GnRH antagonists VII

Details GnRH antagonists VII GnRH antagonists VII

1984-09-21

1987-03-24

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530313, 514800, A61K 3743, C07K 720

Patent

active

046525505

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: X-R.sub.1 -R.sub.2 -R.sub.3 -Ser-Tyr-R.sub.6 -R.sub.7 -Arg-Pro-R.sub.10 wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R.sub.1 is dehydro-Pro or .beta.-D-NAL; R.sub.2 is Cl-D-Phe, F-D-Phe, NO.sub.2 -D-Phe, C.sup..alpha. Me-4-Cl-D-Phe, Cl.sub.2 -D-Phe or Br-D-Phe; R.sub.3 is D-Trp, substituted D-Trp, .beta.-D-NAL, or D-PAL; R.sub.6 is a D-isomer of a lipophilic amino acid or is 4-NH.sub.2 -D-Phe, D-Lys, D-Orn, D-Har, D-His, 4-gua-D-Phe, D-PAL or D-Arg; R.sub.7 is Nle, Phe, Met, Tyr, Nva, Trp, Cys, PAL or 4F-D-Phe; and R.sub.10 is Gly-NH.sub.2 or D-Ala-NH.sub.2 ; provided however that when R.sub.1 is .beta.-D-NAL, then R.sub.6 is 4-NH.sub.2 -D-Phe, D-Lys, D-Orn, D-Har, D-His, 4-gua-D-Phe, D-PAL or D-Arg.

REFERENCES:
patent: 4234571 (1980-11-01), Nestor et al.
patent: 4317815 (1982-03-01), Coy et al.
patent: 4341767 (1982-07-01), Nestor et al.
patent: 4444759 (1984-04-01), Rivier et al.
patent: 4481190 (1984-11-01), Nestor et al.
Coy et al., Endocrinology, vol. 110, No. 4, 1982, pp. 1445-1447.
Yalie et al., Chem. Pharm. Bull., vol. 27, No. 8, 1979, pp. 1907-1911.

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