CL2016002681A1 - 1h-pirrolo[2,3-c]piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h)-onas como inhibidores de proteínas bet. - Google Patents

1h-pirrolo[2,3-c]piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h)-onas como inhibidores de proteínas bet.

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Publication number
CL2016002681A1
CL2016002681A1 CL2016002681A CL2016002681A CL2016002681A1 CL 2016002681 A1 CL2016002681 A1 CL 2016002681A1 CL 2016002681 A CL2016002681 A CL 2016002681A CL 2016002681 A CL2016002681 A CL 2016002681A CL 2016002681 A1 CL2016002681 A1 CL 2016002681A1
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CL
Chile
Prior art keywords
pyridin
ones
inhibitors
pyrazolo
pyrrolo
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CL2016002681A
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English (en)
Inventor
Andrew P Combs
Thomas P Maduskuie Jr
Nikoo Falahatpisheh
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Incyte Corp
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Publication of CL2016002681A1 publication Critical patent/CL2016002681A1/es

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    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

<p>COMPUESTOS DERIVADOS DE 1H-PIRROLO[2,3-c]PIRIDIN-7(6H)-ONAS Y PIRAZOLO[3,4-c]PIRIDIN-7(6H)-ONAS O SUS SALES, COMO INHIBIDORES DE PROTEÍNAS BET; COMPOSICION FARMACEUTICA QUE LOS COMPRENDE, UTIL PARA EL TRATAMIENTO DE UN TRASTORNO PROLIFERATIVO TAL COMO CANCER, ALERGIA, ARTRITIS, EPOC, PSORIASIS, ENTRE OTRAS.  </p>
CL2016002681A 2014-04-23 2016-10-21 1h-pirrolo[2,3-c]piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h)-onas como inhibidores de proteínas bet. CL2016002681A1 (es)

Applications Claiming Priority (1)

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US201461983289P 2014-04-23 2014-04-23

Publications (1)

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CL2016002681A1 true CL2016002681A1 (es) 2017-02-03

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CL2016002681A CL2016002681A1 (es) 2014-04-23 2016-10-21 1h-pirrolo[2,3-c]piridin-7(6h)-onas y pirazolo[3,4-c]piridin-7(6h)-onas como inhibidores de proteínas bet.

Country Status (36)

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US (7) US9540368B2 (es)
EP (3) EP3674302B1 (es)
JP (2) JP6572237B2 (es)
KR (2) KR102430144B1 (es)
CN (1) CN106414442B (es)
AR (1) AR100160A1 (es)
AU (3) AU2015249810B2 (es)
BR (1) BR112016024626B1 (es)
CA (1) CA2946731C (es)
CL (1) CL2016002681A1 (es)
CR (2) CR20200231A (es)
CY (2) CY1122948T1 (es)
DK (2) DK3674302T3 (es)
EA (2) EA039678B1 (es)
EC (1) ECSP16088983A (es)
ES (2) ES2784846T3 (es)
FI (1) FI3674302T3 (es)
HR (2) HRP20230340T1 (es)
HU (2) HUE061770T2 (es)
IL (3) IL248415B (es)
LT (2) LT3674302T (es)
MA (1) MA39985B1 (es)
ME (1) ME03763B (es)
MX (2) MX2016013851A (es)
MY (1) MY180775A (es)
NZ (3) NZ763740A (es)
PE (1) PE20170144A1 (es)
PH (1) PH12016502115A1 (es)
PL (2) PL3674302T3 (es)
PT (2) PT3134403T (es)
RS (2) RS60139B1 (es)
SG (2) SG10201809353TA (es)
SI (2) SI3674302T1 (es)
TW (2) TWI735002B (es)
UA (1) UA119870C2 (es)
WO (1) WO2015164480A1 (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112015022942B1 (pt) 2013-03-15 2022-02-22 Incyte Holdings Corporation Compostos heterocíciclos tricíclicos, método para inibir proteína bet in vitro e composição farmacêutica compreendendo os referidos compostos
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
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
NZ763740A (en) * 2014-04-23 2023-06-30 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
JP6599979B2 (ja) 2014-09-15 2019-10-30 インサイト・コーポレイション Betタンパク質阻害剤として用いるための三環式複素環化合物
MA40940A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
MA40943A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
JP6639497B2 (ja) 2014-11-10 2020-02-05 ジェネンテック, インコーポレイテッド ブロモドメインインヒビターおよびその使用
WO2016123391A1 (en) 2015-01-29 2016-08-04 Genentech, Inc. Therapeutic compounds and uses thereof
AR104259A1 (es) * 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
WO2017024408A1 (en) * 2015-08-11 2017-02-16 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
WO2017024406A1 (en) * 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
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
WO2017075377A1 (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
PL3442972T3 (pl) 2016-04-15 2020-07-27 Abbvie Inc. Inhibitory bromodomeny
FI3472157T3 (fi) 2016-06-20 2023-06-01 Incyte Corp Bet-inhibiittorin kiteisiä kiinteitä muotoja
WO2018086605A1 (zh) 2016-11-10 2018-05-17 山东罗欣药业集团股份有限公司 一种含氮大环类化合物、其制备方法、药物组合物及应用
TW201825490A (zh) * 2017-01-11 2018-07-16 大陸商江蘇豪森藥業集團有限公司 吡咯並[2,3-c]吡啶類衍生物、其製備方法及其在醫藥上的應用
JP2020527588A (ja) 2017-07-18 2020-09-10 ニューベイション・バイオ・インコーポレイテッドNuvation Bio Inc. アデノシンアンタゴニストとしてのヘテロ環式化合物
SG11202000431PA (en) 2017-07-18 2020-02-27 Nuvation Bio Inc 1,8-naphthyridinone compounds and uses thereof
JP7254075B2 (ja) 2017-11-06 2023-04-07 サントル ナショナル ドゥ ラ ルシェルシュ シアンティフィック キサンチン誘導体及びbetタンパク質のブロモドメインの阻害剤としてのその使用
JP2021506903A (ja) 2017-12-20 2021-02-22 貝達薬業股▲ふん▼有限公司Betta Pharmaceuticals Co.,Ltd ブロモドメインタンパク質阻害剤である化合物、および組成物
TWI813611B (zh) 2017-12-21 2023-09-01 美商律幫治療股份有限公司 作為parp14抑制劑之喹唑啉酮
CN111683932A (zh) * 2018-02-06 2020-09-18 上海海和药物研究开发有限公司 具有bet抑制活性的化合物及其制备方法和用途
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***放射性气溶胶扩散的源项估算方法
EP3873474A4 (en) 2018-10-30 2022-07-13 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS AS BET Inhibitors
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
EP3911324A4 (en) 2019-01-18 2022-08-17 Nuvation Bio Inc. 1,8-NAPHTHYRIDINONE COMPOUNDS AND THEIR USES
CA3133131A1 (en) * 2019-03-17 2020-09-24 Shanghai Ringene Biopharma Co., Ltd. Pyrrole amidopyridone compound, preparation method therefor and use thereof
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
CN112094266B (zh) * 2019-06-17 2023-03-21 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
MA56513A (fr) * 2019-06-19 2022-04-27 Ribon Therapeutics Inc Dégradation de protéine ciblée de parp14 pour une utilisation en thérapie
MX2022000050A (es) 2019-07-02 2022-05-24 Nuvation Bio Inc Compuestos heterocíclicos como inhibidores de bromodominio extraterminal (bet).
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
BR112022012641A2 (pt) 2019-12-27 2022-09-06 Lupin Ltd Compostos tricíclicos substituídos
AU2020451061A1 (en) 2020-06-03 2022-12-15 Incyte Corporation Combination of ruxolitinib with INCB057643 for treatment of myeloproliferative neoplasms
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4183785A1 (en) * 2020-12-01 2023-05-24 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
EP4281078A1 (en) 2021-01-19 2023-11-29 Lupin Limited Pharmaceutical combinations of sos1 inhibitors for treating and/or preventing cancer

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 (es) 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
CA2405565A1 (en) 2000-04-21 2001-11-01 Pharmacia & Upjohn Company Compounds for treating fibromyalgia and chronic fatigue syndrome
CZ303572B6 (cs) 2000-06-28 2012-12-12 Smithkline Beecham P. L. C. Jemne rozmelnený prostredek a zpusob jeho prípravy
FR2816619B1 (fr) 2000-11-15 2003-01-31 Sanofi Synthelabo Derives de benzimidazole, leur preparation et leur application en therapeutique
MXPA03000753A (es) 2000-08-08 2003-10-15 Sanofi Synthelabo Derivados de benzimidazola, su preparacion y su aplicacion terapeutica.
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
RU2342388C2 (ru) 2002-11-22 2008-12-27 Джапан Тобакко Инк. Конденсированные бициклические азотсодержащие гетероциклы, обладающие dgat ингибирующим действием
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
EP1732541A4 (en) 2004-04-07 2008-03-05 Takeda Pharmaceutical 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
CA2616020A1 (en) 2005-08-05 2007-02-15 Astrazeneca Ab Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators
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
WO2009084693A1 (ja) 2007-12-28 2009-07-09 Mitsubishi Tanabe Pharma Corporation 抗癌剤
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
TW201105681A (en) 2009-06-10 2011-02-16 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
TW201103941A (en) 2009-06-10 2011-02-01 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
ME02356B (me) 2009-11-05 2016-06-20 Glaxosmithkline Llc Inhibitor bromodomena benzodiazepina
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
JP5524343B2 (ja) 2009-11-05 2014-06-18 グラクソスミスクライン エルエルシー ベンゾジアゼピンブロモドメイン阻害剤
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
EP2955524A3 (en) 2009-11-05 2016-03-23 GlaxoSmithKline LLC Novel process
AU2011242683A1 (en) 2010-04-23 2012-12-13 Kineta, Inc. Anti-viral compounds
MX354217B (es) 2010-05-14 2018-02-19 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
BR122014024883A2 (pt) 2010-05-14 2019-08-20 Dana-Farber Cancer Institute, Inc. Compostos no tratamento de neoplasia
CN103180318B (zh) 2010-05-14 2017-05-10 达那-法伯癌症研究所 雄性避孕组合物以及使用方法
US9085582B2 (en) 2010-06-22 2015-07-21 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
JP5766820B2 (ja) 2011-02-09 2015-08-19 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Pi3キナーゼ阻害剤としての複素環化合物
US20140066410A1 (en) 2011-02-23 2014-03-06 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
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106799D0 (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
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2721031B1 (en) 2011-06-17 2016-01-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US20150197497A1 (en) 2011-06-24 2015-07-16 Dana-Farber Cancer Institute, Inc. 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
AU2012290261A1 (en) 2011-07-29 2014-02-20 The Children's Hospital Of Philadelphia Compositions and methods for the treatment of HIV
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
EA030867B1 (ru) 2011-08-31 2018-10-31 Оцука Фармасьютикал Ко., Лтд. Производное хинолона
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
WO2013043553A1 (en) 2011-09-22 2013-03-28 Glaxosmithkline Llc Pyrrolopyridinone compounds and methods for treating hiv
WO2013044511A1 (zh) 2011-09-30 2013-04-04 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
PT2773354T (pt) 2011-11-01 2019-07-17 Resverlogix Corp Formulações orais de libertação imediata para quinazolinonas substituídas
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
EP2838881B1 (en) 2012-04-20 2018-08-08 AbbVie Inc. Isoindolone derivatives
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
CN104718201A (zh) 2012-06-12 2015-06-17 艾伯维公司 吡啶酮和哒嗪酮衍生物
MX2014015986A (es) 2012-06-25 2016-02-11 Oncoethix Gmbh Metodo para tratar linfoma utilizando compuestos de tienotriazolodiazepina.
WO2014015175A1 (en) 2012-07-18 2014-01-23 Massachusetts Institute Of Technology Compositions and methods for modulating brd4 bioactivity
MX2015001880A (es) 2012-08-16 2015-05-11 Bayer Pharma AG 2,3-benzodiacepinas.
CN104582708A (zh) 2012-08-16 2015-04-29 葛兰素史克有限责任公司 用于治疗小细胞肺癌的苯并二氮*类
US20140107107A1 (en) 2012-09-28 2014-04-17 Oncoethix Sa Pharmaceutical formulation containing thienotriazolodiazepine compounds
ES2625959T3 (es) 2012-09-28 2017-07-21 Bayer Pharma Aktiengesellschaft 5-Aril-triazolo-azepinas inhibidoras de la proteína BET
SG11201503517WA (en) 2012-11-09 2015-06-29 Jacobus Pharmaceutical Company Inc Heteroaryl derivatives and uses thereof
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
WO2014078257A1 (en) 2012-11-14 2014-05-22 Glaxosmithkline Llc Thieno[3,2-c]pyridin-4(5h)-ones as bet inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US20160193206A1 (en) 2012-12-20 2016-07-07 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones
CN104995190A (zh) 2012-12-20 2015-10-21 拜耳医药股份有限公司 Bet蛋白抑制剂二氢喹喔啉酮
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
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
CN105189488B (zh) 2013-02-27 2018-07-24 百时美施贵宝公司 用作溴区结构域抑制剂的咔唑化合物
AU2014249192B2 (en) 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
TW201444843A (zh) 2013-03-11 2014-12-01 Abbvie Inc 溴區結構域蛋白抑制劑
JP2016512524A (ja) 2013-03-11 2016-04-28 アッヴィ・インコーポレイテッド ブロモドメイン阻害剤
CN105026403B (zh) 2013-03-12 2018-05-18 艾伯维公司 四环布罗莫结构域抑制剂
MX2015011984A (es) 2013-03-12 2015-12-15 Abbvie Inc Inhibidores de bromodominio de dihidro-pirrolopiridinona.
WO2014165127A1 (en) 2013-03-12 2014-10-09 Abbvie Inc. Pyrrole amide inhibitors
CA2901537C (en) 2013-03-14 2021-09-07 Glaxosmithkline Intellectual Property (No.2) Limited 2,3-disubstituted 1- acyl-4-amino-1 ,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
US9670221B2 (en) 2013-03-14 2017-06-06 Glaxosmithkline Intellectual Property (No. 2) Limited Furopyridines as bromodomain inhibitors
MX367420B (es) 2013-03-14 2019-08-21 Convergene Llc Metodos y composiciones para inhibicion de proteinas que contienen bromodominio.
BR112015022942B1 (pt) 2013-03-15 2022-02-22 Incyte Holdings Corporation Compostos heterocíciclos tricíclicos, método para inibir proteína bet in vitro e composição farmacêutica compreendendo os referidos compostos
CA2904364A1 (en) 2013-03-15 2014-09-25 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
KR102244719B1 (ko) 2013-03-15 2021-04-26 플렉시콘 인코퍼레이티드 헤테로시클릭 화합물 및 그의 용도
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
EP2978758B1 (en) 2013-03-27 2017-02-08 Boehringer Ingelheim International GmbH Dihydroquinazolinone analogues as brd4 inhibitors
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
WO2014170350A1 (en) 2013-04-17 2014-10-23 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
WO2014173241A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
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
MX2015016344A (es) 2013-05-27 2016-03-01 Novartis Ag Derivados de imidazo-pirrolidinona y su uso en el tratamiento de enfermedades.
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
MX2015016421A (es) 2013-05-28 2016-03-03 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades.
PL3004112T3 (pl) 2013-05-28 2018-02-28 Novartis Ag Pochodne pirazolo-pirolidyn-4-onu oraz ich zastosowanie w leczeniu choroby
CA2915419A1 (en) 2013-06-17 2014-12-24 Bayer Pharma Aktiengesellschaft Substituted phenyl-2,3-benzodiazepines
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.
CA2915622C (en) 2013-06-21 2020-08-18 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
AU2014284616B2 (en) 2013-06-21 2019-02-28 Zenith Epigenetics Ltd. Novel bicyclic bromodomain inhibitors
RU2016102647A (ru) 2013-06-28 2017-08-01 Эббви Инк. Ингибиторы бромодомена
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
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
AU2014292193B2 (en) 2013-07-16 2018-04-26 Basf Se Herbicidal azines
WO2015013635A2 (en) 2013-07-25 2015-01-29 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
PL3640241T3 (pl) 2013-10-18 2022-12-05 Celgene Quanticel Research, Inc. Inhibitory bromodomeny
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081246A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 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
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP3083559B1 (en) 2013-12-20 2021-03-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
HUE041546T2 (hu) 2014-01-09 2019-05-28 Orion Corp Biciklusos heterociklusos származékvegyületek mint bromo doméninhibitorok
CN107074861A (zh) 2014-02-28 2017-08-18 密执安大学评议会 作为bet溴结构域抑制剂的9h嘧啶并[4,5‑b]吲哚和相关类似物
NZ763740A (en) 2014-04-23 2023-06-30 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
NZ725921A (en) 2014-04-23 2023-09-29 Takeda Pharmaceuticals Co Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease
JP6538077B2 (ja) 2014-04-23 2019-07-03 ビーエーエスエフ ソシエタス・ヨーロピアBasf Se 除草剤としてのジアミノトリアジン化合物
RU2016146099A (ru) 2014-05-02 2018-06-05 Онкоэтикс Гмбх Способ лечения острого миелоидного лейкоза и/или острого лимфобластного лейкоза с помощью тиенотриазолодиазепиновых соединений
CA2947593A1 (en) 2014-05-02 2015-11-05 Oncoethix Gmbh Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or alk+non-small cell lung cancer using thienotriazolodiazepine compounds
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
WO2015169951A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating triple-negative breast cancer using thienotriazolodiazepine compounds
US10065951B2 (en) 2014-05-30 2018-09-04 Icahn School Of Medicine At Mount Sinai Small molecule transcription modulators of bromodomains
US9969747B2 (en) 2014-06-20 2018-05-15 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[C]isoxazolo[4,5-e]azepin-4-yl)acetamide
JP6599979B2 (ja) 2014-09-15 2019-10-30 インサイト・コーポレイション Betタンパク質阻害剤として用いるための三環式複素環化合物
AR102426A1 (es) 2014-10-24 2017-03-01 Bristol Myers Squibb Co Compuestos de indolcarboxamida como inhibidores de btk
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
WO2016123709A1 (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
CA2987384A1 (en) 2015-05-29 2016-12-08 Shionogi & Co., Ltd. Nitrogen-containing tricyclic derivative having hiv replication inhibitory activity
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
WO2017075377A1 (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
US20190263799A1 (en) 2015-12-14 2019-08-29 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
WO2017133681A1 (zh) 2016-02-05 2017-08-10 正大天晴药业集团股份有限公司 溴区结构域蛋白抑制剂的三环类化合物及其制备、药物组合物和用途
FI3472157T3 (fi) 2016-06-20 2023-06-01 Incyte Corp Bet-inhibiittorin kiteisiä kiinteitä muotoja
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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