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49 条记录 (耗时 0.041 秒)

    Carbamate caspase inhibitors and uses thereof
    2.
    发明授权
    Carbamate caspase inhibitors and uses thereof 失效
    氨基甲酸酯半胱天冬酶抑制剂及其用途

    公开(公告)号：US06689784B2

    公开(公告)日：2004-02-10

    申请号：US09821161

    申请日：2001-03-29

    申请人： David Bebbington ,  Ronald Knegtel ,  Michael Mortimore ,  David Kay ,  Julian M. C. Golec

    发明人： David Bebbington ,  Ronald Knegtel ,  Michael Mortimore ,  David Kay ,  Julian M. C. Golec

    IPC分类号： C07D20982

    CPC分类号： C07D403/12 ,  C07D209/08 ,  C07D209/86 ,  C07D221/12 ,  C07D223/26 ,  C07D223/28 ,  C07D279/30

    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; 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 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1&bgr; 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 1，CH 2 OR，CH 2 SR或-CH 2 Y; Y是电负离子团; R 2是CO 2 H，CH 2 CO 2 H或其酯，酰胺或等体积体; R 3是能够适应半胱天冬酶的S2亚位点的基团; R 4和R 5与中间的氮一起形成杂环，R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。

    Caspase inhibitors and uses thereof
    3.
    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：US07053057B2

    公开(公告)日：2006-05-30

    申请号：US09863649

    申请日：2001-05-23

    申请人： Julian M. C. Golec ,  David Bebbington ,  Guy Brenchley ,  Ronald Knegtel ,  Michael Mortimore

    发明人： Julian M. C. Golec ,  David Bebbington ,  Guy Brenchley ,  Ronald Knegtel ,  Michael Mortimore

    IPC分类号： A61K38/05 ,  C07K5/078

    CPC分类号： C07D401/12 ,  C07D211/60 ,  C07D215/48 ,  C07D409/12

    摘要： This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2, R, or —CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R3 is hydrogen, an optionally substituted C1-6 alkyl, F2, CN, aryl or R3 is attached to Ar to form an unsaturated or partially saturated five or six membered fused ring having 0–2 heteroatoms. The compounds are useful for treating caspase-mediated diseases in mammals.

    摘要翻译： 本发明提供了具有下式的半胱天冬酶抑制剂：其中环A是任选取代的哌啶，四氢喹啉或四氢异喹啉环; R 1是氢，CHN 2，R或-CH 2 Y; R是选自脂族基团，芳基，芳烷基，杂环基或杂环基烷基的任选取代的基团; 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; Ar是任选取代的芳基; 和R 3是氢，任选取代的C 1-6烷基，F 2，CN，芳基或R 3， SUP>与Ar连接形成不饱和或部分饱和的具有0-2个杂原子的五元或六元稠环。 该化合物可用于治疗哺乳动物中半胱天冬酶介导的疾病。