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A host Guest Complex, Process for their preparation, Pharmaceutical composition containing same and Use thereof for producing a medicament

机译:宿主客体,其制备方法,包含该客体的药物组合物及其在制备药物中的用途

摘要

A host Guest Complex, where the host is a Cyclodextrin or a mixture of Cyclodextrins, Cyclodextrin and the Guest is 5 - [4 - [2 - (n-methyl-n - (2-pyridyl) amino) ethoxy] benzyl] tiazolidin - 2.4 - dione (Compound (1)) or one of its pharmaceutically acceptable derivative or its m Ezclas.Process for the preparation of said compound and Pharmaceutical composition containing Said compound and a pharmaceutically acceptable vehicle to him. In addition, the composition may contain one or more of a combination of different Active Agent of this pharmaceutically acceptable vehicle and optionally pharmaceutically acceptable to him.Use of said Compound for preparing medicaments for the prophylaxis and / or treatment of diabetes mellitus, situations associated with Diabetes mellitus and certain complications.Claim 17: a process for the preparation of a host Guest Complex, where the host is a Cyclodextrin or a mixture of Cyclodextrins (hereinafter referred to as "also Henceforth the Cyclodextrin and the guest") is the compound (1) or one of its Pharmaceutically acceptable derivative or one of their mixtures, according to claim 1,The process is characterised in that it comprises: (a) Mixing and the Cyclodextrin Compound (1) and / or one of its pharmaceutically acceptable Derivatives with water and the process continues with the mixture until the formation of the complex is complete; or (b) To Neutralize a solution or dispersion The Cyclodextrin compound and a Derivative of (1), in an aqueous LiquidThe Neutralization is carried out by adding a suitable Neutralization Reagent, so that the host Guest Complex precipitate required; or (c) mixing a solution of compound (1), and / or one of its pharmaceutically acceptable Derivatives, in a First Solvent With a solution of a Cyclodextrin in a Second SolventIn the first and the second Solvent is chosen so that the composition of the host - Guest required precipitate Solvent mixture; or (d) mixing a solution of Cyclodextrin and the compound (1), and / or one of its pharmaceutically acceptable derivative in an aqueous LiquidWith a proper Composition of antisolvent form host Guest required to precipitate out of the Solvent mixture; or (e) Prepare a solution of the composition - Cyclodextrin and guest host mixing Compound (1), and / or one of its pharmaceutically acceptable Derivatives,In an appropriate Solvent and then separating the Solvent; or (f) generate a Cyclodextrin and a dispersion of the compound (1), and / or one of its pharmaceutically acceptable Derivatives, in a liquid and Stir until the formation of the complex is complete; and after this as To isolate the composition host - Guest required, for example by Filtration.
机译:宿主客体复合物,其中主体是环糊精或环糊精,环糊精的混合物,并且客体是5-[4- [2--(n-甲基-n-(2-吡啶基)氨基)乙氧基]苄基]噻唑烷- 2.4-二酮(化合物(1))或其药学上可接受的衍生物之一或其化合物。制备所述化合物的方法和含有所述化合物和对其的药学上可接受的载体的药物组合物。另外,该组合物可以包含该药学上可接受的媒介物和他任选地药学上可接受的媒介物的不同活性剂的组合中的一种或多种。所述化合物在制备用于预防和/或治疗糖尿病的药物中的用途,权利要求17:一种制备宿主客体的方法,其中宿主是环糊精或环糊精的混合物(下文中也称为“环糊精和客体”)。 2.根据权利要求1的化合物(1)或其药学上可接受的衍生物之一或其混合物之一,该方法的特征在于它包括:(a)与环糊精化合物(1)和/或其混合物之一混合用水可药用的衍生物,并且该过程继续进行直到混合物形成完全为止。 (b)在水溶液中中和溶液或分散体环糊精化合物和(1)的衍生物。通过加入合适的中和试剂进行中和,从而需要主体客体复合物沉淀;或或(c)在第一溶剂中将化合物(1)和/或其一种药学上可接受的衍生物的溶液与环糊精在第二溶剂中的溶液混合在第一和第二溶剂中选择这样的组合物主体-宾客所需的沉淀溶剂混合物; (d)将环糊精与化合物(1)和/或其一种药学上可接受的衍生物的溶液在水性液体中与需要从溶剂混合物中沉淀出来的合适的抗溶剂形式的主体客体混合;或(e)在适当的溶剂中制备混合化合物(1)和/或其一种药学上可接受的衍生物的组合物-环糊精和客体宿主的溶液,然后分离溶剂;或(f)在液体和搅拌下产生环糊精和化合物(1)和/或其一种药学上可接受的衍生物的分散体,直到络合物完全形成为止;或然后作为隔离合成主机-要求客户,例如通过过滤。

著录项

  • 公开/公告号AR040052A1

    专利类型

  • 公开/公告日2005-03-09

    原文格式PDF

  • 申请/专利权人 GLAXO GROUP LIMITED;

    申请/专利号AR2003P101817

  • 发明设计人

    申请日2003-05-23

  • 分类号C07D417/04;C07H3/06;C08B30/18;A61K31/724;A61K47/48;C07D417/04;C07D213/16;C07D277/34;

  • 国家 AR

  • 入库时间 2022-08-21 22:18:51

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