WO2002058732A3 - Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications - Google Patents

Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications Download PDF

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Publication number
WO2002058732A3
WO2002058732A3 PCT/US2002/002009 US0202009W WO02058732A3 WO 2002058732 A3 WO2002058732 A3 WO 2002058732A3 US 0202009 W US0202009 W US 0202009W WO 02058732 A3 WO02058732 A3 WO 02058732A3
Authority
WO
WIPO (PCT)
Prior art keywords
activated receptor
peroxisome proliferator
activator
absorption inhibitor
combinations
Prior art date
Application number
PCT/US2002/002009
Other languages
French (fr)
Other versions
WO2002058732A2 (en
WO2002058732B1 (en
Inventor
Teddy Kosoglou
Harry R Davis
Gilles Jean Bernard Picard
Wing-Kee Philip Cho
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
Family has litigation
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Priority to SK50001-2012A priority Critical patent/SK288217B6/en
Priority to EP02714773A priority patent/EP1353696B1/en
Priority to JP2002559066A priority patent/JP4777602B2/en
Priority to MEP-278/08A priority patent/MEP27808A/en
Priority to CA002434682A priority patent/CA2434682C/en
Priority to YUP-586/03A priority patent/RS51449B/en
Priority to BR0206654-8A priority patent/BR0206654A/en
Priority to SK948-2003A priority patent/SK287988B6/en
Priority to DK02714773T priority patent/DK1353696T3/en
Priority to KR1020037009749A priority patent/KR100596257B1/en
Priority to SI200230471T priority patent/SI1353696T1/en
Priority to MXPA03006725A priority patent/MXPA03006725A/en
Priority to DE60216890T priority patent/DE60216890T2/en
Application filed by Schering Corp filed Critical Schering Corp
Priority to AU2002247019A priority patent/AU2002247019C1/en
Priority to NZ525921A priority patent/NZ525921A/en
Priority to IL15644502A priority patent/IL156445A0/en
Priority to HU1500186A priority patent/HU230253B1/en
Priority to HU0303915A priority patent/HUP0303915A3/en
Priority to DK04000161T priority patent/DK1413331T3/en
Publication of WO2002058732A2 publication Critical patent/WO2002058732A2/en
Priority to IL156445A priority patent/IL156445A/en
Publication of WO2002058732A3 publication Critical patent/WO2002058732A3/en
Priority to ZA2003/05693A priority patent/ZA200305693B/en
Priority to NO20033355A priority patent/NO331512B1/en
Publication of WO2002058732B1 publication Critical patent/WO2002058732B1/en
Priority to HK03109220A priority patent/HK1056696A1/en
Priority to CL200401174A priority patent/CL2004001174A1/en
Priority to IL191417A priority patent/IL191417A/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/02Halogenated hydrocarbons
    • A61K31/025Halogenated hydrocarbons carbocyclic
    • A61K31/03Halogenated hydrocarbons carbocyclic aromatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05Phenols
    • A61K31/055Phenols the aromatic ring being substituted by halogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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

Abstract

The present invention provides compositions, therapeutic combinations and methods including: (a) at least one peroxisome proliferator-activated receptor activator; and (b) at least one substituted azetidinone or substituted b-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.
PCT/US2002/002009 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications WO2002058732A2 (en)

Priority Applications (25)

