Nucleotide phosphoramidates as anticancer agents

C - Chemistry – Metallurgy – 07 – H

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C07H 19/10 (2006.01) A61K 31/7068 (2006.01) A61K 31/7072 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2518115

Phosphoramidate derivatives of nucleotides and their use in the treatment of cancer are described. The base moieties of, for example, each of deoxyuridine, cytarabine, gemcitabine and citidine may be substituted at the 5-position. The phosphoramidate moiety has attached to the P atom an aryl-O moiety and an .alpha.-amino acid moiety. The .alpha.-amino acid moiety may correspond to or be derived from either a naturally occurring or a non-naturally occurring amino acid.

L'invention concerne des dérivés de phosphoramidate de nucléotides, ainsi que leur utilisation dans le traitement du cancer. Les fractions de base de désoxyuridine, de cytarabine, de gemcitabine et de cytidine, par exemple, peuvent être substituées en position 5. La fraction de phosphoramidate comporte une fraction aryl-O et une fraction .alpha.-acide aminé fixées sur l'atome P. La fraction .alpha.-acide aminé peut correspondre à un acide aminé d'origine naturelle ou à un acide aminé d'origine non naturelle, ou être issue de celui-ci.

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