Crystalline macrolides and process for their preparation

Details Crystalline macrolides and process for their preparation Crystalline macrolides and process for their preparation

C - Chemistry, Metallurgy

07

D

C07D 498/18 (2006.01)

Patent

CA 2290412

33-Epichloro-33-desoxyascomycin of formula (I) and various tautomeric or solvated forms thereof, in crystalline form, such as Form A and Form B. Their preparation involves appropriately converting amorphous compound of formula (I), or compound of formula (I) in other than Form A, or compound of formula (I) in other than Form B, respectively, from a solution thereof under crystallization-inducing conditions or conditions inducing preferential crystallization of Form A or B, respectively. Such crystals are particularly indicated for use in the preparation of topical galenical forms of the compound for pharmaceutical use, e.g. creams, emulsions and ointments.

L'invention concerne des composés 33-épichloro-33-désoxyascomycine correspondant à la formule (I), ainsi que plusieurs formes tautomères ou solvatées de ceux-ci, sous forme cristalline, comme la forme A et la forme B. Le procédé de préparation de ces composés consiste à convertir de manière appropriée un composé amorphe de la formule (I), ou un composé de la formule (I) sous une autre forme que A, ou un composé de la formule (I) sous une autre forme que B, respectivement à partir d'une solution de ces composés, et dans des conditions induisant une cristallisation ou dans des conditions induisant une cristallisation préférentielle de la forme A ou B. De tels cristaux sont tout à fait indiqués pour la préparation de formes galéniques topiques dudit composé destiné à un usage pharmaceutique, par exemple des crèmes, émulsions et onguents.

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