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    • 9. 发明授权
    • Polymorphic form of a tachykinin receptor antagonist
    • 速激肽受体拮抗剂的多形态
    • US06229010B1
    • 2001-05-08
    • US09458168
    • 1999-12-09
    • Louis CrockerJames McCauley
    • Louis CrockerJames McCauley
    • C07D41300
    • C07D413/06
    • 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(trifluoro-methyl)-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.
    • 本发明涉及新化合物2-(R) - (1-(R) - (3,5-双(三氟甲基) - 苯基) - 乙氧基)-3-(S) - (4- 氟代)苯基-4-(3-(5-氧代-1H,4H-1,2,4-三唑并)甲基吗啉,其是用于治疗或预防中枢神经系统疾病,炎症性疾病的速激肽受体拮抗剂, 本发明的多晶型物质具有优于其它已知形式的2-(R) - (1-(R) - (3,5-双(三氟 - 甲基) - 苯基)乙氧基 )-3-(S) - (4-氟)苯基-4-(3-(5-氧代-1H,4H-1,2,4-三唑并)甲基吗啉)在热力学稳定性和药物制剂中的适用性 。