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68 条记录 (耗时 0.073 秒)

    Modulators of p38 MAP kinase
    61.
    发明授权
    Modulators of p38 MAP kinase 失效
    p38 MAP激酶的调节剂

    公开(公告)号：US06537996B2

    公开(公告)日：2003-03-25

    申请号：US09792876

    申请日：2001-02-23

    申请人： David J. Morgans, Jr. ,  Silke Thode ,  Dongxu Sun

    发明人： David J. Morgans, Jr. ,  Silke Thode ,  Dongxu Sun

    IPC分类号： A61K31506

    CPC分类号： C07D213/78 ,  C07D239/28

    摘要： Compounds of formula 1 are effective modulators of p38 MAP kinase. wherein R1 is H, lower alkyl, or OR5, where R5 is aryl, heterocyclyl, acyl, N—R6-4-piperidinyl, N—R6-4-piperidinylmethyl, or N—R6-4-pipelidinylethyl, where aryl and heterocyclyl are substituted with 1-3 R6 substituents selected from the group consisting of H, lower alkyl, lower alkenyl, OH, NO2, NH2, halo, trihalomethyl, —CN, SH, SO, SO2, SO3H, —OR, —COR, —COOR, —CONHR, —OCOR, and —NCOR, where R is lower alkyl; R2 is H or lower alkyl; R3 is aryl substituted with 1-3 R6 substituents; R4 is H, lower alkyl, aryl, aralkyl, —OH, —NH2, —NHR, or —OR, where R is lower alkyl or aryl-lower alkyl; and A is —CH— or —N—; and pharmaceutically acceptable salts thereof.

    摘要翻译： 式1的化合物是p38MAP激酶的有效调节剂，其中R1是H，低级烷基或OR5，其中R5是芳基，杂环基，酰基，N-R6-4-哌啶基，N-R6-4-哌啶基甲基或N R 6 4-哌啶基乙基，其中芳基和杂环基被1-3个选自H，低级烷基，低级烯基，OH，NO 2，NH 2，卤素，三卤代甲基，-CN，SH，SO， SO 2，SO 3 H，-OR，-COR，-COOR，-CONHR，-OCOR和-NCOR，其中R是低级烷基; R2是H或低级烷基; R3是被1-3个R6取代基取代的芳基; R4是H，低级烷基，芳基，芳烷基，-OH，-NH2，-NHR或-OR，其中R是低级烷基或芳基 - 低级烷基; A是-CH-或-N-; 及其药学上可接受的盐。

    Heterocyclic sulfonamides
    66.
    发明授权
    Heterocyclic sulfonamides 有权
    杂环磺酰胺

    公开(公告)号：US08101620B2

    公开(公告)日：2012-01-24

    申请号：US13008432

    申请日：2011-01-18

    申请人： Bradley Paul Morgan ,  Fady Malik ,  Erica Anne Kraynack ,  Alexander Ramon Muci ,  Xiangping Qian ,  David J. Morgans, Jr.

    发明人： Bradley Paul Morgan ,  Fady Malik ,  Erica Anne Kraynack ,  Alexander Ramon Muci ,  Xiangping Qian ,  David J. Morgans, Jr.

    IPC分类号： A61K31/4965 ,  A61K31/41

    CPC分类号： C07D295/26 ,  C07D207/14 ,  C07D213/75 ,  C07D233/88 ,  C07D257/06 ,  C07D261/14 ,  C07D263/48 ,  C07D277/46 ,  C07D285/135 ,  C07D295/18 ,  C07D403/12

    摘要： Provided is a compound of the following formula: wherein: R3 is an aryl or heteroaryl group, which is optionally substituted with a halogen, lower alkoxy, aryl or heteroaryl group; R4 is halogen; R5 is hydrogen, halogen, hydroxy, or lower alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxy, and lower alkyl; and R8 is hydrogen, alkyl, halogen, hydroxy, alkoxy, alkylenedioxy, carboxy, acyloxy, alkoxycarbonyl, alkoxycarbonylamino, alkylcarbonylamino, aminocarbonyl, aminocarbonylamino, cyano, acyl, oxo, nitro, amino, sulfanyl, sulfinyl, sulfonyl, aminosulfonyl, amidino, phenyl, benzyl, heteroaryl, heterocyclyl, aryloxy, arallkoxy, heteroaryloxy, or heteroaralkoxy, wherein the amino(s) in the alkoxycarbonylamino, alkylcarbonylamino, aminocarbonyl, aminocarbonylamino, amino, or aminosulfonyl is optionally substituted with alkyl; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明提供下式的化合物：其中：R3是芳基或杂芳基，其任选被卤素，低级烷氧基，芳基或杂芳基取代; R4是卤素; R5是氢，卤素，羟基或低级烷基; R6和R7独立地选自氢，卤素，羟基和低级烷基; 氨基羰基，氨基羰基氨基，氰基，酰基，氧代，硝基，氨基，硫烷基，亚磺酰基，磺酰基，氨基磺酰基，脒基，苯基 烷氧基羰基氨基，烷基羰基氨基，氨基羰基，氨基羰基氨基，氨基或氨基磺酰基中的氨基任选被烷基取代; 或其药学上可接受的盐。