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    Quinoline derivatives which are 5-hydroxytryptamine antagonists
    3.
    发明授权
    Quinoline derivatives which are 5-hydroxytryptamine antagonists 失效
    喹啉衍生物是5-羟色胺拮抗剂

    公开(公告)号：US4435405A

    公开(公告)日：1984-03-06

    申请号：US382116

    申请日：1982-05-26

    申请人： Thomas P. Blackburn ,  Barry Cox ,  Allen J. Guildford ,  David J. Le Count ,  Robert J. Pearce ,  Craig W. Thornber

    发明人： Thomas P. Blackburn ,  Barry Cox ,  Allen J. Guildford ,  David J. Le Count ,  Robert J. Pearce ,  Craig W. Thornber

    IPC分类号： A61K31/47 ,  A61P25/08 ,  A61P43/00 ,  C07C233/11 ,  C07D211/42 ,  C07D215/18 ,  C07D215/36 ,  C07D277/28 ,  C07D333/24 ,  C07D401/04 ,  C07D401/12 ,  C07D409/04 ,  C07D417/04 ,  C07F7/08

    CPC分类号： C07D211/42 ,  C07C233/11 ,  C07D215/18 ,  C07D215/36 ,  C07D277/28 ,  C07D333/24 ,  C07F7/0812

    摘要： Compounds of the formula: ##STR1## wherein A stands for the radical --(CH.sub.2).sub.2 -- which may bear one or two defined substituents; R.sup.1 stands for a (3-4C) alkyl or cyclopropyl radical, or a phenyl radical which may optionally bear one or two defined substituents, or a heteroaryl radical of five or six ring atoms which may optionally bear a (1-3C)alkyl substituent; R.sup.2 and R.sup.3 stand for hydrogen or a (1-2C)alkyl radical, or R.sup.2 stands for a (2-4C)alkylene radical which is linked to one of the carbon atoms forming the two-carbon-atom-backbone of A so as to form, together with the adjacent nitrogen atom, a pyrrolidinyl or piperidyl radical; and one of R.sup.4 and R.sup.5 stands for hydrogen, and the other stands for hydrogen, a halogen atom or a (1-3C)alkyl or (1-3C)alkoxy radical; and acid-addition salts thereof. Processes for the manufacture of said compounds. Pharmaceutical compositions comprising one of said compounds and a pharmaceutical diluent or carrier. The compounds are 5-hydroxytryptamine antagonists.

    摘要翻译： 下式的化合物：其中A代表可具有一个或两个限定取代基的 - （CH 2）2 - 基团; R1代表（3-4C）烷基或环丙基，或可任选地带有一个或两个限定取代基的苯基或五或六个环原子的杂芳基，其可任选地带有（1-3C）烷基取代基 ; R2和R3代表氢或（1-2C）烷基，或R2代表（2-4C）亚烷基，其连接到形成A的双碳原子骨架的碳原子之一，以便 与相邻的氮原子一起形成吡咯烷基或哌啶基; R4和R5之一代表氢，另一个代表氢，卤原子或（1-3C）烷基或（1-3C）烷氧基; 及其酸加成盐。 用于制备所述化合物的方法。 药物组合物，其包含所述化合物之一和药物稀释剂或载体。 该化合物是5-羟色胺拮抗剂。

    Morpholine derivatives
    4.
    发明授权
    Morpholine derivatives 失效
    吗啉衍生物

    公开(公告)号：US4088814A

    公开(公告)日：1978-05-09

    申请号：US735125

    申请日：1976-10-22

    申请人： Bernard J. McLoughlin ,  Allen J. Guildford

    发明人： Bernard J. McLoughlin ,  Allen J. Guildford

    IPC分类号： C07D265/30 ,  C07D265/32 ,  C07F9/6533

    CPC分类号： C07D265/30 ,  C07D265/32 ,  C07F9/6533

    摘要： Morpholine derivatives, typically those of the formula: ##STR1## wherein A is an ethylene or vinylene radical and X is a phenyl radical optionally substituted by one or two substituents selected from halogen atoms, alkyl and alkoxy radicals of 1 to 6 carbon atoms and aryloxy radicals of 1 to 6 carbon atoms, the aryloxy radicals themselves being optionally substituted by one or two substituents selected from halogen atoms and alkyl radicals of 1 to 4 carbon atoms, and the pharmaceutically-acceptable acid-addition salts thereof. Processes for making these compounds, pharmaceutical compositions containing them and a method of restoring to normal abnormal mental states in warm-blooded animals are also disclosed.

    摘要翻译： 吗啉衍生物，通常是下式的那些：其中A是乙烯或亚乙烯基，X是任选地被一个或两个选自卤素原子，1-6个碳原子的烷基和烷氧基的取代基取代的苯基和芳氧基 1至6个碳原子的基团，芳氧基本身任选被一个或两个选自卤素原子和1-4个碳原子的烷基的取代基取代，及其药物上可接受的酸加成盐。 还公开了制备这些化合物的方法，含有它们的药物组合物和在温血动物中恢复正常的异常精神状态的方法。