Cyclic gnrh antagonists

Details Cyclic gnrh antagonists Cyclic gnrh antagonists

C - Chemistry, Metallurgy

07

K

C07K 7/23 (2006.01) A61K 38/09 (2006.01) C07K 7/64 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2073766

2073766 9112013 PCTABS00006 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 GnRG, 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 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.

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