Novel mmp-2 derivatives for use as inhibitors of integrin...

Details Novel mmp-2 derivatives for use as inhibitors of integrin... Novel mmp-2 derivatives for use as inhibitors of integrin...

C - Chemistry, Metallurgy

12

N

C12N 9/64 (2006.01) A61K 38/48 (2006.01)

Patent

CA 2421283

The invention relates to novel compounds of the formula (I), which are biologically active as the ligands of integrin .alpha.~V.beta.~3and wherein X represents H, an acyl or a peptide fragment of 1 to 20 amino acids, selected from the list of the naturally occurring amino acids, Y represents a peptide fragment selected from the sequence range 466-660 of human Pro-MMP-2, Z represents OH, NH~2, NHA, NA~2 or a peptide fragment of 1 to 20 amino acids, selected from the list of the naturally occurring amino acids, A represents an alkyl having 1-10 C atoms, and acyl represents an alkanoyl having 1-10 C atoms, wherein the primary amino groups can be also provided with conventional amine protecting groups. The invention further relates to the physiologically acceptable salts and solvates of these novel compounds.

L'invention concerne de nouveaux composés de formule (I), présentant une activité biologique en tant que ligands de l'intégrine alpha v beta 3. Dans la formule, X représente H, acyle ou un fragment de peptide de 1 à 20 acides aminés, sélectionné dans la liste des acides aminés d'origine naturelle ; Y représente un fragment de peptide sélectionné dans la plage de séquences 466-660 de la pro-MMP-2 humaine ; Z représente OH, NH2, NHA, NA2 ou un fragment de peptide de 1 à 20 acides aminés, sélectionné dans la liste des acides aminés d'origine naturelle , A représente alkyle comportant 1-10 atomes de carbone ; et acyl représente alcanoyle comportant 1 à 10 atomes de carbone. Les groupes amino primaires peuvent également être pourvus de groupes protégeant les groupes amino classiques. L'invention concerne enfin des sels et solvates physiologiquement tolérables desdits composés.

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