EA200900793A1 - Способ получения эзетимиба и его производных - Google Patents

Способ получения эзетимиба и его производных

Info

Publication number
EA200900793A1
EA200900793A1 EA200900793A EA200900793A EA200900793A1 EA 200900793 A1 EA200900793 A1 EA 200900793A1 EA 200900793 A EA200900793 A EA 200900793A EA 200900793 A EA200900793 A EA 200900793A EA 200900793 A1 EA200900793 A1 EA 200900793A1
Authority
EA
Eurasian Patent Office
Prior art keywords
ezetimibe
derivatives
intermediates
obtaining
producing
Prior art date
Application number
EA200900793A
Other languages
English (en)
Other versions
EA017349B1 (ru
Inventor
Антон Стимац
Барбара Мохар
Мишель Стефан
Мойца Бевц
Рок Зупет
Андрей Гартнер
Весна Кросель
Матей Смрколь
Давор Кидемет
Грегор Седмак
Примоз Бенкиц
Ален Кляйиц
Миха Плевник
Original Assignee
Крка
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from EP07001537A external-priority patent/EP1953140A1/en
Application filed by Крка filed Critical Крка
Publication of EA200900793A1 publication Critical patent/EA200900793A1/ru
Publication of EA017349B1 publication Critical patent/EA017349B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Настоящее изобретение относится к способу получения эзетимиба, в частности к новым промежуточным соединениям для его синтеза, и улучшенному способу получения таких промежуточных соединений. Указанные промежуточные соединения можно получать с высокими выходами экономичным способом. Настоящее изобретение также относится к новой кристаллической форме эзетимиба.
EA200900793A 2007-01-24 2008-01-24 Способ получения эзетимиба и его производных EA017349B1 (ru)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
EP07001537A EP1953140A1 (en) 2007-01-24 2007-01-24 Process for the preparation of ezetimibe and derivatives thereof
EP07015107 2007-08-01
EP07020070 2007-10-12
EP07023686 2007-12-06
EP07024430 2007-12-17
PCT/EP2008/000546 WO2008089984A2 (en) 2007-01-24 2008-01-24 Process for the preparation of ezetimibe and derivatives thereof

Publications (2)

Publication Number Publication Date
EA200900793A1 true EA200900793A1 (ru) 2009-12-30
EA017349B1 EA017349B1 (ru) 2012-11-30

Family

ID=39301774

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200900793A EA017349B1 (ru) 2007-01-24 2008-01-24 Способ получения эзетимиба и его производных

Country Status (5)

