IN2014MN02106A - - Google Patents
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- Publication number
- IN2014MN02106A IN2014MN02106A IN2106MUN2014A IN2014MN02106A IN 2014MN02106 A IN2014MN02106 A IN 2014MN02106A IN 2106MUN2014 A IN2106MUN2014 A IN 2106MUN2014A IN 2014MN02106 A IN2014MN02106 A IN 2014MN02106A
- Authority
- IN
- India
- Prior art keywords
- compound
- formula
- disclosed
- preparation
- pharmaceutically acceptable
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 4
- 238000000034 method Methods 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229930195695 Halichondrin Natural products 0.000 abstract 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 abstract 1
- 229960003649 eribulin Drugs 0.000 abstract 1
- 239000000543 intermediate Substances 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D307/20—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- 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
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Furan Compounds (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261618004P | 2012-03-30 | 2012-03-30 | |
| US201261647127P | 2012-05-15 | 2012-05-15 | |
| PCT/CA2013/050254 WO2013142999A1 (en) | 2012-03-30 | 2013-03-28 | Synthetic process for preparation of macrocyclic c1-keto analogs of halichondrin b and intermediates useful therein |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IN2014MN02106A true IN2014MN02106A (enEXAMPLES) | 2015-09-11 |
Family
ID=49258019
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IN2106MUN2014 IN2014MN02106A (enEXAMPLES) | 2012-03-30 | 2013-03-28 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US9278979B2 (enEXAMPLES) |
| EP (1) | EP2831082B1 (enEXAMPLES) |
| JP (1) | JP6531911B2 (enEXAMPLES) |
| CN (1) | CN104334562A (enEXAMPLES) |
| AU (1) | AU2013239290B2 (enEXAMPLES) |
| CA (1) | CA2868627C (enEXAMPLES) |
| IN (1) | IN2014MN02106A (enEXAMPLES) |
| WO (1) | WO2013142999A1 (enEXAMPLES) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101434673B1 (ko) | 2004-06-03 | 2014-08-26 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 ｂ 유사체의 제조를 위한 중간체 |
| EP2200992B1 (en) | 2007-10-03 | 2014-02-26 | Eisai R&D Management Co., Ltd. | Intermediates and methods for the synthesis of halichondrin b analogs |
| JP5800834B2 (ja) | 2010-01-26 | 2015-10-28 | 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 |
| CN104053645A (zh) | 2011-11-30 | 2014-09-17 | 阿方拉研究股份有限公司 | 用于制备(3r)-2,4-二-离去基团-3-甲基丁-1-烯的工艺 |
| WO2013086634A1 (en) | 2011-12-16 | 2013-06-20 | Alphora Research Inc. | Process for preparation of 3-((2s,5s)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl) propanol derivatives and intermediates useful thereof |
| WO2013097042A1 (en) | 2011-12-29 | 2013-07-04 | Alphora Research Inc. | 2-((2s,3s,4r,5r)-5-((s)-3-amino-2-hydroxyprop-1-yl)-4-methoxy-3-(phenylsulfonylmethyl)tetrahydrofuran-2-yl)acetaldehyde derivatives and process for their preparation |
| 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 |
| CN103483352A (zh) * | 2013-10-18 | 2014-01-01 | 李友香 | 抗肿瘤的药用原料药 |
| 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 |
| SG10201805024YA (en) | 2013-12-06 | 2018-07-30 | Eisai R&D Man Co Ltd | Methods useful in the synthesis of halichondrin b analogs |
| TW201617326A (zh) * | 2014-03-06 | 2016-05-16 | Ａｌｐｈｏｒａ研發股份有限公司 | （ｓ）－１－（（２ｒ，３ｒ，４ｓ，５ｓ）－５－烯丙－３－甲氧－４－（對甲苯磺醯甲基）四氫呋喃－２－基）－３－氨基丙－２－醇之結晶衍生物 |
| US10556910B2 (en) | 2014-06-30 | 2020-02-11 | President And Fellows Of Harvard College | Synthesis of halichondrin analogs and uses thereof |
| CN105713031B (zh) * | 2014-12-05 | 2021-05-07 | 正大天晴药业集团股份有限公司 | 一种用于制备艾日布林的中间体及其制备方法 |
| US10344038B2 (en) | 2015-04-30 | 2019-07-09 | President And Fellows Of Harvard College | Chromium-mediated coupling and application to the synthesis of halichondrins |
| CN107849057B (zh) * | 2015-05-07 | 2020-11-10 | 卫材R&D管理有限公司 | 用于合成软海绵素大环内酯的大环化反应及中间体和其他片段 |
| KR20180107243A (ko) | 2016-02-12 | 2018-10-01 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 에리불린의 합성에서의 중간체 및 관련된 합성 방법 |
| CA3013791A1 (en) | 2016-03-02 | 2017-09-08 | Eisai R&D Management Co., Ltd. | Eribulin-based antibody-drug conjugates and methods of use |
| JP2019521969A (ja) * | 2016-05-26 | 2019-08-08 | ドクター レディズ ラボラトリーズ リミテッド | エリブリン及びその中間体の製造方法 |
| 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 |
