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100 条记录 (耗时 0.048 秒)

    3,4-diaryl thiopenes and analogs thereof having use as antiinflammatory agents
    92.
    发明授权
    3,4-diaryl thiopenes and analogs thereof having use as antiinflammatory agents 失效
    具有用作抗炎剂的3,4-二芳基呋喃及其类似物

    公开(公告)号：US06599934B1

    公开(公告)日：2003-07-29

    申请号：US09711737

    申请日：2000-11-13

    申请人： John J. Talley ,  Stephen R Bertenshaw ,  Paul W Collins ,  Thomas D. Penning ,  David B. Reitz ,  Roland S Rogers

    发明人： John J. Talley ,  Stephen R Bertenshaw ,  Paul W Collins ,  Thomas D. Penning ,  David B. Reitz ,  Roland S Rogers

    IPC分类号： C07D30702

    CPC分类号： C07D307/38 ,  A61K31/341 ,  A61K31/365 ,  C07D307/58 ,  C07D333/16 ,  C07D333/18 ,  C07D333/28 ,  C07D333/38 ,  C07D409/04

    摘要： A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R2 and R3 are independently aryl or heteroaryl; and wherein R2 and R3 are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 一类3,4-二芳基取代的噻吩，呋喃和吡咯衍生物及其类似物，含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。 特别感兴趣的化合物由式I定义：其中Y选自O，S和NR1; 其中R1选自氢和低级烷基; 其中X是一个或两个选自氢，卤素，低级烷氧基羰基和羧基的取代基; 其中R2和R3独立地是芳基或杂芳基; 并且其中R2和R3任选在可取代的位置被一个或多个选自磺酰胺基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

    Substituted pyrazoles for the treatment of inflammation
    96.
    发明授权
    Substituted pyrazoles for the treatment of inflammation 失效
    用于治疗炎症的取代的吡唑

    公开(公告)号：US5580985A

    公开(公告)日：1996-12-03

    申请号：US535688

    申请日：1995-09-28

    申请人： Len F. Lee ,  Thomas D. Penning ,  Steven W. Kramer

    发明人： Len F. Lee ,  Thomas D. Penning ,  Steven W. Kramer

    IPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/505 ,  A61P19/02 ,  A61P25/04 ,  A61P29/00 ,  C07D231/12 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06

    CPC分类号： C07D231/12

    摘要： A class of pyrazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, alkenyl, aralkyl, alkynyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl, arylaminocarbonylalkyl, heterocyciicalkyl, and alkoxycarbonylalkyl; wherein R.sup.3 is aryl substituted at a substitutable position with halo; wherein R.sup.4 is selected from hydrido and haloalkyl; and wherein R.sup.5 is selected from alkyl and amino; or a pharmaceutically-acceptable salt or prodrug thereof.

    摘要翻译： 描述了一类吡唑基化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式II定义：其中R 1选自氢，烷基，烯基，芳烷基，炔基，氰基烷基，羧基烷基，氨基羰基烷基，芳基氨基羰基烷基，杂环烷基和烷氧基羰基烷基; 其中R3是在可取代的位置被卤素取代的芳基; 其中R 4选自氢和卤代烷基; 并且其中R 5选自烷基和氨基; 或其药学上可接受的盐或前药。

    3,4-substituted pyrazoles for the treatment of inflammation
    99.
    发明授权
    3,4-substituted pyrazoles for the treatment of inflammation 失效
    用于治疗炎症的3,4-取代的吡唑

    公开(公告)号：US5486534A

    公开(公告)日：1996-01-23

    申请号：US278297

    申请日：1994-07-21

    申请人： Len F. Lee ,  Thomas D. Penning ,  Steven W. Kramer

    发明人： Len F. Lee ,  Thomas D. Penning ,  Steven W. Kramer

    IPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/505 ,  A61P19/02 ,  A61P25/04 ,  A61P29/00 ,  C07D231/12 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

    CPC分类号： C07D231/12

    摘要： A class of pyrazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, alkenyl, aralkyl, alkynyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl, arylaminocarbonylalkyl, heterocyclicalkyl, and alkoxycarbonylalkyl; wherein R.sup.3 is aryl substituted at a substitutable position with halo; wherein R.sup.4 is selected from hydrido and haloalkyl; and wherein R.sup.5 is selected from alkyl and amino; or a pharmaceutically-acceptable salt or prodrug thereof.

    摘要翻译： 描述了一类吡唑基化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式II定义：其中R 1选自氢，烷基，烯基，芳烷基，炔基，氰基烷基，羧基烷基，氨基羰基烷基，芳基氨基羰基烷基，杂环烷基和烷氧基羰基烷基; 其中R3是在可取代的位置被卤素取代的芳基; 其中R 4选自氢和卤代烷基; 并且其中R 5选自烷基和氨基; 或其药学上可接受的盐或前药。

    Alkoxy-substituted dihydrobenzopyran-2-carboxylic acids and derivatives thereof
    100.
    发明授权
    Alkoxy-substituted dihydrobenzopyran-2-carboxylic acids and derivatives thereof 失效
    烷氧基取代的二氢苯并吡喃-2-羧酸及其衍生物

    公开(公告)号：US5212198A

    公开(公告)日：1993-05-18

    申请号：US958632

    申请日：1992-10-09

    申请人： Stevan W. Djuric ,  Thomas D. Penning ,  James P. Snyder

    发明人： Stevan W. Djuric ,  Thomas D. Penning ,  James P. Snyder

    IPC分类号： C07D405/12 ,  C07D413/12 ,  C07D417/12

    CPC分类号： C07D405/12 ,  C07D413/10 ,  C07D417/12

    摘要： This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or (CH.sub.2).sub.m R.sup.3 whereR.sup.3 is cycloalkyl and m is 1 or 2;R.sup.1 is alkyl;R.sup.2 is hydrogen or alkyl;R.sup.4 is alkyl;n is an integer from 1 to 5;p is an integer from 0 to 6;Y is NH, oxygen or sulfur; andZ is hydrogen, alkyl, alkoxy, NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen or alkyl, or SR.sup.6 wherein R.sup.6 is hydrogen, benzyl or alkyl.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in the treatment of leukotriene B.sub.4 mediated conditions.

    摘要翻译： 本发明涉及式I化合物及其立体异构体和药学上可接受的盐，其中R是烷基，烯基，炔基或（CH 2）m R 3，其中R 3是环烷基，m是1或2; R1是烷基; R2是氢或烷基; R4是烷基; n为1〜5的整数; p是0至6的整数; Y是NH，氧或硫; 并且Z是氢，烷基，烷氧基，NR4R5，其中R4和R5独立地是氢或烷基，或SR6，其中R6是氢，苄基或烷基。 式I化合物是白三烯B4拮抗剂，可用作抗炎剂和治疗白三烯B4介导的病症。