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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

    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
    2.
    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。

    MACROLIDE SYNTHESIS PROCESS AND SOLID-STATE FORMS
    3.
    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。

    Process for the synthesis of cyclic carbamates
    7.
    发明授权
    Process for the synthesis of cyclic carbamates 有权
    合成环状氨基甲酸酯的方法

    公开(公告)号：US08957204B2

    公开(公告)日：2015-02-17

    申请号：US13879258

    申请日：2011-10-14

    申请人： Meinrad Brenner ,  Erick M. Carreira ,  Nicka Chinkov ,  Miriam Lorenzi ,  Aleksander Warm ,  Lothar Zimmermann

    发明人： Meinrad Brenner ,  Erick M. Carreira ,  Nicka Chinkov ,  Miriam Lorenzi ,  Aleksander Warm ,  Lothar Zimmermann

    IPC分类号： C07D265/18

    CPC分类号： C07D265/18

    摘要： The invention is directed to a process for the preparation of a cyclic carbamate starting with a chiral propargylic alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction is carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane. Another aspect of the invention is directed to a process for the synthesis of said cyclic carbamate starting described above, wherein also a process for the preparation of the chiral propargylic alcohol is provided.

    摘要翻译： 本发明涉及一种制备环状氨基甲酸酯的方法，其起始于手性炔丙醇和/或其合适的盐，其与选自光气，双光气，三光气及其混合物的环化剂反应， 反应在碱水溶液和水不混溶的有机溶剂的存在下进行，所述有机溶剂主要包含至少一种选自C 2-5 - C 2-8 - C 2-8 - 羧酸烷基酯的化合物和至少一种C2-5-羧酸盐的混合物 - 烷基C2-5-羧酸酯与至少一种C5-8-烷烃。 本发明的另一方面涉及一种合成上述环状氨基甲酸酯的方法，其中还提供了制备手性炔丙醇的方法。

    PROCESS FOR THE SYNTHESIS OF CYCLIC CARBAMATES
    8.
    发明申请
    PROCESS FOR THE SYNTHESIS OF CYCLIC CARBAMATES 有权
    循环碳酸酯合成方法

    公开(公告)号：US20130217875A1

    公开(公告)日：2013-08-22

    申请号：US13879258

    申请日：2011-10-14

    申请人： Meinrad Brenner ,  Erick M. Carreira ,  Nicka Chinkov ,  Miriam Lorenzi ,  Aleksander Warm ,  Lothar Zimmermann

    发明人： Meinrad Brenner ,  Erick M. Carreira ,  Nicka Chinkov ,  Miriam Lorenzi ,  Aleksander Warm ,  Lothar Zimmermann

    IPC分类号： C07D265/18

    CPC分类号： C07D265/18

    摘要： The invention is directed to a process for the preparation of a cyclic carbamate starting with a chiral propargylic alcohol and/or a suitable salt thereof, which is reacted with a cyclisation agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction is carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane. Another aspect of the invention is directed to a process for the synthesis of said cyclic carbamate starting described above, wherein also a process for the preparation of the chiral propargylic alcohol is provided.

    摘要翻译： 本发明涉及一种由手性炔丙醇和/或其合适的盐开始制备环状氨基甲酸酯的方法，其与选自光气，双极光，三光气及其混合物的环化剂反应， 反应在碱水溶液和水不混溶的有机溶剂的存在下进行，所述有机溶剂主要包含至少一种选自C 2-5 - C 2-8 - C 2-8 - 羧酸烷基酯的化合物和至少一种C2-5-羧酸盐的混合物 - 烷基C2-5-羧酸酯与至少一种C5-8-烷烃。 本发明的另一方面涉及一种合成上述环状氨基甲酸酯的方法，其中还提供了制备手性炔丙醇的方法。

    PROCESS FOR THE SYNTHESIS OF CYCLIC CARBAMATES
    9.
    发明申请
    PROCESS FOR THE SYNTHESIS OF CYCLIC CARBAMATES 有权
    循环碳酸酯合成方法

    公开(公告)号：US20130211077A1

    公开(公告)日：2013-08-15

    申请号：US13879221

    申请日：2011-10-14

    申请人： Meinrad Brenner ,  Erick M. Carreira ,  Nicka Chinkov ,  Miriam Lorenzi ,  Aleksander Warm ,  Lothar Zimmermann

    发明人： Meinrad Brenner ,  Erick M. Carreira ,  Nicka Chinkov ,  Miriam Lorenzi ,  Aleksander Warm ,  Lothar Zimmermann

    IPC分类号： C07D265/18

    CPC分类号： C07D265/18

    摘要： The invention is directed to a process for the preparation of a cyclic carbamate starting with o-aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclisation agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane.

    摘要翻译： 本发明涉及一种由邻氨基苄醇和/或其合适的盐开始制备环状氨基甲酸酯的方法，其与选自光气，双极光，三光气及其混合物的环化剂反应， 在碱水溶液和水不混溶的有机溶剂的存在下进行反应，所述有机溶剂主要包含至少一种选自C 2-5烷基C 2-5 - 羧酸盐的化合物和至少一种C2-5-羧酸盐的混合物， 具有至少一个C 5-8烷烃的C2-5-羧酸烷基酯。

    Process for the synthesis of cyclic carbamates
    10.
    发明授权
    Process for the synthesis of cyclic carbamates 有权
    合成环状氨基甲酸酯的方法

    公开(公告)号：US08969550B2

    公开(公告)日：2015-03-03

    申请号：US13879221

    申请日：2011-10-14

    申请人： Meinrad Brenner ,  Erick M. Carreira ,  Nicka Chinkov ,  Miriam Lorenzi ,  Aleksander Warm ,  Lothar Zimmermann

    发明人： Meinrad Brenner ,  Erick M. Carreira ,  Nicka Chinkov ,  Miriam Lorenzi ,  Aleksander Warm ,  Lothar Zimmermann

    IPC分类号： C07D265/18

    CPC分类号： C07D265/18

    摘要： The invention is directed to a process for the preparation of a cyclic carbamate starting with o-aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane.

    摘要翻译： 本发明涉及一种由邻氨基苄醇和/或其合适的盐开始制备环状氨基甲酸酯的方法，其与选自光气，双极光，三光气及其混合物的环化剂反应， 在碱水溶液和水不混溶的有机溶剂的存在下进行反应，所述有机溶剂主要包含至少一种选自C 2-5烷基C 2-5 - 羧酸盐的化合物和至少一种C2-5-羧酸盐的混合物， 具有至少一个C 5-8烷烃的C2-5-羧酸烷基酯。