9A-AZALIDES ELICITING ANTI-INFLAMMATORY ACTIVITY Russian patent published in 2008 - IPC C07H17/00 A61K31/7042 A61P29/00 

Abstract RU 2320668 C2

FIELD: organic chemistry, antibiotics.

SUBSTANCE: invention relates to 9A-azalide compounds of the formula (I): wherein R, R1, R2 and R3 have values given in the invention description, to their pharmaceutically acceptable salts and pharmaceutical compositions used in treatment of inflammatory pathologies and comprising these compounds as an active component. Also, invention relates to a method for synthesis of compounds of the formula (I) that involves removal of L-cladinose at position 3 by acid-catalyzed hydrolysis reaction of azithromycin derivatives of the formula (II): wherein R, R1, R2 and R3 have values given in the invention description wherein this reaction is carried out in the presence of inorganic acid and proton organic solvent. Invention provides preparing compounds that possess strong anti-inflammatory activity and remove antibiotic properties.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

14 cl, 40 ex

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RU 2 320 668 C2

Authors

Napoletano Mauro

Mereu Andrea

Moridzhi Ehrmanno

Ornagi Fernando

Moratstsoni Gabriele

Pellachini Franko

Dates

2008-03-27Published

2003-10-28Filed