公开(公告)号：US20180230140A1

公开(公告)日：2018-08-16

申请号：US15320608

申请日：2015-06-24

Applicant: BASF SE

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

IPC: C07D417/14 ,  C07C39/06 ,  C07C47/58 ,  A61P35/02

CPC classification number: C07D417/14 ,  A61P35/02 ,  C07B2200/13 ,  C07C39/06 ,  C07C47/58 ,  C07D417/12

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

公开(公告)号：US20140194453A1

公开(公告)日：2014-07-10

申请号：US14169844

申请日：2014-01-31

Applicant: BASF SE

Inventor： Andreas HAFNER ,  Fritz BLATTER ,  Martin SZELAGIEWICZ ,  Bernd SIEBENHAAR

IPC: 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。

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。

公开(公告)号：US20160168142A1

公开(公告)日：2016-06-16

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 VOSSER

IPC: C07D417/12 ,  C07C55/12 ,  C07D213/80 ,  C07D275/06

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.

Abstract translation: 本发明主要涉及达沙替尼的盐，其中盐是无定形的。 本文所述的盐优选包含式1的化合物的阳离子和选自戊二酸，烟酸和糖精的第二化合物的阴离子。 本发明还涉及包含这种盐的药物组合物。 此外，本发明涉及制备所述盐的方法。 本发明还涉及使用所述盐或药物组合物治疗疾病的若干方面。

公开(公告)号：US20160168143A1

公开(公告)日：2016-06-16

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。