SG10201805024YA - Methods useful in the synthesis of halichondrin b analogs - Google Patents
Methods useful in the synthesis of halichondrin b analogsInfo
- Publication number
- SG10201805024YA SG10201805024YA SG10201805024YA SG10201805024YA SG10201805024YA SG 10201805024Y A SG10201805024Y A SG 10201805024YA SG 10201805024Y A SG10201805024Y A SG 10201805024YA SG 10201805024Y A SG10201805024Y A SG 10201805024YA SG 10201805024Y A SG10201805024Y A SG 10201805024YA
- Authority
- SG
- Singapore
- Prior art keywords
- halichondrin
- analogs
- synthesis
- methods useful
- eribulin
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 3
- FXNFULJVOQMBCW-VZBLNRDYSA-N halichondrin b Chemical class O([C@@H]1[C@@H](C)[C@@H]2O[C@@H]3C[C@@]4(O[C@H]5[C@@H](C)C[C@@]6(C[C@@H]([C@@H]7O[C@@H](C[C@@H]7O6)[C@@H](O)C[C@@H](O)CO)C)O[C@H]5C4)O[C@@H]3C[C@@H]2O[C@H]1C[C@@H]1C(=C)[C@H](C)C[C@@H](O1)CC[C@H]1C(=C)C[C@@H](O1)CC1)C(=O)C[C@H](O2)CC[C@H]3[C@H]2[C@H](O2)[C@@H]4O[C@@H]5C[C@@]21O[C@@H]5[C@@H]4O3 FXNFULJVOQMBCW-VZBLNRDYSA-N 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- 238000003786 synthesis reaction Methods 0.000 title abstract 3
- UFNVPOGXISZXJD-JBQZKEIOSA-N eribulin Chemical compound C([C@H]1CC[C@@H]2O[C@@H]3[C@H]4O[C@@H]5C[C@](O[C@H]4[C@H]2O1)(O[C@@H]53)CC[C@@H]1O[C@H](C(C1)=C)CC1)C(=O)C[C@@H]2[C@@H](OC)[C@@H](C[C@H](O)CN)O[C@H]2C[C@@H]2C(=C)[C@H](C)C[C@H]1O2 UFNVPOGXISZXJD-JBQZKEIOSA-N 0.000 abstract 2
- ZBLLGPUWGCOJNG-UHFFFAOYSA-N Halichondrin B Natural products CC1CC2(CC(C)C3OC4(CC5OC6C(CC5O4)OC7CC8OC9CCC%10OC(CC(C(C9)C8=C)C%11%12CC%13OC%14C(OC%15CCC(CC(=O)OC7C6C)OC%15C%14O%11)C%13O%12)CC%10=C)CC3O2)OC%16OC(CC1%16)C(O)CC(O)CO ZBLLGPUWGCOJNG-UHFFFAOYSA-N 0.000 abstract 1
- 229960003649 eribulin Drugs 0.000 abstract 1
- 229960000439 eribulin mesylate Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 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)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (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 (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361912714P | 2013-12-06 | 2013-12-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG10201805024YA true SG10201805024YA (en) | 2018-07-30 |
Family
ID=53270478
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG10201805024YA SG10201805024YA (en) | 2013-12-06 | 2014-12-05 | Methods useful in the synthesis of halichondrin b analogs |
| SG11201604545XA SG11201604545XA (en) | 2013-12-06 | 2014-12-05 | Methods useful in the synthesis of halichondrin b analogs |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201604545XA SG11201604545XA (en) | 2013-12-06 | 2014-12-05 | Methods useful in the synthesis of halichondrin b analogs |
Country Status (13)
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2748200T3 (es) | 2004-06-03 | 2020-03-13 | Eisai R&D Man Co Ltd | Productos intermedios para la preparación de halicondrina B |
| CN101883763B (zh) | 2007-10-03 | 2016-04-20 | 卫材R&D管理有限公司 | 用于合成软海绵素b类似物的中间体和方法 |
| RU2517167C2 (ru) | 2008-04-04 | 2014-05-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Аналоги галихондрина в |
| MX2012008510A (es) | 2010-01-26 | 2012-11-21 | Eisai R&D Man Co Ltd | Derivados de furo [3, 2-b] pirano utiles en la sintesis de analogos de halicondrina b. |
| RU2710545C2 (ru) | 2013-11-04 | 2019-12-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Реакции макроциклизации и промежуточные соединения и другие фрагменты, пригодные в получении аналогов халихондрина b |
| MX376869B (es) * | 2013-12-06 | 2025-03-07 | Eisai R&D Man Co Ltd | Metodos utiles en la sintesis de analogos de halicondrina b. |
| EP3160970A4 (en) | 2014-06-30 | 2017-12-27 | 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 |
| CN117024469A (zh) | 2015-05-07 | 2023-11-10 | 卫材R&D管理有限公司 | 可用于合成软海绵素大环内酯的大环化反应以及中间体和其他片段 |
| RU2732575C2 (ru) | 2016-02-12 | 2020-09-21 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Промежуточные продукты в синтезе эрибулина и соответствующие способы синтеза |
| PE20231049A1 (es) | 2016-03-02 | 2023-07-11 | Eisai Randd Man Co Ltd | Conjugados de anticuerpo y farmaco basados en eribulina y metodos para su uso |
| JP7068204B2 (ja) | 2016-06-30 | 2022-05-16 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ハリコンドリンマクロライドおよびその類縁体の合成に有用なプリンス反応および中間体 |
| 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 |
| US9938288B1 (en) | 2017-04-05 | 2018-04-10 | President And Fellows Of Harvard College | Macrocyclic compound and uses thereof |
| PE20200602A1 (es) * | 2017-04-05 | 2020-03-10 | Harvard College | Compuesto macrociclico y sus usos |
| WO2018217894A1 (en) * | 2017-05-24 | 2018-11-29 | Eisai R&D Management Co., Ltd. | Fluorine-labelled halichondrin derivatives and related methods of synthesis |
| KR102438417B1 (ko) | 2017-07-06 | 2022-09-01 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 할리콘드린의 합성 |
