Thiophene derivatives
    1.
    发明授权
    Thiophene derivatives 失效
    噻吩衍生物

    公开(公告)号:US5571810A

    公开(公告)日:1996-11-05

    申请号:US422545

    申请日:1995-04-13

    摘要: This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsubstituted lower alkenyl, acyl, nitro, substituted or unsubstituted amino, sulfo, substituted or unsubstituted sulfamoyl, N-containing heterocyclicsulfonyl, hydoxy, substituted or unsubstituted heterocyclic group,R.sup.2 is substituted or unsubstituted aryl, andR.sup.3 is substituted or unsubstituted aryl, provided that R.sup.3 is aryl substituted with substituent(s) selected from the group consisting of amino, mono(lower)-alkylamino, acylamino, lower alkyl(acyl)amino and sulfamoyl when R.sup.1 is hydrogen, halogen or cyano, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.

    摘要翻译: 本发明涉及具有抗炎和止痛活性的新噻吩衍生物,由通式[I]表示:其中R 1是氢,卤素,氰基,取代的低级烷基,取代或未取代的低级烯基,酰基,硝基 取代或未取代的氨基,磺基,取代或未取代的氨磺酰基,含N杂环基磺酰基,羟基,取代或未取代的杂环基,R2为取代或未取代的芳基,R3为取代或未取代的芳基,条件是R3为被取代基取代的芳基 s)选自氨基,单(低级) - 烷基氨基,酰氨基,低级烷基(酰基)氨基和氨磺酰基,当R 1为氢时,卤素或氰基,及其药学上可接受的盐,其制备方法和 包含其的药物组合物。

    Imidazole compounds
    10.
    发明授权
    Imidazole compounds 失效
    咪唑化合物

    公开(公告)号:US06359145B1

    公开(公告)日:2002-03-19

    申请号:US09764995

    申请日:2001-03-09

    IPC分类号: C07D23366

    摘要: Imidazole compounds having adenosine deaminase inhibitory activity represented by formula (I) wherein R1 is hydrogen, hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s); R2 is hydrogen or lower alkyl; R3 is hydroxy or protected hydroxy; R4 is cyano, (hydroxy)iminoamino(lower)alkyl, carboxy, protected carboxy, heterocyclic group optionally substituted with amino, or carbamoyl optionally substituted with suitable substituent(s); and —A— is —Q— or —O—Q—, wherein Q is single bond or lower alkylene, provided that when R2 is lower alkyl, then R1 is hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s), its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.

    摘要翻译: 式(I)表示的具有腺苷脱氨酶抑制活性的咪唑化合物,其中R 1为氢,羟基,保护的羟基或任选被合适的取代基取代的芳基; R2是氢或低级烷基; R3是羟基或被保护的羟基; R4是氰基,(羟基)亚氨基氨基(低级)烷基,羧基,受保护的羧基,任选被氨基取代的杂环基或任选被合适的取代基取代的氨基甲酰基; 并且-A-是-Q-或-OQ-,其中Q是单键或低级亚烷基,条件是当R 2是低级烷基时,则R 1是羟基,保护的羟基或任选地被合适的取代基取代的芳基,其 前药或其盐。 该化合物可用于治疗和/或预防腺苷有效的疾病。