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ECSP078052A - Nuevos derivados de la 2-azetidinona como inhibidores de la absorción del colesterol para el tratamiento de condiciones hiperlipidémicas - Google Patents

Nuevos derivados de la 2-azetidinona como inhibidores de la absorción del colesterol para el tratamiento de condiciones hiperlipidémicas

Info

Publication number
ECSP078052A
ECSP078052A EC2007008052A ECSP078052A ECSP078052A EC SP078052 A ECSP078052 A EC SP078052A EC 2007008052 A EC2007008052 A EC 2007008052A EC SP078052 A ECSP078052 A EC SP078052A EC SP078052 A ECSP078052 A EC SP078052A
Authority
EC
Ecuador
Prior art keywords
treatment
inhibitors
cholesterol absorption
azetidinone
new derivatives
Prior art date
Application number
EC2007008052A
Other languages
English (en)
Inventor
Susanne Alenfalk
Mikael Dahlstroem
Fana Hunegnaw
Staffan Karlsson
Ingemar Starke
Malin Lemurell
Original Assignee
Astrazeneca Ab
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37570734&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP078052(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of ECSP078052A publication Critical patent/ECSP078052A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06Heterocyclic 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
    • C07D205/08Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Biophysics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuestos de fórmula (I) (donde los grupos variables son como los definidos aquí), sales farmacéuticamente aceptables, solvatos, solvatos de tales sales o profármacos de los mismos y su uso como inhibidores de la absorción del colesterol para el tratamiento de la hiperlipidemia son descritos. Los procesos para su fabricación y las composiciones farmacéuticas que los contienen también son descritos.
EC2007008052A 2005-06-22 2007-12-26 Nuevos derivados de la 2-azetidinona como inhibidores de la absorción del colesterol para el tratamiento de condiciones hiperlipidémicas ECSP078052A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE0501465 2005-06-22

Publications (1)

Publication Number Publication Date
ECSP078052A true ECSP078052A (es) 2008-01-23

Family

ID=37570734

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2007008052A ECSP078052A (es) 2005-06-22 2007-12-26 Nuevos derivados de la 2-azetidinona como inhibidores de la absorción del colesterol para el tratamiento de condiciones hiperlipidémicas

Country Status (19)

Country Link
US (1) US7893048B2 (es)
EP (1) EP1896410A4 (es)
JP (1) JP2008546773A (es)
KR (1) KR20080019709A (es)
CN (1) CN101243044A (es)
AR (1) AR054481A1 (es)
AU (1) AU2006259897B2 (es)
BR (1) BRPI0611633A2 (es)
CA (1) CA2609993A1 (es)
EC (1) ECSP078052A (es)
IL (1) IL187740A0 (es)
MX (1) MX2007016397A (es)
NO (1) NO20076254L (es)
RU (1) RU2409562C2 (es)
SA (1) SA06270191B1 (es)
TW (1) TW200726747A (es)
UY (1) UY29614A1 (es)
WO (1) WO2006137796A1 (es)
ZA (1) ZA200710609B (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0215579D0 (en) 2002-07-05 2002-08-14 Astrazeneca Ab Chemical compounds
BRPI0418004A (pt) 2003-12-23 2007-04-17 Astrazeneca Ab composto ou um sal, solvato, solvato de um tal sal ou uma pró-droga deste farmaceuticamente aceitáveis, métodos para tratar ou prevenir condições hiperlipidêmicas, aterosclerose, mal de alzheimer, e tumores associados com colesterol, formulação farmacêutica, combinação, e, processo para preparar um composto ou um sal, solvato, solvato de um tal sal ou uma pró-droga deste farmaceuticamente aceitáveis
UY29607A1 (es) * 2005-06-20 2007-01-31 Astrazeneca Ab Compuestos quimicos
AR054482A1 (es) * 2005-06-22 2007-06-27 Astrazeneca Ab Derivados de azetidinona para el tratamiento de hiperlipidemias
AR057383A1 (es) * 2005-06-22 2007-12-05 Astrazeneca Ab Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto
AR057380A1 (es) * 2005-06-22 2007-11-28 Astrazeneca Ab Compuestos quimicos derivados de 2-azetidinona y uso terapeutico de los mismos
MY148538A (en) * 2005-06-22 2013-04-30 Astrazeneca Ab Novel 2-azetidinone derivatives as cholesterol absorption inhibitors for the treatment of hyperlipidaemic conditions
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
TW200811098A (en) 2006-04-27 2008-03-01 Astrazeneca Ab Chemical compounds
AU2007283113A1 (en) 2006-08-08 2008-02-14 Sanofi-Aventis Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, processes for preparing them, medicaments comprising these compounds, and their use
EP2133347A4 (en) * 2007-03-06 2010-03-17 Teijin Pharma Ltd 1-BIARYLAZETIDINONDERIVATE
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
DE102007054497B3 (de) 2007-11-13 2009-07-23 Sanofi-Aventis Deutschland Gmbh Neue kristalline Diphenylazetidinonhydrate und Verfahren zu deren Herstellung
EP2310372B1 (en) 2008-07-09 2012-05-23 Sanofi Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof
WO2010068601A1 (en) 2008-12-08 2010-06-17 Sanofi-Aventis A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof
EP2403848A1 (en) 2009-03-06 2012-01-11 Lipideon Biotechnology AG Pharmaceutical hypocholesterolemic compositions
JP2013503135A (ja) 2009-08-26 2013-01-31 サノフイ 新規な結晶性複素芳香族フルオログリコシド水和物、その化合物を含んでなる医薬及びその使用
WO2011157827A1 (de) 2010-06-18 2011-12-22 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
RU2013114390A (ru) 2010-08-31 2014-10-10 СНУ Ар энд ДиБи ФАУНДЕЙШН Применение фетального репрограммирования посредством ppar-дельта-агониста
EP2683700B1 (de) 2011-03-08 2015-02-18 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
WO2012120052A1 (de) 2011-03-08 2012-09-13 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2012120055A1 (de) 2011-03-08 2012-09-13 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof

