Nonapeptide and decapeptide derivatives of luteinizing...

Details Nonapeptide and decapeptide derivatives of luteinizing... Nonapeptide and decapeptide derivatives of luteinizing...

C - Chemistry, Metallurgy

07

K

530/7.06

C07K 7/23 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1157851

21060 NONAPEPTIDE AND DECAPEPTIDE DERIVATIVES OF LUTEINIZING HORMONE RELEASING HORMONE Abstract of the Disclosure 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-pentafluoro- phenyl)-L-alanyl; X is a D-amino acid residue Image 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, perhydro- naphthyl, 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 Image wherein R2 is hydrogen or lower alkyl, are disclosed. These compounds exhibit potent LH-RH agonist properties.

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