发明名称 N-PYRROLIDIN-3-YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALINE RE-UPTAKE INHIBITORS, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITION CONTAINING THEM
摘要 A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, -C(X)Y, C3-8cyc1oa1ky1, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-8allkyl, C1-8alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkaxy-C1-6alkyl and C1-4alkyl-S-C1-4alkyl; R2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C1-8alkyl, C1-8alkoxy, OH, halo, CF3, OCF3 SCF3, hydroxy-C1-6alkyl, C1-4alkcoxy-C1-6alkyl and C1-4alkyl-S-C1-4alkyl; R3 is C1-6alkyl, C3-8cyc1oa1kcyl, C3-8cyc1oa1ky1-C1-4a1ky1, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C1-6alkyl, C1-6alkoxy, OH, halo, CF3, OCF3, SCF3, hydroxy-C1-6alkyl, C1-4alkoxy - C1-6alkyl and C1-4alkyl-SC1-4alkyl; X is S or O; Y is H, C1-6alkyl, aryl, het, aryl-C1-4alkyl or het-C1-4alkyl; 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.
申请公布号 UA80338(C2) 申请公布日期 2007.09.10
申请号 UA20050011011 申请日期 2004.06.07
申请人 PFIZER INC. 发明人 STOBIE ALAN
分类号 A61P13/00;A61P25/24;A61P29/00;C07D207/14 主分类号 A61P13/00
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