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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Peptides Or Proteins (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
METHODS USEFUL IN THE SYNTHESIS OF HALICHONDRIN B ANALOGS In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate). No Suitable Figure
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 |
|---|---|---|---|
| SG11201604545XA SG11201604545XA (en) | 2013-12-06 | 2014-12-05 | Methods useful in the synthesis of halichondrin b analogs |
| SG10201805024YA SG10201805024YA (en) | 2013-12-06 | 2014-12-05 | Methods useful in the synthesis of halichondrin b analogs |
Family Applications Before (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)
| Country | Link |
|---|---|
| US (4) | US9303039B2 (en) |
| EP (2) | EP3505520A1 (en) |
| JP (3) | JP6443812B2 (en) |
| CN (1) | CN105916861B (en) |
| BR (1) | BR112016012237B1 (en) |
| CA (1) | CA2931788C (en) |
| ES (1) | ES2723355T3 (en) |
| HU (1) | HUE043088T2 (en) |
| IL (4) | IL245661A0 (en) |
| MX (3) | MX370611B (en) |
| RU (1) | RU2676486C1 (en) |
| SG (2) | SG11201604545XA (en) |
| WO (1) | WO2015085193A1 (en) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101899026B (en) | 2004-06-03 | 2016-08-03 | 卫材R&D管理有限公司 | For preparing the intermediate of the analog of halichondrin B |
| MX2010003599A (en) | 2007-10-03 | 2010-09-10 | Eisai R&D Man Co Ltd | Intermediates and methods for the synthesis of halichondrin b analogs. |
| JP6001857B2 (en) | 2008-04-04 | 2016-10-05 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Halichondrin B analog |
| SG182612A1 (en) | 2010-01-26 | 2012-08-30 | Eisai R&D Man Co Ltd | Furo [3, 2 -b] pyrane derivatives useful in the synthesis of halichondrin b analogs |
| CA2929084C (en) | 2013-11-04 | 2022-01-11 | Eisai R&D Management Co., Ltd. | Macrocyclization reactions and intermediates and other fragments useful in the synthesis of analogs of halichondrin b |
| ES2723355T3 (en) * | 2013-12-06 | 2019-08-26 | Eisai R&D Man Co Ltd | Useful methods in the synthesis of halicondrine B analogues |
| WO2016003975A1 (en) | 2014-06-30 | 2016-01-07 | 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 (en) | 2015-05-07 | 2024-12-18 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrine macrolides |
| CN108601760A (en) * | 2016-02-12 | 2018-09-28 | 卫材R&D管理有限公司 | Intermediate in the synthesis of eribulin and relevant synthetic method |
| CA3013791A1 (en) | 2016-03-02 | 2017-09-08 | 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 (en) | 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 | Palladium-mediated ketolization |
| US9938288B1 (en) | 2017-04-05 | 2018-04-10 | President And Fellows Of Harvard College | Macrocyclic compound and uses thereof |
| SMT202200455T1 (en) * | 2017-04-05 | 2023-01-13 | 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 |
| IL307273B1 (en) | 2017-07-06 | 2024-11-01 | Harvard College | Synthesis of halichondrins |
| CN109694379B (en) * | 2017-10-24 | 2020-09-11 | 江苏恒瑞医药股份有限公司 | Intermediate for preparing eribulin and preparation method thereof |
| CN111566113B (en) | 2017-11-15 | 2024-01-09 | 哈佛大学的校长及成员们 | Macrocyclic compounds and uses thereof |
| WO2019097073A1 (en) | 2017-11-20 | 2019-05-23 | Basilea Pharmaceutica International AG | Pharmaceutical combinations for use in the treatment of neoplastic diseases |
| US11542269B2 (en) | 2018-01-03 | 2023-01-03 | Eisai R&D Management Co., Ltd. | Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof |
| WO2020016847A2 (en) * | 2018-07-20 | 2020-01-23 | Dr. Reddy’S Laboratories Limited | Purification process for preparation of eribulin and intermediates thereof |
| WO2020075027A1 (en) * | 2018-10-09 | 2020-04-16 | Dr. Reddy's Laboratories Limited | Process for preparation of eribulin and intermediates thereof |
| US20220089607A1 (en) * | 2018-11-28 | 2022-03-24 | 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 (en) | 2021-06-08 | 2022-04-08 | 江苏慧聚药业股份有限公司 | Synthesis of eribulin mesylate |
| CN114380840B (en) * | 2022-01-27 | 2024-01-26 | 江苏慧聚药业股份有限公司 | Synthesis of eribulin |
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| SU652180A1 (en) | 1975-12-16 | 1979-03-15 | Краснодарский политехнический институт | Method of obtaining 1-(furyl-2')-2-(2-"formyl-furyl-5") ethylene and its methyl derivative as intermediate product for synthesis of furan-2,5-dicarboxylic acid |
