AR096846A1 - Dihidroquinoxalinonas y dihidropiridopirazinonas modificadas como inhibidores de la proteína bet - Google Patents

Dihidroquinoxalinonas y dihidropiridopirazinonas modificadas como inhibidores de la proteína bet

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AR096846A1
AR096846A1 ARP140102526A ARP140102526A AR096846A1 AR 096846 A1 AR096846 A1 AR 096846A1 AR P140102526 A ARP140102526 A AR P140102526A AR P140102526 A ARP140102526 A AR P140102526A AR 096846 A1 AR096846 A1 AR 096846A1
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alkyl
optionally
heterocycloalkyl
monosubstituted
cycloalkyl
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Dr Stckigt Detlef
Dr Haendler Bernard
Dr Schmees Norbert
Dr Gallenkamp Daniel
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Bayer Pharma Aktiengellschaft
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Abstract

Dihidroquinoxalinonas y dihidropiridopirazinonas inhibidoras de la proteína BET, en especial inhibidoras de BRD4, composiciones farmacéuticas que comprenden a éstos compuestos de la presente y el uso profiláctico y terapéutico de los mismos para casos de trastornos hiperproliferativos, en especial para casos de trastornos neoplásicos. Uso de inhibidores de la proteína BET en infecciones virales, en trastornos neurodegenerativos, en enfermedades inflamatorias, en trastornos ateroescleróticos y en el control de la fertilidad masculina. Reivindicación 1: Compuestos caracterizados porque son de la fórmula general (1) en donde A es -NH-, -N(C₁₋₃-alquilo) o -O-; X es -N- o -CH-; n es 0, 1 ó 2; R¹ es un grupo -C(=O)NR⁷R⁸ o -S(=O)₂NR⁷R⁸, o es heteroarilo monocíclico de 5 miembros que opcionalmente puede estar monosustituido, disustituido o trisustituido en forma idéntica o diferente con halógeno, ciano, C₁₋₄-alquilo, C₂₋₄-alquenilo, C₂₋₄ alquinilo, halo-C₁₋₄-alquilo, C₁₋₄-alcoxi, halo-C₁₋₄-alcoxi, C₁₋₄-alquiltio, halo-C₁₋₄-alquiltio, -NR⁹R¹⁰, -C(=O)OR¹¹, -C(=O)NR⁹R¹⁰, -C(=O)R¹¹, -S(=O)₂R¹¹, -S(=O)₂NR⁹R¹⁰; R² es hidrógeno, halógeno, ciano, C₁₋₃-alquilo, C₂₋₄-alquenilo, C₂₋₄-alquinilo, halo-C₁₋₄-alquilo, C₁₋₄-alcoxi, halo-C₁₋₄-alcoxi, C₁₋₄-alquiltio o halo-C₁₋₄-alquiltio, y, si n es 2, R² puede ser igual o diferente; o R¹ y R² juntos son un grupo *-S(=O)₂NR⁸-CH₂-**, *-S(=O)₂-NR⁸-CH₂-CH₂-**, *-C(=O)-NR⁸-CH₂-** o *-C(=O)-NR⁸-CH₂-CH₂-** en donde "*" denota el punto de unión de R¹ al anillo fenilo en la fórmula (1), y en donde "**" denota un átomo de carbono de este anillo fenilo adyacente a este punto de unión; R³ es metilo o etilo; R⁴ es hidrógeno o C₁₋₃-alquilo; R⁵ es hidrógeno o C₁₋₃-alquilo; o R⁴ y R⁵ junto con el átomo de carbono al cual están unidos son C₃₋₆-cicloalquileno; R⁶ es C₁₋₆alquilo que opcionalmente puede estar monosustituido con C₁₋₃alcoxi, fenilo, C₃₋₈-cicloalquilo, o heterocicloalquilo de entre 4 y 8 miembros, en donde fenilo a su vez puede estar opcionalmente monosustituido, disustituido o trisustituido en forma idéntica o diferente con: halógeno, ciano, C₁₋₄-alquilo, C₂₋₄-alquenilo, C₂₋₄-alquinilo, C₁₋₄-alcoxi, halo-C₁₋₄-alquilo, halo-C₁₋₄-alcoxi, y en donde C₃₋₈-cicloalquilo y heterocicloalquilo de entre 4 y 8 miembros a su vez pueden estar opcionalmente monosustituidos o disustituidos en forma idéntica o diferente con C₁₋₃-alquilo, o es C₃₋₈-cicloalquilo o heterocicloalquilo de entre 4 y 8 miembros, que opcionalmente puede estar monosustituido o disustituido en forma idéntica o diferente con C₁₋₃-alquilo o C₁₋₄-alcoxicarbonilo, o es fenilo que opcionalmente puede estar monosustituido o disustituido en forma idéntica o diferente con halógeno, C₁₋₃-alquilo o heterocicloalquilo de entre 4 y 8 miembros, en donde el heterocicloalquilo de entre 4 y 8 miembros a su vez puede estar opcionalmente monosustituido o disustituido en forma idéntica o diferente con C₁₋₃-alquilo o C₁₋₄-alcoxicarbonilo; R⁷ es hidrógeno, o es C₁₋₆-alquilo que opcionalmente puede estar monosustituido, disustituido o trisustituido en forma idéntica o diferente con: hidroxilo, oxo, flúor, ciano, C₁₋₄-alcoxi, halo-C₁₋₄-alcoxi, -NR⁹R¹⁰, C₃₋₈-cicloalquilo, C₄₋₈-cicloalquenilo, heterocicloalquilo de entre 4 y 8 miembros, heterocicloalquenilo de entre 4 y 8 miembros, -C₅₋₁₁-espirocicloalquilo, C₅₋₁₁-heteroespirocicloalquilo, C₆₋₁₂-cicloalquilo en puente, C₆₋₁₂-heterocicloalquilo en puente, C₆₋₁₂-bicicloalquilo, C₆₋₁₂-heterobicicloalquilo, fenilo, heteroarilo de 5 ó 6 miembros, en donde C₃₋₈-cicloalquilo, C₄₋₈-cicloalquenilo, heterocicloalquilo de entre 4 y 8 miembros, heterocicloalquenilo de entre 4 y 8 miembros, C₅₋₁₁-espirocicloalquilo, C₅₋₁₁-heteroespirocicloalquilo, C₆₋₁₂-cicloalquilo en puente, C₆₋₁₂-heterocicloalquilo en puente, C₆₋₁₂-bicicloalquilo, C₆₋₁₂-heterobicicloalquilo a su vez puede estar opcionalmente monosustituido o disustituido en forma idéntica o diferente con: hidroxilo, flúor, oxo, ciano, C₁₋₃-alquilo, fluoro-C₁₋₃-alquilo, C₃₋₆-cicloalquilo, ciclopropilmetilo, C₁₋₃-alquilcarbonilo, C₁₋₄-alcoxicarbonilo o -NR⁹R¹⁰, y en donde fenilo y heteroarilo de 5 ó 6 miembros opcionalmente puede estar monosustituido o disustituido en forma idéntica o diferente con: halógeno, ciano, trifluorometilo, C₁₋₃-alquilo, C₁₋₃-alcoxi, o es C₃₋₆-alquenilo o C₃₋₆-alquinilo, o es C₃₋₈-cicloalquilo, C₄₋₈-cicloalquenilo, C₅₋₁₁-espirocicloalquilo, C₆₋₁₂-cicloalquilo en puente o C₆₋₁₂-bicicloalquilo, que opcionalmente puede estar monosustituido o disustituido en forma idéntica o diferente con: hidroxilo, oxo, ciano, flúor, C₁₋₃-alquilo, C₁₋₃-alcoxi, trifluorometilo, -NR⁹-R¹⁰, o es heterocicloalquilo de entre 4 y 8 miembros, heterocicloalquenilo de entre 4 y 8 miembros, C₅₋₁₁-heteroespirocicloalquilo, C₆₋₁₂-heterocicloalquilo en puente o C₆₋₁₂-heterobicicloalquilo, que opcionalmente puede estar monosustituido o disustituido en forma idéntica o diferente con: hidroxilo, flúor, oxo, ciano, C₁₋₃-alquilo, fluoro-C₁₋₃-alquilo, C₃₋₆-cicloalquilo, ciclopropilmetilo, C₁₋₃-alquilcarbonilo, C₁₋₄-alcoxicarbonilo o -NR⁹R¹⁰; R⁸ es hidrógeno o C₁₋₃-alquilo opcionalmente sustituido con hidroxilo, oxo o C₁₋₃-alcoxi una o dos veces, en forma idéntica o diferente, o fluoro-C₁₋₃-alquilo; o R⁷ y R⁸ junto con el átomo de nitrógeno al cual están unidos son heterocicloalquilo de entre 4 y 8 miembros, heterocicloalquenilo de entre 4 y 8 miembros, C₅₋₁₁-heteroespirocicloalquilo, C₆₋₁₂-heterocicloalquilo en puente o C₆₋₁₂-heterobicicloalquilo, que opcionalmente puede estar monosustituido o disustituido en forma idéntica o diferente con: hidroxilo, flúor, oxo, ciano, C₁₋₃-alquilo, fluoro-C₁₋₃-alquilo, C₃₋₆-cicloalquilo, ciclopropilmetilo, C₁₋₃-alquilcarbonilo, C₁₋₄-alcoxicarbonilo o -NR⁹R¹⁰; R⁹ y R¹⁰ es cada uno en forma independiente hidrógeno o C₁₋₃-alquilo opcionalmente sustituido con hidroxilo, oxo o C₁₋₃-alcoxi una o dos veces, en forma idéntica o diferente, o fluoro-C₁₋₃-alquilo, o heterocicloalquilo de entre 4 y 8 miembros, en donde el heterocicloalquilo de entre 4 y 8 miembros a su vez puede estar opcionalmente monosustituido o disustituido en forma idéntica o diferente con C₁₋₃-alquilo; o R⁹ y R¹⁰ junto con el átomo de nitrógeno al cual están unidos son heterocicloalquilo de entre 4 y 8 miembros que opcionalmente puede estar monosustituido o disustituido en forma idéntica o diferente con: hidroxilo, flúor, oxo, ciano, C₁₋₃-alquilo, fluoro-C₁₋₃-alquilo, C₃₋₆-cicloalquilo, ciclopropilmetilo, C₁₋₃-alquilcarbonilo o C₁₋₄-alcoxicarbonilo; R¹¹ es C₁₋₆-alquilo o fenil-C₁₋₃-alquilo; y los diasterómeros, racematos, polimorfos y sales fisiológicamente aceptables de los mismos.
ARP140102526A 2013-07-09 2014-07-08 Dihidroquinoxalinonas y dihidropiridopirazinonas modificadas como inhibidores de la proteína bet AR096846A1 (es)

