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AR038823A1 - Composiciones farmaceuticas para inhibidores de proteasa viral de la hepatitis c - Google Patents

Composiciones farmaceuticas para inhibidores de proteasa viral de la hepatitis c

Info

Publication number
AR038823A1
AR038823A1 ARP030100386A ARP030100386A AR038823A1 AR 038823 A1 AR038823 A1 AR 038823A1 AR P030100386 A ARP030100386 A AR P030100386A AR P030100386 A ARP030100386 A AR P030100386A AR 038823 A1 AR038823 A1 AR 038823A1
Authority
AR
Argentina
Prior art keywords
pharmaceutically acceptable
cycloalkyl
alkyl
optionally
alkoxy
Prior art date
Legal status (The legal status 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 status listed.)
Suspension/Interruption
Application number
ARP030100386A
Other languages
English (en)
Inventor
Xiaohui Mei
Shirlynn Chen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH Co KG
Boehringer Ingelheim Pharmaceuticals Inc
Original Assignee
Boehringer Ingelheim Pharma GmbH Co KG
Boehringer Ingelheim Pharmaceuticals 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 Boehringer Ingelheim Pharma GmbH Co KG, Boehringer Ingelheim Pharmaceuticals Inc filed Critical Boehringer Ingelheim Pharma GmbH Co KG
Publication of AR038823A1 publication Critical patent/AR038823A1/es
Suspension/Interruption legal-status Critical Current

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
    • A61K31/435—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
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • 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
    • A61K9/145—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 compounds
    • 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
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Composiciones farmacéuticas de inhibidores de proteasa viral de hepatitis C que tienen una biodisponibilidad mejorada, y métodos para usar estas composiciones para inhibir la replicación del virus de la hepatitis C (HCV) y para el tratamiento de una infección de HCV. Estas composiciones incluyen sistemas de co-disolventes, sistemas basados en lípidos, dispersiones sólidas y granulaciones. Reivindicación 1: Una composición farmacéutica, que comprende: (a) un compuesto de fórmula (1), en la cual la línea de puntos indica un enlace opcional que forma un enlace doble entre las posiciones 13 y 14; R1 es H, alquilo C1-6, cicloalquilo C3-6, haloalquilo C1-6, alcoxi C1-6, cicloalcoxi C3-6, hidroxi o N(R5)2, en donde cada R5 es independientemente H, alquilo C1-6 o cicloalquilo C3-6; R2 es H, halo, alquilo C1-6, cicloalquilo C3-6, haloalquilo C1-6, tioalquilo C1-6, alcoxi C1-6, cicloalcoxi C3-6, alcoxialquilo C2-7, arilo C6 o C10 o Het, en donde Het es un heterociclo saturado o insaturado de cinco, seis o siete miembros que contiene de uno a cuatro heteroátomos en el anillo seleccionado entre N, O, y S; en que dicho cicloalquilo, arilo o Het está opcionalmente sustituido con R6; en donde R6 es H, halo, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, cicloalcoxi C3-6, NO2, N(R7)2, NH-C(O)-R7 o NH-C(O)-NH-R7 en donde cada R7 es independientemente H, alquilo C1-6 o cicloalquilo C3-6; o R6 es NH-C(O)-OR8 en donde R8 es alquilo C1-6 o cicloalquilo C3-6; R3 es R9O- o R9NH-, en donde R9 es alquilo C1-6 o cicloalquilo C3-6; R4 es H o de uno a tres sustituyentes en cualquier átomo de C disponible en las posiciones 8, 9, 10, 11, 12, 13 o 14, estando seleccionado dicho sustituyente independientemente entre el grupo que consiste en: alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, hidroxi, halo, amino, oxo, tio o tioalquilo C1-6 o un tautómero del mismo; (b) aproximadamente 0,1 a 10% en peso de una amina farmacéuticamente aceptable o una mezcla de aminas farmacéuticamente aceptables; (c) uno o más aceites, vehículos o disolventes hidrófilos farmacéuticamente aceptables; y cuando (c) es uno o más aceites farmacéuticamente aceptables, la composición farmacéutica comprende adicionalmente; (d) opcionalmente, uno o más disolventes hidrófilos farmacéuticamente aceptables; (e) opcionalmente, uno o más polímeros farmacéuticamente aceptables; y (f) opcionalmente, uno o más tensioactivos farmacéuticamente aceptables; y cuando (c) es uno o más vehículos farmacéuticamente aceptables, la composición farmacéutica comprende adicionalmente: (d) opcionalmente, uno o más tensioactivos farmacéuticamente aceptables.
ARP030100386A 2002-02-07 2003-02-07 Composiciones farmaceuticas para inhibidores de proteasa viral de la hepatitis c Suspension/Interruption AR038823A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US35569402P 2002-02-07 2002-02-07

Publications (1)

Publication Number Publication Date
AR038823A1 true AR038823A1 (es) 2005-01-26

Family

ID=27734548

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030100386A Suspension/Interruption AR038823A1 (es) 2002-02-07 2003-02-07 Composiciones farmaceuticas para inhibidores de proteasa viral de la hepatitis c

Country Status (25)

Country Link
US (1) US6828301B2 (es)
EP (1) EP1474172B1 (es)
JP (1) JP2005518423A (es)
KR (1) KR20040089605A (es)
CN (1) CN1627959A (es)
AR (1) AR038823A1 (es)
AT (1) ATE344056T1 (es)
AU (1) AU2003208989A1 (es)
BR (1) BR0307524A (es)
CA (1) CA2472249A1 (es)
CO (1) CO5611167A2 (es)
DE (1) DE60309433T2 (es)
EA (1) EA200400991A1 (es)
EC (1) ECSP045223A (es)
ES (1) ES2276045T3 (es)
HR (1) HRP20040720A2 (es)
IL (1) IL162673A0 (es)
MX (1) MXPA04007699A (es)
NO (1) NO20043722L (es)
PE (1) PE20030865A1 (es)
PL (1) PL371287A1 (es)
TW (1) TW200302734A (es)
UY (1) UY27650A1 (es)
WO (1) WO2003066103A1 (es)
ZA (1) ZA200405064B (es)

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