EA201890906A1 - ПРОИЗВОДНЫЕ ХИНОКСАЛИНА И ПИРИДОПИРАЗИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PI3Kβ - Google Patents

ПРОИЗВОДНЫЕ ХИНОКСАЛИНА И ПИРИДОПИРАЗИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PI3Kβ

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Publication number
EA201890906A1
EA201890906A1 EA201890906A EA201890906A EA201890906A1 EA 201890906 A1 EA201890906 A1 EA 201890906A1 EA 201890906 A EA201890906 A EA 201890906A EA 201890906 A EA201890906 A EA 201890906A EA 201890906 A1 EA201890906 A1 EA 201890906A1
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EA
Eurasian Patent Office
Prior art keywords
derivatives
pyridopyrasine
chinoxaline
compounds
present
Prior art date
Application number
EA201890906A
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English (en)
Other versions
EA037401B1 (ru
Inventor
Патрик Рене Анжибо
Оливье Алексис Жорж Керолль
Дидье Жан-Клод Бертело
Кристоф Мейер
Мэттью Филипп Виктор Виллот
Ливен Мерпул
Тьерри Франсуа Алан Жан Жуссом
Original Assignee
Янссен Фармацевтика Нв
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Application filed by Янссен Фармацевтика Нв filed Critical Янссен Фармацевтика Нв
Publication of EA201890906A1 publication Critical patent/EA201890906A1/ru
Publication of EA037401B1 publication Critical patent/EA037401B1/ru

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    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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Abstract

Настоящее изобретение относится к замещенным производным хиноксалина и пиридопиразина формулы (I)где переменные имеют значения, определенные в формуле изобретения. Соединения согласно настоящему изобретению являются пригодными в качестве ингибиторов pI3Kβ. Кроме того, настоящее изобретение относится к фармацевтическим композициям, содержащим указанные соединения в качестве активного ингредиента, а также к применению указанных соединений в качестве лекарственного препарата.
EA201890906A 2015-10-09 2016-10-07 Производные хиноксалина и пиридопиразина в качестве ингибиторов pi3k EA037401B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15189163 2015-10-09
EP16174710 2016-06-16
PCT/EP2016/073962 WO2017060406A1 (en) 2015-10-09 2016-10-07 Quinoxaline and pyridopyrazine derivatives as pi3kbeta inhibitors

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EA201890906A1 true EA201890906A1 (ru) 2018-09-28
EA037401B1 EA037401B1 (ru) 2021-03-24

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US (2) US10526316B2 (ru)
EP (1) EP3359533B1 (ru)
JP (1) JP6912460B2 (ru)
KR (1) KR102630111B1 (ru)
CN (1) CN108349946B (ru)
AU (1) AU2016335086B2 (ru)
BR (1) BR112018007068B1 (ru)
CA (1) CA2999818C (ru)
EA (1) EA037401B1 (ru)
ES (1) ES2905673T3 (ru)
IL (1) IL258513B (ru)
MA (1) MA45896A (ru)
MX (1) MX2018004304A (ru)
WO (1) WO2017060406A1 (ru)

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Publication number Priority date Publication date Assignee Title
WO2017060406A1 (en) 2015-10-09 2017-04-13 Janssen Pharmaceutica Nv Quinoxaline and pyridopyrazine derivatives as pi3kbeta inhibitors
EA037361B1 (ru) 2016-06-16 2021-03-18 Янссен Фармацевтика Нв Производные бициклического пиридина, пиразина и пиримидина в качестве ингибиторов pi3k бета
CN110461827A (zh) * 2017-03-29 2019-11-15 詹森药业有限公司 作为PI3K-β抑制剂的喹喔啉和吡啶并吡嗪衍生物
MX2020009228A (es) 2018-03-08 2021-01-08 Incyte Corp Compuestos diolicos de aminopirazina como inhibidores de fosfoinositida 3-cinasas-gamma.
CN111892597B (zh) * 2020-09-01 2023-07-25 山西天宏达安医药科技有限公司 一种喹喔啉基吡啶并吡嗪类化合物及其制备方法与应用
WO2024026419A1 (en) * 2022-07-27 2024-02-01 Black Diamond Therapeutics, Inc. Quinoxaline derivatives as pik3 alpha modulators

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007103756A2 (en) 2006-03-02 2007-09-13 Smithkline Beecham Corporation Thiazolones for use as pi3 kinase inhibitors
WO2008014219A2 (en) 2006-07-24 2008-01-31 Smithkline Beecham Corporation Thiozolidinedione derivatives as p13 kinase inhibitors
AU2008219297B2 (en) * 2007-02-22 2013-07-04 Merck Serono S.A. Quinoxaline compounds and use thereof
EP2173354A4 (en) 2007-08-09 2011-10-05 Glaxosmithkline Llc CHINOXALIN DERIVATIVES AS PI3 KINASE INHIBITORS
MX2010007418A (es) 2008-01-04 2010-11-12 Intellikine Inc Ciertas entidades quimicas, composiciones y metodos.
CN105078978A (zh) 2009-08-17 2015-11-25 因特利凯公司 杂环化合物及其用途
JP2013505965A (ja) 2009-09-29 2013-02-21 エックスカバリー ホールディング カンパニー エルエルシー Ｐｉ３ｋ（デルタ）選択的阻害剤
US8399460B2 (en) * 2009-10-27 2013-03-19 Astrazeneca Ab Chromenone derivatives
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
EA022623B1 (ru) 2010-10-06 2016-02-29 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Производные бензимидазола в качестве ингибиторов pi3-киназ
EP2678016B1 (en) 2011-02-23 2016-08-10 Intellikine, LLC Heterocyclic compounds and uses thereof
US8530470B2 (en) * 2011-04-13 2013-09-10 Astrazeneca Ab Chromenone derivatives
US9096605B2 (en) 2011-08-24 2015-08-04 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as PI3 kinase inhibitors
US8906910B2 (en) 2011-12-20 2014-12-09 Glaxosmithkline Llc Imidazopyridine derivatives as PI3 kinase
US8778937B2 (en) 2011-12-20 2014-07-15 Glaxosmithkline Llc Benzimidazole boronic acid derivatives as PI3 kinase inhibitors
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
WO2016097359A1 (en) 2014-12-19 2016-06-23 Janssen Pharmaceutica Nv Heterocyclyl linked imidazopyridazine derivatives as pi3kbeta inhibitors
LT3233862T (lt) 2014-12-19 2019-09-10 Janssen Pharmaceutica Nv Imidazopiridazino dariniai, kaip pi3kbeta slopikliai
WO2017060406A1 (en) 2015-10-09 2017-04-13 Janssen Pharmaceutica Nv Quinoxaline and pyridopyrazine derivatives as pi3kbeta inhibitors

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