AR089999A1 - Compuestos triciclicos y metodos para el uso de los mismos - Google Patents

Compuestos triciclicos y metodos para el uso de los mismos

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AR089999A1
AR089999A1 ARP130100469A ARP130100469A AR089999A1 AR 089999 A1 AR089999 A1 AR 089999A1 AR P130100469 A ARP130100469 A AR P130100469A AR P130100469 A ARP130100469 A AR P130100469A AR 089999 A1 AR089999 A1 AR 089999A1
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Argentina
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alkyl
halo
haloalkyl
group
cycloalkyl
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ARP130100469A
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Castanedo Georgette
Feng Jianwen
A G N Montalbetti Christian
Staben Steven
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Hoffmann La Roche
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Publication of AR089999A1 publication Critical patent/AR089999A1/es

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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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Abstract

Los compuestos de la fórmula (1) y las composiciones farmacéuticas de los mismos son útiles para el tratamiento de enfermedades y trastornos, en los que se observa una activación no deseada o una sobreactivación de la señalización de la NF-kB. Reivindicación 1: Un compuesto de la fórmula (1) en la que: A¹, A², A³ y A⁴ se eligen entre el grupo formado por: A¹, A², A³ son en cada caso N y A⁴ es C; A¹ y A² son en cada caso N, A³ es C(RA³) y A⁴ es C; A¹ es C, A² es N, A³ es N(RN³) y A⁴ es C; A¹ es C, A² es N(RN²), A³ es N y A⁴ es C, dicho RN² es hidrógeno, alquilo C₁₋₃, haloalquilo C₁₋₃, (alquil C₁₋₃)-C(=O)- o (haloalquil C₁₋₃)-C(=O)-; A¹ es C y uno de A² y A³ es N y el otro es S y A⁴ es C; A¹ es C, A² es S, A³ es C(RA³) y A4 es C; A¹ es C, A² es N, A³ y A⁴ es N; A¹ es C, A² es N, A³ es C(RA³) y A⁴ es N; A¹ es C, A² es C(RC²), A³ es S y A⁴ es C, dicho RC² es hidrógeno, halógeno, alquilo C₁₋₃, haloalquilo C₁₋₃, (alquil C₁₋₃)-C(=O)- o (haloalquil C₁₋₃)-C(=O)-; y A¹ es C, A² y A³ y A⁴ son en cada caso N; A⁵ y A⁶ son en cada caso con independencia C o N; X es O ó C(R¹)₂; m es un número entero de 0 a 4; R¹, R² y RA³ y RN³ se eligen con independencia de cada aparición entre el grupo formado por hidrógeno, -F, -Cl, -Br, -I, -(X¹)₀₋₁-CN, -(X¹)₀₋₁-NO₂, -(X¹)₀₋₁-SF₅, -(X¹)₀₋₁-OH, -(X¹)₀₋₁-NH₂, -(X¹)₀₋₁-N(H)(R¹ᵃ), -(X¹)₀₋₁-N(R¹ᵇ)(R¹ᵃ), -(X¹)₀₋₁-CF₃, alquilo