| US11498892B2 (en) | 2017-07-06 | 2022-11-15 | President And Fellows Of Harvard College | Fe/Cu-mediated ketone synthesis |
| 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 |
| WO2020110146A1 (en) * | 2018-11-28 | 2020-06-04 | 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 (enrdf_load_stackoverflow) | 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 |
| IL139960A0 (en) | 1998-06-17 | 2002-02-10 | Eisai Co Ltd | Macrocylic 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 |
| ES2748200T3 (es) | 2004-06-03 | 2020-03-13 | Eisai R&D Man Co Ltd | Productos intermedios para la preparación de halicondrina B |
| CN1993342A (zh) * | 2004-06-03 | 2007-07-04 | 卫材株式会社 | 用于制备软海绵素b的中间体 |
| US20060045846A1 (en) | 2004-08-30 | 2006-03-02 | Horstmann Thomas E | Reagents and methods for labeling terminal olefins |
| WO2006076100A2 (en) | 2004-12-09 | 2006-07-20 | Eisai Co. Ltd. | Tubulin isotype screening in cancer therapy using halichondrin b analogs |
| 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 |
| US8119839B2 (en) | 2007-07-20 | 2012-02-21 | Yamada Apiculture Center, Inc. | Carboxylic acid and antidepressant composition containing the same as active ingredient |
| CN101883763B (zh) | 2007-10-03 | 2016-04-20 | 卫材R&D管理有限公司 | 用于合成软海绵素b类似物的中间体和方法 |
| WO2009064029A1 (en) | 2007-11-16 | 2009-05-22 | Eisai R & D Management Co., Ltd. | Novel intermediate for halichondrin b analog synthesis and novel desulfonylation reaction used for the intermediate |
| RU2517167C2 (ru) * | 2008-04-04 | 2014-05-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Аналоги галихондрина в |
| 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 |
| MX2012008510A (es) | 2010-01-26 | 2012-11-21 | Eisai R&D Man Co Ltd | Derivados de furo [3, 2-b] pirano utiles en la sintesis de analogos de halicondrina b. |
| 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 |
| CA2857385A1 (en) | 2011-11-30 | 2013-06-06 | Alphora Research Inc. | Process for preparation of (3r)-2,4-di-leaving group-3-methylbut-1-ene |
| EP2831082B1 (en) | 2012-03-30 | 2019-02-20 | Sandoz AG | 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 |
| RU2710545C2 (ru) | 2013-11-04 | 2019-12-27 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Реакции макроциклизации и промежуточные соединения и другие фрагменты, пригодные в получении аналогов халихондрина b |
| MX376869B (es) * | 2013-12-06 | 2025-03-07 | Eisai R&D Man Co Ltd | Metodos utiles en la sintesis de analogos de halicondrina b. |
| CN117024469A (zh) | 2015-05-07 | 2023-11-10 | 卫材R&D管理有限公司 | 可用于合成软海绵素大环内酯的大环化反应以及中间体和其他片段 |
| RU2732575C2 (ru) | 2016-02-12 | 2020-09-21 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Промежуточные продукты в синтезе эрибулина и соответствующие способы синтеза |
| JP7068204B2 (ja) | 2016-06-30 | 2022-05-16 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ハリコンドリンマクロライドおよびその類縁体の合成に有用なプリンス反応および中間体 |
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2014
- 2014-12-05 MX MX2019011926A patent/MX376869B/es active IP Right Grant
- 2014-12-05 CA CA2931788A patent/CA2931788C/en active Active
- 2014-12-05 WO PCT/US2014/068834 patent/WO2015085193A1/en active Application Filing
- 2014-12-05 HU HUE14866945A patent/HUE043088T2/hu unknown
- 2014-12-05 MX MX2016006891A patent/MX370611B/es active IP Right Grant
- 2014-12-05 EP EP14866945.0A patent/EP3077399B1/en active Active
- 2014-12-05 CN CN201480066353.XA patent/CN105916861B/zh active Active
- 2014-12-05 US US14/562,086 patent/US9303039B2/en active Active
- 2014-12-05 BR BR112016012237-2A patent/BR112016012237B1/pt active IP Right Grant
- 2014-12-05 ES ES14866945T patent/ES2723355T3/es active Active
- 2014-12-05 EP EP18209462.3A patent/EP3505520A1/en active Pending
- 2014-12-05 SG SG10201805024YA patent/SG10201805024YA/en unknown
- 2014-12-05 SG SG11201604545XA patent/SG11201604545XA/en unknown
- 2014-12-05 JP JP2016532033A patent/JP6443812B2/ja active Active
- 2014-12-05 MX MX2020004855A patent/MX384292B/es unknown
- 2014-12-05 RU RU2016124265A patent/RU2676486C1/ru active
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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
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2017
- 2017-06-30 US US15/638,493 patent/US10030032B2/en active Active
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2018
- 2018-07-10 US US16/031,629 patent/US10450324B2/en active Active
- 2018-10-16 JP JP2018194871A patent/JP6634135B2/ja active Active
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2019
- 2019-03-26 IL IL265640A patent/IL265640B/en active IP Right Grant
- 2019-12-13 JP JP2019225297A patent/JP6905041B2/ja active Active
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2020
- 2020-04-01 IL IL273736A patent/IL273736B/en active IP Right Grant
-
2021
- 2021-03-04 IL IL281275A patent/IL281275B/en unknown
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