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    • 1. 发明授权
    • Quinazoline derivatives and pharmaceutical compositions containing them
    • 喹唑啉衍生物和含有它们的药物组合物
    • US08586608B2
    • 2013-11-19
    • US12563340
    • 2009-09-21
    • Frank HimmelsbachElke LangkopfStefan BlechBirgit JungAnke BaumFlavio Solca
    • Frank HimmelsbachElke LangkopfStefan BlechBirgit JungAnke BaumFlavio Solca
    • A61K31/47A01N43/42
    • C07D405/12C07D239/94
    • A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
    • 通式I的化合物,其中:R a是苄基,1-苯乙基或3-氯-4-氟苯基; Rb是二甲基氨基,N-甲基-N-乙基氨基,二乙基氨基,N-甲基-N-异丙基氨基,N-甲基-N-环丙基氨基,N-甲基-N-(2-甲氧基乙基)氨基,N-乙基-N- (2-甲氧基乙基)氨基,双(2-甲氧基乙基)氨基,吗啉代,N-甲基-N-(四氢呋喃-3-基)氨基,N-甲基-N-(四氢呋喃-2-基甲基)氨基,N - 甲基-N-(四氢呋喃-3-基甲基)氨基,N-甲基-N-(四氢吡喃-4-基)氨基或N-甲基-N-(四氢吡喃-4-基甲基)氨基; Rc为环丙基甲氧基,环丁氧基,环戊氧基,四氢呋喃-3-基氧基,四氢呋喃-2-基甲氧基,四氢呋喃-3-基甲氧基,四氢吡喃-4-基氧基或四氢吡喃-4-基甲氧基,或互变异构体,立体异构体或盐 特别是其具有有价值的药理学特性的无机或有机酸或碱的生理上可接受的盐,特别是对由酪氨酸激酶介导的信号转导的抑制作用,它们在治疗疾病尤其是肿瘤疾病和肺疾病中的用途 和气道及其制备。
    • 5. 发明申请
    • METHODS OF TREATING DISEASES USING QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • 使用喹唑啉衍生物和含有它们的药物组合物治疗疾病的方法
    • US20110046168A1
    • 2011-02-24
    • US12914003
    • 2010-10-28
    • Frank HIMMELSBACHElke LANGKOPFStefan BLECHBirgit JUNGAnke BAUMFlavio SOLCA
    • Frank HIMMELSBACHElke LANGKOPFStefan BLECHBirgit JUNGAnke BAUMFlavio SOLCA
    • A61K31/517A61P35/00A61P1/00A61P11/00A61P17/06
    • C07D405/12C07D239/94
    • A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
    • 通式I的化合物,其中:R a是苄基,1-苯乙基或3-氯-4-氟苯基; Rb是二甲基氨基,N-甲基-N-乙基氨基,二乙基氨基,N-甲基-N-异丙基氨基,N-甲基-N-环丙基氨基,N-甲基-N-(2-甲氧基乙基)氨基,N-乙基-N- (2-甲氧基乙基)氨基,双(2-甲氧基乙基)氨基,吗啉代,N-甲基-N-(四氢呋喃-3-基)氨基,N-甲基-N-(四氢呋喃-2-基甲基)氨基,N-甲基 -N-(四氢呋喃-3-基甲基)氨基,N-甲基-N-(四氢吡喃-4-基)氨基或N-甲基-N-(四氢吡喃-4-基甲基)氨基; Rc为环丙基甲氧基,环丁氧基,环戊氧基,四氢呋喃-3-基氧基,四氢呋喃-2-基甲氧基,四氢呋喃-3-基甲氧基,四氢吡喃-4-基氧基或四氢吡喃-4-基甲氧基,或互变异构体,立体异构体或盐 特别是其具有有价值的药理学特性的无机或有机酸或碱的生理上可接受的盐,特别是对由酪氨酸激酶介导的信号转导的抑制作用,它们在治疗疾病尤其是肿瘤疾病和肺疾病中的用途 和气道及其制备。