Peptides exhibiting oxytocin antagonistic activity

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/16 (2006.01) A61K 38/08 (2006.01) A61K 38/11 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2163114

A peptide having formula a) wherein Mpa is 3-mercaptopropionic acid residue (-S CH2 CH2-CO); X is D-trytophan (D Trp) or .beta.-(2-Naphtyl)-D-alanine (D Nal); Ile is isoleucine; Y is alloisolencine (alloIle) or (S)-2-Amino-3-ethyl-pentanoic acid (Ala(.beta.-Et2)); Asn is asparqgine; .alpha.-Abu is .alpha.-aminobutyric acid residue (II) and N.alpha.MeOm is N.alpha.-methyl-ornithine, is disclosed. The peptides may be used as an active ingredient in a medicament, especially in a pharmaceutical composition for therapeutic treatment of excessive uterus muscle contractions.

L'invention concerne un peptide ayant la formule (I) dans laquelle Mpa représente un reste d'acide 3-mercaptopropionique (-S-CH2-CH2-CO-), X représente D-tryptophan (D-Trp) ou beta -(2-Naphtyl)-D-alanine (D-Nal), Ile représente isoleucine, Y représente alloisoleucine (alloIle) ou l'acide (S)-2-Amino-3-éthyl-pentanoïque (Ala( beta -Et2)), Asn représente asparagine, alpha -Abu représente un reste d'acide alpha -aminobutyrique de la formule (II) et N alpha MeOrn représente N alpha -méthyl-ornithine. Les peptides peuvent être utilisés comme ingrédients actifs dans un médicament, notamment dans une composition pharmaceutique destinée au traitement thérapeutique des contractions musculaires excessives de l'utérus.

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