Antagonists of the antidiuretic action of arginine vasopressin

Details Antagonists of the antidiuretic action of arginine vasopressin Antagonists of the antidiuretic action of arginine vasopressin

1983-01-05

1985-01-01

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Immunoglobulin, antiserum, antibody, or antibody fragment,...

Reduced antigenicity, reduced ability to bind complement, or...

2601125R, A61K 3700, C07C10352

Patent

active

044915772

ABSTRACT:
Compounds acting as antagonists of the antidiuretic activity of arginine vasopressin are those of the formula ##STR1## wherein X is (D- or L-)Tyr(R), D-Tyr, D-Phe, D-Val, D-Leu D-Ile, D-Arg, D-Gln, D-Asn, D-NVa, D-Nle, D-Cha, D-Abu, D-Thr or D-Met; R is methyl, ethyl, propyl or butyl and Z is D- or L-Arg. Also acting as antagonists of the antidiuretic action of arginine vasopressin are compounds of the formula ##STR2## wherein X and Z are as above and n is 4 or 5. Other antagonists of the antidiuretic action of arginine vasopressin are of the formula ##STR3## wherein X and n are as above and Z' is (D- or L-)Orn or (D- or L-)Lys. Other antagonists of the antidiuretic action of arginine vasopressin are of the formula ##STR4## wherein X is above, W is D-Pro, .DELTA..sup.3 -Pro or HO-Pro; Z" is (D- or L-)Arg, (D- or L-)Lys or (D- or L-)Orn and n is 4 or 5; provided that when X is (D- or L-)Tyr(R) and n is 5, W is HO-Pro or D-Pro and that when X is D-Gln or D-Asn and n is 5, W is also Pro.

REFERENCES:
patent: 4367225 (1983-01-01), Manning et al.
patent: 4399125 (1983-08-01), Manning et al.

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