Family Cites Families (115)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69222532T2 (de) 1991-07-23 1998-02-26 Schering Corp Substituierte beta-lactam-verbindungen als hypocholesterolemische mittel und verfahren zu deren herstellung
LT3300B (en) 1992-12-23 1995-06-26 Schering Corp Combination of a cholesterol biosynhtesis inhibitor and a beta- lactam cholesterol absorbtion inhibitor
LT3595B (en) 1993-01-21 1995-12-27 Schering Corp Spirocycloalkyl-substituted azetidinones useful as hypocholesterolemic agents
EP0707567B1 (en) 1993-07-09 2001-09-12 Schering Corporation Process for the synthesis of azetidinones
US5631365A (en) 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
US5627176A (en) 1994-03-25 1997-05-06 Schering Corporation Substituted azetidinone compounds useful as hypocholesterolemic agents
WO1995035277A1 (en) 1994-06-20 1995-12-28 Schering Corporation Substituted azetidinone compounds useful as hypocholesterolemic agents
MX9702175A (es) 1994-09-20 1997-06-28 Pfizer Combinacion de un inhibidor de absorcion de colesterol y un inhibidor de sintesis de colesterol.
US5633246A (en) * 1994-11-18 1997-05-27 Schering Corporation Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents
US5656624A (en) 1994-12-21 1997-08-12 Schering Corporation 4-[(heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinones useful as hypolipidemic agents
CA2235943C (en) 1995-10-31 2002-10-01 Schering Corporation Sugar-substituted 2-azetidinones 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
US5886171A (en) 1996-05-31 1999-03-23 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
US5739321A (en) 1996-05-31 1998-04-14 Schering Corporation 3-hydroxy γ-lactone based enantionselective synthesis of azetidinones
US5756470A (en) 1996-10-29 1998-05-26 Schering Corporation Sugar-substituted 2-azetidinones useful as hypocholesterolemic agents
US5919672A (en) 1998-10-02 1999-07-06 Schering Corporation Resolution of trans-2-(alkoxycarbonylethyl)-lactams useful in the synthesis of 1-(4-fluoro-phenyl)-3(R)- (S)-hydroxy-3-(4-fluorophenyl)-propyl!-4(S)-(4-hydroxyphenyl)-2-azetidinone
WO2000034240A1 (en) 1998-12-07 2000-06-15 Schering Corporation Process for the synthesis of azetidinones
EP1354604A1 (en) 1998-12-23 2003-10-22 G.D. Searle LLC. Combinations for cardiovascular indications
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
US6593078B1 (en) 1999-04-16 2003-07-15 Schering Corporation Use of azetidinone compounds
DE10042447A1 (de) 2000-08-29 2002-03-28 Aventis Pharma Gmbh Protein aus dem Darm von Wirbeltieren, welches Cholesterin absorbiert, sowie Verwendung dieses Proteins zur Identifizierung von Inhibitoren des intestinalen Cholesterintransports
IL155771A0 (en) 2000-12-20 2003-12-23 Schering Corp Sugar-substituted 2-azetidinones useful as hypocholesterolemic agents
IL156552A0 (en) 2000-12-21 2004-01-04 Aventis Pharma Gmbh Diphenyl azetidinone derivatives, method for the production thereof, medicaments containing these compounds, and their use
