公开(公告)号：EP3411370A1

公开(公告)日：2018-12-12

申请号：EP17702109.4

申请日：2017-01-31

申请人： Hexal AG

发明人： BORN, Max ,  LANGES, Christoph ,  LENGAUER, Hannes

IPC分类号： C07D409/12 ,  A61K31/4704 ,  A61K31/496 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28

CPC分类号： C07D409/12

摘要： The present invention relates to a brexpiprazole dihydrate crystalline form having a particle size distribution of d50 of at most 10 µm and less than 5% w/w of brexpiprazole anhydrate . The present invention also relates to a process for preparing this brexpiprazole dihydrate crystalline form and to pharmaceutical compositions thereof. The present invention also relates to a process for determining the absence of brexpiprazole anhydrate in this brexpiprazole dihydrate crystalline form. This brexpiprazole dihydrate crystalline form is used for the preparation of pharmaceutical compositions having delayed release properties upon intramuscular injection .

公开(公告)号：EP3293196A1

公开(公告)日：2018-03-14

申请号：EP16188159.4

申请日：2016-09-09

申请人： Hexal AG

发明人： LENGAUER, Hannes ,  HOTTER, Andreas

IPC分类号： C07J9/00

CPC分类号： C07J9/005 ,  C07B2200/13

摘要： The invention relates to a process for purifying obeticholic acid. In addition, crystalline forms of obeticholic acid are provided which are useful synthetic intermediates for the production of highly pure amorphous obeticholic acid. Accordingly, the invention also relates to a process for preparing amorphous obeticholic acid.

摘要翻译： 本发明涉及一种纯化奥茨油酸的方法。 此外，提供了奥贝胆酸的结晶形式，其是用于生产高纯度无定形obeticholic酸的有用的合成中间体。 因此，本发明还涉及制备无定形obeticholic酸的方法。