Combinations of substituted 1-phenyl-1,5-dihydro-pyrido-...

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A61K 31/475 (2006.01) A61K 31/496 (2006.01) A61K 31/5377 (2006.01) A61K 45/06 (2006.01) A61P 31/12 (2006.01) A61P 31/18 (2006.01)

Patent

CA 2563601

The present invention concerns combinations comprising a compound of formula (I); the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters or metabolites thereof, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(=O), C(=O)OH, C1-4alkyloxyC(=O), C1-4 alkylC(=O), mono- or di(C1- 4alkyl)aminoC(=O), arylaminoC(=O), N-(aryl)-N-(C1-4 alkyl)aminoC(=O), methanimidamidyl,N-hydroxy-methanimidamidyl, mono- or di(C1- 4alkyl)methanimidamidyl, Het1 or Het2; R2 is H, C1-10alkyl, C2-10alkenyl, C3- 7cycloalkyl, wherein said C1-10alkyl, C2-10alkenyl and C3-7 cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy, C1- 4alkyloxy, hydroxyC(=O), aminoC(=O), C1-4alkyloxyC(=O), mono- or di(C1- 4alkyl)aminoC(=O), C1-4alkylC(=O), methanimidamidyl, mono- or di(C1- 4alkyl)methanimidamidyl,N-hydroxy-methanimidamidyl or Het1; and another HIV inhibitor. The invention also concerns products comprising a compound of formula (I) and another HIV inhibitor, as a combined preparation for simultaneous, separate or sequential use in treatment of retroviral infections such as HIV infection, in particular, in the treatment of infections with multi-drug resistant retroviruses.

La présente invention concerne des combinaison comprenant un composé représenté par la formule (I); les oxydes N, sels, stéréo-isomères, mélanges racémiques, promédicaments, esters ou métabolites de ces composées, dans laquelle n vaut 1, 2 ou 3; R¿1? est H, CN, halo, aminoC(=O), C(=O)OH, C¿1-4?alkyloxyC(=O), C¿1-4 ?alkylC(=O), mono- ou di(C¿1-4?alkyl)aminoC(=O), arylaminoC(=O), <i>N</i>-(aryl)-<i>N</i>-(C¿1-4? alkyl)aminoC(=O), méthanimidamidyle, <i>N</i>-hydroxy-méthanimidamidyle, mono- ou di(C¿1-4?alkyl)méthanimidamidyle, Het¿1? ou Het¿2?; R¿2? est H, C¿1-10?alkyle, C¿2-10?alcényle, C¿3-7?cycloalkyle, lesdits C¿1-10?alkyle, C¿2-10?alcényle et C¿3-7? cycloalkyle pouvant être éventuellement substitués; R¿3? est nitro, cyano, amino, halo, hydroxy, C¿1-4?alkyloxy, hydroxyC(=O), aminoC(=O), C¿1-4?alkyloxyC(=O), mono- ou di(C¿1-4?alkyl)aminoC(=O), C¿1-4?alkylC(=O), méthanimidamidyle, mono- ou di(C¿1-4?alkyl)méthanimidamidyle, <i>N</i>-hydroxy-méthanimidamidyle ou Het¿1?; et un autre inhibiteur du VIH. L'invention concerne également des produits contenant le composé de formule (I) et un autre inhibiteur du VIH, en tant que préparaion combinée pour utilisation simultanée, distincte ou séqentielle dans le traitement d'infections à rétrovirus telles que l'infection au VIH, en particulier pour le traitement d'infections à rétrovirus à résistance pléiotrope.

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