| abstract |
The novel benzazine derivatives of formula (1) or salts thereof exhibit excellent antibasopressin activity, oxytocin antagonist activity and vasopressin agonist activity, and are useful as vasopressin antagonists, vasopressin agonists and oxytocin antagonists.n n n Formula 1n n n n n n n n In the above formula,n n n R 1 is a hydrogen atom or a halogen atom,n n n A is lower alkylene,n n n R 2 and R 3 are the same or different and each is hydrogen atom, lower alkoxy, lower alkyl having any lower alkoxy substituent, or the like, or R 2 and R 3 are bonded together with the nitrogen atom to which they are attached to be optionally lower alkyl and the like. To form a 5 to 7 membered saturated heterocyclic group which may be substituted,n n n R 4 is a hydrogen atom, lower alkyl, OH or the like,n n n R 5 is —NHR 6 where R 6 is a lower alkyl group or pyrrolidinyl. |