Difluoronucleoside phosphonic acids and derivatives thereof

Details Difluoronucleoside phosphonic acids and derivatives thereof Difluoronucleoside phosphonic acids and derivatives thereof

A - Human Necessities

61

K

A61K 31/70 (2006.01) C07H 19/00 (2006.01) C07H 19/10 (2006.01) C07H 19/20 (2006.01)

Patent

CA 2284263

Difluoronucleoside phosphonic acids and derivatives thereof of formula (II) where R is base selected from the group consisting of: (i), (ii), (iii), (iv), and (v) wherein R1 is hydrogen, methyl, bromo, fluoro, chloro or iodo; R2 is hydroxy or -NR4R5, where R4 and R5 are independently selected from the group consisting of hydrogen, methyl, ethyl and propyl; R3 is hydrogen, bromo, chloro or iodo; both R6 are the same, and are either -OR7 or -(O-R8), where R7 is selected from the group consisting of hydrogen, methyl, ethyl, and isopropyl; R8 is a pharmaceutically acceptable cation; and pharmaceutically acceptable salts and solvates thereof; are described and claimed as antiviral and antineoplastic agents.

L'invention concerne des acides difluoronucléosides-phosphoniques et leurs dérivés, de formule (II), dans laquelle R est une base choisie dans le groupe constitué de (i), (ii), (iii), (iv) et (v). Dans ces formules, R?1¿ est hydrogène, méthyle, bromo, fluoro, chloro ou iodo; R?2¿ est hydroxy ou -NR?4¿R?5¿, dans laquelle R?4¿ et R?5¿ sont choisis indépendamment dans un groupe comprenant hydrogène, méthyle, éthyle et propyle; R?3¿ est hydrogène, bromo, chloro ou iodo; les deux R?6¿ sont identiques et sont soit -OR?7¿, soit -(O?-¿R?8¿), R?7¿ choisi dans le groupe constitué d'hydrogène, méthyle, éthyle et isopropyle; R?8¿ est un cation pharmaceutiquement acceptable. La présente invention concerne également des sels et des solvates pharmaceutiquement acceptables de ces acides. Lesdits acides, sels et solvates sont utilisés, conformément à l'invention, comme agents antiviraux et antinéoplasiques.

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