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1.发明授权Methods and compounds useful in the synthesis of orexin-2 receptor antagonists 有权用于合成食欲肽-2受体拮抗剂的方法和化合物公开(公告)号：US09416109B2
公开(公告)日：2016-08-16
申请号：US14379063
申请日：2013-02-14
Applicant: Eisai R&D Management Co., Ltd.
Inventor： George Anthony Moniz , Annie Zhu Wilcoxen , Farid Benayoud , Jaemoon Lee , Huiming Zhang , Taro Terauchi , Ayumi Takemura , Yu Yoshida , Toshiaki Tanaka , Keiichi Sorimachi , Yoshimitsu Naoe , Yuji Kazuta
IPC: C07D239/34 , C07C69/16 , C07C309/66 , C12P7/22 , C07C309/73 , C07D401/12 , C07C303/28 , C07C29/147
CPC classification number: C07C309/73 , C07B2200/07 , C07C29/147 , C07C69/16 , C07C303/28 , C07C303/44 , C07C309/66 , C07C2601/02 , C07D239/34 , C07D401/12 , C12P7/22 , C07C33/50
Abstract: The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.
Abstract translation: 本公开提供了可用于制备可用作食欲素-2受体拮抗剂的化合物的化合物和方法。
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公开(公告)号：US10934307B2
公开(公告)日：2021-03-02
申请号：US16833923
申请日：2020-03-30
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor： Francis G. Fang , Dae-Shik Kim , Hyeong-Wook Choi , Charles E. Chase , Jaemoon Lee
IPC: C07D493/22 , C07F7/18 , C07D407/14 , C07D307/28 , C07D407/06 , C07D493/14
Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
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公开(公告)号：US20190315754A1
公开(公告)日：2019-10-17
申请号：US16391882
申请日：2019-04-23
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Wanjun Zheng , Xiaojie Zhu , Hong Du , Maarten Postema , Yimin Jiang , Jing Li , Robert Yu , Hyeong-wook Choi , Jaemoon Lee , Frank Fang , Daniel Custar
IPC: C07D487/04 , C07D519/00 , A61P35/00
Abstract: We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
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公开(公告)号：US11434246B2
公开(公告)日：2022-09-06
申请号：US17141557
申请日：2021-01-05
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Wanjun Zheng , Xiaojie Zhu , Hong Du , Maarten Postema , Yimin Jiang , Jing Li , Robert Yu , Hyeong-Wook Choi , Jaemoon Lee , Francis G. Fang , Daniel Custar
IPC: C07D487/04 , C07D519/00 , A61P35/00
Abstract: We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
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公开(公告)号：US10941148B2
公开(公告)日：2021-03-09
申请号：US16391882
申请日：2019-04-23
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Wanjun Zheng , Xiaojie Zhu , Hong Du , Maarten Postema , Yimin Jiang , Jing Li , Robert Yu , Hyeong-wook Choi , Jaemoon Lee , Frank Fang , Daniel Custar
IPC: C07D487/04 , C07D519/00 , A61P35/00
Abstract: We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
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Patent Agency Ranking
公开(公告)号：US20180305362A1
公开(公告)日：2018-10-25
申请号：US15768668
申请日：2016-10-14
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Wanjun Zheng , Xiaojie Zhu , Hong Du , Maarten Postema , Yimin Jiang , Jing Li , Robert Yu , Hyeong-wook Choi , Jaemoon Lee , Frank Fang , Daniel Custar
IPC: C07D487/04 , C07D519/00 , A61P35/00
CPC classification number: C07D487/04 , A61P35/00 , C07D519/00
Abstract: We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
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公开(公告)号：US11643418B2
公开(公告)日：2023-05-09
申请号：US17188819
申请日：2021-03-01
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor： Francis G. Fang , Dae-Shik Kim , Hyeong-Wook Choi , Charles E. Chase , Jaemoon Lee
IPC: C07D493/22 , C07F7/18 , C07D407/14 , C07D307/28 , C07D407/06 , C07D493/14
CPC classification number: C07D493/22 , C07D307/28 , C07D407/06 , C07D407/14 , C07D493/14 , C07F7/1804
Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
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公开(公告)号：US10316040B2
公开(公告)日：2019-06-11
申请号：US15768668
申请日：2016-10-14
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Wanjun Zheng , Xiaojie Zhu , Hong Du , Maarten Postema , Yimin Jiang , Jing Li , Robert Yu , Hyeong-wook Choi , Jaemoon Lee , Frank Fang , Daniel Custar
IPC: C07D487/04 , C07D519/00 , A61P35/00
Abstract: We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
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9.发明授权公开(公告)号：US09783549B2
公开(公告)日：2017-10-10
申请号：US15033970
申请日：2014-11-04
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Francis G. Fang , Dae-Shik Kim , Hyeong-Wook Choi , Charles E. Chase , Jaemoon Lee
IPC: C07D493/22 , C07F7/18 , C07D307/28 , C07D407/06 , C07D493/14 , C07D407/14
CPC classification number: C07D493/22 , C07D307/28 , C07D407/06 , C07D407/14 , C07D493/14 , C07F7/1804
Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
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10.发明授权公开(公告)号：US10221189B2
公开(公告)日：2019-03-05
申请号：US15707412
申请日：2017-09-18
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor： Francis G. Fang , Dae-Shik Kim , Hyeong-Wook Choi , Charles E. Chase , Jaemoon Lee
IPC: C07D493/22 , C07D407/14 , C07D307/28 , C07D407/06 , C07F7/18 , C07D493/14
Abstract: The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
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