[go: up one dir, main page]

PE20070493A1 - Compuestos derivados de 2-azetidinonas como inhibidores de la absorcion de colesterol - Google Patents

Compuestos derivados de 2-azetidinonas como inhibidores de la absorcion de colesterol

Info

Publication number
PE20070493A1
PE20070493A1 PE2006001201A PE2006001201A PE20070493A1 PE 20070493 A1 PE20070493 A1 PE 20070493A1 PE 2006001201 A PE2006001201 A PE 2006001201A PE 2006001201 A PE2006001201 A PE 2006001201A PE 20070493 A1 PE20070493 A1 PE 20070493A1
Authority
PE
Peru
Prior art keywords
alkyl
phenyl
aryl
inhibitors
substituted
Prior art date
Application number
PE2006001201A
Other languages
English (en)
Inventor
Robert J Devita
Gregori J Morriello
Peter Lin
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of PE20070493A1 publication Critical patent/PE20070493A1/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
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • C07D405/10Heterocyclic 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 carbon chain containing aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A COMPUESTOS 2-AZETIDINONAS SUSTITUIDAS DE FORMULA (I) DONDE Ar1 ES ARILO OPCIONALMENTE SUSTITUIDO CON R4 DONDE R4 ES OR5, O(CO)R5, COR5, ENTRE OTROS; X, Y Y Z SON CH2, CH(ALQUILO(C1-C6)) O C(ALQUILO(C1-C6))2; R ES OR6, O(CO)R6, UN RESTO AZUCAR, ENTRE OTROS; R1 ES H, ALQUILO(C1-C6), ARILO O R Y R1 JUNTOS SON OXO; R2 ES OR6, O(CO)R6, ENTRE OTROS, DONDE R5 Y R6 SON H, ALQUILO(C1-C6), ARILO O ALQUILO(C1-C6)ARIL SUSTITUIDO; R3 ES H, ALQUILO(C1-C6), ARILO O R2 Y R3 JUNTOS SON OXO; q Y r SON 0 O 1; m, n Y p SON DE 0 A 4; R9 ES -C=C-(CH2)y-NR10R11, -C=C-(CH2)y-NR10R11 O -(CH2)w-NR10R11, DONDE w ES DE 1 A 8; y ES DE 1 A 6; R10 ES H O ALQUILO(C1-C3); R11 ES H, ALQUILO(C1-C3), -C(O)-ALQUILO(C1-C3), ENTRE OTROS; R12 ES ALQUILO(C1-C15) SUSTITUIDO CON OH, ENTRE OTROS; R13 ES H U OH. SON COMPUESTOS PREFERIDOS: N-[3-(4-{(2S,3R)-2-{4-[3,4-DIHIDROXI-3-(HIDROXIMETIL)BUTIL]FENIL}-3-[(3S)-3-(4-FLUOROFENIL)-3-HIDROXIPROPIL]-4-OXOAZETIDIN-1-IL}FENIL)PROPIL]METANOSULFONAMIDA, N-[3-(4-{(2S,3R)-3-[(3S)-3-(4-FLUOROFENIL)-3-HIDROXIPROPIL]-2-[4-(6-HIDROXIHEXIL)FENIL]-4-OXOAZETIDIN-1-IL}FENIL)PROPIL]-N-METILMETANOSULFONAMIDA, N-[3-(4-{(2S,3R)-2-{4-[3,4-DIHIDROXI-3-(HIDROXIMETIL)BUTIL]-2-HIDROXIFENIL}-3-[(3S)-3-(4-FLUOROFENIL)-3-HIDROXIPROPIL]-4-OXOAZETIDIN-1-IL}FENIL)PROPIL]METANOSULFONAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ABSORCION DE COLESTEROL SIENDO UTILES EN EL TRATAMIENTO DE HIPERCOLESTEROLEMIA
PE2006001201A 2005-10-05 2006-10-03 Compuestos derivados de 2-azetidinonas como inhibidores de la absorcion de colesterol PE20070493A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US72378105P 2005-10-05 2005-10-05

Publications (1)

Publication Number Publication Date
PE20070493A1 true PE20070493A1 (es) 2007-06-13

