Dinucleoside-5',5'-pyrophosphates

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) A61K 31/70 (2006.01)

Patent

CA 2195091

5',5'-Pyrophosphates of non-naturally occurring nucleosides selected from thymine-3'-azido-2',3'-dideoxy-D-riboside, 5-fluorouracil-2'-deoxy-D-riboside, uracil-3'-azido-2',3'-dideoxy-D-riboside, guanine-2',3'-dideoxy-D-riboside, hypoxanthine-2',3'-dideoxy-D-riboside, cytosine-2',3'-dideoxy-D-riboside, and adenine-2',3'-dideoxy-D-riboside, are described as well as their manufacture and use as therapeutical agents against tumors and retroviral infections including HIV infections. The compounds may be administered as the active ingredients of pharmaceutical compositions or as pro-drugs encapsulated into biological carriers, e.g., transformed erythrocytes, for targeting to specific cell population responsible of the development of the pathological disorders.

L'invention concerne des 5',5'-pyrophosphates de nucléosides d'origine non naturelle, sélectionnés parmi le thymine-3'-azido-2',3'-didésoxy-D-riboside, le 5-fluorouracil-2'-désoxy-D-riboside, l'uracil-3'-azido-2',3'-didésoxy-D-riboside, le guanine-2',3'-didésoxy-D-riboside, l'hypoxanthine-2',3'-didésoxy-D-riboside, le cytosine-2',3'-didésoxy-D-riboside et l'adénine-2',3'-didésoxy-D-riboside. L'invention concerne également leur procédé de production et leur utilisation en tant qu'agents thérapeutiques contre les tumeurs et les infections rétrovirales y compris les infections au VIH. Ces composés peuvent être administrés en tant que principe actif de compositions pharmaceutiques ou sous forme de promédicaments encapsulés dans des excipients biologiques, par ex. des érythrocytes transformés, afin de lutter contre des populations de cellules cibles responsables du développement de troubles pathologiques.

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