AR064429A1 - Derivados indolicos con anillo unidos en las posiciones 4,5, composiciones farmaceuticas que los contienen y usos de los mismos en la prevencion y/o tratamiento de infecciones virales. - Google Patents

Derivados indolicos con anillo unidos en las posiciones 4,5, composiciones farmaceuticas que los contienen y usos de los mismos en la prevencion y/o tratamiento de infecciones virales.

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AR064429A1
AR064429A1 ARP070105706A ARP070105706A AR064429A1 AR 064429 A1 AR064429 A1 AR 064429A1 AR P070105706 A ARP070105706 A AR P070105706A AR P070105706 A ARP070105706 A AR P070105706A AR 064429 A1 AR064429 A1 AR 064429A1
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alkyl
cycloalkyl
heterocycloalkyl
aryl
heteroaryl
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Schering Corp
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/58[b]- or [c]-condensed
    • C07D209/60Naphtho [b] pyrroles; Hydrogenated naphtho [b] pyrroles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

Composiciones farmacéuticas para tratar o prevenir una infeccion viral o un trastorno relacionado con virus en un paciente. Reivindicacion 1: Un compuesto que tiene la formula (1), o una sal aceptable para uso farmacéutico, solvatos, profármaco o éster del mismo donde el anillo Z de la formula (1) es un ciclohexilo, ciclohexenilo, heterocicloalquilo de 6 miembros, heterocicloalquenilo de 6 miembros, arilo de 6 miembros o heteroarilo de 6 miembros, donde el anillo Z puede estar: (i) sustituido en forma opcional sobre uno o más átomos de carbono anulares con sustituyentes, que son iguales o diferentes, y que se seleccionan de alquilo, alquenilo, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, halo, haloalquilo, hidroxialquilo, hidroxi, -CN, -C(O)R8, -C(O)OR9, -C(O)N(R9)2, -[C(R12)2]q-OR9, -[C(R12)2]qN(R9)2, -NHC(O)R8, -NHSO2R11, -S(O)pR11 o -SO2N(R9)2; y/o (ii) sustituido en forma opcional sobre un átomo de nitrogeno anular con sustituyentes, que son iguales o diferentes, y que se seleccionan de alquilo, arilo, haloalquilo, heteroarilo, hidroxialquilo, -C(O)R8, -C(O)OR9, -C(O)N(R9)2, -[C(R12)2]r-OR9, -[C(R12)2]rN(R9)2, -NHC(O)R8, -NHSO2R11, -S(O)pR11 o -SO2N(R9)2; R1 es un enlace, -[C(R12)2]r-, - [C(R12)2]r-O-[C(R12)2]q-, -[C(R12)2]r-N(R9)-[C(R12)2]q-, -[C(R12)2]q-CH=CH-[C(R12)2]q-, -[C(R12)2]q-C:::C-[C(R12)2]q- o -[C(R12)2]q-SO2-[C(R12)2]q-; R2 es -C(O)R9, -C(O)OR9, -C(O)OCH2OR9, -C(O)N(R9)2, -[C(R12)2]q-C(O)OR9, -[C(R12)2]q-C(O)N(R9)2, - [C(R12)2]q-C(O)N(R9)C=N(R9)2, -[C(R12)2]q-arilo, -[C(R12)2]q-cicloalquilo, -[C(R12)2]q-cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q-heteroarilo, -[C(R12)2]q-heterocicloalquenilo, -[C(R12)2]q-C(O)N(R9)SOR11, -[C(R12)2]q- C(O)N(R9)SO2R11, -[C(R12)2]q-C(O)N(R9)SO2N(R9)2, alquilo, grupo de formulas (2), donde un grupo arilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquenilo o heteroarilo puede estar sustituido en forma opcional con hasta 4 sustituyentes, que se seleccionan cada uno en forma independiente de alquilo, alquenilo, alquinilo, arilo, -[C(R12)2]q-cicloalquilo, -[C(R12)2]q-cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q-heterocicloalquenilo, -[C(R12)2]q- heteroarilo, -[C(R12)2]q-haloalquilo, -[C(R12)2]q-hidroxialquilo, halo, hidroxi, -OR9, -CN, -[C(R12)2]q-C(O)R8, -[C(R12)2]q-C(O)OR9, -[C(R12)2)q-C(O)N(R9)2, -[C(R12)2]q-OR9, -[C(R12)2]q-N(R9)2, -[C(R12)2]q-NHC(O)R8, -[C(R12)2]q-NR8C(O)N(R9)2, - [C(R12)2]q-NHSO2R11, -[C(R12)2]q-S(O)pR11, -[C(R12)2]q-SO2N(R9)2 