TH17690B - The polymorphic form of the tachikinin receptor antagonist. - Google Patents

Abstract

DC60 (03/09/41) This invention involves a new polymerization model of the compound. 2- (R) - (1- (R) - (3,5-bis (trifluorometric) - feneel) ethoxi) -3- (S) - (4-F Fluoro) phenyl-4- (3- (5-oxo-1H, 4H- 1,2,4-triazolo) methymorpholine), a receptor antagonist of Taggi kinin useful in Treatment or prevention of CNS disorders, inflammatory disease, pain or unilateral headache, asthma, and vomiting. This polymorphic pattern contains Advantages over 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) methymorpholy N) in terms of thermodynamic stability And suitability for inclusion in the construction Pharmaceutical formulas The invention involved a new polymer form of the compound. 2- (R) - (1- (R) - (3,5-bis (trifluoromethyl) phenyl) ethoxy) -3- (S) - (4- flu Auro) phenyl-4- (3- (5-oxo-1H, 4H- 1,2,4-triazolo) methyl morpholine), a receptor antagonist drug. Kikikinin useful in Treatment or prevention of CNS disorders, inflammatory diseases, pain or unilateral headache, asthma, and vomiting. This polymorphic pattern contains Advantages over 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) methyl morfoli N) in terms of thermodynamic stability And suitability for inclusion in the construction Pharmaceutical formulas, drug patents

Claims (8)

1.Polymeric form of the compound 2- (R) - (1- (R) - (3,5-bis (trifluoromethyl) phenyl) ethoxy) -3- (S) - (4- flu Auro) phenyl-4- (3- (5-oxo-1H, 4H-1,2,4-triazolo) methyl morpholine, which is characterized by a diffraction model. Of X-ray powder With significant reflections of approximately 12.0,15.3,16.6,17.0,17.6,19.4,20.0,21.9,23.6,23.8 and 24.8 (2 tetra) independent of the polymerized form of the compound. 2- (R) - (1- (R) - (3,5-bis (trifluor Romethyl) phenyl) ethoxy) -3- (S) - (4-fluoro) - phenyl-4- (3- (5-oxo-1H, 4H-1,2 , 4-triazolo) methyl morpholine, which was characterized by the X-ray powder diffraction model, with significant reflections at approximately 12.6,16.7,17.1,17.2,18.0. , 20.1,20.6,21.1,22.8,23.9 and 24.8 ํ (2-tetra) 2. Pharmaceutical components It consists of a pharmacologically acceptable carrier and a polymerized form of the compound. 2- (R) - (1- (R) - (3,5-bis (trifluoromethyl) phenyl) ethoxy) -3- (S) - (4- flu Auro) phenyl-4- (3- (5-oxo-1H, 4H-1,2,4-triazolo) methyl morpholine Which was shown to you Characteristics by X-ray powder diffraction model With significant reflections of approximately 12.0,15.3,16.6,17.0,17.6,19.4,20.0,21.9,23.6,23.8 and 24.8 ํ (2 tetra), independent of the polymeric form of the compound. 2- (R) - (1- (R) - (3,5-bis (trifluoromethyl) phi Nyl) ethoxy) -3- (S) - (4-fluoro) phenyl -4- (3- (5-oxo-1H, 4H-1,2,4-triazolo) Methyl morpholine, which was characterized by the X-ray diffraction model. With significant reflections at approximately 12.6,16.7,17.1,17.2,18.0,20.1,20.6,21.1,22.8,23.9 and 24.8 (2-tetr). 3.Use of the polymorphic form of claim 1 for the manufacture of drugs to counteract the effects of P matter at its receptor sites or to block nerokinin-1 receptors. In mammals 4.Use of the polymorphic form of claim 1 for the manufacture of therapeutic or prophylactic drugs in mammals. 5.Use of the polymorphic form of claim No. 1 for the manufacture of drugs for the treatment or prevention of depression in humans. 6. Use of the polymorphic form of claim 1 for the manufacture of drugs for the treatment or prevention of anxiety disorders in humans. 7. Use of the polymorphic form of claim 1 for the manufacture of drugs for the treatment of or the prevention of psychosis in humans. 8.Use of the polymorphic form of claim 1 for the manufacture of drugs for the treatment or prevention of schizophrenia. (schizophrenia) in humans