GnRH Antagonists VI

Details GnRH Antagonists VI GnRH Antagonists VI

1984-09-07

1986-01-21

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

2601125R, 2601125LH, C07C10352, A61K 3702

Patent

active

045658048

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 -(W)D-Phe-R.sub.3 -R.sub.4 -R.sub.5 -R.sub.6 (V)-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, Pro, D-pGlu, D-Phe, D-Trp or .beta.-D-NAL; W is F, Cl, Cl.sub.2 Br, NO.sub.2 or C.sup..alpha. Me-Cl; R.sub.3 is D-Trp, (N.sup.in For)D-Trp or D-Trp which is substituted in the 5- or 6-position with NO.sub.2, NH.sub.2, OCH.sub.3, F, Cl, Br or CH.sub.3 ; R.sub.4 is Ser, Orn, AAL or aBu; R.sub.5 is Tyr, (3F)Phe, (2F)Phe, (3I)Tyr, (3CH.sub.3)Phe, (2CH.sub.3)Phe, (3Cl)Phe or (2Cl)Phe; R.sub.6 is D-Lys, D-Orn or D-Dap; V is (arg-R',R").sub.n (X), with n being 1 to 5 and R' and R" being H, methyl, ethyl, propyl or butyl; R.sub.7 is Leu, NML, Nle or Nva; and R.sub.10 is Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-Y, with Y being lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR1## where Q is H or lower alkyl.

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.
Yabe et al., Chem. Pharm. Bull., vol. 27, No. 8, 1979, pp. 1907-1911.

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