Bristol-myers Squibb Compnay

Bristol Meyers Squibb Company

Bristol-myers Squibb Holdings Ireland

Martha Davidovich

Jack Z Gougoutas

John D DiMarco

Soojin Kim

Michael A Galella

Mary F Malley

Sushil K Srivastava

Timothy M Malloy

Denis Favreau

Zhenrong Guo

Bruce T Lotz

Imre M Vitez

William L Parker

Krishnaswamy Srinivas Raghavan

Ann W Newman

Sunanda A Ranadive

Michael Galella

A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

Process for preparing atazanavir bisulfate and novel forms

There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.

Polymorphs of an epothilone analog

There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formulaAlso provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.

Gatifloxacin pentahydrate

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East Brunswick, NJ, United States of America

Martha Davidovich