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    Piperidyindoles as serotonin receptor ligands
    2.
    发明授权
    Piperidyindoles as serotonin receptor ligands 失效
    哌啶啶吲哚作为5-羟色胺受体配体

    公开(公告)号：US06844338B2

    公开(公告)日：2005-01-18

    申请号：US10258356

    申请日：2001-05-04

    申请人： John Fairhurst ,  Peter Gallagher

    发明人： John Fairhurst ,  Peter Gallagher

    IPC分类号： A61P25/24 ,  C07D401/14 ,  C07D417/14 ,  A61K31/517 ,  A61K31/5415

    CPC分类号： C07D401/14 ,  C07D417/14

    摘要： A pharmaceutical compound of the formula (I) in which R1 and R2 are each hydrogen or C1-6 alkyl, R3 is —SR10, —SOR10, —SO2R10, —COR10, —CH2OH or —CONHR11, where R10 is C1-6 alkyl and R11 is hydrogen or C1-6 alkyl, R4, R5, R6 and R7 are each hydrogen or C1-6alkyl, provided that at least one of R4, R5, R6 and R7 is C1-6alkyl, R8 and R9 are each hydrogen, halo, C1-6 alkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein R12 and R13 are each hydrogen, C1- alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl; and salts thereof.

    摘要翻译： R 1和R 2各自为氢或C 1-6烷基的式（I）的药物化合物，R 3为-SR 10，-SOR 10，-SO 2 R 10 ，-COR 10，-CH 2 OH或-CONHR 11，其中R 10是C 1-6烷基，R 11是氢或C 1-6烷基，R 4，R 5， R 6和R 7各自为氢或C 1-6烷基，条件是R 4，R 5，R 6和R 7中的至少一个为C 1-6烷基，R 8为 和R 9各自为氢，卤素，C 1-6烷基或氰基，n为0或1，m为2或3，x为a（a）或（b），y为（c）或（ d），其中R 12和R 13各自为氢，C 1烷基，环丙基或环丙基-C 1-6烷基; 及其盐。

    Pharmaceutical compounds
    3.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号：US5338735A

    公开(公告)日：1994-08-16

    申请号：US104272

    申请日：1993-08-12

    申请人： John Fairhurst ,  David E. Tupper

    发明人： John Fairhurst ,  David E. Tupper

    IPC分类号： A61K31/38 ,  A61K31/381 ,  A61P25/00 ,  A61P43/00 ,  C07D333/70 ,  C07D409/12 ,  C07D417/12

    CPC分类号： C07D409/12 ,  C07D333/70 ,  C07D417/12

    摘要： Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.

    摘要翻译： 下式的化合物：其中每个R 1为氢，C 1-4烷基，C 1-4烷氧基，卤素或硝基，n为0,1,2或3，R 2为氢，C 1-4烷基或C 2 -4-烯基，R 3和R 4各自为氢，C 1-4烷基，任选取代的苯基或任选被1至4个C 1-4烷基取代的C 6-9环烷基，R 5为任选取代的苯基，四氢萘基，苯二甲酰亚氨基，糖精，戊二酰氨基， 任选被1至4个C 1-4烷基或苯基取代的C 6-10环烷基或任选被1至4个烷基取代的C 4-9杂取代环烷基，x为1,2或3，y为0或1，z为 是0，1，2或3; 及其盐。 化合物被指示用于治疗中枢神经系统疾病。

    1H-2,1,3-benzothiadiazine-2,2-dioxide compounds or derivatives thereof
    5.
    发明授权
    1H-2,1,3-benzothiadiazine-2,2-dioxide compounds or derivatives thereof 失效
    1H-2,1,3-苯并噻二嗪-2,2-二氧化物化合物或其衍生物

    公开(公告)号：US5929072A

    公开(公告)日：1999-07-27

    申请号：US137788

    申请日：1998-08-21

    申请人： John Fairhurst

    发明人： John Fairhurst

    IPC分类号： A61K31/54 ,  A61P25/00 ,  C07D285/16 ,  C07D417/14 ,  C07D513/04 ,  C07D279/00

    CPC分类号： C07D285/16 ,  A61K9/2059 ,  A61K9/4866 ,  C07D417/14 ,  C07D513/04

    摘要： A pharmaceutical compound having the formula: ##STR1## in which n is 1 or 2, m is 1 or 2, p is 1 to 6, q is 0 or 1 to 3,R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.3 and R.sup.4 together form an alkylene link of formula --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, or R.sup.4 and R.sup.5 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group,R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, carboxy, hydroxy, cyano, halo, trifluoromethyl, nitro or amino,the dotted line represents an optional double bond, andthe fluorine atom is attached at the 6 or 7-position;and salts and esters thereof.

