WO2006137782A1 - Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia - Google Patents

Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia Download PDF

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Publication number
WO2006137782A1
WO2006137782A1 PCT/SE2006/000741 SE2006000741W WO2006137782A1 WO 2006137782 A1 WO2006137782 A1 WO 2006137782A1 SE 2006000741 W SE2006000741 W SE 2006000741W WO 2006137782 A1 WO2006137782 A1 WO 2006137782A1
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WO
WIPO (PCT)
Prior art keywords
solvate
alkyl
formula
compound
salt
Prior art date
Application number
PCT/SE2006/000741
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English (en)
French (fr)
Inventor
Susanne Alenfalk
Mikael Dahlström
Fana Hunegnaw
Staffan Karlsson
Malin Lemurell
Ann-Margret Lindqvist
Tore SKJÄRET
Ingemar Starke
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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.)
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Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Priority to US11/993,033 priority Critical patent/US7863265B2/en
Priority to JP2008518077A priority patent/JP2008546766A/ja
Priority to BRPI0612254A priority patent/BRPI0612254A2/pt
Priority to MX2007016483A priority patent/MX2007016483A/es
Priority to EP06747933A priority patent/EP1896407A4/en
Priority to AU2006259949A priority patent/AU2006259949A1/en
Priority to CA002610890A priority patent/CA2610890A1/en
Publication of WO2006137782A1 publication Critical patent/WO2006137782A1/en
Priority to NO20076137A priority patent/NO20076137L/no
Priority to IL187736A priority patent/IL187736A0/en

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    • 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
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
PCT/SE2006/000741 2005-06-20 2006-06-19 Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia WO2006137782A1 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
US11/993,033 US7863265B2 (en) 2005-06-20 2006-06-19 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia
JP2008518077A JP2008546766A (ja) 2005-06-20 2006-06-19 新規2−アゼチジノン誘導体、および高脂血症の処置のためのコレステロール吸収阻害剤としてのそれらの使用
BRPI0612254A BRPI0612254A2 (pt) 2005-06-20 2006-06-19 composto, formulação farmacêutica, combinação, e, processo para preparar um composto
MX2007016483A MX2007016483A (es) 2005-06-20 2006-06-19 Nuevos derivados de 2-azetidinona y su uso como inhibidores de absorcion del colesterol para el tratamiento de hiperlipidemia.
EP06747933A EP1896407A4 (en) 2005-06-20 2006-06-19 NOVEL 2-AZETIDINONE DERIVATIVES AND THEIR USE AS CHOLESTEROL ABSORPTION INHIBITORS FOR THE TREATMENT OF HYPERLIPEMICS
AU2006259949A AU2006259949A1 (en) 2005-06-20 2006-06-19 Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia
CA002610890A CA2610890A1 (en) 2005-06-20 2006-06-19 Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia
NO20076137A NO20076137L (no) 2005-06-20 2007-11-28 Nye 2-azetidinonderivater og deres anvendelse som kolestrolabsorpsjonsinhibitorer for behandling av hyperlipidemi
IL187736A IL187736A0 (en) 2005-06-20 2007-11-28 Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE0501425 2005-06-20
SE0501425-3 2005-06-20

Publications (1)

Publication Number Publication Date
WO2006137782A1 true WO2006137782A1 (en) 2006-12-28

Family

ID=37570721

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/SE2006/000741 WO2006137782A1 (en) 2005-06-20 2006-06-19 Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia

Country Status (18)

Country Link
US (1) US7863265B2 (US20100216759A1-20100826-C00014.png)
EP (1) EP1896407A4 (US20100216759A1-20100826-C00014.png)
JP (1) JP2008546766A (US20100216759A1-20100826-C00014.png)
KR (1) KR20080019710A (US20100216759A1-20100826-C00014.png)
CN (1) CN101228123A (US20100216759A1-20100826-C00014.png)
AR (1) AR054484A1 (US20100216759A1-20100826-C00014.png)
AU (1) AU2006259949A1 (US20100216759A1-20100826-C00014.png)
BR (1) BRPI0612254A2 (US20100216759A1-20100826-C00014.png)
CA (1) CA2610890A1 (US20100216759A1-20100826-C00014.png)
EC (1) ECSP088114A (US20100216759A1-20100826-C00014.png)
IL (1) IL187736A0 (US20100216759A1-20100826-C00014.png)
MX (1) MX2007016483A (US20100216759A1-20100826-C00014.png)
NO (1) NO20076137L (US20100216759A1-20100826-C00014.png)
RU (1) RU2007147338A (US20100216759A1-20100826-C00014.png)
TW (1) TW200730493A (US20100216759A1-20100826-C00014.png)
UY (1) UY29607A1 (US20100216759A1-20100826-C00014.png)
WO (1) WO2006137782A1 (US20100216759A1-20100826-C00014.png)
ZA (1) ZA200710415B (US20100216759A1-20100826-C00014.png)

