GnRH antagonists VIII

Details GnRH antagonists VIII GnRH antagonists VIII

1986-12-23

1988-04-26

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514800, 530313, A61K 3743, C07K 720

Patent

active

047405007

ABSTRACT:
Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure: Ac-.beta.-D-NAL-R.sub.2 -D-3PAL-Ser-Arg-R.sub.6 -Leu-Arg-Pro-R.sub.10 wherein R.sub.2 is Cl-D-Phe, F-D-Phe, NO.sub.2 -D-Phe, Br-D-Phe, 3,4Cl.sub.2 -D-Phe or C.alpha.Me-Cl-D-Phe; R.sub.6 is D-3PAL, D-Trp, For-D-Trp, NO.sub.2 -D-Trp, (imBzl)D-His, D-Tyr or .beta.-D-NAL; and R.sub.10 is Gly-NH.sub.2, NHCH.sub.2 CH.sub.3, NHNHCONH.sub.2 or D-Ala-NH.sub.2.

REFERENCES:
patent: 4253997 (1981-03-01), Sarantakis
patent: 4292313 (1981-09-01), Vale, Jr. et al.
patent: 4341767 (1982-07-01), Nestor et al.
patent: 4481190 (1984-11-01), Nestor et al.
patent: 4504414 (1985-03-01), Folkers et al.
patent: 4547370 (1985-10-01), Roeske
patent: 4569927 (1986-02-01), Rivier et al.

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