公开(公告)号：WO2016020324A1

公开(公告)日：2016-02-11

申请号：PCT/EP2015/067822

申请日：2015-08-03

Applicant: BASF SE

Inventor： VIERTELHAUS, Martin ,  CHIODO, Tiziana ,  SALVADOR, Beate ,  VOSSEN, Marcus ,  HAFNER, Andreas ,  HINTERMANN, Tobias ,  WEISHAAR, Walter ,  HELLMANN, Rolf

IPC: C07D213/40

CPC classification number: A61K31/4402 ,  C07D213/40

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 sol-vents. 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.

Abstract translation: 本发明主要涉及包含式1化合物和选自共晶体形成剂和溶剂的第二种化合物的多组分晶体。 本发明还涉及包含这种多组分晶体的药物组合物。 此外，本发明涉及制备所述多组分晶体的方法。 本发明还涉及使用所述多组分晶体或药物组合物治疗疾病的若干方面。

公开(公告)号：WO2015011120A2

公开(公告)日：2015-01-29

申请号：PCT/EP2014/065675

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: 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的盐，其包含式1化合物，优选式1化合物的阳离子和选自 由戊二酸，烟酸和糖精组成的组，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几个方面。

公开(公告)号：WO2014023682A1

公开(公告)日：2014-02-13

申请号：PCT/EP2013/066360

申请日：2013-08-05

Applicant: BASF SE ,  BASF SCHWEIZ AG

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

IPC: C07D249/08 ,  A61K31/4196 ,  A61P7/00

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：WO2013186726A2

公开(公告)日：2013-12-19

申请号：PCT/IB2013/054832

申请日：2013-06-13

Applicant: BASF SE ,  BASF SCHWEIZ AG ,  BASF (CHINA) COMPANY LIMITED

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

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.

Abstract translation: 本发明涉及包含式1化合物（INN：达沙替尼）和选自甲基-4-羟基苯甲酸酯或烟酰胺或没食子酸乙酯的第二化合物或没食子酸甲酯或丙基的多组分结晶体（共晶体） 乙酸麦芽糖醇或香草醛，或者吗啉，或（1R，2S，5R） - （ - ） - 薄荷醇，以及获得它们的方法。

公开(公告)号：WO2016001025A1

公开(公告)日：2016-01-07

申请号：PCT/EP2015/064201

申请日：2015-06-24

Applicant: BASF SE

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

IPC: C07D417/12 ,  A61K31/506

CPC classification number: 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.

Abstract translation: 本发明主要涉及包含式1化合物的多组分晶体和选自薄荷醇和香草醛的第二化合物。 本发明进一步涉及包含这种多组分晶体的药物组合物。 此外，本发明涉及制备所述多组分晶体的方法。 本发明还涉及使用所述多组分晶体或药物组合物治疗疾病的几个方面。

公开(公告)号：WO2015086596A1

公开(公告)日：2015-06-18

申请号：PCT/EP2014/077044

申请日：2014-12-09

Applicant: BASF SE

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

IPC: C07J43/00 ,  A61K9/14 ,  A61K31/58 ,  A61P35/00

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：WO2015011119A3

公开(公告)日：2015-01-29

申请号：PCT/EP2014/065674

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

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：WO2014060449A1

公开(公告)日：2014-04-24

申请号：PCT/EP2013/071580

申请日：2013-10-16

Applicant: BASF SE

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

IPC: C07D401/14 ,  A61K31/506 ,  A61P35/02

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：WO2013189910A1

公开(公告)日：2013-12-27

申请号：PCT/EP2013/062579

申请日：2013-06-18

Applicant: BASF SE ,  BASF SCHWEIZ AG

Inventor： CHIODO, Tiziana ,  HELLMANN, Rolf ,  VOSSEN, Marcus ,  SALVADOR, Beate ,  HAFNER, Andreas ,  HINTERMANN, Tobias

IPC: C07D401/04 ,  A61K31/505 ,  A61P35/02

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 saltand 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: 新型固体形式的伊马替尼甲磺酸盐，其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，并且作为共结晶前体苯甲酸，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：WO2013124791A1

公开(公告)日：2013-08-29

申请号：PCT/IB2013/051359

申请日：2013-02-20

Applicant: BASF SE ,  BASF (CHINA) COMPANY LIMITED

Inventor： CHIODO, Tiziana ,  HAFNER, Andreas ,  HINTERMANN, Tobias ,  SALVADOR, Beate ,  VOSSEN, Marcus ,  WEISHAAR, Walter

IPC: C07D239/69 ,  A61K31/506 ,  A61P9/12

CPC classification number: A61K31/506 ,  A61K31/194 ,  C07D239/69 ,  A61K2300/00

Abstract: A novel solid form of bosentan comprises as the active ingredient the N-[6-(2- Hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]-4-tert-butyl- benzenesulfonamide] and maleic acidor gentisic acid, especially as cocrystal former. The composition shows improved properties such as dissolution kinetic and hydration stability.

Abstract translation: 一种新型固体形式的波生坦含有作为活性成分的N- [6-（2-羟基乙氧基）-5-（2-甲氧基苯氧基）-2-嘧啶-2-基 - 嘧啶-4-基] -4-叔 - 丁基苯磺酰胺]和马来酸或龙胆酸，特别是共晶体。 该组合物显示改进的性质，例如溶解动力学和水合稳定性。