    摘要翻译： 一种具有下式的药物化合物：其中n为1或2，m为1或2，p为1至6，q为0或1至3，R1和R2各自为氢或C1-4烷基，R3，R4 和R 5各自为氢，C 1-4烷基，任选取代的苯基或任选取代的苯基-C 1-4烷基，或者R 3和R 4一起形成式 - （CH 2）3 - 或 - （CH 2）4 - 的亚烷基连接，或 R4和R5与它们所连接的碳原子一起形成C 3-6环烷基，R 6是C 1-4烷基，C 1-4烷氧基，羧基，羟基，氰基，卤素，三氟甲基，硝基或氨基，虚线 表示任选的双键，氟原子连接在6位或7位; 及其盐和酯。

    Naphthalene carboxamides
    6.
    发明授权
    Naphthalene carboxamides 失效
    萘甲酰胺

    公开(公告)号：US5389684A

    公开(公告)日：1995-02-14

    申请号：US108038

    申请日：1993-08-17

    申请人： John Fairhurst ,  David E. Tupper

    发明人： John Fairhurst ,  David E. Tupper

    IPC分类号： A61K31/165 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61P1/00 ,  A61P3/04 ,  A61P9/12 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07C231/14 ,  C07C235/66 ,  C07C237/48 ,  C07C319/20 ,  C07C323/38 ,  C07C323/62 ,  C07D209/48 ,  C07C233/22

    CPC分类号： C07C323/38 ,  C07C235/66 ,  C07C237/48 ,  C07C2101/14 ,  C07C2101/18

    摘要： Pharmaceutical compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, nitro or --NR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.6 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1-4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.

    摘要翻译： 下式的药物化合物：烷氧基，卤素或硝基，n为0,1,2或3，R2为氢，C1-4烷基或C2-4烯基，R3为氢，C1-4烷基，C1 -4-烷氧基，C 1-4烷硫基，卤素，硝基或-NR'R“，其中R'和R”各自为氢或C 1-4烷基，R 4和R 5各自为氢，C 1-4烷基，任选取代的苯基 或任选被1至4个C 1-4烷基取代的C 6-9环烷基，R 6是任选取代的苯基，四氢萘基，苯二甲酰亚氨基，糖精，戊二酰氨基，任选被1至4个C 1-4烷基取代的C 6-10环烷基或苯基 或任选被1-4个烷基取代的C 4-9杂取代的环烷基，x为1,2或3，y为0或1，z为0,1,2或3; 及其盐。

    Pharmaceutical compounds
    7.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号：US06329366B1

    公开(公告)日：2001-12-11

    申请号：US09442904

    申请日：1999-11-18

    申请人： John Fairhurst ,  Peter Thaddeus Gallagher ,  Martin Victor Miles

    发明人： John Fairhurst ,  Peter Thaddeus Gallagher ,  Martin Victor Miles

    IPC分类号： C07D41714

    CPC分类号： C07D215/227 ,  C07D209/34 ,  C07D215/36 ,  C07D285/10 ,  C07D285/16 ,  C07D401/14 ,  C07D417/14

    摘要： A pharmaceutical compound of the formula in which R1 and R2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, where R4 and R5 are each hydrogen, C1-6 alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl, n is 0 or 1, and R3 is —SR6, —SOR6, —SO2R6, —COR6, —CH2OH or —CONHR7, where R6 is C1-6 alkyl and R7 is hydrogen or C1-6 alkyl; provided that when one of R1 and R2 is hydrogen and the other is fluoro, R4 and R5 are each hydrogen or C1-6 alkyl, and n is 0, then R3 is not —COR6 or —CONHR7; and salts thereof.