| KR20190084065A (ko) | 2016-11-23 | 2019-07-15 | 닥터 레디스 레보러터리즈 리미티드 | 에리불린 및 그 중간체의 제조방법 |
| 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 |
| US9938288B1 (en) | 2017-04-05 | 2018-04-10 | President And Fellows Of Harvard College | Macrocyclic compound and uses thereof |
| PT3606928T (pt) | 2017-04-05 | 2022-12-05 | Harvard College | Composto macrocíclico e utilizações deste |
| 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 |
| WO2018217894A1 (en) * | 2017-05-24 | 2018-11-29 | Eisai R&D Management Co., Ltd. | Fluorine-labelled halichondrin derivatives and related methods of synthesis |
| MX2020000142A (es) * | 2017-07-06 | 2020-07-22 | Harvard College | Sintesis de halicondrinas. |
| US11498892B2 (en) | 2017-07-06 | 2022-11-15 | President And Fellows Of Harvard College | Fe/Cu-mediated ketone synthesis |
| EP4403560A3 (en) | 2017-11-15 | 2024-10-23 | President And Fellows Of Harvard College | Macrocyclic compounds and uses thereof |
| WO2019136145A1 (en) * | 2018-01-03 | 2019-07-11 | Eisai R&D Management Co., Ltd. | Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof |
| IL279168B (en) | 2020-12-02 | 2022-04-01 | Finetech Pharmaceutical Ltd | A process for the preparation of eribulin |
| CN114213429B (zh) * | 2021-12-22 | 2023-06-20 | 苏州正济药业有限公司 | 一种甲磺酸艾立布林杂质的制备方法 |
| AU2024209545A1 (en) * | 2023-01-17 | 2025-08-07 | Systimmune, Inc. | Conjugate of eribulin drug |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| RU2153491C2 (ru) | 1993-07-09 | 2000-07-27 | Лаборатуар Терамекс С.А. | Аналоги витамина d, соединения, способы их получения и фармацевтическая композиция |
| EP2272840B1 (en) * | 1998-06-17 | 2012-08-22 | Eisai R&D Management Co., Ltd. | Intermediate compound for the preparation of halichondrin analogs |
| US7001982B2 (en) | 2003-03-31 | 2006-02-21 | Council Of Scientific And Industrial Research | Non-natural C-linked carbo-β-peptides with robust secondary structures |
| KR101434673B1 (ko) | 2004-06-03 | 2014-08-26 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 할리콘드린 ｂ 유사체의 제조를 위한 중간체 |
| US20060045846A1 (en) * | 2004-08-30 | 2006-03-02 | Horstmann Thomas E | Reagents and methods for labeling terminal olefins |
| US8598373B2 (en) | 2008-04-04 | 2013-12-03 | Eisai R&D Management Co., Ltd. | Halichondrin B analogs |
| CN104053645A (zh) | 2011-11-30 | 2014-09-17 | 阿方拉研究股份有限公司 | 用于制备(3r)-2,4-二-离去基团-3-甲基丁-1-烯的工艺 |
| WO2013086634A1 (en) | 2011-12-16 | 2013-06-20 | Alphora Research Inc. | Process for preparation of 3-((2s,5s)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl) propanol derivatives and intermediates useful thereof |
| WO2013097042A1 (en) * | 2011-12-29 | 2013-07-04 | Alphora Research Inc. | 2-((2s,3s,4r,5r)-5-((s)-3-amino-2-hydroxyprop-1-yl)-4-methoxy-3-(phenylsulfonylmethyl)tetrahydrofuran-2-yl)acetaldehyde derivatives and process for their preparation |
| CA2909209A1 (en) | 2013-05-15 | 2014-11-20 | Alphora Research Inc. | 3-((2s,5s)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivatives, their preparation and intermediates useful thereof |
-
2013
- 2013-03-28 IN IN2106MUN2014 patent/IN2014MN02106A/en unknown
- 2013-03-28 EP EP13769493.1A patent/EP2831082B1/en not_active Not-in-force
- 2013-03-28 WO PCT/CA2013/050254 patent/WO2013142999A1/en active Application Filing
- 2013-03-28 AU AU2013239290A patent/AU2013239290B2/en not_active Ceased
- 2013-03-28 US US14/389,439 patent/US9278979B2/en not_active Expired - Fee Related
- 2013-03-28 JP JP2015502027A patent/JP6531911B2/ja not_active Expired - Fee Related
- 2013-03-28 CA CA2868627A patent/CA2868627C/en active Active
- 2013-03-28 CN CN201380028907.2A patent/CN104334562A/zh active Pending
-
2016
- 2016-02-04 US US15/015,161 patent/US9695187B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| AU2013239290B2 (en) | 2017-08-03 |
| EP2831082A4 (en) | 2016-01-06 |
| JP2015512897A (ja) | 2015-04-30 |
| CA2868627C (en) | 2021-02-16 |
| US9695187B2 (en) | 2017-07-04 |
| AU2013239290A1 (en) | 2014-10-30 |
| WO2013142999A1 (en) | 2013-10-03 |
| US20160152631A1 (en) | 2016-06-02 |
| US9278979B2 (en) | 2016-03-08 |
| CA2868627A1 (en) | 2013-10-03 |
| EP2831082A1 (en) | 2015-02-04 |
| US20150065733A1 (en) | 2015-03-05 |
| EP2831082B1 (en) | 2019-02-20 |
| JP6531911B2 (ja) | 2019-06-19 |
| CN104334562A (zh) | 2015-02-04 |
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