杂环，R和R 5如说明书所述。这些化合物是有效的凋亡抑制剂和IL-1和bgr; 分泌。

7. 发明授权

US07652153B2 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：US07652153B2
公开(公告)日：2010-01-26
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： A61K31/401 , A61K31/403 , A61K31/4025 , C07D207/09 , C07D209/02
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 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.
摘要翻译：本发明提供式I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。

8. 发明申请

US20090215736A1 CASPASE INHIBITORS AND USES THEREOF 有权
标题翻译： CASPASE抑制剂及其用途
公开(公告)号：US20090215736A1
公开(公告)日：2009-08-27
申请号：US12235820
申请日：2008-09-23
申请人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
发明人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
IPC分类号： A61K31/58 , A61K31/403 , C07D209/56 , A61K31/5415 , C07D279/18 , A61K31/473 , C07D221/12 , A61K31/55 , C07D223/18 , A61K31/496 , C07D403/02 , C07J43/00 , A61K31/4439 , C07D471/02 , A61K31/444 , C07D471/12 , A61K31/502 , C07D237/26 , A61K31/542 , C07D513/02 , A61K31/536 , C07D265/38 , A61K31/498 , C07D241/46 , A61K31/445 , A61K31/40 , C07D211/00 , C07D207/00 , A61P35/00 , A61P37/00
CPC分类号： A61K31/55 , A61K31/4015 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/45 , A61K31/498 , A61K31/5025 , A61K31/538 , A61K31/54 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
摘要翻译：本发明提供了式I的半胱天冬酶抑制剂：其中Z是氧或硫; R1是氢，-CHN2，R，CH2OR，CH2SR或-CH2Y; R3和R4之间代表单键或双键; 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; R3是能够适应胱天蛋白酶的S2亚位点的基团; R4是氢或C1-6烷基或R3和R4一起形成环; 环A和环B各自为杂环，R和R 5如说明书所述。这些化合物是凋亡和IL-1β分泌的有效抑制剂。

9. 发明申请

US20080015172A1 CASPASE INHIBITORS AND USES THEREOF 失效
标题翻译： CASPASE抑制剂及其用途
公开(公告)号：US20080015172A1
公开(公告)日：2008-01-17
申请号：US11770093
申请日：2007-06-28
申请人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
发明人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
IPC分类号： A61K31/403 , A61K31/404 , A61K31/407 , A61K31/437 , A61K31/495 , A61K31/502 , A61K31/538 , A61K31/5415 , A61K31/55 , A61K31/58 , A61P1/00 , A61P11/00 , A61P13/12 , A61P17/00 , A61P19/02 , A61P25/00 , A61P3/10 , A61P31/00 , A61P35/00 , A61P37/00 , A61P43/00 , A61P9/00 , C07D209/04 , C07D209/82 , C07D219/00 , C07D221/02 , C07D221/12 , C07D223/14 , C07D237/26 , C07D241/36 , C07D279/18 , C07D295/00 , C07J43/00
CPC分类号： A61K31/55 , A61K31/4015 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/45 , A61K31/498 , A61K31/5025 , A61K31/538 , A61K31/54 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
摘要翻译：本发明提供了式I的半胱天冬酶抑制剂：其中Z是氧或硫; R 1是氢，-CHN 2，R 2，CH 2 OR，CH 2 SR或-CH 2 Y; R 3和R 4之间代表单键或双键; 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; R 3是能够适应半胱天冬酶的S2亚位点的基团; R 4是氢或C 1-6烷基或R 3和R 4合在一起形成环 ; 环A和环B各自是杂环，R和R 5如说明书中所述。这些化合物是凋亡和IL-1β分泌的有效抑制剂。

10. 发明授权

US07351702B2 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：US07351702B2
公开(公告)日：2008-04-01
申请号：US10153971
申请日：2002-05-23
申请人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
发明人： Michael Mortimore , Andrew Miller , John Studley , Jean-Damien Charrier
IPC分类号： A01N31/55 , A61K31/55
CPC分类号： A61K31/55 , A61K31/4015 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/45 , A61K31/498 , A61K31/5025 , A61K31/538 , A61K31/54 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： This invention provides compounds of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; next to R3 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion.
摘要翻译：本发明提供式I化合物：其中Z是氧或硫; R 1是氢，-CHN 2，R 2，CH 2 OR，CH 2 SR或-CH 2 Y; “img id =”CUSTOM-CHARACTER-00001“he =”1.78mm“wi =”6.01mm“file =”US07351702-20080401-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/> R 3旁边代表单键或双键; 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; R 3是能够适应半胱天冬酶的S2亚位点的基团; R 4是氢或C 1-6烷基或R 3和R 4合在一起形成环 ; 环A和环B各自是杂环，R和R 5如说明书中所述。这些化合物是凋亡和IL-1β分泌的有效抑制剂。

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