Polymorphic form of a tachykinin receptor antagonist

Details Polymorphic form of a tachykinin receptor antagonist Polymorphic form of a tachykinin receptor antagonist

C - Chemistry, Metallurgy

07

D

C07D 413/06 (2006.01) A61K 31/5377 (2006.01) A61P 25/00 (2006.01) C07C 17/12 (2006.01) C07C 45/00 (2006.01)

Patent

CA 2388202

This invention is concerned with a novel polymorphic forms of the compound 2- (R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-4-(5-(dimethyl-amino)methyl- 1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic forms have advantages over the other known forms of 2-(R)-(1-(R)-(3,5- bis(trifluoromethyl)phenyl)ethoxy)-4-(5-(dimethylamino)methyl-1,2,3-triazol-4- yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

La présente invention concerne de nouvelles formes polymorphes du composé 2-(R)-(1-(R)-(3,5-bis(trifluorométhyl)phényl)éthoxy)-4-(5-(diméthyl-amino)méthyl-1,2,3-triazol-4-yl)méthyl-3-(S)-(4-fluorophényl)morpholine hydrochlorure qui est un antagoniste du récepteur de tachykinine utilisé dans le traitement ou la prévention des troubles du système nerveux central, des maladies inflammatoires, de la douleur ou de la migraine, de l'asthme et des vomissements. Ces formes polymorphes présentent des avantages par rapport aux autres formes connues de 2-(R)-(1-(R)-(3,5-bis(trifluorométhyl)phényl)éthoxy)-4-(5-(diméthylamino)méthyl-1,2,3-triazol-4-yl)méthyl-3-(S)-(4-fluorophényl)morpholine hydrochlorure en terme de stabilité thermodynamique et d'aptitude à être contenues dans des formulations pharmaceutiques.

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