Antiviral combinations

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/505 (2006.01) A61K 31/52 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2344172

The present invention relates to therapeutic combinations comprising (2R, cis) -4-amino-1- (2-hydroxymethyl-1, 3-oxathiolan-5-yl) -pyrimidin-2-one (lamivudine) and a second therapeutic agent selected from (9-[(R) -2- (phosphonomethoxy) ethyl]adenine, (PMEA or adefovir) and bis(pivaloyloxymethyl) (9-[(R) -2- (phosphonomethoxy)ethyl]adenine, (the oral prodrug of PMEA, adefovir dipivoxil) w hich have anti-hepatitis B virus (HBV) activity. The present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HBV infections including infections with HBV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors.

L'invention concerne des combinaisons thérapeutiques comprenant une (2R,cis)-4-amino-1-(2-hydroxyméthyl-1,3-oxathiolan-5-yl)-pyrimidin-2-one (lamivudine) ainsi qu'un second agent thérapeutique choisi dans le groupe constitué par (9-[(R)-2-(phosphonométhoxy)éthyl]adénine, (PMEA ou adéfovir) et bis(pivaloyloxyméthyl)(9-[(R)-2-(phosphonométhoxy)éthyl]adénine, (promédicament oral de PMEA ou adéfovir dipivoxil), lesquels possèdent une activité dirigée contre le virus de l'hépatite B (HBV). L'invention concerne également des compositions pharmaceutiques contenant ces combinaisons ainsi que l'utilisation de ces compositions dans le traitement d'infections à HBV, notamment d'infections provoquées par des mutants de ce virus, lesquels sont résistants aux inhibiteurs nucléosidiques et/ou non nucléosidiques.

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