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25 条记录 (耗时 0.04 秒)

    Lactam derivatives
    11.
    发明授权
    Lactam derivatives 失效

    公开(公告)号：US5013733A

    公开(公告)日：1991-05-07

    申请号：US485532

    申请日：1990-02-27

    申请人： Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North ,  Thomas Miller ,  Anthony D. Baxter ,  Kevin I. Hammond

    发明人： Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North ,  Thomas Miller ,  Anthony D. Baxter ,  Kevin I. Hammond

    IPC分类号： C07D453/02 ,  A61K31/435 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P43/00 ,  C07D519/00

    CPC分类号： C07D519/00

    摘要： The invention provides lactam derivatives of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.3, --COR.sup.3, --CONR.sup.3 R.sup.4 or --SO.sub.2 R.sup.3 (wherein R.sup.3 and R.sup.4, which may be the same or different each represents a hydrogen atom, a C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl group, or a phenyl or phenylC.sub.1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R.sup.3 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.3 or --SO.sub.2 R.sup.3);and R.sup.2 represents a group of formula (a), (b) or (c): ##STR2## wherein R.sup.5 represents a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl or phenylC.sub.1-3 alkyl group;n represents 2, 3 or 4;Q represents a hydrogen or a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy or C.sub.1-6 alkyl group or a group --NH.sup.6 R.sup.7 or --CONR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.3-4 alkenyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring); and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.3 receptors and are useful, for example in the treatment of psychotic disorders, anxiety and nausea and vomiting.

    Lactam derivatives
    12.
    发明授权
    Lactam derivatives 失效

    公开(公告)号：US4985422A

    公开(公告)日：1991-01-15

    申请号：US343359

    申请日：1989-04-26

    申请人： Peter C. North ,  Alexander W. Oxford ,  Ian H. Coates ,  Paul J. Beswick

    发明人： Peter C. North ,  Alexander W. Oxford ,  Ian H. Coates ,  Paul J. Beswick

    IPC分类号： A61K31/435 ,  A61K31/55 ,  A61P43/00 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

    CPC分类号： C07D491/04 ,  C07D495/04

    摘要： Compounds which are potent and selective antagonists of the effect of 5-HT.sub.3 receptors and are useful in the treatment of psychotic disorders, anxiety, and nausea and vomiting, of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula (a), (b) or (c): ##STR2## one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;n represents 1 or 2;Q represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenyl C.sub.1-3 alkoxy or C.sub.1-6 alkyl group, or a group --NR.sup.4 R.sup.5 or --CONR.sup.4 R.sup.5 ; andX represents an oxygen or a sulphur atom, and, when Im represents an imidazolyl group of formula (c), X may also represent the group NR.sup.6, where R.sup.6 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl, C.sub.1-4 alkyl, phenyl, phenyl C.sub.1-3 alkyl, --CO.sub.2 R.sup.7, --COR.sup.7, --CONR.sup.7 R.sup.8 or --SO.sub.2 R.sup.7 ; and physiologically acceptable salts or solvates thereof.

    Indole derivatives
    14.
    发明授权
    Indole derivatives 失效

    公开(公告)号：US5026722A

    公开(公告)日：1991-06-25

    申请号：US366462

    申请日：1989-06-15

    申请人： Alexander W. Oxford ,  Peter C. North ,  David J. Cavalla

    发明人： Alexander W. Oxford ,  Peter C. North ,  David J. Cavalla

    IPC分类号： A61K31/415 ,  A61P43/00 ,  C07D403/12

    CPC分类号： C07D403/12

    摘要： The invention relates to indole derivatives of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl or phenylC.sub.1-3 alkyl;R.sup.2 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-7 cycloalkyl, phenyl or phenylC.sub.1-3 alkyl;X represents an oxygen atom or the group NR.sup.3 (where R.sup.3 represents a hydrogen atom or a C.sub.1-6 alkyl group);one of the groups represented by R.sup.4, R.sup.5 and R.sup.6 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Q represents a hydrogen or a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy or C.sub.1-6 alkyl group or a group -NR.sup.7 R.sup.8 or -CONR.sup.7 R.sup.8 (wherein R.sup.7 and R.sup.8, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.3-4 alkenyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring);and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.

    Ketone derivatives
    16.
    发明授权
    Ketone derivatives 失效
    酮衍生物

    公开(公告)号：US5019586A

    公开(公告)日：1991-05-28

    申请号：US440880

    申请日：1989-11-24

    申请人： Alexander W. Oxford ,  Peter C. North

    发明人： Alexander W. Oxford ,  Peter C. North

    IPC分类号： C07D233/54 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06

    CPC分类号： C07D233/64 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06

    摘要： The present invention provides ketones of the general formula (I): ##STR1## and physiologically acceptable salts and solvates thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a C.sub.1-6 alkyl group;Im represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.3, R.sup.4 and R.sup.5 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and p0 A is a group of the formula (a), (b), (c), (d), (e), (f) or (g): ##STR3## and when A is the group (g), the group --COCR.sup.1 R.sup.2 CH.sub.2 Im is attached at the 2- or 4- position of the indole moiety.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety and nausea and vomiting.

    摘要翻译： 本发明提供通式（I）的酮：其中R 1和R 2可以相同或不同，表示氢原子或C 1-6烷基 组; Im表示下式的咪唑基：其中，由R 3，R 4和R 5表示的基团之一是氢原子或C 1-6烷基，C 3-7环烷基，C 3-6烯基，苯基或苯基C 1-3烷基， 可以相同或不同的其它两个基团表示氢原子或C 1-6烷基; （a），（b），（c），（d），（e），（f）或（g）中的一个基团：（a） （c）<图像>（d）（e）（f）（g），当A是组（g）时，组-COCR1R2CH2Im被附加在2-或 吲哚部分的4-位。 这些化合物是5-HT在5-HT 3受体上的作用的有效和选择性拮抗剂，可用于例如治疗精神病，焦虑和恶心和呕吐。