AR082960A1 - Uso de analogos de carba-nucleosidos-2-fluor sustituidos para preparar medicamentos para el tratamiento de infecciones por virus de la influenza, y compuestos relacionados - Google Patents

Uso de analogos de carba-nucleosidos-2-fluor sustituidos para preparar medicamentos para el tratamiento de infecciones por virus de la influenza, y compuestos relacionados

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AR082960A1
AR082960A1 ARP110103311A ARP110103311A AR082960A1 AR 082960 A1 AR082960 A1 AR 082960A1 AR P110103311 A ARP110103311 A AR P110103311A AR P110103311 A ARP110103311 A AR P110103311A AR 082960 A1 AR082960 A1 AR 082960A1
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alkyl
independently
substituted
alkynyl
alkenyl
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Gilead Sciences Inc
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    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
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    • C07H7/06Heterocyclic radicals

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Abstract

Reivindicación 1: Uso de un compuesto de fórmula (1) o una de sus sales o ésteres farmacéuticamente aceptables; donde cada R1 es H o halógeno; cada R2 es halógeno; cada R3 o R5 es de manera independiente, H, ORa, N(Ra)2, N3, CN, NO2, S(O)nRa, halógeno, alquilo C1-8, carbociclilalquilo C4-8, alquilo C1-8 sustituido, alquenilo C2-8, alquenilo C2-8 sustituido, alquinilo C2-8 o alquinilo C2-8 sustituido; R6 es H, ORa, N(Ra)2, N3, CN, NO2, S(O)nRa, -C(=O)R11, -C(=O)OR11, -C(=O)NR11R12, -C(=O)SR11, -S(O)R11, -S(O)2R11, -S(O)(OR11), -S(O)2(OR11), -SO2NR11R12, halógeno, alquilo C1-8, carbociclilalquilo C4-8, alquilo C1-8 sustituido, alquenilo C2-8, alquenilo C2-8 sustituido, alquinilo C2-8, alquinilo C2-8 sustituido o arilalquilo C1-8; cada n es, de manera independiente, 0, 1 ó 2; cada Ra es, de manera independiente, H, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, arilalquilo C1-8, carbociclilalquilo C4-8, -C(=O)R11, -C(=O)OR11, -C(=O)NR11R12, -C(=O)SR11, -S(O)R11, -S(O)2R11, -S(O)(OR11), -S(O)2(OR11), o -SO2NR11R12; R7 es H, -C(=O)R11, -C(=O)OR11, -C(=O)NR11R12, -C(=O)SR11, -S(O)R11, -S(O)2R11, -S(O)(OR11), -S(O)2(OR11), -SO2NR11R12, o bien un resto de fórmula (2); cada Y o Y1 es, de manera independiente, O, S, NR, +N(O)(R), N(OR), +N(O)(OR), o N-NR2; W1 y W2, cuando se los toma en conjunto, son -Y3(C(Ry)2)3Y3-; o uno de W1 o W2 en conjunto con R3 es -Y3- y el otro de W1 o W2 tiene la fórmula (3); cada uno de W1 y W2 es, de manera independiente, un grupo de la fórmula (3), donde cada Y2 es, de manera independiente, una unión, O, CR2, NR, +N(O)(R), N(OR), +N(O)(OR), N-NR2, S, S-S, S(O), o S(O)2; cada Y3 es, de manera independiente, O, S, o NR; M2 es 0, 1 ó 2; cada Rx es, de manera independiente, Ry o la fórmula (4) donde cada M1a, M1c, y M1d es, de manera independiente, 0 ó 1; M12c es 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 ó 12; cada Ry es, de manera