EA200900793A1 - Способ получения эзетимиба и его производных - Google Patents
Способ получения эзетимиба и его производныхInfo
- 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
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.
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) | CN101679236B (ru) |
EA (1) | EA017349B1 (ru) |
WO (1) | WO2008089984A2 (ru) |
Families Citing this family (27)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HU0501164D0 (en) * | 2005-12-20 | 2006-02-28 | Richter Gedeon Vegyeszet | 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 |
SI2413911T1 (sl) | 2009-03-31 | 2014-04-30 | Krka, D.D., Novo Mesto | Progresivna emulzijska kristalizacija |
CA2757722C (en) | 2009-04-01 | 2018-05-22 | Matrix Laboratories Ltd. | 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. |
CA2797458A1 (en) * | 2010-06-07 | 2011-12-15 | Telik, Inc. | Tablet formulation of ezatiostat |
US8841476B2 (en) | 2010-06-07 | 2014-09-23 | Telik, Inc. | Preparation of crystalline ezatiostat hydrochloride ansolvate form D |
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2160125T3 (es) | 1993-07-09 | 2001-11-01 | Schering Corp | Proceso para la sintesis de azetidinonas. |
US5631365A (en) * | 1993-09-21 | 1997-05-20 | Schering Corporation | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
EP1169468B1 (en) | 1999-04-05 | 2012-03-14 | 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 |
JP2007526251A (ja) * | 2004-12-03 | 2007-09-13 | テバ ファーマシューティカル インダストリーズ リミティド | エゼチミベ多形体 |
US20060234996A1 (en) * | 2005-04-14 | 2006-10-19 | Itai Adin | Novel crystalline form of ezetimibe and processes for the preparation thereof |
WO2006137080A1 (en) * | 2005-06-22 | 2006-12-28 | Manne Satyanarayana Reddy | Improved process for the preparation of ezetimibe |
KR20070063592A (ko) * | 2005-09-08 | 2007-06-19 | 테바 파마슈티컬 인더스트리즈 리미티드 | 에제티밉의 합성을 위한 중간체인(3r,4s)-4-((4-벤질옥시)페닐)-1-(4-플루오로페닐)-3-((s)-3-(4-플루오로페닐)-3-히드록시프로필)-2-아제티디논의제조 방법 |
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 |
-
2008
- 2008-01-24 WO PCT/EP2008/000546 patent/WO2008089984A2/en active Search and Examination
- 2008-01-24 EP EP08707257A patent/EP2125715A2/en not_active Withdrawn
- 2008-01-24 CN CN2008800075049A patent/CN101679236B/zh not_active Expired - Fee Related
- 2008-01-24 US US12/524,346 patent/US20130190487A1/en not_active Abandoned
- 2008-01-24 CN CN201110171600.0A patent/CN102285906B/zh not_active Expired - Fee Related
- 2008-01-24 EA EA200900793A patent/EA017349B1/ru not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
WO2008089984A3 (en) | 2008-09-18 |
US20130190487A1 (en) | 2013-07-25 |
CN102285906B (zh) | 2014-11-19 |
EA017349B1 (ru) | 2012-11-30 |
CN101679236A (zh) | 2010-03-24 |
CN102285906A (zh) | 2011-12-21 |
EP2125715A2 (en) | 2009-12-02 |
WO2008089984A2 (en) | 2008-07-31 |
CN101679236B (zh) | 2013-03-06 |
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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 |