JP2013518116A5 - - Google Patents
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- Publication number
- JP2013518116A5 JP2013518116A5 JP2012551271A JP2012551271A JP2013518116A5 JP 2013518116 A5 JP2013518116 A5 JP 2013518116A5 JP 2012551271 A JP2012551271 A JP 2012551271A JP 2012551271 A JP2012551271 A JP 2012551271A JP 2013518116 A5 JP2013518116 A5 JP 2013518116A5
- Authority
- JP
- Japan
- Prior art keywords
- protecting group
- hydroxyl protecting
- alkyl
- silyl
- oxygen atom
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29833710P | 2010-01-26 | 2010-01-26 | |
| US61/298,337 | 2010-01-26 | ||
| PCT/US2011/022611 WO2011094339A1 (en) | 2010-01-26 | 2011-01-26 | Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013518116A JP2013518116A (ja) | 2013-05-20 |
| JP2013518116A5 true JP2013518116A5 (https=) | 2014-03-13 |
| JP5800834B2 JP5800834B2 (ja) | 2015-10-28 |
Family
ID=43726543
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012551271A Active JP5800834B2 (ja) | 2010-01-26 | 2011-01-26 | ハリコンドリンｂ類似体の合成において有用なフロ［３，２−ｂ］ピラン誘導体 |
Country Status (11)
| Country | Link |
|---|---|
| US (6) | US8203010B2 (https=) |
| EP (1) | EP2528914B1 (https=) |
| JP (1) | JP5800834B2 (https=) |
| CN (1) | CN102803254B (https=) |
| BR (1) | BR112012018232B8 (https=) |
| CA (1) | CA2787919C (https=) |
| IL (1) | IL220913A (https=) |
| MX (1) | MX2012008510A (https=) |
| RU (1) | RU2579511C2 (https=) |
| SG (2) | SG182612A1 (https=) |
| WO (1) | WO2011094339A1 (https=) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6214865B1 (en) | 1998-06-17 | 2001-04-10 | Eisai Co., Ltd. | Macrocyclic analogs and methods of their use and preparation |
| EP2522663B1 (en) | 2004-06-03 | 2015-04-01 | Eisai R&D Management Co., Ltd. | Intermediates for the preparation of halichondrin B |
| RU2489437C2 (ru) | 2007-10-03 | 2013-08-10 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Промежуточные соединения и способы синтеза аналогов галихондрина в |
| CN105801599A (zh) | 2008-04-04 | 2016-07-27 | 卫材R&D管理有限公司 | 软海绵素b类似物 |
| ES2593027T3 (es) | 2009-03-30 | 2016-12-05 | Eisai R&D Management Co., Ltd. | Composición liposomal |
| WO2011094339A1 (en) | 2010-01-26 | 2011-08-04 | Eisai R&D Management Co., Ltd. | Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs |
| CN110097416B (zh) | 2011-09-18 | 2022-05-10 | 踏途音乐公司 | 具有卡拉ok和照相亭功能的数字点播设备及相关方法 |
| MX2015007185A (es) | 2012-12-04 | 2017-09-05 | Eisai R&D Man Co Ltd | Uso de eribulina en el tratamiento de cancer de pecho. |
| KR102265952B1 (ko) | 2013-06-26 | 2021-06-16 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 암 치료 병용요법으로서 에리불린 및 렌바티닙의 용도 |
| CA2916537C (en) | 2013-07-03 | 2021-07-27 | Alphora Research Inc. | Synthetic process for preparation of macrocyclic c1-keto analogs of halichondrin b and intermediates useful therein including intermediates containing -so2-(p-tolyl) groups |
| CN103483352A (zh) * | 2013-10-18 | 2014-01-01 | 李友香 | 抗肿瘤的药用原料药 |
| EP3689881B1 (en) * | 2013-11-04 | 2022-01-12 | Eisai R&D Management Co., Ltd. | Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b |
| MX384292B (es) | 2013-12-06 | 2025-03-14 | Eisai R&D Man Co Ltd | Metodos utiles en la sintesis de analogos de halicondrina b. |
| RU2699545C2 (ru) | 2014-05-28 | 2019-09-06 | ЭЙСАЙ Ар ЭНД Ди МЕНЕДЖМЕНТ КО., ЛТД | Применение эрибулина в лечении рака |
| US10556910B2 (en) | 2014-06-30 | 2020-02-11 | President And Fellows Of Harvard College | Synthesis of halichondrin analogs and uses thereof |
| KR102662228B1 (ko) | 2015-03-04 | 2024-05-02 | 머크 샤프 앤드 돔 코포레이션 | 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합 |
| CA2978311A1 (en) | 2015-03-04 | 2016-09-09 | Merck Sharp & Dohme Corp. | Combination of a pd-1 antagonist and eribulin for treating cancer |
| US10344038B2 (en) | 2015-04-30 | 2019-07-09 | President And Fellows Of Harvard College | Chromium-mediated coupling and application to the synthesis of halichondrins |
