Antagonists of the antidiuretic and/or vasopressor action of arginine vasopressin

摘要

The invention provides compounds of the formula: …CHEM… in which:… X is D-Phe, D-Val, D-Leu, D-Ile, D-Arg, D-norvaline, D-norleucine, D-cyclohexylalanine, D- alpha -amino-butyric acid, D-threonine, D-methionine, D-Tyr(H), D-or-L-Tyr(X1) (in th which X1 is methyl, ethyl, n-propyl, isopropyl or butyl) or Tyr(X11) in which X11 is H, methyl or ethyl);… Y is Val, when X is other than Tyr (X11), or Gln, when X is Tyr (X11);… W is Pro or, when X is Tyr (X1), DELTA 3-Pro; and… Z is D- or L-Arg. …??Compounds of the above formula in which X is Tyr (X1) are antagonists of the diuretic action of ADH; compounds of the above formula in which X is other than Tyr (H), Tyr (X1) or Tyr (X11) and antagonists of the ADH activity of arginine vasopression; and compounds of the above formula in which X is Tyr (X11) are antagonists of the vasodepression activity of ADH. The invention also provides pharmaceutical compositions comprising compounds of the above formula in association with a pharmaceutical carrier or diluent.