Benzazepine derivatives with vasopressin agonistic activity

摘要

PCT No. PCT/JP96/03652 Sec. 371 Date Jun. 12, 1998 Sec. 102(e) Date Jun. 12, 1998 PCT Filed Dec. 13, 1996 PCT Pub. No. WO97/22591 PCT Pub. Date Jun. 26, 1997Novel benzazepine derivative of the formula [1]: wherein R1 is H or halogen, A is lower alkylene, R2 and R3 are the same or different and each H, lower alkoxy, lower alkyl having optionally a lower alkoxy substituent, etc., or R2 and R3 may combine together with the nitrogen to which they bond to form a 5- to 7-membered saturated heterocyclic group which may optionally be substituted by a lower alkyl, etc., R4 is H, lower alkyl, OH, etc., R5 is -NHR6 (R6 is lower alkyl) or pyrrolidinyl, or a salt thereof, which show excellent anti-vasopressin activity, oxytocin antagonistic activity and vasopressin agonistic activity, and are useful as a vasopressin antagonist, a vasopressin agonist and an oxytocin antagonist.