AR044749A1 - Inhibidor de la arn polimerasa dependiente de arn del virus de la hepatitis c y composiciones y tratamientos que lo usan - Google Patents

Inhibidor de la arn polimerasa dependiente de arn del virus de la hepatitis c y composiciones y tratamientos que lo usan

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Publication number
AR044749A1
AR044749A1 ARP040100543A ARP040100543A AR044749A1 AR 044749 A1 AR044749 A1 AR 044749A1 AR P040100543 A ARP040100543 A AR P040100543A AR P040100543 A ARP040100543 A AR P040100543A AR 044749 A1 AR044749 A1 AR 044749A1
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AR
Argentina
Prior art keywords
cr8r9
aryl
alkyl
integer
membered heterocyclyl
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ARP040100543A
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English (en)
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Pfizer
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Publication of AR044749A1 publication Critical patent/AR044749A1/es

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    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/06—1,2,3-Thiadiazoles; Hydrogenated 1,2,3-thiadiazoles
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    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
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    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
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    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D407/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
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    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Abstract

La presente se refiere a métodos para el tratamiento del virus de la Hepatitis C en mamíferos por medio de la administración de los compuestos (1), y a composiciones farmacéuticas para tratar dichos trastornos, que contienen los compuestos de fórmula (1). La presente también se refiere a métodos para preparar los compuestos de fórmula (1). Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable, solvato o profármaco del mismo, caracterizado porque: W-Z es -C(=O)-C(-R3)(H)- o -C(-OR6)=C(-R3')-; cada R1 se selecciona independientemente entre hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo (C3-10), heterociclilo de 4 a 10 miembros y arilo C6-10, donde los grupos R1 anteriores, con la excepción de H, están opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados entre R4; R2 se selecciona entre el grupo de sustituyentes R1, -(CR8R9)t(arilo C6-10), -(CR8R9)t(heterociclilo de 4-10 miembros), -(CR8R9)qC(O)(CR8R9)t(arilo C6-10), -(CR8R9)qC(O)(CR8R9)t(heterociclilo de 4-10 miembros), -(CR8R9)tO(CR8R9)q(arilo C6-10), -(CR8R9)tO(CR8R9)q(heterociclilo de 4-10 miembros), -(CR8R9)qSOn(CR8R9)t(arilo C6-10) y -(CR8R9)qSOn(CR8R9)t(heterociclilo de 4-10 miembros), donde cada uno de q y t es independientemente un número entero de 0 a 5, n es un número entero de 0 a 2, los restos alquilo, cicloalquilo, arilo y heterociclilo de dichos grupos R2 están opcionalmente sustituidos con 1 a 5 grupos R4, y con la condición de que R2 nos sea H; R3 es hidrógeno, -OR6, -SR6, -NR6R7 y el grupo de sustituyentes R2; R3' se selecciona entre el grupo de sustituyentes R3, con la excepción de que R3' no sea H; cada R4 se selecciona independientemente entre halo, ciano, nitro, trifluorometoxi, trifluorometilo, azido, alquilo C1-10, alquenilo C2-6, alquinilo C2-6, -C(O)R6, -C(O)OR6, -OC(O)R6, -NR6C(O)R7, -NR6C(O)NR7, -C(O)NR6R7, -NR6R7, -NR6OR7, -SO2NR6R7, -NR6SO2R7, -(CR8R9)t(arilo C6-10) (donde t es un número entero de 0 a 5), -(CR8R9)t(heterociclilo de 4-10 miembros) (donde t es un número entero de 0 a 5), cicloalquilo C3-10, R6-O-, R6-SOn- (donde n es un número entero de 0 a 2) y oxo (=O), y donde los restos alquilo, arilo y heterociclilo de dichos grupos R4 están opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados entre R5; cada R5 se selecciona independientemente entre halo, trifluorometilo, trifluorometoxi, ciano, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -OR8, cicloalquilo C3-10, arilo C6-10, heterociclilo de 4 a 10 miembros, oxo (=O), -C(O)R6, -C(O)OR6, -OC(O)R6, -NR6C(O)R6, -NR6C(O)NR7, -C(O)NR6R7, -NR6R7, -NR6OR7, -NR6SO2R7 y -SO2NR6R7, donde los restos alquilo, arilo y heterociclilo de los grupos R5 anteriores están opcionalmente sustituidos con 1 a 3 R10; cada uno de R6 y R7 se seleccionan independientemente entre H, alquilo C1-6, cicloalquilo C3-10, -(CR8R9)t(arilo C6-10) y -(CR8R9)t(heterociclilo de 4-10 miembros), donde t es un número entero de 0 a 5, 1 ó 2 átomos de carbono del anillo del grupo heterocíclico están opcionalmente sustituidos con un resto oxo (=O), y los restos alquilo, arilo y heterociclilo de los grupos R6 y R7 anteriores están opcionalmente sustituidos con 1 a 3 halo, ciano, trifluorometilo, trifluorometoxi, alquilo C1-6, alcoxi C1-6, alquenilo C2-6, alquinilo C2-6, -(CR8R9)t(arilo C6-10) y -(CR8R9)t(heterociclilo de 4-10 miembros), donde t es un número entero de 0 a 5; cada uno de R8 y R9 se selecciona independientemente entre H y alquilo C1-4; y cada R10 se selecciona independientemente entre halo, ciano, trifluorometilo, trifluorometoxi, -C(O)O-R6, -OR6, -C(O)(CR8R9)pC(O)OR6, donde p es un número entero de 1 a 5, alquilo C1-6, alquenilo C2-6, alquinilo C2-6 y -NR6R7.
ARP040100543A 2003-02-21 2004-02-20 Inhibidor de la arn polimerasa dependiente de arn del virus de la hepatitis c y composiciones y tratamientos que lo usan AR044749A1 (es)

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US44908803P 2003-02-21 2003-02-21
US47235503P 2003-05-20 2003-05-20

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US (3) US7148226B2 (es)
EP (1) EP1597246A2 (es)
JP (1) JP3940430B2 (es)
AR (1) AR044749A1 (es)
AU (1) AU2004213247A1 (es)
BR (1) BRPI0407699A (es)
CA (1) CA2516235A1 (es)
IS (1) IS7896A (es)
MX (1) MXPA05007133A (es)
NL (1) NL1025544C2 (es)
PA (1) PA8596001A1 (es)
PE (1) PE20050289A1 (es)
TW (1) TW200426143A (es)
UY (1) UY28192A1 (es)
WO (1) WO2004074270A2 (es)

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