Gnrh antagonists ix

Details Gnrh antagonists ix Gnrh antagonists ix

C - Chemistry, Metallurgy

07

K

530/7.64

C07K 7/64 (2006.01) C07K 7/23 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1288195

GnRH ANTAGONISTS IX ABSTRACT OF THE DISCLOSURE 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. An amide linkage with the 4-position residue having the carboxyl group side chain is preferred, with Asp and daP being most preferred.

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