AR099138A1 - Piridinas fusionadas como inhibidores del complejo p97 - Google Patents

Piridinas fusionadas como inhibidores del complejo p97

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AR099138A1
AR099138A1 ARP150100150A ARP150100150A AR099138A1 AR 099138 A1 AR099138 A1 AR 099138A1 AR P150100150 A ARP150100150 A AR P150100150A AR P150100150 A ARP150100150 A AR P150100150A AR 099138 A1 AR099138 A1 AR 099138A1
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independently
group
hydrogen
optionally substituted
ring
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Cleave Biosciences Inc
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Publication of AR099138A1 publication Critical patent/AR099138A1/es

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Abstract

La presente se refiere a ciertas pirimidinas fusionadas que tienen un anillo homo- o hetero-ciclopentilo, ciclohexilo o cicloheptilo como par de fusión de la pirimidina; que tienen un grupo aminobencilo o aminobencilo sustituido en la posición 4 del anillo pirimidina; y un anillo heterobiciclo 5:6 con al menos un N, O ó S en la posición 2 del anillo pirimidina. Estos compuestos son útiles para el tratamiento del cáncer por inhibición del complejo p97. Reivindicación 1: Un compuesto de pirimidina fusionada de fórmula (1), en donde: Y es CR⁴, NH, NR⁵, O ó S y C cuando CR⁴ es un átomo sp³; m y n son cada uno independientemente un número entero de 0 a 4, y la suma de m y n es un número entero de 2, 3 ó 4; Ar es un grupo arilo opcionalmente sustituido; A, D y E son cada uno independientemente C o N, en donde C es un carbono sp² sustituido por hidrógeno o alquilo de 1 a 4 carbonos cuando una de las valencias de C no está designada de otro modo; Z y B son cada uno independientemente CR⁶, N, NR⁷, O ó S, en donde C como CR⁶ es un carbono sp²; R¹, R², R³, R⁴, R⁵, R⁶ y R⁷ se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, un grupo alifático opcionalmente sustituido, un grupo aromático opcionalmente sustituido y un grupo funcional opcionalmente sustituido; con la condición de que; a) al menos uno de D y E sea C; b) al menos uno de A, D, E, Z y B sea distinto de C; c) Z y B no pueden ser ambos simultáneamente cualquiera de NR⁷, O ó S; d) cuando uno de D y E es N y A es C, entonces Z y B son cada uno independientemente CR⁶, N o NR⁷; e) cuando ambos D y E son C y A es N, Z y B son cada uno independientemente CR⁶ o N, pero cuando Y es carbono y R³ es hidrógeno, entonces Z y B no pueden ser ambos CR⁶ y B no puede ser N; f) cuando ambos D y E son C y A es N, Z y B son cada uno independientemente CR⁶ o N, pero cuando ni m ni n es cero y R³ es hidrógeno, entonces Z y B no pueden ser ambos CR⁶ y B no puede ser N; g) cuando D, E y A son todos C, entonces Z y B son cada uno independientemente CR⁶, N, NR⁷, O ó S; h) cuando uno de Z y B es O ó S, entonces el otro es CR⁶ o N, y A, D y E son todos C; i) cuando uno de Z y B es NR⁷, entonces el otro es N o CR⁶, A, D y E son todos C.
ARP150100150A 2014-01-20 2015-01-20 Piridinas fusionadas como inhibidores del complejo p97 AR099138A1 (es)

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US (2) US9828363B2 (es)
EP (1) EP3097092B1 (es)
JP (1) JP6387111B2 (es)
KR (1) KR101922317B1 (es)
CN (1) CN106458996B (es)
AR (1) AR099138A1 (es)
AU (1) AU2015206292B2 (es)
BR (1) BR112016016421B1 (es)
CA (1) CA2936559C (es)
CL (1) CL2016001840A1 (es)
EA (1) EA031317B1 (es)
ES (1) ES2819867T3 (es)
IL (1) IL246692B (es)
MX (1) MX2016009465A (es)
NZ (1) NZ722624A (es)
SG (1) SG11201605699QA (es)
TW (1) TWI640516B (es)
WO (1) WO2015109285A1 (es)
ZA (1) ZA201605107B (es)

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JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
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CN110872291B (zh) * 2019-11-26 2021-06-25 五邑大学 一种四氢吡啶并嘧啶类化合物及其制备方法和应用
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