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公开(公告)号:US20190300542A1
公开(公告)日:2019-10-03
申请号:US16076028
申请日:2017-02-10
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor: Phil S. BARAN , Charles E. CHASE , Francis G. FANG
IPC: C07D493/22
Abstract: The invention relates to methods and intermediates useful in the synthesis of eribulin.
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12.
公开(公告)号:US20190161495A1
公开(公告)日:2019-05-30
申请号:US16313196
申请日:2017-06-30
Applicant: Charles E. Chase , Hyeong-Wook CHOI , Atsushi ENDO , Francis G. FANG , Dae-Shik KIM , EISAI R&D MANAGEMENT CO., LTD.
Inventor: Charles E. CHASE , Hyeong-Wook CHOI , Atsushi ENDO , Francis G. FANG , Dae-Shik KIM
IPC: C07D493/22
Abstract: The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
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13.
公开(公告)号:US20180118755A1
公开(公告)日:2018-05-03
申请号:US15571921
申请日:2016-05-09
Applicant: Francis G. FANG , Charles E. CHASE , EISAI R&D MANAGEMENT CO., LTD.
Inventor: Francis G. FANG , Dae-Shik KIM , Hyeong-Wook CHOI , Charles E. CHASE
IPC: C07D493/22 , C07F9/655
CPC classification number: C07D493/22 , C07F9/6552
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:US20170240560A1
公开(公告)日:2017-08-24
申请号:US15501658
申请日:2015-08-04
Applicant: Eisai R&D Management Co., Ltd.
Inventor: Francis G. FANG , Hyeong-Wook CHOI , Silvio CAMPAGNA , Steven MATHIEU
IPC: C07D493/22 , C07D313/00 , C07D493/08 , C07B57/00
CPC classification number: C07D493/22 , C07B57/00 , C07D313/00 , C07D493/08 , C07D493/18
Abstract: The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries.
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公开(公告)号:US20250092392A1
公开(公告)日:2025-03-20
申请号:US18557876
申请日:2022-04-28
Applicant: Eisai R&D Management Co., Ltd.
Inventor: Vinod VATHIPADIEKAL , Branko MITASEV , Courtney EASLEY-NEAL , Hyeong Wook CHOI , Francis G. FANG , John WANG , Praveen VEMULA , Jung Hwa LEE
IPC: C12N15/113
Abstract: Novel antisense oligonucleotides that induce Exon-2 skipping in the CD33 gene during pre-mRNA splicing, and their use in the treatment of a neurodegenerative disease, such as Alzheimer's disease, are disclosed.
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公开(公告)号:US20230279018A1
公开(公告)日:2023-09-07
申请号:US18188249
申请日:2023-03-22
Applicant: The Broad Institute, Inc. , President and Fellows of Harvard College , Eisai R&D Management Co., LTD.
Inventor: Eamon COMER , Bruno MELILLO , Francis G. FANG , Branko MITASEV
IPC: C07D487/04 , A61P33/06 , A61P33/02
CPC classification number: C07D487/04 , A61P33/06 , A61P33/02
Abstract: The invention provides agents that inhibit L-Phe in cytoplasmic phenylalanine tRNA-synthetase (cFRS), methods for identifying them, compositions comprising such agents, and therapeutic methods of using such agents.
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17.
公开(公告)号:US20190308992A1
公开(公告)日:2019-10-10
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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18.
公开(公告)号:US20190144463A1
公开(公告)日:2019-05-16
申请号:US16246999
申请日:2019-01-14
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 , C07D493/14 , C07D407/14 , C07D307/28 , C07D407/06
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:US20180037588A1
公开(公告)日:2018-02-08
申请号:US15787268
申请日:2017-10-18
Applicant: EISAI R&D MANAGEMENT CO., LTD.
Inventor: Charles E. CHASE , Atsushi ENDO , Francis G. FANG , Jing LI
IPC: C07D493/18 , C07D405/14 , C07D307/26 , C07D309/16 , C07D307/20 , C07D493/04 , C07D405/06
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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公开(公告)号:US20160214992A1
公开(公告)日:2016-07-28
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 , 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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