N-terminal site selective inhibitors of human angiotensin...

Details N-terminal site selective inhibitors of human angiotensin... N-terminal site selective inhibitors of human angiotensin...

C - Chemistry, Metallurgy

07

F

C07F 9/30 (2006.01) A61K 31/66 (2006.01) C07F 9/572 (2006.01)

Patent

CA 2335918

The invention concerns peptide derivatives useful as N-terminal site selective inhibitor of the human angiotensin conversion enzyme. Said derivatives comprise the amino acid sequence of the following formula: -Asp-Phe-?(PO¿2?CH¿2?)-Ala-Xaa'- wherein: ?(PO¿2?CH¿2?) indicates that the peptide bond (CONH) between Phe and Ala has been replaced by the phosphonic bond PO¿2?CH¿2?; and Xaa' represents an amino acid residue. Said derivatives can be used in pharmaceutical compositions, in particular for protecting hematopoietic strain cells of patients subjected to aggressive chemotherapeutic or radiotherapy treatment.

L'invention concerne des dérivés de peptides utilisables comme inhibiteur sélectif du site N-terminal de l'enzyme de conversion de l'angiotensine humaine. Les dérivés comportent la séquence d'acides aminés de formule suivante: -Asp-Phe-(PO2CH2)-Ala-Xaa'- dans laquelle: (PO2CH2) indique que la liaison peptidique (CONH) entre Phe et Ala a été remplacée par la liaison phosphonique PO2CH2; et Xaa' représente un résidu d'acide aminé. Ils peuvent être utilisés dans des compositions pharmaceutiques, notamment pour protéger les cellules souches hématopoïétiques de patients soumis à un traitement chimiothérapeutique ou radiothérapeutique agressif.

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