发明名称 NONAPEPTIDE AND DECAPEPTIDE AGONISTS OF LUTEINIZING HORMONE RELEASING HORMONE CONTAINING HETEROCYCLIC AMINO ACID RESIDUES
摘要 Nonapeptide and decapeptide analogs of LH-RH of the formula <IMAGE> (I) and the pharmaceutically acceptable salts thereof wherein: V is tryptophyl, phenylalanyl or 3-(1-naphthyl)-L-alanyl; W is tyrosyl, phenylalanyl or 3-(1-pentafluorophenyl)-L-alanyl; X is a D-amino acid residue of the formula: <IMAGE> wherein R is a heterocyclic aryl containing radical selected from the group consisting of radicals represented by the following structural formulas: <IMAGE> <IMAGE> +TR <IMAGE> wherein A and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine, and bromine, and G is selected from the group consisting of oxygen, nitrogen, and sulfur; Y is leucyl, isoleucyl, nor-leucyl or N-methyl-leucyl; Z is glycinamide or -NH-R1, wherein: R1 is lower alkyl, cycloalkyl, fluoro lower alkyl or <IMAGE> wherein R2 is hydrogen or lower alkyl, are disclosed. These compounds exhibit potent LH-RH agonist properties.
申请公布号 ZA8104214(B) 申请公布日期 1983.02.23
申请号 ZA19810004214 申请日期 1981.06.22
申请人 SYNTEX INC 发明人 JONES G;NESTOR J;VICKERY B
分类号 C07D235/16;C07D277/64;C07K7/23 主分类号 C07D235/16
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