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    Phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives
    6.
    发明授权
    Phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives 失效
    苯基乙腈烷基氨基烷基邻位取代的芳基化合物作为免疫抑制剂

    公开(公告)号：US06451852B2

    公开(公告)日：2002-09-17

    申请号：US09766722

    申请日：2001-01-22

    申请人： Chi-Dean Liang ,  John P. McKearn ,  John M. Farah, Jr. ,  Richard A. Mueller

    发明人： Chi-Dean Liang ,  John P. McKearn ,  John M. Farah, Jr. ,  Richard A. Mueller

    IPC分类号： A61K31277

    CPC分类号： C07C255/43

    摘要： A class of substituted phenylacetonitrile-alkylaminoalkyl-ortho-substituted aryl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula wherein m is one or two; wherein n is a number selected from one to five, inclusive; wherein R1 is selected from hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkenyl and alkynyl; wherein R6 is selected from loweralkyl; wherein each of R8, R9, R10 and R12 through R16 is independently selected from hydrido, hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; with the proviso that at least one of R12 and R16 must be selected from hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类具有免疫抑制特性的取代的苯基乙腈 - 烷基氨基烷基邻位取代的芳基化合物。 该类化合物可用于减少移植器官的受体排斥和治疗自身免疫性或炎性疾病。 特别感兴趣的化合物是一种或两种; 其中n是选自1至5的数字，包括1和5; 其中R1选自氢化，烷基，羟基烷基，环烷基，环烷基烷基，烷氧基烷基，烯基和炔基; 其中R 6选自低级烷基; 其中R8，R9，R10和R12至R16各自独立地选自氢，羟基，烷基，羟基烷基，烷氧基，烯基，炔基，烷基羰基，烷氧基羰基，烷基羰基烯基，烷基氨基羰基和烷氧基烷基; 条件是R12和R16中的至少一个必须选自羟基，烷基，羟烷基，烷氧基，烯基，炔基，烷基羰基，烷氧基羰基，烷基羰基烯基，烷基氨基羰基和烷氧基烷基; 或其互变异构体或其药学上可接受的盐。

    Method of using phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives
    8.
    发明授权
    Method of using phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives 失效
    使用苯乙腈烷基氨基烷基邻位取代的芳基化合物作为免疫抑制剂的方法

    公开(公告)号：US5486539A

    公开(公告)日：1996-01-23

    申请号：US204121

    申请日：1994-03-01

    申请人： Chi-Dean Liang ,  John P. McKearn ,  John M. Farah, Jr. ,  Richard A. Mueller

    发明人： Chi-Dean Liang ,  John P. McKearn ,  John M. Farah, Jr. ,  Richard A. Mueller

    IPC分类号： C07C255/43 ,  A61K31/275

    CPC分类号： C07C255/43

    摘要： A class of substituted phenylacetonitrile-alkylaminoalkyl-ortho-substituted aryl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein m is one or two; wherein n is a number selected from one to five, inclusive; wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkenyl and alkynyl; wherein R.sup.6 is selected from loweralkyl; wherein each of R.sup.8, R.sup.9, R.sup.10 and R.sup.12 through R.sup.16 is independently selected from hydrido, hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; with the proviso that at least one of R.sup.12 and R.sup.16 must be selected from hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类具有免疫抑制特性的取代的苯基乙腈 - 烷基氨基烷基邻位取代的芳基化合物。 该类化合物可用于减少移植器官的受体排斥和治疗自身免疫性或炎性疾病。 特别感兴趣的化合物具有下式：其中m是一个或两个; 其中n是选自1至5的数字，包括1和5; 其中R1选自氢化，烷基，羟基烷基，环烷基，环烷基烷基，烷氧基烷基，烯基和炔基; 其中R 6选自低级烷基; 其中R8，R9，R10和R12至R16各自独立地选自氢，羟基，烷基，羟基烷基，烷氧基，烯基，炔基，烷基羰基，烷氧基羰基，烷基羰基烯基，烷基氨基羰基和烷氧基烷基; 条件是R12和R16中的至少一个必须选自羟基，烷基，羟烷基，烷氧基，烯基，炔基，烷基羰基，烷氧基羰基，烷基羰基烯基，烷基氨基羰基和烷氧基烷基; 或其互变异构体或其药学上可接受的盐。