Novel semisynthetic macrolide antibiotics of the azalide series

Details Novel semisynthetic macrolide antibiotics of the azalide series Novel semisynthetic macrolide antibiotics of the azalide series

C - Chemistry, Metallurgy

07

H

C07H 17/00 (2006.01) A61K 31/70 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2509599

The invention relates to N"-substituted 9a-N-(N'-carbamoyl-.gamma.- aminopropyl), 9a--N-(N'-thiocarbamoyl-.gamma.-aminopropyl), 9a-N-[N'-((.beta.- cyanoethyl)-N'-carbamoyl-.gamma. -aminopropyl] and 9a-N-[N'-((.beta.- cyanoethyl)-N'-thiocarbamoyl-.gamma.-aminopropyl] derivatives of 9-deoxo-9- dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-dihydro-9a- aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, R1 represents H or (.beta.-cyanoethyl moiety, R2 represents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, .beta.-phenylethyl, ethoxycarbonylmethyl, 1-(1-naphtyl)ethyl, 3,4,5- trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents 0 and S, and their acceptable addition salts thereof with inorganic or organic acids, to the process for preparation of their pharmaceutical compositions as well as the use their compositions in the treatment of bacterial infections.

L'invention concerne des dérivés 9a-N-(N'-carbamoyl-.gamma.-aminopropyle), 9a-N-(N'- -thiocarbamoyl-.gamma.-aminopropyle), 9a-N-[N'-((.beta.-cyanoéthyl)-N'-carbamoyl-.gamma.-aminopropyle] et 9a-N-[N'-(.beta.-cyanoéthyl)-N'-thiocarbamoyl-.gamma.-aminopropyle] N"-substitués de 9-déoxo-9-dihydro-9a-aza-9a-homoérythromycine A, qui constituent de nouveaux antibiotiques semi-synthétiques de la série des azalides, de formule générale (1), dans laquelle R représente H ou une fraction cladinosyle, R?1¿ représente H ou une fraction .beta.-cyanoéthyle, R?2¿ représente un groupe isopropyle, 1-naphtyle, 2-naphtyle, benzyle, 2-(trifluorométhyl)phényle, 3-phénylpropyle, .beta.-phényléthyle, éthoxycarbonylméthyle, 1-(1-naphtyl)éthyle, 3,4,5-triméthoxyphényle et 2,4-dichlorophényle, et X représente O et S. L'invention concerne également les sels d'addition avec des acides inorganiques ou organiques, pharmaceutiquement acceptables, desdits dérivés. L'invention concerne en outre un procédé de préparation de compositions pharmaceutiques ainsi que l'utilisation de ces dernières pour le traitement d'infections bactériennes.

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