AU1609702A (en) 2000-12-21 2002-07-01 Aventis Pharma Gmbh Novel 1,2-diphenzylazetidinones, method for producing the same, medicaments containing said compounds, and the use thereof for treating disorders of the lipid metabolism
WO2002050060A1 (de) 2000-12-21 2002-06-27 Avantis Pharma Deutschland Gmbh Diphenylazetidinonderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
KR20080067717A (ko) 2001-01-26 2008-07-21 쉐링 코포레이션 스테롤 흡수 억제제와 혈액 조절제를 포함하는 혈관 질환의치료 또는 예방용 약제학적 조성물
ES2287250T3 (es) 2001-01-26 2007-12-16 Schering Corporation Combinaciones de secuestrante(s) de acidos biliares e inhibidor(es) de la absorcion de esteroles y tratamientos para indicaciones vasculares.
ME00145B (me) 2001-01-26 2010-10-10 Merck Sharp & Dohme Upotreba supstituisanih jedinjenja azetidinona za lečenje sitosterolemije
IL156445A0 (en) 2001-01-26 2004-01-04 Schering Corp Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
JP2004517916A (ja) 2001-01-26 2004-06-17 シェーリング コーポレイション ニコチン酸およびその誘導体ならびにステロール吸収阻害剤の併用、および血管適応症の治療
JP2004517919A (ja) 2001-01-26 2004-06-17 シェーリング コーポレイション 血管状態の処置のための心臓血管薬剤とステロール吸収インヒビターとの組み合わせ
TWI291957B (en) 2001-02-23 2008-01-01 Kotobuki Pharmaceutical Co Ltd Beta-lactam compounds, process for repoducing the same and serum cholesterol-lowering agents containing the same
WO2002072104A2 (en) 2001-03-08 2002-09-19 Merck & Co., Inc. Antihypertensive agent and cholesterol absorption inhibitor combination therapy
WO2002079174A2 (en) 2001-03-28 2002-10-10 Schering Corporation Enantioselective synthesis of azetidinone intermediate compounds
PT1392287E (pt) 2001-05-25 2007-02-28 Schering Corp Métodos para tratamento de doença de alzheimer e/ou regulação dos níveis de peptídeos β amilóide num sujeito
ES2272776T3 (es) 2001-09-21 2007-05-01 Schering Corporation Tratamiento de xantomas con derivados de azetidinona como inhibidores de la absorcion de esterol.
US7053080B2 (en) 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
AU2002335770B2 (en) 2001-09-21 2005-08-18 Merck Sharp & Dohme Corp. Methods for treating or preventing vascular inflammation using sterol absorption inhibitor(s)
WO2003088962A1 (en) 2002-04-16 2003-10-30 Merck & Co., Inc. Combination therapy using a ppar alpha/gamma agonist
DE10227506A1 (de) 2002-06-19 2004-01-08 Aventis Pharma Deutschland Gmbh Ringsubstituierte Diphenylazetidinone, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
DE10227507A1 (de) 2002-06-19 2004-01-08 Aventis Pharma Deutschland Gmbh Kationisch substituierte Diphenylazetidinone, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
DE10227508A1 (de) 2002-06-19 2004-01-08 Aventis Pharma Deutschland Gmbh Säuregruppen-substituierte Diphenylazetidinone, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
US6941867B2 (en) 2002-07-01 2005-09-13 Special Devices, Inc. Initiator with a slip plane between an ignition charge and an output charge
GB0215579D0 (en) * 2002-07-05 2002-08-14 Astrazeneca Ab Chemical compounds
AR040588A1 (es) 2002-07-26 2005-04-13 Schering Corp Formulacion farmaceutica que comprende un inhibidor de la absorcion del colesterol y un inhibidor de una hmg- co a reductasa
