Solid forms of a chemokine receptor antagonist and methods...

Details Solid forms of a chemokine receptor antagonist and methods... Solid forms of a chemokine receptor antagonist and methods...

C - Chemistry, Metallurgy

07

D

C07D 491/044 (2006.01) A61K 31/194 (2006.01) A61K 31/4545 (2006.01) A61P 29/00 (2006.01) C07C 59/265 (2006.01)

Patent

CA 2590157

The citrate salt of (S)-4-(4-Chloro-phenyl)-1-{3-[7-(1-hydroxy-l-methyl-ethyl)- 11H-10-oxa-1-aza-dibenzo[a,d]cyclohepten-5-ylidene]-propyl}-3,3-dimethyl- piperidin-4-ol, which may be used in pharmaceutical applications, is disclosed. The crystalline Citrate Salt, including particular single crystal forms and combinations of the single crystalline forms, are also discussed. Mixtures for forming the crystalline salts are discussed. As well, methods of producing the Citrate Salt, and crystalline forms thereof, and using such Citrate Salt, and crystalline forms thereof, in treating diseases associated with aberrant leukocyte recruitment, activation, or recruitment and activation are also discussed.

L'invention concerne le sel de citrate de (S)-4-(4-chloro-phényl)-1-{3-[7-(1-hydroxy-l-méthyl-éthyl)-11H-10-oxa-1-aza-dibenzo[a,d]cycloheptène-5-ylidène]-propyl}-3,3-diméthyl-piperidine-4-ol, qui peut être utilisé dans des applications pharmaceutiques, ainsi que le sel de citrate cristallin, y compris, des formes cristallines uniques spécifiques et des combinaisons des formes cristallines uniques. Cette invention a aussi pour objet des mélanges de formation des sels cristallins, ainsi que des méthodes de production du sel de citrate et de ses formes cristallines, et des méthodes d'utilisation dudit sel de citrate et de ses formes cristallines dans le traitement de maladies associées à un recrutement, à une activation de leucocytes aberrants ou à un recrutement et à une activation de leucocytes aberrants.

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