JP6443812B2 - ハリコンドリンb類縁体の合成に有用な方法 - Google Patents
ハリコンドリンb類縁体の合成に有用な方法 Download PDFInfo
- Publication number
- JP6443812B2 JP6443812B2 JP2016532033A JP2016532033A JP6443812B2 JP 6443812 B2 JP6443812 B2 JP 6443812B2 JP 2016532033 A JP2016532033 A JP 2016532033A JP 2016532033 A JP2016532033 A JP 2016532033A JP 6443812 B2 JP6443812 B2 JP 6443812B2
- Authority
- JP
- Japan
- Prior art keywords
- eribulin
- pharmaceutically acceptable
- acceptable salt
- alkyl
- acetonitrile
- 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.)
- Active
Links
- 0 C[C@](C[C@@](*C1C[C@@]2OC(CC(CO)O)[C@@](*)C2CC(CC(CCC2O[C@]3C4O[C@](CC(C*C(C5)*6)=O)C3O)*[C@@]2C4O)=O)CCC6C5=C)C1=C Chemical compound C[C@](C[C@@](*C1C[C@@]2OC(CC(CO)O)[C@@](*)C2CC(CC(CCC2O[C@]3C4O[C@](CC(C*C(C5)*6)=O)C3O)*[C@@]2C4O)=O)CCC6C5=C)C1=C 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/22—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361912714P | 2013-12-06 | 2013-12-06 | |
| US61/912,714 | 2013-12-06 | ||
| PCT/US2014/068834 WO2015085193A1 (en) | 2013-12-06 | 2014-12-05 | Methods useful in the synthesis of halichondrin b analogs |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018194871A Division JP6634135B2 (ja) | 2013-12-06 | 2018-10-16 | ハリコンドリンb類縁体の合成に有用な方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016540752A JP2016540752A (ja) | 2016-12-28 |
| JP6443812B2 true JP6443812B2 (ja) | 2018-12-26 |
Family
ID=53270478
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016532033A Active JP6443812B2 (ja) | 2013-12-06 | 2014-12-05 | ハリコンドリンb類縁体の合成に有用な方法 |
| JP2018194871A Active JP6634135B2 (ja) | 2013-12-06 | 2018-10-16 | ハリコンドリンb類縁体の合成に有用な方法 |
| JP2019225297A Active JP6905041B2 (ja) | 2013-12-06 | 2019-12-13 | ハリコンドリンb類縁体の合成に有用な方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018194871A Active JP6634135B2 (ja) | 2013-12-06 | 2018-10-16 | ハリコンドリンb類縁体の合成に有用な方法 |
| JP2019225297A Active JP6905041B2 (ja) | 2013-12-06 | 2019-12-13 | ハリコンドリンb類縁体の合成に有用な方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (4) | US9303039B2 (https=) |
| EP (2) | EP3077399B1 (https=) |
| JP (3) | JP6443812B2 (https=) |
| CN (1) | CN105916861B (https=) |
| BR (1) | BR112016012237B1 (https=) |
| CA (1) | CA2931788C (https=) |
| ES (1) | ES2723355T3 (https=) |
| HU (1) | HUE043088T2 (https=) |
| IL (4) | IL245661A0 (https=) |
| MX (3) | MX384292B (https=) |
| RU (1) | RU2676486C1 (https=) |
| SG (2) | SG11201604545XA (https=) |
| WO (1) | WO2015085193A1 (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| 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. |
| US10556910B2 (en) | 2014-06-30 | 2020-02-11 | President And Fellows Of Harvard College | Synthesis of halichondrin analogs and uses thereof |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2018217894A1 (en) * | 2017-05-24 | 2018-11-29 | Eisai R&D Management Co., Ltd. | Fluorine-labelled halichondrin derivatives and related methods of synthesis |
| 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 |
| CN109694379B (zh) * | 2017-10-24 | 2020-09-11 | 江苏恒瑞医药股份有限公司 | 用于制备艾日布林的中间体及其制备方法 |
| 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 |
| JP2021532102A (ja) * | 2018-07-20 | 2021-11-25 | ドクター レディズ ラボラトリーズ リミテッド | エリブリンおよびその中間体の調製のための精製プロセス |
| EP3864011A4 (en) * | 2018-10-09 | 2022-06-29 | Dr. Reddy's Laboratories Ltd. | Process for preparation of eribulin and intermediates thereof |
| US12522611B2 (en) * | 2018-11-28 | 2026-01-13 | Natco Pharma Limited | Process for the preparation of high pure Eribulin and its Mesylate salt |
| US11447499B2 (en) | 2019-06-14 | 2022-09-20 | Rk Pharma Inc. | Process for the preparation of eribulin mesylate intermediate |
| WO2022101931A1 (en) * | 2020-11-10 | 2022-05-19 | Natco Pharma Limited | Process for the preparation of eribulin and its intermediates |
| CN113354659B (zh) * | 2021-06-08 | 2022-04-08 | 江苏慧聚药业股份有限公司 | 甲磺酸艾日布林的合成 |
| CN114380840B (zh) * | 2022-01-27 | 2024-01-26 | 江苏慧聚药业股份有限公司 | 艾日布林的合成 |
| WO2025106586A1 (en) * | 2023-11-13 | 2025-05-22 | Luxvitae Therapeutics Inc. | Macrocyclic ketone compounds and applications thereof |
Family Cites Families (30)
| 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 |
| US8097648B2 (en) | 1998-06-17 | 2012-01-17 | Eisai R&D Management 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 |
