C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
260/57, 260/9
C07J 31/00 (2006.01) C07J 13/00 (2006.01) C07J 33/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01) C07J 51/00 (2006.01)
Patent
CA 1100941
ABSTRACT OF THE DISCLOSURE Processes are provided herein for preparing a new series of fusidic acid derivatives and pharmaceutically acceptable salts and easily hydrolyzable pharmaceutically acceptable esters thereof. The new fusidic acid derivatives have the general formula: Image I in which the dotted line between C-24 and C-25 indicates that the carbon atoms in question are connected by either a double bond or a single bond; Q1 represents oxygen or one of the groupings Image or Image , in which Z is a hydroxy group, a halogen atom, an alkylsulfonyloxy or arylsulfony- loxy group, e.g., methanesulfonyloxy or p-toluenesulfonyloxy, an azido or a nitro group; Q2 is oxygen or the grouping Image ; and R1 stands for a straight or branched alkyl radical having from 1 to 6 carbon atoms, e.g., methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl or the known isomers of pentyl and hexyl, a phenyl or a heterocyclyl radical having 5 or 6 ring atoms and containing nitrogen, oxygen and/or sulfur atoms, these radicals being optionally substituted with halogen, nitro, lower alkyl or lower alkoxy radicals. These new compounds show interes- ting antimicrobial and pharmacokinetic properties both in vitro and in vivo.
281930
Daehne Welf von
Rasmussen Poul R.
Leo Pharmaceutical Products Ltd. A/s (lovens Kemiske Fabrik Prod
Marcus & Associates
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