ES2135050T3 - Compuestos de azetidinona sustituida utiles como agentes hipocolesterolemicos. - Google Patents

Compuestos de azetidinona sustituida utiles como agentes hipocolesterolemicos.

Info

Publication number
ES2135050T3
ES2135050T3 ES95914719T ES95914719T ES2135050T3 ES 2135050 T3 ES2135050 T3 ES 2135050T3 ES 95914719 T ES95914719 T ES 95914719T ES 95914719 T ES95914719 T ES 95914719T ES 2135050 T3 ES2135050 T3 ES 2135050T3
Authority
ES
Spain
Prior art keywords
aryl
lower alkyl
substituted
alkyl
coor6
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES95914719T
Other languages
English (en)
Inventor
Michael P Kirkup
Sundeep Dugar
Banderpalle B Shankar
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme Corp
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
Application granted granted Critical
Publication of ES2135050T3 publication Critical patent/ES2135050T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/30—Preparation of optical isomers
    • C07C227/32—Preparation of optical isomers by stereospecific synthesis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

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

Abstract

AGENTES HIPOCOLESTEROLEMICOS DE ACETIDINONA SUSTITUIDA DE FORMULA (I) O UNA SAL FARMACEUTICAMENTE ACEPTABLE DE LOS MISMOS, EN DONDE: AR{SUP,1} ES ARILO R{SUP,3} SUSTITUIDO; AR{SUP,2} ES ARILO R{SUP,4} SUSTITUIDO; AR{SUP,3} ES ARILO R{SUP,5} SUSTITUIDO; Y Y Z SON INDEPENDIENTEMENTE -CH{SUB,2}-, -CH(ALQUILO BAJO)- O -C(ALQUILO DOBLEMENTE BAJO)-; A ES -O-, -S-, -S(O)- O S(O){SUB,2}-; R{SUP,1} ES -OR{SUP,6}, -O(CO)R{SUP,6}, O(CO)OR{SUP9} O -O(CO)NR{SUP,6}R{SUP,7}; R{SUP,2} ES HIDROGENO, ALQUILO BAJO O ARILO; O R{SUP,1} Y R{SUP,2} SON JUNTOS =O; Q ES 1, 2 O 3; P ES 0, 1, 2, 3 O 4; R{SUP,5} ES 1-3 SUSTITUYENTES SELECCIONADOS INDEPENDIENTEMENTE DE -OR{SUP,6}, -O(CO)R{SUP,6}, O(CO)OR{SUP,9}, -O(CH{SUB,2}){SUB,1-5}OR{SUP,9}, O(CO)NR{SUP,6}R{SUP,7}, -NR{SUP,6}R{SUP,7}, NR{SUP,6}(CO)R{SUP,7}, -NR{SUP,6}(CO)OR{SUP,9}, NR{SUP,6}(CO)NR{SUP,7}R{SUP,8}, -NR{SUP,6}SO{SUB,2}-ALQUILO BAJO, -NR{SUP,6}SO{SUB,2}-ARILO, -CONR{SUP,6}R{SUP,7}, -COR{SUP,6}, SO{SUB,2}NR{SUP,6}R{SUP,7}, S(O){SUB,0-2}-ALQUILO, -S(O){SUB,02}-ARILO, -O(CH{SUB,2}){SUB,1-10}-COOR{SUP,6}, O(CH{SUB,2}){SUB,0-10}CONR{SUP,6}R{SUP,7}, O-HALOGENO, MHALOGENO, O-ALQUILO BAJO, M-ALQUILO BAJO, -(ALQUILENO BAJO)COOR{SUP,6} Y -CH=CH-COOR{SUP,6}; R{SUP,3} Y R{SUP,4} SON SUSTITUYENTES 1-3 SELECCIONADOS INDEPENDIENTEMENTE DE R{SUP,5}, HIDROGENO, P-ALQUILO BAJO, ARILO, -NO{SUB,2}, CF{SUB,3} Y PHALOGENO; R{SUP,6}, R{SUP,7} Y R{SUP,8} SON HIDROGENO, ALQUILO BAJO, ARILO O ARILO SUSTITUIDO POR ALQUILO BAJO; Y R{SUP,9} ES ALQUILO BAJO, ARILO O ARILO SUSTITUIDO POR ALQUILO BAJO; SON DESCRITOS, ASI COMO UN METODO PARA REDUCIR EL SUERO DE COLESTEROL MEDIANTE LA ADMINISTRACION DE DICHOS COMPUESTOS, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN, LA COMBINACION DE UNA ACETIDINONA SUSTITUIDA Y UN INHIBIDOR DE BIOSINTESIS DE COLESTEROL PARA EL TRATAMIENTO Y PREVENCION DE ATEROSCLEROSIS, NUEVOS INTERMEDIOS Y METODOS PARA PREPARAR DICHOS INTERMEDIOS.
ES95914719T 1994-03-25 1995-03-22 Compuestos de azetidinona sustituida utiles como agentes hipocolesterolemicos. Expired - Lifetime ES2135050T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US21849894A 1994-03-25 1994-03-25

