Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Stephan Goetzoe

Michelangelo Scalone

Urs Schwitter

Olaf Grassmann

Shaoning Wang

Franziska E Rohrer

Stefan Abrecht

Francois Montavon

Andre Bubendorf

Armin Ruf

Regina Moog

Thomas Ammann

Bernd Thern

Sandra Welz

Klaus-Juergen Wolter

The invention is concerned with (S)-1-{[2-(5-Methyl-2-phenyl-oxazol-4-yl)-ethylamino]-acetyl}-pyrrolidine-2-carbonitrile mesylate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.

Salt and polymorphs of a DPPIV inhibitor

Disclosed is a process for the manufacture of pseudo proline dipeptides of the formula wherein Ris a side chain of an alpha amino acid, Ris an amino protecting group and Rand Rare independently either hydrogen or C-alkyl, and Ris hydrogen or methyl starting from an amino acid derivative of the formula wherein Rand Rare as defined above. Pseudo proline dipeptides can be used as reversible protecting groups for Ser, Thr and Cys and thus are versatile tools in peptide chemistry.

Pseudo proline dipeptides

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Muttenz, Switzerland

Stephan Goetzoe