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    • 4. 发明授权
    • Pyrazolo(3,4-d)pyrimidine compounds, compositions and method of use
    • 吡唑并(3,4-d)嘧啶化合物,组合物和使用方法
    • US4904666A
    • 1990-02-27
    • US181729
    • 1988-04-14
    • Walter-Gunar FriebeWolfgang KampeOtto-Henning Wilhelms
    • Walter-Gunar FriebeWolfgang KampeOtto-Henning Wilhelms
    • A61K31/505A61K31/519A61P11/08A61P11/16A61P29/00A61P37/08C07D487/04
    • C07D487/04
    • The present invention provides pyrazolo[3,4-d]-pyrimidines of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 to C.sub.6 -alkyl radical, a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aryl radical, R.sub.2 is a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aralkyl or hetaralkyl radical with 1 to 6 carbon atoms in the alkyl moiety and substituted, if desired, one or more times by halogen, C.sub.1 to C.sub.6 -alkyl, hydroxyl, C.sub.1 to C.sub.6 -alkoxy, C.sub.1 to C.sub.3 -haloalkyl, C.sub.3 to C.sub.7 -alkoxy carbonyl, aminocarbonyl, C.sub.2 to C.sub.7 -alkylaminocarbonyl, C.sub.3 to C.sub.13 -dialkylaminocarbonyl, cyano or C.sub.1 to C.sub.6 -alkylthio and R.sub.3 is a hydrogen atom or a C.sub.2 to C.sub.6 -alkyl radical substituted, if desired, one or more times by hydroxyl or is a tetrahydrofuranyl or tetrahydropyranyl radical, with the proviso that R.sub.2 cannot be an unsubstituted benzyl radical when R.sub.1 is a methyl radical, and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
    • 本发明提供通式如下的吡唑并[3,4-d] - 嘧啶:其中R 1为C 1至C 6 - 烷基,C 2至C 6链烯基,C 3至C 7环烷基 基团或芳基,R 2是C 2至C 6 - 烯基,C 3至C 7 - 环烷基或在烷基部分具有1至6个碳原子的芳烷基或杂烷基,如果需要, 卤素,C1至C6烷基,羟基,C1至C6烷氧基,C1至C3-卤代烷基,C3至C7-烷氧基羰基,氨基羰基,C2至C7-烷基氨基羰基,C3至C13-二烷基氨基羰基,氰基或C1至C6-烷硫基 并且R 3是氢原子或C 2至C 6烷基如果需要,被羟基取代一次或多次,或者是四氢呋喃基或四氢吡喃基,条件是当R 1是甲基时,R 2不能是未被取代的苄基 ,以及其与无机和有机酸的生理上可接受的盐。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。