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AR083792A1 - PHARMACEUTICAL COMPOSITION TO TREAT HCV INFECTIONS - Google Patents

PHARMACEUTICAL COMPOSITION TO TREAT HCV INFECTIONS

Info

Publication number
AR083792A1
AR083792A1 ARP110104158A ARP110104158A AR083792A1 AR 083792 A1 AR083792 A1 AR 083792A1 AR P110104158 A ARP110104158 A AR P110104158A AR P110104158 A ARP110104158 A AR P110104158A AR 083792 A1 AR083792 A1 AR 083792A1
Authority
AR
Argentina
Prior art keywords
formula
pyrimidin
furan
fluorine
amino
Prior art date
Application number
ARP110104158A
Other languages
Spanish (es)
Inventor
Michael Thomas Brandl
Karen Elizabeth Olocco
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR083792A1 publication Critical patent/AR083792A1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Biotechnology (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Reivindicación 1: Una composición sólida de tableta o de cápsula de uso oral formada por un primer componente granular que contiene la 4-amino-1-((2R,3R,4R,5R)-3-flúor-4-hidroxi-5-hidroximetil-3-metil-tetrahidro-furan-2-il)-1H-pirimidin-2-ona de fórmula (1a) y por lo menos un ingrediente farmacéuticamente activo antiviral adicional elegido entre el grupo formado por el 4-flúor-1,3-dihidro-isoindol-2-carboxilato de (Z)-(1S,4R,6S,14S,18R)-14-tert-butoxicarbonilamino-4-ciclopropanosulfonilaminocarbonil-2,15-dioxo-3,16-diaza-triciclo[14.3.0.04,6]nonadec-7-en-18-ilo de fórmula (2), el isobutirato de (2R,3R,4R,5R)-5-(4-amino-2-oxo-2H-pirimidin-1-il)-4-flúor-2-isobutiriloximetil-4-metil-tetra-hidro-furan-3-ilo de fórmula (1b) y el isobutirato de (2R,3S,4R,5R)-5-(4-amino-2-oxo-2H-pirimidin-1-il)-2-azido-3,4-bis-isobutiril-oxi-tetrahidro-furan-2-ilmetilo de fórmula (3) y un aglutinante.Reivindicación 13: Uso de una composición según una cualquiera de las reivindicaciones de 1 a 12 para el tratamiento de infecciones del HCV.Claim 1: A solid tablet or capsule composition for oral use formed by a first granular component containing 4-amino-1 - ((2R, 3R, 4R, 5R) -3-fluorine-4-hydroxy-5- hydroxymethyl-3-methyl-tetrahydro-furan-2-yl) -1 H -pyrimidin-2-one of formula (1a) and at least one additional pharmaceutically active antiviral ingredient chosen from the group consisting of 4-fluorine-1, (Z) 3-dihydro-isoindole-2-carboxylate (1S, 4R, 6S, 14S, 18R) -14-tert-butoxycarbonylamino-4-cyclopropanesulfonylaminocarbonyl-2,15-dioxo-3,16-diaza-tricycle [ 14.3.0.04.6] nonadec-7-en-18-yl of formula (2), the isobutyrate of (2R, 3R, 4R, 5R) -5- (4-amino-2-oxo-2H-pyrimidin-1 -yl) -4-fluorine-2-isobutyryloxymethyl-4-methyl-tetra-hydro-furan-3-yl of formula (1b) and the isobutyrate of (2R, 3S, 4R, 5R) -5- (4-amino -2-oxo-2H-pyrimidin-1-yl) -2-azido-3,4-bis-isobutyryl-oxy-tetrahydro-furan-2-ylmethyl of formula (3) and a binder. Claim 13: Use of a composition according to any one of claims 1 to 1 2 for the treatment of HCV infections.

ARP110104158A 2010-11-09 2011-11-08 PHARMACEUTICAL COMPOSITION TO TREAT HCV INFECTIONS AR083792A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US41181010P 2010-11-09 2010-11-09

Publications (1)

Publication Number Publication Date
AR083792A1 true AR083792A1 (en) 2013-03-20

Family

ID=45044542

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104158A AR083792A1 (en) 2010-11-09 2011-11-08 PHARMACEUTICAL COMPOSITION TO TREAT HCV INFECTIONS

Country Status (3)

Country Link
AR (1) AR083792A1 (en)
TW (1) TW201300106A (en)
WO (1) WO2012062691A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6122879B2 (en) * 2012-06-05 2017-04-26 武田薬品工業株式会社 Solid preparation

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1633766B1 (en) 2003-05-30 2019-03-06 Gilead Pharmasset LLC Modified fluorinated nucleoside analogues
RS20110578A3 (en) 2003-10-14 2016-02-29 F. Hoffmann-La Roche Ltd Macrocyclic carboxylic acids and acyl sulfonamides as inhibitors of hcv replication
JP4979710B2 (en) 2005-12-09 2012-07-18 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Antiviral nucleoside
ATE482690T1 (en) * 2005-12-14 2010-10-15 Hoffmann La Roche HCV PRODRUG FORMULATION
DK2389164T3 (en) * 2009-01-21 2014-09-15 Hoffmann La Roche PHARMACEUTICAL COMPOSITIONS INCLUDING AN HCV POLYMERASE INHIBITOR PRO DRUG
AR075584A1 (en) * 2009-02-27 2011-04-20 Intermune Inc THERAPEUTIC COMPOSITIONS THAT INCLUDE beta-D-2'-DESOXI-2'-FLUORO-2'-C-METHYLYCTIDINE AND A CARDIEX ISOINDOL ACID DERIVATIVE AND ITS USES. COMPOUND.

Also Published As

Publication number Publication date
TW201300106A (en) 2013-01-01
WO2012062691A1 (en) 2012-05-18

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Legal Events

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