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    • 14. 发明授权
    • Substituted 4-amino-7H-pyrrolo [2,3,-d]-pyrimidines as PTK inhibitors
    • 取代的4-氨基-7H-吡咯并[2,3,-d] - 嘧啶作为PTK抑制剂
    • US6001839A
    • 1999-12-14
    • US42702
    • 1998-03-17
    • David J. CalderwoodDavid N. JohnstonPaul RaffertyHelen L. TwiggerRainer MunschauerLee Arnold
    • David J. CalderwoodDavid N. JohnstonPaul RaffertyHelen L. TwiggerRainer MunschauerLee Arnold
    • A61K31/519A61P35/00A61P37/02A61P43/00C07D487/04A61K31/505
    • C07D487/04
    • Compounds of formula I ##STR1## including pharmaceutically acceptable salts thereof in which R.sub.1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C.sub.1-6 alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.5-7 cycloalkenyl group or an (optionally substituted phenyl)C.sub.1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula OR.sub.A in which R.sub.A represents H or a C.sub.1-6 alkyl group provided that a group of formula OR.sub.A is not located on the carbon attached to nitrogen;R.sub.2 represents hydrogen, a C.sub.1-6 alkyl group, a C.sub.3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C.sub.1-6 alkyl group, optionally substituted phenyl or R.sub.4 ; andR.sub.3 represents a group of formula (a) ##STR2## in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO.sub.2, SO.sub.2 NH, a C.sub.1-4 alkylene chain, NHCO, NHCO.sub.2, CONH, NHCONH, CO.sub.2 or S(O).sub.p in which p is 0, 1 or 2, or A is absent and R.sub.5 is attached directly to the phenyl ring;and R.sub.5 represents optionally substituted phenyl and, additionally, when A is absent R.sub.5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl;R.sub.4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.
    • 式I化合物,其包括其药学上可接受的盐,其中R 1表示氢,2-苯基-1,3-二恶烷-5-基,C 1-6烷基,C 3-8环烷基,C 5-7环烯基或 (任选取代的苯基)C 1-6烷基,其中烷基,环烷基和环烯基任选被一个或多个RAA代表H或C 1-6烷基的式ORA基团取代,条件是式ORA基团为 不位于附着在氮上的碳上; R 2表示氢,C 1-6烷基,C 3-8环烷基,卤素,羟基,(任选取代的苯基)C 1-6烷基,任选取代的苯基或R 4; 并且R 3表示式(a)的基团,其中苯环另外被任意取代,A代表NH,O,NHSO 2,SO 2 NH,C 1-4亚烷基链,NHCO,NHCO 2,CONH,NHCONH,CO 2或S )p,其中p是0,1或2,或A不存在,R 5直接连接到苯环上; 并且另外,当A不存在时,R 5表示a)任选被卤素取代的苯二甲酰亚氨基,或b)吡唑基氨基,其中吡唑环任选被一个或多个下述取代基取代:羟基或任选地 取代的苯基; R4表示杂环基; 被描述为可用于治疗哺乳动物免疫系统的增殖性疾病和病症。 还描述了制备这些化合物的方法和含有这些化合物的药物组合物。