PT906278E - Sintese enantioselectiva de azetidinonas baseada na 3-hidroxi-gama-lactona - Google Patents

Sintese enantioselectiva de azetidinonas baseada na 3-hidroxi-gama-lactona

Info

Publication number
PT906278E
PT906278E PT97928831T PT97928831T PT906278E PT 906278 E PT906278 E PT 906278E PT 97928831 T PT97928831 T PT 97928831T PT 97928831 T PT97928831 T PT 97928831T PT 906278 E PT906278 E PT 906278E
Authority
PT
Portugal
Prior art keywords
azetidinonas
gama
lactone
hydroxy
enantioselective synthesis
Prior art date
Application number
PT97928831T
Other languages
English (en)
Inventor
Xing Chen
Yee-Shing Wong
Guang-Zhong Wu
Doris P Schumacher
Martin Steinman
Original Assignee
Schering Corp
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
Application filed by Schering Corp filed Critical Schering Corp
Publication of PT906278E publication Critical patent/PT906278E/pt

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
    • A61P3/06—Antihyperlipidemics

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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
PT97928831T 1996-05-31 1997-05-28 Sintese enantioselectiva de azetidinonas baseada na 3-hidroxi-gama-lactona PT906278E (pt)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/655,785 US5739321A (en) 1996-05-31 1996-05-31 3-hydroxy γ-lactone based enantionselective synthesis of azetidinones

Publications (1)

Publication Number Publication Date
PT906278E true PT906278E (pt) 2003-01-31

Family

ID=24630339

Family Applications (1)

Application Number Title Priority Date Filing Date
PT97928831T PT906278E (pt) 1996-05-31 1997-05-28 Sintese enantioselectiva de azetidinonas baseada na 3-hidroxi-gama-lactona

Country Status (14)

