利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

25 条记录 (耗时 0.027 秒)

    Tetrahydro-1H-pyrido[4,3-b]indol-1-one derivatives
    11.
    发明授权
    Tetrahydro-1H-pyrido[4,3-b]indol-1-one derivatives 失效
    四氢-1H-吡啶并[4,3-b]吲哚-1-酮衍生物

    公开(公告)号：US5360800A

    公开(公告)日：1994-11-01

    申请号：US741570

    申请日：1991-08-07

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

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

    IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D401/06 ,  A61K31/44 ,  A61K31/55

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The invention relates to tricyclic lactams 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, phenyl C.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl or phenoxymethyl,one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 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 alkhyl group;n represents 2 or 3; 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.

    摘要翻译： 本发明涉及通式（I）的三环内酰胺（I）其中Im表示下式的咪唑基，R1表示氢原子或选自C1-6烷基，C3-6烯基 ，C3-10炔基，C3-7环烷基，C3-7环烷基C1-4烷基，苯基，苯基C1-3烷基，苯基甲氧基甲基，苯氧基乙基或苯氧基甲基，由R2，R3和R4表示的基团之一是氢原子或C1-6烷基，C3 7-环烷基，C 3-6烯基，苯基或苯基C 1-3烷基，其它可以相同或不同的两个基团表示氢原子或C1-6烷基; n表示2或3; 及其生理上可接受的盐和溶剂合物。 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，可用于治疗精神病，焦虑和恶心和呕吐。

    Lactam derivatives
    12.
    发明授权
    Lactam derivatives 失效
    内酰胺衍生物

    公开(公告)号：US5183820A

    公开(公告)日：1993-02-02

    申请号：US691814

    申请日：1991-04-26

    申请人： Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North ,  Barry J. Price

    发明人： Ian H. Coates ,  Alexander W. Oxford ,  Peter C. North ,  Barry J. Price

    IPC分类号： C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The invention provides potent and selective antagonists of 5-HT at 5-HT.sub.3 receptors which are tricyclic lactams of the 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, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 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 same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Y represents the group CH.dbd.CH or (CH.sub.2).sub.n, wherein n represents 2 or 3;Q represents a halogen atom, or a group selected from hydroxy, C.sub.1-4 alkoxy, phenylC.sub.1-3 alkoxy, C.sub.1-6 alkyl, cyano, phenyl which may be unsubstituted or substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy groups or halogen atoms, --NR.sup.7 R.sup.8, --CONR.sup.7 R.sup.8 , --(CH.sub.2).sub.p CONR.sup.7 R.sup.8, --(CH.sub.2).sub.q NR.sup.9 R.sup.10 or --(CH.sub.2).sub.2 CO.sub.2 R.sup.11 ;Q' represents a hydrogen or a fluorine atom;and physiologically acceptable salts and solvates thereof.

    摘要翻译： 本发明提供5-HT受体的有效和选择性拮抗剂，其为作为式（I）的三环内酰胺的5-HT 3受体，其中Im表示下式的咪唑基：其中R1表示氢 原子或选自C 1-6烷基，C 3-6烯基，C 3-10炔基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苯基C 1-3烷基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5中的基团; 由R 2，R 3和R 4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，其它两个基团可以相同或不同 表示氢原子或C 1-6烷基; Y表示基团CH = CH或（CH 2）n，其中n表示2或3; Q表示卤原子，或选自羟基，C 1-4烷氧基，苯基C 1-3烷氧基，C 1-6烷基，氰基，可未被取代或被一个或多个C 1-4烷基，C 1-4烷氧基或羟基或卤素取代的苯基的基团 原子，-NR 7 R 8，-CONR 7 R 8， - （CH 2）p CONR 7 R 8， - （CH 2）q NR 9 R 10或 - （CH 2）2 CO 2 R 11; Q'表示氢或氟原子; 及其生理上可接受的盐和溶剂合物。

    Lactam derivatives
    14.
    发明授权
    Lactam derivatives 失效
    内酰胺衍生物

    公开(公告)号：US5008272A

    公开(公告)日：1991-04-16

    申请号：US393145

    申请日：1989-08-14

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

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

    IPC分类号： C07D233/64 ,  A61K31/435 ,  A61P1/00 ,  A61P1/04 ,  A61P3/06 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The invention provides potent and selective antagonists of 5-HT and 5-HT.sub.3 receptors which are tricyclic lactams 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, phenylC.sub.1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;one of the group represented by R.sup.2, R.sup.3 and R.sup.4 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 physiologically acceptable salts and solvates thereof.

    Imidazole derivatives
    17.
    发明授权
    Imidazole derivatives 失效

    公开(公告)号：US5116984A

    公开(公告)日：1992-05-26

    申请号：US333967

    申请日：1989-04-06

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

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

    IPC分类号： A61K31/415 ,  A61P25/00 ,  C07D233/54 ,  C07D233/64 ,  C07D401/06 ,  C07D403/06

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

    摘要： The invention relates to imidazole derivatives of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of formula: ##STR2## A represents the group CH or a nitrogen atom; R.sup.1 and R.sup.2, which may be the same or different, and may be attached to either the same or different fused rings of the naphthalene moiety, each represents a hydrogen atom, a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl or C.sub.1-4 alkylthio group, and one of R.sup.1 and R.sup.2 may also represent a group --NR.sup.3 R.sup.4 (wherein R.sup.3 and R.sup.4, which may be the same or different, each represents a hydrogen atom or a C.sub.1-4 alkyl group, or together with the nitrogen atom to which they are attached form a saturated 5 to 7 membered ring);n represents 1, 2 or 3;R.sup.5, R.sup.6, R.sup.7, are as defined in the specification; and physiologically acceptable salts and solvates thereof.

    Lactam derivatives
    19.
    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
    20.
    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.