公开(公告)号：EP3024830A2

公开(公告)日：2016-06-01

申请号：EP14741630.9

申请日：2014-07-22

Applicant: BASF SE

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

IPC: C07D417/12 ,  A61K31/506

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，烟酸的第二化合物 和糖精，优选其阴离子。 本发明进一步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：EP2699552A1

公开(公告)日：2014-02-26

申请号：EP12714011.9

申请日：2012-04-16

Applicant: BASF SE

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

IPC: C07D239/42 ,  A61K31/505 ,  A61P9/00

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.

公开(公告)号：EP2861589B1

公开(公告)日：2017-05-17

申请号：EP13804937.4

申请日：2013-06-13

Applicant: BASF SE

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

IPC: C07D417/12 ,  A61K31/506 ,  A61P35/02

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

公开(公告)号：EP3024831A2

公开(公告)日：2016-06-01

申请号：EP14741880.0

申请日：2014-07-22

Applicant: BASF SE

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

IPC: C07D417/12

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.

Abstract translation: 本发明主要涉及达沙替尼的盐，其中盐是无定形形式。 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。 本发明进一步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几个方面。

公开(公告)号：EP2861589A2

公开(公告)日：2015-04-22

申请号：EP13804937.4

申请日：2013-06-13

Applicant: BASF SE

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

IPC: C07D417/12 ,  A61K31/506 ,  A61P35/00

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: The present invention refers to a multicomponent crystalline system (co-crystal) comprising a compound of formula 1 (INN: Dasatinib) and a second compound selected from methyl-4-hydroxybenzoate, or nicotinamide, or ethyl gallate, or methyl gallate, or propyl gallate, or ethyl maltol or vanillin, or men- thol, or (1R,2S,5R)-(-)-menthol,as well as to a process for obtaining the same.

公开(公告)号：EP2643305A1

公开(公告)日：2013-10-02

申请号：EP11784683.2

申请日：2011-11-21

Applicant: BASF SE

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

IPC: C07D239/42 ,  A61K31/505 ,  A61P3/06

CPC classification number: C07D239/42 ,  A61K31/505 ,  A61K47/26 ,  A61K47/6941 ,  C07C29/00 ,  C07C31/26

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 sorbitol. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystal- lization behaviour and stability.