Country Link
US (1) US20130190487A1 (ru)
EP (1) EP2125715A2 (ru)
CN (2) CN102285906B (ru)
EA (1) EA017349B1 (ru)
WO (1) WO2008089984A2 (ru)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUP0501164A2 (en) * 2005-12-20 2007-07-30 Richter Gedeon Nyrt New industrial process for the production of ezetimibe
CZ2007843A3 (cs) * 2007-11-30 2009-06-10 Zentiva, A. S. Zpusob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu a jeho meziprodukty
EP2965752A1 (en) 2007-12-10 2016-01-13 ratiopharm GmbH Pharmaceutical formulation comprising ezetimibe
WO2010112222A1 (en) 2009-03-31 2010-10-07 Krka, D.D., Novo Mesto Progressive emulsion crystallization
US9388440B2 (en) 2009-04-01 2016-07-12 Mylan Laboratories Limited Enzymatic process for the preparation of (S)-5-(4-fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one, an intermediate of Ezetimibe and further conversion to Ezetimibe
TR200904500A2 (tr) 2009-06-10 2009-10-21 Öner Levent Ezetimib nanokristallerinin hazırlanması için yöntem ve farmasötik formülasyonları.
JP2013528214A (ja) 2010-06-07 2013-07-08 テリック，インコーポレイテッド 結晶性エザチオスタット塩酸塩非溶媒和物ｄ型の調製
EP2576591A2 (en) * 2010-06-07 2013-04-10 Telik, Inc. Tablet formulation of ezatiostat
CN102477008B (zh) * 2010-11-22 2014-05-21 沈阳药科大学 依泽替米贝的合成方法
CN102731489B (zh) * 2011-04-11 2016-10-26 天津药物研究院有限公司 一种依折麦布关键中间体的制备方法
WO2012155932A1 (en) 2011-05-17 2012-11-22 Pharmathen S.A. Improved process for the preparation of ezetimibe
CN102952055A (zh) * 2011-08-16 2013-03-06 凯瑞斯德生化(苏州)有限公司 一种依泽替米贝和其中间体的制备方法
TWI605045B (zh) * 2013-01-14 2017-11-11 杜邦股份有限公司 殺線蟲磺醯胺之製備
CN104059009A (zh) * 2013-03-21 2014-09-24 四川金辉药业有限公司 一种依折麦布重要中间体的合成方法
WO2015039675A1 (en) 2013-09-23 2015-03-26 Pharmathen S.A. Novel process for the preparation of ezetimibe intermediates
KR20150079373A (ko) * 2013-12-30 2015-07-08 한미약품 주식회사 에제티미브 및 로수바스타틴을 포함하는 경구용 복합제제
CN103755616A (zh) * 2013-12-31 2014-04-30 北京万全德众医药生物技术有限公司 一种制备依泽替米贝异构体的方法
CN105294426B (zh) * 2014-06-09 2019-05-14 浙江海正药业股份有限公司 氮杂环丁酮化合物制备方法及其中间体
CN105330579B (zh) * 2014-08-08 2019-08-30 杭州雷索药业有限公司 依泽替米贝及其衍生物在治疗或预防癫痫中的应用
CN104860862A (zh) * 2015-04-09 2015-08-26 浙江普洛得邦制药有限公司 一种依折麦布及其中间体的合成方法
CN104940153A (zh) * 2015-07-23 2015-09-30 青岛蓝盛洋医药生物科技有限责任公司 一种治疗高血脂症的药物依折麦布组合物片剂
CN104958261A (zh) * 2015-08-05 2015-10-07 青岛蓝盛洋医药生物科技有限责任公司 一种治疗心脑血管疾病的药物依折麦布组合物干混悬剂
CN105541690B (zh) * 2015-12-16 2018-08-21 江苏恒盛药业有限公司 一种氮杂环丁酮衍生物的制备方法
CN105503686A (zh) * 2015-12-31 2016-04-20 安徽美诺华药物化学有限公司 一种依替米贝的合成方法
CN109810038A (zh) * 2019-01-18 2019-05-28 南通常佑药业科技有限公司 一种丙内酰胺类降血脂药物依泽替米贝的制备方法
CN110420180A (zh) * 2019-07-24 2019-11-08 西北农林科技大学 一种含有维生素e的纳米乳药物及其制备方法
CN112409212B (zh) * 2020-11-30 2023-03-14 四川新迪医药化工有限公司 西酞普兰二醇中间体氢溴酸盐的制备方法及西酞普兰二醇中间体氢溴酸盐、西酞普兰

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2840452B2 (ja) 1993-07-09 1998-12-24 シェリング・コーポレーション アゼチジノンの合成方法
US5631365A (en) * 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
WO2000060107A1 (en) 1999-04-05 2000-10-12 Schering Corporation Stereoselective microbial reduction for the preparation of 1 - (4-fluorophenyl) - 3(r)-[3(s) - hydroxy-3 - (4-fluorophenyl) propyl)]-4(s) - (4-hydroxyphenyl)-2-azetidinone
WO2005009955A1 (en) * 2003-07-31 2005-02-03 Hetero Drugs Limited Ezetimibe polymorphs
WO2005062897A2 (en) * 2003-12-23 2005-07-14 Dr. Reddy's Laboratories Ltd. Polymorphs of ezetimibe and processes for the preparation thereof
WO2006060808A1 (en) * 2004-12-03 2006-06-08 Teva Pharmaceutical Industries Ltd. Ezetimibe polymorphs
US20060234996A1 (en) * 2005-04-14 2006-10-19 Itai Adin Novel crystalline form of ezetimibe and processes for the preparation thereof
EP1893570A4 (en) * 2005-06-22 2009-12-23 Reddy Manne Satynarayana IMPROVED PROCESS FOR THE PREPARATION OF EZETIMIBE
MX2007005493A (es) * 2005-09-08 2007-09-11 Teva Pharma Procesos para la preparacion de (3r,4s)-4-((4-benciloxi)fenil)-1- (4-fluorofenil)-3-((s)-3-(4-fluorofenil)-3-hidroxipropil-2- azetidinona, un intermedio para la sintesis de ezetimibe.
WO2007108007A1 (en) * 2006-03-23 2007-09-27 Unichem Laboratories Limited A process for the preparation of ezetimibe via a novel intermediate
CN100564357C (zh) * 2006-10-20 2009-12-02 浙江天宇药业有限公司 一种氮杂环丁酮衍生物及其合成方法

Also Published As

Publication number Publication date
CN102285906B (zh) 2014-11-19
CN101679236B (zh) 2013-03-06
EP2125715A2 (en) 2009-12-02
WO2008089984A3 (en) 2008-09-18
CN102285906A (zh) 2011-12-21
EA017349B1 (ru) 2012-11-30
US20130190487A1 (en) 2013-07-25
WO2008089984A2 (en) 2008-07-31
CN101679236A (zh) 2010-03-24

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU