AR043298A1 - Prodrogas 2' y 3' de nucleosidos para tratar infecciones de flaviviridae, composiciones farmaceuticas, sus usos en la manufactura de medicamentos y metodos de tratamiento - Google Patents

Prodrogas 2' y 3' de nucleosidos para tratar infecciones de flaviviridae, composiciones farmaceuticas, sus usos en la manufactura de medicamentos y metodos de tratamiento

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Publication number
AR043298A1
AR043298A1 ARP030102365A ARP030102365A AR043298A1 AR 043298 A1 AR043298 A1 AR 043298A1 AR P030102365 A ARP030102365 A AR P030102365A AR P030102365 A ARP030102365 A AR P030102365A AR 043298 A1 AR043298 A1 AR 043298A1
Authority
AR
Argentina
Prior art keywords
alkyl
acyl
group
formula
aryl
Prior art date
Application number
ARP030102365A
Other languages
English (en)
Original Assignee
Centre Nat Rech Scient
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=AR043298(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Centre Nat Rech Scient, Idenix Cayman Ltd, Univ Cagliari filed Critical Centre Nat Rech Scient
Publication of AR043298A1 publication Critical patent/AR043298A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids

Landscapes

  • 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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (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

En una realización los compuestos poseen la fórmula (1), o una sal aceptable para uso farmacéutico del mismo, donde: R1, R2 y R3 son en forma independiente H, fosfato o un fosfato estabilizado; alquilo de cadena lineal, ramifica o cíclica; acilo; CO-alquilo, CO-arilo, CO-alcoxialquilo, CO-ariloxialquilo, CO-arilo sustituido, éster de sulfonato, bencilo, donde el grupo bencilo es opcionalmente sustituido con uno o más sustituyentes; alquilsulfonilo, arilsulfonilo, aralquilsulfonilo, un lípido; un aminoácido; y residuo de aminoácido, un carbohidrato; un péptido; un colesterol; u otro grupo saliente aceptable para uso farmacéutico que al administrarse in vivo sea capaz de proveer un compuesto donde R1, R2 y/o R3 es en forma independiente H o fosfato; donde al menos uno de R2 y R3 no es hidrógeno; Y es hidrógeno, bromo, cloro, fluoro, yodo, OH, OR4, NH, NHR5, NR4R5, SH o SR4; X1 y X2 se seleccionan en forma independiente del grupo formado por H, alquilo de cadena lineal, ramificada o cíclica, CO-alquilo, CO-arilo, CO-alcoxialquilo, cloro, bromo, fluoro, yodo, OH, OR4, NH, NHR5, NR4R5, SH y SR4; y R4 y R5 son en forma independiente hidrógeno, acilo, o alquilo. En otra realización los compuestos poseen un resto de grupo de fórmula (2), o una sal farmacéuticamente aceptable de los mismos. R1, R2 y R3 son en forma independiente H, fosfato o un fosfato estabilizado; alquilo de cadena lineal, ramificada o cíclica; acilo; CO-alquilo, CO-arilo, CO-alcoxialquilo, CO-ariloxialquilo, CO-arilo sustituido, éster de sulfonato, bencilo, donde el grupo bencilo es opcionalmente sustituido con uno o más sustituyentes; alquilsulfonilo, arilsulfonilo, aralquilsulfonilo, un lípido; un aminoácido; y residuo de aminoácido, un carbohidrato; un péptido; un colesterol; u otro grupo saliente aceptable para uso farmacéutico que al menos al administrarse in vivo sea capaz de proveer un compuesto donde R1, R2 y/o R3 es en forma independiente H o fosfato; donde la menos uno de R2 y R3 no es hidrógeno; R6 es alquilo, CH3, CF3, azido, ciano, alquenilo, alquinilo, Br-vinilo, 2-Br-etilo, -C(O)O(alquilo), -C(O)O(alquilo inferior), -O(acilo), -O(acilo inferior), -O(alquilo), -O(alquilo inferior), -O(alquenilo), CF3, cloro, bromo, fluoro, yodo, NO2, NH2, -NH(alquilo inferior), -NH(acilo), -N(alquilo inferior)2, o -N(acil)2; y R7 y R9 son en forma independiente hidrógeno, OR2, hidroxi, alquilo incluyendo alquilo