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 2550729

The present invention features rifamycin analogs that can be used as therapeutics for treating 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~- hydroxy analogs, 4~-and/or 6~ halo and/or alkoxy analogs, and various 5~ substituents that incorporate a cyclic amine moiety.

L'invention concerne des analogues de rifamycine que l'on peut utiliser comme agents thérapeutiques dans le traitement ou la prévention de diverses infections microbiennes. Dans une forme, les analogues sont acétylés en position 25, comme la rifamycine. Dans une autre forme, ils sont déacétylés en position 25. Dans d'autres formes encore, des analogues de benzoxazinorifamycine, benzthiazinorifamycine et benzdiazinorifamycine sont dérivés à des positions diverses du cycle benzénique, notamment des analogues 3'-hydroxy, 4'- et/ou 6' halo et/ou alcoxy, et divers 5' substituants comprenant un fragment amine cyclique.

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