Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Franziska E Rohrer

Olaf Grassmann

Regina Moog

Andre Bubendorf

Urs Schwitter

Roland Meier

Thomas Cleary

Jason Yang

Shan-Ming Kuang

Doreen Miller

Alexander Glomme

Emmanuel Pinard

Michelangelo Scalone

Shaoning Wang

Pirmin Hidber

Ralph Diodone

Goesta Rimmler

Stefan Abrecht

Francois Montavon

Michael Hennig

Thomas P Cleary

Armin Ruf

Stephan Goetzoe

Kai Lindenstruth

Annette Deynet-Vucenovic

André Bubendorf

Andre Gerard Bubendorf

André Gerard Bubendorf

The present invention relates to mono-sulfate and hemi-sulfate salts of 2-Chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine, to crystalline and amorphous forms thereof and to their use in pharmaceutical formulations.

Solid forms of 2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine

The present invention relates to the mono-sulfate salt, crystalline forms A and B of the mono-sulfate salt, an amorphous form of the mono-sulfate salt, hemi-sulfate salts, and a crystalline form A of the hemi-sulfate salt of the compound 2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine.

Solid forms of 2-Chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine

The present invention relates to four distinct crystalline forms and to an amorphous form of [4-(3-Fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone, and to their use in the preparation of pharmaceutical compositions. The compounds of present invention are suitable for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.

Solid forms of [4-(3-fluoro-5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone

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

The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. The [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride is an inhibitor of tyrosine kinase enzymes, and are useful in the treatment of cancer. Also disclosed are methods of making and using the novel polymorph, as well as pharmaceutical compositions containing the novel polymorph.

[6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride polymorph

Growing community of inventors

Riehen, Switzerland

Franziska E Rohrer