Novel derivatives of arginine vasopressin antagonists

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

1986-12-30

1988-09-20

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514807, 530315, A61K 3734, C07K 716

Patent

active

047725869

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-Ile, D-Nva, D-Nle, D-Cha, D-Abu, D-Thr, D-Asn, D-Met or D-Gln; Y is Val, Ile, 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 NH(CH.sub.2).sub.3-6 NH.sub.2, NH(CH.sub.2).sub.2-6 OH, NHalk or NHbzl, provided that when Y is Val, Q is other than NHalk or NHbzl. Other compounds are those wherein Q is M-P, wherein M is Gly, (D- or L-)beta-Ala, (D- or L-)Ala, Sar, Orn, Val, Phe, Ile, Thr, Pro, Tyr, Arg or Ser and P is NHalk, NHbzl, NH(CH.sub.2).sub.2-6 OH, NH(CH.sub.2).sub.2-6 NH.sub.2 or OH, provided that when M is Gly, P is other than OH, and that when M is (D-or L-)beta-Ala, P is also NH.sub.2. Further compounds include decapeptides wherein Q is M-A-P', wherein M and A are selected independently from Gly, (D- or L-)beta-Ala, (D-or L-)Ala, Sar, Orn, Val, Phe, Ile, Thr, Pro, Tyr, Arg or Ser and P' is OH, NH.sub.2, NHalk, NH(CH.sub.2).sub.2-6 NH.sub.2, NHbzl or NH(CH.sub.2).sub.2-6 OH. Additional compounds include those wherein X is D-Tyr.

REFERENCES:
patent: 4285858 (1981-08-01), Cort et al.
patent: 4543349 (1985-09-01), Callahan et al.
patent: 4551445 (1985-11-01), Manning et al.
patent: 4624943 (1986-11-01), Callahan et al.
patent: 4649130 (1987-03-01), Manning et al.
patent: 4656248 (1987-04-01), Kalbag et al.
Manning, M. et al., Journal of Cardiovascular Pharmacology, vol. 8, Suppl. 7 (1986).
Hruby, V. J. et al., The Peptides, vol. 8, pp. 77-207, Academic, Orlando, Fl. (1987).

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