公开(公告)号：US09340536B2

公开(公告)日：2016-05-17

申请号：US14406339

申请日：2013-06-13

Applicant: BASF SE

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

IPC: C07D417/12 ,  A61K31/506 ,  C07C35/12 ,  C07C47/58 ,  C07C65/03 ,  C07D213/82 ,  C07D309/40

CPC classification number: C07D417/12 ,  A61K31/506 ,  C07B2200/07 ,  C07B2200/13 ,  C07C35/12 ,  C07C47/58 ,  C07C65/03 ,  C07C69/84 ,  C07D213/82 ,  C07D309/40 ,  A61K2300/00

Abstract: Provided are a multicomponent crystalline system (co-crystal), use thereof, as well as a process for obtaining the same. The said multicomponent crystalline system (co-crystal) comprises Dasatinib and a second compound selected from methyM-hydrobenzoate, nicotinamide, ethyl gallate, methyl gallate, propyl gallate, ethyl maltol, vanillin, menthol, or (1R,2S,5R)-(−)-menthol.

Abstract translation: 提供多组分结晶体（共晶体）及其用途，以及获得该组合物的方法。 所述多组分结晶体（共晶体）包含达沙替尼和选自甲基 - 羟基苯甲酸甲酯，烟酰胺，没食子酸乙酯，没食子酸甲酯，没食子酸丙酯，乙基麦芽酚，香草醛，薄荷醇或（1R，2S，5R） - （ - ） - 薄荷脑

公开(公告)号：US09884857B2

公开(公告)日：2018-02-06

申请号：US14906974

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 ,  C07D213/80 ,  C07C55/12

CPC classification number: C07D417/12 ,  C07C55/12 ,  C07D213/80 ,  C07D275/06

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

公开(公告)号：US20150133463A1

公开(公告)日：2015-05-14

申请号：US14406339

申请日：2013-06-13

Applicant: BASF SE

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

IPC: C07D417/12 ,  C07D213/82 ,  A61K31/506 ,  C07C47/58 ,  C07C35/12 ,  C07C65/03 ,  C07D309/40

CPC classification number: C07D417/12 ,  A61K31/506 ,  C07B2200/07 ,  C07B2200/13 ,  C07C35/12 ,  C07C47/58 ,  C07C65/03 ,  C07C69/84 ,  C07D213/82 ,  C07D309/40 ,  A61K2300/00

Abstract: Provided are a multicomponent crystalline system (co-crystal), use thereof, as well as a process for obtaining the same. The said multicomponent crystalline system (co-crystal) comprises Dasatinib and a second compound selected from methyM-hydrobenzoate, nicotinamide, ethyl gallate, methyl gallate, propyl gallate, ethyl maltol, vanillin, menthol, or (1R,2S,5R)-(−)-menthol.

Abstract translation: 提供多组分结晶体（共晶体）及其用途，以及获得该组合物的方法。 所述多组分结晶体（共晶体）包含达沙替尼和选自甲基 - 羟基苯甲酸甲酯，烟酰胺，没食子酸乙酯，没食子酸甲酯，没食子酸丙酯，乙基麦芽酚，香草醛，薄荷醇或（1R，2S，5R） - （ - ） - 薄荷脑

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。

公开(公告)号：US08841316B2

公开(公告)日：2014-09-23

申请号：US14169844

申请日：2014-01-31

Applicant: BASF SE

Inventor： Andreas Hafner ,  Fritz Blatter ,  Martin Szelagiewicz ,  Bernd Siebenhaar

IPC: A01N43/42 ,  A61K31/44 ,  A61K31/505 ,  A61K47/10

CPC classification number: A61K31/505 ,  A61K31/11 ,  A61K47/10 ,  C07D239/42

Abstract: A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior.

Abstract translation: 新型固体形式的罗苏伐他汀作为活性成分包含双[（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基） - 氨基]嘧啶-5-基 ] - （3R，5S）-3,5-二羟基庚-6-烯酸]和香草醛或香草醛衍生物。 包含两种组分的晶体和少量的水显示出改进的性能，例如结晶行为稳定性和降低的吸水行为。