| KR102743950B1 (ko) * | 2015-05-07 | 2024-12-18 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 마크롤라이드의 합성에 유용한 마크로고리화 반응 및 중간체 및 기타 단편 |
| EP3413887B1 (en) | 2016-02-12 | 2021-04-07 | Eisai R&D Management Co., Ltd. | Intermediates in the synthesis of eribulin and related methods of synthesis |
| EP3423105B1 (en) | 2016-03-02 | 2021-05-05 | Eisai R&D Management Co., Ltd. | Eribulin-based antibody-drug conjugates and methods of use |
| US12029724B2 (en) | 2016-04-28 | 2024-07-09 | Eisai R&D Management Co., Ltd. | Method for inhibiting tumor growth |
| US11136335B2 (en) | 2016-06-30 | 2021-10-05 | Eisai R&D Management Co., Ltd. | Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof |
| BR112019007145A2 (pt) | 2016-10-14 | 2019-07-02 | Eisai R&D Man Co Ltd | combinação de um antagonista de pd-1 e eribulina para o tratamento de câncer urotelial |
| JP6978758B2 (ja) | 2016-11-11 | 2021-12-08 | プレジデント アンド フェローズ オブ ハーバード カレッジ | パラジウム媒介ケトール化 |
| CN108658956B (zh) * | 2017-03-28 | 2021-02-02 | 上海时莱生物技术有限公司 | 艾日布林中间体及其制备方法 |
| ES2931533T3 (es) | 2017-04-05 | 2022-12-30 | Harvard College | Compuesto macrocíclico y usos del mismo |
| US9938288B1 (en) | 2017-04-05 | 2018-04-10 | President And Fellows Of Harvard College | Macrocyclic compound and uses thereof |
| CN108948064B (zh) * | 2017-05-17 | 2021-02-02 | 上海时莱生物技术有限公司 | 一种艾日布林中间体及其制备方法 |
| US11498892B2 (en) | 2017-07-06 | 2022-11-15 | President And Fellows Of Harvard College | Fe/Cu-mediated ketone synthesis |
| HUE061306T2 (hu) | 2017-07-06 | 2023-06-28 | Harvard College | Halikondrinok szintézise |
| US20190046513A1 (en) | 2017-08-10 | 2019-02-14 | Huya Bioscience International, Llc | Combination therapies of hdac inhibitors and tubulin inhibitors |
| CN111566113B (zh) | 2017-11-15 | 2024-01-09 | 哈佛大学的校长及成员们 | 大环化合物及其用途 |
| US11419856B2 (en) | 2017-11-20 | 2022-08-23 | Basilea Pharmaceutica International AG | Pharmaceutical combinations for use in the treatment of neoplastic diseases |
| SG11202005548WA (en) | 2018-01-03 | 2020-07-29 | Eisai R&D Man Co Ltd | Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof |
| US11083705B2 (en) | 2019-07-26 | 2021-08-10 | Eisai R&D Management Co., Ltd. | Pharmaceutical composition for treating tumor |
| US12036204B2 (en) | 2019-07-26 | 2024-07-16 | Eisai R&D Management Co., Ltd. | Pharmaceutical composition for treating tumor |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU652180A1 (ru) * | 1975-12-16 | 1979-03-15 | Краснодарский политехнический институт | 1(Фурил-2,)-2-(2-,, формилфурил-5,, ) этилен или его метильное производное как промежуточный продукт дл синтеза фуран-2,5-дикарбоновой кислоты и способ его получени |
| US5436238A (en) * | 1992-03-12 | 1995-07-25 | President And Fellows Of Harvard College | Halichondrins and related compounds |
| US5338865A (en) * | 1992-03-12 | 1994-08-16 | President And Fellows Of Harvard College | Synthesis of halichondrin B and norhalichondrin B |
| GB9206244D0 (en) | 1992-03-23 | 1992-05-06 | Pharma Mar Sa | Cytotoxic compound from a marine sponge |
| TW255880B (https=) | 1992-09-09 | 1995-09-01 | Hoechst Ag | |
| WO1998009942A1 (en) | 1996-09-06 | 1998-03-12 | Eli Lilly And Company | Catalytic selective sulfonylation process |
| US6653341B1 (en) * | 1998-06-17 | 2003-11-25 | Eisai Co., Ltd. | Methods and compositions for use in treating cancer |
| US6214865B1 (en) * | 1998-06-17 | 2001-04-10 | Eisai Co., Ltd. | Macrocyclic analogs and methods of their use and preparation |
| US8097648B2 (en) | 1998-06-17 | 2012-01-17 | Eisai R&D Management Co., Ltd. | Methods and compositions for use in treating cancer |
| EP2522663B1 (en) | 2004-06-03 | 2015-04-01 | Eisai R&D Management Co., Ltd. | Intermediates for the preparation of halichondrin B |
