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公开(公告)号：US10407439B2
公开(公告)日：2019-09-10
申请号：US15906401
申请日：2018-02-27
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Francis G. Fang , Hyeong-Wook Choi , Silvio Campagna , Steven Mathieu
IPC: C07D493/22 , C07D493/08 , C07D493/18 , C07B57/00 , C07D313/00
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：US09382262B2
公开(公告)日：2016-07-05
申请号：US14577417
申请日：2014-12-19
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Atsushi Endo , Charles E. Chase , Francis G. Fang
IPC: C07D407/06 , C07D493/04 , C07D405/06 , C07D405/12 , 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：US10981929B2
公开(公告)日：2021-04-20
申请号：US16313196
申请日：2017-06-30
Applicant: 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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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：US10214539B2
公开(公告)日：2019-02-26
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: C07D493/20 , 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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Patent Agency Ranking
公开(公告)号：US09604993B2
公开(公告)日：2017-03-28
申请号：US14624033
申请日：2015-02-17
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Charles E. Chase , Atsushi Endo , Francis G. Fang , Jing Li
IPC: C07D493/20 , A61K31/335 , C07D307/28 , C07D307/33 , C07D493/08 , C07D493/18
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：US08975422B2
公开(公告)日：2015-03-10
申请号：US14250086
申请日：2014-04-10
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Francis G. Fang , Bryan M. Lewis , Matthew Schnaderbeck
IPC: C07D493/20 , C07D307/28 , C07D307/33 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C07D493/18 , C07D493/22 , C07D493/10 , C07F7/18 , C07D317/72 , C07H15/26
CPC classification number: C07F7/1804 , A61K31/341 , C07C33/423 , C07D307/12 , C07D307/28 , C07D307/33 , C07D317/72 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C07D493/10 , C07D493/18 , C07D493/20 , C07D493/22 , C07F7/188 , C07H15/26 , Y02P20/55
Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.
Abstract translation: 提供了中间体及其在合成类软绵母B合成中的应用方法。
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公开(公告)号：US20140163242A1
公开(公告)日：2014-06-12
申请号：US14096549
申请日：2013-12-04
Applicant: Eisai R&D Management Co., Ltd.
Inventor： Charles E. Chase , Francis G. Fang
IPC: C07D493/20 , C07D493/10 , C07D493/18 , C07F7/18
CPC classification number: C07F7/1804 , A61K31/341 , C07C33/423 , C07D307/12 , C07D307/28 , C07D307/33 , C07D317/72 , C07D407/06 , C07D407/14 , C07D493/04 , C07D493/08 , C07D493/10 , C07D493/18 , C07D493/20 , C07D493/22 , C07F7/188 , C07H15/26 , Y02P20/55
Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.
Abstract translation: 提供了中间体及其在合成类软绵母B合成中的应用方法。
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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：US10160768B2
公开(公告)日：2018-12-25
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: C07D493/18 , C07D493/22 , C07B57/00 , C07D313/00 , C07D493/08
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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