申请人:Syntex (U.S.A.) Inc.
公开号:US04957914A1
公开(公告)日:1990-09-18
1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl; each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; and Y is lower alkylene having from two to four carbon atoms; and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.
1,9-烷基桥联的2,3,4,5-四氢-1H-3-苯并氮平及其衍生物,即化合物I的化合物:##STR1##其中:R选自以下组:氢,氰基,较低的烷基,较低的烯基和芳基烷基;每个R1、R2和R3分别独立地选自以下组:氢,羟基,卤素,三氟甲基,硝基,酰胺基,较低的烷氧基,较低的烷基和较低的烷基硫基;Y为具有2至4个碳原子的较低烷基,以及其药学上可接受的盐,可用作中枢神经系统药物,例如抗抑郁剂,抗焦虑剂和降压剂,和/或其前体。