inferior, azido, ciano, alquenilo, alquinilo, Br-vinilo, -C(O)O(alquilo), -C(O)O(alquilo inferior), -O(acilo), -O(acilo inferior), -O(alquilo), -O(alquilo inferior), -O(alquenilo), cloro, bromo, yodo, NO2, NH2, -NH(alquilo inferior), -NH(acilo), -N(alquilo inferior)2, o -N(acil)2; donde al menos uno de R7 y R9 es OR2, donde cada R2 es en forma independiente fosfato incluyendo mono, di o tri-fosfato y un fosfato estabilizado; alquilo de cadena lineal, ramificada o cíclica; acilo (incluyendo acilo inferior); CO-alquilo, CO-arilo, CO-alcoxialquilo, CO-ariloxialquilo, CO-arilo sustituido, éster de sulfonato, incluyendo alquilo o arialquilo sulfonato incluyendo metanosulfonilo y bencilo donde el grupo fenilo es opcionalmente sustituido con uno o más sustituyentes como se define en la definición de arilo; alquilsulfonilo, arilsulfonilo, aralquilsulfonilo, un lípido; un aminoácido, un residuo de aminoácido, un carbohidrato; un péptido; un colesterol; u otro grupo saliente aceptable para uso farmacéutico que al administrarse in vivo sea capaz de proveer un compuesto donde R2 es H o fosfato; R8 y R10 son en forma independiente H, alquilo incluyendo alquilo inferior, cloro, bromo, o yodo; como alternativa, R7 y R10, R8 y R9, o R8 y R10 pueden unirse para formar un enlace pi; y X es O, S, SO2 o CH2; X1 y X2 se seleccionan en forma independiente del grupo formado por H, alquilo de cadena lineal, ramificado o cíclica, CO-alquilo, CO-arilo, CO-alcoxialquilo, cloro, bromo, fluoro, yodo, OH, OR4, NH, NHR5, NR4R5, SH y SR4; y R4 y R5 son en forma independiente hidrógeno, acilo, o alquilo. Una composición farmacéutica que comprende una cantidad eficaz de un compuesto de fórmula (1) a resto de grupo de fórmula (2), o una sal farmacéuticamente aceptable de los mismos para tratamiento y profilaxis una infección por Flaviviridae en un vehículo aceptable para uso farmacéutico. Un método para tratar un huésped infectado con un flavivirus o pestivirus, que comprende administrar al huésped que necesita dicho tratamiento una cantidad eficaz de un compuesto de fórmula (1) a resto de grupo de fórmula (2), o una sal farmacéuticamente aceptable o prodroga de los mismos, opcionalmente en un vehículo farmacéuticamente aceptable. El uso de un compuesto de fórmula (1) a resto de grupo de fórmula (2), o una sal farmacéuticamente aceptable o prodroga de los mismos, opcionalmente en la manufactura de un medicamento para el tratamiento de un huésped infectado con un virus Flaviviridae. Preferiblemente el huésped infectado es un humano. En una realización los compuestos de fórmula (1) a resto de grupo de fórmula (2), son manufacturados o usados con un segundo agente anti-viral. El segundo agente antiviral se selecciona del grupo formado por interferón, ribavirina, interleukina, un inhibidor de NS3 proteasa, inhibidor de cisteína proteasa, derivado de la tiazolidina, benzanilida, fenantrenequinona, un inhibidor de helicasa, un inhibidor de polimerasa, un análogo nucleótido, gliotoxina, cerulenina, oligodesoxinucléotidos de fosforotiato antisentido, inhibidor de la traducción IRES-dependiente, y una ribozima.
ARP030102365A 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 AR043298A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US39235002P 2002-06-28 2002-06-28
US39235102P 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
AR043298A1 true AR043298A1 (es) 2005-07-27

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

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Application Number Title Priority Date Filing Date
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

Country Status (27)

Country Link
EP (3) EP1523489B1 (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) TW200500375A (es)
UY (3) UY27875A1 (es)
WO (1) WO2004002999A2 (es)

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