AR043101A1 - Ester de 2'-c-metil-3'-o-l-valina de ribofuranosilcitidina para el tratamiento de infecciones de flaviviridae, sus usos en la manufactura de medicamentos y metodos para el tratamiento de infecciones de flaviviridae - Google Patents

Ester de 2'-c-metil-3'-o-l-valina de ribofuranosilcitidina para el tratamiento de infecciones de flaviviridae, sus usos en la manufactura de medicamentos y metodos para el tratamiento de infecciones de flaviviridae

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Publication number
AR043101A1
AR043101A1 ARP030102363A ARP030102363A AR043101A1 AR 043101 A1 AR043101 A1 AR 043101A1 AR P030102363 A ARP030102363 A AR P030102363A AR P030102363 A ARP030102363 A AR P030102363A AR 043101 A1 AR043101 A1 AR 043101A1
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AR
Argentina
Prior art keywords
formula
interferon
compound
treatment
pharmaceutically acceptable
Prior art date
Application number
ARP030102363A
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English (en)
Original Assignee
Idenix Cayman Ltd
Univ Cagliari
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.)
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=30003988&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR043101(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Idenix Cayman Ltd, Univ Cagliari filed Critical Idenix Cayman Ltd
Publication of AR043101A1 publication Critical patent/AR043101A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/10Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • C07H19/20Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Un compuesto que posee la estructura de fórmula (1), o sal farmacéuticamente aceptable o prodroga del mismo, opcionalmente en un vehículo farmacéuticamente aceptable para uso en el tratamiento de un huésped infectado con Flaviviridae. En una realización particular, la sal farmacéuticamente aceptable es una sal de hidrocloruro de la fórmula (2), en otra realización la sal farmacéuticamente aceptable de fórmula (1) se selecciona de tosilato, metansulfonato, acetato, citrato, malonato, tartarato, succinato, benzoato, ascorbato, alfa-acetoglutarato y alfa-glicerofosfato, formato, fumarato, propionato, glicolato, lactato, piruvato, oxalato, maleato, salicilato, sulfato, sulfonato, nitrato, bicarbonato, hidrobromato, hidrobromuro, hidroioduro, carbonato y sales de ácido fosfórico. Un compuesto de fórmula (1) o (2), en donde el grupo 5'-hidroxilo se reemplaza con un 5'-OR, donde R es fosfato; una prodroga de fosfato estabilizado; acilo; alquilo; éster de sulfonato, incluyendo alquilo o arilalquil sulfonilo, incluyendo metanosulfonilo y bencilo, donde el grupo fenilo está opcionalmente sustituido; un lípido; un aminoácido; un hidrato de carbono; un péptido; colesterol; u otro grupo saliente aceptable para el uso farmacéutico que, cuando se administra in vivo, es capaz de proveer un compuesto donde R es independientemente H o fosfato. Una composición farmacéutica que comprende una cantidad efectiva del compuesto de fórmula (1) ó fórmula (2) o una sal del mismo aceptable para el uso farmacéutico, para tratar una infección de Flaviviridae, en un vehículo aceptable para el uso farmacéutico. Los compuestos de fórmula (1) ó fórmula (2) son útiles para el tratamiento y profilaxis de infecciones de Flaviviridae incluyendo infecciones del virus Hepatitis C (VHC). Un método para el tratamiento de un huésped infectado con un flavivirus o pestivirus, comprendiendo administrar a un huésped en necesidad de ello una cantidad efectiva de un compuesto que posee la estructura de la fórmula (1) o (2) o una sal farmacéuticamente aceptable o prodroga del mismo opcionalmente en un vehículo farmacéuticamente aceptable. Uso de un compuesto que posee la estructura de fórmula (1) o (2) o una sal farmacéuticamente aceptable o prodroga del mismo opcionalmente en la manufactura de un medicamento para el tratamiento de un huésped infectado con un flavivirus o pestivirus. Preferiblemente el huésped infectado es un humano. En una realización el compuesto de fórmula (1) ó (2) es manufacturado en combinación con un segundo agente anti-viral. El segundo agente anti-viral se selecciona del grupo que consiste en interferón, ribavirina, una interleuquina, un inhibidor de proteasa NS3, un inhibidor de proteasa de cisteina, un derivado de tiazolidina, tiazolidina, benzanilida, fenantrenequinona, un inhibidor de helicasa, un inhibidor de polimerasa, un análogo de nucleótido, gliotoxina, cerutenina, fosforotiato oligodesoxinucleótidos antisentido, inhibidores de la traducción dependiente de IRES, una ribozima, interferón alfa 2a pegilado, interferón alfacon-1, interferón natural, albuferón, interferón beta-1a, omega interferón, interferón alfa, interferón gamma, interferón tau, interferón delta e interferón gamma-1b. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1), o una sal del mismo aceptable para el uso farmacéutico.
ARP030102363A 2002-06-28 2003-06-30 Ester de 2'-c-metil-3'-o-l-valina de ribofuranosilcitidina para el tratamiento de infecciones de flaviviridae, sus usos en la manufactura de medicamentos y metodos para el tratamiento de infecciones de flaviviridae AR043101A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US39235102P 2002-06-28 2002-06-28
US39235002P 2002-06-28 2002-06-28
US46619403P 2003-04-28 2003-04-28
US47094903P 2003-05-14 2003-05-14

Publications (1)

Publication Number Publication Date
AR043101A1 true AR043101A1 (es) 2005-07-20

Family

ID=30003988

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP030102365A AR043298A1 (es) 2002-06-28 2003-06-30 Prodrogas 2' y 3' de nucleosidos para tratar infecciones de flaviviridae, composiciones farmaceuticas, sus usos en la manufactura de medicamentos y metodos de tratamiento
ARP030102363A AR043101A1 (es) 2002-06-28 2003-06-30 Ester de 2'-c-metil-3'-o-l-valina de ribofuranosilcitidina para el tratamiento de infecciones de flaviviridae, sus usos en la manufactura de medicamentos y metodos para el tratamiento de infecciones de flaviviridae

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP030102365A AR043298A1 (es) 2002-06-28 2003-06-30 Prodrogas 2' y 3' de nucleosidos para tratar infecciones de flaviviridae, composiciones farmaceuticas, sus usos en la manufactura de medicamentos y metodos de tratamiento

Country Status (27)

Country Link
EP (3) EP2332952B1 (es)
JP (7) JP2005533817A (es)
KR (1) KR20050048544A (es)
CN (6) CN102424698A (es)
AP (1) AP2005003212A0 (es)
AR (2) AR043298A1 (es)
AU (1) AU2003247084B9 (es)
BR (2) BR0312271A (es)
CA (1) CA2490191C (es)
CY (2) CY1115417T1 (es)
DE (1) DE14169110T1 (es)
DK (1) DK1523489T3 (es)
ES (1) ES2469569T3 (es)
HK (3) HK1204624A1 (es)
IL (1) IL165893A0 (es)
MA (1) MA27375A1 (es)
MX (1) MXPA04012709A (es)
MY (1) MY140819A (es)
NO (3) NO330755B1 (es)
PE (3) PE20040635A1 (es)
PL (1) PL374831A1 (es)
PT (1) PT1523489E (es)
RS (1) RS114004A (es)
RU (1) RU2483075C2 (es)
TW (3) TW200500374A (es)
UY (3) UY27875A1 (es)
WO (1) WO2004002999A2 (es)

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