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公开(公告)号：US08933108B2
公开(公告)日：2015-01-13
申请号：US13603990
申请日：2012-09-05
申请人： Jun Cao , Bernhard Erb , Robin Alec Fairhurst , Arnaud Grandeury , Shinji Hatakeyama , Magdalena Koziczak-Holbro , Xinzhong Lai , Philipp Lustenberger , Bernd Riebesehl , Nicola Tufilli , Thomas Ullrich , Xiang Wu , Jianguang Zhou
发明人： Jun Cao , Bernhard Erb , Robin Alec Fairhurst , Arnaud Grandeury , Shinji Hatakeyama , Magdalena Koziczak-Holbro , Xinzhong Lai , Philipp Lustenberger , Bernd Riebesehl , Nicola Tufilli , Thomas Ullrich , Xiang Wu , Jianguang Zhou
IPC分类号： A01N43/78 , A61K31/425 , C07D277/62 , C07D277/68 , C07D327/04 , C07D343/00 , C07D327/10 , C07D339/02 , C07D341/00 , C07D409/00 , C07D411/00 , C07D495/00 , C07D497/00 , A61K31/428 , A61K45/06
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
摘要翻译： 本发明提供游离形式或药学上可接受的盐形式的式（I）化合物，其制备本发明化合物的方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。
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公开(公告)号：US20160279107A1
公开(公告)日：2016-09-29
申请号：US15178579
申请日：2016-06-10
申请人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Xinzhong LAI , Philipp LUSTENBERGER , Bernd Ulrich RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang Wu , Jianguang ZHOU
发明人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Xinzhong LAI , Philipp LUSTENBERGER , Bernd Ulrich RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang Wu , Jianguang ZHOU
IPC分类号： A61K31/428
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
摘要翻译： 制备本发明化合物的方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。
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公开(公告)号：US20150094346A1
公开(公告)日：2015-04-02
申请号：US14566021
申请日：2014-12-10
申请人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
发明人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
IPC分类号： C07D277/68 , A61K31/167 , A61K31/428
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
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公开(公告)号：US20160075670A1
公开(公告)日：2016-03-17
申请号：US14947458
申请日：2015-11-20
申请人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
发明人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
IPC分类号： C07D277/68 , C07C53/10
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
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![Preparation of anhydrous and hydrated polymorphs 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-YL)-1H-benzimidazol-2-YL]-1H-quinolin-2-one-lactic acid salt](/abs-image/US/2015/03/24/US08987448B2/abs.jpg.150x150.jpg)
5.发明授权Preparation of anhydrous and hydrated polymorphs 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-YL)-1H-benzimidazol-2-YL]-1H-quinolin-2-one-lactic acid salt 有权无水水合多晶型物的制备4-氨基-5-氟-3- [6-（4-甲基哌嗪-1-基）-1H-苯并咪唑-2-基] -1H-喹啉-2-酮 - 乳酸盐公开(公告)号：US08987448B2
公开(公告)日：2015-03-24
申请号：US13637048
申请日：2011-03-25
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present technology provides methods of making anhydrous crystalline Form II and monohydrate crystalline Form B of the lactic acid salt of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one.
摘要翻译： 本技术提供了制备4-氨基-5-氟-3- [6-（4-甲基哌嗪-1-基）-1H-苯并咪唑-2-酮的乳酸盐的无水结晶II型和一水合物晶形B的方法 - 基] -1H-喹啉-2-酮。
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公开(公告)号：US20160000761A1
公开(公告)日：2016-01-07
申请号：US14770819
申请日：2014-02-26
申请人： Miloud ACHOUR , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Nicola TUFILLI , Thomas ULLRICH
发明人： Miloud ACHOUR , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Nicola TUFILLI , Thomas ULLRICH
IPC分类号： A61K31/428 , A61K9/48 , A61K9/20 , A61K31/19 , A61K9/00
CPC分类号： A61K31/428 , A61K9/0053 , A61K9/2018 , A61K9/2054 , A61K9/485 , A61K9/4858 , A61K9/4866 , A61K31/19
摘要： The present invention relates to a pharmaceutical composition in solid oral dosage form comprising (R)-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-hydroxybenzo[d]thiazol-2(3H)-one acetate salt.