| US5338865A (en) | 1992-03-12 | 1994-08-16 | President And Fellows Of Harvard College | Synthesis of halichondrin B and norhalichondrin B |
| US5436238A (en) | 1992-03-12 | 1995-07-25 | President And Fellows Of Harvard College | Halichondrins and related compounds |
| GB9206244D0 (en) | 1992-03-23 | 1992-05-06 | Pharma Mar Sa | Cytotoxic compound from a marine sponge |
| TW255880B (en) | 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 |
| AU762998B2 (en) | 1998-06-17 | 2003-07-10 | Eisai R&D Management 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 |
| CN101899026B (en) | 2004-06-03 | 2016-08-03 | 卫材R&D管理有限公司 | For preparing the intermediate of the analog of halichondrin B |
| CN1993342A (en) * | 2004-06-03 | 2007-07-04 | 卫材株式会社 | 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 |
| 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 |
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| MX2010003599A (en) | 2007-10-03 | 2010-09-10 | Eisai R&D Man Co Ltd | Intermediates and methods for the synthesis of halichondrin b analogs. |
| JP5134686B2 (en) | 2007-11-16 | 2013-01-30 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Novel intermediates for the synthesis of halichondrin B analogues and novel desulfonylation reactions for use in said intermediates |
| JP6001857B2 (en) | 2008-04-04 | 2016-10-05 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Halichondrin B analog |
| JP5371091B2 (en) | 2009-01-23 | 2013-12-18 | 三菱レイヨン株式会社 | Method for producing monosulfonic acid ester |
| SG182612A1 (en) | 2010-01-26 | 2012-08-30 | Eisai R&D Man 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 |
| AU2012344697A1 (en) | 2011-11-30 | 2014-07-10 | Alphora Research Inc. | Process for preparation of (3R)-2,4-di-leaving group-3-methylbut-1-ene |
| JP6531911B2 (en) | 2012-03-30 | 2019-06-19 | サンド アーゲー | Synthetic process for preparing macrocyclic C1-keto analogues of halichondrin B and useful intermediates therefor |
| AU2014286880B2 (en) | 2013-07-03 | 2017-12-14 | Sandoz Ag | Synthetic process for preparation of macrocyclic C1-keto analogs of Halichondrin B and intermediates useful therein including intermediates containing -SO2-(p-TOLYL) groups |
| CA2929084C (en) | 2013-11-04 | 2022-01-11 | Eisai R&D Management Co., Ltd. | Macrocyclization reactions and intermediates and other fragments useful in the synthesis of analogs of halichondrin b |
| ES2723355T3 (en) * | 2013-12-06 | 2019-08-26 | Eisai R&D Man Co Ltd | Useful methods in the synthesis of halicondrine B analogues |
| KR102743950B1 (en) | 2015-05-07 | 2024-12-18 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrine macrolides |
| CN108601760A (en) | 2016-02-12 | 2018-09-28 | 卫材R&D管理有限公司 | Intermediate in the synthesis of eribulin and relevant synthetic method |
| 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 |
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2014
- 2014-12-05 ES ES14866945T patent/ES2723355T3/en active Active
- 2014-12-05 MX MX2016006891A patent/MX370611B/en active IP Right Grant
- 2014-12-05 US US14/562,086 patent/US9303039B2/en active Active
- 2014-12-05 MX MX2020004855A patent/MX2020004855A/en unknown
- 2014-12-05 RU RU2016124265A patent/RU2676486C1/en active
- 2014-12-05 BR BR112016012237-2A patent/BR112016012237B1/en active IP Right Grant
- 2014-12-05 CN CN201480066353.XA patent/CN105916861B/en active Active
- 2014-12-05 EP EP18209462.3A patent/EP3505520A1/en active Pending
- 2014-12-05 SG SG11201604545XA patent/SG11201604545XA/en unknown
- 2014-12-05 CA CA2931788A patent/CA2931788C/en active Active
- 2014-12-05 HU HUE14866945A patent/HUE043088T2/en unknown
- 2014-12-05 SG SG10201805024YA patent/SG10201805024YA/en unknown
- 2014-12-05 JP JP2016532033A patent/JP6443812B2/en active Active
- 2014-12-05 WO PCT/US2014/068834 patent/WO2015085193A1/en active Application Filing
- 2014-12-05 EP EP14866945.0A patent/EP3077399B1/en active 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
- 2016-05-26 MX MX2019011926A patent/MX2019011926A/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/en 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/en active Active
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2020
- 2020-04-01 IL IL273736A patent/IL273736B/en active IP Right Grant
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2021
- 2021-03-04 IL IL281275A patent/IL281275B/en unknown
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