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38 条记录 (耗时 0.024 秒)

    5-substituted 3-aninoalkyl indoles
    2.
    发明授权
    5-substituted 3-aninoalkyl indoles 失效
    5-取代的3-苯基烷基吲哚

    公开(公告)号：US4870096A

    公开(公告)日：1989-09-26

    申请号：US940652

    申请日：1986-12-11

    申请人： Alexander W. Oxford ,  Ian H. Coates ,  David E. Bays ,  Colin F. Webb

    发明人： Alexander W. Oxford ,  Ian H. Coates ,  David E. Bays ,  Colin F. Webb

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  A61P25/04 ,  C07D209/16

    CPC分类号： C07D209/16

    摘要： Indoles are disclosed of formula (I): ##STR1## wherein R.sub.1 represents R.sub.5 R.sub.6 NCOCH.sub.2 --, R.sub.5 CONH(CH.sub.2).sub.p --,R.sub.5 R.sub.6 NSO.sub.2 (CH.sub.2).sub.p -- or R.sub.7 SO.sub.2 NH(CH.sub.2).sub.p --, (where R.sub.5 and R.sub.6 each represents a hydrogen atom or a C.sub.1-3 alkyl group, R.sub.7 represents C.sub.1-3 alkyl and p is zero or one),R.sub.2 is hydrogen or C.sub.1-3 alkyl;R.sub.3 and R.sub.4 each represents hydrogen atom, C.sub.1-3 alkyl, or 2-propenyl;m is zero or an integer from 1 to 4; andn is an integer from 2 to 5; and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds have potent and selective vasoconstrictor activity and are indicated as useful for the treatment of migraine. They may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers of excipients for administration by any convenient route.Various methods for the preparation of the compounds (I) are disclosed.

    摘要翻译： 公开了式（I）的吲哚：其中R1表示R5R6NCOCH2-，R5CONH（CH2）p-，R5R6NSO2（CH2）p-或R7SO2NH（CH2）p-，（其中R5和R6各自表示 氢原子或C 1-3烷基，R 7表示C 1-3烷基，p为0或1），R 2为氢或C 1-3烷基; R3和R4各自表示氢原子，C1-3烷基或2-丙烯基; m为0或1至4的整数; n为2〜5的整数。 和其生理上可接受的盐和溶剂合物（例如水合物）。 这些化合物具有有效和选择性的血管收缩剂活性，并被用于治疗偏头痛。 它们可以配制成具有药学上可接受的赋形剂载体的药物组合物，用于通过任何方便的途径给药。 公开了制备化合物（I）的各种方法。

    Medicaments
    4.
    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。

    Medicaments
    5.
    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。

    Tetrahydro-1H-pyrido[4,3-b]indol-1-one derivatives
    6.
    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
    7.
    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
    8.
    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.

    Medicaments
    9.
    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。