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Nonapeptide and decapeptide agonists of luteinizing hormone releasing hormone containing heterocyclic amino acid residues

机译:黄体化激素释放激素的九肽和十肽激动剂,含杂环氨基酸残基

摘要

Nonapeptide and decapeptide analogs of LH-RH of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein: V is tryptophyl, phenylalanyl or 3-(1-naphthyl)-L-alanyl;PPW is tyrosyl, phenylalanyl or 3-(1-pentafluorophenyl)-L-alanyl;P PX is a D-amino acid residue of the formula: ##STR2## wherein R is a heterocyclic aryl containing radical selected from the group consisting of radicals represented by the following structural formulas: ##STR3## 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;PPY is leucyl, isoleucyl, nor-leucyl or N-methyl-leucyl;PPZ is glycinamide or --NH--R.sup.1, wherein:PPR.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR4## wherein R.sup.2 is hydrogen or lower alkyl,PPare disclosed. These compounds exhibit potent LH- RH agonist properties.
机译:式## STR1 ##的LH-RH的九肽和十肽类似物及其药学上可接受的盐,其中:V是色氨酸,苯丙氨酰基或3-(1-萘基)-L-丙氨酰基;& P& W&酪氨酰基,苯丙氨酰基或3-(1-五氟苯基)-L-丙氨酰基; P是下式的D-氨基酸残基:其中R是选自以下的基团的杂环芳基:由以下结构式表示的基团组成的基团:其中A和A'独立地选自氢,低级烷基,氯和溴,而G选自氧, N是硫,氮和硫; Y是亮基,异亮基,正亮基或N-甲基亮基; Z是甘氨酰胺或-NH-Rupup.1,其中:公开了

R 1是低级烷基,环烷基,氟代低级烷基或其中R 2是氢或低级烷基的化合物。这些化合物表现出有效的LH-RH激动剂性质。

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