    摘要翻译： R1和R2各自为氢，卤素，氰基或甲基的化学式为化合物，虚线表示任选的双键，其中R 4和R 5各自为氢，C 1-6烷基，环丙基或环丙基-C 1-6烷基 ，n为0或1，R 3为-SR 6，-SOR 6，-SO 2 R 6，-COR 6，-CH 2 OH或-CONHR 7，其中R 6为C 1-6烷基，且R 7为氢或C 1-6烷基; 并且R 2是氢，另一个是氟，R 4和R 5各自是氢或C 1-6烷基，n是0，则R 3不是-COR 6或-CONHR 7;及其盐。

    Indole compounds
    8.
    发明授权
    Indole compounds 失效
    吲哚化合物

    公开(公告)号：US06166040A

    公开(公告)日：2000-12-26

    申请号：US309420

    申请日：1999-05-11

    申请人： John Fairhurst ,  Peter Thaddeus Gallagher ,  Martin Victor Miles ,  William Martin Owton ,  Colin William Smith

    发明人： John Fairhurst ,  Peter Thaddeus Gallagher ,  Martin Victor Miles ,  William Martin Owton ,  Colin William Smith

    IPC分类号： A61K31/4427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61P1/00 ,  A61P1/08 ,  A61P3/04 ,  A61P9/00 ,  A61P9/12 ,  A61P15/10 ,  A61P25/04 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P25/34 ,  A61P43/00 ,  C07D401/14 ,  A61K31/40 ,  A61K31/435 ,  C07D209/36 ,  C07D401/00

    CPC分类号： C07D401/14

    摘要： Pharmaceutical compounds of the formula: ##STR1## in which n is 1 to 6, m is 1 or 2 and p is 1 or 2, R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, HO--C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, halo, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group, >C.dbd.O, C.dbd.NOR' where R' is hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, halo, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkyl-CO--, where m is 0, 1 or 2, R'R"N--SO.sub.2 --, --COOR', --CONR'R", --NR'R", --N(OR')COOR", --COR', --NHSO.sub.2 R', where R' and R' are each hydrogen or C.sub.1-4 alkyl,R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl,X is oxygen or sulphur,the dotted line represents an optional double bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.

    摘要翻译： 下式的药物化合物：其中n为1至6，m为1或2，p为1或2，R 1和R 2各自为氢，C 1-4烷基，C 1-4烷氧基，HO-C 1-4烷基， C 1-4烷氧基-C 1-4烷基，C 1-4烷硫基，卤素，任选取代的苯基，任选取代的苯基-C 1-4烷基，或R 1和R 2与它们所连接的碳原子一起形成C 3-6环烷基 基团，C = O，C = NOR，其中R'是氢或C 1-4烷基，R 3，R 4和R 5各自是氢，卤素，硝基，C 1-4烷基，C 1-4烷氧基，C 1-4烷基 - CO-，其中m是0,1或2，R'R''N-SO2-，-COOR'，-CONR'R“，-NR'R”，-N（OR'）COOR“ -COR'，-NHSO 2 R'，其中R'和R'各自为氢或C 1-4烷基，R 6和R 7各自为氢或C 1-4烷基，X为氧或硫，虚线为任选的双键， 并且氟原子连接在6-或7-位; 及其盐。

    Thienobenzodiazepine compounds
    10.
    发明授权
    Thienobenzodiazepine compounds 失效
    噻吩并二氮杂化合物

    公开(公告)号：US6034078A

    公开(公告)日：2000-03-07

    申请号：US886847

    申请日：1997-07-01

    申请人： John Fairhurst ,  Terrence Michael Hotten ,  David Edward Tupper ,  David Taiwai Wong

    发明人： John Fairhurst ,  Terrence Michael Hotten ,  David Edward Tupper ,  David Taiwai Wong

    IPC分类号： C07D495/04 ,  A61K31/55

    CPC分类号： C07D495/04

    摘要： Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or halo, and R.sup.2 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-6 cycloalkyl optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl in which the cycloalkyl group is optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, or optionally substituted phenyl-C.sub.1-4 alkyl; or a salt thereof. Such compounds are useful for treating a disorder of the central nervous system which is associated with the modulation of a 5-HT.sub.3 receptor.

    摘要翻译： 下式的药物化合物，其中R 1是氢或卤素，且R 2是C 1-10烷基，C 2-10烯基，C 2-10炔基，任选被1至3个C 1-4烷基取代的C 3-6环烷基，C 3-6 环烷基-C 1-4烷基，其中环烷基任选被1至3个C 1-4烷基取代，或任选取代的苯基-C 1-4烷基; 或其盐。 这样的化合物可用于治疗与5-HT 3受体的调节相关的中枢神经系统病症。