公开(公告)号：US20150126520A1

公开(公告)日：2015-05-07

申请号：US14406264

申请日：2013-06-18

Applicant: BASF SE

Inventor： Tiziana Chiodo ,  Rolf Hellmann ,  Marcus Vossen ,  Beate Salvador ,  Andreas Hafner ,  Tobias Hintermann

IPC: C07D401/04 ,  C07C55/10 ,  C07C57/15 ,  C07C63/06

CPC classification number: C07D401/04 ,  C07B2200/13 ,  C07C55/10 ,  C07C57/15 ,  C07C63/06

Abstract: Novel solid forms of imatinib mesilate comprising as active ingredient 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]-benzamide methanesulfonic acid salt and as co-crystal former benzoic acid, fumaric acid or succinic acid are described. The said multi-component crystalline forms possess improved physical and biological properties with respect to the crystalline forms of the active pharmaceutical ingredient previously known.

Abstract translation: 包含作为活性成分的4 - [（4-甲基-1-哌嗪基）甲基] -N- [4-甲基-3 - [[4-（3-吡啶基）-2-嘧啶基]氨基] - 苯基] - 苯甲酰胺甲磺酸盐和共结晶前体苯甲酸，富马酸或琥珀酸。 所述多组分结晶形式相对于先前已知的活性药物成分的结晶形式具有改善的物理和生物学性质。

公开(公告)号：US09556164B2

公开(公告)日：2017-01-31

申请号：US14907148

申请日：2014-07-22

Applicant: BASF SE

Inventor： Andreas Hafner ,  Fritz Blatter ,  Martin Szelagiewicz ,  Bernd Siebenhaar ,  Tiziana Chiodo ,  Tobias Hintermann ,  Beate Salvador ,  Marcus Vossen

IPC: C07D417/12 ,  C07D275/06

CPC classification number: C07D417/12 ,  C07B2200/13 ,  C07D275/06

Abstract: The present invention primarily relates to molecular crystalline substances, preferably salts of Dasatinib in crystalline form, comprising a compound of formula 1, preferably a cation of a compound of formula 1, and a second compound selected from the group consisting of glutaric acid, nicotinic acid and saccharin, preferably an anion thereof. The invention is further related to pharmaceutical compositions comprising such a substance. Furthermore, the invention relates to processes for preparing said substances. The invention also relates to several aspects of using said substances or pharmaceutical compositions to treat a disease.

Abstract translation: 本发明主要涉及分子结晶物质，优选结晶形式的达沙替尼盐，其包含式1化合物，优选式1化合物的阳离子和选自戊二酸，烟酸 和糖精，优选其阴离子。 本发明还涉及包含这种物质的药物组合物。 此外，本发明涉及制备所述物质的方法。 本发明还涉及使用所述物质或药物组合物治疗疾病的若干方面。