Diketoacid-derivatives as inhibitors of polymerases

C - Chemistry – Metallurgy – 07 – C

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C07C 59/76 (2006.01) A61K 31/19 (2006.01) A61K 31/335 (2006.01) A61K 31/38 (2006.01) A61K 31/40 (2006.01) A61K 31/42 (2006.01) A61K 31/445 (2006.01) C07C 59/90 (2006.01) C07D 207/30 (2006.01) C07D 207/337 (2006.01) C07D 211/34 (2006.01) C07D 211/96 (2006.01) C07D 213/30 (2006.01) C07D 213/89 (2006.01) C07D 249/18 (2006.01) C07D 249/20 (2006.01) C07D 261/12 (2006.01) C07D 307/34 (2006.01) C07D 307/80 (2006.01) C07D 333/04 (2006.01) C07D 333/28 (2006.01) C07D 333/34 (2006.01) C07D 333/36 (2006.01) C07D 333/38

Patent

CA 2338490

Diketoacids of Formula (A) are useful as inhibitors of viral polymerases. In particular hepatitis C virus RNA dependent RNA polymerase (HCV RdRp), hepatitis B virus polymerase (HBV pol) and reverse transcriptase of human immunodeficiency virus (HIV RT). The group R may be broadly chosen and is an organic moiety which contains 2 to 24 carbon atoms and includes an optionally cyclic or heterocyclic group in which the atom directly bonded to the adjacent carbonyl in the diketoacid is part of the ring structure.

Selon cette invention, les dicétoacides correspondant à la formule (A) sont utilisés comme inhibiteurs de polymérases, notamment de la polymérase ARN dépendante de l'ARN du virus de l'hépatite C (HCV RdRp), de la polymérase du virus de l'hépatite B (HBV pol) et de la transcriptase inverse du virus de l'immunodéficience humaine (VIH RT). Dans cette formule, le groupe R peut être librement choisi et se présente comme une fonctionnalité organique qui contient entre 2 et 24 atomes de carbone et comprend un éventuel groupe cyclique ou hétérocyclique dans lequel l'atome directement attaché au carbonyle adjacent dans le dicétoacide fait partie de la structure cyclique.

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