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AR086094A1 - Derivados nucleosidicos 2’-azido sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar enfermedades virales por vhc - Google Patents

Derivados nucleosidicos 2’-azido sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar enfermedades virales por vhc

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Publication number
AR086094A1
AR086094A1 ARP120101281A ARP120101281A AR086094A1 AR 086094 A1 AR086094 A1 AR 086094A1 AR P120101281 A ARP120101281 A AR P120101281A AR P120101281 A ARP120101281 A AR P120101281A AR 086094 A1 AR086094 A1 AR 086094A1
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AR
Argentina
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group
alkylene
alkyl
haloalkyl
aryl
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ARP120101281A
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English (en)
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Merck Sharp & Dohme
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    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
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    • A61K31/7072—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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
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    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
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    • A61K31/708—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 containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
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    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
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    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
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Abstract

Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1) o una sal farmacéuticamente aceptable del mismo, en la que: X es O, S o CH2; B es una base de purina o pirimidina natural o no natural, o B se selecciona entre uno de los restos del grupo de fórmulas (2); Y es N o -C(R19)-; Z es N o CH; R1 es H, o un resto del grupo de fórmulas (3); R2 es H o el resto de fórmula (4); o R1 y R2 se unen para formar un resto del grupo de fórmulas (5); R3 es alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, alquenilo C2-6, alquinilo C2-6 o cicloalquilo C3-7; cada uno de R4, R5, R7 y R8 es independientemente H, alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, halo, -OR20, -SR20 o -N(R20)2; cada uno de R6, R9, R10, R11 se selecciona independientemente entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, heteroarilo monocíclico de 5 ó 6 miembros, heteroarilo bicíclico de 9 ó 10 miembros, heterocicloalquilo de 4 a 7 miembros, halo, -OR20, -SR20, -S(O)R20, -S(O)2R20, -S(O)2N(R20)2, -NHC(O)OR20, -NHC(O)N(R20)2, haloalquilo C1-6, hidroxialquilo C1-6, -O-(haloalquilo C1-6), -CN, -NO2, -N(R20)2, -NH(alquileno C1-6)-(heteroarilo monocíclico de 5 ó 6 miembros), -NH(alquileno C1-6)-(heteroarilo bicíclico de 9 ó 10 miembros), -C(O)R20, -C(O)OR20, -C(O)N(R20)2 y -NHC(O)R20, en la que dicho grupo alquenilo C2-6 y dicho grupo alquinilo C2-6 pueden estar opcionalmente sustituidos con un grupo halo; cada aparición de R12 se selecciona independientemente entre H, -(alquileno C1-6)-T-R21, -(alquileno C1-6)m-(arilo C6-10), -(alquileno C1-6)m-(heterocicloalquilo de 4 a 7 miembros), -(alquileno C1-6)m-(heterocicloalquenilo de 4 a 7 miembros), -CH(arilo C6-10)-C(O)OR20 y el resto de fórmula (6), donde dicho resto arilo C6-10 de dicho grupo -(alquileno C1-6)m-(arilo C6-10), dicho resto heterocicloalquilo de 4 a 7 miembros de dicho grupo -(alquileno C1-6)m-(heterocicloalquilo de 4 a 7 miembros) y dicho resto heterocicloalquenilo de 4 a 7 miembros de dicho grupo -(alquileno C1-6)m-(heterocicloalquenilo de 4 a 7 miembros) puede ser opcionalmente sustituido con hasta