CO2017004898A2 - Inhibidores del bromodominio derivados de 6h-tieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepina - Google Patents

Inhibidores del bromodominio derivados de 6h-tieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepina

Info

Publication number
CO2017004898A2
CO2017004898A2 CONC2017/0004898A CO2017004898A CO2017004898A2 CO 2017004898 A2 CO2017004898 A2 CO 2017004898A2 CO 2017004898 A CO2017004898 A CO 2017004898A CO 2017004898 A2 CO2017004898 A2 CO 2017004898A2
Authority
CO
Colombia
Prior art keywords
diazepine
thieno
triazolo
bromodomain inhibitors
inhibitors derived
Prior art date
Application number
CONC2017/0004898A
Other languages
English (en)
Spanish (es)
Inventor
B Steven Landau
Michael Kagey
Original Assignee
Tensha Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tensha Therapeutics Inc filed Critical Tensha Therapeutics Inc
Publication of CO2017004898A2 publication Critical patent/CO2017004898A2/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/04—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 condensed with carbocyclic rings or ring systems
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    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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CONC2017/0004898A 2014-10-27 2017-05-16 Inhibidores del bromodominio derivados de 6h-tieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepina CO2017004898A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462068983P 2014-10-27 2014-10-27
PCT/US2015/057538 WO2016069578A1 (en) 2014-10-27 2015-10-27 Bromodomain inhibitors

Publications (1)

Publication Number Publication Date
CO2017004898A2 true CO2017004898A2 (es) 2017-10-31

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ID=54478264

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CONC2017/0004898A CO2017004898A2 (es) 2014-10-27 2017-05-16 Inhibidores del bromodominio derivados de 6h-tieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepina

Country Status (19)

Country Link
US (1) US10124009B2 (enExample)
EP (1) EP3212654B1 (enExample)
JP (1) JP6715243B2 (enExample)
KR (1) KR20170068597A (enExample)
CN (1) CN107635979A (enExample)
AU (1) AU2015339511B2 (enExample)
BR (1) BR112017008714A2 (enExample)
CA (1) CA2965330A1 (enExample)
CL (1) CL2017001046A1 (enExample)
CO (1) CO2017004898A2 (enExample)
CR (1) CR20170219A (enExample)
EA (1) EA033325B1 (enExample)
IL (1) IL251784A0 (enExample)
MX (1) MX376748B (enExample)
PE (1) PE20171042A1 (enExample)
PH (1) PH12017500745A1 (enExample)
SG (1) SG11201703414VA (enExample)
UA (1) UA122130C2 (enExample)
WO (1) WO2016069578A1 (enExample)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
EP2902030B1 (en) 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
EP3608317A1 (en) 2012-01-12 2020-02-12 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
EA035727B1 (ru) 2013-10-18 2020-07-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы бромодомена
EP3066101B1 (en) 2013-11-08 2020-07-29 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
CN106456653A (zh) * 2014-02-28 2017-02-22 腾沙治疗公司 高胰岛素血症相关病症的治疗
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
SG11201703414VA (en) 2014-10-27 2017-05-30 Tensha Therapeutics Inc Bromodomain inhibitors
JP7269731B2 (ja) 2015-03-18 2023-05-09 アルビナス・オペレーションズ・インコーポレイテッド 標的タンパク質の分解向上のための化合物および方法
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
US20190247302A1 (en) * 2016-10-21 2019-08-15 University Of Miami Materials and methods for treating ophthalmic inflammation
IL312367A (en) 2017-01-31 2024-06-01 Arvinas Operations Inc Cereblon ligands and bifunctional compounds comprising the same
CN109503618A (zh) * 2017-09-14 2019-03-22 成都海创药业有限公司 一种brd4抑制剂
EP3743066A4 (en) 2018-01-26 2021-09-08 Yale University IMIDE-BASED PROTEOLYSIS MODULATORS AND RELATED METHODS OF USE
KR20210003804A (ko) 2018-04-13 2021-01-12 아비나스 오퍼레이션스, 인코포레이티드 세레브론 리간드 및 이를 포함하는 2작용성 화합물
CN112312916A (zh) 2018-06-13 2021-02-02 戴布里股份公司 缩合三氮杂卓衍生物的制备及其作为bet抑制剂的用途
JP7526721B2 (ja) * 2018-09-11 2024-08-01 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト 癌治療のためのブロモドメインＢＲＤ４阻害剤としてのｔｅｒｔ－ブチル（Ｓ）－２－（４－（フェニル）－６Ｈ－チエノ［３，２－ｆ］［１，２，４］トリアゾロ［４，３－ａ］［１，４］ジアゼピン－６－イル）アセテート誘導体及び関連化合物
CN118638043A (zh) 2019-12-19 2024-09-13 阿尔维纳斯运营股份有限公司 用于雄激素受体的靶向降解的化合物和方法
WO2024123929A1 (en) * 2022-12-06 2024-06-13 Bioventures, Llc Development of potent dual hdac/brd4 inhibitors
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
WO2025053994A1 (en) * 2023-09-08 2025-03-13 The Regents Of The University Of California Small molecule enhancers of secreted clusterin (sclu)

