Nonapeptide and decapeptide agonists of luteinizing hormone releasing hormone containing heterocyclic amino acid residues, methods for their preparation, pharmaceutical compounds containing them, and their pharmaceutical use

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.