tres grupos, cada uno seleccionado independientemente entre alquilo C1-6, halo, -OR20, haloalquilo C1-6, -N(R20)2, -C(O)OR20, -C(O)N(R20)2 y -NHC(O)R20; R13 es H, -(alquileno C1-6)-T-R21 o -(alquileno C1-6)m-(arilo C6-10), o R12 y R13 pueden unirse para formar un grupo alquileno C2-4 entre los átomos de oxígeno a los cuales R12 y R13 están unidos, donde dicho grupo alquileno C2-4 está sustituido con por lo menos un grupo arilo C6-10, donde dicho resto arilo C6-10 de dicho grupo -(alquileno C1-6)m-(arilo C6-10) puede ser opcionalmente sustituido con hasta tres grupos, cada uno seleccionado independientemente del grupo puede ser opcionalmente sustituido con hasta tres grupos, cada uno seleccionado independientemente entre alquilo C1-6, halo, -OR20, haloalquilo C1-6, -N(R20)2, -C(O)OR20, -C(O)N(R20)2 y -NHC(O)R20; R14 es H, arilo C6-10, heteroarilo monocíclico de 5 ó 6 miembros o heteroarilo bicíclico de 9 ó 10 miembros, en la que dicho grupo arilo C6-10, dicho grupo heteroarilo monocíclico de 5 ó 6 miembros y dicho grupo heteroarilo bicíclico de 9 ó 10 miembros pueden estar opcionalmente sustituidos con R22; R15 es H, alquilo C1-6, cicloalquilo C3-7, fenilo o bencilo, en la que dicho alquilo C1-6 puede estar opcionalmente sustituido con un grupo seleccionado entre halo, -OR20, -SR20, guanidino, -N(R20)2, -C(O)OR20, -C(O)N(R20)2, -NHC(O)R20, heteroarilo monocíclico de 5 ó 6 miembros y heteroarilo bicíclico de 9 ó 10 miembros, y en la que dicho grupo fenilo y dicho grupo bencilo pueden estar opcionalmente sustituidos con hasta 2 grupos, cada uno seleccionado independientemente entre alquilo C1-6, halo y -OR20; R16 es H, alquilo C1-6, cicloalquilo C3-7, fenilo o bencilo, en la que dicho alquilo C1-6 puede estar opcionalmente sustituido con un grupo seleccionado entre halo, -OR20, -SR20, guanidino, -N(R20)2, -C(O)OR20, -C(O)N(R20)2, -NHC(O)R20, heteroarilo monocíclico de 5 ó 6 miembros y heteroarilo bicíclico de 9 ó 10 miembros, y en la que dicho grupo fenilo y dicho grupo bencilo pueden estar opcionalmente sustituidos con hasta 2 grupos, cada uno seleccionado independientemente entre alquilo C1-6, halo y -OR20; R17 es H, alquilo C1-20, alquenilo C2-20, -(alquileno C1-3)m-cicloalquilo C3-7, -(alquileno C1-3)m-arilo C6-10 o adamantilo, en la que dicho grupo alquilo C1-20, dicho grupo alquenilo C2-20, dicho grupo arilo C6-10 y dicho grupo adamantilo pueden estar opcionalmente sustituidos con hasta tres grupos, cada uno seleccionado independientemente entre halo, -OR20, -C(O)OR20, CN, NO2, haloalquilo C1-6, hidroxialquilo C1-6, cicloalquilo C3-7, arilo C6-10, heteroarilo monocíclico de 5 ó 6 miembros, heteroarilo bicíclico de 9 ó 10 miembros, -N(R20)2, -C(O)N(R20)2, -SR20, -S(O)R20, -S(O)2R20, -S(O)2N(R20)2, -NHC(O)R20, -NHC(O)OR20 y -NHC(O)N(R20)2 y; R18 es H, alquilo C1-6, cicloalquilo C3-7, -(alquileno C1-3)m-arilo C6-10, (alquileno C1-3)-C(O)OR20, heteroarilo monocíclico de 5 ó 6 miembros, heteroarilo bicíclico de 9 ó 10 miembros, heterocicloalquilo de 4 a 7 miembros o el resto de fórmula (6), en la que dicho grupo arilo C6-10, dicho grupo heteroarilo monocíclico de 5 ó 6 miembros y dicho grupo heteroarilo bicíclico de 9 ó 10 miembros pueden estar opcionalmente sustituidos con hasta cinco grupos, cada uno seleccionado independientemente entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halo, -OR20, -SR20, haloalquilo C1-6, hidroxialquilo C1-6, -O-(haloalquilo C1-6), -CN, -NO2, -N(R20)2, -C(O)OR20, -C(O)N(R20)2 y -NHC(O)R20; R19 es H, alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, halo, -OR20, -SR20, N(R20)2, cicloalquilo C3-7, arilo C6-10, heteroarilo monocíclico de 5 ó 6 miembros o heteroarilo bicíclico de 9 ó 10 miembros; cada aparición de R20 es independientemente H, alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, -(alquileno C1-3)m-(cicloalquilo C3-7), -(alquileno C1-3)m-(arilo C6-10), -(alquileno C1-3)m-(heterocicloalquilo de 4 a 7 