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1. 发明申请

US20190100513A1 SOLID STATE FORM OF PLADIENOLIDE PYRIDINE COMPOUNDS AND METHODS OF USE 审中-公开
公开(公告)号：US20190100513A1
公开(公告)日：2019-04-04
申请号：US15529798
申请日：2016-11-17
申请人： EISAI R&D MANAGEMENT CO., LTD.
发明人： Gregg F. Keaney , John Wang , Baudouin Gerard , Kenzo Arai , Xiang Liu , Guo Zhu Zheng , Kazunobu Kira , Parcharee Tivitmahaisoon , Sudeep Prajapati , Nicholas C. Gearhart , Yoshihiko Kotake , Satoshi Nagao , Regina Mikie Kanada Sonobe , Masayuki Miyano , Norio Murai , Silvia Buonamici , Lihua Yu , Eunice Sun Park , Betty Chan , Peter G. Smith , Michael P. Thomas , Ermira Pazolli , Kian Huat Lim , Atsushi Endo , Arani Chanda
IPC分类号： C07D405/14 , A61P35/02
摘要： The present disclosure provides a novel solid state form of pladienolide pyridine compounds, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.

2. 发明授权

US10745387B2 Crystalline form of (2S,3S,6S,7R,10R,E)-7,10-dihydroxy-3,7-dimethyl-12-oxo-2-((R,2E,4E)-6-(piridin-2-yl)hepta-2,4-dien-2-yl)oxacyclododec-4-en-6-yl-4-methylpiperazine-1-carboxylate and methods of use thereof 有权
公开(公告)号：US10745387B2
公开(公告)日：2020-08-18
申请号：US15529798
申请日：2016-11-17
申请人： EISAI R&D MANAGEMENT CO., LTD.
发明人： Gregg F. Keaney , John Wang , Baudouin Gerard , Kenzo Arai , Xiang Liu , Guo Zhu Zheng , Kazunobu Kira , Parcharee Tivitmahaisoon , Sudeep Prajapati , Nicholas C. Gearhart , Yoshihiko Kotake , Satoshi Nagao , Regina Mikie Kanada Sonobe , Masayuki Miyano , Norio Murai , Silvia Buonamici , Lihua Yu , Eunice Sun Park , Betty Chan , Peter G. Smith , Michael P. Thomas , Ermira Pazolli , Kian Huat Lim , Atsushi Endo , Arani Chanda
IPC分类号： A61K31/496 , C07D295/182 , C07D405/14 , C07D405/06 , A61P35/02
摘要： The present disclosure provides a novel solid state form of pladienolide pyridine compounds having Formula I, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.

3. 发明申请

US20140235614A1 MONOCYCLIC PYRIDINE DERIVATIVE 有权
标题翻译：单环吡啶衍生物
公开(公告)号：US20140235614A1
公开(公告)日：2014-08-21
申请号：US14183864
申请日：2014-02-19
申请人： Eisai R&D Management Co., Ltd.
发明人： Setsuo Funasaka , Toshimi Okada , Keigo Tanaka , Satoshi Nagao , Isao Ohashi , Yoshinobu Yamane , Yusuke Nakatani , Yuki Karoji
IPC分类号： C07D409/14 , C07D401/14 , C07D401/12
CPC分类号： C07D409/14 , C07D401/12 , C07D401/14
摘要： The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.
摘要翻译：本发明提供了具有FGFR抑制活性的新化合物或其药学上可接受的盐，以及含有该化合物的药物组合物。具体地说，本发明提供由下式（I）表示的化合物或其药学上可接受的盐：其中n表示0〜2; A表示亚芳基或亚杂芳基; G表示单键，氧原子或-CH 2 - ; E表示含氮非芳族杂环; R1表示烷氧基等; R2表示氢原子等; 并且R 3表示氢原子，烷基，烷氧基等，条件是当E表示氮杂环丁烷环且R 2或R 3存在于氮杂环丁烷环上的氮原子上时，R 2或R 3不表示氢原子。

4. 发明授权

US11926619B2 Certain pladienolide compounds and methods of use 有权
公开(公告)号：US11926619B2
公开(公告)日：2024-03-12
申请号：US17045952
申请日：2019-04-08
申请人： EISAI R&D MANAGEMENT CO., LTD.
发明人： Gregg F. Keaney , John Wang , Baudouin Gerard , Kenzo Arai , Xiang Liu , Guo Zhu Zheng , Kazunobu Kira , Lisa A. Marcaurelle , Marta Nevalainen , Ming-Hong Hao , Morgan Welzel O'Shea , Parcharee Tivitmahaisoon , Sudeep Prajapati , Tuoping Luo , Nicholas C. Gearhart , Jason T. Lowe , Yoshihiko Kotake , Satoshi Nagao , Regina Mikie Kanada Sonobe , Masayuki Miyano , Norio Murai , Andrew Cook , Shelby Ellery , Atsushi Endo , James Palacino , Dominic Reynolds
IPC分类号： C07D407/12 , A61K31/365 , A61K31/4427 , A61K31/497 , A61K45/06 , A61P35/00 , C07D313/00 , C07D405/12 , C07D405/14 , C07D407/06 , C07D407/14 , C07D413/12 , C07D417/12 , C07D487/08 , C07D487/10 , C07D491/107
CPC分类号： C07D407/06 , A61K45/06 , A61P35/00 , C07D313/00 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D487/08 , C07D487/10 , C07D491/107
摘要： The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.

