Bicyclic GnRH antagonists and a method for regulating the secret

Details Bicyclic GnRH antagonists and a method for regulating the secret Bicyclic GnRH antagonists and a method for regulating the secret

1992-11-09

1994-12-06

Hill, Jr., Robert J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530317, 530313, 530328, 514 11, 514 15, C07K 706, C07K 512, A61K 3738

Patent

active

053710703

ABSTRACT:
Peptides which have substantial bioactivity to inhibit the secretion of gonadotropins by the pituitary gland and to inhibit the release of steroids by the gonads. Administration of an effective amount of such GnRH antagonists prevents ovulation and/or the release of steroids by the gonads. They may also be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are bicyclic analogs of the decapeptide GnRH having two covalent bonds, between the residues in the 4- and 10-positions and the residues in the 5- and 8-positions. The latter linkage includes peptide bonds between a residue of an .alpha.-amino acid outside of the main chain and a side-chain carboxyl group of the 5-position residue and a side-chain amino group of the 8-position residue.

REFERENCES:
patent: 4133805 (1979-01-01), Yardley
patent: 5043322 (1991-08-01), Rivier et al.
patent: 5064939 (1991-11-01), Rivier et al.
Theobald, et al., "Novel Gonadotropin-Releasing Hormone Antagonists: Peptides Incorporating Modified N.sup.107 -Cyanoguanidino Moieties", J. of Medicinal Chemistry, 34, 2395-2402 (1991).

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