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    Macrolide synthesis process and solid-state forms
    1.
    发明授权
    Macrolide synthesis process and solid-state forms 有权
    大环内酯合成过程和固态形式

    公开(公告)号：US08263753B2

    公开(公告)日：2012-09-11

    申请号：US12804847

    申请日：2010-07-30

    申请人： Monika Brink ,  Hans P. Niedermann ,  Tanja Schweisel ,  Stephan Veit ,  Kerstin Fleischhauer ,  Ralf Warrass ,  Heinz-Jorg Wennesheimer

    发明人： Monika Brink ,  Hans P. Niedermann ,  Tanja Schweisel ,  Stephan Veit ,  Kerstin Fleischhauer ,  Ralf Warrass ,  Heinz-Jorg Wennesheimer

    IPC分类号： C07H17/08

    CPC分类号： C07H17/08

    摘要： This invention relates to a method 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, inter alia, may be used to make macrolides. This invention also relates to 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.

    摘要翻译： 本发明涉及一种制备大环内酯类的方法，特别涉及制备任选取代的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，方法 使用大环内酯的处理，以及制备中间体的方法，其特别可用于制备大环内酯。 本发明还涉及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， 制造包含（或衍生自）这种结晶形式的药物，使用这种结晶形式的治疗方法，以及包含这种结晶形式的试剂盒。

    Macrolide synthesis process and solid-state forms
    4.
    发明授权
    Macrolide synthesis process and solid-state forms 有权
    大环内酯合成过程和固态形式

    公开(公告)号：US08518900B2

    公开(公告)日：2013-08-27

    申请号：US13359327

    申请日：2012-01-26

    申请人： Ralf Warrass ,  Fritz Blatter ,  Meinrad Brenner ,  Guixan Hu ,  Timo Rager

    发明人： Ralf Warrass ,  Fritz Blatter ,  Meinrad Brenner ,  Guixan Hu ,  Timo Rager

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： 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.

    摘要翻译： 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。

    PROCESS FOR THE ENZYMATIC PRODUCTION OF CYCLIC DIGUANOSINE MONOPHOSPHATE EMPLOYING A DIGUANYLATE CYCLASE COMPRISING A MUTATED RXXD MOTIF
    5.
    发明申请
    PROCESS FOR THE ENZYMATIC PRODUCTION OF CYCLIC DIGUANOSINE MONOPHOSPHATE EMPLOYING A DIGUANYLATE CYCLASE COMPRISING A MUTATED RXXD MOTIF 审中-公开
    使用包含突变的RXXD MOTIF的含葡聚糖环状酶的环糊精单磷酸酯的生产方法

    公开(公告)号：US20110288286A1

    公开(公告)日：2011-11-24

    申请号：US13133458

    申请日：2009-12-07

    申请人： Thomas Simon Ilg ,  Volker Spehr ,  Ralf Warrass

    发明人： Thomas Simon Ilg ,  Volker Spehr ,  Ralf Warrass

    IPC分类号： C07H19/213 ,  C12P19/36 ,  C12N9/12

    CPC分类号： C12P19/36 ,  C07H19/207 ,  C12N9/1241 ,  C12N15/52 ,  Y02P20/55

    摘要： A process is disclosed for the production of cyclic di-guanosine monophosphate (c-di-GMP) without the use of protecting groups by means of an enzymatic synthesis. The process comprises the coupling of two guanosine triphosphate (GTP) molecules so as to form a c-di-GMP molecule. This is done under the influence of a mutant diguanylate cyclase (DGC) comprising the amino acid sequence V153M154G155G156. It has been found that the DGC is obtainable from inclusion bodies, and therewith can be made available in amounts sufficient to improve the c-di-GMP synthesis. Particularly, the latter synthesis can be conducted in a one-pot method starting from commercially available bulk chemicals and allows upscaling to a commercial production scale.

    摘要翻译： 公开了不通过酶合成使用保护基的环状二鸟苷一磷酸（c-di-GMP）的生产方法。 该方法包括两个鸟苷三磷酸（GTP）分子的偶合以形成c-di-GMP分子。 这是在包含氨基酸序列V153M154G155G156的突变体二叉二酸环化酶（DGC）的影响下进行的。 已经发现，DGC可以从包涵体获得，并且因此可以以足以改善c-di-GMP合成的量获得。 特别地，后一种合成可以以一锅法从市售散装化学品开始进行，并允许将其放大到商业生产规模。

    Macrolide synthesis process and solid-state forms
    6.
    发明授权
    Macrolide synthesis process and solid-state forms 有权
    大环内酯合成过程和固态形式

    公开(公告)号：US08461121B2

    公开(公告)日：2013-06-11

    申请号：US13401991

    申请日：2012-02-22

    申请人： Ralf Warrass ,  Fritz Blatter ,  Timo Rager

    发明人： Ralf Warrass ,  Fritz Blatter ,  Timo Rager

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： 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, inter alia, 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.

    摘要翻译： 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 ，以及制备中间体的方法，其特别可用于制备大环内酯。 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。

    Macrolide synthesis process and solid-state forms
    8.
    发明授权
    Macrolide synthesis process and solid-state forms 有权

    公开(公告)号：US08227429B2

    公开(公告)日：2012-07-24

    申请号：US11828404

    申请日：2007-07-26

    申请人： Ralf Warrass ,  Fritz Blatter ,  Meinrad Brenner ,  Guixan Hu ,  Tamo Rager

    发明人： Ralf Warrass ,  Fritz Blatter ,  Meinrad Brenner ,  Guixan Hu ,  Tamo Rager

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： This invention relates to a method 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, inter alia, may be used to make macrolides. This invention also relates to 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.

    MACROLIDE SYNTHESIS PROCESS AND SOLID-STATE FORMS
    9.
    发明申请
    MACROLIDE SYNTHESIS PROCESS AND SOLID-STATE FORMS 有权
    MACROLIDE合成方法和固体形式

    公开(公告)号：US20120122808A1

    公开(公告)日：2012-05-17

    申请号：US13359327

    申请日：2012-01-26

    申请人： Ralf Warrass ,  Fritz Blatter ,  Meinrad Brenner ,  Guixan Hu ,  Timo Rager

    发明人： Ralf Warrass ,  Fritz Blatter ,  Meinrad Brenner ,  Guixan Hu ,  Timo Rager

    IPC分类号： A61K31/706 ,  A61P31/04 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： 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.

    摘要翻译： 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。