GnRH antagonist quality II

摘要

A peptide having formula X-beta-D-2NAL-R2-D-Trp-Ser-R5-R6-R7Arg-Pro- R10[where X=H or an acyl gp. having 7 or less carbon atoms; R2= Cl-D- Phe, F-D-Phe, NO2-D-Phe, Cl2-D-Phe or Br-D-Phe; R5=Tyr or 2-Cl-Phe; R6=4-NH2-D-Phe or D-Arh; R7= Leu or NaMe-Leu; R10= Gly-NH2 NHCH2CH3 or D-Arh-; R7= Leu or NaMe-Leu; R10= Gly-NH2, NHCH2CH3 or D-Ala-NH2 or its pharmaceutically nontoxical salt or its intrmediate of formula X1-beta-D-2NAL-R2-DTrp-Ser (X2)-R5(X3)-R6(X4)-R7-Arg(X4)-Pro-X5 is provided. The peptide is useful to inhibit prodn. of gonadotropin and sex hormones and to suppress ovulation.