AR052995A1 - Compuestos de 3h-oxazolo y 3h-tiazolo[4, 5 - d]pirimidin-2-ona3, 5-disustituidos y 3, 5, 7-trisustituidos con actividad inmunomoduladora, sus profarmacos, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de enfermedades de origen viral - Google Patents

Compuestos de 3h-oxazolo y 3h-tiazolo[4, 5 - d]pirimidin-2-ona3, 5-disustituidos y 3, 5, 7-trisustituidos con actividad inmunomoduladora, sus profarmacos, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de enfermedades de origen viral

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AR052995A1
AR052995A1 ARP050105306A ARP050105306A AR052995A1 AR 052995 A1 AR052995 A1 AR 052995A1 AR P050105306 A ARP050105306 A AR P050105306A AR P050105306 A ARP050105306 A AR P050105306A AR 052995 A1 AR052995 A1 AR 052995A1
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Argentina
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alkyl
nhc
heterocyclyl
aryl
cycloalkyl
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ARP050105306A
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English (en)
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S E Webber
G J Haley
J R Lennox
A X Xiang
E J Rueden
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Anadys Pharmaceuticals Inc
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Publication of AR052995A1 publication Critical patent/AR052995A1/es

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Abstract

Compuestos de 3H-oxazolo y 3H-tiazolo[4,5-d]pirimidin-2-ona 3,5-disustituidos y 3,5,7-trisustituidos y su profármacos que tienen actividad inmunomoduladora, uso terapéutico o preventivo de tales compuestos y composiciones farmacéuticas que los contienen y se emplea en el tratamiento de enfermedad de origen viral. Reivindicacion 1: Un compuesto de la formula (1), en donde: X es O o S, Y es O o S, R1 es H, alquilo, arilo, cicloalquilo o heterociclilo; R2 es NH2, -NHC(O)R4, -NHR5, - N=CHNR6R7, R3 es H, Cl, Br, u OR8, R4 es -alquiloC1-7 u -OalquiloC1-7, R5 es -alquiloC1-7; R6 y R7 son, de modo independiente, -alquiloC1-7 o junto con nitrogeno forman un anillo heterocíclico de 5 o 6 miembros; R8 es -CHR9R10; R9 es H, -alquiloC1- 7, cicloalquilo, arilo, heterociclilo, -NR11R12, u OR5; R10 es -alquiloC1-7, cicloalquilo, arilo, heterociclilo, -NR11R12, u OR5; R11 y R12 son, de modo independiente, H, -alquiloC1-7 o -C(O)R4; en donde, cuando X es O, Y es S, y R3 es H, Cl, Br, u OR8, R1 no es H o beta-D-ribosa o sus ésteres; en donde los restos anteriores de alquilo, arilo, cicloalquilo o heterociclilo están opcionalmente sustituidos con 1-4 sustituyentes seleccionados de hidrogeno; alcanoilo; alquilamina; amino; arilo, cicloalquilo, heterociclilo; azido; alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, alcoxi C1-6, alquilamina C1-6, dialquilamina C1-6, alquenilo C2-6 o alquinilo C2-6, en donde cada uno de los cuales puede estar interrumpido por uno o varios heteroátomos; carboxilo; ciano; halo; hidroxi; mercapto; nitro; tioalquilo; -N=N-NH2; -C(O)2-alquiloC1-6, -C(O)2-arilo, -C(O)2-cicloalquilo, -C(O)2-heterociclilo, -O-haloalquiloC1-6, -O-(alquil C1-6l)arilo, -O-(alquil C1-6)cicloalquilo, -O-(alquil C1-6)heterociclilo, -O-(alquil C1-6)amino, -O-(alquil C1-6)alquilamino, -O-(alquil C1-6)dialquilamino, -O-alquilC1-6-C(O)-amino, -O-alquilC1-6-C(O)-alquilamino, -O-alquilC1-6-S(O)2-amino, -O-alquilC1-6-S(O)2-alquilamino, -O-alquilC1-6-S(O)2- dialquilamino, -O-alquilC1-6-C(O)-dialquilamino, -O-arilo, -O-heterociclilo, -NHC(O)-alquiloC1-6, -NHC(O)-alqueniloC1-6, -NHC(O)-arilo, -NHC(O)-cicloalquilo, -NHC(O)-heterociclilo, -NHC(O)-(alquil C1-6)arilo, -NHC(O)-(alquil C1-6)cicloalquilo, - NHC(O)-(alquil C1-6)heterociclilo, -NHC(O)-(alquil C1-6)amino, -NHC(O)-(alquil C1-6)alquilamina, -NHC(O)-(alquil C1-6)dialquilamina, -NHC(O)-alquilC1-6C(O)amino, -NHC(O)-alquilC1-6C(O)alquilamina, -NHC(O)-alquilC1-6C(O)dialquilamina, -NHC(O)- alquilC1-6N(H)-alquilC1-6C(O)2-alquiloC1-6, -NH-alquilC1-6-C(O)-amino, -NH-alquilC1-6-C(O)-alquilamino, -NH-alquilC1-6-C(O)-dialquilamino, -NHC(O)-alquilC1-6S(O)2alquiloC1-6, -NHC(O)-alquilC1-6-S-heterociclilo, -NHS(O)2-alquiloC1-6, -NHS(O)2-arilo, - NH-alquilC1-6-S(O)2-amino, -NH-alquilC1-6-S(O)2-alquilamino, -NH-alquilC1-6-S(O)2-dialquilamino, -NHS(O)2-cicloalquilo, -NHS(O)2-heterociclilo, -NHS(O)alquiloC1-6, -NHS(O)arilo, -NHS(O)cicloalquilo, -NHS(O)heterociclilo, -NHSalquiloC1-6, -NHSarilo, - NHScicloalquilo, y -NH-S-heterociclilo; en donde cada uno de los sustituyentes anteriores pueden estar además opcionalmente sustituidos con 1-5 sustituyentes seleccionados de: amino; alquilamina C1-6, dialquilamina C1-6; alquilo C1-6, alcoxi C1-6, alquenilo C1-6, hidroxilo C1-6, e hidroxialquilo C1-6, cada uno opcionalmente sustituido con: ciano; halo; y nitro; o una de sus sales o hidratos farmacéuticamente aceptables. Reivindicacion 8: Un compuesto de la formula (2), en donde: X es O o S, Y es O o S, Z es O o CH2; R2 es -NH2, -NHC(O)R4, -NHR5, -N=CHNR6R7, R4 es -alquiloC1-7 u -OalquiloC1-7, R5 es -alquiloC1-7; R6 y R7 son, de modo independiente, -alquiloC1-7 o junto con nitrogeno forman un anillo heterocíclico de 5 o 6 miembros; R13 es OH o SH; R14 es H, -CH2OH o -CH2-O-C(O)alquiloC1-18; R15 es OH, alquenilo, -OC(O)alquiloC1-18, -OC(O)arilo u -OC(O)heterociclilo; R16, 17, R18, y R19 son, de modo independiente, H, halo, N3, alquilo, -(CH2)mOR20, -(CH2)mOC(O)alquiloC1-18, - OC(O)arilo, -OS(O)2arilo o R16 y R17 son un alquenilo o R17 y R19 se combinan para formar un anillo dioxol; R20 es H o alquilo; m es 0 o 1; n es 1 o 2; en donde cuando R2 es NH2, entonces uno de los siguientes debe estar presente: Z es CH2; n es 2 o m es 1; al menos de R16, R17, R18, y R19 es halo, N3, alquilo o -(CH2)mOR20, en donde m es 1, y en donde cuando R17 es N3, entonces R18 y R19 no son H, y en donde cuando R17 es OH y R16 y R19 son H, R18 no es F; o R16 y R17 son un alquenilo; en donde los restos de alquilo, arilo, cicloalquilo o heterociclilo están opcionalmente sustituidos con 1-4 sustituyentes seleccionados de hidrogeno; alcanoilo; alquilamina; amino; arilo, cicloalquilo, heterociclilo; azido; alquilo C1-6, haloalquilo C1- 6, hidroxialquilo C1-6, alcoxi C1-6, alquilamina C1-6, dialquilamina C1-6, alquenilo C2-6 o alquinilo C2-6, en donde cada uno de los cuales puede estar interrumpido por uno o varios heteroátomos; carboxilo; ciano; halo; hidroxi; mercapto; nitro; tioalquilo; -N=N-NH2; -C(O)2-alquiloC1-6, -C(O)2-arilo, -C(O)2-cicloalquilo, -C(O)2-heterociclilo, -O-haloalquiloC1-6, -O-(alquil C1-6l)arilo, -O-(alquil C1-6)cicloalquilo, -O-(alquil C1-6)heterociclilo, -O-(alquil C1-6)amino, -O-(alquil C1- 6)alquilamino, -O-(alquil C1-6)dialquilamino, -O-alquilC1-6-C(O)-amino, -O-alquilC1-6-C(O)-alquilamino, -O-alquilC1-6-S(O)2-amino, -O-alquilC1-6-S(O)2-alquilamino, -O-alquilC1-6-S(O)2-dialquilamino, -O-alquilC1-6-C(O)-dialquilamino, -O-arilo, -O- heterociclilo, -NHC(O)-alquiloC1-6, -NHC(O)-alqueniloC1-6, -NHC(O)-arilo, -NHC(O)-cicloalquilo, -NHC(O)-heterociclilo, -NHC(O)-(alquil C1-6)arilo, -NHC(O)-(alquil C1-6)cicloalquilo, -NHC(O)-(alquil C1-6)heterociclilo, -NHC(O)-(alquil C1-6)amino, - NHC(O)-(alquil C1-6)alquilamina, -NHC(O)-(alquil C1-6)dialquilamina, -NHC(O)-alquilC1-6C(O)amino, -NHC(O)-alquilC1-6C(O)alquilamina, -NHC(O)-alquilC1-6C(O)dialquilamina, -NHC(O)-alquilC1-6N(H)-alquilC1-6C(O)2-alquiloC1-6, -NH-alquilC1-6-C(O)-amino, - NH-alquilC1-6-C(O)-alquilamino, -NH-alquilC1-6-C(O)-dialquilamino, -NHC(O)-alquilC1-6S(O)2alquiloC1-6, -NHC(O)-alquilC1-6-S-heterociclilo, -NHS(O)2-alquiloC1-6, -NHS(O)2-arilo, -NH-alquilC1-6-S(O)2-amino, -NH-alquilC1-6-S(O)2-alquilamino, -NH- alquilC1-6-S(O)2-dialquilamino, -NHS(O)2-cicloalquilo, -NHS(O)2-heterociclilo, -NHS(O)alquiloC1-6, -NHS(O)arilo, -NHS(O)cicloalquilo, -NHS(O)heterociclilo, -NHSalquiloC1-6, -NHSarilo, -NHScicloalquilo, y -NH-S-heterociclilo; en donde cada uno de los sustituyentes anteriores pueden estar además opcionalmente sustituidos con 1-5 sustituyentes seleccionados de: amino; alquilamina C1-6, dialquilamina C1-6; alquilo C1-6, alcoxi C1-6, alquenilo C1-6, hidroxilo C1-6, e hidroxialquilo C1-6, cada uno opcionalmente sustituido con: ciano; halo; y nitro; o una de sus sales, hidratos o tautomeros farmacéuticamente aceptables.
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