申请人:Brodney A. Michael
公开号:US20050245521A1
公开(公告)日:2005-11-03
The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I
wherein R
1
is a group of the formula G
1
or G
2
depicted below,
wherein R
1
, R
3
, R
6
, R
13
X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT
1
) receptors, specifically, of one or both of the 5-HT
1A
and 5-HT
1B
receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT
1
agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.
本发明涉及一种新型苯甲基(亚)内酰胺衍生物,化合物的式子为I,其中R1是下面所示的式子G1或G2的基团,其中R1、R3、R6、R13、X、a、n和m的定义如本说明书所述,其药学上可接受的盐,以及包括选择性5-羟色胺1(5-HT1)受体的拮抗剂、反向激动剂和部分激动剂的药物组合物,具体来说,是5-HT1A和5-HT1B受体中的一个或两个。本发明的化合物在治疗或预防抑郁症、焦虑症、强迫症和其他需要5-HT1受体激动剂或拮抗剂的疾病方面有用,并且具有减少心脏副作用的潜力,特别是QTc延长。