Application Number Priority Date Filing Date Title
DK04000161T DK1413331T3 (en) 2001-01-26 2002-01-25 Combinations of the peroxisome proliferator-activated receptor (PPAR) activator fenofibrate and the sterol absorption inhibitor ezetimibe for vascular indications
NZ525921A NZ525921A (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (PPAR) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
AU2002247019A AU2002247019C1 (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (PPAR) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
MEP-278/08A MEP27808A (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
EP02714773A EP1353696B1 (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
YUP-586/03A RS51449B (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
BR0206654-8A BR0206654A (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferation-activated receptor (s) activator (s) and sterol absorption inhibitor (s) and treatments for vascular indications
SK948-2003A SK287988B6 (en) 2001-01-26 2002-01-25 Composition, oral dosage form and use thereof
DK02714773T DK1353696T3 (en) 2001-01-26 2002-01-25 Combinations of Peroxisome Proliferator Activated Receptor (PPAR) Activator (s) and Sterol Absorption Inhibitor (s) and Treatments for Vascular Indications
KR1020037009749A KR100596257B1 (en) 2001-01-26 2002-01-25 A composition comprising sterol absorption inhibitor, and a composition and a therapeutic combinations comprising peroxisome proliferator-activated receptorPPAR activator and sterol absorption inhibitor
SI200230471T SI1353696T1 (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
IL15644502A IL156445A0 (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
DE60216890T DE60216890T2 (en) 2001-01-26 2002-01-25 COMBINATIONS OF A STARTER ABSORPTION HEMMER AND A PPAR ACTIVATOR FOR THE TREATMENT OF CARDIOVASCULAR INDICATIONS
SK50001-2012A SK288217B6 (en) 2001-01-26 2002-01-25 Composition, therapeutic combination, pharmaceutical preparation and use thereof
JP2002559066A JP4777602B2 (en) 2001-01-26 2002-01-25 Combination of peroxisome proliferator activated receptor (PPAR) activator and sterol absorption inhibitor and treatment of vascular symptoms
CA002434682A CA2434682C (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
MXPA03006725A MXPA03006725A (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications.
HU1500186A HU230253B1 (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and their use in the treatment of vascular indications
HU0303915A HUP0303915A3 (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
IL156445A IL156445A (en) 2001-01-26 2003-06-15 Composition of sterol absorption inhibitor or therapeutic combination thereof with cholesterol biosynthesis inhibitor, which may further comprise peroxisome proliferator activated receptor (ppar) activator
ZA2003/05693A ZA200305693B (en) 2001-01-26 2003-07-23 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
NO20033355A NO331512B1 (en) 2001-01-26 2003-07-25 Composition comprising sterol absorption inhibitor, oral dosage form comprising the composition and use of the composition for the preparation of a medicament for co-administration with activator (s) of peroxisome proliferator-activated receptor (PPAR) for the treatment and / or prevention of vascular indications
HK03109220A HK1056696A1 (en) 2001-01-26 2003-12-18 Combinations of peroxisome proliferator-activated receptor (ppar) activator (S) and sterol absorption inhibitor (S) and treatments for vascular indications
CL200401174A CL2004001174A1 (en) 2001-01-26 2004-05-20 PHARMACEUTICAL COMPOSITION INCLUDING: 1- (4-FLUOROPHENYL) -3 (R) - [3- (4-FLUOROPHENYL) -3 (S) -HYDROXIPROPIL] -4 (S) - (4-HYDROXIFENYL) -2-ACETIDINONE ( EZETIMIBA) AND EXCIPIENTS; AND ITS USE IN THE TREATMENT AND / OR PREVENTION OF ATEROSCLEROSIS, HIPERCOLESTEROLEMIA, DAY
IL191417A IL191417A (en) 2001-01-26 2008-05-13 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US26439601P 2001-01-26 2001-01-26
US60/264,396 2001-01-26
US32383901P 2001-09-21 2001-09-21
US60/323,839 2001-09-21

Publications (3)

Publication Number Publication Date
WO2002058732A2 WO2002058732A2 (en) 2002-08-01
WO2002058732A3 true WO2002058732A3 (en) 2003-07-03
WO2002058732B1 WO2002058732B1 (en) 2003-09-12

Family

ID=26950511

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/002009 WO2002058732A2 (en) 2001-01-26 2002-01-25 Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications

Country Status (33)

Country Link
US (5) US20020151536A1 (en)
EP (2) EP1353696B1 (en)
JP (4) JP4777602B2 (en)
KR (1) KR100596257B1 (en)
CN (1) CN100509058C (en)
AR (2) AR033855A1 (en)
AT (2) ATE348649T1 (en)
AU (1) AU2002247019C1 (en)
BR (1) BR0206654A (en)
CA (3) CA2563051A1 (en)
CL (1) CL2004001174A1 (en)
CY (2) CY1108000T1 (en)
CZ (2) CZ301871B6 (en)
DE (2) DE60216890T2 (en)
DK (2) DK1413331T3 (en)
EC (1) ECSP11004702A (en)
ES (2) ES2290562T3 (en)
HK (2) HK1063607A1 (en)
HU (2) HU230253B1 (en)
IL (3) IL156445A0 (en)
ME (1) MEP27808A (en)
MX (1) MXPA03006725A (en)
NO (1) NO331512B1 (en)
NZ (1) NZ525921A (en)
PL (1) PL208110B1 (en)
PT (2) PT1353696E (en)
RS (2) RS20100015A (en)
RU (1) RU2356550C2 (en)
SI (2) SI1353696T1 (en)
SK (2) SK288217B6 (en)
TW (1) TWI337083B (en)
WO (1) WO2002058732A2 (en)
ZA (1) ZA200305693B (en)

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