Country Link
US (1) US5739321A (pt)
EP (1) EP0906278B1 (pt)
JP (1) JP3155759B2 (pt)
AR (1) AR007314A1 (pt)
AT (1) ATE226191T1 (pt)
AU (1) AU3299497A (pt)
CA (1) CA2255662C (pt)
CO (1) CO4770966A1 (pt)
DE (1) DE69716426T2 (pt)
DK (1) DK0906278T3 (pt)
ES (1) ES2185026T3 (pt)
PT (1) PT906278E (pt)
WO (1) WO1997045406A1 (pt)
ZA (1) ZA974678B (pt)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
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US5631365A (en) * 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
US5886171A (en) * 1996-05-31 1999-03-23 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
US6207822B1 (en) 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
AR025144A1 (es) * 1998-12-07 2002-11-13 Schering Corp Proceso para preparar azetidinonas, proceso para preparar compuestos intermediarios asi como dichos compuestos intermediarios
ATE349425T1 (de) * 2000-12-21 2007-01-15 Sanofi Aventis Deutschland Neue diphenzylazetidinone, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung zur behandlung von lipidstoffwechselstörungen
US20060287254A1 (en) * 2001-01-26 2006-12-21 Schering Corporation Use of substituted azetidinone compounds for the treatment of sitosterolemia
ES2290562T3 (es) * 2001-01-26 2008-02-16 Schering Corporation Combinaciones del activador del receptor activado por el proliferador de los peroxisomas (ppar) fenofibrato con el inhibidor de la absorcion de esteroles ezetimiba para indicaciones vasculares.
WO2002079174A2 (en) 2001-03-28 2002-10-10 Schering Corporation Enantioselective synthesis of azetidinone intermediate compounds
EP1429756B1 (en) * 2001-09-21 2006-11-22 Schering Corporation Treatment of xanthoma with azetidinone derivatives as sterol absorption inhibitors
US20030204096A1 (en) * 2002-03-25 2003-10-30 Schering Corporation Enantioselective synthesis of azetidinone intermediate compounds
US7176193B2 (en) 2002-06-19 2007-02-13 Sanofi-Aventis Deutschland Gmbh Acid-group-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use
US7176194B2 (en) 2002-06-19 2007-02-13 Sanofi-Aventis Deutschland Gmbh Ring-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use
US7671047B2 (en) 2002-06-19 2010-03-02 Sanofi-Aventis Deutschland Gmbh Cationically substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use
GB0215579D0 (en) * 2002-07-05 2002-08-14 Astrazeneca Ab Chemical compounds
US7135556B2 (en) * 2002-07-19 2006-11-14 Schering Corporation NPC1L1 (NPC3) and methods of use thereof
US7208486B2 (en) * 2003-03-07 2007-04-24 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
WO2004081002A1 (en) 2003-03-07 2004-09-23 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
US7459442B2 (en) * 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
AR041089A1 (es) 2003-05-15 2005-05-04 Merck & Co Inc Procedimiento y composiciones farmaceutiicas para tratar aterosclerosis, dislipidemias y afecciones relacionadas
WO2005009955A1 (en) * 2003-07-31 2005-02-03 Hetero Drugs Limited Ezetimibe polymorphs
WO2005049592A1 (en) 2003-11-24 2005-06-02 Hetero Drugs Limited A novel process for ezetimibe intermediate
GB0329778D0 (en) * 2003-12-23 2004-01-28 Astrazeneca Ab Chemical compounds
US7871998B2 (en) * 2003-12-23 2011-01-18 Astrazeneca Ab Diphenylazetidinone derivatives possessing cholesterol absorption inhibitory activity
WO2005069900A2 (en) * 2004-01-16 2005-08-04 Merck & Co., Inc. Npc1l1 (npc3) and methods of identifying ligands thereof
US20060211752A1 (en) 2004-03-16 2006-09-21 Kohn Leonard D Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression
US20070244107A1 (en) * 2004-08-25 2007-10-18 Waters M Gerard Method of Treating Atherosclerosis, Dyslipidemias and Related Conditions
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
WO2007001975A1 (en) * 2005-06-20 2007-01-04 Schering Corporation Piperidine derivatives useful as histamine h3 antagonists
AR054482A1 (es) * 2005-06-22 2007-06-27 Astrazeneca Ab Derivados de azetidinona para el tratamiento de hiperlipidemias
SA06270191B1 (ar) * 2005-06-22 2010-03-29 استرازينيكا ايه بي مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم
US20070049748A1 (en) * 2005-08-26 2007-03-01 Uppala Venkata Bhaskara R 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.
WO2007048027A2 (en) 2005-10-21 2007-04-26 Novartis Ag Combination of a renin-inhibitor and an anti-dyslipidemic agent and/or an antiobesity agent
HUP0501164A2 (en) * 2005-12-20 2007-07-30 Richter Gedeon Nyrt New industrial process for the production of ezetimibe
