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42 条记录 (耗时 0.059 秒)

    Caspase inhibitors and uses thereof
    12.
    发明授权
    Caspase inhibitors and uses thereof 失效
    胱天蛋白酶抑制剂及其用途

    公开(公告)号：US07553852B2

    公开(公告)日：2009-06-30

    申请号：US10609147

    申请日：2003-06-27

    申请人： Ronald Knegtel ,  Michael Mortimore ,  John Studley ,  David Millan

    发明人： Ronald Knegtel ,  Michael Mortimore ,  John Studley ,  David Millan

    IPC分类号： A01N43/42 ,  C07D215/12

    CPC分类号： C07D239/90 ,  C07D217/24

    摘要： The present invention relates to compounds of formula I: useful as inhibitors of caspases. The present invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for preparing the compounds, and methods of using the compounds and compositions in the treatment of various diseases, conditions, or disorders.

    摘要翻译： 本发明涉及式I化合物：可用作半胱天冬酶的抑制剂。 本发明还提供包含所述化合物的药学上可接受的组合物，制备化合物的方法，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。

    Caspase inhibitors and uses thereof
    15.
    发明授权
    Caspase inhibitors and uses thereof 失效
    胱天蛋白酶抑制剂及其用途

    公开(公告)号：US08129381B2

    公开(公告)日：2012-03-06

    申请号：US12464380

    申请日：2009-05-12

    申请人： Ronald Knegtel ,  Michael Mortimore ,  John Studley ,  David Millan

    发明人： Ronald Knegtel ,  Michael Mortimore ,  John Studley ,  David Millan

    IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D239/72

    CPC分类号： C07D239/90 ,  C07D217/24

    摘要： The present invention relates to compounds of formula I: useful as inhibitors of caspases. The present invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for preparing the compounds, and methods of using the compounds and compositions in the treatment of various diseases, conditions, or disorders.

    摘要翻译： 本发明涉及式I化合物：可用作半胱天冬酶的抑制剂。 本发明还提供包含所述化合物的药学上可接受的组合物，制备化合物的方法，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。

    Caspase inhibitors and uses thereof
    16.
    发明授权
    Caspase inhibitors and uses thereof 失效
    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。

    Caspase inhibitors and uses thereof
    18.
    发明授权
    Caspase inhibitors and uses thereof 有权
    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。

    Caspase inhibitors and uses thereof
    20.
    发明授权
    Caspase inhibitors and uses thereof 失效
    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。