C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 413/06 (2006.01) A61K 31/535 (2006.01) A61K 31/5377 (2006.01) C07D 265/32 (2006.01)
Patent
CA 2293836
This invention is concerned with a novel polymorphic form of the compound 2- (R)-(1-(R) -(3,5-bis(trifluoromethyl) -phenyl)-ethoxy)-3-(S)-(4-fluoro) phenyl-4-(3-5 (-oxo-1H,4H-1,2,4-triazolo) methylmorpholine 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 form has advantages over the other known forms of 2-(R)-(1-(R) -(3,5-bis(trifluoromethyl) -phenyl)ethoxy)-3-(S )-(4-fluoro) phenyl-4-(3-5 (-oxo-1H,4H-1,2,4-triazolo) methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
L'invention concerne une nouvelle forme polymorphe du composé 2-(R)-(1-(R) -(3,5-bis(trifluorométhyl) phényl)éthoxy)-3-(s)-(4-fluoro) phényl-4-(3-5 (-oxo-1h,4h-1,2,4,-triazolo) méthylmorpholine, qui est un antagoniste de récepteur de tachykinine utilisé dans le traitement ou la prévention des troubles du système nerveux central, des maladies inflammatoires, des douleurs ou des migraines, de l'asthme et du vomissement. La forme polymorphe proposée se distingue avantageusement des formes connues de 2-(R)-(1-(R) -(3,5-bis(trifluorométhyl) phényl)éthoxy)-3-(s)-(4-fluoro) phényl-4-(3-5 (-oxo-1h,4h-1,2,4,-triazolo) méthylmorpholine en termes de stabilité thermodynamique et d'acceptation dans des préparations pharmaceutiques.
Crocker Louis
Mccauley James
Merck & Co. Inc.
Merck Sharp & Dohme Corp.
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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