AR034127A1 - Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento - Google Patents

Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento

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Publication number
AR034127A1
AR034127A1 ARP010103435A ARP010103435A AR034127A1 AR 034127 A1 AR034127 A1 AR 034127A1 AR P010103435 A ARP010103435 A AR P010103435A AR P010103435 A ARP010103435 A AR P010103435A AR 034127 A1 AR034127 A1 AR 034127A1
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Argentina
Prior art keywords
alkyl
aryl
heteroaryl
cycloalkyl
group
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ARP010103435A
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English (en)
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Schering Corp
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Publication of AR034127A1 publication Critical patent/AR034127A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/30Oxygen or sulfur atoms
    • C07D233/32One oxygen atom
    • C07D233/38One oxygen atom with acyl radicals or hetero atoms directly attached to ring nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Animal Behavior & Ethology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Imidazolidinonas, que comprenden un compuesto, que incluye enantiómeros, estereoisómeros, rotámeros y tautómeros de dicho compuesto, y sales o solvatos farmacéuticamente aceptable de dicho compuesto, donde dicho compuesto tiene la estructura general que se muestra en la fórmula (1), en la cual: R1 es COR5 ó B(OR)2, donde R5 está seleccionado del grupo que consiste en: H, OH, OR8, NR9R10, CF3, C2F5, C3F7, CF2R6, R6, y COR7, donde R7 es H, OH, OR8, CHR9R10, o NR9R10, donde R6, R8, R9 y R10 están independientemente seleccionados del grupo consistente en H, alquilo, arilo, heteroalquilo, heteroarilo, cicloalquilo, arilalquilo, heteroarilalquilo, CH(R1')COOR11, CH(R1')CONR12R13, CH(R1')CONHCH(R2')COOR11, CH(R1')CONHCH(R2')CONR12R13, CH(R1')CONHCH(R2')R', CH(R1')CONHCH(R2')CONHCH(R3')COOR11, CH(R1')CONHCH(R2')CONHCH(R3')CONR12R13, donde R1', R2', R3', R', R11, R12 y R13 están independientemente seleccionados de un grupo que consiste en H, alquilo, arilo, heteroalquilo, heteroarilo, cicloalquilo, alquil-arilo, alquil-heteroarilo, aril-alquilo y heteroaralquilo; Z es O, N, ó CH; X está seleccionado del grupo que consiste en: C=O, C=S y (CRR')p; p es un número de 1-6; G está seleccionado del grupo que consiste en: H, alquilo, arilo, heteroalquilo, heteroarilo, alquil-arilo y alquil-heteroarilo, con la condición de que G puede estar adicionalmente opcional y químicamente apropiadamente substituido con U11 o U12; R, R2 y R3 pueden ser iguales o diferentes y están independientemente seleccionados del grupo que consiste en H, alquilo C1-10, alquenilo C2-10, cicloalquilo C3-8, heterocicloalquilo C3-8, alcoxi, ariloxi, alquiltio, ariltio, amino, amido, éster, ácido carboxílico, carbamato, urea, cetona, aldehido, ciano, nitro, (cicloalquilo)alquilo y (heterocicloalquilo)alquilo, donde dicho cicloalquilo está constituido por C3-8, y 0-6 átomos de oxígeno, nitrógeno, azufre, o fósforo, y donde dicho alquilo tiene C1-6; arilo, heteroarilo, alquil-arilo, y alquil-heteroarilo; R4 puede estar presente o ausente, y si R4 está presente, R4 está seleccionado entre H, alquilo, o arilo; e Y está seleccionado del grupo que consiste en H, alquilo, arilo, heteroalquilo, heteroarilo, cicloalquilo, arilalquilo, heteroarilalquilo, y U, donde U está seleccionado entre alquil-arilo, aril-heteroarilo, alquil-heteroarilo, alquilcarbonilo, arilalquilcarbonilo, arilcarbonilo, heteroalquilcarbonilo, heteroarilcarbonilo, cicloalquilcarbonilo, alquiloxicarbonilo, alquil-ariloxicarbonilo, ariloxicarbonilo, arilalquiloxicarbonilo, heteroariloxicarbonilo, heterocicloalquiloxicarbonilo, cicloalquiloxicarbonilo, alquilaminocarbonilo, arilaminocarbonilo, alquil-arilaminocarbonilo, arilaminocarbonilo, arilalquilaminocarbonilo, heteroarilaminocarbonilo, cicloalquilaminocarbonilo, heterocicloalquilaminocarbonilo, alquilsulfonilo, arilsulfonilo, alquil-srilsulfonilo, arilalquilsulfonilo, cicloalquilsulfonilo, y heterocicloalquilsulfonilo, con al condición de que U puede estar adicionalmente opcionalmente y químicamente apropiadamente substituido con U11 ó U12; donde U11 es una porción alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquil-alquilo, heterociclilo, heterociclilalquilo, arilo, alquilarilo, arilalquilo, heteroarilo, alquilheteroarilo, o heteroarilalquilo, con la condición de que U11 puede estar adicionalmente opcionalmente substituido con U12; y U12 es una porción hidroxi, alcoxi, ariloxi, tio, alquiltio, ariltio, amino, alquilamino, arilamino, alquilsulfonilo, arilsulfonilo, alquilsulfonamido, arilsulfonamido, carboxi, carbalcoxi, carboxamido, alcoxicarbonilamino, alcoxicarboniloxi, alquilureido, halógeno, ciano, o nitro, con la condición de que alquilo, alcoxi, y arilo pueden estar adicionalmente opcionalmente substituidos por porciones independientes seleccionados de U12; y que dicha porción (1a) puede representar alternativamente un grupo arilalquiloxi; donde dichas porciones alquilo, heteroalquilo, alquenilo, heteroalquenilo, arilo, heteroarilo, cicloalquilo, y heterocicloalquilo pueden estar opcionalmente substituidas, donde dicho término "substituido" se refiere a una substitución opcional y apropiada con una o más porciones seleccionadas del grupo que consiste en alquilo, alquenilo, alquinilo, arilo, arilalquilo, cicloalquilo, heterocíclico, halógeno, hidroxi, tio, alcoxi, ariloxi, alquiltio, ariltio, amino, amido, éster, ácido carboxílico, carbamato, urea, cetona, aldehido, ciano, nitro, sulfonamida, sulfóxido, sulfona, sulfonilurea, hidrazina, e hidroxamato; que tienen una actividad inhibidora de proteasa de HCV. En otra realización, describe composiciones farmacéuticas que comprenden dichas imidazolidinonas así como también los métodos de su preparación y el uso de las mismas para la manufactura de un medicamento para tratar los desórdenes que están asociados con la proteasa HCV.
ARP010103435A 2000-07-21 2001-07-18 Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento AR034127A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US22011000P 2000-07-21 2000-07-21

Publications (1)

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AR034127A1 true AR034127A1 (es) 2004-02-04

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ARP010103435A AR034127A1 (es) 2000-07-21 2001-07-18 Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento

Country Status (10)

Country Link
US (1) US6838475B2 (es)
EP (1) EP1301486B1 (es)
JP (1) JP2004515464A (es)
AR (1) AR034127A1 (es)
AT (1) ATE435211T1 (es)
AU (1) AU2001282922A1 (es)
CA (1) CA2410766A1 (es)
DE (1) DE60139127D1 (es)
ES (1) ES2327819T3 (es)
WO (1) WO2002008198A2 (es)

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