| 摘要 |
<p>This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V<SUP>1 </SUP>and V<SUP>2 </SUP>are both H, OMe or F, or one of V<SUP>1 </SUP>and V<SUP>2 </SUP>is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N<SUB>3</SUB>, NH<SUB>2</SUB>, NHBn or NH-acyl and the other is H, or V<SUP>1 </SUP>and V<SUP>2 </SUP>together are -O, -O(CH<SUB>2</SUB>)<SUB>p</SUB>O- or -S(CH<SUB>2</SUB>)<SUB>p</SUB>S-; W<SUP>1 </SUP>is either O or S; X<SUP>1 </SUP>and X<SUP>2 </SUP>are both H, or together are -O or -S; Y is OR<SUP>5 </SUP>or NR<SUP>6</SUP>R<SUP>7</SUP>; R<SUP>1</SUP>, R<SUP>2</SUP>, R<SUP>3 </SUP>and R<SUB>4 </SUB>are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R<SUP>5 </SUP>is selected from H and lower alkyl; R<SUP>6 </SUP>and R<SUP>7 </SUP>are independently selected from H and lower alkyl, or together are -(CH<SUB>2</SUB>)<SUB>n</SUB>-; 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.</p> |
