公开(公告)号：US20110053875A1

公开(公告)日：2011-03-03

申请号：US12804847

申请日：2010-07-30

申请人： Fritz Blatter ,  Meinrad Brenner ,  Monika Brink ,  Kerstin Fleischhauer ,  Guixian Hu ,  Hans Peter Niedermann ,  Timo Rager ,  Tanja Schweisel ,  Stephan Veit ,  Ralf Warrass ,  Heinz-Jörg Wennesheimer

发明人： Fritz Blatter ,  Meinrad Brenner ,  Monika Brink ,  Kerstin Fleischhauer ,  Guixian Hu ,  Hans Peter Niedermann ,  Timo Rager ,  Tanja Schweisel ,  Stephan Veit ,  Ralf Warrass ,  Heinz-Jörg Wennesheimer

IPC分类号： A61K31/706 ,  C07H17/08 ,  A61P11/00 ,  A61P31/04

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。

公开(公告)号：US20090042815A1

公开(公告)日：2009-02-12

申请号：US11828404

申请日：2007-07-26

申请人： Fritz Blatter ,  Meinrad Brenner ,  Monika Brink ,  Kerstin Fleischhauer ,  Guixian Hu ,  Hans Peter Niedermann ,  Timo Rager ,  Tanja Schweisel ,  Stephan Veit ,  Ralf Warrass ,  Heinz-Jorg Wennesheimer

发明人： Fritz Blatter ,  Meinrad Brenner ,  Monika Brink ,  Kerstin Fleischhauer ,  Guixian Hu ,  Hans Peter Niedermann ,  Timo Rager ,  Tanja Schweisel ,  Stephan Veit ,  Ralf Warrass ,  Heinz-Jorg Wennesheimer

IPC分类号： A61K31/7048 ,  C07H17/08 ,  A61P11/00

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。

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。

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。

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.

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。

公开(公告)号：US20120208779A1

公开(公告)日：2012-08-16

申请号：US13401991

申请日：2012-02-22

申请人： Fritz Blatter ,  Timo Rager ,  Ralf Warras

发明人： Fritz Blatter ,  Timo Rager ,  Ralf Warras

IPC分类号： A61K31/7048 ,  A61P31/04 ,  A61P11/00

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。

公开(公告)号：US20140155371A1

公开(公告)日：2014-06-05

申请号：US14234158

申请日：2012-07-24

申请人： Andreas Hafner ,  Tobias Hintermann ,  Martin Szelagiewicz ,  Bernd Siebenhaar ,  Fritz Blatter

发明人： Andreas Hafner ,  Tobias Hintermann ,  Martin Szelagiewicz ,  Bernd Siebenhaar ,  Fritz Blatter

IPC分类号： C07D205/08

CPC分类号： C07D205/08 ,  C07B57/00

摘要： Provided is a crystalline composition comprising a mixture of a compound of formula 1 (Ezetimibe) and proline or proline derivatives, or a hydrate/solvate thereof, as well as a process for obtaining the same. And a process for the purification of Ezetimibe is also disclosed.

摘要翻译： 提供了包含式1化合物（依泽替米贝）和脯氨酸或脯氨酸衍生物或其水合物/溶剂化物的混合物的结晶组合物，以及其获得方法。 还公开了纯化依泽替米贝的方法。

公开(公告)号：US20140128444A1

公开(公告)日：2014-05-08

申请号：US14116110

申请日：2012-05-15

申请人： Fritz Blatter ,  Katharina Reichenbächer

发明人： Fritz Blatter ,  Katharina Reichenbächer

IPC分类号： C07D491/044 ,  C07C59/42 ,  C07C55/08

CPC分类号： C07D491/044 ,  C07C55/08 ,  C07C59/42 ,  C07D491/04

摘要： Novel crystalline salts of Asenapine (I) with organic di-acids and tri-acids and to methods of their preparation are disclosed along with related pharmaceutical compositions and methods of treating psychotic diseases or disorders.

摘要翻译： 与有机二酸和三酸的新型结晶盐及其制备方法一起公开了治疗精神病或疾病的相关药物组合物和方法。

公开(公告)号：US20120101126A1

公开(公告)日：2012-04-26

申请号：US13280431

申请日：2011-10-25

申请人： Paul Adriaan Van Der Schaaf ,  Fritz Blatter ,  Martin Szelagiewicz ,  Kai-Uwe Schöning

发明人： Paul Adriaan Van Der Schaaf ,  Fritz Blatter ,  Martin Szelagiewicz ,  Kai-Uwe Schöning

IPC分类号： A61K31/47 ,  C07D215/14

CPC分类号： C07D215/14 ,  C07B2200/13

摘要： The present invention is directed to new crystalline forms of Pitavastatin hemicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous form.

摘要翻译： 本发明涉及匹伐他汀半钙盐的新结晶形式，以下称为多晶型A，B，C，D，E和F，以及无定形形式。 此外，本发明涉及制备这些结晶形式的方法和包含这些结晶形式或无定形形式的无定形形式和药物组合物。