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25 条记录 (耗时 0.023 秒)

    Lactam derivatives
    21.
    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.

    Indolyl compounds and their use in treatment of cephalic pain
    22.
    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。

    Ethanolamine derivatives
    24.
    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.

    Indoline derivatives, method of preparation and use
    25.
    发明授权
    Indoline derivatives, method of preparation and use 失效
    二氢吲哚衍生物，制备和使用方法

    公开(公告)号：US5633276A

    公开(公告)日：1997-05-27

    申请号：US652460

    申请日：1996-06-14

    申请人： Peter C. North ,  Malcolm C. Carter

    发明人： Peter C. North ,  Malcolm C. Carter

    IPC分类号： A61K31/40 ,  A61P3/04 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  C07D307/79 ,  C07D311/58 ,  C07D491/04 ,  C07D491/048 ,  C07D491/052

    CPC分类号： C07D307/79 ,  C07D311/58 ,  C07D491/04

    摘要： A compound of formula (I) ##STR1## wherein, R.sup.1 is hydrogen, halogen or C.sub.1-6 alkyl;R.sup.2 is a group of formula --CR.sup.3 R.sup.4 (CH.sub.2).sub.p NR.sup.5 COR.sup.6 ;R.sup.3, R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or C.sub.l-6 alkyl;R.sup.6 is C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl;n is an integer of 2, 3 or 4;p is an integer of 1, 2, 3 or 4;and pharmaceutically acceptable salts and solvates thereof. A compound of formula (I) is useful in the treatment of conditions associated with a disturbed functioning of the melatonin system.

    摘要翻译： PCT No.PCT / EP94 / 04220 Sec。 371日期1996年6月14日第 102（e）1996年6月14日PCT 1994年12月20日PCT PCT。 公开号WO95 / 17405 日期：1995年6月29日A式（I）化合物其中R1为氢，卤素或C1-6烷基; R2是式-CR3R4（CH2）pNR5COR6的基团; R 3，R 4和R 5可以相同或不同，是氢或C 1-6烷基; R6是C1-6烷基或C3-7环烷基; n是2,3或4的整数; p是1，2，3或4的整数; 及其药学上可接受的盐和溶剂化物。 式（I）化合物可用于治疗与褪黑激素系统紊乱功能相关的病症。