C₁₋₆, haloalquilo C₁₋₆, heteroalquilo C₁₋₆, alcoxi C₁₋₆, alquiltio C₁₋₆, -(X¹)₀₋₁-alquilo C₁₋₆, -(X¹)₀₋₁-cicloalquilo C₃₋₁₀, -(X¹)₀₋₁-heterocicloalquilo C₂₋₉, -(X¹)₀₋₁-heteroarilo de 5 - 10 eslabones, -(X¹)₀₋₁-arilo de 6 - 10 eslabones, -C(=O)(X¹)₁-cicloalquilo C₃₋₁₀, -C(=O)(X¹)₁-heterocicloalquilo C₂₋₉, =O, -(X¹)₀₋₁-C(=Y¹)N(H)(R¹ᵃ), -(X¹)₀₋₁-C(=Y¹)-NH₂, -(X¹)₀₋₁-C(=Y¹)-N(R¹ᵃ)(R¹ᵇ), -(X¹)₀₋₁-C(=Y¹)OR¹ᵃ, -(X¹)₀₋₁-C(=Y¹)OH, -(X¹)₀₋₁-N(H)-C(=Y¹)(R¹ᵃ), -(X¹)₀₋₁-N(R¹ᵇ)C(=Y¹)(R¹ᵃ), -(X¹)₀₋₁-N(R¹ᵇ)C(=Y¹)(H), -(X¹)₀₋₁-N(H)C(=Y¹)OR¹ᵃ, -(X¹)₀₋₁-N(R¹ᵇ)C(=Y¹)OR¹ᵃ, -(X¹)₀₋₁-S(O)₁₋₂R¹ᵃ, -(X¹)₀₋₁-N(H)S(O)₁₋₂R¹ᵃ, -(X¹)₀₋₁-N(R¹ᵇ)S(O)₁₋₂R¹ᵃ, -(X¹)₀₋₁-S(O)₀₋₁N(H)(R¹ᵃ), -(X¹)₀₋₁-S(O)₀₋₁N(R¹ᵇ)(R¹ᵃ), -(X¹)₀₋₁-S(O)₀₋₁NH₂, -(X¹)₀₋₁-S(=O)(=NR¹ᵇ)R¹ᵃ, -(X¹)₀₋₁-C(=Y)R¹ᵃ, -(X¹)₀₋₁-C(=Y¹)H, -(X¹)₀₋₁-C(=NOH)R¹ᵃ, -(X¹)₀₋₁-C(=NOR¹ᵇ)R¹ᵃ, -(X¹)₀₋₁-NHC(=Y¹)N(H)(R¹ᵃ), -(X¹)₀₋₁-NHC(=Y¹)NH₂, -(X¹)₀₋₁-NHC(=Y¹)-N(R¹ᵇ)(R¹ᵃ), -(X¹)₀₋₁-N(R¹ᵃ)C(=Y¹)N(H)(R¹ᵃ), -(X¹)₀₋₁-N(R¹ᵃ)C(=Y¹)-N(R¹ᵃ)(R¹ᵃ), -(X¹)₀₋₁-N(R¹ᵃ)C(=Y¹)NH₂, -(X¹)₀₋₁-OC(=Y¹)R¹ᵃ, -(X¹)₀₋₁-OC(=Y¹)H, -(X¹)₀₋₁-OC(=Y¹)OR¹ᵃ, -(X¹)₀₋₁-OP(=Y¹)(OR¹ᵃ)-(OR¹ᵇ), -(X¹)-SC(=Y¹)OR¹ᵃ y -(X¹)-SC(=Y¹)N(R¹ᵃ)(R¹ᵇ), en los que X¹ se elige entre el grupo formado por alquileno C₁₋₄, haloalquileno C₁₋₄, heteroalquileno C₁₋₄, alquenileno C₂₋₄, alquinileno C₂₋₄, alquilenoxi C₁₋₄, cicloalquileno C₃₋₇ y heterocicloalquileno C₂₋₄, fenileno, heteroarileno de 5 - 6 eslabones, R¹ᵃ y R¹ᵇ se eligen en cada caso con independencia entre el grupo formado por alquilo C₁₋₆, haloalquilo C₁₋₆, heteroalquilo C₁₋₆, cicloalquilo C₃₋₇, (cicloalquil C₃₋₇)-alquilo C₁₋₄, heterocicloalquilo C₂₋₆, (heterocicloalquil C₂₋₆)-alquilo C₁₋₄, heteroarilo de 5 - 6 eslabones, (heteroarilo de 5 - 6 eslabones)-alquilo C₁₋₄, arilo C₆, (aril C₆)-alquilo C₁₋₄ y bencilo, o R¹ᵃ y R¹ᵇ cuando están unidos al mismo átomo de nitrógeno pueden combinarse opcionalmente para formar un anillo heterocíclico de 3 a 7 eslabones que contiene 0 - 2 heteroátomos adicionales elegidos entre N, O y S; Y¹ es O, NR¹ᵈ o S, dicho R¹ᵈ es hidrógeno o alquilo C₁₋₆; cualquier porción del sustituyente R¹, R² y RA³ y RN³ está sustituida con independencia de cada aparición de 0 a 4 veces por sustituyentes R¹/² elegidos entre el grupo formado por -F, -Cl, -Br, -I, -CN, -NO₂, -SF₅, -OH, -NH₂, -N(alquilo C₁₋₆)₂, -NH(alquilo C₁₋₆), -CF₃, =O, alquilo C₁₋₆, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆, heteroalquilo C₁₋₆, alcoxi C₁₋₆, alquiltio C₁₋₆, cicloalquilo C₃₋₇, heterocicloalquilo C₂₋₆, -C(=O)N(H)-((halo)alquilo