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    • 3. 发明授权
    • Halogenated phenylacetonitrile alkylaminoalkylphenyl compounds as
immunosuppressives
    • 卤代苯乙腈烷基氨基烷基苯基化合物作为免疫抑制剂
    • US5451604A
    • 1995-09-19
    • US97809
    • 1993-07-26
    • Richard A. MuellerThomas E. BartaJohn P. McKearnSusan A. GregoryRichard A. PartisFrancis J. Koszyk
    • Richard A. MuellerThomas E. BartaJohn P. McKearnSusan A. GregoryRichard A. PartisFrancis J. Koszyk
    • C07C255/42A61K31/275C07C247/06C07C255/35
    • C07C255/42C07C2101/10
    • 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.
    • 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。