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1. 发明申请

WO2004110995A1 N-PYRROLIDIN-3-YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALINE RE-UPTAKE INHIBITORS 审中-公开
标题翻译： N-吡咯烷-3-基酰胺衍生物作为丝氨酸蛋白酶和肾上腺素再摄取抑制剂
公开(公告)号：WO2004110995A1
公开(公告)日：2004-12-23
申请号：PCT/IB2004/001943
申请日：2004-06-07
申请人： PFIZER LIMITED , PFIZER INC. , FISH, Paul, Vincent , FRAY, Michael, Jonathan , LOVERING, Deborah, Jane , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
发明人： FISH, Paul, Vincent , FRAY, Michael, Jonathan , LOVERING, Deborah, Jane , STOBIE, Alan , WAKENHUT, Florian , WHITLOCK, Gavin, Alistair
IPC分类号： C07D207/14
CPC分类号： C07D207/14
摘要： A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R 1 is H, C 1 _ 6 alkyl, -C(X)Y, C 3 _ 8 cycloalkyl, aryl, het, aryl-C l _ 4 alkyl or het-C l _ 4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1_ 8 allkyl, C 1 _ 8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C l _ 6 alkyl, C 1 _ 4 alkoxy-C 1 _ 6 alkyl and C1_ 4 alkyl-S-C 1 _ 4 alkyl; R 2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C 1 _ 8 alkyl, C 1 _ 8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF3, hydroxy-C 1 _ 6 alkyl, C1_4alkoxy-C 1 _ 6 alkyl and C1_ 4 alkyl-S-C 1 _ 4 alkyl; R 3 is C 1 _ 6 alkyl, C 3 _ 8 cycloalkyl, C 3 _ 8 cycloalkyl-C 1 _ 6 alkyl, aryl, het, aryl-C l _ 4 alkyl or het-C 1 _ 4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C 1 _ 6 alkyl, C 1 _ 6 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1 _ 6 alkyl, C 1 _ 4 alkoxy - C 1 _ 6 alkyl and C 1 _ 4 alkyl-SC 1 _ 4 alkyl; X is S or O; Y is H, C 1 _ 6 alkyl, aryl, het, aryl-C 1 _ 4 alkyl or het-C 1 _ 4 alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.
摘要翻译：式（I）化合物及其药学和/或兽医学上可接受的衍生物，其中R 1是H，C 1-6烷基，-C（X）Y，C 3-8环烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基-C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基的取代基取代; R 2是芳基或杂芳基，各自任选被至少一个独立地选自C 1-8烷基，C 1-8烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-S-C 1-4烷基的取代基取代; R 3是C 1-6烷基，C 3-8环烷基，C 3-8环烷基-C 1-6烷基，芳基，杂芳基，C 1-4烷基或叔丁基C 1-4烷基，其中环烷基，芳基或苯基基团任选被至少一个独立地选自C 1-6烷基，C 1-6烷氧基，OH，卤素，CF 3，OCF 3，SCF 3，羟基-C 1-6烷基，C 1-4烷氧基-C 1-6烷基和C 1-4烷基-C 1-4烷基; X是S或O; Y是H，C 1-6烷基，芳基，杂环基，芳基-C 1-4烷基或叔丁基C 1-4烷基; n为1或2，条件是当n为1时，m为0或1，当n为2时，m为0，其中如果m为0，则*表示手性中心。本发明的化合物表现出5-羟色胺和去甲肾上腺素再摄取抑制剂的活性，因此可用于各种治疗领域，例如尿失禁。

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