CA2634648A1 (en) * 2005-12-22 2007-10-25 Medichem, S.A. Processes for preparing intermediate compounds useful for the preparation of ezetimibe
EP1986489A2 (en) * 2006-02-24 2008-11-05 Schering Corporation Npc1l1 orthologues
WO2007108007A1 (en) * 2006-03-23 2007-09-27 Unichem Laboratories Limited A process for the preparation of ezetimibe via a novel intermediate
EP2007718A2 (en) * 2006-03-29 2008-12-31 Medichem, S.A. Processes for preparing ezetimibe and intermediate compounds useful for the preparation thereof
TW200811098A (en) * 2006-04-27 2008-03-01 Astrazeneca Ab Chemical compounds
JP2009503119A (ja) * 2006-08-29 2009-01-29 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 （３ｒ，４ｓ）−４−（４−ヒドロキシ保護−フェニル）−１−（４−フルオロフェニル）−３−［３−（４−フルオロフェニル）−３−オキソプロピル］アゼチジン−２−オンを精製する方法
WO2008030382A1 (en) * 2006-09-05 2008-03-13 Schering Corporation Pharmaceutical combinations for lipid management and in the treatment of atherosclerosis and hepatic steatosis
WO2008032338A2 (en) * 2006-09-11 2008-03-20 Manne Satyanarayana Reddy Improved process for the preparation of ezetimibe and its intermediates
CA2668371A1 (en) * 2006-11-02 2008-05-15 Merck & Co., Inc. Heterocyclyl-substituted anti-hypercholesterolemic compounds
US20090047716A1 (en) * 2007-06-07 2009-02-19 Nurit Perlman Reduction processes for the preparation of ezetimibe
US20080319221A1 (en) 2007-06-22 2008-12-25 Bernd Junker Esters of Pentahydroxyhexylcarbamoyl Alkanoic Acids
DE102007054497B3 (de) 2007-11-13 2009-07-23 Sanofi-Aventis Deutschland Gmbh Neue kristalline Diphenylazetidinonhydrate und Verfahren zu deren Herstellung
CZ305066B6 (cs) * 2008-02-25 2015-04-22 Zentiva, K.S. Způsob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu
EP2128133A1 (en) * 2008-05-26 2009-12-02 Lek Pharmaceuticals D.D. Ezetimibe process and composition
PL387331A1 (pl) 2009-02-24 2010-08-30 Instytut Chemii Organicznej Polskiej Akademii Nauk Sposób wytwarzania aldehydowego związku beta-laktamowego, związek pośredni, sposób wytwarzania związku pośredniego oraz zastosowanie związku pośredniego
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
EP2566497B1 (en) 2010-05-04 2015-07-29 Codexis, Inc. Biocatalysts for ezetimibe synthesis
ES2372460B1 (es) 2010-07-09 2012-11-16 Moehs Ibérica S.L. Nuevo método para la preparación de ezetimiba.
CN102477008B (zh) * 2010-11-22 2014-05-21 沈阳药科大学 依泽替米贝的合成方法
WO2012076030A1 (en) * 2010-12-10 2012-06-14 Pharmathen S.A. Process for the preparation of intermediate compounds useful in the preparation of ezetimibe
WO2012155932A1 (en) 2011-05-17 2012-11-22 Pharmathen S.A. Improved process for the preparation of ezetimibe
PL231215B1 (pl) 2011-06-15 2019-02-28 Inst Chemii Organicznej Polskiej Akademii Nauk Sposób wytwarzania podstawionych azetydynonów oraz związków pośrednich do ich syntezy
CN103086938A (zh) * 2011-10-28 2013-05-08 沈阳药科大学 依泽替米贝的合成方法
CN102531986A (zh) * 2012-02-23 2012-07-04 苏州朗科生物技术有限公司 一种依替米贝的制备方法
CN103570574B (zh) 2012-07-20 2016-04-13 中国科学院上海有机化学研究所 一种依泽替米贝的合成方法及该方法中所用的中间体
CN103044305A (zh) * 2013-01-24 2013-04-17 上海现代制药股份有限公司 一种依折麦布中间体的制备方法
WO2015039675A1 (en) 2013-09-23 2015-03-26 Pharmathen S.A. Novel process for the preparation of ezetimibe intermediates
CN103739537B (zh) * 2013-12-24 2015-05-20 连云港恒运医药科技有限公司 依折麦布的新合成方法
CN104072398B (zh) * 2014-07-03 2016-02-03 河南省科学院化学研究所有限公司 一种合成依折麦布的方法
JP2016145173A (ja) * 2015-02-09 2016-08-12 株式会社トクヤマ （３ｒ，４ｓ）‐１‐（４‐フルオロフェニル）‐［３（ｓ）‐ヒドロキシ‐３‐（４‐フルオロフェニル）プロピル］‐（４‐ヒドロキシフェニル）‐２‐アゼチジノンの製造方法
CN107098841A (zh) * 2016-02-19 2017-08-29 常州方楠医药技术有限公司 一种依折麦布的制备方法及该方法中所用的中间体
CN107033051A (zh) * 2017-06-08 2017-08-11 武汉励合生物医药科技有限公司 一种依泽替米贝的制备方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5631365A (en) * 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
AU7472896A (en) * 1995-11-02 1997-05-22 Schering Corporation Process for preparing 1-(4-fluorophenyl)-3(r)-(3(s)-hydroxy-3-({phenyl or 4-fluorophenyl})-propyl)-4(s)-(4-hydroxyphenyl)-2-azetidinon

Also Published As

Publication number Publication date
EP0906278A1 (en) 1999-04-07
WO1997045406A1 (en) 1997-12-04
EP0906278B1 (en) 2002-10-16
JP3155759B2 (ja) 2001-04-16
JPH11511754A (ja) 1999-10-12
AR007314A1 (es) 1999-10-27
ATE226191T1 (de) 2002-11-15
DK0906278T3 (da) 2003-02-17
CO4770966A1 (es) 1999-04-30
ZA974678B (en) 1997-11-28
CA2255662C (en) 2005-11-08
CA2255662A1 (en) 1997-12-04
DE69716426D1 (de) 2002-11-21
US5739321A (en) 1998-04-14
ES2185026T3 (es) 2003-04-16
AU3299497A (en) 1998-01-05
DE69716426T2 (de) 2003-08-14

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