发明名称 GNRH ANTAGONISTS VI
摘要 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-(W)D-Phe-R3-R4-R5-R6(V)-R7-Arg-Pro-R10 wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R1 is dehydro-Pro, Pro, D-pGlu, D-Phe, D-Trp or beta -D-NAL; W is F, Cl, Cl2 Br, NO2 or C alpha Me-Cl; R3 is D-Trp, (NinFor)D-Trp or D-Trp which is substituted in the 5- or 6-position with NO2, NH2, OCH3, F, Cl, Br or CH3; R4 is Ser, Orn, AAL or aBu; R5 is Tyr, (3F)Phe, (2F)Phe, (3I)Tyr, (3CH3)Phe, (2CH3)Phe, (3Cl)Phe or (2Cl)Phe; R6 is D-Lys, D-Orn or D-Dap; V is (arg-R',R'')n(X), with n being 1 to 5 and R' and R'' being H, methyl, ethyl, propyl or butyl; R7 is Leu, NML, Nle or Nva; and R10 is Gly-NH2, D-Ala-NH2 or NH-Y, with Y being lower alkyl, cycloalkyl, fluoro lower alkyl or <IMAGE> where Q is H or lower alkyl.
申请公布号 ZA8506449(B) 申请公布日期 1986.04.30
申请号 ZA19850006449 申请日期 1985.08.23
申请人 THE SALK INSTITUTE FOR BIOLOGICAL STUDIES 发明人 WYLIE WALKER VALE, JR.;JEAN EDOUARD FREDERIC RIVIER
分类号 A61K38/04;A61K38/00;A61K38/22;A61P5/00;C07K7/23;C07K14/575 主分类号 A61K38/04
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