US6761509B2 (en) 2002-07-26 2004-07-13 Jan Erik Jansson Concrete module for retaining wall and improved retaining wall
CA2493614C (en) 2002-07-30 2011-09-13 Karykion Inc. Compositions of ezetimibe and methods for the treatment of cholesterol-associated benign and malignant tumors
US6960047B2 (en) 2002-08-02 2005-11-01 Innovative Technology Application, Inc. Protection barrier apparatus
RU2345089C2 (ru) 2002-08-06 2009-01-27 Санофи-Авентис Дойчланд Гмбх ОЧИЩЕННЫЙ 145 кДа-БЕЛОК, СПОСОБНЫЙ СВЯЗЫВАТЬ ХОЛЕСТЕРИН И/ИЛИ ИНГИБИТОРЫ ПОГЛОЩЕНИЯ ХОЛЕСТЕРИНА, СПОСОБЫ ЕГО ПОЛУЧЕНИЯ И ОЧИСТКИ И ПРИМЕНЕНИЕ 145 кДа-БЕЛКА
WO2004043457A1 (en) 2002-11-06 2004-05-27 Schering Corporation Cholesterol absorptions inhibitors for the treatment of autoimmune disorders
DE602004016123D1 (de) 2003-03-07 2008-10-09 Schering Corp Substituierte azetidinon-derivate, deren pharmazeutische formulierungen und deren verwendung zur behandlung von hypercholesterolemia
CN1805926A (zh) 2003-05-05 2006-07-19 兰贝克赛实验室有限公司 二苯基氮杂环丁酮衍生物的反式异构体的制备方法
US20040259179A1 (en) 2003-05-30 2004-12-23 Gerd Assmann Sterol markers as diagnostic tools in the prevention of atherosclerotic diseases and as tools to aid in the selection of agents to be used for the prevention and treatment of atherosclerotic disease
US7002008B2 (en) 2003-06-16 2006-02-21 Bomi Patel Framroze Process for the preparation of 1-(4-fluorophenyl)-4(S)-(4-hydroxyphenyl)-azetidin-2-one
JP2005015434A (ja) 2003-06-27 2005-01-20 Kotobuki Seiyaku Kk 血清コレステロール低下剤或はアテローム性硬化症の予防又は治療剤
EP1660456A2 (en) 2003-08-25 2006-05-31 Microbia Inc. Quaternary salt derivatives of 1,4-diphenylazetidin-2-ones
WO2005021497A2 (en) 2003-08-28 2005-03-10 Microbia, Inc. Tethered dimers and trimers of 1,4-diphenylazetidn-2-ones
EP1522541A1 (en) 2003-10-07 2005-04-13 Lipideon Biotechnology AG Novel hypocholesterolemic compounds
CA2543943A1 (en) 2003-10-30 2005-05-19 Merck & Co., Inc. 2-azetidinones as anti-hypercholesterolemic agents
WO2005042692A2 (en) 2003-10-31 2005-05-12 Forbes Medi-Tech Inc. A method of inhibiting the expression of genes which mediate cellular cholesterol influx in animal cells and inhibiting the production of proteins resulting from the expression of such genes using cholesterol absorption inhibitors
EP1680189A2 (en) 2003-11-05 2006-07-19 Schering Corporation Combinations of lipid modulating agents and substituted azetidinones and treatments for vascular conditions
KR20070050861A (ko) 2003-11-10 2007-05-16 마이크로비아 인코포레이티드 4-비아릴일-1-페닐아제티딘-2-온
US7067675B2 (en) 2003-11-24 2006-06-27 Hetero Drugs Limited Process for ezetimibe intermediate
CA2548790A1 (en) 2003-12-17 2005-06-30 Dainippon Sumitomo Pharma Co., Ltd. Medicinal compositions and combinations
BRPI0418004A (pt) 2003-12-23 2007-04-17 Astrazeneca Ab composto ou um sal, solvato, solvato de um tal sal ou uma pró-droga deste farmaceuticamente aceitáveis, métodos para tratar ou prevenir condições hiperlipidêmicas, aterosclerose, mal de alzheimer, e tumores associados com colesterol, formulação farmacêutica, combinação, e, processo para preparar um composto ou um sal, solvato, solvato de um tal sal ou uma pró-droga deste farmaceuticamente aceitáveis
