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    Ethanolamine derivatives
    1.
    发明授权
    Ethanolamine derivatives 失效

    公开(公告)号：US4990664A

    公开(公告)日：1991-02-05

    申请号：US230357

    申请日：1988-08-10

    申请人： Ian F. Skidmore ,  Alan Naylor ,  Harry Finch ,  Lawrence H. C. Lunts ,  Ian B. Campbell ,  Peter C. North

    发明人： Ian F. Skidmore ,  Alan Naylor ,  Harry Finch ,  Lawrence H. C. Lunts ,  Ian B. Campbell ,  Peter C. North

    IPC分类号： C07D295/18 ,  A61K31/135 ,  A61K31/165 ,  A61K31/18 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61K31/47 ,  A61P5/38 ,  C07C67/00 ,  C07C231/00 ,  C07C237/30 ,  C07C301/00 ,  C07C303/34 ,  C07C309/66 ,  C07C313/00 ,  C07C323/25 ,  C07C323/27 ,  C07C323/41 ,  C07C323/42 ,  C07C323/43 ,  C07C323/44 ,  C07C323/49 ,  C07C323/60 ,  C07C323/62 ,  C07C323/65 ,  C07C325/00 ,  C07D213/32 ,  C07D213/65 ,  C07D215/26

    CPC分类号： C07C323/62 ,  C07C323/25 ,  C07D213/32

    摘要： The invention provides compounds of the general formula ##STR1## and physiologically acceptable salts and solvates thereof, wherein Z represents the group ##STR2## where A represents a group selected from HOR.sup.3 --, R.sup.6 NH(CH.sub.2)p--, R.sup.10 R.sup.11 N--, R.sup.12 OCH.sub.2 --, CH.sub.3 SO.sub.2 CH.sub.2 -- or NCCH.sub.2 --;where R.sup.3 is a C.sub.1-3 alkylene group,R.sup.6 is a group selected from R.sup.7 CO--, R.sup.7 NHCO--, R.sup.7 R.sup.8 NSO.sub.2 -- orR.sup.9 SO.sub.2 --, and p is zero or 1,R.sup.7 and R.sup.8 each represent a hydrogen atom or a C.sub.1-3 alkyl group,R.sup.9 is a C.sub.1-3 alkyl group,R.sup.10 and R.sup.11 each represent a hydrogen atom or a C.sub.1-4 alkyl group or, when R.sup.10 is a hydrogen atom, R.sup.11 may also be a C.sub.1-4 alkoxycarbonyl group, andR.sup.12 is a C.sub.1-3 alkyl group; ##STR3## where one of R.sup.4 and R.sup.5 is a hydroxy group and the other is a hydrogen or halogen atom or a hydroxy group; ##STR4## where A.sup.1 is either a chlorine atom or a --CF.sub.3 group; ##STR5## X represents a bond or a C.sub.1-7 alkenylene or C.sub.2-7 alkynylene chain, andY represents a bond, or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain, with the proviso that the sum total of carbon atoms in X and Y is 2 to 10;R represents a hydrogen atom or a C.sub.1-3 alkyl group;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group; with the proviso that the sum total of carbon atoms inR.sup.1 and R.sup.2 is not more than 4;Q represents a pyridyl group optionally substituted by one or two substituents selected from halogen atoms or hydroxy, C.sub.1-3 alkyl or C.sub.1-3 alkoxy groups, or Q represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-6 alkyl, nitro, --(CH.sub.2).sub.q R.sup.13 or --O(CH.sub.2).sub.r R.sup.14, or Q represents a phenyl group substituted by an alkylenedioxy group of formula --O(CH.sub.2).sub.t O--; whereR.sup.13 represents hydroxy, C.sub.1-6 alkoxy, cyano, --NR.sup.15 R.sup.16, --NR.sup.17 COR.sup.18, --NR.sup.17 SO.sub.2 R.sup.19, --COR.sup.20, --SR.sup.21, --SOR.sup.22 or --SO.sub.2 R.sup.22 ;R.sup.14 represents hydroxy or C.sub.1-4 alkoxy;R.sup.15 and R.sup.16 each represent a hydrogen atom or a C.sub.1-4 alkyl group or --NR.sup.15 R.sup.16 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--;R.sup.17 represents a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.18 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or --NR.sup.15 R.sup.16 group;R.sup.19 represents C.sub.1-4 alkyl, phenyl or --NR.sup.15 R.sup.16 ;R.sup.20 represents hydroxy, C.sub.1-4 alkoxy or --NR.sup.15 R.sup.16 ;R.sup.21 represents a hydrogen atom or a C.sub.1-4 alkyl or phenyl group;R.sup.22 represents a C.sub.1-4 alkyl or phenyl group;q represents an integer from 0 to 3;r represents 2 or 3; andt represents 1 or 2.The compounds have a stimulant action at .beta..sub.2 -adrenoreceptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    Medicaments
    2.
    发明授权
    Medicaments 失效
    药剂

