AR055104A1 - Inhibidores macrociclicos del virus de la hepatitis c - Google Patents

Inhibidores macrociclicos del virus de la hepatitis c

Info

Publication number
AR055104A1
AR055104A1 ARP060103306A ARP060103306A AR055104A1 AR 055104 A1 AR055104 A1 AR 055104A1 AR P060103306 A ARP060103306 A AR P060103306A AR P060103306 A ARP060103306 A AR P060103306A AR 055104 A1 AR055104 A1 AR 055104A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
het
aryl
optionally substituted
Prior art date
Application number
ARP060103306A
Other languages
English (en)
Original Assignee
Tibotec Pharm Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37036843&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR055104(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of AR055104A1 publication Critical patent/AR055104A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

Reivindicacion 1: Un compuesto que tiene la formula (1), un N-oxido, sal de adicion, amina cuaternaria, complejo metálico y forma estereoquímicamente isomérica de éste, en el cual: la línea de punto representa un doble enlace opcional C7-8; R1 es arilo o un sistema anular saturado, parcialmente insaturado o completamente insaturado de 5 o 6 miembros o bicíclico heterocíclico de 9 a 12 miembros donde dicho sistema anular contiene un nitrogeno, y en forma opcional uno a tres heteroátomos adicionales seleccionados del grupo que consiste en oxígeno, azufre y nitrogeno, y donde el resto de los miembros del anillo son átomos de carbono; donde dicho sistema anular puede estar sustituido en forma opcional en cualquier átomo de carbono o nitrogeno del anillo con uno, dos, tres o cuatro sustituyentes seleccionados, cada uno en forma independiente, de; cicloalquilo C3-7, arilo, Het, -C(=O)NR5aR5b, -C(=O)R7, -C(=O)OR6a, y alquilo C1-6 sustituido en forma opcional con cicloalquilo C3-7, arilo, Het, -C(=O)NR5aR5b, -NR5aR5b, -C(=O)R7, -NR5aC(=O)R7, -NR5aSOpR8, -SOpR8, -SOpNR5aR5b, -C(=O) OR6, o -NR5aC(=O)OR6a; y donde los sustituyentes en cada átomo de carbono del anillo heterocíclico pueden seleccionarse, además de -OR8, - SR8, halo, polihaloalquilo C1-6, oxo, tio, ciano, nitro, azido, -NR5aR5b, -NR5aC(=O)R7, -NR5aSOpR8, -SOpR8, -SOpNR5aR5b, -C(O)OH, y - NR5aC(=O)OR6a; L es un enlace directo, -O-, -O-alcandiiloC1-4, -O-CO-, -O-C(=O)-NR5a- u -O-C(=O)-NR5a-alcandiiloC1-4; R2 representa hidrogeno, -OR6, -C(O)OR6, -C(O)R7, -C(O)NR5aR5b, -C(O)NHR5c, -NR5aR5b, -NHR5c, -NHSOpNR5aR5b, -NR5aSOpR8, o -B(OR6)2; R3 y R4 son hidrogeno o alquilo C1-6; o R3 y R4 tomados juntos pueden formar un anillo cicloalquilo C3-7; n es 3, 4, 5, o 6; p es 1 o 2; cada R5a y R5b son, en forma independiente, hidrogeno, cicloalquilo, C3-7, arilo, Het, alquilo C1-6 sustituido en forma opcional con halo, alcoxi, C1-6, ciano, polihaloalcoxi C1-6, cicloalquilo C3-7, arilo, o con Het; o R5a y R5b tomados junto con el átomo de nitrogeno al cual están unidos forman pirrolidinilo, piperidinilo, piperazinilo, 4-alquilpiperaziniloC1-6, 4-alquilcarbonoC1-6-piperazinilo y morfolinilo; donde los grupos morfolinilo y piperidinilo pueden estar sustituido en forma opcional con uno o dos radicales alquilo C1-6; R5c es cicloalquilo C3-7, arilo, Het, -O- cicloalquiloC3-7, -O-arilo, -O-Het, alquilo C1-6, o alcoxi C1-6, donde dicho alquilo C1-6 o alcoxi C1-6 pueden estar sustituidos, cada uno en forma independiente, con -C(=O)OR6, cicloalquilo C3-7, arilo, o Het; R6 es hidrogeno; alquenilo C2-6; Het; cicloalquilo C3-7 sustituido en forma opcional con alquilo C1-6; o alquilo C1-6sustituido en forma opcional con cicloalquilo C3-7, arilo o Het; R6a es alquenilo C2-6, cicloalquilo C3-7, Het, o alquilo C1-6 sustituido en forma opcional con cicloalquilo C3-7, arilo or Het; R7 es hidrogeno, alquilo C1-6, cicloalquilo C3-7, o arilo; R8 es hidrogeno, polihaloalquiloC1-6, arilo, Het, cicloalquilo C3-7 sustituido en forma opcional con alquilo C1-6, o alquilo C1-6 sustituido en forma opcional con cicloalquilo C3-7, arilo o Het; arilo como grupo o parte de un grupo es fenilo, naftilo, indanilo o 1,2,3,4-tetrahidronaftilo, cada uno de los cuales puede estar sustituido en forma opcional con uno, dos o tres sustituyentes seleccionados de halo, alquilo C1-6, polihaloalquilo C1-6, hidroxi, alcoxi C1-6, polihaloalcoxi C1-6, alcoxiC1-6-alquiloC1-6, carboxilo, alquilcarbonilo C1-6, alcoxicarbonilo C1-6, ciano, nitro, amino, mono- o dialquilamino C1-6, aminocarbonilo, mono- o dialquilaminocarbonilo C1-6, azido, mercapto, cicloalquilo C3-7, fenilo, piridilo, tiazolilo, pirazolilo, pirrolidinilo, piperidinilo, piperazinilo, 4- alquilpiperaziniloC1-6, 4-alquilcarbonilC1-6-piperazinilo, y morfolinilo; donde los grupos morfolinilo y piperidinilo pueden estar sustituidos en forma opcional con uno o dos radicales alquilo C1-6; y los grupos fenilo, piridilo, tiazolilo, pirazolilo pueden estar sustituidos en forma opcional con 1, 2 o 3 sustituyentes seleccionados, cada uno en forma independiente, de alquilo C1-6, alcoxi C1-6, halo, amino, mono- o dialquilamino C1-6; Het como grupo o parte de un grupo es un anillo heterocíclico saturado, parcialmente insaturado o completamente insaturado de 5 o 6 miembros que contiene 1 a 4 heteroátomos, seleccionado cada uno en forma independiente de nitrogeno, oxígeno y azufre, dicho anillo heterocíclico está condensado en forma opcional con un anillo bencénico, y donde el grupo Het como un todo puede estar sustituido en forma opcional con uno, dos o tres sustituyentes seleccionados, cada uno en forma independiente, del grupo que consiste en halo, alquilo C1-6, polihaloalquilo C1-6, hidroxi, alcoxi C1-6, polihaloalcoxi C1-6, alcoxiC1-6- alquiloC1-6, carboxilo, alquilcarbonilo, C1-6, alcoxicarbonilo C1-6, ciano, nitro, amino, mono- o dialquilamino C1-6, aminocarbonilo, mono- o dialquilaminocarbonilo C1-6, cicloalquilo C3-7, fenilo, piridilo, tiazolilo, pirazolilo, pirrolidinilo, piperidinilo, piperazinilo, 4-alquilpiperaziniloC1-6, 4-alquilcarbonilC1-6-piperazinilo, y morfolinilo; donde los grupos morfolinilo y piperidinilo pueden estar sustituidos en forma opcional con uno o dos radicales alquilo C1-6; y los grupos fenilo, piridilo, tiazolilo, pirazolilo pueden estar sustituidos en forma opcional con 1, 2 o 3 sustituyentes seleccionados, cada uno en forma independiente, de alquilo C1-6, alcoxi C1-6, halo, amino, mono- o dialquilamino C1-6.
ARP060103306A 2005-07-29 2006-07-28 Inhibidores macrociclicos del virus de la hepatitis c AR055104A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP05107067 2005-07-29
EP05107413 2005-08-11

