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MX9606319A - Compuestos de acetidinonas sustituidas utiles como agentes hipocolesterolemicos. - Google Patents

Compuestos de acetidinonas sustituidas utiles como agentes hipocolesterolemicos.

Info

Publication number
MX9606319A
MX9606319A MX9606319A MX9606319A MX9606319A MX 9606319 A MX9606319 A MX 9606319A MX 9606319 A MX9606319 A MX 9606319A MX 9606319 A MX9606319 A MX 9606319A MX 9606319 A MX9606319 A MX 9606319A
Authority
MX
Mexico
Prior art keywords
aryl
lower alkyl
coor6
substituted
hypocholesterolemic agents
Prior art date
Application number
MX9606319A
Other languages
English (en)
Inventor
Wayne Vaccaro
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 MX9606319A publication Critical patent/MX9606319A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • 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
    • C07D205/085—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 with a nitrogen atom directly attached in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

Landscapes

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

Abstract

Se presentan agentes hipocolesterolémicos de acetidinona sustituido de formula (I) o bien una sal farmacéuticamente aceptable de los mismos, donde: Arl es arilo o bien R3-arilo, Ar2 es arilo o bien R4-arilo; R1 se selecciona dentro del grupo que consiste de -(CH2)q-, donde q es 2-6; -(CH2)e-Z-(CH2)r, donde Z es -O-, -C(O)-, fenileno, -NR10- o -S(O)0-Z, e ES 0-5 y r es 0-5, a condicion que la suma de e y r sea 1-6; (alquenileno C2-C6)-; y (CH2)f-V-(CH2)g-, donde V es cicloalquileno C3-C6, f es 1-5 y g es 0-5, a condicion que la suma de f y g sea 1-6; R2 es -(alquileno inferior)-COR5 o bien (CH-CH)-COR5; R3 y R4 son independientemente 1-3 sustituyentes seleccionados entre alquilo inferior, -OR6, O(CO)R6, -O(CO)OR9, -O(CH2)1-SOR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -0(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -(alquileno inferior)-COOR6, -CH=CH-COOR6, -CF3, -CH, -NO2 y halogeno; R5 es -OR o bien - NRR12; R, R6, R7, R8 y R12 se seleccionan independientemente entre hidrogeno, alquilo inferior, arilo y alquilo inferior aril sustituido; R9 es alquilo inferior, arilo o alquilo inferior aril sustituido; y R10 es hidrogeno, alquilo inferior, aril alquilo inferior o bien -C(O)R6; se presentan también un método para disminuir el nivel de colesterol sérico mediante la administracion de dichos compuestos, solos o en combinacion con un inhibidor de la biosíntesis de colesterol, y composiciones farmacéuticas que los contienen.
MX9606319A 1994-06-20 1995-06-15 Compuestos de acetidinonas sustituidas utiles como agentes hipocolesterolemicos. MX9606319A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26178594A 1994-06-20 1994-06-20
PCT/US1995/007117 WO1995035277A1 (en) 1994-06-20 1995-06-15 Substituted azetidinone compounds useful as hypocholesterolemic agents

Publications (1)

Publication Number Publication Date
MX9606319A true MX9606319A (es) 1997-05-31

Family

ID=22994864

Family Applications (1)

Application Number Title Priority Date Filing Date
MX9606319A MX9606319A (es) 1994-06-20 1995-06-15 Compuestos de acetidinonas sustituidas utiles como agentes hipocolesterolemicos.

Country Status (6)

Country Link
EP (1) EP0766667A1 (es)
JP (1) JPH10501811A (es)
AU (1) AU2943095A (es)
CA (1) CA2191455A1 (es)
MX (1) MX9606319A (es)
WO (1) WO1995035277A1 (es)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
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US5633246A (en) * 1994-11-18 1997-05-27 Schering Corporation Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents
US6982251B2 (en) 2000-12-20 2006-01-03 Schering Corporation 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
DE10064402A1 (de) * 2000-12-21 2002-06-27 Aventis Pharma Gmbh Diphenylazetidinonderivate, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
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
AU2006203175B2 (en) * 2001-01-26 2008-07-24 Organon Llc Combinations of peroxisome proliferator-activated receptor (PPAR) activators(s) and sterol absorption inhibitors(s) and treatments for vascular indications
AU2007201970B2 (en) * 2001-01-26 2008-04-17 Organon Llc Combinations of peroxisome proliferator-activated receptor (PPAR) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
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
CN1915429B (zh) * 2001-01-26 2010-12-15 先灵公司 过氧化物酶体增殖物激活受体(ppar)活化剂和甾醇吸收抑制剂的组合药
US7071181B2 (en) 2001-01-26 2006-07-04 Schering Corporation Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors
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
EP1864680A3 (en) * 2001-01-26 2012-03-28 Schering Corporation Combinations of peroxisome proliferator-activated receptor (PPAR) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
EP1911462A3 (en) * 2001-01-26 2011-11-30 Schering Corporation Compositions comprising a sterol absorption inhibitor
ME00145B (me) 2001-01-26 2010-10-10 Merck Sharp & Dohme Upotreba supstituisanih jedinjenja azetidinona za lečenje sitosterolemije
AU2008201609B8 (en) * 2001-01-26 2009-01-08 Organon Llc Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitors(s) and treatments for vascular indications
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.
AU2006202618B2 (en) * 2001-01-26 2007-04-19 Organon Llc 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
ES2272776T3 (es) 2001-09-21 2007-05-01 Schering Corporation Tratamiento de xantomas con derivados de azetidinona como inhibidores de la absorcion de esterol.
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
US7053080B2 (en) 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
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
WO2004043457A1 (en) 2002-11-06 2004-05-27 Schering Corporation Cholesterol absorptions inhibitors for the treatment of autoimmune disorders
US7192944B2 (en) 2003-03-07 2007-03-20 Schering Corp. Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
DE602004018617D1 (de) 2003-03-07 2009-02-05 Schering Corp Substituierte azetidinon-derivate, deren pharmazeutische formulierungen und deren verwendung zur behandlung von hypercholesterolemia
US7459442B2 (en) 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
DE602004016123D1 (de) 2003-03-07 2008-10-09 Schering Corp Substituierte azetidinon-derivate, deren pharmazeutische formulierungen und deren verwendung zur behandlung von hypercholesterolemia
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
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
TW200806623A (en) * 2005-10-05 2008-02-01 Merck & Co Inc Anti-hypercholesterolemic compounds
TW200811098A (en) 2006-04-27 2008-03-01 Astrazeneca Ab Chemical compounds
EP2133347A4 (en) 2007-03-06 2010-03-17 Teijin Pharma Ltd 1-BIARYLAZETIDINONDERIVATE
UA103179C2 (ru) 2007-12-10 2013-09-25 Ратиофарм Гмбх Фармацевтическая композиция, которая содержит эзетимиб
EP2403848A1 (en) 2009-03-06 2012-01-11 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
US9926269B2 (en) * 2013-12-18 2018-03-27 Rudjer Boskovic Institute Beta-lactam cholesterol absorption inhibitors

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DE69222532T2 (de) * 1991-07-23 1998-02-26 Schering Corp Substituierte beta-lactam-verbindungen als hypocholesterolemische mittel und verfahren zu deren herstellung
US5631365A (en) * 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents

Also Published As

Publication number Publication date
WO1995035277A1 (en) 1995-12-28
JPH10501811A (ja) 1998-02-17
CA2191455A1 (en) 1995-12-28
AU2943095A (en) 1996-01-15
EP0766667A1 (en) 1997-04-09

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