AR055343A1 - INDOLCARBOXAMIDE INHIBITORS DERIVATIVES OF QUINASAS IKK2 - Google Patents

INDOLCARBOXAMIDE INHIBITORS DERIVATIVES OF QUINASAS IKK2

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Publication number
AR055343A1
AR055343A1 ARP060102790A ARP060102790A AR055343A1 AR 055343 A1 AR055343 A1 AR 055343A1 AR P060102790 A ARP060102790 A AR P060102790A AR P060102790 A ARP060102790 A AR P060102790A AR 055343 A1 AR055343 A1 AR 055343A1
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Argentina
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alkyl
group
cycloalkyl
heteroaryl
optionally substituted
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ARP060102790A
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Spanish (es)
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Smithkline Beecham Corp
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Abstract

Reivindicacion 1: Un compuesto de indolcarboxamida caracterizado porque tiene la formula (1) en la que: R1 es el grupo -XYZ o X es fenilo, heteroarilo, 1,2,3,4-tetrahidronaftalenilo o 2,3-dihidro-1H-indenilo, donde dichos grupos fenilo, heteroarilo, 1,2,3,4-tetrahidronaftalenilo y 2,3-dihidro-1H-indenilo están opcionalmente sustituidos con uno o dos sustituyentes cada uno de ellos seleccionado independientemente entre los siguientes: halo, nitro, ciano, -NR7R8, alquilo C1-6, CHO, CONH2 y -OR4, donde dicho grupo alquilo C1-6 está opcionalmente sustituido con un grupo -NR4R5; Y es un enlace o alquileno C1-6, donde alquileno C1-6 está opcionalmente sustituido con uno o dos sustituyentes cada uno de ellos seleccionado independientemente entre los siguientes: alquilo X1-3 opcionalmente sustituido con un grupo -OR4, cicloalquilo C3-7, metoxi, hidroxi y heteroarilo; Z es -NR4R5 o heterocicloalquilo, donde dicho grupo heterocicloalquilo está opcionalmente sustituido con uno o dos sustituyentes cada uno de ellos seleccionado independientemente entre los siguientes: alquilo C1-6 opcionalmente sustituido con un grupo -OR4 o un grupo heterocicloalquilo, cicloalquilo C3-7, metoxi, -CONH2, hidroxi, heteroarilo, CF3, fenilo, heterocicloalquilo y N(CH3)2; R2 se selecciona entre H, F, y Cl; R3 se selecciona entre H, F y Cl; R4 se selecciona entre H u alquilo C1-6, donde dicho grupo alquilo C1-6 está opcionalmente sustituido con un grupo hidroxi o un grupo metoxi; R5 se selecciona entre H, heterocicloalquilo C5-6, -CO2Et, alcoxi C1-6, cicloalquilo C3-7, alquilo C1-6, -SO2R10 y -C(O)R10, donde dichos grupos cicloalquilo C3-7 y alquilo C1-6 están opcionalmente sustituidos con uno a tres sustituyentes seleccionados entre R6; cada R6 se selecciona independientemente entre -NR7R8, -SO2R7, -CONH2, -CF3, -CN, -CO2R7, -OCH2CH2OR7, -SR5, alquenilo C3-4, OH, alcoxi C1-6, heteroarilo, cicloalquilo C3-7, fenilo, heterocicloalquilo y halo, donde dichos grupos heteroarilo, cicloalquilo, fenilo y heterocicloalquilo están opcionalmente sustituidos con uno a dos sustituyentes seleccionados entre R9; R7 se selecciona entre H, alquilo C1-3 y fenilo; R8 se selecciona entre H, alquilo C1-3 y -C(O)R4; cada R9 se selecciona independientemente entre hidroxi, -OMe, nitro, alquilo C1-6, NH2, halo, CF3, alcoxi C1-6 y CN; R10 se selecciona entre alquilo C1-6, fenilo, cicloalquilo C3-7, heteroarilo, heteroarilo C1-6 y heterocicloalquilo, donde dicho grupo alquilo C1-6 está sustituido con uno a dos sustituyentes cada uno de ellos seleccionado independientemente entre cicloalquilo C3-7 y -S-R7, donde dicho grupo heterocicloalquilo está opcionalmente sustituido con un grupo -C(O)R78; y donde dichos grupos fenilo, heteroarilo y heteroarilo C1-6 están opcionalmente sustituidos con uno a dos sustituyentes seleccionados