Immunosuppressive effects of administration of a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor
    2.
    发明授权
    Immunosuppressive effects of administration of a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor 失效
    施用环氧合酶-2抑制剂和5-脂肪氧合酶抑制剂的免疫抑制作用

    公开(公告)号:US07132441B2

    公开(公告)日:2006-11-07

    申请号:US10098644

    申请日:2002-03-15

    IPC分类号: A61K31/415 A61K31/34

    摘要: This invention is in the field of a combination comprising a therapeutically-effective amount of a cyclooxygenase-2 inhibitor, a 5-lipoxygenase inhibitor and an immunosuppressive drug selected from antiproliferative agents, antiinflammatory-acting compounds and inhibitors of leukocyte activation. This combination may be used, for example, to suppress the immune response associated with organ transplantation, graft versus host disease, and conditions with underlying autoimmune or inflammatory reactivities or responses.

    摘要翻译: 本发明涉及包含治疗有效量的环加氧酶-2抑制剂,5-脂氧合酶抑制剂和选自抗增生剂,抗炎作用化合物和白细胞活化抑制剂的免疫抑制药物的组合领域。 这种组合可以用于例如抑制与器官移植相关的免疫应答,移植物抗宿主病和具有潜在的自身免疫或炎性反应性或反应的病症。

    Halogenated phenylacetonitrile alkylaminoalkylphenyl compounds as
immunosuppressives
    3.
    发明授权
    Halogenated phenylacetonitrile alkylaminoalkylphenyl compounds as immunosuppressives 失效
    卤代苯乙腈烷基氨基烷基苯基化合物作为免疫抑制剂

    公开(公告)号:US5451604A

    公开(公告)日:1995-09-19

    申请号:US97809

    申请日:1993-07-26

    CPC分类号: C07C255/42 C07C2101/10

    摘要: A class of halogenated phenylacetonitrile alkylaminoalkylphenyl 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 a number selected from three to five, inclusive; wherein n one or two; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein each of R.sup.3 through R.sup.7 is selected from hydrido, fluoro, chloro, bromo, azide, trifluoromethyl, difluorochloromethyl, 1,1-difluoroethyl, 2,2,2-trifluoroethyl, perfluoroethyl and 2,2,2,3-tetrafluoropropyl; with the proviso that at least one of R.sup.3 through R.sup.7 is selected from fluoro and trifluoromethyl; 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卤代苯基乙腈烷基氨基烷基苯基化合物。 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是选自三至五的数字,包括端值; 其中n个或两个; 其中R1选自甲基,乙基,正丙基,异丙基,正丁基,仲丁基,叔丁基,异丁基,正戊基,异戊基,环丙基,环丁基,环戊基,环己基,环丙基甲基,环丁基甲基,环戊基甲基 ,环己基甲基,苄基和苯乙基; 其中R2选自甲基,乙基,正丙基,异丙基,正丁基,仲丁基,叔丁基,异丁基,正戊基,异戊基,环丙基,环丁基,环戊基,环己基,环丙基甲基,环丁基甲基,环戊基甲基 ,环己基甲基,苄基和苯乙基; 其中R3至R7各自选自氢,氟,氯,溴,叠氮化物,三氟甲基,二氟氯甲基,1,1-二氟乙基,2,2,2-三氟乙基,全氟乙基和2,2,2,3-四氟丙基; 条件是R3至R7中的至少一个选自氟和三氟甲基; 或其互变异构体或其药学上可接受的盐。

    Phenylacetonitrilehydroxyalkylaminoalkyl-ortho-substituted aryl
compounds as immunosuppressives
    6.
    发明授权
    Phenylacetonitrilehydroxyalkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives 失效
    苯基乙腈 - 羟基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:US5247119A

    公开(公告)日:1993-09-21

    申请号:US889733

    申请日:1992-05-28

    IPC分类号: C07C255/43

    CPC分类号: C07C255/43

    摘要: A class of substituted phenylacetonitrilehydroxyalkylaminoalkyl-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 each of m and n is a number independently 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; 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苯乙腈羟烷基氨基烷基邻位取代芳基化合物。 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式“IMAGE”,其中m和n各自独立地选自1至5个,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; 或其互变异构体或其药学上可接受的盐。