发明名称 GnRH antagonists
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-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 beta -(naphthyl)-D-Ala; R4 is a D-isomer aromatic amino acid or beta -(naphthyl)-D-Ala; R5 is Leu or N alpha Me-Leu; and R6 is Gly-NH2 or NHCH2CH3; provided however that either R3 or R4 is beta -(naphthyl)-D-Ala.
申请公布号 US4409208(A) 申请公布日期 1983.10.11
申请号 US19810256063 申请日期 1981.04.21
申请人 THE SALK INSTITUTE FOR BIOLOGICAL STUDIES 发明人 RIVIER, JEAN E. F.;VALE, JR., WYLIE W.
分类号 C07K14/575;A61K38/00;A61K38/04;A61P43/00;C07C231/00;C07K1/113;C07K7/16;C07K7/23;(IPC1-7):A61K37/00;C07C103/52 主分类号 C07K14/575
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