IL260717B - Intermediates in the synthesis of eribulin and related methods of synthesis - Google Patents
Intermediates in the synthesis of eribulin and related methods of synthesisInfo
- Publication number
- IL260717B IL260717B IL260717A IL26071718A IL260717B IL 260717 B IL260717 B IL 260717B IL 260717 A IL260717 A IL 260717A IL 26071718 A IL26071718 A IL 26071718A IL 260717 B IL260717 B IL 260717B
- Authority
- IL
- Israel
- Prior art keywords
- eribulin
- intermediates
- synthesis
- synthetic methods
- related synthetic
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title 1
- UFNVPOGXISZXJD-XJPMSQCNSA-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-XJPMSQCNSA-N 0.000 title 1
- 229960003649 eribulin Drugs 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 238000010189 synthetic method Methods 0.000 title 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Materials For Photolithography (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662294538P | 2016-02-12 | 2016-02-12 | |
| PCT/US2017/017501 WO2017139664A1 (en) | 2016-02-12 | 2017-02-10 | Intermediates in the synthesis of eribulin and related methods of synthesis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL260717B true IL260717B (en) | 2020-10-29 |
Family
ID=59563582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL260717A IL260717B (en) | 2016-02-12 | 2018-07-22 | Intermediates in the synthesis of eribulin and related methods of synthesis |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US10676481B2 (https=) |
| EP (1) | EP3413887B1 (https=) |
| JP (1) | JP6786610B2 (https=) |
| KR (1) | KR20180107243A (https=) |
| CN (1) | CN108601760A (https=) |
| IL (1) | IL260717B (https=) |
| MX (1) | MX377663B (https=) |
| RU (1) | RU2732575C2 (https=) |
| SG (1) | SG11201806133UA (https=) |
| WO (1) | WO2017139664A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2522663T1 (sl) | 2004-06-03 | 2015-08-31 | Eisai R&D Management Co., Ltd. | Vmesne spojine za pripravo halihondrina B |
| BRPI0817909B1 (pt) | 2007-10-03 | 2022-06-21 | Eisai R&D Management Co., Ltd | Métodos de obtenção e de preparação de uma composição diastereomericamente pura, compostos, e método para produzir os referidos compostos |
| RU2579511C2 (ru) | 2010-01-26 | 2016-04-10 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Производные фуро[3,2-в]пирана, применимые в синтезе аналогов |
| BR112016009452B1 (pt) | 2013-11-04 | 2022-06-07 | Eisai R&D Management Co., Ltd | Métodos de preparar intermediários na síntese de eribulina, métodos de preparar eribulina e mesilato de eribulina, e compostos intermediários |
| EP3077399B1 (en) | 2013-12-06 | 2019-02-20 | Eisai R&D Management Co., Ltd. | Methods useful in the synthesis of halichondrin b analogs |
| MX392296B (es) | 2015-05-07 | 2025-03-24 | Eisai R&D Man Co Ltd | Reacciones de macrociclizacion e intermediarios y otros fragmentos utiles en la sintesis de macrolidos de halicondrina. |
| KR102404629B1 (ko) | 2016-06-30 | 2022-06-02 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 마크롤리드 및 그의 유사체의 합성에 유용한 프린스 반응 및 중간체 |
| IL275729B2 (en) | 2018-01-03 | 2023-09-01 | Eisai R&D Man Co Ltd | Prins reaction and compounds useful in the synthesis of helicondrin macrolides and their analogs |
| CN110568121A (zh) * | 2019-07-11 | 2019-12-13 | 山东省药学科学院 | 一种艾日布林及含艾日布林的制剂中有关物质的检测方法 |
| KR102377262B1 (ko) * | 2020-05-11 | 2022-03-22 | 연성정밀화학(주) | 결정성 에리불린 염 |
Family Cites Families (33)
| 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 | |
| AU4255697A (en) | 1996-09-06 | 1998-03-26 | Eli Lilly And Company | Catalytic selective sulfonylation process |
| US6870058B2 (en) | 1996-12-03 | 2005-03-22 | The Trustees Of The University Of Pennsylvania | Compounds which mimic the chemical and biological properties of discodermolide |
| JP4454151B2 (ja) | 1998-06-17 | 2010-04-21 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 大環状類似体及びそれらの使用並びに調製方法 |
| US6653341B1 (en) | 1998-06-17 | 2003-11-25 | Eisai Co., Ltd. | Methods and compositions for use in treating cancer |
| US8097648B2 (en) | 1998-06-17 | 2012-01-17 | Eisai R&D Management Co., Ltd. | Methods and compositions for use in treating cancer |
| DE10106647A1 (de) | 2001-02-12 | 2002-08-22 | Univ Hannover | Ratjadon-Derivate zum Hemmen des Zellwachstums |
| SI2522663T1 (sl) | 2004-06-03 | 2015-08-31 | Eisai R&D Management Co., Ltd. | Vmesne spojine za pripravo halihondrina B |
