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    • 9. 发明授权
    • Macrolide synthesis process and solid-state forms
    • 大环内酯合成过程和固态形式
    • US08518900B2
    • 2013-08-27
    • US13359327
    • 2012-01-26
    • Ralf WarrassFritz BlatterMeinrad BrennerGuixan HuTimo Rager
    • Ralf WarrassFritz BlatterMeinrad BrennerGuixan HuTimo Rager
    • A61K31/70C07H17/08
    • C07H17/08
    • Described are methods for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, among other uses, may be used to make macrolides. Also described are solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.
    • 描述了制备大环内酯类的方法,特别是制备任选取代的20,23-二哌啶基-5-O-碳霉糖基 - 太乐内酯及其衍生物的方法,以及大环内酯类制备药物的用途,使用大环内酯类的治疗方法 以及用于制造中间体的方法,除了其它用途之外,可以使用它们来制备大环内酯类。 还描述了20,23-二哌啶基-5-O-碳霉糖基 - 太乐内酯的溶剂化和非溶剂化结晶形式,以及制备这种结晶形式的方法,包含(或衍生自)这种结晶形式的药物,制备药物的方法 包括(或衍生自)这种结晶形式,使用这种结晶形式的处理方法,以及包含这种结晶形式的试剂盒。