公开(公告)号：US20170216266A1

公开(公告)日：2017-08-03

申请号：US15501908

申请日：2015-08-03

Applicant: BASF SE

Inventor： MARTIN VIERTELHAUS ,  Tiziana CHIODO ,  Beate SALVADOR ,  Marcus VOSSEN ,  Andreas HAFNER ,  Tobias HINTERMANN ,  Walter WEISHAAR ,  Rolf HELLMANN

IPC: A61K31/4402 ,  C07D213/40

CPC classification number: A61K31/4402 ,  C07D213/40

Abstract: The present invention primarily relates to multi-component crystals comprising a compound of formula 1 and a second compound selected from the group consisting of co-crystal formers and solvents. The invention is further related to pharmaceutical compositions comprising such multi-component crystals. Furthermore, the invention relates to processes for preparing said multi-component crystals. The invention also relates to several aspects of using said multi-component crystals or pharmaceutical compositions to treat a disease.

公开(公告)号：US20160303143A1

公开(公告)日：2016-10-20

申请号：US15103146

申请日：2014-12-09

Applicant: BASF SE

Inventor： Tiziana CHIODO ,  Beate SALVADOR ,  Marcus VOSSEN ,  Andreas HAFNER ,  Tobias HINTERMANN ,  Martin SZELAGIEWICZ ,  Fritz BLATTER ,  Martin VIERTELHAUS ,  Walter WEISHAAR

IPC: A61K31/58 ,  C07J43/00

CPC classification number: A61K31/58 ,  A61K9/14 ,  C07B2200/13 ,  C07J43/003

Abstract: Combinations of (3β)-17-(pyridin-3-yl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) with acidic substances such as citric acid, ascorbic acid, methyl-4-hydroxy benzoate, saccharin, vanillic acid, adipic acid, maleic acid, malic acid, tartaric acidare useful as pharmaceutical preparations and show improved properties such as aqueous solubility and dissolution kinetics, especially in the form of cocrystals or their combination with a suitable acid.

Abstract translation: （3β）-17-（吡啶-3-基）雄甾-5,16-二烯-3-基乙酸酯（醋酸阿比酮酮）与酸性物质如柠檬酸，抗坏血酸，甲基-4-羟基苯甲酸酯，糖精 ，香草酸，己二酸，马来酸，苹果酸，酒石酸可用作药物制剂，并显示出改善的性质，例如水溶性和溶解动力学，特别是以共晶体形式或与合适的酸的组合。