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    • 1. 发明授权
    • N-(pyridinylalkyl)-thieno-or benzo-isothiazol-3-amine derivatives
    • N-(吡啶基烷基) - 噻吩并或苯并异噻唑-3-胺衍生物
    • US4743692A
    • 1988-05-10
    • US913876
    • 1986-09-30
    • Daniel M. TellerDonald P. StrikeArthur A. SantilliGuy A. Schiehser
    • Daniel M. TellerDonald P. StrikeArthur A. SantilliGuy A. Schiehser
    • C07D417/12C07D513/04
    • C07D417/12C07D513/04
    • A compound of the formula: ##STR1## in which A is a 3,4-; 3,2-; or 2,3-fused thieno- moiety or a benzo- moiety;X is alkylene of 2 to 5 carbon atoms;R.sup.1 is hydrogen, bromo or methyl;R.sup.2 is methoxy when R.sup.1 is hydrogen, methyl when R.sup.1 is bromo, and bromo when R.sup.1 is methyl;R.sup.3 is hydrogen or alkyl of 1 to 6 carbon atoms;R.sup.4 is hydrogen or alkyl of 1 to 6 carbon atoms;R.sup.3 and R.sup.4, taken together, are ethylene when X is ethylene;R.sup.5 is hydrogen when A is thieno, and when A is benzo, R.sup.5 is hydrogen, alkyl of 1 to 6 carbon atoms, halo or alkoxy of 1 to 6 carbon atoms;R.sup.6 is hydrogen when A is thieno, and when A is benzo, R.sup.5 is hydrogen, alkyl of 1 to 6 carbon atoms, halo, alkoxy of 1 to 6 carbon atoms, amino, nitro, sulfamoyl or pyridinyl;m is one of the integers 0 or 1;n is one of the integers 3, 4 or 5;p is one of the integers 0, 1 or 2; andthe dotted line in the thiazole ring represents unsaturation necessary to complete the 3,2- or 2,3- thieno- ring;or a pharmaceutically acceptable salt thereof are histamine H.sub.1 -antagonists useful in the treatment of various allergic reactions in the mammal.
    • 下式的化合物:其中A是3,4-; 3,2; 或2,3-稠合的噻吩并 - 部分或苯并 - 部分; X是2至5个碳原子的亚烷基; R1是氢,溴或甲基; 当R 1为氢时,R 2为甲氧基,当R 1为溴时,R 2为甲基; R3是氢或1至6个碳原子的烷基; R4是氢或1至6个碳原子的烷基; 当X是亚乙基时,R 3和R 4一起是乙烯; 当A为噻吩并且当A为苯甲基时,R 5为氢,R 5为氢,1至6个碳原子的烷基,卤素或1至6个碳原子的烷氧基; 当A为噻吩并且当A为苯甲基时,R 6为氢,R 5为氢,1至6个碳原子的烷基,卤素,1至6个碳原子的烷氧基,氨基,硝基,氨磺酰基或吡啶基; m是整数0或1之一; n是整数3,4或5之一; p是整数0,1或2之一; 并且噻唑环中的虚线表示完成3,2-或2,3-噻吩环所必需的不饱和键; 或其药学上可接受的盐是用于治疗哺乳动物各种过敏反应的组胺H1拮抗剂。