Cyclic GnRH antagonists

Details Cyclic GnRH antagonists Cyclic GnRH antagonists

1990-02-06

1991-11-12

Lee, Lester L.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Cyclic peptides

530311, A61K 3700, A61K 3738, C07K 512, C07K 720

Patent

active

050649396

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 include cyclic, bicyclic and tricyclic analogs of the decapeptide GnRH, and preferably there are at least two covalent bonds between the residues in the 4- and 10-positions, the residues in the 5- and 8-positions and the residues in the 1- and 3-positions, respectively. Examples of such bonds include a disulfide linkage between Cys residues, an amide linkage between a side chain amino group and a side chain carboyxl 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.

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patent: 4801577 (1989-01-01), Nestor, Jr. et al.
Nestor et al., "Design of Luteinizing Hormone Releasing Hormone Antagonists with Reduced Potential for Side Effects", Peptides 1988, 592-594.
Eleventh American Peptide Symposium, The Salk Institute and University of California, San Diego, La Jolla, CA., Jul. 9-14, 1989: Abstract LT7.
Third Symposium of the Protein Society, Seattle, WA., Jul. 29-Aug. 2, 1989: Abstract re Design of GnRH Antagonists.

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