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公开(公告)号:US07432293B2
公开(公告)日:2008-10-07
申请号:US10545245
申请日:2004-02-13
IPC分类号: A61K31/42 , A61K31/4245 , C07D263/30 , C07D271/06
CPC分类号: C07D271/06 , C07D261/08 , C07D263/32 , C07D413/04
摘要: The present invention relates to compounds of formula (I): wherein R1 is hydroxy, C1-4 alkoxy, amino, C1-4 alkyl-amino, di C1-4alkylamino, benzyloxy or C2-C7 alkanoyl, R2 is C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxy C1-4alkoxy, CF3, halogen, C1-4alkylamino, di C1-4alkylamino, di C1-4 alkylamino C1-4 alkoxy or N—C1-4 alkoxy C1-4 alkyl-N—C1-4 alkylamino, N—C1-4 alkyl-piperazinyl, morpholinyl or pyrrolidinyl-C1-4 alkoxy, wherein the C1-4 alkyl radicals in R2 are optionally further substituted by C1-4 alkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3, X is O, Y is CH, Z is N and W is CH, (b) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3 or chloro, X is N, Y is O, Z is CH and W is CH, (c) R1 is not hydroxy when R2 is CF3, X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them.
摘要翻译: 本发明涉及式(I)的化合物:其中R 1是羟基,C 1-4烷氧基,氨基,C 1-4 烷基 - 氨基,二C 1-4烷基氨基,苄氧基或C 2 -C 7烷酰基,R 2 SUB >为C 1-4烷基,C 1-4烷氧基,C 1-4烷氧基C 1-4烷基 烷氧基,CF 3,卤素,C 1-4烷基氨基,二C 1-4烷基氨基,二C 1-4 烷基氨基C 1-4烷氧基或NC 1-4烷氧基C 1-4烷基-NC 1-4 烷基氨基,NC 1-4烷基 - 哌嗪基,吗啉基或吡咯烷基-C 1-4烷氧基,其中C 1-4 - R 2中的烷基任选进一步被C 1-4烷基,卤素,氰基,氨基,烷氧基或烷硫基取代,X是N或O,Y是N ,O或CH,Z是N或CH,W是N或CH,条件是当R(R)不为羟基或C 1-4烷氧基时, 2是CF 3,X是O,Y是C H,Z是N,W是CH,(b)当R 2是CF时,R 1不是羟基或C 1-4烷氧基 3是或氯,X是N,Y是O,Z是CH,W是CH,(c)R 1不是羟基, SUB>是CF 3,X是O,Y是N,Z是CH,W是CH,(d)X和Y不同时为O,其盐; 它们的制备,它们的用途和含有它们的药物组合物。
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公开(公告)号:US20060089365A1
公开(公告)日:2006-04-27
申请号:US10545245
申请日:2004-02-13
IPC分类号: A61K31/5377 , A61K31/496 , A61K31/4439 , A61K31/4245 , A61K31/4196 , C07D413/14 , C07D403/14
CPC分类号: C07D271/06 , C07D261/08 , C07D263/32 , C07D413/04
摘要: The present invention relates to compounds of formula (I): wherein R1 is hydroxy, C1-4 alkoxy, amino, C1-4 alkyl-amino, di C1-4alkylamino, benzyloxy or C2-C7 alkanoyl, R2 is C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxy C1-4alkoxy, CF3, halogen, C1-4alkylamino, di C1-4alkylamino, di C1-4 alkylamino C1-4 alkoxy or N—C1-4 alkoxy C1-4 alkyl-N—C1-4 alkylamino, N—C1-4 alkyl-piperazinyl, morpholinyl or pyrrolidinyl-C1-4 alkoxy, wherein the C1-4 alkyl radicals in R2 are optionally further substituted by C1-4 alkyl, halogen, cyano, amino, alkoxy or alkylthio, X is N or O, Y is N, O or CH, Z is N or CH, and W is N or CH, provided that (a) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3, X is O, Y is CH, Z is N and W is CH, (b) R1 is not hydroxy or C1-4 alkoxy when R2 is CF3 or chloro, X is N, Y is O, Z is CH and W is CH, (c) R1 is not hydroxy when R2 is CF3, X is O, Y is N, Z is CH and W is CH and (d) X and Y are not simultaneously O, the salts thereof; their preparation, their use and pharmaceutical compositions containing them.
摘要翻译: 本发明涉及式(I)的化合物:其中R 1是羟基,C 1-4烷氧基,氨基,C 1-4 烷基 - 氨基,二C 1-4烷基氨基,苄氧基或C 2 -C 7烷酰基,R 2 SUB >为C 1-4烷基,C 1-4烷氧基,C 1-4烷氧基C 1-4烷基 烷氧基,CF 3,卤素,C 1-4烷基氨基,二C 1-4烷基氨基,二C 1-4 烷基氨基C 1-4烷氧基或NC 1-4烷氧基C 1-4烷基-NC 1-4 烷基氨基,NC 1-4烷基 - 哌嗪基,吗啉基或吡咯烷基-C 1-4烷氧基,其中C 1-4 - R 2中的烷基任选进一步被C 1-4烷基,卤素,氰基,氨基,烷氧基或烷硫基取代,X是N或O,Y是N ,O或CH,Z是N或CH,W是N或CH,条件是当R(R)不为羟基或C 1-4烷氧基时, 2是CF 3,X是O,Y是C H,Z是N,W是CH,(b)当R 2是CF时,R 1不是羟基或C 1-4烷氧基 3是或氯,X是N,Y是O,Z是CH,W是CH,(c)R 1不是羟基, SUB>是CF 3,X是O,Y是N,Z是CH,W是CH,(d)X和Y不同时为O,其盐; 它们的制备,它们的用途和含有它们的药物组合物。
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公开(公告)号:US07087756B2
公开(公告)日:2006-08-08
申请号:US10486569
申请日:2002-08-14
IPC分类号: C07D471/02
CPC分类号: C07D498/04
摘要: The invention provides compounds of formula I, wherein X, Y, R1, R2, and R3 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.
摘要翻译: 本发明提供式I化合物,其中X,Y,R 1,R 2和R 3是如说明书中所定义的, 及其制备。 式I的化合物可用作药物。
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