NOVEL AMORPHOUS 9-DEOXO-9A-AZA-9A-METHYL-9A-HOMOERYTHROMYCIN A, PROCESS FOR PREPARING THE SAME, AND USE THEREOF

Substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A. In addition, this disclosure is directed to a process for the preparation thereof from crude 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A via orthorhombic isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homo...

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Main Authors VINKOVIC MLADEN, BUCAR DEJAN-KRESIMIR, DUMBOVIC ALOJZ, CINCIC DOMINIK, DUMIC MILJENKO, DANILOVSKI ALEKSANDAR, FILIC DARKO, LAZARIC KATICA, LAZAREVSKI GORJANA, ORESIC MARINA, MESTROVIC ERNEST, KNEZEVIC ZDRAVKA
Format Patent
LanguageEnglish
Polish
Published 14.11.2005
Edition7
Subjects
CHEMISTRY
DERIVATIVES THEREOF
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
SUGARS
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Summary:Substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A. In addition, this disclosure is directed to a process for the preparation thereof from crude 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A via orthorhombic isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, of the general formula I: wherein S represents a water-miscible or water-immiscible organic solvent, characterized by the orthorhombic space group P212121, with average unit cell parameters a=8.2 to 9.7 Å, b=11.5 to 13.5 Å, c=44.5 to 47.0 Å, alpha=beta=gamma=90°, wherein a, b and c represent the crystal axes lengths and alpha, beta and gamma represent the angles between the crystal axes. In addition, pharmaceutical compositions containing the substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A are disclosed, as well as a method for the treatment of bacterial and protozoal infections, and inflammation related diseases in humans and animals by administration of a pharmaceutical composition containing same.
Bibliography:Application Number: PL20030374855