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    • 8. 发明申请
    • CYANOPYRROLE CONTAINING CYCLIC CARBAMATE AND THIOCARBAMATE BIARYLS AND METHODS FOR PREPARING THE SAME
    • 含有环状碳酸酯和硫代氨基甲酸酯的CYANOPYRROLE及其制备方法
    • WO2005105739A2
    • 2005-11-10
    • PCT/US2005/014342
    • 2005-04-25
    • WYETHWILK, Bogdan, Kazimierz
    • WILK, Bogdan, Kazimierz
    • C07D207/00
    • C07D413/04C07D207/34
    • Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided: Formula (I) Z are the same or different and are H, optionally substituted C 1 to C 6 alkyl, or COR A ; R A is H, optionally substituted C 1 to C 6 alkyl, optionally substituted C 1 to C 6 alkoxy, or optionally substituted C 1 to C 6 aminoalkyl; Q are the same or different and are H, OH, NH 2 , CN, halogen, optionally substituted C 1 to C 6 alkyl, optionally substituted C 1 to C 6 alkenyl, optionally substituted C 1 to C 6 alkynyl, optionally substituted C 1 to C 6 alkoxy, optionally substituted C 1 to C 6 aminoalkyl, or COR B ; and R B is H, optionally substituted C 1 to C 6 alkyl, optionally substituted C 1 to C 6 alkoxy, or optionally substituted C 1 to C 6 aminoalkyl. Compounds including 2-amino-5-(5-cyano-l-methyl-1H-pyrrol-2-yl) benzoic acid methyl ester, 5-[4-amino-3-(1-hydroxy-l-methyl-ethyl)-phenyl]-1-methyl-1H-pyrrole-2-carbonitrile, and 2-amino-5-(5-cyano-1-methyl-lH-pyrrol-2-yl)-phenyl-ethanone, or pharmaceutically acceptable salts thereof, and the uses thereof are also provided.
    • 提供了含有氰基吡咯部分和下式的环状氨基甲酸酯和硫代氨基甲酸酯的方法:式(I)Z相同或不同,为H,任选取代的C 1至C 6烷基或COR A; 任选取代的C 1 -C 6烷基,任选取代的C 1至C 6烷氧基或任选取代的C 1至C 6氨基烷基; Q相同或不同,为H,OH,NH 2,CN,卤素,任选取代的C 1至C 6烷基,任选取代的C 1至C 6烯基,任选取代的C 1至C 6炔基,任选取代的C 1至C 6烷氧基, C6氨基烷基或CORB; 和R B是H,任选取代的C 1 -C 6烷基,任选取代的C 1 -C 6烷氧基或任选取代的C 1至C 6氨基烷基。 包括2-氨基-5-(5-氰基-1-甲基-1H-吡咯-2-基)苯甲酸甲酯,5- [4-氨基-3-(1-羟基-1-甲基 - 乙基) - 苯基] -1-甲基-1H-吡咯-2-甲腈和2-氨基-5-(5-氰基-1-甲基-1H-吡咯-2-基) - 苯基 - 乙酮或其药学上可接受的盐 ,并提供其用途。