Pliva Hrvatska D.o.o.

Pliva Pharmaceutical Industry, Incorporated

Ernest Mestrovic

Gorjana Lazarevski

Aleksandar Danilovski

Darko Filic

Alojz Dumbovic

Dominik Cincic

Katica Lazaric

Marina Oresic

Miljenko Dumic

Mladen Vinkovic

Knezevic Zdravka

Miljenko Dumić

Zdravka Knezevic

Dejan Kresimir Bucar

Mladen Vinković

Dejan-Kresimir Bucar

Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A having the Formula I: wherein S is an organic solvent which is at least partially miscible with water, x is 1, 1.25, 1.5 or 2, y is 0, 0.5, or 1, the pseudopolymorph being characterized by the monoclinic space group P2and average unit cell parameters comprising: crystal axis lengths of a=15.5-17.0 &#x212b;, b=15.5-17.0 &#x212b;, and c=17.5-19.5 &#x212b;, and angles between the crystal axes of &#x3b1;=&#x3b3;=90&#xb0; and &#x3b2;=106&#xb0;-112&#xb0;. In addition, this disclosure is directed to processes for the preparation of the substantially pure isostructural pseudopolymorphs of Formula I; to pharmaceutical compositions containing substantially pure isostructural pseudopolymorphs of Formula I; and to a method for the treatment of bacterial and protozoan infections, and inflammation-related diseases by administration of a pharmaceutical composition containing the substantially pure isostructural pseudopolymorphs of Formula I.

Isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A

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 P222, with average unit cell parameters a=8.2 to 9.7 &#x212b;, b=11.5 to 13.5 &#x212b;, c=44.5 to 47.0 &#x212b;, &#x3b1;=&#x3b2;=&#x3b3;=90&#xb0;, wherein a, b and c represent the crystal axes lengths and &#x3b1;, &#x3b2; and &#x3b3; 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.

Amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, process for preparing the same, and uses thereof

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Bjelovar, Croatia

Ernest Mestrovic