AR105820A1 - Análogos de nucleósidos sustituidos en el anillo aromático bicíclico 6-6 para su uso como inhibidores de prmt5 - Google Patents

Análogos de nucleósidos sustituidos en el anillo aromático bicíclico 6-6 para su uso como inhibidores de prmt5

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AR105820A1
AR105820A1 ARP160102600A ARP160102600A AR105820A1 AR 105820 A1 AR105820 A1 AR 105820A1 AR P160102600 A ARP160102600 A AR P160102600A AR P160102600 A ARP160102600 A AR P160102600A AR 105820 A1 AR105820 A1 AR 105820A1
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alkyl
group
cycloalkyl
halo
aromatic ring
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Janssen Pharmaceutica Nv
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Abstract

Reivindicación 1: Un compuesto de fórmula (1), donde R¹ representa hidrógeno o -C(=O)-(alquilo C₁₋₄); R² representa hidrógeno o -C(=O)-(alquilo C₁₋₄); Y representa -O-, -CH₂- o -CF₂-; Z representa -CH₂-, -X-CR⁵ᵃR⁵ᵇ-, -CR⁵ᶜ=CR⁵ᵈ-, -CR⁵ᵉR⁵ᵍ-CR⁵ᶠR⁵ʰ- o -CºC-; y cuando Y representa -CH₂- o -CF₂-, entonces Z también puede representar -O- o -CR⁵ᵃR⁵ᵇ-X-; R⁵ᵃ, R⁵ᵇ, R⁵ᶜ, R⁵ᵈ, R⁵ᵉ, R⁵ᶠ, R⁵ᵍ y R⁵ʰ representan cada uno independientemente hidrógeno o alquilo C₁₋₄; X representa -O-, -S- o -NR¹¹-; R¹¹ representa hidrógeno, alquilo C₁₋₄ o alquilo C₁₋₄ sustituido con un sustituyente seleccionado a partir del grupo constituido por -OH, -O-(alquilo C₁₋₄), R¹², -NH₂, -NH-(alquilo C₁₋₄) y -N(alquilo C₁₋₄)₂; R¹² representa un anillo heterocíclico de 4, 5, 6 ó 7 miembros y contiene un átomo de nitrógeno y opcionalmente un átomo de oxigeno; donde dicho anillo heterocíclico de 4, 5, 6 ó 7 miembros está unido al resto de la molécula mediante un átomo de nitrógeno anular; Ar representa un sistema anular aromático bicíclico de 10 miembros constituido por dos anillos de 6 miembros condensados, donde opcionalmente 1 ó 2 átomos de carbono anulares son reemplazados por un átomo de nitrógeno; siempre que cuando el átomo de nitrógeno reemplace uno de los dos átomos de carbono condensados, un grupo carbonilo esté presente en dicho sistema anular aromático bicíclico; Ar está sustituido opcionalmente con uno, dos, tres o cuatro sustituyentes cada uno seleccionado independientemente a partir del grupo constituido por halo, -OH, -NH₂, -NH-(alquilo C₁₋₄), -N(alquilo C₁₋₄)₂, -NHR¹⁰ᵈ, -NR¹⁰ᶜR¹⁰ᵈ, ciano, -CF₃, -C(=O)-NH₂, -C(=O)-NH-(alquilo C₁₋₄), -C(=O)-(alquilo C₁₋₄), alquiloxi C₁₋₄ -C(=O)-O-(alquilo C₁₋₄), cicloalquilo C₃₋₆, -O-(cicloalquilo C₃₋₆), -NH-(cicloalquilo C₃₋₆), -N(cicloalquilo C₃₋₆)₂, alquenilo C₂₋₆, alquilo C₁₋₄ sustituido con un alquiloxi C₁₋₄ y alquilo C₁₋₄ sustituido opcionalmente con un -NR¹⁰ᵃR¹⁰ᵇ; R¹⁰ᵃ y R¹⁰ᵇ representan cada uno independientemente hidrógeno o alquilo C₁₋₄; R¹⁰ᶜ y R¹⁰ᵈ representan cada uno independientemente cicloalquilo C₃₋₆; R¹³; R¹⁴; cicloalquilo C₃₋₆ sustituido con uno, dos o tres sustituyentes cada uno seleccionado independientemente a partir del grupo constituido por halo, -OH y -O-(alquilo C₁₋₄); alquilo C₁₋₄ sustituido con uno, dos o tres sustituyentes cada uno seleccionado independientemente a partir del grupo constituido por halo, -OH y -O-(alquilo C₁₋₄); o alquilo C₁₋₄ sustituido con un sustituyente seleccionado a partir del grupo constituido por cicloalquilo C₃₋₆, R¹³ y R¹⁴; R¹³ representa un anillo aromático monocíclico de 4 a 7 miembros que contiene uno, dos o tres heteroátomos cada uno seleccionado independientemente entre O, S, S(=O)ₚ y N; o un anillo aromático condensado bicíclico de 6 a 11 miembros que contiene uno, dos o tres heteroátomos cada uno seleccionado independientemente entre O, S, S(=O)ₚ y N; dicho anillo aromático monocíclico de 4 a 7 miembros o anillo aromático condensado bicíclico de 6 a 11 miembros está sustituido opcionalmente con uno o dos sustituyentes seleccionados a partir del grupo constituido por alquilo C₁₋₄; p representa 1 ó 2; R¹⁴ representa fenilo sustituido opcionalmente con uno, dos o tres sustituyentes cada uno seleccionado independientemente a partir del grupo constituido por halo; Het representa un sistema anular heterocíclico aromático bicíclico seleccionado a partir del grupo constituido por (a-1), (a-2), (a-3), (a-4) y (a-5) del grupo de fórmulas (2); R³ᵃ, R³ᵇ, R³ᶜ, R³ᵈ y R³ᵉ representan cada uno independientemente hidrógeno, halo, -NR⁷ᵃR⁷ᵇ, alquilo C₁₋₄, alquenilo C₂₋₄, cicloalquilo C₃₋₆, -OH o -O-(alquilo C₁₋₄); R⁷ᵃ representa hidrógeno; R⁷ᵇ representa hidrógeno, cicloalquilo C₃₋₆ o alquilo C₁₋₄; R⁴ᵃ, R⁴ᵇ, R⁴ᶜ, R⁴ᵈ, R⁴ᵉ, R⁴ᶠ y R⁴ᵍ representan cada uno hidrógeno, halo, -NR⁸ᵃR⁸ᵇ o alquilo C₁₋₄; R⁸ᵃ y R⁸ᵇ representan cada uno independientemente hidrógeno o alquilo C₁₋₄; Q¹ representa N o CR⁶ᵃ; Q² representa N o CR⁶ᵇ; Q³ representa N o CR⁶ᶜ; Q⁴ representa N o CR⁶ᵈ; siempre que como máximo uno de Q³ y Q⁴ represente N; Q⁸ representa N o CR⁶ᵍ; Q⁹ representa N o CR⁶ʰ; Q¹⁰ representa N o CR⁶ⁱ; Q¹¹ representa N o CR⁶ʲ; Q⁵ representa CR³ᵈ; Q⁶ representa N; y Q⁷ representa CR⁴ᶠ; o Q⁵ representa CR³ᵈ; Q⁶ representa CR⁴ᵉ; y Q⁷ representa N; o Q⁵ representa N; Q⁶ representa CR⁴ᵉ; y Q⁷ representa CR⁴ᶠ; o Q⁵ representa N; Q⁶ representa CR⁴ᵉ; y Q⁷ representa N; o Q⁵ representa N; Q⁶ representa N; y Q⁷ representa CR⁴ᶠ; o Q⁵ representa N; Q⁶ representa N; y Q⁷ representa N; R⁶ᵃ, R⁶ᵇ, R⁶ᶜ, R⁶ᵈ, R⁶ᵉ, R⁶ᶠ, R⁶ᵍ, R⁶ʰ, R⁶ⁱ y R⁶ʲ representan cada uno independientemente hidrógeno, halógeno, alquilo C₁₋₄, -NR⁹ᵃR⁹ᵇ o alquilo C₁₋₄ sustituido con uno, dos o tres átomos halo; R⁹ᵃ y R⁹ᵇ representan cada uno independientemente hidrógeno o alquilo C₁₋₄; o uno de sus solvatos o una de sus sales de adición farmacéuticamente aceptables; siempre que se excluyan los compuestos y sus solvatos y sales de adición farmacéuticamente aceptables de fórmula (3), (4) y (5).
ARP160102600A 2015-08-26 2016-08-25 Análogos de nucleósidos sustituidos en el anillo aromático bicíclico 6-6 para su uso como inhibidores de prmt5 AR105820A1 (es)

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TW202321249A (zh) * 2015-08-26 2023-06-01 比利時商健生藥品公司 使用作為ｐｒｍｔ５抑制劑之新穎經６－６雙環芳香環取代之核苷類似物
MA43671A (fr) * 2016-03-10 2018-11-28 Janssen Pharmaceutica Nv Analogues de nucléosides substitués destinés à être utilisés en tant qu'inhibiteurs de prmt5
CA2969295A1 (en) 2016-06-06 2017-12-06 Pfizer Inc. Substituted carbonucleoside derivatives, and use thereof as a prmt5 inhibitor
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