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

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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)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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
Publication number Priority date Publication date Assignee Title
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
IL156548A0 (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
DK1385548T3 (da) * 2001-01-26 2007-09-10 Schering Corp Kombinationer af sterolabsorptionsinhibitor(er) med (et eller flere) kardiovaskulære midler til behandling af vaskulære tilstande
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
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
CA2434488A1 (en) * 2001-01-26 2002-08-01 Harry R. Davis Combinations of nicotinic acid and derivatives thereof and sterol absorption inhibitor(s) and treatments for vascular indications
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
EP1911462A3 (en) * 2001-01-26 2011-11-30 Schering Corporation Compositions comprising a sterol absorption inhibitor
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
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
JP4711600B2 (ja) 2001-01-26 2011-06-29 シェーリング コーポレイション シト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の使用
EP1785144A3 (en) * 2001-01-26 2007-05-23 Shering Corporation Combinations of bile acid sequestrant(s) and sterol absorption inhibitor(s) and treatments for vascular indications
US7071181B2 (en) 2001-01-26 2006-07-04 Schering Corporation Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors
SI1413331T1 (sl) * 2001-01-26 2008-02-29 Schering Corp Kombinacije fenofibrata peroksisomskega proliferator aktivirajocega receptorja (PPAR) z ezetimib zaviralcem absorpcije sterola za vaskularne indikacije
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
US20020147184A1 (en) * 2001-01-26 2002-10-10 Schering Corporation Combinations of sterol absorption inhibitor(s) with blood modifier(s) for treating vascular conditions
US7053080B2 (en) 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
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
US7132415B2 (en) 2001-09-21 2006-11-07 Schering Corporation Methods and therapeutic combinations for the treatment of xanthoma 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
CA2504878A1 (en) 2002-11-06 2004-05-27 Schering Corporation Cholesterol absorption inhibitors for the treatment of demyelination
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
CN1756755A (zh) 2003-03-07 2006-04-05 先灵公司 取代的2－吖丁啶酮化合物、其制剂及其治疗高胆甾醇血症的用途
CN100439361C (zh) 2003-03-07 2008-12-03 先灵公司 取代的2-吖丁啶酮化合物、其制剂及其治疗高胆甾醇血症的用途
US7459442B2 (en) 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
CA2550215A1 (en) 2003-12-23 2005-07-07 Astrazeneca Ab Diphenylazetidinone derivates possessing cholesterol absorption inhibitory activity
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
PE20081877A1 (es) 2007-03-06 2008-12-27 Teijin Pharma Ltd Derivado de la 1,4-diarilacetidinona
US8858994B2 (en) 2007-12-10 2014-10-14 Ratiopharm Gmbh Pharmaceutical formulation comprising ezetimibe
US9212175B2 (en) 2009-03-06 2015-12-15 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
WO2015092448A1 (en) * 2013-12-18 2015-06-25 Rudjer Boskovic Institute Beta-lactam cholesterol absorption inhibitors

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CZ14294A3 (en) * 1991-07-23 1994-07-13 Schering Corp Substituted beta-lactam compounds usable as hypocholesterol pharmaceutical preparations and process for preparing thereof
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
AU2943095A (en) 1996-01-15
CA2191455A1 (en) 1995-12-28
JPH10501811A (ja) 1998-02-17
EP0766667A1 (en) 1997-04-09
WO1995035277A1 (en) 1995-12-28

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