GnRH antagonists IX

Details GnRH antagonists IX GnRH antagonists IX

1985-05-09

1987-04-28

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530328, A61K 3743, C07K 706

Patent

active

046614729

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 of such GnRH antagonists prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. These peptides may be used to treat steroid-dependent tumors, such as prostatic and mammary tumors. The peptides are cyclic analogs of the decapeptide GnRH wherein there is a covalent bond between the residue in the 4-position and the residue in the 10-position. Examples of such bonds include the disulfide linkage between Cys residues, an amide linkage between a side chain amino group and a side chain carboxyl group, a dicarba linkage between side-chain alkyl groups, and a carba linkage between a side-chain alkyl group and a side-chain sulfhydryl group.

REFERENCES:
patent: 4133805 (1979-01-01), Yardley
patent: 4140767 (1979-02-01), Veber
patent: 4482486 (1984-11-01), Brtnik et al.
patent: 4492651 (1985-01-01), Sarantakis
GnRh Analogs: Structure--Activity Relationships, Jean Rivier et al., pp. 13-23, 1981.
Design of Peptide Analogs, Struthers and Hagler, pp. 239-261, 1984, American Chemical Society.

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