Publications (1)

Publication Number Publication Date
ES2135050T3 true ES2135050T3 (es) 1999-10-16

Family

ID=22815366

Family Applications (1)

Application Number Title Priority Date Filing Date
ES95914719T Expired - Lifetime ES2135050T3 (es) 1994-03-25 1995-03-22 Compuestos de azetidinona sustituida utiles como agentes hipocolesterolemicos.

Country Status (20)

Country Link
US (2) US5627176A (es)
EP (1) EP0751934B1 (es)
JP (1) JP3524927B2 (es)
KR (1) KR100338171B1 (es)
CN (1) CN1144522A (es)
AT (1) ATE183738T1 (es)
AU (1) AU686361B2 (es)
CA (1) CA2186364C (es)
CZ (1) CZ281596A3 (es)
DE (1) DE69511687T2 (es)
DK (1) DK0751934T3 (es)
ES (1) ES2135050T3 (es)
FI (1) FI963817A (es)
GR (1) GR3031105T3 (es)
HU (1) HU221309B1 (es)
NO (1) NO964008L (es)
NZ (1) NZ283528A (es)
PL (1) PL316431A1 (es)
SK (1) SK119796A3 (es)
WO (1) WO1995026334A1 (es)

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US5633246A (en) * 1994-11-18 1997-05-27 Schering Corporation Sulfur-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
US5756470A (en) * 1996-10-29 1998-05-26 Schering Corporation Sugar-substituted 2-azetidinones useful as hypocholesterolemic agents
US6593078B1 (en) 1999-04-16 2003-07-15 Schering Corporation Use of azetidinone compounds
US6584357B1 (en) * 2000-10-17 2003-06-24 Sony Corporation Method and system for forming an acoustic signal from neural timing difference data
SI1593670T1 (sl) * 2000-12-20 2007-12-31 Schering Corp S hidroksi substituirani 2-azetidinoni, uporabni kot sredstva za zniĹľevanje holesterola
US6982251B2 (en) 2000-12-20 2006-01-03 Schering Corporation Substituted 2-azetidinones useful as hypocholesterolemic agents
US7417039B2 (en) * 2001-01-26 2008-08-26 Schering Corporation Use of substituted azetidinone compounds for the treatment of sitosterolemia
US7071181B2 (en) * 2001-01-26 2006-07-04 Schering Corporation Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors
ATE381347T1 (de) * 2001-01-26 2008-01-15 Schering Corp Kombinationen von ezetimibe und aspirin zur behandlung von kardiovaskulären erkrankungen
DK1413331T3 (da) * 2001-01-26 2007-12-10 Schering Corp Kombinationer af peroxisomproliferatoraktiveret receptor (PPAR)-aktivatoren fenofibrat og sterolabsorptionsinhibitoren ezetimib til vaskulære indikationer
EP1911462A3 (en) 2001-01-26 2011-11-30 Schering Corporation Compositions comprising a sterol absorption inhibitor
AU2005246926B2 (en) * 2001-01-26 2008-02-28 Merck Sharp & Dohme Corp. The use of substituted azetidinone compounds for the treatment of sitosterolemia
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US7056906B2 (en) * 2001-09-21 2006-06-06 Schering Corporation Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women
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US20040132058A1 (en) 2002-07-19 2004-07-08 Schering Corporation NPC1L1 (NPC3) and methods of use thereof
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