5. 发明授权

US09481669B2 Pladienolide pyridine compounds and methods of use 有权
标题翻译：吡啶衍生物吡啶化合物及其使用方法
公开(公告)号：US09481669B2
公开(公告)日：2016-11-01
申请号：US14710687
申请日：2015-05-13
申请人： Eisai R&D Management Co., Ltd.
发明人： Gregg F. Keaney , John Wang , Baudouin Gerard , Kenzo Arai , Xiang Liu , Guo Zhu Zheng , Kazunobu Kira , Parcharee Tivitmahaisoon , Sudeep Prajapati , Nicholas C. Gearhart , Yoshihiko Kotake , Satoshi Nagao , Regina Mikie Kanada Sonobe , Masayuki Miyano , Norio Murai , Silvia Buonamici , Lihua Yu , Eunice Sun Park , Betty Chan , Peter G. Smith , Michael P. Thomas , Ermira Pazolli , Kian Huat Lim
IPC分类号： C07D405/06 , C07D405/14 , A61K31/496
CPC分类号： C07D405/14 , C07D405/06
摘要： The present invention provides novel pladienolide pyridine compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.
摘要翻译：本发明提供新颖的扁桃苷内酰吡啶化合物，含有这些化合物的药物组合物，以及使用该化合物作为治疗剂的方法。这些化合物可用于治疗癌症，特别是癌症，其中靶向剪接体的试剂和其中的突变已知是有用的。

6. 发明申请

US20150329528A1 Pladienolide Pyridine Compounds and Methods of Use 有权
标题翻译：普拉二烯内酯吡啶化合物和使用方法
公开(公告)号：US20150329528A1
公开(公告)日：2015-11-19
申请号：US14710687
申请日：2015-05-13
申请人： Eisai R&D Management Co., Ltd.
发明人： Gregg F. Keaney , John Wang , Baudouin Gerard , Kenzo Arai , Xiang Liu , Guo Zhu Zheng , Kazunobu Kira , Parcharee Tivitmahaisoon , Sudeep Prajapati , Nicholas C. Gearhart , Yoshihiko Kotake , Satoshi Nagao , Regina Mikie Kanada Sonobe , Masayuki Miyano , Norio Murai
IPC分类号： C07D405/14 , C07D405/06
CPC分类号： C07D405/14 , C07D405/06
摘要： The present invention provides novel pladienolide pyridine compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.
摘要翻译：本发明提供新颖的扁桃苷内酰吡啶化合物，含有这些化合物的药物组合物，以及使用该化合物作为治疗剂的方法。这些化合物可用于治疗癌症，特别是癌症，其中靶向剪接体的试剂和其中的突变已知是有用的。

7. 发明授权

US08933099B2 Monocyclic pyridine derivative 有权
标题翻译：单环吡啶衍生物
公开(公告)号：US08933099B2
公开(公告)日：2015-01-13
申请号：US14183864
申请日：2014-02-19
申请人： Eisai R&D Management Co., Ltd.
发明人： Setsuo Funasaka , Toshimi Okada , Keigo Tanaka , Satoshi Nagao , Isao Ohashi , Yoshinobu Yamane , Yusuke Nakatani , Yuki Karoji
IPC分类号： A61K31/445 , C07D401/14 , C07D409/14 , C07D401/12
CPC分类号： C07D409/14 , C07D401/12 , C07D401/14
摘要： The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.
摘要翻译：本发明提供了具有FGFR抑制活性的新化合物或其药学上可接受的盐，以及含有该化合物的药物组合物。具体地说，本发明提供由下式（I）表示的化合物或其药学上可接受的盐：其中n表示0〜2; A表示亚芳基或亚杂芳基; G表示单键，氧原子或-CH 2 - ; E表示含氮非芳族杂环; R1表示烷氧基等; R2表示氢原子等; 并且R 3表示氢原子，烷基，烷氧基等，条件是当E表示氮杂环丁烷环且R 2或R 3存在于氮杂环丁烷环上的氮原子上时，R 2或R 3不表示氢原子。

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