Patent CS-196304-B2 (CS)
Title: Process for preparing new derivatives of erythromycine
Inventor: MAIER ROLAND
IPC: A61P31/04
Filed: 1976-04-06
Abstract: 1520963 Antibacterial preparations of erythromycin derivatives DR KARL THOMAE GmbH 6 April 1976 [7 April 1975 14 Feb 1976] 13942/76 Heading A5B [Also in Division C2] Pharmaceutical compositions having antibacterial activity comprise, as active ingredient an erythromycin derivative of the probable general formula A or B: wherein R represents a hydroxy or phenoxy group; a phenylalkoxy group in which the alkylene moiety contains from 1 to 3 carbon atoms; an alkoxy or hydroxyalkoxy group containing from 1 to 4 carbon atoms; an alkoxyalkoxy, dialkylaminoalkoxy or alkoxycarbonylalkoxy group wherein the alkylene moiety contains from 1 to 4 carbon atoms and the alkyl moiety or moieties each contain from 1 to 3 carbon atoms; a mercapto group; a phenylmercapto group optionally substituted by at least one methyl, methoxy, ethoxy, isopropoxy and/or propoxy group; a phenylalkylmercapto group wherein the alkylene moiety contains from 1 to 3 carbon atoms; a straight or branched chain alkylmercapto group containing from 1 to 5 carbon atoms; a cyclohexylmercapto group; a hydroxyalkylmercapto or cyanoalkylmercapto group wherein the alkylene moiety contains from 1 to 3 carbon atoms; a dialkylaminoalkylmercapto or alkoxycarbonylalkylmercapto group wherein the alkylene and the or both alkyl moieties each contain from 1 to 3 carbon atoms; an amino group of formula: -N(R 2 )R 3  (in which either R 2  and R 3 , which may be the same or different, each represents a hydrogen atom, phenyl group, phenylalkyl group wherein the alkylene moiety contains from 1 to 3 carbon atoms or alkyl group containing from 1 to 4 carbon atoms, or R 2  and R 3 , together with the nitrogen atom to which they are attached represent a 5- or 6-membered monoheterocyclic ring optionally interrupted by an oxygen, sulphur or further nitrogen atom); an acyloxy group of formula R 4 COO- (in which R 4  represents a straight or branched chain alkyl group containing from 1 to 5 carbon atoms, a benzyl or a phenyl group); an amido group of formula -NH-CO-R 5  (in which R 5  represents a straight or branched chain alkyl group containing from 1 to 5 carbon atoms optionally substituted by one or two halogen atoms or by a cyano group; a phenylalkyl group wherein the phenyl moiety is optionally substituted by one or two halogen atoms or by from one to three methoxy groups and the alkylene moiety contains from 1 to 3 carbon atoms and is optionally substituted by a halogen atom; a phenoxyalkyl group wherein the alkylene moiety contains from 1 to 3 carbon atoms; a phenylalkenyl group wherein the alkenylene moiety contains from 2 to 4 carbon atoms; a phenyl group optionally substituted by one or more methyl, hydroxy, methoxy or nitro groups or chlorine atoms; or a pyridyl, furyl, thienyl or fluorofuryl group); a phenylaminocarbonyl group; an aminocarbonylmethoxy group of formula R 6 R 7 NCOCH 2 O- (in which R 6  and R 7 , which may be the same or different, each represents a methyl, ethyl, propyl or isopropyl group); a dialkylphosphono group of formula R 8 OP(=O)(OR 8 ')- in which R 8  and R 8 ', which may be the same or different, each represents a straight or branched chain alkyl group containing from 1 to 5 carbon atoms); a sulfonamido group of formula -NH-SO 2 -R 9  (in which R 9  represents an alkyl group containing. from 1 to 4 carbon atoms or a phenyl group optionally substituted by an alkyl group containing from 1 to 3 carbon atoms); or a sulfonyl group of formula -SO 2 -R 10  (in which P 10  represents an alkyl group containing from 1 to 3 carbon atoms or a phenyl group optionally substituted by an alkyl group containing from 1 to 3 carbon atoms); or a physiologically compatible acid addition salt thereof, in association with a pharmaceutical carrier or excipient. They may be administered in the form of tablets, coated tablets, suppositories, suspensions or solutions. An example is given in which papaverine is an additional active ingredient.