Publications (1)

Publication Number Publication Date
AR055104A1 true AR055104A1 (es) 2007-08-08

Family

ID=37036843

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060103306A AR055104A1 (es) 2005-07-29 2006-07-28 Inhibidores macrociclicos del virus de la hepatitis c

Country Status (28)

Country Link
US (1) US7989471B2 (es)
EP (1) EP1912995B1 (es)
JP (1) JP5426163B2 (es)
KR (1) KR101074673B1 (es)
CN (1) CN101233137B (es)
AP (1) AP2473A (es)
AR (1) AR055104A1 (es)
AT (1) ATE517902T1 (es)
AU (1) AU2006274858B2 (es)
BR (1) BRPI0614670A2 (es)
CA (1) CA2617095C (es)
DK (1) DK1912995T3 (es)
EA (1) EA014646B1 (es)
GT (1) GT200600341A (es)
HK (1) HK1116772A1 (es)
IL (1) IL188283A (es)
JO (1) JO2768B1 (es)
MX (1) MX2008001395A (es)
MY (1) MY152153A (es)
NO (1) NO20081071L (es)
NZ (1) NZ564541A (es)
PE (1) PE20070221A1 (es)
SG (1) SG163613A1 (es)
SI (1) SI1912995T1 (es)
SV (1) SV2008002639A (es)
TW (1) TWI412534B (es)
UY (1) UY29705A1 (es)
WO (1) WO2007014919A1 (es)

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