C₁₋₆), -C(=O)N((halo)alquilo C₁₋₆)₂, -C(=O)NH₂, -C(=O)O-(halo)alquilo C₁₋₆, -C(=O)OH, -N(H)-C(=O)((halo)alquilo C₁₋₆), -N((halo)alquilo C₁₋₆)C(=O)-((halo)alquilo C₁₋₆) -N(H)C(=O)O-(halo)alquilo C₁₋₆, -N((halo)alquilo C₁₋₆)-C(=O)O-(halo)alquilo C₁₋₆, -S(O)₁₋₂-(halo)alquilo C₁₋₆, -N(H)-S(O)₁₋₂(halo)alquilo C₁₋₆, -N((halo)alquilo C₁₋₆)-S(O)₁₋₂(halo)alquilo C₁₋₆, -S(O)₀₋₁N(H)((halo)alquilo C₁₋₆), -S(O)₀₋₁N((halo)alquilo C₁₋₆)₂, -S(O)₀₋₁NH₂, -C(=O)(halo)alquilo C₁₋₆, -C(=O)cicloalquilo C₃₋₇, -C(=NOH)(halo)alquilo C₁₋₆, -C(=NO-alquil C₁₋₆)-(halo)alquilo C₁₋₆, -NHC(=O)N(H)-((halo)alquilo C₁₋₆), -NHC(=O)-N((halo)alquilo C₁₋₆)₂, -NHC(=O)NH₂, -N((halo)alquilo C₁₋₆)C(=O)N(H)((halo)alquilo C₁₋₆), -N((halo)alquilo C₁₋₆)C(=O)NH₂, -OC(=O)(halo)alquilo C₁₋₆, -OC(=O)O(halo)alquilo C₁₋₆, -OP(=O)(O-(halo)alquilo C₁₋₆)₂, -SC(=O)O(halo)alquilo C₁₋₆ y -SC(=O)N((halo)alquilo C₁₋₆)₂, en los que cualquier par de sustituyentes R² unidos al mismo vértice o a diferentes vértices del anillo B o los sustituyentes R¹ y R² unidos a diferentes vértices del anillo B se combinan opcionalmente para formar un anillo carbocíclico o heterocíclico de 3 a 6 eslabones que contiene 1 ó 2 heteroátomos elegidos entre N, O y S, dicho anillo carbocíclico o heterocíclico de 3 a 6 eslabones está opcionalmente sustituido por 1 ó 2 sustituyentes R¹/²; R⁴ y R⁶ están en cada caso con independencia ausentes si tuvieran que unirse a un átomo de nitrógeno o se eligen entre el grupo formado por hidrógeno, alquilo C₁₋₃, haloalquilo C₁₋₃, (alquil C₁₋₃)-C(=O)- o (haloalquil C₁₋₃)-C(=O)-, alcoxi C₁₋₃, (alquil C₁₋₃)-amino, di(alquil C₁₋₃)-amino, alquiltio C₁₋₃, NH₂, OH, F, Cl, Br, I, CN y NO₂; R⁵ se elige entre el grupo formado por hidrógeno, alquilo C₁₋₃, haloalquilo C₁₋₃, (alquil C₁₋₃)-C(=O)- o (haloalquil C₁₋₃)-C(=O)-, alcoxi C₁₋₃, (alquil C₁₋₃)-amino, di(alquil C₁₋₃)-amino, alquiltio C₁₋₃, NH₂, OH, F, Cl, Br, I, CN y NO₂; R⁷ se elige con independencia de cada aparición entre el grupo formado por hidrógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, cicloalquilo C₃₋₁₀, heterocicloalquilo C₂₋₉, arilo de 6 - 10 eslabones, heteroarilo de 5 - 10 eslabones, C(=O)R⁷ᵃ, -C(=O)H, C(=O)OR⁷ᵃ o -C(=O)NR⁷ᵃR⁷ᵇ, dichos R&#x2
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US20110086834A1 (en) 2008-06-26 2011-04-14 Amgen Inc. Alkynyl alcohols as kinase inhibitors
US8263633B2 (en) 2009-09-28 2012-09-11 F. Hoffman-La Roche Ag Benzoxepin PI3K inhibitor compounds and methods of use
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