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Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106573931A (zh) * 2014-06-18 2017-04-19 拜耳医药股份有限公司 抑制BET蛋白的具有间位取代的芳族氨基或醚基的3，4‑二氢吡啶并[2，3‑b]吡嗪酮
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
JP2018527340A (ja) * 2015-08-11 2018-09-20 ネオメド インスティテュートＮｅｏｍｅｄ Ｉｎｓｔｉｔｕｔｅ アリール置換ジヒドロキノリノン、その調製及び医薬品としてのその使用
WO2017024412A1 (en) 2015-08-12 2017-02-16 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
WO2017066876A1 (en) 2015-10-21 2017-04-27 Neomed Institute Substituted imidazopyridines, their preparation and their use as pharmaceuticals
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
DE102017005089A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
CN107793371B (zh) * 2016-09-05 2020-12-15 中国科学院上海药物研究所 一类溴结构域识别蛋白抑制剂及其制备方法和用途
EP3725768A1 (en) * 2019-04-17 2020-10-21 Newron Pharmaceuticals S.p.A. Process for the production of substituted 2-[2-(phenyl) ethylamino]alkaneamide derivatives
CA3152923A1 (en) 2019-09-30 2021-04-08 Keisuke Yamamoto Bet degrader
CN115947728B (zh) * 2021-10-09 2024-01-09 沈阳药科大学 含磺酰基的二氢喋啶酮衍生物及其应用

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2458699C (en) * 2001-09-04 2010-10-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Novel dihydropteridinones, method for producing the same and the use thereof as medicaments
US6861422B2 (en) * 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
KR20080052611A (ko) * 2005-08-26 2008-06-11 메틸진 인크. 히스톤 탈아세틸 효소의 벤조디아제핀 및 벤조피페라진유도체 억제제
WO2009071480A2 (en) * 2007-12-04 2009-06-11 Nerviano Medical Sciences S.R.L. Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
MY152386A (en) * 2009-01-23 2014-09-15 Takeda Pharmaceutical Substituted 6a,7,8,9-tetrahydropyrido[3,2-e] pyrrolo[1,2-a]pyrazin-6(5h)-ones
JP2012197231A (ja) * 2009-08-06 2012-10-18 Oncotherapy Science Ltd Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体
WO2013027168A1 (en) * 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2014095774A1 (de) * 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydropyridopyrazinone

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ES2635003T3 (es) 2017-10-02
WO2015004075A1 (de) 2015-01-15
UY35654A (es) 2015-02-27
US20160176867A1 (en) 2016-06-23
HK1221721A1 (zh) 2017-06-09
JP2016523941A (ja) 2016-08-12
CN105518001A (zh) 2016-04-20
EP3019493B1 (de) 2017-06-14
EP3019493A1 (de) 2016-05-18

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