    公开(公告)号：US5221687A

    公开(公告)日：1993-06-22

    申请号：US934307

    申请日：1992-08-25

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

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

    IPC分类号： A61K31/00 ,  A61K31/445 ,  A61K31/55

    CPC分类号： A61K31/00 ,  A61K31/445 ,  A61K31/55

    摘要： The invention relates to the use of compounds of formula (I) ##STR1## wherein Im represents an imidazolyl group of 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 (wherein R.sup.5 and R.sup.6, 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.5 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.5 or --SO.sub.2 R.sup.5);one of the groups represented by R.sup.2, R.sup.3 and R4 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 n represents 2 or 3,and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of depression.

    摘要翻译： 本发明涉及式（I）化合物其中Im表示下式的咪唑基，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，苯基甲氧基甲基，苯氧基乙基，苯氧基甲基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5（其中R 5和R 6可以相同或不同 各自表示氢原子，C 1-6烷基或C 3-7环烷基，或苯基或苯基C 1-4烷基，其中苯基任选被一个或多个C 1-4烷基，C 1-4烷氧基或羟基或卤素 原子，条件是当R 1表示-CO 2 R 5或-SO 2 R 5基团时，R 5不表示氢原子）; 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，代表氢原子或C1-6烷基; 和n表示2或3，以及其生理上可接受的盐和溶剂合物，用于制备用于治疗抑郁症的药物。

    Indolyl compounds and their use in treatment of cephalic pain
    3.
    发明授权
    Indolyl compounds and their use in treatment of cephalic pain 失效
    吲哚类化合物及其在治疗头痛方面的应用

    公开(公告)号：US5475020A

    公开(公告)日：1995-12-12

    申请号：US256089

    申请日：1994-06-27

    申请人： Martin R. Johnson ,  Peter C. North

    发明人： Martin R. Johnson ,  Peter C. North

    IPC分类号： A61K31/40 ,  A61P25/04 ,  A61P25/06 ,  C07D403/04 ,  A61K31/405

    CPC分类号： C07D403/04

    摘要： The invention relates to indoles of general formula (I) ##STR1## wherein R.sub.0 represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sub.1 represents a group R.sub.4 CONH--, R.sub.4 R.sub.5 NSO.sub.2 --, R.sub.4 SO.sub.2 NH-- or R.sub.4 R.sub.5 NCO-- (where R.sub.4 is a hydrogen atom or a C.sub.1-6 alkyl group, provided that R.sub.4 does not represent a hydrogen atom when R.sub.1 represents R.sub.4 SO.sub.2 NH--, and R.sub.5 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, phenyl or phen(C.sub.1-3)alkyl group in which the phenyl ring is optionally substituted by a halogen atom or a C.sub.1-4 alkoxy, hydroxy or C.sub.1-3 alkyl group); R.sub.2 is a hydrogen atom, a C.sub.1-3 alkyl, a C.sub.3-6 alkenyl, a phenyl or a phen(C.sub.1-3)alkyl group; R.sub.3 is a hydrogen atom, a C.sub.1-3 alkyl group or a group --CO.sub.2 R.sub.6, --COR.sub.6, --COCO.sub.2 R.sub.6 or --CONHR.sub. 6 where R.sub.6 is a hydrogen atom or a C.sub.1-4 alkyl, a C.sub.3-7 cycloalkyl, a C.sub.3-6 alkenyl, an aryl or an ar(C.sub.1-4)alkyl group in which the aryl group may be unsubstituted or substituted by a halogen atom or a C.sub.1-4 alkoxy, C.sub.1-4 alkyl or hydroxy group, provided that when R.sub.3 is --CO.sub.2 R.sub.6, R.sub.6 is other than hydrogen; n is zero or an integer from 1 to 5; and pharmaceutically acceptable salts thereof.

    摘要翻译： PCT No.PCT / EP93 / 00074 Sec。 371日期1994年6月27日第 102（e）日期1994年6月27日PCT提交1993年1月12日PCT公布。 公开号WO93 / 14087 日本公开号为1993年7月22日。本发明涉及通式（I）的吲哚，其中R 0表示氢原子或C 1-3烷基; R1表示R4CONH-，R4R5NSO2-，R4SO2NH-或R4R5NCO-基团（其中R4为氢原子或C1-6烷基），条件是当R1表示R4SO2NH-时R4不表示氢原子，R5表示氢 原子或C 1-6烷基，C 3-7环烷基，苯基或苯基（C 1-3）烷基，其中苯环任选被卤素原子或C 1-4烷氧基，羟基或C 1-3烷基取代）; R2是氢原子，C1-3烷基，C3-6烯基，苯基或苯基（C1-3）烷基; R3是氢原子，C1-3烷基或-CO2R6，-COR6，-COCO2R6或-CONHR6，其中R6是氢原子或C1-4烷基，C3-7环烷基，C3-6链烯基， 芳基或芳（C 1-4）烷基，其中芳基可以是未取代的或被卤素原子或C 1-4烷氧基，C 1-4烷基或羟基取代，条件是当R 3为-CO 2 R 6时，R 6 不是氢; n为0或1〜5的整数; 及其药学上可接受的盐。