independiente, H, F, Cl, Br, I, OH, R, -C(=Y1)R, -C(=Y1)OR, -C(=Y1)N(R)2, -N(R)2, -+N(R)3, -SR, -S(O)R, -S(O)2R, -S(O)(OR), -S(O)2(OR), -OC(=Y1)R, -OC(=Y1)OR, -OC(=Y1)(N(R)2), -SC(=Y1)R, -SC(=Y1)OR, -SC(=Y1)(N(R)2), -N(R)C(=Y1)R, -N(R)C(=Y1)OR, -N(R)C(=Y1)N(R)2, -SO2NR2, -CN, -N3, -NO2, -OR, o W3; o cuando se los toma en conjunto, dos Ry en el mismo átomo de carbono forman un anillo carbocíclico de entre 3 y 7 átomos de carbono; cada R es, de manera independiente, H, alquilo C1-8, alquilo C1-8 sustituido, alquenilo C2-8, alquenilo C2-8 sustituido, alquinilo C2-8, alquinilo C2-8 sustituido, arilo C6-20, arilo C6-20 sustituido, heterociclilo C2-20, heterociclilo C2-20 sustituido, arilalquilo o arilalquilo sustituido; W3 es W4 o W5; W4 es R, -C(Y1)Ry, -C(Y1)W5, -SO2Ry, o -SO2W5; y W5 es un carbociclo o un heterociclo donde W5 está, de manera independiente, sustituido con 0 a 3 grupos Ry; cada R8 es halógeno, NR11R12, N(R11)OR11, NR11NR11R12, N3, NO, NO2, CHO, CN, -CH(=NR11), -CH=NNHR11, -CH=N(OR11), -CH(OR11)2, -C(=O)NR11R12, -C(=S)NR11R12, -C(=O)OR11, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, carbociclilalquilo C4-8, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, -C(=O)alquilo C1-8, -S(O)n-alquilo C1-8, arilalquilo C1-8, OR11 o SR11; cada R9 o R10 es, de manera independiente, H, halógeno, NR11R12, N(R11)OR11, NR11NR11R12, N3, NO, NO2, CHO, CN, -CH(=NR11), -CH=NHNR11, -CH=N(OR11), -CH(OR11)2, -C(=O)NR11R12, -C(=S)NR11R12, -C(=O)OR11, R11, OR11 o SR11; cada R11 o R12 es, de manera independiente, H, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, carbociclilalquilo C4-8, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, -C(=O)alquilo C1-8, -S(O)alquilo C1-8 o arilalquilo C1-8; o R11 y R12 tomados en conjunto con un nitrógeno al cual ambos están unidos forman un anillo heterocíclico de 3 a 7 miembros donde cualquiera de los átomos de carbono de dicho anillo heterocíclico puede ser opcionalmente reemplazados con -O-, -S- o -NRa-; y donde cada alquilo C1-8, alquenilo C2-8, alquinilo C2-8 o arilalquilo C1-8 de cada R3, R5, R6, R11 o R12 está, de manera independiente, opcionalmente sustituido con uno o más halo, hidroxi, CN, N3, N(Ra)2 o ORa; y donde uno o más de los átomos de carbono no terminales de cada uno de dicho alquilo C1-8 pueden ser opcionalmente reemplazados con -O-, -S- o -NRa-; para la preparación de un medicamento para el tratamiento de una infección por Orthomyxoviridae.Reivindicación 30: Un compuesto que tiene una estructura de fórmula (5) ó (6); o una de sus sales o ésteres farmacéuticamente aceptables.
ARP110103311A 2010-09-13 2011-09-12 Uso de analogos de carba-nucleosidos-2-fluor sustituidos para preparar medicamentos para el tratamiento de infecciones por virus de la influenza, y compuestos relacionados AR082960A1 (es)

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US (3) US20120107274A1 (es)
EP (1) EP2616080A1 (es)
JP (1) JP2013541519A (es)
KR (1) KR20140091459A (es)
CN (1) CN103153314A (es)
AR (1) AR082960A1 (es)
AU (1) AU2011302310A1 (es)
BR (1) BR112013005888A2 (es)
CA (1) CA2807584C (es)
EA (1) EA201390142A1 (es)
MX (1) MX2013002871A (es)
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