C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 498/08 (2006.01) A61K 31/4709 (2006.01) A61P 31/04 (2006.01)
Patent
CA 2574301
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 R1 comprises hydrogen or acetyl and a prefered R2 comprises 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.
La présente invention a trait à des dérivés de la rifamycine de formule générale (I),(de formes hydroquinone et de quinone correspondant en C1-C4) dans laquelle: un R1 comporte de préférence hydrogène ou acétyle et un R2 comporte de préférence hydrogène, méthyle ou autres alkyles inférieurs; l'astérisque (*) représente l'atome de carbone portant le centre chiral, et une configuration absolue est attribuée à <I>R</I> ou <I>S</I>; ou leurs sels, hydrates ou prodrogues. L'invention a également trait à des procédés de préparation desdits dérivés de la rifamycine. Les composés présentent des activités antimicrobiennes, comprenant des activités contre des micro-organismes résistants aux médicaments.
Combrink Keith D.
Ding Charles Z.
Harran Susan
He Yong
Jin Yafei
Cumbre Ip Ventures L.p.
Cumbre Pharmaceuticals Inc.
Kirby Eades Gale Baker
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