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6 条记录 (耗时 0.011 秒)

    Indole compounds
    2.
    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。

    5HT receptor binding benzimidazolylpiperidines
    4.
    发明授权
    5HT receptor binding benzimidazolylpiperidines 失效
    5HT受体结合苯并咪唑基哌啶

    公开(公告)号：US6075039A

    公开(公告)日：2000-06-13

    申请号：US880450

    申请日：1997-06-24

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

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

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61P25/00 ,  C07D401/06 ,  C07D407/14 ,  C07D413/14

    CPC分类号： C07D401/06 ,  C07D407/14 ,  C07D413/14

    摘要： A pharmaceutical compound of the formula ##STR1## in which X is --CR'R"-- or --C(O)-- where R' and R" are each hydrogen, C.sub.1-6 alkyl or optionally substituted phenyl, Y is oxygen or sulphur, R.sup.1, R.sup.2 and R.sup.7 are each selected from halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, nitro, cyano, amino, phenyl, phenoxy, benzyl, benzyloxy, acylamino, C.sub.1-4 alkylsulphonylamino, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, carboxamido, sulphonamido, hydroxy, methylenedioxy, carboxy, and heteroaryl, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each hydrogen, C.sub.1-6 alkyl or optionally substituted phenyl, n, m and p are each 0, 1, 2 or 3;or a salt or ester thereof.

    摘要翻译： 其中X为-CR'R“ - 或-C（O） - 的式的药物化合物，其中R'和R”各自为氢，C 1-6烷基或任选取代的苯基，Y为氧或硫， R1，R2和R7各自选自卤素，C1-4烷基，C1-4烷氧基，三氟甲基，硝基，氰基，氨基，苯基，苯氧基，苄基，苄氧基，酰氨基，C1-4烷基磺酰氨基，C1-4烷硫基，C1 -4-烷基磺酰基，甲酰氨基，磺酰氨基，羟基，亚甲二氧基，羧基和杂芳基，R 3，R 4，R 5和R 6各自为氢，C 1-6烷基或任选取代的苯基，n，m和p各自为0,1,2或 3; 或其盐或酯。

    Pharmaceutical compounds
    6.
    发明授权
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号：US5663375A

    公开(公告)日：1997-09-02

    申请号：US293786

    申请日：1994-08-22

    申请人： Michael Brunavs ,  Colin Peter Dell ,  Peter Thaddeus Gallagher ,  William Martin Owton ,  Colin William Smith

    发明人： Michael Brunavs ,  Colin Peter Dell ,  Peter Thaddeus Gallagher ,  William Martin Owton ,  Colin William Smith

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61K31/36 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61P1/16 ,  A61P3/10 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00 ,  C07D311/92 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D215/00 ,  C07D333/62 ,  C07D409/00

    CPC分类号： C07D405/04 ,  A61K31/35 ,  A61K31/36 ,  A61K31/38 ,  A61K31/40 ,  A61K31/44 ,  C07D311/92 ,  C07D407/04 ,  C07D409/04

    摘要： Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.12, --N(COR.sup.11).sub.2 or --N.dbd.CHOCH.sub.2 R.sup.11 where R.sup.11 and R.sup.12 are each hydrogen or C.sub.1-4 alkyl optionally substituted with carboxy, --N.dbd.CH--NR.sup.13 R.sup.14 where R.sup.13 is hydrogen or C.sub.1-4 alkyl and R.sup.14 is C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted heteroaryl, ##STR2## where X is C.sub.2-4 alkylene, or --NHSO.sub.2 R.sup.15 where R.sup.15 is C.sub.1-4 alkyl, trifluoromethyl or optionally substituted phenyl; and salts thereof.

    摘要翻译： 其中n为0,1或2并且R 1连接在7,8,9或10位的任何位置的式“IMAGE”的药物化合物，并且每个R 1为卤素，羧基，三氟甲基，羟基，C 1-4烷基 C 1-4烷氧基，C 1-4烷硫基，羟基-C 1-4烷基，羟基-C 1-4烷氧基，含氮杂环基，硝基，三氟甲氧基，-COOR 5，其中R5是酯基，-COR6，-CONR6R7或 - NR 6 R 7，其中R 6和R 7各自为氢或C 1-4烷基; R 2是选自噻吩基，吡啶基，苯并噻吩基，喹啉基，苯并呋喃基或苯并咪唑基的苯基，萘基或杂芳基，所述苯基，萘基和杂芳基任选被取代，或R 2是任选被C 1-4烷基取代的呋喃基; R3是腈，羧基，-COOR8，其中R8是酯基，或-CONR9R10，其中R9和R10各自是氢或C1-4烷基; 并且R 4为-NR 11 R 12，-NR 11 COR 12，-N（COR 11）2或-N = CHOCH 2 R 11，其中R 11和R 12各自为氢或任选被羧基取代的C 1-4烷基，-N = CH-NR 13 R 14，其中R 13为氢或C1- 4烷基和R 14是C 1-4烷基，任选取代的苯基或任选取代的杂芳基，其中X是C 2-4亚烷基或-NHSO 2 R 15，其中R 15是C 1-4烷基，三氟甲基或任选取代的苯基; 及其盐。