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    7-phenyl-1, 4-diazepane compounds, process for their preparation, and pharmaceutical compositions containing them
    2.
    发明授权
    7-phenyl-1, 4-diazepane compounds, process for their preparation, and pharmaceutical compositions containing them 有权
    7-苯基-1,4-二氮杂环丁烷化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：US6040303A

    公开(公告)日：2000-03-21

    申请号：US141312

    申请日：1998-08-27

    申请人： Samuel David ,  Jochen Antel ,  Reinhard Brueckner ,  Dieter Ziegler ,  Christian Eeckhout ,  Gerhard-Wilhelm Bielenberg ,  Michael Peck

    发明人： Samuel David ,  Jochen Antel ,  Reinhard Brueckner ,  Dieter Ziegler ,  Christian Eeckhout ,  Gerhard-Wilhelm Bielenberg ,  Michael Peck

    IPC分类号： A61K31/55 ,  A61P1/00 ,  A61P43/00 ,  C07D243/08

    CPC分类号： C07D243/08 ,  Y02P20/55

    摘要： Neurokinin-antagonistic compounds corresponding to formula I: ##STR1## in which R.sup.1 is hydrogen or lower alkyl,R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, andR.sup.3 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, orR.sup.2 and R.sup.3 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring,R.sup.4 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, andR.sup.5 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, orR.sup.4 and R.sup.5 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring,R.sup.6 is lower alkyl, halogen or trifluoromethyl,R.sup.7 is lower alkyl, halogen or trifluoromethyl,A is a --(CH.sub.2).sub.n -- group in which n represents an integer from 1 to 3, or an --NH--(CH.sub.2).sub.m -- group in which m represents an integer from 2 to 3, andB is an alkylene chain with 1 to 3 carbon atoms optionally substituted by lower alkyl,and physiologically acceptable salts thereof and processes for the preparation of these compounds.

    摘要翻译： 对应于式I的神经激肽拮抗化合物：其中R1是氢或低级烷基，R2是氢，低级烷基，低级烷氧基，卤素或三氟甲基，R3是氢，低级烷基，低级烷氧基，卤素或三氟甲基，或R2和 R3一起是具有1至2个碳原子的亚烷基二氧基，与苯环的相邻碳原子键合，R4是氢，低级烷基，低级烷氧基，卤素或三氟甲基，R5是氢，低级烷基，低级烷氧基，卤素或三氟甲基， 或R4和R5一起是具有1至2个碳原子的亚烷基二氧基，与苯环的相邻碳原子键合，R6是低级烷基，卤素或三氟甲基，R7是低级烷基，卤素或三氟甲基，A是 - （CH2）n - 其中n表示1至3的整数的基团，或其中m表示2至3的整数的-NH-（CH 2）m - 基团，B是具有1至3个碳原子的亚烷基链，其任选被 低级烷基和其生理上可接受的盐 d制备这些化合物的方法。