Family

ID=37845278

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006001201A PE20070493A1 (es) 2005-10-05 2006-10-03 Compuestos derivados de 2-azetidinonas como inhibidores de la absorcion de colesterol

Country Status (25)

Country Link
US (2) US20090137546A1 (es)
EP (1) EP1934175B1 (es)
JP (1) JP4879991B2 (es)
KR (1) KR20080050610A (es)
CN (1) CN101277930A (es)
AR (1) AR058068A1 (es)
AT (1) ATE488495T1 (es)
AU (1) AU2006302584B2 (es)
BR (1) BRPI0616834A2 (es)
CA (1) CA2624481C (es)
CR (1) CR9903A (es)
DE (1) DE602006018341D1 (es)
DO (1) DOP2006000211A (es)
EA (1) EA200801008A1 (es)
ES (1) ES2354460T3 (es)
GT (1) GT200600444A (es)
IL (1) IL190434A0 (es)
MA (1) MA30006B1 (es)
NO (1) NO20082075L (es)
PE (1) PE20070493A1 (es)
SV (1) SV2009002863A (es)
TN (1) TNSN08153A1 (es)
TW (1) TW200806623A (es)
WO (1) WO2007044318A2 (es)
ZA (1) ZA200802587B (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
GB0215579D0 (en) * 2002-07-05 2002-08-14 Astrazeneca Ab Chemical compounds
JP4688819B2 (ja) * 2003-12-23 2011-05-25 アストラゼネカ アクチボラグ コレステロール吸収阻害活性を有するジフェニルアゼチジノン誘導体
CN100471835C (zh) * 2003-12-23 2009-03-25 默克公司 抗高胆固醇血症化合物
GB0329778D0 (en) * 2003-12-23 2004-01-28 Astrazeneca Ab Chemical compounds
UY29607A1 (es) * 2005-06-20 2007-01-31 Astrazeneca Ab Compuestos quimicos
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
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
AR054482A1 (es) * 2005-06-22 2007-06-27 Astrazeneca Ab Derivados de azetidinona para el tratamiento de hiperlipidemias
TW200806623A (en) * 2005-10-05 2008-02-01 Merck & Co Inc Anti-hypercholesterolemic compounds
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
TW200811098A (en) * 2006-04-27 2008-03-01 Astrazeneca Ab Chemical compounds
AU2007342603A1 (en) * 2006-12-20 2008-07-17 Merck Sharp & Dohme Corp. Anti-hypercholesterolemic compounds
DE102009023046B4 (de) 2008-05-30 2016-10-13 Hyundai Motor Company Automatisch schaltbares Getriebe eines Kraftfahrzeuges
WO2010056788A1 (en) * 2008-11-17 2010-05-20 Merck Sharp & Dohme Corp. Anti-hypercholesterolemic compounds

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0596015B1 (en) * 1991-07-23 1997-10-01 Schering Corporation Substituted beta-lactam compounds useful as hypocholesterolemic agents and processes for the preparation thereof
US5631365A (en) * 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
CA2191455A1 (en) * 1994-06-20 1995-12-28 Wayne Vaccaro Substituted azetidinone compounds useful as hypocholesterolemic agents
US5624920A (en) * 1994-11-18 1997-04-29 Schering Corporation Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents
NZ526593A (en) * 2000-12-21 2005-02-25 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
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
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
CA2517571C (en) * 2003-03-07 2011-07-05 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
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
CN100471835C (zh) * 2003-12-23 2009-03-25 默克公司 抗高胆固醇血症化合物
WO2006086562A2 (en) * 2005-02-09 2006-08-17 Microbia, Inc. Phenylazetidinone derivatives
CA2611142A1 (en) * 2005-06-15 2006-12-28 Merck & Co., Inc. Anti-hypercholesterolemic compounds
TW200806623A (en) * 2005-10-05 2008-02-01 Merck & Co Inc Anti-hypercholesterolemic compounds
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
EP2091915A1 (de) * 2006-11-02 2009-08-26 Sanofi-Aventis Deutschland GmbH Neues mit piperazin-1-sulfonsäure substituiertes diphenylazetidinon mit verbesserten pharmakologischen eigenschaften

