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    Tricyclic ketone derivatives as 5-HT antagonists
    1.
    发明授权
    Tricyclic ketone derivatives as 5-HT antagonists 失效
    三环酮衍生物作为5-HT拮抗剂

    公开(公告)号：US4939144A

    公开(公告)日：1990-07-03

    申请号：US260680

    申请日：1988-10-21

    申请人： Ian H. Coates ,  David C. Humber ,  James A. Bell ,  George B. Ewan ,  Alexander W. Oxford ,  William L. Mitchell

    发明人： Ian H. Coates ,  David C. Humber ,  James A. Bell ,  George B. Ewan ,  Alexander W. Oxford ,  William L. Mitchell

    IPC分类号： A61K31/415 ,  A61P1/00 ,  A61P1/08 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06

    摘要： The invention relates to ketones of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##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, 2 or 3;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, (wherein R.sup.4 and R.sup.5, 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 X represents an oxygen or a sulphur atom, or, when Im represents an imidazolyl group of formula (c) and n represents 1 or 3, X may also represent the group NR.sup.6, wherein R.sup.6 represents a hydrogen atom or a group selected from C.sub.1-10 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 (wherein R.sup.7 and R.sup.8, 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 phenyl C.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.7 does not represent a hydrogen atom when R.sup.6 represents a group --CO.sub.2 R.sup.7); and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT and 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.

    Process for preparing tetrahydrocarbazolones
    2.
    发明授权
    Process for preparing tetrahydrocarbazolones 失效
    四氢咔唑酮的制备方法

    公开(公告)号：US4739072A

    公开(公告)日：1988-04-19

    申请号：US888254

    申请日：1986-07-23

    申请人： Alexander W. Oxford ,  Colin D. Eldred ,  Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

    发明人： Alexander W. Oxford ,  Colin D. Eldred ,  Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

    IPC分类号： C07D403/06 ,  A61K31/415 ,  C07C221/00 ,  C07C225/14 ,  C07D233/60 ,  C07D233/61 ,  C07D521/00 ,  C07D403/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The invention relates to a process for the preparation of a compound of general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group, and 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.2-6 alkenyl or phenyl-(C.sub.1-3)alkyl group and each of the other two groups, which may be the same or different, represent a hydrogen atom or a C.sub.1-6 alkyl group;or a salt or protected derivative thereof, by cyclization of a compound of general formula (II) ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.

    摘要翻译： 本发明涉及一种制备通式（I）化合物的方法，其中R1表示氢原子或C1-10烷基，C3-7环烷基，C3-7环烷基 - （C1- 4）烷基，C 3-6烯基，C 3-10炔基，苯基或苯基 - （C 1-3）烷基，并且由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 2-6烯基或苯基 - （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C 1-6烷基; 或其盐或被保护的衍生物，通过使通式（II）化合物（II）其中R 1，R 2，R 3和R 4如上所定义的化合物或其盐或其保护的衍生物环化。 式（I）化合物是“神经元”5-羟色胺受体的有效和选择性拮抗剂。

    Tricyclic ketones useful as HT.sub.3 -receptor antagonists
    5.
    发明授权
    Tricyclic ketones useful as HT.sub.3 -receptor antagonists 失效
    TRICYCLIC KETONES有用作为HT3受体拮抗剂

    公开(公告)号：US5202343A

    公开(公告)日：1993-04-13

    申请号：US887607

    申请日：1992-05-22

    申请人： Ian H. Coates ,  John Bradshaw ,  James A. Bell ,  David C. Humber ,  George B. Ewan ,  William L. Mitchell ,  Barry J. Price

    发明人： Ian H. Coates ,  John Bradshaw ,  James A. Bell ,  David C. Humber ,  George B. Ewan ,  William L. Mitchell ,  Barry J. Price

    IPC分类号： C07D403/06

    CPC分类号： C07D403/06

    摘要： The invention relates to compounds of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## 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 ;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;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 ;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;n represents 1, 2 or 3; andA-B represents the group CH--CH.sub.2 or C.dbd.CH; 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）的化合物：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， 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; R 5和R 6可以相同或不同，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 不同的是氢原子或C1-6烷基; Q表示氢或卤素原子，或羟基，C 1-4烷氧基，苯基C 1-3烷氧基或C 1-6烷基或基团-NR 7 R 8或-CONR 7 R 8; R 7和R 8可以相同或不同，各自表示氢原子或C 1-4烷基或C 3-4烯基，或与它们所连接的氮原子一起形成饱和的5至7元环; n表示1,2或3; A-B表示基团CH-CH 2或C = CH; 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。

    Carbazole derivatives and their use as 5HT-induced antagonists
    6.
    发明授权
    Carbazole derivatives and their use as 5HT-induced antagonists 失效
    咔唑衍生物及其用作5HT诱导的拮抗剂

