23-Demycinosyltylosin compounds, pharmaceutical compositions and method of use

Claim 1

A compound of the formula ##STR22## wherein R 1 is hydrogen or an acyl group selected from alkanoyl of 2 to 5 carbon atoms, palmityl, stearyl, lauryl, oleyl, chloroacetyl, benzoyl, adamantanecarbonyl, cyclopropanecarbonyl, cyclohexanecarbonyl, β-cyclohexylpropionyl, phenylacetyl, phenoxyacetyl, mandelyl, 2-thienylacetyl, alkyl-, aryl- and aralkylsulfonyl, substituted aryl- and aralkylsulfonyl, wherein the substituents on the aryl portions are halogen, nitro and alkoxy groups, succinyl, maleyl, fumaryl, malonyl and phthalyl; R 2 is acyl, wherein acyl is as defined in R 1 ; R 3 is hydrogen or acyl, wherein acyl is as defined in R 1 ; or R 2 and R 3 are together a carbonyl group linking the 3"- and 4"-hydroxyl groups; R 4 is hydrogen or acyl, wherein acyl is as defined in R 1 ; R 5 is selected from the group consisting of N-NH-aralkyl, ##STR23## wherein n is 0-2, and Q is selected from the group consisting of ##STR24## wherein R 7 and R 8 are independently selected from the group consisting of (C 1 -C 6 ) alkyl, (C 7 -C 10 ) aralkyl and (C 6 -C 10 ) aryl including X-substituted aryl and aralkyl, wherein X is halogen, trifluoromethyl, (C 1 -C 6 ) alkoxy, or (C 1 -C 6 ) alkylcarbonyl; R 6 is methyl, hydroxymethyl, fluoromethyl, chloromethyl, bromomethyl, iodomethyl, di (C 1 -C 6 ) alkylamino, acyloxymethyl, CHO or a group of the formula CH=R 5 wherein R 5 is as hereinbefore defined; and the pharmaceutically acceptable salts thereof.