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16 条记录 (耗时 0.026 秒)

    Pharmaceutically active pyridinyl substituted 5,7-dihydropyrrolo-[3,2-f]benzoxazole-6-ones
    8.
    发明授权
    Pharmaceutically active pyridinyl substituted 5,7-dihydropyrrolo-[3,2-f]benzoxazole-6-ones 失效
    取代5,7-二氢吡喃并（3,2-F）苯并噻唑-6-酮的药物活性吡啶基

    公开(公告)号：US5057526A

    公开(公告)日：1991-10-15

    申请号：US327827

    申请日：1989-03-23

    申请人： Wolfgang von der Saal ,  Rainer Haag

    发明人： Wolfgang von der Saal ,  Rainer Haag

    IPC分类号： A61K31/42 ,  A61P37/00 ,  C07D498/04

    CPC分类号： C07D498/04

    摘要： Compounds of the formula I ##STR1## wherein R is a hydrogen atom or an alkyl radical, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or a cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl or hydrazinocarbonyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a cycloalkyl ring, X is a valency bond or an alkylene or vinylene radical, R.sub.3 is an aromatic heterocyclic five-membered ring containing 1 to 4 heteroatoms or pyridinyl which the five- and six-membered rings are optionaly substituted one or more times by alkyl, alkoxy, alkoxycarbonyl, carboxyl, alkylthio, hydroxyl, nitro, amino, halogen or cyano and the tautomers, optically-active forms and physiologically acceptable salts thereof with inorganic and organic acids.These compounds are useful for treatment of immunological disorders or autoimmune diseases such as aids/ARC, rheumatoid arthritis, lupus erythematosus and to suppress rejection reactions after organ/tissue transplants.

    摘要翻译： 式I的化合物其中R为氢原子或烷基，R 1为氢原子或烷基，烯基或环烷基，R 2为氢原子或烷基，烯基，烷基羰基， 烷氧基羰基，氨基羰基或肼基羰基或R 1和R 2与它们所连接的碳原子一起形成环烷基环，X是价键或亚烷基或亚乙烯基，R 3是含有1个 至4个杂原子或吡啶基，其中五和六元环任选被烷基，烷氧基，烷氧基羰基，羧基，烷硫基，羟基，硝基，氨基，卤素或氰基取代一次或多次，互变异构体，光学活性形式和 其生理上可接受的盐与无机和有机酸形成。 这些化合物可用于治疗免疫疾病或自身免疫疾病如艾滋病/ ARC，类风湿性关节炎，红斑狼疮，并抑制器官/组织移植后的排斥反应。

    Imidazolidine derivatives as immunosuppressives
    10.
    发明授权
    Imidazolidine derivatives as immunosuppressives 失效
    咪唑烷衍生物作为免疫抑制剂

    公开(公告)号：US4996219A

    公开(公告)日：1991-02-26

    申请号：US448129

    申请日：1989-12-13

    申请人： Christos Tsaklakidis ,  Elmar Bosies ,  Michael Schultz ,  Rainer Haag ,  Dieter Herrmann ,  Wulf Pahlke

    发明人： Christos Tsaklakidis ,  Elmar Bosies ,  Michael Schultz ,  Rainer Haag ,  Dieter Herrmann ,  Wulf Pahlke

    IPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/4427 ,  A61P37/06 ,  C07D233/96 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06

    CPC分类号： C07D401/06 ,  C07D233/96 ,  C07D405/06 ,  C07D409/06

    摘要： The present invention provides compounds of the general formulae: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are hydrogen atoms or C.sub.1 -C.sub.5 -alkyl radicals, C.sub.3 -C.sub.5 -alkenyl radicals or phenyl radicals or, together with the carbon atom to which they are attached, form a saturated or unsaturated C.sub.3 -C.sub.7 ring, R.sub.3 and R.sub.4, which can be the same or different, are hydrogen atoms, straight-chained or branched C.sub.1 -C.sub.10 -alkyl radicals, straight-chained or branched C.sub.3 -C.sub.7 -alkenyl radicals, C.sub.3 -C.sub.7 -cycloalkyl radicals, C.sub.3 -C.sub.7 -cycloalkenyl radicals, phenyl, arylalkyl or hetarylalkyl radicals, R.sub.5 is a hydrogen atom or a lower alkyl radical and X is an oxygen or sulphur atom or an imino group.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions with immunosuppressive action containing them.

    摘要翻译： 本发明提供以下通式的化合物：其中R 1和R 2可相同或不同，为氢原子或C 1 -C 5 - 烷基，C 3 -C 5 - 烯基或苯基，或与 它们连接的碳原子形成饱和或不饱和的C 3 -C 7环，可以相同或不同的R 3和R 4是氢原子，直链或支链C 1 -C 10 - 烷基，直链 或支链C 3 -C 7 - 烯基，C 3 -C 7环烷基，C 3 -C 7 - 环烯基，苯基，芳烷基或杂芳基烷基，R 5是氢原子或低级烷基，X是氧或硫原子或 亚氨基组。 本发明还提供了制备这些化合物的方法，以及含有它们的具有免疫抑制作用的药物组合物。