(R/S) rifamycin derivatives, their preparations and...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C540S458000, C548S138000, C548S208000

Reexamination Certificate

active

11186425

ABSTRACT:
Rifamycin derivatives having the following structure of general formula I (both hydroquinone and corresponding quinone (C1-C4) forms):or its salts, hydrates or prodrugs thereof; wherein a preferred R1comprises hydrogen or acetyl and a prefered R2comprises hydrogen, methyl or other lower alkyls; wherein asterik (*) denotes the carbon bearing the chiral center, wherein absolute configuration is assigned as R or S. Methods of preparation of the aforementioned rifamycin derivatives are also described. The compounds exhibit antimicrobial activities, including activities against drug-resistant microorganisms.

REFERENCES:
patent: WO 94/28002 (1994-12-01), None
patent: WO 03/045319 (2003-06-01), None
patent: WO 2005/070940 (2005-08-01), None
patent: WO 2005/070941 (2005-08-01), None
Brufani M, Cerrini S, Fedeli W, Vaciago A. Rifamycins: an insight into biological activity based on structural investigations. J Mol Biol. Aug. 15, 1974;87(3):409-35.
Farr, BM. Rifamycins, in Principles and Practice of Infectious Diseases. Mandell GL, Bennett JE, Dolin R, Eds. Churchhill Livingstone Philadelphia pp. 348-361.
Li Q, Mitscher LA, Shen LL. The 2-pyridone antibacterial agents: bacterial topoisomerase inhibitors. Med Res Rev. Jul. 2000;20(4):231-93.
PCT Notification of Transmittal of the International Search Report and the Written Opinion of the International Searching Authority, or the Declaration. Dec. 12, 2005.

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