Abstract: The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given.
Type:
Grant
Filed:
November 12, 2008
Date of Patent:
February 8, 2011
Assignee:
Cumbre IP Ventures, L.P.
Inventors:
Charles Z. Ding, Yafei Jin, Keith Combrink, In Ho Kim
Abstract: Substituted rifamycin derivatives in which a nitroimidazole, nitrothiazole or nitrofuran pharmacophore is covalently bonded to a rifamycin, methods of using the rifamycin derivatives, and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.
Type:
Grant
Filed:
July 12, 2007
Date of Patent:
March 16, 2010
Assignee:
Cumbre IP Ventures, L.P.
Inventors:
Charles Z. Ding, In Ho Kim, Jiancheng Wang, Zhenkun Ma, Yafei Jin, Keith D. Combrink, Genliang Lu, A. Simon Lynch