| US20060045846A1 (en) | 2004-08-30 | 2006-03-02 | Horstmann Thomas E | Reagents and methods for labeling terminal olefins |
| US20060154312A1 (en) | 2004-12-09 | 2006-07-13 | Sergei Agoulnik | Tubulin isotype screening in cancer therapy using halichondrin B analogs |
| JP2009510005A (ja) | 2005-09-26 | 2009-03-12 | シムライズ・ゲゼルシヤフト・ミツト・ベシユレンクテル・ハフツング・ウント・コンパニー・コマンジツト・ゲゼルシヤフト | 分子内プリンス反応および該反応に適する触媒 |
| 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 |
| BRPI0817909B1 (pt) * | 2007-10-03 | 2022-06-21 | Eisai R&D Management Co., Ltd | Métodos de obtenção e de preparação de uma composição diastereomericamente pura, compostos, e método para produzir os referidos compostos |
| CN101910180A (zh) | 2007-11-16 | 2010-12-08 | 卫材R&D管理有限公司 | 用于软海绵素b类似物合成的新颖中间体和用于该中间体的新颖脱磺酰化反应 |
| CA2720632C (en) | 2008-04-04 | 2016-12-20 | Eisai R&D Management Co., Ltd. | Halichondrin b analogs |
| 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 |
| RU2579511C2 (ru) | 2010-01-26 | 2016-04-10 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Производные фуро[3,2-в]пирана, применимые в синтезе аналогов |
| WO2012147900A1 (en) * | 2011-04-28 | 2012-11-01 | Eisai R&D Management Co., Ltd. | Microreactor process for halichondrin b analog synthesis |
| WO2013078559A1 (en) | 2011-11-30 | 2013-06-06 | Alphora Research Inc. | Process for preparation of (3r)-2,4-di-leaving group-3-methylbut-1-ene |
| US9278979B2 (en) | 2012-03-30 | 2016-03-08 | Alphora Research Inc. | Synthetic process for preparation of macrocyclic C1-keto analogs of halichondrin B and intermediates useful therein |
| EP3016957A4 (en) | 2013-07-03 | 2016-11-30 | Alphora Res Inc | SYNTHETIC METHOD FOR THE PRODUCTION OF CYCLIC C1-KETO ANALOGUE OF HALICHONDRIN B AND USEFUL INTERMEDIATE PRODUCTS, INCLUDING INTERMEDIATE PRODUCTS WITH -SO2- (P-TOLYL) GROUPS |
| BR112016009452B1 (pt) | 2013-11-04 | 2022-06-07 | Eisai R&D Management Co., Ltd | Métodos de preparar intermediários na síntese de eribulina, métodos de preparar eribulina e mesilato de eribulina, e compostos intermediários |
| EP3077399B1 (en) | 2013-12-06 | 2019-02-20 | Eisai R&D Management Co., Ltd. | Methods useful in the synthesis of halichondrin b analogs |
| US10208058B2 (en) | 2014-09-09 | 2019-02-19 | Cipla Limited | Process for the preparation of macrocyclic ketone analogs of halichondrin B or pharmaceutically acceptable salts and intermediates thereof |
| MX392296B (es) | 2015-05-07 | 2025-03-24 | Eisai R&D Man Co Ltd | Reacciones de macrociclizacion e intermediarios y otros fragmentos utiles en la sintesis de macrolidos de halicondrina. |
| KR102404629B1 (ko) | 2016-06-30 | 2022-06-02 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 마크롤리드 및 그의 유사체의 합성에 유용한 프린스 반응 및 중간체 |
| WO2018217894A1 (en) | 2017-05-24 | 2018-11-29 | Eisai R&D Management Co., Ltd. | Fluorine-labelled halichondrin derivatives and related methods of synthesis |
| IL275729B2 (en) | 2018-01-03 | 2023-09-01 | Eisai R&D Man Co Ltd | Prins reaction and compounds useful in the synthesis of helicondrin macrolides and their analogs |
-
2017
- 2017-02-10 CN CN201780010903.XA patent/CN108601760A/zh active Pending
- 2017-02-10 EP EP17750887.6A patent/EP3413887B1/en active Active
- 2017-02-10 WO PCT/US2017/017501 patent/WO2017139664A1/en not_active Ceased
- 2017-02-10 JP JP2018539136A patent/JP6786610B2/ja not_active Expired - Fee Related
- 2017-02-10 KR KR1020187025945A patent/KR20180107243A/ko not_active Withdrawn
- 2017-02-10 RU RU2018132264A patent/RU2732575C2/ru active
- 2017-02-10 MX MX2018009794A patent/MX377663B/es active IP Right Grant
- 2017-02-10 US US16/076,028 patent/US10676481B2/en not_active Expired - Fee Related
- 2017-02-10 SG SG11201806133UA patent/SG11201806133UA/en unknown
-
2018
- 2018-07-22 IL IL260717A patent/IL260717B/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| EP3413887A1 (en) | 2018-12-19 |
| CN108601760A (zh) | 2018-09-28 |
| JP2019504839A (ja) | 2019-02-21 |
| EP3413887A4 (en) | 2019-08-14 |
| US20190300542A1 (en) | 2019-10-03 |
| RU2018132264A3 (https=) | 2020-04-15 |
| RU2018132264A (ru) | 2020-03-12 |
| KR20180107243A (ko) | 2018-10-01 |
| JP6786610B2 (ja) | 2020-11-18 |
| SG11201806133UA (en) | 2018-08-30 |
| RU2732575C2 (ru) | 2020-09-21 |
| EP3413887B1 (en) | 2021-04-07 |
| MX2018009794A (es) | 2018-12-17 |
| WO2017139664A8 (en) | 2018-07-26 |
| MX377663B (es) | 2025-03-11 |
| WO2017139664A1 (en) | 2017-08-17 |
| US10676481B2 (en) | 2020-06-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted |