Merck + Co., Inc.

Robert M Wenslow, Jr

Michael D Ward

John M Williams

Raymond Cvetovich

Louis S Crocker

Daniel Richard Sidler

Ronald B Jobson

Karel M J Brands

Amar J Mahajan

Russell R Ferlita

Karl Hansen

Alex Minhua Chen

Elizabeth S Fisher

Ivan Lee

Vicky K Vydra

Charles Orella

Stephen Howard Cypes

The dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The invention also relates to a crystalline monohydrate of the dihydrogenphosphate salt as well as a process for its preparation, pharmaceutical compositions containing this novel form and methods of use for the treatment of diabetes, obesity, and high blood pressure.

Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor

A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than &#x2212;5&#xb0; C., c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a Calcohol at between &#x2212;5 and &#x2212;25&#xb0; C.

Crystalline forms of carbapenem antibiotics and methods of preparation

Growing community of inventors

East Windsor, NJ, United States of America

Robert M Wenslow, Jr