摘要翻译： 本发明涉及一种固体口服剂型的药物组合物，其包含（R）-7-（2-（1-（4-丁氧基苯基）-2-甲基丙-2-基氨基）-1-羟乙基）-5-羟基苯并[ d]噻唑-2（3H） - 酮乙酸盐。
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公开(公告)号：US20130245080A1
公开(公告)日：2013-09-19
申请号：US13603990
申请日：2012-09-05
申请人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Xinzhong LAI , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
发明人： Jun CAO , Bernhard ERB , Robin Alec FAIRHURST , Arnaud GRANDEURY , Shinji HATAKEYAMA , Magdalena KOZICZAK-HOLBRO , Xinzhong LAI , Philipp LUSTENBERGER , Bernd RIEBESEHL , Nicola TUFILLI , Thomas ULLRICH , Xiang WU , Jianguang ZHOU
IPC分类号： A61K31/428 , A61K45/06 , C07D277/68
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
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![PREPARATION OF ANHYDROUS AND HYDRATED POLYMORPHS OF 4-AMINO-5-FLUORO-3-[6-(4-METHYLPIPERAZIN-1-YL)-1H-BENZIMIDAZOL-2-YL]-1H-QUINOLIN-2-ONE-LACTIC ACID SALT](/abs-image/US/2013/01/17/US20130018188A1/abs.jpg.150x150.jpg)
8.发明申请PREPARATION OF ANHYDROUS AND HYDRATED POLYMORPHS OF 4-AMINO-5-FLUORO-3-[6-(4-METHYLPIPERAZIN-1-YL)-1H-BENZIMIDAZOL-2-YL]-1H-QUINOLIN-2-ONE-LACTIC ACID SALT 有权4-氨基-5-氟-3- [6-（4-甲基哌嗪-1-基）-1H-苯并咪唑-2-基] -1H-喹啉-2-酮酸盐的无水和水解多聚体的制备公开(公告)号：US20130018188A1
公开(公告)日：2013-01-17
申请号：US13637048
申请日：2011-03-25
IPC分类号： C07D401/14
CPC分类号： C07D401/04
摘要： The present technology provides methods of making anhydrous crystalline Form II and monohydrate crystalline Form B of the lactic acid salt of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one.
摘要翻译： 本技术提供了制备4-氨基-5-氟-3- [6-（4-甲基哌嗪-1-基）-1H-苯并咪唑-2-酮的乳酸盐的无水结晶II型和一水合物晶形B的方法 - 基] -1H-喹啉-2-酮。
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公开(公告)号：US20180071292A1
公开(公告)日：2018-03-15
申请号：US15564534
申请日：2016-04-14
IPC分类号： A61K31/519 , A61K9/28 , A61K9/20
摘要： The present disclosure is directed to oral tablet of ribociclib including its salt(s). One embodiment of the present disclosure is directed to tablet of ribociclib with high drug load with an immediate release profile. One embodiment of the present disclosure is directed to coated tablet of ribociclib. Another embodiment of the present disclosure is directed to coated tablet of ribociclib where the coating is an advanced moisture barrier coating (e.g., Opadry® amb II coating where the coating is PVA based).
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公开(公告)号：US20160128979A1
公开(公告)日：2016-05-12
申请号：US14897439
申请日：2014-06-11
申请人： Bruno GALLI , Hubert THOMA , Arnaud GRANDEURY , Dirk SPICKERMANN , Karsten PUTZBACH , Klaus-Peter MOLL , Mike UFER , Jean-Marie GLANTZMANN , Martin MUELLER-ZSIGMONDY
发明人： Hubert THOMA , Bruno GALLI , Dirk SPICKERMANN , Karsten PUTZBACH , Klaus-Peter MOLL , Mike UFER , Arnaud GRANDEURY , Jean-Marie GLANTZMANN , Martin MUELLER-ZSIGMONDY
CPC分类号： A61K31/404 , A61J3/02 , A61J3/10 , A61K9/1652 , A61K9/1682 , A61K9/2004 , A61K9/2072 , A61K9/28 , A61K9/50 , A61K9/5089 , A61K31/4045 , A61K47/38
摘要： Drug products in the form of modified release formulations comprising the drug substance (-)-(3aR,4S,7aR)-4-Hydroxy-4m-tolylethynyl-octahydro-indole-1-carboxylic acid methyl ester (AFQ056), as well as processes for making such drug products are provided. The drug products are useful in treating patients with Parkinson's disease and exhibiting L-dopa induced dyskinesia.
摘要翻译： 包含药物（ - ） - （3aR，4S，7aR）-4-羟基-4m-甲苯乙炔基 - 八氢 - 吲哚-1-羧酸甲酯（AFQ056）的改性释放制剂形式的药物产品，以及 提供了制备这些药物的方法。 该药物可用于治疗帕金森病患者，并表现出左旋多巴引起的运动障碍。
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