WO2005062824A2 (en) 2003-12-23 2005-07-14 Merck & Co., Inc. Anti-hypercholesterolemic compounds
WO2005062897A2 (en) 2003-12-23 2005-07-14 Dr. Reddy's Laboratories Ltd. Polymorphs of ezetimibe and processes for the preparation thereof
GB0329778D0 (en) * 2003-12-23 2004-01-28 Astrazeneca Ab Chemical compounds
WO2005066120A2 (en) 2003-12-30 2005-07-21 Ranbaxy Laboratories Limited Process for asymmetric synthesis of hydroxy-alkyl substituted azetidinone derivatives
US7901893B2 (en) 2004-01-16 2011-03-08 Merck Sharp & Dohme Corp. NPC1L1 (NPC3) and methods of identifying ligands thereof
RS20060437A (sr) 2004-01-20 2008-11-28 Panacea Boitec Ltd., Farmaceutski sastavi koji sadrže više primarne alkohole i ezetimib i postupak za njihovo dobijanje
PL1756049T3 (pl) 2004-05-21 2008-02-29 Sanofi Aventis Deutschland Sposób wytwarzania pochodnych 1,4-difenyloazetydynonu
DE102004025072A1 (de) 2004-05-21 2005-12-15 Sanofi-Aventis Deutschland Gmbh Verfahren zur Herstellung von Diphenyl-azetidinon-Derivaten
WO2006017257A2 (en) 2004-07-12 2006-02-16 Phenomix Corporation Azetidinone derivatives
US20060046996A1 (en) 2004-08-31 2006-03-02 Kowa Co., Ltd. Method for treating hyperlipidemia
CA2581596A1 (en) 2004-09-29 2006-04-13 Schering Corporation Combinations of substituted azetidonones and cb1 antagonists
EP1817280A1 (en) 2004-12-03 2007-08-15 Teva Pharmaceutical Industries Ltd. Ezetimibe polymorphs
CN101119966B (zh) 2004-12-20 2014-08-13 默沙东公司 合成2-吖丁啶酮的方法
IL166149A0 (en) 2005-01-05 2006-01-15 Hadasit Med Res Service Use of ezetimibe and amiodarone in protection against beta-amyloid neurotoxicity
EP1851197A2 (en) 2005-02-09 2007-11-07 Microbia, Inc. Phenylazetidinone derivatives
US20090186834A1 (en) 2005-03-24 2009-07-23 Microbia, Inc. Diphenylheterocycle cholesterol absorption inhibitors
US8361999B2 (en) 2005-04-04 2013-01-29 Pontificia Universidad Catolica De Chile Methods of treating cholesterol gallstone disease with ezetimibe
JP2008539255A (ja) 2005-04-26 2008-11-13 マイクロビア インコーポレーテッド 高コレステロール血症のための4−ビアリーリル−1−フェニルアゼチジン−2−オングルクロニド誘導体
US20090131395A1 (en) 2005-05-05 2009-05-21 Microbia, Inc. Biphenylazetidinone cholesterol absorption inhibitors
WO2006122186A2 (en) 2005-05-10 2006-11-16 Microbia, Inc. 1,4-diphenyl-3-hydroxyalkyl-2-azetidinone derivatives for treating hypercholestrolemia
EP1885703A4 (en) 2005-05-11 2009-09-02 Microbia Inc METHODS FOR PRODUCING 4-BIPHENYLYLAZETIDIN-2-ONE PHENOLIC DERIVATIVES
JP2008540573A (ja) 2005-05-13 2008-11-20 マイクロビア インコーポレーテッド 4−ビアリーリル−1−フェニラゼチジン−2−オン類
WO2006127893A2 (en) 2005-05-25 2006-11-30 Microbia, Inc. Processes for production of 4-(biphenylyl)azetidin-2-one phosphonic acids
WO2006134604A1 (en) 2005-06-15 2006-12-21 Hetero Drugs Limited Combination composition of cholesterol absorption inhibitor and 3-hydroxy-3-methylglutaryl-coenzyme a (hmg-coa) reductase inhibitor
CN101198338A (zh) 2005-06-15 2008-06-11 默克公司 抗高胆固醇血化合物
UY29607A1 (es) * 2005-06-20 2007-01-31 Astrazeneca Ab Compuestos quimicos
