Rifamycin analogs and uses thereof

Details Rifamycin analogs and uses thereof Rifamycin analogs and uses thereof

C - Chemistry, Metallurgy

07

D

C07D 498/14 (2006.01) A61K 31/498 (2006.01) A61K 31/5383 (2006.01) A61K 31/542 (2006.01) A61P 31/04 (2006.01) A61P 31/10 (2006.01) C07D 491/14 (2006.01)

Patent

CA 2549001

The present invention features rifamycin analogs that can be used as therapeutics for treatics or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3~- hydrxyl analogs, and/or various fused ring systems with the benzene ring at the 4~, 5~ or 5~, 6~ positions.

L'invention concerne des analogues de la rifamycine utilisables comme agents thérapeutiques pour le traitement ou la prévention de diverses infections microbiennes. Selon un mode de réalisation de l'invention, les analogues sont acétylés au niveau de la position 25, comme l'est la rifamycine. Selon un autre mode de réalisation de l'invention, les analogues sont désacétylés au niveau de la position 25. Selon encore d'autres modes de réalisation de l'invention, des analogues de la benzoxazinorifamycine, de la benzthiazinorifamycine et de la benzdiazinorifamycine sont soumis à une dérivatisation à diverses positions du noyau benzène, notamment des analogues 3'-hydroxyle et/ou divers systèmes à cycles accolés ayant le noyau benzène aux positions 4',5' ou 5',6'.

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