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NONAPEPTIDE AND DECAPEPTIDE DERIVATIVES OF LUTEINIZING HORMONE RELEASING HORMONE, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
NONAPEPTIDE AND DECAPEPTIDE DERIVATIVES OF LUTEINIZING HORMONE RELEASING HORMONE, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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机译:促黄体激素释放激素的降肽和十肽衍生物,其制备和组成它们的药物成分
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摘要
Nonapeptide and decapeptide analogs of LH-RH of the formula (pyro)Glu-His-V-Ser-W-X-Y-Arg-Pro-Z (I) and the pharmaceutically acceptable salt 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 CHEM wherein R is (a) a carbocyclic aryl-containing radical selected from the group consisting of naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl, benzhydryl and phenyl substituted with three or more straight chain lower alkyl groups; or (b) a saturated carbocyclic radical selected from the group consisting of cyclohexyl substituted with three or more straight chain lower alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl and adamantyl; 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 -NH-@-NH-R2 wherein R2 is hydrogen or lower alkyl, are disclosed. These compounds exhibit potent LH-RH agonist properties.
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