Synergistic combinations of zidovudine, 1592u89 and 3tc or ftc

Details Synergistic combinations of zidovudine, 1592u89 and 3tc or ftc Synergistic combinations of zidovudine, 1592u89 and 3tc or ftc

A - Human Necessities

61

K

A61K 31/70 (2006.01) A61K 31/165 (2006.01) A61K 31/33 (2006.01) A61K 31/39 (2006.01) A61K 31/44 (2006.01) A61K 31/505 (2006.01) A61K 31/513 (2006.01) A61K 31/52 (2006.01) A61K 31/55 (2006.01) A61K 31/706 (2006.01) A61K 31/7072 (2006.01) A61K 31/7076 (2006.01) A61P 31/12 (2006.01) A61P 31/18 (2006.01) C07D 411/04 (2006.01) C07D 473/16 (2006.01) C07H 19/073 (2006.01)

Patent

CA 2216634

The present invention relates to therapeutic combinations of (1S,4R)-cis-4-[2- amino-6-(cyclopropylamino)-9H-purin-9-yl]-2- cyclopentene-1-methanol (1592U89), 3'-azido-3'-deoxythymidine (zidovudine) and (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan- 5-yl)-(1H)-pyrimidin-2-one (3TC) (or, alternatively to 3TC, (2R,cis)-4-amino-5- fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)- pyrimidin-2-one (FTC)) which have anti-HIV activity. The present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HIV infections including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors.

L'invention concerne des combinaisons thérapeutiques de (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-méthanol (1592U89), de 3'-azido-3'-désoxythymidine (zidovudine) et de (2R,cis)-4-amino-5-fluoro-1-(2-hydroxyméthyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (3TC) (ou à la place de 3TC, la (2R,cis)-4-amino-5-fluoro-1-(2-hydroxyméthyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (FTC). Ces combinaisons ont une activité anti-VIH. L'invention concerne également des compositions pharmaceutiques contenant ces combinaisons et leur utilisation pour le traitement d'infections causées par VIH et en particulier celles causées par les VIH mutants qui sont résistants aux inhibiteurs nucléosidiques et/ou non nucléosidiques.

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