公开(公告)号：US10045998B2

公开(公告)日：2018-08-14

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 ,  A61K9/14 ,  C07J43/00

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 acid are 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.

公开(公告)号：US10105355B2

公开(公告)日：2018-10-23

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: C07D213/40 ,  A61K31/4402

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：US09861104B2

公开(公告)日：2018-01-09

申请号：US14383731

申请日：2013-03-11

Applicant: BASF SE

Inventor： Torsten Knieriem ,  Tiziana Chiodo ,  Christopher Koradin ,  Tanja Weber ,  Walter Weishaar

IPC: A01N53/00 ,  A01N25/08 ,  A01N43/90

CPC classification number: A01N53/00 ,  A01N25/08 ,  A01N43/90 ,  A01N25/04 ,  A01N2300/00

Abstract: The present invention relates to a method for producing an aqueous suspension concentrate formulation and novel suspension concentrate formulations of the compound of formula I. The method comprises: a) providing an aqueous slurry of coarse particles of the compound of the formula I, where the compound of the formula I is at least partially present in its crystalline form B, which, in an X-ray powder diffractogram at 25° C. and Cu-Kα radiation, shows at least three, preferably at least four, in particular at least 5 or at least 7 or at least 9 or all of the following reflexes, given as 2θ values: 8.0±0.2°, 9.5±0.2°, 10.7±0.2°, 11.0±0.2°, 11.2±0.2°, 11.7±0.2°, 14.2±0.2°, 15.6±0.2°, 16.5±0.2°, 17.7±0.2°, 21.5±0.2°; b) comminuting the coarse particles in the slurry of the compound of formula I, which is at least partially present in its form B, in the presence of the at least one surfactant.

公开(公告)号：US20150018207A1

公开(公告)日：2015-01-15

申请号：US14383731

申请日：2013-03-11

Applicant: BASF SE

Inventor： Torsten Knieriem ,  Tiziana Chiodo ,  Christopher Koradin ,  Tanja Weber ,  Walter Weishaar

IPC: A01N53/00 ,  A01N25/08

CPC classification number: A01N53/00 ,  A01N25/08 ,  A01N43/90 ,  A01N25/04 ,  A01N2300/00

Abstract: The present invention relates to a method for producing an aqueous suspension concentrate formulation and novel suspension concentrate formulations of the compound of formula I. The method comprises: a) providing an aqueous slurry of coarse particles of the compound of the formula I, where the compound of the formula I is at least partially present in its crystalline form B, which, in an X-ray powder diffractogram at 25° C. and Cu-Kα radiation, shows at least three, preferably at least four, in particular at least 5 or at least 7 or at least 9 or all of the following reflexes, given as 2θ values: 8.0±0.2°, 9.5±0.2°, 10.7±0.2°, 11.0±0.2°, 11.2±0.2°, 11.7±0.2°, 14.2±0.2°, 15.6±0.2°, 16.5±0.2°, 17.7±0.2°, 21.5±0.2°; b) comminuting the coarse particles in the slurry of the compound of formula I, which is at least partially present in its form B, in the presence of the at least one surfactant.

Abstract translation: 本发明涉及一种制备水性悬浮液浓缩物制剂的方法和式I化合物的新型悬浮浓缩物制剂。该方法包括：a）提供式I化合物的粗颗粒的含水浆液，其中化合物 式I的至少一部分至少部分以其结晶形式B存在，其在25℃的X射线粉末衍射图和Cu-Kα辐射中显示出至少三个，优选至少四个，特别是至少5个 或至少7个或至少9个或全部以下反射，以2＆ 值：8.0±0.2°，9.5±0.2°，10.7±0.2°，11.0±0.2°，11.2±0.2°，11.7±0.2°，14.2±0.2°，15.6±0.2°，16.5±0.2°，17.7±0.2 °，21.5±0.2°; b）在存在至少一种表面活性剂的情况下粉碎至少部分以其B形式存在的式I化合物的浆料中的粗颗粒。