Gnrh antagonists

Details Gnrh antagonists Gnrh antagonists

C - Chemistry, Metallurgy

07

K

530/7.06, 167/10

C07K 7/06 (2006.01) C07K 7/23 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1241950

GnRH ANTAGONISTS 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 prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure. X-R1-R2-R3-Ser-TYr-R4-R5-Arg-Pro-R6 wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R1 is dehydro Pro or dehydro D-Pro; R2 is D-Phe, Cl-D-Phe, dichloro-D-Phe, CF3-D-Phe, F-D-Phe, difluoro-D-Phe, AcNH-D-Phe, NO2-D-Phe, dinitro-D-Phe, Br-D-Phe, dibromo-D-Phe, CH3-S-D-Phe, OCH3-D-Phe or CH3-D-Phe; R3 is D-Trp or B-D-NAL; R4 is a D-isomer amino acid and preferably B-D-NAL; R5 is Leu or N.alpha.Me-Leu; and R6 i8 Gly-NH2 or NHCH2CH3; provided however that either R3 or R4 is B-D-NAL.

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