| US6653341B1 (en) | 1998-06-17 | 2003-11-25 | Eisai Co., Ltd. | Methods and compositions for use in treating cancer |
| CA2822994C (en) * | 2004-06-03 | 2016-09-27 | Eisai R&D Management Co., Ltd. | Intermediates for the preparation of analogs of halichondrin b |
| EP2522663B1 (en) | 2004-06-03 | 2015-04-01 | Eisai R&D Management Co., Ltd. | Intermediates for the preparation 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 |
| JPWO2009014105A1 (ja) | 2007-07-20 | 2010-10-07 | 株式会社山田養蜂場本社 | 新規カルボン酸およびそれを有効成分とする抗うつ用組成物 |
| 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 |
| JP5371091B2 (ja) | 2009-01-23 | 2013-12-18 | 三菱レイヨン株式会社 | モノスルホン酸エステルの製造方法 |
| 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 |
| EP2354128A1 (en) | 2010-02-10 | 2011-08-10 | Sandoz Ag | Method for the preparation of rivaroxaban |
| 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 |
-
2014
- 2014-12-05 MX MX2020004855A patent/MX384292B/es unknown
- 2014-12-05 WO PCT/US2014/068834 patent/WO2015085193A1/en not_active Ceased
- 2014-12-05 US US14/562,086 patent/US9303039B2/en active Active
- 2014-12-05 SG SG11201604545XA patent/SG11201604545XA/en unknown
- 2014-12-05 BR BR112016012237-2A patent/BR112016012237B1/pt active IP Right Grant
- 2014-12-05 EP EP14866945.0A patent/EP3077399B1/en active Active
- 2014-12-05 EP EP18209462.3A patent/EP3505520A1/en active Pending
- 2014-12-05 CA CA2931788A patent/CA2931788C/en active Active
- 2014-12-05 RU RU2016124265A patent/RU2676486C1/ru active
- 2014-12-05 JP JP2016532033A patent/JP6443812B2/ja active Active
- 2014-12-05 MX MX2019011926A patent/MX376869B/es active IP Right Grant
- 2014-12-05 CN CN201480066353.XA patent/CN105916861B/zh active Active
- 2014-12-05 SG SG10201805024YA patent/SG10201805024YA/en unknown
- 2014-12-05 ES ES14866945T patent/ES2723355T3/es active Active
- 2014-12-05 MX MX2016006891A patent/MX370611B/es active IP Right Grant
- 2014-12-05 HU HUE14866945A patent/HUE043088T2/hu unknown
-
2016
- 2016-03-03 US US15/059,965 patent/US9695188B2/en active Active
- 2016-05-16 IL IL245661A patent/IL245661A0/en active IP Right Grant
-
2017
- 2017-06-30 US US15/638,493 patent/US10030032B2/en active Active
-
2018
- 2018-07-10 US US16/031,629 patent/US10450324B2/en active Active
- 2018-10-16 JP JP2018194871A patent/JP6634135B2/ja active Active
-
2019
- 2019-03-26 IL IL265640A patent/IL265640B/en active IP Right Grant
- 2019-12-13 JP JP2019225297A patent/JP6905041B2/ja active Active
-
2020
- 2020-04-01 IL IL273736A patent/IL273736B/en active IP Right Grant
-
2021
- 2021-03-04 IL IL281275A patent/IL281275B/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6443812B2 (ja) | ハリコンドリンb類縁体の合成に有用な方法 | |
| CN106470975B (zh) | 多环氨基甲酰基吡啶酮化合物的合成 | |
| CA2861150C (en) | Morphinan derivative | |
| RU2603261C2 (ru) | Региоселективное ацилирование рапамицина в положении с-42 | |
| CN111320610B (zh) | 大环hcv ns3抑制三肽的合成 | |
| JP2019510087A (ja) | ホスホラミダイト及びオリゴヌクレオチド合成のための組成物並びに方法 | |
| CN104011035A (zh) | 卡巴他赛的晶型和用于制备其的方法 | |
| CN106977415A (zh) | 一种沙库必曲的中间体及其制备方法 | |
| CN108752308B (zh) | 一种盐酸兰地洛尔的制备方法 | |
| CN109694379B (zh) | 用于制备艾日布林的中间体及其制备方法 | |
| Stoffman et al. | Synthesis of 4-haloserotonin derivatives and synthesis of the toad alkaloid dehydrobufotenine | |
| TWI462931B (zh) | β-核苷的合成技術 | |
| CN112574056A (zh) | 一种α,α-二氟-γ-羟基乙酰胺衍生物的合成方法 | |
| WO2023000135A1 (en) | Processes of making onapristone and intermediates thereof | |
| CN107043405B (zh) | 多环杂环化合物的晶型、其制备方法、应用及组合物 | |
| WO2002044136A1 (en) | PROCESSES FOR PREPARATION OF N-PROTECTED-ss-AMINO ALCOHOLS AND N-PROTECTED-ss-AMINO EPOXIDES | |
| FR3022907A1 (fr) | Derives d'osw-1 et leur utilisation en tant que medicament | |
| HK40022676B (en) | Synthesis of a macrocyclic hcv ns3 inhibiting tripeptide |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20161107 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20171130 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20180904 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20181016 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20181030 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20181116 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6443812 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |