BR112016024626A8 - compostos 1h-pirrolo[2,3-c]piridin-7(6h)-onas e pirazolo[3,4-c]piridin-7(6h)-onas, uso dos mesmos, composição farmacêutica que os compreende e método de inibição de uma proteína bet - Google Patents

compostos 1h-pirrolo[2,3-c]piridin-7(6h)-onas e pirazolo[3,4-c]piridin-7(6h)-onas, uso dos mesmos, composição farmacêutica que os compreende e método de inibição de uma proteína bet

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Publication number
BR112016024626A8
BR112016024626A8 BR112016024626A BR112016024626A BR112016024626A8 BR 112016024626 A8 BR112016024626 A8 BR 112016024626A8 BR 112016024626 A BR112016024626 A BR 112016024626A BR 112016024626 A BR112016024626 A BR 112016024626A BR 112016024626 A8 BR112016024626 A8 BR 112016024626A8
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Brazil
Prior art keywords
pyridin
ones
pyrazolo
pyrrolo
inhibition
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BR112016024626A
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English (en)
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BR112016024626B1 (pt
BR112016024626A2 (pt
Inventor
P Combs Andrew
Falahatpisheh Nikoo
P Maduskuie Thomas Jr
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Incyte Corp
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Publication of BR112016024626A2 publication Critical patent/BR112016024626A2/pt
Publication of BR112016024626A8 publication Critical patent/BR112016024626A8/pt
Publication of BR112016024626B1 publication Critical patent/BR112016024626B1/pt

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
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Abstract

compostos 1h-pirrolo[2,3-c]piridin- 7(6h)-onas e pirazolo[3,4-c]piridin-7(6h)-onas, uso dos mesmos, composição farmacêutica que os compreende e método de inibição de uma proteína bet a presente invenção refere-se a pirrolopiridinonas substituídas e pirazolopiridinonas substituídas que são inibidores de proteínas bet, tais como brd2, brd3, brd4 e brd-t e são úteis no tratamento de doenças, tais como o câncer.
BR112016024626-8A 2014-04-23 2015-04-22 Compostos 1h-pirrolo[2,3-c]piridin-7(6h)-onas e pirazolo[3,4-c]piridin-7 (6h)-onas, uso dos mesmos, composição farmacêutica que os compreende e método de inibição de uma proteína bet BR112016024626B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461983289P 2014-04-23 2014-04-23
US61/983,289 2014-04-23
PCT/US2015/027047 WO2015164480A1 (en) 2014-04-23 2015-04-22 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS

Publications (3)

Publication Number Publication Date
BR112016024626A2 BR112016024626A2 (pt) 2017-08-15
BR112016024626A8 true BR112016024626A8 (pt) 2021-07-20
BR112016024626B1 BR112016024626B1 (pt) 2023-03-21

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BR112016024626-8A BR112016024626B1 (pt) 2014-04-23 2015-04-22 Compostos 1h-pirrolo[2,3-c]piridin-7(6h)-onas e pirazolo[3,4-c]piridin-7 (6h)-onas, uso dos mesmos, composição farmacêutica que os compreende e método de inibição de uma proteína bet

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US (7) US9540368B2 (pt)
EP (3) EP3674302B1 (pt)
JP (2) JP6572237B2 (pt)
KR (2) KR20220113552A (pt)
CN (1) CN106414442B (pt)
AR (1) AR100160A1 (pt)
AU (3) AU2015249810B2 (pt)
BR (1) BR112016024626B1 (pt)
CA (1) CA2946731C (pt)
CL (1) CL2016002681A1 (pt)
CR (2) CR20200231A (pt)
CY (2) CY1122948T1 (pt)
DK (2) DK3674302T3 (pt)
EA (2) EA039678B1 (pt)
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Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA035469B1 (ru) 2013-03-15 2020-06-22 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
JP2016523964A (ja) 2013-07-08 2016-08-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｂｅｔタンパク質阻害剤としての三環式複素環
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
MX2016013851A (es) 2014-04-23 2017-07-14 Incyte Corp 1h-pirrolo[2,3-c]piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h) -onas como inhibidores de proteinas de bromodominio y extra terminal (bet).
EP3194406B8 (en) 2014-09-15 2021-03-31 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
MA40940A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
CN107108613B (zh) 2014-11-10 2020-02-25 基因泰克公司 布罗莫结构域抑制剂及其用途
MA40943A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
JP6709792B2 (ja) 2015-01-29 2020-06-17 ジェネンテック， インコーポレイテッド 治療用化合物およびその使用
AR104259A1 (es) 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
US10501438B2 (en) 2015-08-11 2019-12-10 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
CA2994478C (en) 2015-08-12 2023-10-03 Neomed Institute Substituted benzimidazoles, their preparation and their use as pharmaceuticals
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
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
LT3442972T (lt) 2016-04-15 2020-06-10 Abbvie Inc. Bromodomeno inhibitoriai
CR20220651A (es) 2016-06-20 2023-01-23 Incyte Corp FORMAS SOLIDAS CRISTALINAS DE UN INHIBIDOR DE BET (Divisional expediente 2019-0027.)
CA3045855A1 (en) 2016-11-10 2018-05-17 Shandong Luoxin Pharmaceutical Group Stock Co., Ltd. Nitrogenous macrocyclic compound, preparation method therefor, pharmaceutical composition and application thereof
CN110167939B (zh) * 2017-01-11 2021-12-31 江苏豪森药业集团有限公司 吡咯并[2,3-c]吡啶类衍生物、其制备方法及其在医药上的应用
SG11202000431PA (en) 2017-07-18 2020-02-27 Nuvation Bio Inc 1,8-naphthyridinone compounds and uses thereof
WO2019018584A1 (en) 2017-07-18 2019-01-24 GiraFpharma LLC HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
CA3081753A1 (en) 2017-11-06 2019-05-09 Centre National De La Recherche Scientifique Xanthine derivatives and uses thereof as inhibitors of bromodomains of bet proteins
MX2020006612A (es) * 2017-12-20 2020-11-09 Betta Pharmaceuticals Co Ltd Compuesto que funciona como inhibidor de proteína de bromodominio y composición.
FI3728207T3 (fi) 2017-12-21 2023-04-24 Ribon Therapeutics Inc Kinatsolinoneja parp14:n inhibiittoreina
JP2021512960A (ja) * 2018-02-06 2021-05-20 シャンハイ ハイファ ファーマシューティカル カンパニー，リミティッド Ｂｅｔ阻害活性を有する化合物並びにその製造方法及び使用
CN110776508B (zh) * 2018-07-27 2021-07-16 海创药业股份有限公司 一种brd4抑制剂及其制备方法和用途
CN109580433B (zh) * 2018-10-26 2021-05-28 中国辐射防护研究院 一种常规爆炸放射性气溶胶扩散的源项估算方法
BR112021007982A2 (pt) 2018-10-30 2021-08-03 Nuvation Bio Inc. compostos heterocíclicos como inibidores de bet
CN109432093A (zh) * 2018-12-23 2019-03-08 黄泳华 由吡唑并吡啶酮类化合物构成的乙酰胆碱酯酶抑制剂的增效体系
AU2020208644A1 (en) 2019-01-18 2021-08-26 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
WO2020150676A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
CN111704610B (zh) * 2019-03-17 2022-03-22 上海凌达生物医药有限公司 一类吡咯酰胺并吡啶酮类化合物、制备方法和用途
CN110003204B (zh) * 2019-04-30 2020-08-11 上海勋和医药科技有限公司 一种bet蛋白抑制剂、其制备方法及用途
WO2020253711A1 (zh) * 2019-06-17 2020-12-24 中国科学院上海药物研究所 一种吡咯并吡啶酮类化合物、其制备方法、其组合物和用途
JP2022537349A (ja) * 2019-06-19 2022-08-25 ライボン・セラピューティクス・インコーポレイテッド 療法に使用するためのｐａｒｐ１４の標的タンパク質分解
US11584756B2 (en) 2019-07-02 2023-02-21 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
CN112625036A (zh) * 2019-10-08 2021-04-09 上海海和药物研究开发股份有限公司 一类具有brd4抑制活性的化合物、其制备方法及用途
WO2021130731A1 (en) 2019-12-27 2021-07-01 Lupin Limited Substituted tricyclic compounds
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
JP2023529365A (ja) 2020-06-03 2023-07-10 インサイト・コーポレイション 骨髄増殖性腫瘍の治療のための、ルキソリチニブとｉｎｃｂ０５７６４３との組合わせ
AU2021392700B2 (en) 2020-12-01 2023-11-23 Chengdu Easton Biopharmaceuticals Co., Ltd. Novel n-heterocyclic bet bromodomain inhibitor, and preparation method therefor and medical use thereof
WO2022132049A1 (en) * 2020-12-17 2022-06-23 National University Of Singapore Treating cancers using bet inhibitors
KR20230137368A (ko) 2021-01-19 2023-10-04 루핀 리미티드 암을 치료 및/또는 예방하기 위한 sos1 저해제들의약학적 조합물

Family Cites Families (167)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2404E (fr) 1899-12-05 1904-03-26 Louis Olivier Victor Parmentie Machine à copier les lettres
JPS59170313A (ja) 1983-03-14 1984-09-26 Kurimoto Iron Works Ltd スクリ−ンゲ−ト
JPS6053449A (ja) 1983-09-01 1985-03-27 M K Seikou Kk 洗車機
JPS6085739U (ja) 1983-11-18 1985-06-13 クラリオン株式会社 テ−プレコ−ダにおけるピンチロ−ラ装置
JPS6243003U (pt) 1985-09-05 1987-03-14
JPH0314566A (ja) 1989-06-09 1991-01-23 Sankyo Co Ltd ベンズイミダゾール誘導体
US5244912A (en) 1991-03-28 1993-09-14 Eli Lilly And Company 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz(cd)indoles and pharmaceutical use thereof
FR2710915B1 (fr) 1993-10-04 1995-11-24 Synthelabo Dérivés de pipéridine, leur préparation et leur utilisation en thérapeutique.
GB9410469D0 (en) 1994-05-25 1994-07-13 Erba Farmitalia Imidazolylalkyl derivatives of imidazo (5,1-c) (1,4) benzoxazin-1-one and process for their preparation
FR2731708B1 (fr) 1995-03-13 1997-04-30 Synthelabo Derives de piperidine, leur procede de preparation et leur application en therapeutique
FR2747678B1 (fr) 1996-04-22 1998-05-22 Synthelabo Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique
US6287693B1 (en) 1998-02-25 2001-09-11 John Claude Savoir Stable shaped particles of crystalline organic compounds
AU5311401A (en) 2000-04-21 2001-11-07 Upjohn Co Compounds for treating fibromyalgia and chronic fatigue syndrome
CA2413330A1 (en) 2000-06-28 2002-01-03 Smithkline Beecham P.L.C. Wet milling process
FR2816619B1 (fr) 2000-11-15 2003-01-31 Sanofi Synthelabo Derives de benzimidazole, leur preparation et leur application en therapeutique
AR030121A1 (es) 2000-08-08 2003-08-13 Sanofi Aventis Derivados de benzimidazol, su preparacion y su aplicacion en terapeutica
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
BR0315688A (pt) 2002-11-22 2005-09-06 Japan Tobacco Inc Compostos, composições farmacêuticas e seus usos no tratamento ou prevenção de doenças ou condições de proliferação celular metabólicas
EP1462103A1 (en) 2003-03-25 2004-09-29 Faust Pharmaceuticals NO donors, combination products and uses as modulators of neurotransmitter release
CN1922141A (zh) 2004-02-23 2007-02-28 大日本住友制药株式会社 新的杂环化合物
CA2562244A1 (en) 2004-04-07 2005-10-27 Takeda Pharmaceutical Company Limited Cyclic compounds
US7713954B2 (en) 2004-09-30 2010-05-11 Roche Palo Alto Llc Compositions and methods for treating cognitive disorders
DE102005011058A1 (de) 2005-03-10 2006-09-14 Merck Patent Gmbh Substituierte Tetrahydro-pyrrolo-chinolinderivate
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
RU2008101923A (ru) 2005-08-05 2009-09-10 Астразенека Аб (Se) Трициклические бензимидазолы и их применение в качестве модуляторов метаботропного глутаматного рецептора
US8975259B2 (en) 2007-04-27 2015-03-10 University Of Rochester Compositions and methods for inhibiting G protein signaling
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
WO2009020559A2 (en) 2007-08-03 2009-02-12 The J. David Gladstone Institutes Agents that inhibit p-tefb interactions and methods of use thereof
KR101600634B1 (ko) 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 항암제
DE102008052618A1 (de) 2008-10-21 2010-04-22 Henkel Ag & Co. Kgaa Tricyclische Aldehyde und C,H-acide Verbindungen
WO2010111626A2 (en) 2009-03-27 2010-09-30 Takeda Pharmaceutical Company Limited Poly (adp-ribose) polymerase (parp) inhibitors
TW201103941A (en) 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
TW201105681A (en) 2009-06-10 2011-02-16 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
WO2011024987A1 (ja) 2009-08-31 2011-03-03 塩野義製薬株式会社 芳香族縮合へテロ環誘導体およびそれらを含有する医薬組成物
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US9023842B2 (en) 2009-11-05 2015-05-05 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP2955524A3 (en) 2009-11-05 2016-03-23 GlaxoSmithKline LLC Novel process
RS54645B1 (en) 2009-11-05 2016-08-31 Glaxosmithkline Llc BENZODIAZEPINE AS A BROMODOMEN INHIBITOR
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
MX2012012353A (es) 2010-04-23 2013-02-07 Kineta Inc Compuestos anti-virales.
BR122014024883A2 (pt) 2010-05-14 2019-08-20 Dana-Farber Cancer Institute, Inc. Compostos no tratamento de neoplasia
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
WO2011143657A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Male contraceptive compositions and methods of use
BR112012029057A2 (pt) 2010-05-14 2020-10-13 Dana-Farber Cancer Institute, Inc. composições e métodos de tratamento de leucemia
EP2585465B1 (en) 2010-06-22 2014-11-12 GlaxoSmithKline LLC Benzotriazolodiazepine compounds inhibitors of bromodomains
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
CA2825028A1 (en) 2011-02-09 2012-08-16 F. Hoffman-La Roche Ag Heterocyclic compounds as pi3 kinase inhibitors
AU2012220620A1 (en) 2011-02-23 2013-10-03 Icahn School Of Medicine At Mount Sinai Inhibitors of bromodomains as modulators of gene expression
BR112013024122A2 (pt) 2011-03-21 2019-09-24 Hoffmann La Roche compostos de benzoxazepina seletivos para p110 delta pi3k e métodos de uso
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2721031B1 (en) 2011-06-17 2016-01-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012178208A2 (en) 2011-06-24 2012-12-27 The Trustees Of The Stevens Institute Of Technology Selective inhibitors of histone deacetylase isoform 6 and methods thereof
JP2013010719A (ja) 2011-06-30 2013-01-17 Dainippon Sumitomo Pharma Co Ltd ベンズイミダゾロンおよびオキシインドール誘導体ならびにそれらの医薬用途
JP2014524409A (ja) 2011-07-29 2014-09-22 ザ・チルドレンズ・ホスピタル・オブ・フィラデルフィア Ｈｉｖの治療のための組成物および方法
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
PL2751083T3 (pl) 2011-08-31 2018-08-31 Otsuka Pharmaceutical Co., Ltd. Związek chinolonowy
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
EP2757887B1 (en) 2011-09-22 2017-04-26 VIIV Healthcare UK Limited Pyrrolopyridinone compounds and methods for treating hiv
CN103857391B (zh) 2011-09-30 2016-06-08 沈阳蓝桑医药生物技术研发有限公司 含有瑞利格内酯的药物组合物及其应用
WO2013060636A1 (en) 2011-10-25 2013-05-02 Sanofi 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
DK2773354T3 (da) 2011-11-01 2019-08-05 Resverlogix Corp Oralformuleringer med øjeblikkelig frigivelse for substituerede quinazolinoner
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
WO2013148197A1 (en) 2012-03-28 2013-10-03 The J. David Gladstone Institutes Compositions and methods for reactivating latent immunodeficiency virus
US20130281396A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
WO2013155695A1 (en) 2012-04-20 2013-10-24 Abbott Laboratories Isoindolone derivatives
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
WO2013185284A1 (en) 2012-06-12 2013-12-19 Abbott Laboratories Pyridinone and pyridazinone derivatives
IN2014DN11269A (pt) 2012-06-25 2015-10-09 Oncoethix Sa
US9610332B2 (en) 2012-07-18 2017-04-04 Massachusetts Institute Of Technology Compositions and methods for modulating BRD4 bioactivity
JP6333251B2 (ja) 2012-08-16 2018-05-30 バイエル ファーマ アクチエンゲゼルシャフト ２，３−ベンゾジアゼピン類
KR20150042231A (ko) 2012-08-16 2015-04-20 글락소스미스클라인 엘엘씨 소세포폐암을 치료하기 위한 벤조디아제핀
CN104781259B (zh) 2012-09-28 2018-06-01 拜耳制药股份公司 抑制bet蛋白的5-芳基三唑并氮杂*
IN2015DN03135A (pt) 2012-09-28 2015-10-02 Oncoethix Sa
RS59690B1 (sr) 2012-11-09 2020-01-31 Medicines For Malaria Venture Mmv Derivativi heteroarila i njihova upotreba
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
ES2625945T3 (es) 2012-11-14 2017-07-21 Glaxosmithkline Llc Tieno[3,2-c]piridin-4(5H)-onas como inhibidores de bet
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US20160193206A1 (en) 2012-12-20 2016-07-07 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones
JP2016509576A (ja) 2012-12-20 2016-03-31 バイエル ファーマ アクチエンゲゼルシャフト Ｂｅｔタンパク質阻害性ジヒドロキノキザリノン類
AU2013365926B9 (en) 2012-12-21 2019-01-17 Zenith Epigenetics Ltd. Novel heterocyclic compounds as bromodomain inhibitors
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
JP6404838B2 (ja) 2013-02-27 2018-10-17 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ブロモドメイン阻害剤として有用なカルバゾール化合物
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
CN105377851B (zh) 2013-03-11 2018-07-20 密执安州立大学董事会 Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法
MX2015012005A (es) 2013-03-11 2016-04-04 Abbvie Inc Inhibidores de bromodominio.
BR112015022674A2 (pt) 2013-03-11 2017-07-18 Abbvie Inc inibidores de bromodomínio
TWI635087B (zh) 2013-03-12 2018-09-11 艾伯維有限公司 四環布羅莫域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑
TW201443051A (zh) 2013-03-12 2014-11-16 Abbvie Inc 二氫－吡咯并吡啶酮抑制劑
EP2970193B1 (en) 2013-03-12 2018-07-25 AbbVie Inc. Pyrrole amide inhibitors
ES2654362T3 (es) 2013-03-14 2018-02-13 Glaxosmithkline Intellectual Property (No. 2) Limited Furopiridinas como inhibidores de bromodominio
EA028174B1 (ru) 2013-03-14 2017-10-31 Глаксосмитклайн Интеллекчуал Проперти (№2) Лимитед 2,3-дизамещенные производные 1-ацил-4-амино-1,2,3,4-тетрагидрохинолинов и их применение в качестве ингибиторов бромодомена
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
JP6464139B2 (ja) 2013-03-14 2019-02-06 コンバージーン・リミテッド・ライアビリティ・カンパニーＣｏｎｖｅｒｇｅｎｅ Ｌｌｃ ブロモドメイン含有タンパク質の阻害のための方法および組成物
AU2014236606A1 (en) 2013-03-15 2015-09-24 Epigenetix, Inc. Oxazolo(5,4-c)quinolin-2-one compounds as bromodomain inhibitors
SI2970265T1 (sl) 2013-03-15 2018-10-30 Plexxikon Inc. Heterociklične spojine in njihova uporaba
EA035469B1 (ru) 2013-03-15 2020-06-22 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
EP2978758B1 (en) 2013-03-27 2017-02-08 Boehringer Ingelheim International GmbH Dihydroquinazolinone analogues as brd4 inhibitors
JP6370368B2 (ja) 2013-03-27 2018-08-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｒｄ４阻害剤としてのインドリノン類似体
TWI530499B (zh) 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類
EP2996689A1 (en) 2013-04-17 2016-03-23 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
EA027139B1 (ru) 2013-04-26 2017-06-30 Бейджин, Лтд. Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны
TWI527811B (zh) 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
AU2014272774B2 (en) 2013-05-27 2016-12-08 Novartis Ag Imidazopyrrolidinone derivatives and their use in the treatment of disease
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
US9624247B2 (en) 2013-05-28 2017-04-18 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
PT3004112T (pt) 2013-05-28 2017-12-11 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona e sua utilização no tratamento de doença
ITMI20130991A1 (it) 2013-06-17 2014-12-18 Industrie De Nora Spa Sistema per la misurazione di correnti presenti sugli elettrodi in celle elettrolitiche interconnesse.
WO2014202578A1 (de) 2013-06-17 2014-12-24 Bayer Pharma Aktiengesellschaft Substituierte phenyl-2,3-benzodiazepine
EA035601B1 (ru) 2013-06-21 2020-07-14 Зенит Эпидженетикс Лтд. Бициклические ингибиторы бромодомена
CA2915561C (en) 2013-06-21 2020-09-22 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
MX2015017963A (es) 2013-06-28 2016-11-10 Abbvie Inc Inhibidores de bromodominio.
JP2016523964A (ja) 2013-07-08 2016-08-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｂｅｔタンパク質阻害剤としての三環式複素環
JP6441334B2 (ja) 2013-07-16 2018-12-19 ビーエーエスエフ ソシエタス・ヨーロピアＢａｓｆ Ｓｅ 除草性アジン
US9975896B2 (en) 2013-07-25 2018-05-22 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
KR101672096B1 (ko) 2013-09-30 2016-11-02 주식회사 엘지화학 헤테로환 화합물 및 이를 포함하는 유기 발광 소자
FI3640241T3 (fi) 2013-10-18 2023-01-13 Bromodomeeni-inhibiittorit
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US20150148372A1 (en) 2013-11-26 2015-05-28 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
JP2016539970A (ja) 2013-12-09 2016-12-22 アッヴィ・インコーポレイテッド ブロモドメイン阻害薬として有用なジヒドロピリジノンおよびジヒドロピリダジノン誘導体
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
KR102394518B1 (ko) 2014-01-09 2022-05-06 오리온 코포레이션 브로모도메인 억제제로서의 비사이클릭 헤테로사이클릭 유도체
JP2017511801A (ja) 2014-02-28 2017-04-27 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン ＢＥＴブロモドメイン阻害剤としての９Ｈ−ピリミド［４，５−ｂ］インドールおよび関連類似体
MX2016013851A (es) * 2014-04-23 2017-07-14 Incyte Corp 1h-pirrolo[2,3-c]piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h) -onas como inhibidores de proteinas de bromodominio y extra terminal (bet).
WO2015162169A1 (en) 2014-04-23 2015-10-29 Basf Se Diaminotriazine compounds as herbicides
RS60524B1 (sr) 2014-04-23 2020-08-31 Takeda Pharmaceuticals Co Derivati izoindolin-1-ona kao pozitivni alosterni modulator aktivnosti holinergičkog muskarinskog m1 receptora za lečenje alzheimer-ove bolesti
EP3137086A4 (en) 2014-05-02 2017-12-27 Oncoethix GmbH Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or alk+non-small cell lung cancer using thienotriazolodiazepine compounds
KR20160145833A (ko) 2014-05-02 2016-12-20 온코에틱스 게엠베하 티에노트리아졸로디아제핀 화합물을 사용한 급성 골수성 백혈병 및/또는 급성 림프아구성 백혈병의 치료 방법
WO2015169951A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating triple-negative breast cancer using thienotriazolodiazepine compounds
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
US10065951B2 (en) 2014-05-30 2018-09-04 Icahn School Of Medicine At Mount Sinai Small molecule transcription modulators of bromodomains
ES2725928T3 (es) 2014-06-20 2019-09-30 Constellation Pharmaceuticals Inc Formas cristalinas de 2-((4S)-6-(4-clorofenil)-1-metil-4H-benzo[c]isoxazolo[4,5-e]azepin-4-il)acetamida
EP3194406B8 (en) 2014-09-15 2021-03-31 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
SI3209656T1 (sl) 2014-10-24 2020-07-31 Bristol-Myers Squibb Company Spojine indol karboksamida, uporabne kot kinazni inhibitorji
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
CA2974153A1 (en) 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins
WO2016186453A1 (en) 2015-05-20 2016-11-24 Kainos Medicine, Inc. Quinoline derivatives as bromodomain inhibitors
JP6614585B2 (ja) 2015-05-29 2019-12-04 塩野義製薬株式会社 Ｈｉｖ複製阻害作用を有する含窒素３環性誘導体
CN105039258B (zh) 2015-07-03 2018-04-17 北京大学 将非神经元细胞重编程为神经元样细胞的方法和组合物
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN105254635A (zh) 2015-10-30 2016-01-20 中国药科大学 一类咪唑并吡嗪类化合物及其药物组合物和用途
US20170127985A1 (en) 2015-11-11 2017-05-11 Medtronic Minimed, Inc. Sensor set
CA3007168A1 (en) 2015-12-14 2017-06-22 Zenith Epigenetics Ltd. 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors
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
JP2019508494A (ja) 2016-02-05 2019-03-28 チーア タイ ティエンチン ファーマシューティカル グループ カンパニー，リミティド ブロモドメインタンパク質阻害剤の三環式化合物、並びにその製造、医薬組成物及び使用
CR20220651A (es) 2016-06-20 2023-01-23 Incyte Corp FORMAS SOLIDAS CRISTALINAS DE UN INHIBIDOR DE BET (Divisional expediente 2019-0027.)
CN108069958A (zh) 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 一种含氮杂环类化合物、其制备方法、药物组合物及应用

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