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    Tricyclic ketones useful as HT.sub.3 -receptor antagonists
    4.
    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。

    5-substituted 3-aminoalkyl indoles useful in treatment of migraine
    6.
    发明授权
    5-substituted 3-aminoalkyl indoles useful in treatment of migraine 失效
    用于治疗偏头痛的5-取代的3-氨基烷基吲哚

    公开(公告)号：US4672067A

    公开(公告)日：1987-06-09

    申请号：US625648

    申请日：1984-06-28

    申请人： Ian H. Coates ,  Keith Mills ,  Colin F. Webb ,  Michael D. Dowle ,  David E. Bays

    发明人： Ian H. Coates ,  Keith Mills ,  Colin F. Webb ,  Michael D. Dowle ,  David E. Bays

    IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61P9/00 ,  A61P25/04 ,  C07D209/16 ,  C07D209/48 ,  C07D471/04

    CPC分类号： C07D209/16

    摘要： Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents CHO, COR.sub.8, CO.sub.2 R.sub.8, CONR.sub.9 R.sub.10, CSNR.sub.9 R.sub.10 or SO.sub.2 NR.sub.9 R.sub.10, whereR.sub.8 represents alkyl, cycloalkyl, aryl or aralkyl,R.sub.9 represents hydrogen or alkyl, andR.sub.10 represents hydrogen or alkyl, cycloalkyl, aryl or aralkyl;R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7 each independently represents hydrogen or C.sub.1-3 alkyl;R.sub.5 represents hydrogen, or alkyl, cycloalkyl, alkenyl or aralkyl, orR.sub.4 and R.sub.5 together form an aralkylidene group or R.sub.4 and R.sub.5 together with the attached nitrogen atom form a saturated monocyclic 5- to 7-membered ring; andAlk represents C.sub.2-3 alkylene chain optionally substituted by not more than two C.sub.1-3 alkyl groups;and physiologically acceptable salts and solvates thereof. The compounds are potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner using pharmaceutically acceptable carriers or excipients. The compounds may be prepared by, for example, reaction of an aminoalkyl indole with an acid of formula R.sub.1 OH or an acylating agent corresponding thereto or with an inorganic cyanate or an organic isocyanate or isothiocyanate in order to introduce the desired R.sub.1 group at the 5-position on the indole nucleus.

    摘要翻译： 公开了式（I）的化合物其中R 1表示CHO，COR8，CO 2 R 8，CONR 9 R 10，CSNR 9 R 10或SO 2 NR 9 R 10，其中R 8表示烷基，环烷基，芳基或芳烷基，R 9表示氢或烷基，R 10表示氢 或烷基，环烷基，芳基或芳烷基; R2，R3，R4，R6和R7各自独立地表示氢或C1-3烷基; R5表示氢或烷基，环烷基，烯基或芳烷基，或R4和R5一起形成芳烷叉基或R4和R5与连接的氮原子一起形成饱和的单环5-至7-元环; 并且Alk表示任选被不多于两个C 1-3烷基取代的C 2-3亚烷基链; 及其生理上可接受的盐和溶剂合物。 这些化合物潜在地可用于治疗偏头痛，并且可以使用药学上可接受的载体或赋形剂以常规方式配制成药物组合物。 化合物可以通过例如氨基烷基吲哚与式R1OH的酸或对应于其的酰化剂或与无机氰酸酯或有机异氰酸酯或异硫氰酸酯反应制备，以便在5- 在吲哚核上的位置。

    3 amino alkyl indoles for use in treating migraine
    7.
    发明授权
    3 amino alkyl indoles for use in treating migraine 失效
    3氨基烷基吲哚，用于治疗偏头痛

    公开(公告)号：US4636521A

    公开(公告)日：1987-01-13

    申请号：US626383

    申请日：1984-06-29

    申请人： Ian H. Coates ,  Keith Mills ,  Colin F. Webb ,  Michael D. Dowle ,  David E. Bays

    发明人： Ian H. Coates ,  Keith Mills ,  Colin F. Webb ,  Michael D. Dowle ,  David E. Bays

    IPC分类号： C07D209/14 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61P9/00 ,  A61P25/04 ,  C07D209/16 ,  C07D209/48 ,  C07D471/04

    CPC分类号： C07D209/16

    摘要： Compounds are disclosed of general formula (I) ##STR1## wherein R.sub.1 represents an alkyl, cycloalkyl, aryl or aralkyl group;R.sub.2, R.sub.3, R.sub.4, R.sub.6 and R.sub.7, which may be the same or different, each represents a hydrogen atom or a C.sub.1-3 alkyl group;R.sub.5 represents a hydrogen atom or an alkyl, cycloalkyl, alkenyl or an aralkyl group; or R.sub.4 and R.sub.5 together form an aralkylidene group or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a saturated monocyclic 5- to 7-membered ring; Alk represents an alkylene chain containing two or three carbon atoms which may be unsubstituted or substituted by not more than two C.sub.1-3 alkyl groups; and physiologically acceptable salts, solvates and bioprecursors thereof. The compounds are described as potentially useful for the treatment of migraine and may be formulated as pharmaceutical compositions in conventional manner using one or more pharmaceutically acceptable carriers or excipients. Various processes for the preparation of the compounds are disclosed including, for example, a process involving reaction of an aminoalkyl indole with a sulphonylating agent in order to introduce the --SO.sub.2 -- group at the 5-position on the indole nucleus.

    摘要翻译： 公开了通式（I）的化合物其中R 1表示烷基，环烷基，芳基或芳烷基; R 2，R 3，R 4，R 6和R 7可以相同或不同，各自表示氢原子或C 1-3烷基; R5表示氢原子或烷基，环烷基，烯基或芳烷基; 或R 4和R 5一起形成亚烷基或R 4和R 5与它们所连接的氮原子一起形成饱和的单环5-至7-元环; Alk表示含有两个或三个碳原子的亚烷基链，其可以是未取代的或被不多于两个C 1-3烷基取代; 和其生理上可接受的盐，溶剂化物和生物前体。 这些化合物被描述为潜在地可用于治疗偏头痛，并且可以使用一种或多种药学上可接受的载体或赋形剂以常规方式配制成药物组合物。 公开了制备化合物的各种方法，包括例如涉及氨基烷基吲哚与磺酰化剂反应的方法，以便在吲哚核上的5-位引入-SO 2 - 基团。

    5-substituted 3-aninoalkyl indoles
    8.
    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。

    Tricyclic ketone derivatives as 5-HT antagonists
    10.
    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.