Rifamycin analogs and uses thereof

Details Rifamycin analogs and uses thereof Rifamycin analogs and uses thereof

A - Human Necessities

61

K

A61K 31/535 (2006.01) C07D 267/22 (2006.01)

Patent

CA 2628403

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, 5 '-halo and/or alkoxy analogs, and various 4 '-and/or 6'- substituents that incorporate a cyclic amine moiety.

La présente invention concerne des analogues de la rifamycine pouvant être utilisés en tant qu~agents thérapeutiques dans le traitement ou la prévention de diverses infections microbiennes. Sous une forme, les analogues sont acétylés en position 25, comme la rifamycine. Sous une autre forme, les analogues sont désacétylés en position 25. Sous encore d~autres formes, des analogues de la benzoxazinorifamycine, de la benzthiazinorifamycine et de la benzdiazinorifamycine sont dérivés à diverses positions du cycle benzénique, notamment des analogues 3'-hydroxy, 5'-halogénés et/ou alcoxy, et divers substituants en 4'- et/ou 6'- lesquels comportent un fragment amine cyclique.

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