US8013150B2 (en) 2005-06-22 2011-09-06 Msn Laboratories Ltd. Process for the preparation of ezetimibe
MY148538A (en) 2005-06-22 2013-04-30 Astrazeneca Ab Novel 2-azetidinone derivatives as cholesterol absorption inhibitors for the treatment of hyperlipidaemic conditions
AR056866A1 (es) 2005-06-22 2007-10-31 Astrazeneca Ab Compuestos quimicos derivados de 2-azetidinona, una formulacion farmaceutica y un proceso de preparacion del compuesto
AR057380A1 (es) * 2005-06-22 2007-11-28 Astrazeneca Ab Compuestos quimicos derivados de 2-azetidinona y uso terapeutico de los mismos
AR054482A1 (es) 2005-06-22 2007-06-27 Astrazeneca Ab Derivados de azetidinona para el tratamiento de hiperlipidemias
AR057383A1 (es) * 2005-06-22 2007-12-05 Astrazeneca Ab Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto
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
EP1741427A1 (en) 2005-07-06 2007-01-10 KRKA, D.D., Novo Mesto Pharmaceutical composition comprising simvastatin and ezetimibe
WO2007008541A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
WO2007008529A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc Celullar cholesterol absorption modifiers
WO2007016643A2 (en) 2005-08-01 2007-02-08 Mount Sinai School Of Medicine Of New York University A method for extending longevity using npc1l1 antagonists
JP2009503049A (ja) 2005-08-01 2009-01-29 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 新規な置換アゼチジノン
WO2007017705A1 (en) 2005-08-09 2007-02-15 Glenmark Pharmaceuticals Limited Process for the preparation of azetidinones
US20070049748A1 (en) 2005-08-26 2007-03-01 Uppala Venkata Bhaskara R Preparation of ezetimibe
EP1922304A2 (en) 2005-09-08 2008-05-21 Teva Pharmaceutical Industries Ltd Processes for the preparation of (3r,4s)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((s)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe
TW200806623A (en) 2005-10-05 2008-02-01 Merck & Co Inc Anti-hypercholesterolemic compounds
TW200803868A (en) 2005-11-15 2008-01-16 Takeda Pharmaceutical Novel method for treating hyperlipidemia
DE102005055726A1 (de) 2005-11-23 2007-08-30 Sanofi-Aventis Deutschland Gmbh Hydroxy-substituierte Diphenylazetidinone, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
US7498431B2 (en) 2005-12-01 2009-03-03 Bomi Patel Framroze Process for the preparation of chiral azetidinones
HU0501164D0 (en) 2005-12-20 2006-02-28 Richter Gedeon Vegyeszet New industrial process for the production of ezetimibe
US20070161578A1 (en) 2005-12-21 2007-07-12 Hwa Joyce J Treatment of nonalcoholic fatty liver disease using cholesterol lowering agents and/or H3 receptor antagonist/inverse agonist
TW200811098A (en) * 2006-04-27 2008-03-01 Astrazeneca Ab Chemical compounds
WO2008033431A1 (en) * 2006-09-15 2008-03-20 Schering Corporation Spirocyclic azetidinone derivatives for the treatment of disorders of lipid metabolism, pain, diabetes and other disorders
EP2133347A4 (en) * 2007-03-06 2010-03-17 Teijin Pharma Ltd 1-BIARYLAZETIDINONDERIVATE

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UY29614A1 (es) 2007-01-31
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