Phospholipid derivatives of nucleosides as antitumoral...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/10 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2468099

The invention relates to medicaments containing phospholipid derivatives preferably of unnatural nucleosides of general formula (I), wherein R1 represents an alkyl chain with 10-14 carbon atoms, R2 represents an alkyl chain with 8-12 carbon atoms, n represents a whole number from 0 to 2, R3 represents a hydroxy group, R4 and R5 represent hydrogen and B is a 5- fluorouracil. Said derivatives are used as antitumoral or antiproliferative active ingredients for the prophylaxis and/or curative, palliative or supportive treatment of tumor diseases or neoplasia such as carcinoma, sarcoma, lymphoma or leukemia, and also as monotherapeutic or monoprophylactic agents in free or fixed combination with other prophylactic or therapeutic modalities.

L'invention concerne des médicaments contenant des dérivés phospholipides de préférence de nucléosides non naturels correspondant à la formule générale (I), dans laquelle R<sb>1</sb> représente une chaîne alkyle comportant 10-14 atomes de carbone ; R<sb>2</sb> représente une chaîne alkyle comportant 8-12 atomes de carbone ; n représente un nombre entier pouvant aller de 0 à 2 ; R<sb>3</sb> représente un groupe hydroxy ; R<sb>4</sb> et R<sb>5</sb> représentent hydrogène et B représente 5-fluoroacil. Ces dérivés sont utilisés comme principes actifs antitumoraux ou antiprolifératifs pour la prophylaxie et/ou le traitement curatif, palliatif ou de soutien de maladies tumorales ou de néoplasies, par exemple, les carcinomes, les sarcomes ou les leucémies, et également comme agents monothérapeutiques ou monoprophylactiques tant en association libre qu'en association fixe avec d'autres modalités de prophylaxie ou de thérapie.

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