entre R11; cada R11 se selecciona independientemente entre H, alquilo C1-6 y halo; U es un enlace, alquileno C1-6 o alquenileno C2-6; V es fenilo, heteroarilo de 5 o 6 miembros, heterocicloalquilo de 5-7 miembros, cicloalquilo C5-7s cicloalquenilo C5-7, estando cada uno de ellos sustituido con -N(R7)S(O)mR12, -S(O)mN(R7)R12, -S(O)mR12, o -C(O)R12; m es 1 o 2, y R12 es alquilo C1-6, cicloalquilo C3-7, alquil C1-6-cicloalquilo C3-7 o alquil C1-6-fenilo, o una sal farmacéuticamente aceptable, solvato o polimorfo del mismo.Claim 1: An indolcarboxamide compound characterized in that it has the formula (1) in which: R1 is the group -XYZ or X is phenyl, heteroaryl, 1,2,3,4-tetrahydronaphthalenyl or 2,3-dihydro-1H- indenyl, wherein said phenyl, heteroaryl, 1,2,3,4-tetrahydronaphthalenyl and 2,3-dihydro-1H-indenyl groups are optionally substituted with one or two substituents each independently selected from the following: halo, nitro, cyano, -NR7R8, C1-6 alkyl, CHO, CONH2 and -OR4, wherein said C1-6 alkyl group is optionally substituted with a group -NR4R5; Y is a bond or C1-6 alkylene, where C1-6 alkylene is optionally substituted with one or two substituents each independently selected from the following: X1-3 alkyl optionally substituted with a group -OR4, C3-7 cycloalkyl, methoxy, hydroxy and heteroaryl; Z is -NR4R5 or heterocycloalkyl, wherein said heterocycloalkyl group is optionally substituted with one or two substituents each independently selected from the following: C1-6 alkyl optionally substituted with a -OR4 group or a heterocycloalkyl group, C3-7 cycloalkyl, methoxy, -CONH2, hydroxy, heteroaryl, CF3, phenyl, heterocycloalkyl and N (CH3) 2; R2 is selected from H, F, and Cl; R3 is selected from H, F and Cl; R4 is selected from H or C1-6 alkyl, wherein said C1-6 alkyl group is optionally substituted with a hydroxy group or a methoxy group; R5 is selected from H, C5-6 heterocycloalkyl, -CO2Et, C1-6 alkoxy, C3-7 cycloalkyl, C1-6 alkyl, -SO2R10 and -C (O) R10, wherein said C3-7 cycloalkyl and C1- alkyl groups 6 are optionally substituted with one to three substituents selected from R6; each R6 is independently selected from -NR7R8, -SO2R7, -CONH2, -CF3, -CN, -CO2R7, -OCH2CH2OR7, -SR5, C3-4 alkenyl, OH, C1-6 alkoxy, heteroaryl, C3-7 cycloalkyl, phenyl , heterocycloalkyl and halo, wherein said heteroaryl, cycloalkyl, phenyl and heterocycloalkyl groups are optionally substituted with one to two substituents selected from R9; R7 is selected from H, C1-3 alkyl and phenyl; R8 is selected from H, C1-3 alkyl and -C (O) R4; each R9 is independently selected from hydroxy, -OMe, nitro, C1-6 alkyl, NH2, halo, CF3, C1-6 alkoxy and CN; R 10 is selected from C 1-6 alkyl, phenyl, C 3-7 cycloalkyl, heteroaryl, C 1-6 heteroaryl and heterocycloalkyl, wherein said C 1-6 alkyl group is substituted with one to two substituents each independently selected from C 3-7 cycloalkyl. and -S-R7, wherein said heterocycloalkyl group is optionally substituted with a -C (O) R78 group; and wherein said phenyl, heteroaryl and C1-6 heteroaryl groups are optionally substituted with one to two substituents selected from R11; each R11 is independently selected from H, C1-6 alkyl and halo; U is a bond, C1-6 alkylene or C2-6 alkenylene; V is phenyl, 5- or 6-membered heteroaryl, 5-7-membered heterocycloalkyl, C5-7 cycloalkyl C5-7 cycloalkenyl, each of which being substituted with -N (R7) S (O) mR12, -S (O) mN (R7) R12, -S (O) mR12, or -C (O) R12; m is 1 or 2, and R 12 is C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkyl-C 3-7 cycloalkyl or C 1-6 alkyl phenyl, or a pharmaceutically acceptable salt, solvate or polymorph thereof.

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