Also Published As

Publication number Publication date
MA30006B1 (fr) 2008-12-01
EP1934175A2 (en) 2008-06-25
NO20082075L (no) 2008-07-04
WO2007044318A3 (en) 2007-07-12
US20090137546A1 (en) 2009-05-28
JP4879991B2 (ja) 2012-02-22
SV2009002863A (es) 2009-02-19
GT200600444A (es) 2007-05-04
TNSN08153A1 (en) 2009-10-30
US7704988B2 (en) 2010-04-27
IL190434A0 (en) 2008-11-03
JP2009511475A (ja) 2009-03-19
ZA200802587B (en) 2009-06-24
US20070078098A1 (en) 2007-04-05
ATE488495T1 (de) 2010-12-15
WO2007044318A2 (en) 2007-04-19
ES2354460T3 (es) 2011-03-15
BRPI0616834A2 (pt) 2016-08-23
CR9903A (es) 2008-07-29
AU2006302584A1 (en) 2007-04-19
TW200806623A (en) 2008-02-01
CA2624481A1 (en) 2007-04-19
EP1934175B1 (en) 2010-11-17
DE602006018341D1 (de) 2010-12-30
CN101277930A (zh) 2008-10-01
CA2624481C (en) 2012-04-03
AU2006302584B2 (en) 2011-10-13
DOP2006000211A (es) 2007-05-31
AR058068A1 (es) 2008-01-23
KR20080050610A (ko) 2008-06-09
EA200801008A1 (ru) 2009-02-27

Similar Documents

Publication Publication Date Title
PE20070493A1 (es) Compuestos derivados de 2-azetidinonas como inhibidores de la absorcion de colesterol
PE20051170A1 (es) DERIVADOS DE PIRROL COMO INHIBIDORES DEL FACTOR Xa
AR058754A1 (es) Procesos para preparar compuestos intermediarios utiles para la preparacion de ezetimibe
PE20091400A1 (es) Derivados de n-(2-amino-fenil)-amida como inhibidores de hdac
PE20110598A1 (es) Inhibidores de las enzimas de proteina cinasa activadas por mitogeno p38
ECSP066414A (es) Derivados de malonamida que bloquean la actividad de gama-secretasa
AR074306A1 (es) Aminotetrahidropiranos como inhibidores de dipeptidil peptidasa-iv para el tratamiento o prevencion de diabetes
RU2409562C2 (ru) Новые производные 2-азетидинона в качестве ингибиторов всасывания холестерина для лечения гиперлипидемических состояний
CY1108445T1 (el) Νεα μεθοδος συνθεσης και νεα κρυσταλλικη μορφη της αγομελατινης καθως και φαρμακευτικες συνθεσεις που την περιεχουν
DK1373230T3 (da) Enantiselektiv syntese af azetidinon mellemprodukter
NO20065830L (no) Substituerte 2-kinolyloksazoler som er anvendbare som PDE4-inhibitorer.
PE20091816A1 (es) Inhibidores de bace
RU2409572C2 (ru) Новые производные 2-азетидинона в качестве ингибиторов всасывания холестерина для лечения гиперлипидемических состояний
PE20081354A1 (es) Compuestos de azaindolilo como inhibidores de mek
PE20142185A1 (es) Pirrolidina-2-carboxamidas sustituidas
PE20081532A1 (es) Compuestos novedosos
NO20074763L (no) (1,5-difenyl-1H-pyrazol-3-yl)oksadiazolderivater, fremgangsmate ved fremstilling derav og anvendelse av samme i terapi
PE20080951A1 (es) DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS
PE20091258A1 (es) Derivados de piridina como activadores de la guanilato ciclasa soluble
AR071617A1 (es) Bencenosulfonamidas de oxazol y tiazol, composiciones farmaceuticas que las contienen, proceso de preparacion y uso de las mismas como agentes anticancerigenos.
PE20040864A1 (es) Derivados de heterobiarilo como inhibidores de metaloproteinasa de la matriz
WO2007030721A3 (en) 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
PE20080856A1 (es) Inhibidores de metaloproteasas de matriz
PE20020718A1 (es) 2-azetidinonas sustituidas con azucares utiles como agentes hipocolesterolemicos
PE20060150A1 (es) Antagonistas de cgrp seleccionados, composiciones farmaceuticas y procedimiento para su preparacion

Legal Events

Date Code Title Description
FC Refusal