AR116993A2 - Compuestos heterociclos bicíclicos y sus usos en terapia - Google Patents

Compuestos heterociclos bicíclicos y sus usos en terapia

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AR116993A2
AR116993A2 ARP190103237A ARP190103237A AR116993A2 AR 116993 A2 AR116993 A2 AR 116993A2 AR P190103237 A ARP190103237 A AR P190103237A AR P190103237 A ARP190103237 A AR P190103237A AR 116993 A2 AR116993 A2 AR 116993A2
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Argentina
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alkyl
groups
crxry
alkenyl
heterocyclyl
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Astex Therapeutics Ltd
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
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  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente se refiere a compuestos heterociclos bicíclicos de fórmula (1), o formas tautoméricas o estereoquímicamente isoméricas, N-óxidos, sus sales farmacéuticamente aceptables o sus solvatos; en donde R¹, R²ᵃ, R²ᵇ, R³ᵃ, R³ᵇ, R⁵, R⁶, R⁷, R⁸, R⁹, p y E son como se encuentran definidos en la presente; composiciones farmacéuticas que comprenden dichos compuestos y el uso de dichos compuestos en el tratamiento de enfermedades, por ejemplo, el cáncer. Reivindicación 1: Un compuesto de fórmula (1), o sus formas tautoméricas o estereoquímicamente isoméricas, N-óxidos, sales farmacéuticamente aceptable o sus solvatos; en donde el anillo E representa un grupo carbocíclico o heterocíclico aromático de 6 miembros; G y J se seleccionan de manera independiente de C o N; Q es CR⁴ o N; R¹ se selecciona de alquilo C₁₋₄, alquenilo C₂₋₄ y cicloalquilo -(CH₂)ₛ-C₃₋₈, donde dicho alquilo C₁₋₄, alquenilo C₂₋₄, y cicloalquilo C₃₋₈ pueden sustituirse opcionalmente por uno o más grupos Rᵃ; Rᵃ se selecciona entre halógeno, -OH y -O-alquilo C₁₋₆; R²ᵃ y R²ᵇ se seleccionan de manera independiente de hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, -C(=O)NH₍₂₋q₎(alquilo C₁₋₆)q, -(CH₂)ₛ-(heterociclilo de 3 - 12 miembros), y -(CH₂)ₛ-carbociclilo C₃₋₁₂, o los grupos R²ᵃ y R²ᵇ, junto con el átomo de carbono al que se encuentran unidos, se pueden unir para formar un grupo carbociclilo o heterociclilo saturado de 3 - 10 miembros, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, los grupos heterociclilo y carbociclilo pueden estar opcionalmente sustituidos por uno o más grupos Rᵇ; R³ᵃ y R³ᵇ se seleccionan de manera independiente de hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, -C(=O)NH₍₂₋q₎(alquilo C₁₋₆)q, -(CH₂)ₛ-(heterociclilo de 3 - 12 miembros), -(CH₂)ₛ-carbociclilo C₃₋₁₂, -C(=O)-(heterociclilo de 3 - 12 miembros), y -C(=O)-carbociclilo C₃₋₁₂, o los grupos R³ᵃ y R³ᵇ, junto con el