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    • 14. 发明授权
    • Tricyclic ketones useful as HT.sub.3 -receptor antagonists
    • TRICYCLIC KETONES有用作为HT3受体拮抗剂
    • US5202343A
    • 1993-04-13
    • US887607
    • 1992-05-22
    • Ian H. CoatesJohn BradshawJames A. BellDavid C. HumberGeorge B. EwanWilliam L. MitchellBarry J. Price
    • Ian H. CoatesJohn BradshawJames A. BellDavid C. HumberGeorge B. EwanWilliam L. MitchellBarry J. Price
    • C07D403/06
    • C07D403/06
    • 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.
    • 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。
    • 16. 发明授权
    • Ketone derivatives
    • 酮衍生物
    • US4950681A
    • 1990-08-21
    • US239750
    • 1988-09-02
    • David J. CavallaWilliam L. Mitchell
    • David J. CavallaWilliam L. Mitchell
    • A61K31/415A61P25/00C07D403/06
    • C07D403/06
    • The invention relates to ketones 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, --CO.sub.2 R.sup.8, --COR.sup.8, --CONR.sup.8 R.sup.9 or --SO.sub.2 R.sup.8 (wherein R.sup.8 and R.sup.9, 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.8 does not represent a hydrogen atom when R.sup.1 represents a group --CO.sub.2 R.sup.8 or --SO.sub.2 R.sup.8);R.sup.2 represents a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-7 cycloalkyl, phenyl or phenylC.sub.1-3 alkyl group;R.sup.3 and R.sup.4, which may be the same or different, each represents a hydrogen atom or a C.sub.1-6 alkyl group; or R.sup.2 and R.sup.3 may together represent an alkylene chain -(CH.sub.2).sub.n --, where n represents 1, 2 or 3;one of the groups represented by R.sup.5, R.sup.6 and R.sup.7 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 atom 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.10 R.sup.11 or --CONR.sup.10 R.sup.11 (wherein R.sup.10 and R.sup.11, 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 and 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.