CONDENSED AZEPINES AS VASOPRESSIN AGONISTS

摘要

This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V¹ and V² are both H, OMe or F, or one of V¹ and V² is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N₃, NH₂, NHBn or NH-acyl and the other is H, or V¹ and V² together are -O, -O(CH₂)_pO- or -S(CH₂)_pS-; W¹ is either O or S; X¹ and X² are both H, or together are -O or -S; Y is OR⁵ or NR⁶R⁷; R¹, R², R³ and R₄ are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R⁵ is selected from H and lower alkyl; R⁶ and R⁷ are independently selected from H and lower alkyl, or together are -(CH₂)_n-; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.