| CA2822994C (en) * | 2004-06-03 | 2016-09-27 | Eisai R&D Management Co., Ltd. | Intermediates for the preparation of analogs of halichondrin b |
| US20060045846A1 (en) | 2004-08-30 | 2006-03-02 | Horstmann Thomas E | Reagents and methods for labeling terminal olefins |
| EP1831697A4 (en) | 2004-12-09 | 2011-01-26 | Eisai R&D Man Co Ltd | SEARCH FOR TUBULINISOTYPES IN CANCER THERAPY USING HALICHONDRIN B ANALOG |
| WO2008010776A1 (en) | 2006-07-21 | 2008-01-24 | Agency For Science, Technology And Research | Aigialomycin d and derivatives thereof and their use in treating cancer or malaria or a microbial infection |
| RU2489437C2 (ru) | 2007-10-03 | 2013-08-10 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Промежуточные соединения и способы синтеза аналогов галихондрина в |
| RU2010118063A (ru) * | 2007-11-16 | 2011-12-27 | ЭЙСАЙ Ар энд Ди МЕНЕДЖМЕНТ КО., ЛТД. (JP) | Новое промежуточное соединение для синтеза аналога галихондрина в и новая реакция десульфонилирования, применяемая для получения промежуточного соединения |
| CN105801599A (zh) | 2008-04-04 | 2016-07-27 | 卫材R&D管理有限公司 | 软海绵素b类似物 |
| WO2011094339A1 (en) | 2010-01-26 | 2011-08-04 | Eisai R&D Management Co., Ltd. | Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs |
| WO2012147900A1 (en) | 2011-04-28 | 2012-11-01 | Eisai R&D Management Co., Ltd. | Microreactor process for halichondrin b analog synthesis |
| EP2785687B1 (en) | 2011-11-30 | 2019-02-20 | Sandoz AG | Process for preparation of (3r)-2,4-di-leaving group-3-methylbut-1-ene |
| WO2013142999A1 (en) | 2012-03-30 | 2013-10-03 | Alphora Research Inc. | Synthetic process for preparation of macrocyclic c1-keto analogs of halichondrin b and intermediates useful therein |
| CA2916537C (en) | 2013-07-03 | 2021-07-27 | Alphora Research Inc. | Synthetic process for preparation of macrocyclic c1-keto analogs of halichondrin b and intermediates useful therein including intermediates containing -so2-(p-tolyl) groups |
| EP3689881B1 (en) | 2013-11-04 | 2022-01-12 | Eisai R&D Management Co., Ltd. | Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin b |
| MX384292B (es) | 2013-12-06 | 2025-03-14 | Eisai R&D Man Co Ltd | Metodos utiles en la sintesis de analogos de halicondrina b. |
| KR102743950B1 (ko) | 2015-05-07 | 2024-12-18 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 마크롤라이드의 합성에 유용한 마크로고리화 반응 및 중간체 및 기타 단편 |
| EP3413887B1 (en) | 2016-02-12 | 2021-04-07 | Eisai R&D Management Co., Ltd. | Intermediates in the synthesis of eribulin and related methods of synthesis |
| US11136335B2 (en) | 2016-06-30 | 2021-10-05 | Eisai R&D Management Co., Ltd. | Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof |
-
2011
- 2011-01-26 WO PCT/US2011/022611 patent/WO2011094339A1/en not_active Ceased
- 2011-01-26 RU RU2012136468/04A patent/RU2579511C2/ru active
- 2011-01-26 CA CA2787919A patent/CA2787919C/en active Active
- 2011-01-26 EP EP11702900.9A patent/EP2528914B1/en active Active
- 2011-01-26 SG SG2012053468A patent/SG182612A1/en unknown
- 2011-01-26 SG SG10201500552PA patent/SG10201500552PA/en unknown
- 2011-01-26 JP JP2012551271A patent/JP5800834B2/ja active Active
- 2011-01-26 CN CN201180015757.2A patent/CN102803254B/zh active Active
- 2011-01-26 MX MX2012008510A patent/MX2012008510A/es unknown
- 2011-01-26 BR BR112012018232A patent/BR112012018232B8/pt active IP Right Grant
- 2011-01-26 US US13/014,517 patent/US8203010B2/en active Active
-
2012
- 2012-05-22 US US13/477,483 patent/US8350067B2/en active Active
- 2012-07-12 IL IL220913A patent/IL220913A/en active IP Right Grant
-
2013
- 2013-01-07 US US13/735,516 patent/US8927597B2/en active Active
-
2014
- 2014-12-19 US US14/577,417 patent/US9382262B2/en active Active
-
2016
- 2016-06-29 US US15/196,600 patent/US9856276B2/en not_active Expired - Fee Related
-
2017
- 2017-12-13 US US15/840,109 patent/US10494388B2/en active Active
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