C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
260/57, 260/9
C07J 13/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01)
Patent
CA 1064906
ABSTRACT OF THE DISCLOSURE A new series of fusidic acid derivatives, salts and easily hydrolyzable esters thereof, and processes for the preparation of these compounds are provided herein. The new compounds have the general formula Image in which the C24-25 bond is a single or a double bond, and in which Q1 and Q2 stand for Image or oxygen; A stands for oxygen, sulphur or a sulfinyl radical; R1 stands for a straight or branched alkyl radical having from 1 to 8 carbon atoms, or such straight or branched alkyl radical having from 1 to 8 carbon atoms when substituted by halogen atoms of hydroxy, alkyloxy, aralkyloxy, aryloxy, alkanoyloxy, aralkanoyl- oxy, aroyloxy, sulfhydryl, alkylthio, aralkylthio, arylthio, alkanoyl- thio, aroylthio, azido, nitro, cyano, thiocyano, hydroxycarbonyl, alkyl- oxycarbonyl, amino, alkylamino, dialkylamino, arylamino, ??anoylamino or aroylamino groups; an alkenyl or alkynyl radical having from 7 to 6 carbon atoms, a cycloalkyl radical having from 3 to 7 carbon atoms in the alicyclic ring, an aryl, aralkyl or heterocyclylalkyl radical, or such alkenyl or alkynyl radical having from 2 to 6 carbon atoms, such cyclo- alkyl radical having from 3 to 7 carbon atoms in the alicyclic ring, such aryl, such aralkyl or such heterocyclylalkyl radical when substituted by halogen, nitro, lower alkyl, hydroxy or alkoxy radicals: or a heterocyclic radical having 5 or 6 ring atoms, containing oxygen, sulphur or nitrogen atoms, and selected from 2- or 3-pyrrolyl, 2- or 3-furyl, 2- or 3-furfuryl, 2- or 3-thienyl, 2-, 3- or 4-pyridyl, 2-, 4- or 5-pyrimidinyl, 2- or 3-pyrazolyl, imidazolyl, 1-methyl-2-immdazolyl, triazolyl, 5-methyl-1,2,4-triazol-3-y1, tetrazoyl, 1-methyl-1H- tetrazol-5-yl, thiazolyl, thiadiazolyl and 5-methyl-1,3,4-thiadiazol- 2-yl: and pharmaceutically acceptable salts and easily hydrolyzable esters thereof. These compounds show interesting antimicrobial and pharmotokinetic properties. These compounds can be used in the treat- ment of bacterial infections in humans and animals.
255603
Daehne Welf von
Rasmussen Poul R.
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