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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。
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2.发明授权公开(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。
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3.发明申请MULTICOMPONENT CRYSTALLINE SYSTEM COMPRISING DEFERASIROX AND ISONICOTINAMIDE AND A PROCESS FOR THE PREPARATION THEREOF 有权包含DEFERASIROX和异烟肼的多组分结晶体系及其制备方法公开(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。
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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
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.
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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.
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Patent Agency Ranking
6.发明授权公开(公告)号：US09290452B2
公开(公告)日：2016-03-22
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。
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7.发明申请MULTICOMPONENT CRYSTALLINE SYSTEM COMPRISING NILOTINIB AND SELECTED CO-CRYSTAL FORMERS 有权包含NILOTINIB和选择性CO晶体的多组分结晶体系公开(公告)号：US20150246901A1
公开(公告)日：2015-09-03
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。
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公开(公告)号：US20150087657A1
公开(公告)日：2015-03-26
申请号：US14360799
申请日：2012-12-03
Applicant: BASF SE
Inventor： Andreas Hafner , Tobias Hintermann , Fritz Blatter , Eva Roedel
IPC: A61K31/506 , A61K31/194
CPC classification number: A61K31/506 , A61K31/194 , C07D403/10 , A61K2300/00
Abstract: A novel solid form of Voriconazole comprises the active ingredient (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol and fumaric acid. The solid composition comprising the two components shows improved properties such as water solubility, crystallization behavior and stability.
Abstract translation: 伏立康唑的新型固体形式包括活性成分（2R，3S）-2-（2,4-二氟苯基）-3-（5-氟嘧啶-4-基）-1-（1H-1,2,4-三唑 -1-基）丁-2-醇和富马酸。 包含两种组分的固体组合物显示出改进的性能，例如水溶性，结晶行为和稳定性。
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9.发明授权Multicomponent crystalline system comprising nilotinib and selected co-crystal formers 有权包括尼罗替尼和选择的共晶体形成剂的多组分结晶体系公开(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。
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10.发明授权公开(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
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