首页> 外国专利> Polymorphous variety of 2-(R)-{1-(R) -3,5-bis(trifluoromethyl) -phenylethoxy}-3-(S)-(4-fluoro)phenyl-4-3-(5-oxo-1H,4H-1,2,4-triazole)methyl morpholine an antagonist of tachykinin

Polymorphous variety of 2-(R)-{1-(R) -3,5-bis(trifluoromethyl) -phenylethoxy}-3-(S)-(4-fluoro)phenyl-4-3-(5-oxo-1H,4H-1,2,4-triazole)methyl morpholine an antagonist of tachykinin

机译: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-oxo-1H,4H-1,2,4-三唑)甲基]吗啉是速激肽的拮抗剂

摘要

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.
机译:本发明涉及化合物2-(R)-(1-(R)-(3,5-双(三氟甲基)-苯基)-乙氧基)-3-(S)-(4-的多晶型物。氟)苯基-4-(3-5(-oxo-1H,4H-1,2,4-三唑并)甲基吗啉,它是速激肽受体拮抗剂,可用于治疗或预防中枢神经系统疾病,炎性疾病,疼痛或偏头痛,哮喘和呕吐的即时多态性形式比2-(R)-(1-(R)-(3,5-双(三氟甲基)-苯基)乙氧基)-3的其他已知形式具有优势-(S)-(4-氟)苯基-4-(3-5(-oxo-1H,4H-1,2,4-三唑并)甲基吗啉在热力学稳定性和适用于药物制剂的方面。

著录项

  • 公开/公告号PL191496B1

    专利类型

  • 公开/公告日2006-05-31

    原文格式PDF

  • 申请/专利权人 MERCK & CO. INC.;

    申请/专利号PL19980337579

  • 发明设计人 CROCKER LOUIS;MCCAULEY JAMES;

    申请日1998-07-01

  • 分类号A61P25/04;C07D413/06;A61K31/5377;A61P1/08;A61P11/06;A61P25;A61P29;A61P43;

  • 国家 PL

  • 入库时间 2022-08-21 21:37:58

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