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175 条记录 (耗时 0.08 秒)

    Caspase inhibitors and uses thereof
    23.
    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：US07517987B2

    公开(公告)日：2009-04-14

    申请号：US10166437

    申请日：2002-06-10

    申请人： Julian M. C. Golec ,  Paul S. Charifson ,  Jean-Damien Charrier ,  Hayley Binch

    发明人： Julian M. C. Golec ,  Paul S. Charifson ,  Jean-Damien Charrier ,  Hayley Binch

    IPC分类号： C07D215/38

    CPC分类号： C07D209/48 ,  C07D209/46 ,  C07D213/64 ,  C07D215/227 ,  C07D217/24 ,  C07D239/36 ,  C07D239/80 ,  C07D239/88 ,  C07D239/90 ,  C07D471/04 ,  C07D495/04

    摘要： This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.

    摘要翻译： 本发明提供可用作半胱天冬酶抑制剂的新化合物及其药学上可接受的衍生物。 这些化合物具有通式I：其中R 1，R 2和R 3如本文所述，环A包含0至2个双键，每个X独立地选自氮或碳，环A中的至少一个X为氮， 环A如所述任选被取代，并且可以与含有0至3个杂原子的饱和或不饱和的5至7元环稠合，并且条件是当X 3是碳时，X 3上的取代基被除氮以外的原子连接。

    Pyrazole compounds useful as protein kinase inhibitors
    26.
    发明授权
    Pyrazole compounds useful as protein kinase inhibitors 失效
    用作蛋白激酶抑制剂的吡唑化合物

    公开(公告)号：US06638926B2

    公开(公告)日：2003-10-28

    申请号：US09953505

    申请日：2001-09-14

    申请人： Robert J. Davies ,  Pan Li ,  Jean-Damien Charrier ,  David Bebbington

    发明人： Robert J. Davies ,  Pan Li ,  Jean-Damien Charrier ,  David Bebbington

    IPC分类号： C07D40312

    CPC分类号： C07D401/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

    摘要： This invention provides novel pyrazole compounds that are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3. The compounds may be used to treat abnormal physiological function leading to diseases such as cancer, diabetes and Alzheimer's disease. The compounds are represented by formula VI: wherein G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Ry is T—R3′; T is a valence bond or a C1-4 alkylidene chain; R3′ is an optionally substituted group selected from C1-6 aliphatic, C3-10 carbocyclyl, C6-10 aryl, a heteroaryl ring having 5-10 ring atoms, or a heterocyclyl ring having 5-10 ring atoms; and R1, R2, and R2′ are as described in the specification.

    摘要翻译： 本发明提供了可用作蛋白激酶抑制剂的新型吡唑化合物，特别是作为极光-2和GSK-3的抑制剂。 该化合物可用于治疗导致癌症，糖尿病和阿尔茨海默病等疾病的异常生理功能。 化合物由式VI表示：其中G是环C或环D; 环C选自苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基或1,2,4-三嗪基，其中所述环C具有一个或两个独立地选自-R 1的邻位取代基; 环D是选自芳基，杂芳基，杂环基或碳环基的5-7元单环或8-10元双环; R y是T-R 3; T是价键或C 1-4亚烷基链; R 3是任选取代的基团，其选自C 1-6脂族基，C 3-10碳环基，C 6-10芳基，具有5-10个环原子的杂芳基环，或具有5-10个环原子的杂环基环; 和R 1，R 2和R 2'如说明书中所述。