JP4589919B2 (ja) * 2003-03-07 2010-12-01 シェーリング コーポレイション 高コレステロール血症の処置のための、置換アゼチジノン化合物、これらの処方物および使用
ATE406364T1 (de) 2003-03-07 2008-09-15 Schering Corp Substituierte azetidinon-derivate, deren pharmazeutische formulierungen und deren verwendung zur behandlung von hypercholesterolemia
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
JP2007510659A (ja) * 2003-11-05 2007-04-26 シェーリング　コーポレイション 脂質調節剤および置換アゼチジノンの組み合わせならびに血管状態の処置
EP1918000A2 (en) 2003-11-05 2008-05-07 Schering Corporation Combinations of lipid modulating agents and substituted azetidinones and treatments for vascular conditions
EP1699759B1 (en) 2003-12-23 2010-10-20 AstraZeneca AB Diphenylazetidinone derivates possessing cholesterol absorption inhibitory activity
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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
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US7910698B2 (en) * 2006-02-24 2011-03-22 Schering Corporation NPC1L1 orthologues
BRPI0708556A2 (pt) * 2006-03-06 2011-05-31 Teva Pharma composição de ezetimiba
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CN101200443B (zh) * 2007-10-17 2011-06-29 中国药科大学 氮杂环丁酮衍生物、其制备方法及含有它们的药物组合
CA2754384A1 (en) 2009-03-06 2010-09-10 Lipideon Biotechnology Ag Pharmaceutical hypocholesterolemic compositions
CN101993403B (zh) * 2009-08-11 2012-07-11 浙江海正药业股份有限公司 氮杂环丁酮类化合物及医药应用
PL2844233T3 (pl) 2012-05-01 2020-09-07 Althera Life Sciences, Llc Preparat w postaci tabletki do stosowania doustnego składający się ze stałego połączenia rosuwastatyny i ezetymibu w leczeniu hiperlipidemii i chorób sercowo-naczyniowych
JP5969958B2 (ja) * 2013-06-27 2016-08-17 国立大学法人お茶の水女子大学 光学活性含フッ素アミノ酸類の製造方法
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
CN104860980B (zh) * 2015-04-23 2018-06-19 上海弈柯莱生物医药科技有限公司 一种用于合成依折麦布的中间体及其制备方法和应用
BR112019015107A2 (pt) 2017-01-23 2020-03-10 Dong Wha Pharm. Co., Ltd. Formulação de complexo compreendendo inibidor de hmg-coa redutase e clopidogrel

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Also Published As

Publication number Publication date
DK0751934T3 (da) 1999-12-13
CA2186364A1 (en) 1995-10-05
JP3524927B2 (ja) 2004-05-10
MX9604030A (es) 1997-09-30
CZ281596A3 (en) 1997-05-14
ATE183738T1 (de) 1999-09-15
NZ283528A (en) 1997-12-19
CN1144522A (zh) 1997-03-05
CA2186364C (en) 2008-12-30
EP0751934B1 (en) 1999-08-25
WO1995026334A1 (en) 1995-10-05
HUT74887A (en) 1997-02-28
HU221309B1 (en) 2002-09-28
FI963817A0 (fi) 1996-09-25
NO964008L (no) 1996-11-22
AU2159695A (en) 1995-10-17
DE69511687D1 (de) 1999-09-30
DE69511687T2 (de) 2000-03-16
AU686361B2 (en) 1998-02-05
EP0751934A1 (en) 1997-01-08
GR3031105T3 (en) 1999-12-31
US5627176A (en) 1997-05-06
PL316431A1 (en) 1997-01-06
JPH09510970A (ja) 1997-11-04
HU9602616D0 (en) 1996-11-28
KR970702246A (ko) 1997-05-13
US5688990A (en) 1997-11-18
KR100338171B1 (ko) 2002-11-23
FI963817A (fi) 1996-09-25
SK119796A3 (en) 1997-05-07
NO964008D0 (no) 1996-09-24

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