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PE20040187A1 - Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo - Google Patents

Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo

Info

Publication number
PE20040187A1
PE20040187A1 PE2003000109A PE2003000109A PE20040187A1 PE 20040187 A1 PE20040187 A1 PE 20040187A1 PE 2003000109 A PE2003000109 A PE 2003000109A PE 2003000109 A PE2003000109 A PE 2003000109A PE 20040187 A1 PE20040187 A1 PE 20040187A1
Authority
PE
Peru
Prior art keywords
dispersion
inhibitor
phenyl
cetp
forming
Prior art date
Application number
PE2003000109A
Other languages
English (en)
Inventor
Marshall David Crew
William John Curatolo
Dwayne Thomas Friesen
Ravi Mysore Shanker
Douglas Alan Lorenz
James Alan Schriver Nightingale
Roger Benjamin Ruggeri
Michael Jon Gumkowski
Original Assignee
Pfizer Prod 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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of PE20040187A1 publication Critical patent/PE20040187A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds

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

Abstract

SE REFIERE A PROCEDIMIENTOS PARA FORMAR COMPOSICIONES FARMACEUTICAS QUE COMPRENDEN UNA DISPERSION AMORFA SOLIDA DE UN INHIBIDOR DE LA PROTEINA DE TRANSFERENCIA DE ESTERES DE COLESTERILO (CETP) Y UN POLIMERO QUE AUMENTA LA CONCENTRACION, MEDIANTE: a) POR UN PROCESADO EN DISOLVENTE,QUE CONSISTE EN FORMAR UNA SOLUCION QUE COMPRENDE UN INHIBIDOR DE CETP Y UN POLIMERO, EN UN DISOLVENTE COMUN PARA LUEGO ELIMINAR RAPIDAMENTE EL DISOLVENTE DE LA SOLUCION FORMANDO ASI LA DISPERSION, b) POR EXTRUSION EN ESTADO FUNDIDO, CONSISTE EN ALIMENTAR A UNA EXTRUSORA UN INHIBIDOR Y EL POLIMERO AMBOS SE EXTRUSIONA Y LUEGO SE SOLIDIFICAN FORMANDOSE UNA DISPERSION, c) POR CONGELACION EN ESTADO FUNDIDO, SE FORMA UNA MEZCLA FUNDIDA QUE COMPRENDE EL INHIBIDOR Y EL POLIMERO, LA MEZCLA SE ENFRIA FORMANDOSE LA DISPERSION. ENTRE LOS INHIBIDORES DE CETP SON PREFERIDOS: (4'S)-5'-(4-FLUOROFENIL)-6'-[(S)-FLUORO[4-(TRIFLUOROMETIL)FENIL]METIL]-3',4'-DIHIDRO-7'-(1-METILETIL)-ESPIRO[CICLOBUTANO-1,2'(1'H)-NAFTALEN]-4'-OL, (2R)-3-[[3-(4-CLORO-3-ETILFENOXI)FENIL][3-(1,1,2,2-TETRAFLUOROETOXI)FENIL]METIL]AMINO]-1,1,1-TRIFLUORO-2-PROPANOLOL, ENTRE OTROS. Y ENTRE LOS POLIMEROS SON SELECCIONADOS: CARBOXIMETILCELULOSA, COPOLIMERO POLIOXIETILENO-POLIOXIPROPILENO, ENTRE OTROS.ESTAS COMPOSICIONES PROPORCIONAN MEJORAS EN LA SOLUBILIDAD DE LOS INHIBIDORES CETP, PERMITIENDO REDUCIR LA DOSIFICACION REQUERIDA PARA OBTENER UNA EFICACIA ADECUADA
PE2003000109A 2002-02-01 2003-01-30 Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo PE20040187A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10/066,091 US7235259B2 (en) 2000-08-03 2002-02-01 Pharmaceutical compositions of cholesteryl ester transfer protein inhibitors

Publications (1)

Publication Number Publication Date
PE20040187A1 true PE20040187A1 (es) 2004-03-20

Family

ID=27658640

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003000109A PE20040187A1 (es) 2002-02-01 2003-01-30 Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo

Country Status (14)

Country Link
US (1) US7235259B2 (es)
EP (2) EP1469831A1 (es)
JP (1) JP2005523895A (es)
AR (1) AR038375A1 (es)
BR (1) BR0307277A (es)
CA (1) CA2474447A1 (es)
GT (1) GT200300021A (es)
MX (1) MXPA04006650A (es)
PA (1) PA8564901A1 (es)
PE (1) PE20040187A1 (es)
SV (1) SV2004001473A (es)
TW (1) TW200307565A (es)
UY (1) UY27639A1 (es)
WO (1) WO2003063832A1 (es)

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CA2474447A1 (en) 2003-08-07
SV2004001473A (es) 2004-05-07
EP1469831A1 (en) 2004-10-27
TW200307565A (en) 2003-12-16
US7235259B2 (en) 2007-06-26
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AR038375A1 (es) 2005-01-12
WO2003063832A1 (en) 2003-08-07
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EP2305217A1 (en) 2011-04-06
EP2305217B1 (en) 2014-07-30
US20030186952A1 (en) 2003-10-02
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