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

Piridinas fusionadas como inhibidores del complejo p97

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Publication number
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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AR
Argentina
Prior art keywords
independently
group
hydrogen
optionally substituted
ring
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ARP150100150A
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English (en)
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Cleave Biosciences Inc
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Application filed by Cleave Biosciences Inc filed Critical Cleave Biosciences Inc
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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EP (1) EP3097092B1 (es)
JP (1) JP6387111B2 (es)
KR (1) KR101922317B1 (es)
CN (1) CN106458996B (es)
AR (1) AR099138A1 (es)
AU (1) AU2015206292B2 (es)
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EP3080101A1 (en) 2013-12-10 2016-10-19 Cleave Biosciences, Inc. Monocyclic pyrimidine/pyridine compounds as inhibitors of p97 complex
BR112016016421B1 (pt) 2014-01-20 2022-10-18 Cleave Biosciences, Inc Composto de pirimidina fundida, composição farmacêutica e respectivos uso
CN110366550A (zh) * 2016-12-22 2019-10-22 美国安进公司 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3679040B1 (en) 2017-09-08 2022-08-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
US11090304B2 (en) 2018-05-04 2021-08-17 Amgen Inc. KRAS G12C inhibitors and methods of using the same
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