miembros), -(alquileno C1-3)m-(heteroarilo monocíclico de 5 ó 6 miembros) o -(alquileno C1-3)m-(heteroarilo bicíclico de 9 ó 10 miembros), en la que dicho grupo cicloalquilo C3-7, dicho grupo arilo C6-10, dicho grupo heterocicloalquilo de 4 a 7 miembros, dicho -(grupo heteroarilo monocíclico de 5 ó 6 miembros) o dicho grupo heteroarilo bicíclico de 9 ó 10 miembros puede estar opcionalmente sustituido con R26; cada aparición de R21 es independientemente H, alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquenilo C3-7, heteroarilo monocíclico de 5 ó 6 miembros, heteroarilo bicíclico de 9 ó 10 miembros, -OR20, -O-(haloalquilo C1-6) o -N(R20)2, en la que dicho grupo alquenilo C2-6, dicho grupo alquinilo C2-6, dicho grupo cicloalquilo C3-7, dicho grupo cicloalquenilo C3-7, dicho grupo arilo C6-10, dicho grupo heteroarilo monocíclico de 5 ó 6 miembros y dicho grupo heteroarilo bicíclico de 9 ó 10 miembros pueden estar opcionalmente sustituidos con hasta cinco grupos, cada uno seleccionado independientemente entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halo, -OR20, -SR20, haloalquilo C1-6, hidroxialquilo C1-6, -O-(haloalquilo C1-6), -CN, -NO2, -N(R20)2, -C(O)R20, -C(O)OR20, -C(O)N(R20)2 y -NHC(O)R20; R22 representa de uno a cinco grupos de sustituyentes, cada uno seleccionado independientemente entre alquilo C1-6, halo, -OR20, -SR20, haloalquilo C1-6, hidroxialquilo C1-6, -O-(haloalquilo C1-6), -CN, -NO2, -N(R20)2, -C(O)OR20, -C(O)N(R20)2 y -NHC(O)R20, o dos grupos R22 cualesquiera en los átomos de carbono adyacentes del anillo pueden combinarse para formar -O-R23-O-; R23 es -[C(R24)2]n-; cada aparición de R24 es independientemente H o alquilo C1-6; cada aparición de R25 es independientemente seleccionado entre H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, -(alquileno C1-3)m-(arilo C6-10), -(alquileno C1-6)m-(alquilo C1-6), -(alquileno C1-6)-C(O)O-(alquilo C1-6), heterocicloalquilo de 4 a 7 miembros, heteroarilo monocíclico de 5 ó 6 miembros y heteroarilo bicíclico de 9 ó 10 miembros, en la que dicho grupo alquilo C1-6, dicho grupo alquenilo C2-6, dicho grupo alquinilo C2-6, dicho grupo cicloalquilo C3-7, dicho grupo arilo C6-10, dicho grupo heterocicloalquilo de 4 a 7 miembros, dicho -(grupo heteroarilo monocíclico de 5 ó 6 miembros) o dicho grupo heteroarilo bicíclico de 9 ó 10 miembros puede estar opcionalmente sustituido con R26; o dos grupos R25, junto con el átomo de nitrógeno común al que están unidos, se unen para formar un grupo heterocicloalquilo de 4 a 7 miembros; R26 representa de uno a cinco grupos de sustituyentes, cada uno seleccionado independientemente entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halo, -OR27, -SR27, haloalquilo C1-6, hidroxialquilo C1-6, -O-(haloalquilo C1-6), -CN, -NO2, -N(R27)2, -C(O)OR27, -C(O)N(R27)2 y -NHC(O)R27; cada aparición de R27 es independientemente H, alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, -(alquileno C1-3)m-(cicloalquilo C3-7), -(alquileno C1-3)m-(arilo C6-10), -(alquileno C1-3)m-(heterocicloalquilo de 4 a 7 miembros), -(alquileno C1-3)m-(heteroarilo monocíclico de 5 ó 6 miembros) o -(alquileno C1-3)m-(heteroarilo bicíclico de 9 ó 10 miembros); R28 es H, alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquenilo C3-7, heteroarilo monocíclico de 5 ó 6 miembros, heteroarilo bicíclico de 9 ó 10 miembros, -OR20, -O-(haloalquilo C1-6) o -N(R20)2, en la que dicho grupo alquenilo C2-6, dicho grupo alquinilo C2-6, dicho grupo cicloalquilo C3-7, dicho grupo cicloalquenilo C3-7, dicho grupo arilo C6-10, dicho grupo heteroarilo monocíclico de 5 ó 6 miembros y dicho grupo heteroarilo bicíclico de 9 ó 10 miembros pueden estar opcionalmente sustituidos con hasta cinco grupos, cada uno seleccionado independientemente entre alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halo, -OR20, -SR20, haloalquilo C1-6, hidroxial
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