átomo de carbono al que se encuentran unidos, se pueden unir para formar un grupo carbociclilo o heterociclilo saturado de 3 - 10 miembros, donde dichos grupos alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, heterociclilo y carbociclilo pueden estar opcionalmente sustituidos por uno o más grupos Rᵇ; R⁴ se selecciona entre hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, -C(=O)NH₍₂₋q₎(alquilo C₁₋₆)q, -(CH₂)ₛ-(heterociclilo de 3 - 12 miembros), -(CH₂)ₛ-carbociclilo C₃₋₁₂, -C(=O)-(heterociclilo de 3 - 12 miembros), y -C(=O)-carbociclilo C₃₋₁₂, donde dichos grupos alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, heterociclilo y carbociclilo pueden estar opcionalmente sustituidos por uno o más grupos Rᵇ; R⁵ se selecciona entre hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, -(CH₂)ₛ-cicloalquilo C₃₋₈ y - (CH₂)ₛ-cicloalquenilo C₃₋₈, donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈ y cicloalquenilo C₃₋₈ pueden estar opcionalmente sustituidos por uno o más grupos Rᵃ; R⁶ y R⁷ se seleccionan de manera independiente de hidrógeno, grupos alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, -Y-carbociclilo C₃₋₁₂, -Z-(heterociclilo de 3 - 12 miembros), -(CRˣRʸ)ₛ-O-Rᶻ, -O-(CRˣRʸ)ₙ-ORᶻ, -(CH₂)ₛ-CN, -S(O)q-Rˣ, -C(=O)Rˣ, -C(=S)Rˣ, -C(=N)Rˣ, -(CRˣRʸ)ₛ-C(=O)ORᶻ, -(CRˣRʸ)ₛ-O-C(=O)-Rᶻ, -(CRˣRʸ)ₛ-C(=O)NRˣRʸ, -(CH₂)ₛ-NRˣC(=O)Rʸ, -(CH₂)ₛ-OC(=O)NRˣRʸ, -(CH₂)ₛ-NRˣC(=O)ORʸ, -(CH₂)ₛ-NRˣRʸ, -NRˣ-(CH₂)ₛ-Rᶻ, -(CRˣRʸ)ₛ-C(=S)NRᶻ, -(CRˣRʸ)ₛ-C(=N)NRᶻ, -(CH₂)ₛ-O-C(=O)-C₁₋₄alquilo-NRˣRʸ, -(CH₂)ₛ-NRˣ-(CH₂)ₙ-O-C(=O)-Rᶻ, -(CH₂)ₛ-NRˣ-(CH₂)ₛ-SO₂-Rʸ, -(CH₂)ₛ-NH-SO₂-NRˣRʸ y -(CH₂)ₛ-SO₂NRˣRʸ, o los grupos R⁶ y R⁷, junto con el átomo de carbono al que se encuentran unidos, se pueden unir para formar un grupo carbociclilo o heterociclilo parcial o completamente saturado de 3 - 10 miembros, y que pueden fusionarse opcionalmente a un anillo carbociclilo o heterociclilo aromático de 5 - 6 miembros, donde dichos grupos alquilo C₁₋₈, alquenilo C₂₋₈ y alquinilo C₂₋₈ pueden sustituirse opcionalmente por uno o más grupos Rᵇ y donde dichos grupos carbociclilo y heterociclilo pueden estar opcionalmente sustituidos por uno o más grupos Rᵇ (por ejemplo, 1, 2 ó 3); R⁸ y R⁹ se seleccionan de manera independiente de hidrógeno, halógeno, grupos alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, -Y-carbociclilo C₃₋₁₂, -Z-(heterociclilo de 3 - 12 miembros), -(CRˣRʸ)ₛ-O-Rᶻ, -O-(CRˣRʸ)ₙ-ORᶻ, =O, =S, nitro, Si(Rˣ)₄, -(CH₂)ₛ-CN, -S(O)q-(CRˣRʸ)ₛ-Rᶻ, -C(=O)Rˣ, -C(=S)Rˣ, -C(=N)Rˣ, -(CRˣRʸ)ₛ-C(=O)ORᶻ, -(CRˣRʸ)ₛ-O-C(=O)-Rᶻ, -(CRˣRʸ)ₛ-C(=O)NRˣRʸ, -(CH₂)ₛ-NRˣC(=O)Rʸ, -(CH₂)ₛ-OC(=O)NRˣRʸ, -(CH₂)ₛ-NRˣC(=O)ORʸ, -(CH₂)ₛ-NRˣRʸ, -NRˣ-(CH₂)ₛ-Rᶻ, -(CRˣRʸ)ₛ-C(=S)NRᶻ, -(CRˣRʸ)ₛ-C(=N)NRˣ, -S(O)(=NRˣ)Rʸ, -(CH₂)ₛ-O-C(=O)-C₁₋₄alquilo-NRˣRʸ, -(CH₂)ₛ-NRˣ-(CH₂)ₙ-O-C(=O)-Rᶻ, -(CH₂)ₛ-NRˣ-(CH₂)ₛ-SO₂-Rʸ, -(CH₂)ₛ-NH-SO₂-NRˣRʸ, -(CH₂)ₛ-SO₂NRˣRʸ y P(=O)(Rˣ)₂, donde dichos grupos alquilo C₁₋₈, alquenilo C₂₋₈ y alquinilo C₂₋₈ pueden estar opcionalmente sustituido por uno o más grupos Rᵇ y donde dichos grupos carbociclilo y heterociclilo pueden estar opcionalmente sustituidos por uno o más grupos Rᵇ (por ejemplo, 1, 2 ó 3); Rᵇ se selecciona independientemente de halógeno, grupos alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, -(CH₂)ₛ-cicloalquilo C₃₋₈, -(CH₂)ₛ-cicloalquenilo C₃₋₈, -(CH₂)ₛ-fenilo, -(CH₂)ₛ-(heterociclilo saturado de 4 - 7 miembros), -(CRˣRʸ)ₛ-O-Rᶻ, -O-(CRˣRʸ)ₙ-ORᶻ, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, alcanol C₁₋₆, =O, =S, nitro, Si(Rˣ)₄, -(CH₂)ₛ-CN, -S(O)q-Rˣ, -C(=O)Rˣ, -(CRˣRʸ)ₛ-C(=O)ORᶻ, -(CRˣRʸ)ₛ-O-C(=O)-Rᶻ, -(CRˣRʸ)ₛ-C(=O)NRˣRʸ, -(CH₂)ₛ-NRˣC(=O)Rʸ, -(CH₂)ₛ-OC(=O)NRˣRʸ, -(CH₂)ₛ-NRˣC(=O)ORʸ -(CH₂)ₛ-NRˣRʸ, -NRˣ-(CH₂)ₛ-Rᶻ, -(CH₂)ₛ-O-C(=O)-C₁₋₄alquilo-NRˣRʸ, -(CH₂)ₛ-NRˣ-(CH₂)ₙ-O-C(=O)-Rᶻ, -(CH₂)ₛ-NRˣ-(CH₂)ₛ-SO₂-Rʸ, -(CH₂)ₛ-NH-SO₂-NRˣRʸ, -(CH₂)ₛ-SO₂NRˣRʸ y -P(=O)(Rˣ)₂, donde dichos grupos alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, cicloalquenilo C₃₋₈ y heterociclilo pueden estar opcionalmente sustituidos por uno o más grupos Rˣ; Rˣ, Rʸ y Rᶻ representan independientemente hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, -(CH₂)ₛ-cicloalquilo C₃₋₈, -(CH₂)ₛ-cicloalquenilo C₃₋₈, -(CH₂)ₛ-fenilo, -(CH₂)ₛ-(heterociclilo saturado de 4 - 7 miembros), alcanol C₁₋₆ opcionalmente sustituido con uno o más halo, -C(=O)O-alquilo C₁₋₆, hidroxi, alcoxi C₁₋₆, haloalquilo C₁₋₆, -(CH₂)ₙ-O-alquilo C₁₋₆, -C(=O)-(CH₂)ₙ-alcoxi C₁₋₆, -C(=O)-alquilo C₁₋₆, -(CH₂)ₛ-CN, alquilo C₁₋₆-N(H)₂₋q(alquilo C₁₋₆)q, -N(H)₂₋q(alquilo C₁₋₆)q, -C(=O)-N(H)₂₋q(alquilo C₁₋₆)q, -(CH₂)ₛ-NH-SO₂-N(H)₂₋q(alquilo C₁₋₆)q, -(CH₂)ₛ-N(alquilo C₁₋₄)-SO₂-N(H)₂₋q(alquilo C₁₋₆)q y -(CH₂)ₛ-O-C(=O)-alquilo C₁₋₄-N(H)₂₋q(alquilo C₁₋₆)q, y cuando se encuentran unidos a un átomo de nitrógeno, carbono, silicio o fósforo, Rˣ y Rʸ pueden unirse para formar un anillo de 3 - 7 miembros que contiene opcionalmente uno o dos heteroátomos adicionales seleccionados de O, N, S y las formas oxidadas de N o S; Y y Z se seleccionan de manera independiente de un enlace, -(CRˣRʸ)ₘ-, -C(=CRˣ)-, -C(=O)-, -NRˣ, -C(=O)NRˣ-, -NRˣC(=O)-, -(CRˣRʸ)q-O-, -O-(CRˣRʸ)q-, -S(O)₂-NH, NH-S(O)₂- y -S(O)q-; s representa de manera independiente un número entero de 0 - 4; n representa de manera independiente un número entero de 1 - 4; p representa de manera independiente un número entero de 0 - 4; q representa un número entero de 0 - 2; y m representa un número entero de 1 - 2.
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