Polyfunctional fullerene c60 amino acid derivatives

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/062 (2006.01) A61K 31/401 (2006.01) A61K 31/4015 (2006.01) A61K 35/02 (2006.01) A61K 38/05 (2006.01) A61P 9/12 (2006.01) C07D 207/16 (2006.01) C07D 207/448 (2006.01)

Patent

CA 2687557

The invention relates to novel polyfunctional fullerene C60 aminoacid derivatives of formula (1), wherein R=H, mono- or dihydroxyalkyl, aminoalkyl, haloidalkyl, mono- or dinitroxyalkyl or maleinimide mm; N-Z are the .alpha.,.beta.,.gamma., .omega.-aminoacid of general formula NH-CmH2 m-COOM or (II) -N- COOM, wherein m=2-5 and M is a nitroxyalkyl group, an alkyl group or an alkali metal salt, or a biologically active dipeptide, to methods for the production thereof and to a method for binding fullerene derivatives with SH-containing proteins. The invention also relates to the use of nitroxyalkyl-(fullerenyl)aminoacids as nitrogen monoxide donors and to the use of said nitroxyalkyl-(fullerenyl)aminoacids in the form of quick-acting vasodilatators for antihypertensive therapy. A method for inhibiting a metastasis process and a method for enhancing antileukemik activity of cyclophosphamide are also disclosed.

L'invention concerne de nouveaux dérivés d'acides aminés polyfonctionnels du fullerène C(60) ayant la formule (I) dans laquelle R=H, mono- ou dihydroxyalkyle, aminoalkyle, haloïdalkyle, mon o- ou dinitroxyalkyle ou maleinimide; N-Z est un fragment d'acide aminé .alpha.,.beta.,.gamma., .omega. possédant la formule NH-CmH2m-COOM ou (II) -N- COOM, dans laquelle m=2-5, et M est un groupe nitroxyalkyle, groupe alkyle ou sel de métal alcalin, ou dipeptide possédant une activité biologique élevée, ainsi que des procédés de fabrication et un procédé de liaison par covalence des dérivés de fullerène avec des protéinescontenant SH. En outre, l'invention concerne l'utilisation d'acides aminés nitroxyalkyle-N-(fullerényl) en tant que donneurs de monoxyde d'azote et l'utilisation d'acides aminés nitroxyalkyle-N-(fullerényl) en tant qu'agents vas

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