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 (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: wherein R is a heterocyclic aryl containing radical selected from the group consisting of radicals represented by the following structural formulas: +TR 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 wherein R2 is hydrogen or lower alkyl, are disclosed. These compounds exhibit potent LH-RH agonist properties.