    Medicaments
    4.
    发明授权
    Medicaments 失效
    药剂

    公开(公告)号：US5229407A

    公开(公告)日：1993-07-20

    申请号：US911395

    申请日：1992-07-10

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

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

    IPC分类号： A61K31/00 ,  A61K31/445 ,  A61K31/55

    CPC分类号： A61K31/445 ,  A61K31/00 ,  A61K31/55

    摘要： The invention relates to the use of compounds of formula (I) ##STR1## wherein Im represents an imidazolyl group of 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 (wherein R.sup.5 and R.sup.6, 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.5 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.5 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 the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and n represents 2 or 3,and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of a cognitive disorder.

    摘要翻译： 本发明涉及式（I）化合物其中Im表示下式的咪唑基，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，苯基甲氧基甲基，苯氧基乙基，苯氧基甲基，-CO 2 R 5，-COR 5，-CONR 5 R 6或-SO 2 R 5（其中R 5和R 6可以相同或不同 各自表示氢原子，C 1-6烷基或C 3-7环烷基，或苯基或苯基C 1-4烷基，其中苯基任选被一个或多个C 1-4烷基，C 1-4烷氧基或羟基或卤素 原子，条件是当R 1表示-CO 2 R 5或-SO 2 R 5基团时，R 5不表示氢原子）; 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，代表氢原子或C1-6烷基; 和n表示2或3，以及其生理上可接受的盐和溶剂合物，用于制备用于治疗认知障碍的药物。

    Imidazole derivatives and pharmaceutical use thereof
    5.
    发明授权
    Imidazole derivatives and pharmaceutical use thereof 失效
    咪唑衍生物及其药物用途

    公开(公告)号：US5006544A

    公开(公告)日：1991-04-09

    申请号：US420324

    申请日：1989-10-12

    申请人： Peter C. North ,  David J. Cavalla ,  Derek J. M. Black

    发明人： Peter C. North ,  David J. Cavalla ,  Derek J. M. Black

    IPC分类号： A61K31/415 ,  A61K31/47 ,  A61P25/00 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06

    CPC分类号： C07D401/06 ,  C07D405/06 ,  C07D409/06

    摘要： The invention provides imidazole derivatives of the general formula (I) ##STR1## wherein Im representes an imidazolyl group of the formula: ##STR2## and 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 cycoalkyl, 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;R.sup.1 and R.sup.2 each represent a hydrogen atom, or together with the carbon atoms to which they are attached form a phenyl ring;X represents an oxygen or a sulphur atom, or a group NR.sup.6, wherein R.sup.6 represents a C.sub.1-6 alkyl group;Z--Y represents the group CH--CH.sub.2 or C.dbd.CH;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.

    Medicaments
    7.
    发明授权
    Medicaments 失效
    药剂

    公开(公告)号：US5276050A

    公开(公告)日：1994-01-04

    申请号：US908329

    申请日：1992-07-06

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

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

    IPC分类号： A61K31/415

    CPC分类号： A61K31/415

    摘要： The invention relates to the use of compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, in which Im represents an imidazolyl group of 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 (wherein R.sup.5 and R.sup.6, 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.5 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.5 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 the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and n represents 2 or 3,for the treatment of a condition involving excessive eating, for example bulimia.

    摘要翻译： 本发明涉及通式（I）化合物（Ⅰ）及其生理上可接受的盐和溶剂化物，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，苯基甲氧基甲基，苯氧基乙基，苯氧基甲基，-CO 2 R 5，-COR 5，-CONR 5 R 6或 -SO 2 R 5（其中R 5和R 6可以相同或不同，各自表示氢原子，C 1-6烷基或C 3-7环烷基或苯基或苯基C 1-4烷基，其中苯基任选被一个 或更多C 1-4烷基，C 1-4烷氧基或羟基或卤素原子，条件是当R 1表示-CO 2 R 5或-SO 2 R 5基团时，R 5不表示氢原子）; 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 不同的是氢原子或C1-6烷基; n表示2或3，用于治疗涉及过度饮食的病症，例如贪食症。

    Indole derivatives
    8.
    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
    10.
    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。