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公开(公告)号：US09802953B2
公开(公告)日：2017-10-31
申请号：US15092850
申请日：2016-04-07
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Charles E. Chase , Atsushi Endo , Francis G. Fang , Jing Li
IPC: C07D493/22 , C07D307/28 , C07D307/33 , C07D493/08 , C07D493/18 , C07D493/20 , C07D493/04
CPC classification number: C07D493/20 , C07D307/20 , C07D307/26 , C07D307/28 , C07D307/33 , C07D309/16 , C07D405/06 , C07D405/14 , C07D493/04 , C07D493/08 , C07D493/18 , C07D493/22 , Y02P20/55
Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.
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12.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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13.发明授权公开(公告)号：US11542269B2
公开(公告)日：2023-01-03
申请号：US16959882
申请日：2019-01-03
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor： Hyeong-Wook Choi , Francis G. Fang
IPC: C07D493/22 , C07D307/28 , C07D493/04 , C07D407/06 , C07D407/14 , A61P35/00
Abstract: The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
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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：US10913749B2
公开(公告)日：2021-02-09
申请号：US16387820
申请日：2019-04-18
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor： Francis G. Fang , Dae-Shik Kim , Hyeong-Wook Choi , Charles E. Chase
IPC: C07D493/22 , C07F9/655
Abstract: The invention provides methods for the synthesis of a halichondrin macrolides 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), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
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Patent Agency Ranking
公开(公告)号：US10717743B2
公开(公告)日：2020-07-21
申请号：US16284405
申请日：2019-02-25
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor： Charles E. Chase , Atsushi Endo , Francis G. Fang , Jing Li
IPC: C07D493/20 , C07D307/28 , C07D307/33 , C07D493/08 , C07D493/18 , C07D493/04 , C07D493/22 , C07D307/20 , C07D307/26 , C07D309/16 , C07D405/06 , C07D405/14
Abstract: Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.
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公开(公告)号：US10308661B2
公开(公告)日：2019-06-04
申请号：US15571921
申请日：2016-05-09
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor： Francis G. Fang , Dae-Shik Kim , Hyeong-Wook Choi , Charles E. Chase
IPC: C07D493/22 , C07F9/655
Abstract: The invention provides methods for the synthesis of a halichondrin macrolides 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), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
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公开(公告)号：US09856276B2
公开(公告)日：2018-01-02
申请号：US15196600
申请日：2016-06-29
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Atsushi Endo , Charles E. Chase , Francis G. Fang
IPC: C07D307/12 , C07F7/18 , C07D405/06 , C07D405/12 , C07D493/04 , C07D407/06 , C07D307/38
CPC classification number: C07F7/1804 , C07D307/12 , C07D307/38 , C07D405/06 , C07D405/12 , C07D407/06 , C07D493/04 , Y02P20/55
Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III):
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公开(公告)号：US20140012011A1
公开(公告)日：2014-01-09
申请号：US13947593
申请日：2013-07-22
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Francis G. Fang , James E. Foy , Lynn Hawkins , Charles Lemelin , Andre LesCarbeau , Xiang Niu , Kuo-Ming Wu
IPC: C07D263/14
CPC classification number: C07D263/14 , C07C217/28 , C07C271/16 , C07F9/091 , C07F9/1411 , C07F9/2408
Abstract: The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
Abstract translation: 本发明提供了制备TLR-4受体激动剂E6020及其立体异构体的方法，当与抗原如用于细菌和病毒疾病的疫苗共同施用时，该化合物可用作免疫佐剂。 还提供了合成中间体。
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20.发明申请INTERMEDIATES AND METHODS FOR MAKING ZEARALENONE MACROLIDE ANALOGS 审中-公开制备ZEARALENONE MACROLIDE ANALOGS的中间体和方法公开(公告)号：US20130211103A1
公开(公告)日：2013-08-15
申请号：US13733562
申请日：2013-01-03
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor： Roch Boivin , Silvio A. Campagna , Hong Du , Francis G. Fang , Thomas Horstmann , Charles-Andre Lemelin , Jing Li , Pamela McGuinness , Xiang Niu , Matthew J. Schnaderbeck , Kevin (kuo-ming) Wu , Xiaojie (jeff) Zhu
IPC: C07D313/00 , C07D317/30
CPC classification number: C07D313/00 , C07D317/22 , C07D317/24 , C07D317/30 , C07D319/08 , C07D493/04 , Y02P20/55
Abstract: Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R1-R12 are as defined herein.
Abstract translation: 本文公开了可用于制备大环内酯类的方法和中间体，例如其中R 1 -R 12如本文所定义的式（IV）化合物。
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