Polymorphs of a mglur5 receptor antagonist

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/06 (2006.01) A61K 31/4439 (2006.01) A61P 25/00 (2006.01)

Patent

CA 2673444

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. Present compounds are active on the mGluR5 receptor for the treatment of diseases, related to this receptor, such acute and/or chronic neurological disorders, in particular anxiety, or for the treatment of chronic and acute pain, protection against liver damage, failure whether drug or disease induced, urinary incontinence, obesity, Fragile-X or Autism.

La présente invention concerne des sels de mono-sulfate et d'hémi-sulfate de 2-chloro-4-[1-(4-fluoro-phényl)-2,5-diméthyl-1H-imidazol-4-yléthynyl]-pyridine, des formes cristallines et amorphes de ceux-ci ainsi que leur utilisation dans des préparations pharmaceutiques. Les présents composés sont actifs sur le récepteur mGluR5 pour traiter des maladies associées à ce récepteur, telles que les troubles neurologiques aigus et/ou chroniques, et notamment l'anxiété, ou pour traiter la douleur chronique et aiguë ou offrir une protection contre les atteintes hépatiques, l'insuffisance induite par un médicament ou une maladie, l'incontinence urinaire, l'obésité, le syndrome de l'X fragile ou l'autisme.

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