Pyrazolo 4,3-c pyridines, a process for their preparation and their use as serotonin reuptake inhibitors
申请人:HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED
公开号:EP0594001A1
公开(公告)日:1994-04-27
The invention relates to compounds of the frmula
wherein
Ar is
or pyridyl;
R₁ is H,-(CH₂)pNR₂R₃,
R₂ is hydrogen or loweralkyl;
R₃ is hydrogen or loweralkyl;
R₄ is hydrogen or loweralkyl;
X and Y are independently halogen, trifluoromethyl, nitro, loweralkyl, loweralkoxy or hydroxy;
n is 0, 1, 2 or 3;
m is 0, 1 or 2;
p and q are independently 2, 3 or 4;
or a pharmaceutically acceptable addition salt and/or hydrate thereof, or where applicable, a geometric or optical isomer or racemic mixture thereof.
This invention also relates to a process for making the compounds and to pharmaceutical compositions, and to their use as serotonin reuptake inhibitors.
本发明涉及下列化合物
其中
Ar 是
或吡啶基;
R₁ 是 H、-(CH₂)pNR₂R₃、
R₂ 是氢或低级烷基;
R₃ 是氢或低级烷基;
R₄ 是氢或低级烷基;
X 和 Y 独立地为卤素、三氟甲基、硝基、低级烷基、低级烷氧基或羟基;
n 是 0、1、2 或 3;
m 是 0、1 或 2;
p 和 q 独立地为 2、3 或 4;
或其药学上可接受的加成盐和/或水合物,或(如适用)其几何或光学异构体或外消旋混合物。
本发明还涉及制造这些化合物的工艺和药物组合物,以及它们作为血清素再摄取抑制剂的用途。