    公开(公告)号：US4749718A

    公开(公告)日：1988-06-07

    申请号：US888257

    申请日：1986-07-23

    申请人： Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

    发明人： Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

    IPC分类号： A61K31/415 ,  A61P1/04 ,  A61P1/08 ,  A61P25/00 ,  A61P25/04 ,  A61P43/00 ,  C07D209/88 ,  C07D403/06 ,  C07D521/00 ,  A61K31/40

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/06

    摘要： The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 represents a group 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 phenyl-(C.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);and 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.2-6 alkenyl 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; and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of "neuronal" 5-hydroxytryptamine receptors and are useful in the treatment of psychotic disorders (e.g. schizophrenia and mania); anxiety; pain; gastric stasis; symptoms of gastrointestinal dysfunction such as occur with dyspepsia, peptic ulcer, reflux oesophagitis and flatulence; migraine; and nausea and vomiting.

    摘要翻译： 本发明涉及通式（I）的化合物：其中R 1表示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，各自代表氢原子 ，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烷氧基或羟基取代 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 2-6烯基或苯基 - （C 1-3）烷基，其它两个基团， 可以相同或不同，表示氢原子或C1-6烷基; 及其生理上可接受的盐和溶剂合物。 这些化合物是“神经元”5-羟色胺受体的有效和选择性拮抗剂，可用于治疗精神病（如精神分裂症和躁狂症）; 焦虑; 疼痛; 胃潴留; 胃肠功能障碍的症状如消化不良，消化性溃疡，反流性食管炎和胃肠气胀等发生; 偏头痛 和恶心呕吐。

    Carbazole derivatives and their use as 5HT-induced antagonists
    7.
    发明授权
    Carbazole derivatives and their use as 5HT-induced antagonists 失效
    咔唑衍生物及其用作5HT诱导的拮抗剂

    公开(公告)号：US4725615A

    公开(公告)日：1988-02-16

    申请号：US888258

    申请日：1986-07-23

    申请人： Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

    发明人： Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

    IPC分类号： A61K31/415 ,  A61P1/04 ,  A61P1/08 ,  A61P25/00 ,  A61P25/04 ,  A61P43/00 ,  C07D209/88 ,  C07D403/06 ,  C07D521/00 ,  A61K31/40 ,  C07D401/06

    CPC分类号： C07D231/12 ,  C07D209/88 ,  C07D233/56 ,  C07D249/08 ,  C07D403/06

    摘要： The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)-alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group;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.2-6 alkenyl 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; and X represents 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.5 R.sup.6 or CONR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6, 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 "neuronal" 5-hydroxytryptamine receptors and are useful in the treatment of psychotic disorders (e.g. schizophrenia and mania;); anxiety, pain; gastric stasis; symptoms of gastrointestinal dysfunction such as occur with dyspepsia, peptic ulcer, reflux oesophagitis and flatulence; migraine; and nausea and vomiting.

    摘要翻译： 本发明涉及通式（I）的化合物：其中R 1表示氢原子或C 1-10烷基，C 3-7环烷基，C 3-7环烷基 - （C 1-4） - 烷基，C 3 -6-烯基，C 3-10炔基，苯基或苯基 - （C 1-3）烷基; 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 2-6烯基或苯基 - （C 1-3）烷基和其它两个基团，其中 可以相同或不同，表示氢原子或C1-6烷基; 并且X表示卤原子或羟基，C 1-4烷氧基，苯基 - （C 1-3） - 烷氧基或C 1-6烷基或NR 5 R 6或CONR 5 R 6基团，其中R 5和R 6可各自相同或不同 表示氢原子或C1-4烷基或C3-4烯基，或与它们所连接的氮原子一起形成饱和的5至7元环; 及其生理上可接受的盐和溶剂合物。 这些化合物是“神经元”5-羟色胺受体的有效和选择性拮抗剂，可用于治疗精神病（如精神分裂症和躁狂症）; 焦虑，痛苦; 胃潴留; 胃肠功能障碍的症状如消化不良，消化性溃疡，反流性食管炎和胃肠气胀等发生; 偏头痛 和恶心呕吐。

    Method for treating nausea and vomiting
    8.
    发明授权
    Method for treating nausea and vomiting 失效
    治疗恶心呕吐的方法

    公开(公告)号：US4753789A

    公开(公告)日：1988-06-28

    申请号：US877805

    申请日：1986-06-24

    申请人： Michael B. Tyers ,  Ian H. Coates ,  David C. Humber ,  George B. Ewan ,  James A. Bell

    发明人： Michael B. Tyers ,  Ian H. Coates ,  David C. Humber ,  George B. Ewan ,  James A. Bell

    IPC分类号： C07D403/06 ,  A61K31/415 ,  A61P1/00 ,  A61P1/08

    CPC分类号： A61K31/415 ,  Y10S514/872 ,  Y10S514/917 ,  Y10S514/922

    摘要： The invention relates to the use of compounds of the general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycoalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group, and one of the groups represented byR.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.2-6 alkenyl 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;and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage of radiological examination procedures.The invention also relates to a product containing a therapeutic agent liable to induce nausea and vomiting, e.g. a cytostatic agent such as a cyclophosphamide, an alkylating agent or a platinum complex, and a compound of the general formula (I) as a combined preparation for simultaneous separate or sequential use in therapy.

