Rifamycin analogs and uses thereof

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 498/14 (2006.01) A61K 31/395 (2006.01) A61K 31/4353 (2006.01) A61K 31/437 (2006.01) A61K 31/4985 (2006.01) A61K 31/5383 (2006.01) A61K 31/542 (2006.01) C07D 487/14 (2006.01) C07D 498/22 (2006.01) C07D 513/14 (2006.01)

Patent

CA 2536378

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 derivated 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 pouvant être utilisés en tant qu'agents thérapeutiques dans le traitement ou la prévention d'une variété d'infections microbiennes. Dans une forme, les analogues sont acétylés en position 25, comme la rifamycine. Dans une autre forme, les analogues sont déacétylés en position 25. Dans d'autres formes, des analogues de benzoxazinorifamycine, de benzthiazinorifamycine, et de 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 qui comprennent un fragment amine cyclique.

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