Novel derivatives of arginine vasopressin antagonists

Details Novel derivatives of arginine vasopressin antagonists Novel derivatives of arginine vasopressin antagonists

1985-01-23

1987-03-10

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514807, 530315, A61K 3724, C07K 716

Patent

active

046491309

ABSTRACT:
Compounds acting as antagonists of the antidiuretic/and or vasopressor activity of arginine vasopressin are those of the formula ##STR1## wherein n is 4 or 5; X is (D- or L-)Tyr(R), D-Phe, D-Val, D-Leu, D-lle, D-Nva, D-Nle, D-Cha, D-Abu, D-Thr, D-Asn, D-Met or D-Gln; Y is Val, lle, Thr, Ala, Lys, Cha, Nva, Met, Nle, Orn, Ser, Asn, Gln, Phe, Tyr, Gly, Abu or Leu; Z is (D- or L-) Arg, Orn or Lys; Q is Arg(NH.sub.2), Ser(NH.sub.2), (D- or L-)Ala(NH.sub.2), Gly, OH or NH.sub.2 and R is methyl, ethyl, propyl or butyl; provided that, when Y is Gln or Val, R may also be H. Further compounds are those wherein Q is Orn(NH.sub.2), NHCH.sub.2 CH.sub.2 NH.sub.2, Val(NH.sub.2), Phe(NH.sub.2), lle(NH.sub.2), Thr(NH.sub.2), Pro(NH.sub.2) or Tyr(NH.sub.2).

REFERENCES:
patent: 4469679 (1984-09-01), Huffman et al.

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