    Medicaments
    9.
    发明授权
    Medicaments 失效
    药剂

    公开(公告)号：US5240954A

    公开(公告)日：1993-08-31

    申请号：US804020

    申请日：1991-12-09

    申请人： Michael B. Tyers ,  Ian H. Coates ,  David C. Humber ,  George B. Ewan ,  James A. Bell

    发明人： Michael B. Tyers ,  Ian H. Coates ,  David C. Humber ,  George B. Ewan ,  James A. Bell

    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## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4) alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-C.sub.1-3 alkyl group; and one of the groups represented byR.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.2-6 alkenyl 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; and physiologically acceptable salts and solvates thereof, for the relief of nausea and vomiting and/or the promotion of gastric emptying and for the manufacture of a medicament for this purpose. Promotion of gastric emptying may be for the relief of gastro-intestinal disorders associated with gastric stasis or may be of advantage in radiological examination procedures.The invention also relates to a product containing a therapeutic agent liable to induce nausea and vomiting, e.g. a cytostatic agent such as a cyclophosphamide, an alkylating agent or a platinum complex, and a compound of the general formula (I) as a combined preparation for simultaneous separate or sequential use in therapy.

    摘要翻译： 本发明涉及通式（I）化合物其中R 1表示氢原子或C 1-10烷基，C 3-7环烷基，C 3-7环烷基 - （C 1-4）烷基 C 3-6烯基，C 3-10炔基，苯基或苯基-C 1-3烷基; 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 2-6烯基或苯基-C 1-3烷基，其它两个基团可以是 相同或不同，表示氢原子或C 1-6烷基; 及其生理上可接受的盐和溶剂化物，用于缓解恶心和呕吐和/或促进胃排空和用于制造用于此目的的药物。 促进胃排空可能是为了缓解与胃潴留相关的胃肠道疾病，或者在放射学检查程序中可能是有利的。 本发明还涉及含有易诱发恶心和呕吐的治疗剂的产品，例如， 细胞生长抑制剂如环磷酰胺，烷化剂或铂络合物，以及通式（I）的化合物作为用于在治疗中同时分开或顺次使用的组合制剂。

    Process for preparing N-heterocyclic compounds
    10.
    发明授权
    Process for preparing N-heterocyclic compounds 失效
    制备N-杂环化合物的方法

    公开(公告)号：US4957609A

    公开(公告)日：1990-09-18

    申请号：US312172

    申请日：1989-02-21

    申请人： Neil Godfrey ,  Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

    发明人： Neil Godfrey ,  Ian H. Coates ,  James A. Bell ,  David C. Humber ,  George B. Ewan

    IPC分类号： C07D403/06 ,  A61K31/415 ,  C07C221/00 ,  C07C225/14 ,  C07D233/60 ,  C07D233/61 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The invention relates to a process for the preparation of compounds of general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-(C.sub.1-4)alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, phenyl or phenyl-(C.sub.1-3)alkyl group, and 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.2-6 alkenyl or phenyl-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; or a salt or protected derivative thereof by cyclization of a compound of general formula (II) ##STR2## wherein X represents a hydrogen atom or a halogen atom and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, or a salt or a protected derivative thereof.The compounds of formula (I) are potent and selective antagonists at "neuronal" 5-hydroxytryptamine receptors.

    摘要翻译： 本发明涉及制备通式（I）化合物的方法，其中R 1表示氢原子或C 1-10烷基，C 3-7环烷基，C 3-7环烷基 - （C 1-4） ）烷基，C 3-6烯基，C 3-10炔基，苯基或苯基 - （C 1-3）烷基，并且由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基， 7个环烷基，C 2-6烯基或苯基 - 苯基 - （C 1-3）烷基，其它两个可以相同或不同的基团表示氢原子或C1-6烷基; 或其盐或其保护的衍生物通过环化通式（II）的化合物其中X表示氢原子或卤素原子，并且R 1，R 2，R 3和R 4如上所定义，或其盐 或其受保护的衍生物。 式（I）化合物是“神经元”5-羟色胺受体的有效和选择性拮抗剂。