Cited By (18)

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WO2008017381A1 (de) 2006-08-08 2008-02-14 Sanofi-Aventis Arylaminoaryl-alkyl-substituierte imidazolidin-2,4-dione, verfahren zu ihrer herstellung, diese verbindungen enthaltende arzneimittel und ihre verwendung
WO2009021740A2 (de) 2007-08-15 2009-02-19 Sanofis-Aventis Substituierte tetrahydronaphthaline, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DE102007063671A1 (de) 2007-11-13 2009-06-25 Sanofi-Aventis Deutschland Gmbh Neue kristalline Diphenylazetidinonhydrate, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
WO2010003624A2 (en) 2008-07-09 2010-01-14 Sanofi-Aventis 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
WO2010100255A1 (en) 2009-03-06 2010-09-10 Lipideon Biotechnology Ag Pharmaceutical hypocholesterolemic compositions
US7842684B2 (en) 2006-04-27 2010-11-30 Astrazeneca Ab Diphenylazetidinone derivatives possessing cholesterol absorption inhibitor activity
US7863265B2 (en) 2005-06-20 2011-01-04 Astrazeneca Ab 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia
US7871998B2 (en) 2003-12-23 2011-01-18 Astrazeneca Ab Diphenylazetidinone derivatives possessing cholesterol absorption inhibitory activity
US7893048B2 (en) 2005-06-22 2011-02-22 Astrazeneca Ab 2-azetidinone derivatives as cholesterol absorption inhibitors for the treatment of hyperlipidaemic conditions
WO2011023754A1 (en) 2009-08-26 2011-03-03 Sanofi-Aventis Novel crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use
US7906502B2 (en) 2005-06-22 2011-03-15 Astrazeneca Ab 2-azetidinone derivatives as cholesterol absorption inhibitors for the treatment of hyperlipidaemic conditions
WO2011157827A1 (de) 2010-06-18 2011-12-22 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
WO2012120054A1 (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
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
WO2012120056A1 (de) 2011-03-08 2012-09-13 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes 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
WO2012120053A1 (de) 2011-03-08 2012-09-13 Sanofi Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung

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US7863265B2 (en) 2005-06-20 2011-01-04 Astrazeneca Ab 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia
US7893048B2 (en) 2005-06-22 2011-02-22 Astrazeneca Ab 2-azetidinone derivatives as cholesterol absorption inhibitors for the treatment of hyperlipidaemic conditions
US7906502B2 (en) 2005-06-22 2011-03-15 Astrazeneca Ab 2-azetidinone derivatives as cholesterol absorption inhibitors for the treatment of hyperlipidaemic conditions
US7842684B2 (en) 2006-04-27 2010-11-30 Astrazeneca Ab Diphenylazetidinone derivatives possessing cholesterol absorption inhibitor activity
WO2008017381A1 (de) 2006-08-08 2008-02-14 Sanofi-Aventis Arylaminoaryl-alkyl-substituierte imidazolidin-2,4-dione, verfahren zu ihrer herstellung, diese verbindungen enthaltende arzneimittel und ihre verwendung
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WO2011023754A1 (en) 2009-08-26 2011-03-03 Sanofi-Aventis Novel crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use
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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
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EP1896407A4 (en) 2010-06-16
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US7863265B2 (en) 2011-01-04
AU2006259949A1 (en) 2006-12-28
UY29607A1 (es) 2007-01-31
EP1896407A1 (en) 2008-03-12
NO20076137L (no) 2008-01-18
ZA200710415B (en) 2008-10-29
MX2007016483A (es) 2008-03-10
CN101228123A (zh) 2008-07-23
KR20080019710A (ko) 2008-03-04
JP2008546766A (ja) 2008-12-25
AR054484A1 (es) 2007-06-27
BRPI0612254A2 (pt) 2016-09-06
IL187736A0 (en) 2008-08-07
RU2007147338A (ru) 2009-07-27
ECSP088114A (es) 2008-02-20
CA2610890A1 (en) 2006-12-28

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