y -SO2N(R9)C(O)N(R9)2; R3 es H, -[C(R12)2]q-alquilo, -[C(R12)2]q-arilo, -[C(R12)2]q-cicloalquilo, -[C(R12)2]q-cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q-heteroarilo o - [C(R12)2]q-heterocicloalquenilo, grupo de formulas (3) donde un grupo arilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquenilo o heteroarilo puede estar sustituido en forma opcional con hasta 3 sustituyentes, que son iguales o diferentes, y se seleccionan de alquilo, arilo, heteroaril-, halo, haloalquilo, hidroxialquilo, hidroxi, -CN, -C(O)R8, -C(O)OR9, -C(O)N(R9)2, -[C(R12)2]q-OR9, -[C(R12)2]q-N(R9)2, -NHC(O)R8, -NHSO2R11, -S(O)pR11 o -SO2N(R9)2; R6 y R7 son cada uno, en forma independiente, H, alquilo, alquenilo, alquinilo, arilo, -[C(R12)2]q-cicloalquilo, -[C(R12)2]q-cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q-heterocicloalquenilo, -[C(R12)2]q-heteroarilo, -[C(R12)2]q-haloalquilo, -[C(R12)2]q- hidroxialquilo, halo, hidroxi, -OR9, -CN, -[C(R12)2]q-C(O)R8, -[C(R12)2]q-C(O)OR9, -[C(R12)2)q-C(O)N(R9)2, -[C(R12)2]q-OR9, -[C(R12)2]q-N(R9)2, -[C(R12)2]q-NHC(O)R8, -[C(R12)2]q-NR8C(O)N(R9)2, -[C(R12)2]q-NHSO2R11, -[C(R12)2]q-S(O)pR11, -[C(R12)2]q- SO2N(R9)2 o -SO2N(R9)C(O)N(R9)2; cada aparicion de R8 es independientemente H, alquilo, alquenilo, alquinilo, -[C(R12)2]q-arilo, -[C(R12)2]q-cicloalquilo, -[C(R12)2]q-cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q-heterocicloalquenilo, - [C(R12)2]q-heteroarilo, haloalquilo o hidroxialquilo; cada aparicion de R9 es independientemente H, alquilo, alquenilo, alquinilo, -[C(R12)2]q-arilo, -[C(R12)2]q-cicloalquilo, -[C(R12)2]q-cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q- heterocicloalquenilo, -[C(R12)2]q-heteroarilo, haloalquilo o hidroxialquilo; R10 es H, cicloalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquenilo, arilo, heteroarilo, donde un grupo cicloalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquenilo, arilo o heteroarilo puede estar sustituido en forma opcional e independiente con hasta 4 sustituyentes, que se seleccionan en forma independiente de H, alquilo, alquenilo, alquinilo, arilo, -[C(R12)2]q-cicloalquilo, -[C(R12)2]q- cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q-heterocicloalquenilo, -[C(R12)2]q-heteroarilo, -[C(R12)2]q-haloalquilo, -[C(R12)2]q-hidroxialquilo, halo, hidroxi, -OR9, -CN, -[C(R12)2]q-C(O)R8, -[C(R12)2]q-C(O)OR9, -[C(R12)2]q- C(O)N(R9)2, -[C(R12)2]q-OR9, -[C(R12)2]q-N(R9)2, -[C(R12)2]q-NHC(O)R8, -[C(R12)2]q-NR8C(O)N(R9)2, -[C(R12)2]q-NHSO2R11, -[C(R12)2]q-S(O)pR11, -[C(R12)2]q-SO2N(R9)2 y -SO2N(R9)C(O)N(R9)2, de modo tal que cuando R1 es un enlace, R10 no es H; cada aparicion de R11 es independientemente alquilo, arilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquenilo, heteroarilo, haloalquilo, hidroxi o hidroxialquilo, donde un grupo cicloalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquenilo, arilo o heteroarilo puede estar sustituido en forma opcional e independiente con hasta 4 sustituyentes, que se seleccionan en forma independiente de -H, alquilo, alquenilo, alquinilo, arilo, -[C(R12)2]q-cicloalquilo, - [C(R12)2]q-cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q-heterocicloalquenilo, -[C(R12)2]q-heteroarilo, -[C(R12)2]q-haloalquilo, -[C(R12)2]q-hidroxialquilo, halo, hidroxi, -OR9, -CN, -[C(R12)2]q-C(O)R8, -[C(R12)2]q-C(O)OR9, -[C(R12)2]q- C(O)N(R9)2, -[C(R12)2]q-OR9, -[C(R12)2]q-N(R9)2, -[C(R12)2]q-NHC(O)R8, -[C(R12)2]q-NR8C(O)N(R9)2, -[C(R12)2]q-NHSO2alquilo, -[C(R12)2]q-NHSO2cicloalquilo, -[C(R12)2]q-NHSO2arilo, -[C(R12)2]q-SO2N(R9)2 y -SO2N(R9)C(O)N(R9)2; cada aparicion de R12 es independientemente H, halo, -N(R9)2, -OR9, alquilo, cicloalquilo, cicloalquenilo, heterocicloalquilo o heterocicloalquenilo, donde un grupo cicloalquilo, cicloalquenilo, heterocicloalquilo o heterocicloalquenilo puede estar sustituido en forma opcional e independiente con hasta 4 sustituyentes, que se seleccionan en forma independiente de alquilo, halo, haloalquilo, hidroxialquilo, hidroxi, -CN, -C(O)alquilo, -C(O)Oalquilo, -C(O)NHalquilo, -C(O)N(alquilo)2, -O-alquilo, -NH2, -NH(alquilo), -N(alquilo)2, -NHC(O)alquilo, -NHSO2aIquilo, -SO2alquiIo o -SO2NH-alquilo, o dos grupos R12, se unen con los átomos de carbono a los que están unidos, para formar un grupo cicloalquilo, heterocicloalquilo o C=O; cada aparicion de R20 es independientemente H, alquilo, arilo, cicloalquilo, heterocicloalquilo o heteroarilo, o ambos grupos R20 y los átomos de carbono a los que están unidos, se unen para formar un grupo cicloalquilo, cicloheteroalquilo, arilo o heteroarilo donde un cicloalquilo, cicloheteroalquilo, arilo o heteroarilo puede estar sustituido con hasta 4 grupos, que se seleccionan en forma independiente de alquilo, alquenilo, alquinilo, halo, hidroxi, -OR9, -CN, -[C(R12)2]q-cicloalquilo, -[C(R12)2]q- cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q-heterocicloalquenilo, -[C(R12)2]q-haloalquilo, -[C(R12)2]q-hidroxialquilo, -[C(R12)2]q-C(O)R8, -[C(R12)2]q-C(O)OR9, -[C(R12)2]q-C(O)N(R9)2, -[C(R12)2]q-OR9, -[C(R12)2]q-N(R9)2, -[C(R12)2]q- NHC(O)R8, -[C(R12)2]q-NR8C(O)N(R9)2, -[C(R12)2]q-NHSO2R11, -[C(R12)2]q-S(O)pR11, -[C(R12)2]q-SO2N(R9)2 y -SO2N(R9)C(O)N(R9)2; cada aparicion de R30 es independientemente H, alquilo, alquenilo, alquinilo, arilo, -[C(R12)2]q-cicloalquilo, -[C(R12)2]q- cicloalquenilo, -[C(R12)2]q-heterocicloalquilo, -[C(R12)2]q-heterocicloalquenilo, -[C(R12)2]q-heteroarilo, -[C(R12)2]q-haloalquilo, -[C(R12)2]q-hidroxialquilo, halo, hidroxi, -OR9, -CN, -[C(R12)2]q-C(O)R8, -[C(R12)2]q-C(O)OR9, -[C(R12)2]q- C(O)N(R9)2, -[C(R12)2]q-OR9, -[C(R12)2]q-N(R9)2, -[C(R12)2]q-NHC(O)R8, -[C(R12)2]q-NR8C(O)N(R9)2, -[C(R12)2]q-NHSO2R11, -[C(R12)2]q-S(O)pR11, -[C(R12)2]q-SO2N(R9)2 o -SO2N(R9)C(O)N(R9)2, o dos grupos R30 adyacentes, junto con los átomos de carbono a los que están unidos, se unen para formar un anillo de 3 a 7 miembros seleccionado de arilo, cicloalquilo, heteroarilo y heterocicloalquilo; cada aparicion de p es independientemente 0, 1 o 2; cada aparicion de q es independientemente un numero entero que oscila entre 0 y 4; y cada aparicion de r es independientemente un numero entero que oscila entre 1 y 4.
ARP070105706A 2006-12-22 2007-12-18 Derivados indolicos con anillo unidos en las posiciones 4,5, composiciones farmaceuticas que los contienen y usos de los mismos en la prevencion y/o tratamiento de infecciones virales. AR064429A1 (es)

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