Nonapeptide and decapeptide derivatives of luteinizing hormone releasing hormone

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United States of America Patent

PATENT NO 4234571
SERIAL NO

06047661

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Abstract

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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 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 ##STR1## 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--R.sup.1, wherein R.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR2## wherein R.sup.2 is hydrogen or lower alkyl, are disclosed. These compounds exhibit potent LH-RH agonist properties.

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Patent Owner(s)

  • G. D. SEARLE & CO.

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Jones, Gordon H Cupertino, CA 25 1617
Nestor, John J San Jose, CA 36 602
Vickery, Brian H Cupertino, CA 30 890

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