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。

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。

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。