公开(公告)号：US20150175544A1

公开(公告)日：2015-06-25

申请号：US14415875

申请日：2013-08-05

Applicant: BASF SE

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

IPC: C07D213/81 ,  C07D249/08

CPC classification number: C07D213/81 ,  C07B2200/13 ,  C07D249/08

Abstract: The present invention refers to a multicomponent crystalline system (co-crystal) comprising a compound of formula (1) (4-[3,5-Bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]benzoic acid; INN: Deferasirox) formula (1) and a compound of formula (2) (Isonicotinamide; pyridine-4-carboxamide) formula (2), as well as to a process for obtaining the same.

Abstract translation: 本发明涉及包含式（1）化合物（4- [3,5-双（2-羟基苯基）-1H-1,2,4-三唑-1-基）的多组分结晶体（共晶体） ]苯甲酸; INN：Deferasirox）式（1）和式（2）化合物（异烟酰胺;吡啶-4-甲酰胺）式（2），以及其获得方法。

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：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：US09567317B2

公开(公告)日：2017-02-14

申请号：US14433147

申请日：2013-10-16

Applicant: BASF SE

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

IPC: C07D401/14

CPC classification number: C07D401/14

Abstract: The present invention relates to crystalline materials comprising nilotinib and a carboxylic acid, carboxylic acid ester, carboxylic acid amide or sulfonic acid as a co-crystal former, and to pharmaceutical compositions comprising said materials. The invention also relates to processes for preparing said crystalline materials and to methods of using said crystalline materials to treat a disease condition in which tyrosine kinase inhibition is beneficial.

Abstract translation: 本发明涉及包含尼罗替尼和羧酸，羧酸酯，羧酸酰胺或磺酸作为共晶体形成剂的结晶材料以及包含所述材料的药物组合物。 本发明还涉及制备所述结晶材料的方法以及使用所述结晶材料治疗其中酪氨酸激酶抑制是有益的疾病状况的方法。

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：US09221789B2

公开(公告)日：2015-12-29

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: A61K31/506 ,  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：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：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：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：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.