Amino acids and peptides having a modified tyrosine residue,...

Details Amino acids and peptides having a modified tyrosine residue,... Amino acids and peptides having a modified tyrosine residue,...

C - Chemistry, Metallurgy

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167/246, 530/5.0

C07K 14/595 (2006.01) C07F 9/38 (2006.01) C07F 9/40 (2006.01) C07K 5/02 (2006.01) C07K 7/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1331499

"Amino acids and peptides having a modified tyrosine residue, their preparation and their application as medicaments." in the name of: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) An invention of : Bernard Pierre ROQUES Isabelle MARSEIGNE Bruno CHARPENTIER ABSTRACT OF DISCLOSURE These compounds are represented by formula (I), in which R1 to R2 = H, C1=C8 alkyl, C3-C1 cycloalkyl, or aromatic; (when R1 = H, R2 can be amine function-protec- ting radical, amino acid residue or peptide fragment; R1 and R2 being capable of forming, with N, a 5-7 component ring); A = carbonyl or methylene; W = hydroxy, phenoxy, C1-C8 alkoxy, phenoxy(C1-C8 alkyl), amino, (C1-C8 alkyl)- amino, di(C1-C8 alkyl)amino, (when A = carbonyl, ~ = amino acid residue or peptide fragment); Y = -OSO2OR3 (II), -OPO(OR3)2 (III), -(CH2)m-SO2OR3 (IV) or -(CH2),-PO(OR3)2 (V) (R3 = H, C1-C3 alkyl; m = 1 to 4); Z = cyclohexane, pyridyl or phenyl; n = 0 to 4; on the condition that when Y = (II) or (III), -A-W is other than a sequence composed of nacural amino acids. They have antipsychotic properties, an effect facilitating the memorization processes, analgesic properties; they are useful as anorexia-producing agents, and they have stimulatory effects on intestinal motility. Image (I)

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