Family Cites Families (132)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2951540A (en) 1956-11-05 1960-09-06 Gen Motors Corp Propeller brake
US3709898A (en) 1971-02-09 1973-01-09 Upjohn Co Process for the production of triazolobenzodiazepines and intermediates
US3681343A (en) 1971-05-11 1972-08-01 Upjohn Co 6-phenyl-s-triazolo{8 4,3-a{9 {8 1,4{9 {0 benzodiazepines
US3812259A (en) 1971-08-09 1974-05-21 Upjohn Co Animal feed and process
CH622019A5 (en) 1975-10-23 1981-03-13 Upjohn Co Process for the preparation of aminotriazolobenzodiazepines
FR2329668A1 (fr) 1975-10-27 1977-05-27 Upjohn Co Procede de preparation d'aminotriazolobenzodiazepines
EP0087850A1 (en) 1982-01-04 1983-09-07 The Upjohn Company Benzodiazepines for anti-hypertensive use
DE3435973A1 (de) 1984-10-01 1986-04-10 Boehringer Ingelheim KG, 6507 Ingelheim Diazepine enthaltende pharmazeutische zusammensetzungen mit paf-antagonistischer wirkung
DE3724164A1 (de) 1986-07-25 1988-01-28 Boehringer Ingelheim Kg Neue 1,4-benzodiazepine, ihre herstellung und verwendung
US4960770A (en) 1987-05-28 1990-10-02 Yoshitomi Pharmaceutical Industries, Ltd. 2-alkyl thieno(triazolo)diazepine compounds and pharmaceutical uses thereof
JPH0676326B2 (ja) 1988-05-24 1994-09-28 吉富製薬株式会社 循環器系疾患治療薬
EP0368175A1 (de) 1988-11-06 1990-05-16 Boehringer Ingelheim Kg 3S,7S-3-(Morpholinocarbonyl)-5-(2-chlorphenyl)-7,10-dimethyl-3,4-dihydro-2H,7H-cyclopenta[4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin.
EP0387613A1 (de) 1989-03-03 1990-09-19 Boehringer Ingelheim Kg Neue Thienodiazepine
CA2020806A1 (en) 1989-07-12 1991-01-13 Karl-Heinz Weber Thienodiazepine derivatives
DE4010528A1 (de) 1990-04-02 1991-10-17 Boehringer Ingelheim Kg Praeparativ chromatographisches trennverfahren zur herstellung enantiomerenreiner hetrazepine
KR100255493B1 (ko) 1991-10-11 2000-08-01 가마쿠라 아키오 골조송증 치료제
EP0661284A1 (en) * 1992-09-18 1995-07-05 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
EP0692483A1 (en) 1993-03-30 1996-01-17 Yoshitomi Pharmaceutical Industries, Ltd. Cell adhesion inhibitor and thienotriazolodiazepine compound
US5604218A (en) 1994-04-01 1997-02-18 Microcide Pharmaceuticals, Inc. Cephalosporin antibiotics
WO1995032963A1 (en) 1994-06-01 1995-12-07 Yoshitomi Pharmaceutical Industries, Ltd. Thienylazole compound and thienotriazolodiazepine compound
WO1996020941A1 (de) 1995-01-06 1996-07-11 F. Hoffmann-La Roche Ag Hydroxymethyl-imidazodiazepine und deren ester
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
BR9610390A (pt) 1995-09-09 1999-07-06 Hoffmann La Roche O uso de uma tienotriazolodiazepina para aumentar os níveis da apoliproteína a-i
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
CA2258053A1 (en) 1996-06-12 1997-12-18 Yoshihisa Yamamoto Cytokine production inhibitors, triazepine compounds, and intermediates thereof
US5693641A (en) 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
DE69717160T2 (de) 1996-09-13 2003-05-08 Mitsubishi Pharma Corp., Osaka Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen
US6444664B1 (en) 1997-04-18 2002-09-03 Nederlandse Organisatie Voor Toegepast - Natuurweten Schappelijk Onderzoek (Tno) Method for controlling the plasma level of lipoproteins to treat alzheimeris disease
JPH11228576A (ja) 1997-12-10 1999-08-24 Japan Tobacco Inc アポトーシス抑制剤
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
FR2779652B1 (fr) 1998-06-15 2001-06-08 Sod Conseils Rech Applic Utilisation de diazepines pour la preparation de medicaments destines a traiter les etats pathologiques ou les maladies dans lesquels un des recepteurs de la somatostatine est implique
KR20000016732A (en) 1998-12-12 2000-03-25 Japan Tobacco Inc Cytokine production inhibitors, triazepine compounds, and intermediates thereof
US6312215B1 (en) 2000-02-15 2001-11-06 United Technologies Corporation Turbine engine windmilling brake
US7589167B2 (en) 2000-02-22 2009-09-15 J. David Gladstone Institutes ZA loops of bromodomains
WO2001095912A1 (fr) 2000-06-16 2001-12-20 Mitsubishi Pharma Corporation Compositions permettant de reguler la plage et/ou la vitesse de liberation du ph
WO2002002557A2 (en) 2000-06-30 2002-01-10 Neurogen Corporation 2-phenylimidazo[1,2-a]pyridine derivatives: a new class of gaba brain receptor ligands
US20060142257A1 (en) 2001-01-19 2006-06-29 Eberhard Nieschlag Male contraceptive formulation comprising norethisterone
US6979682B2 (en) 2001-02-23 2005-12-27 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Platelet-activating factor antagonist inhibition of angiogenesis and tumor growth induced by basic fibroblast
US20030216758A1 (en) 2001-12-28 2003-11-20 Angiotech Pharmaceuticals, Inc. Coated surgical patches
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
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
AU2004215359A1 (en) 2003-02-27 2004-09-10 Abbott Laboratories Heterocyclic kinase inhibitors
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
WO2005002526A2 (en) 2003-07-01 2005-01-13 President And Fellows Of Harvard College Method and compositions for treatment of viral infections
CA2538413A1 (en) 2003-09-18 2005-03-24 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
EP1528056A1 (en) 2003-10-29 2005-05-04 Academisch Ziekenhuis bij de Universiteit van Amsterdam Deoxynojirimycin analogues and their uses as glucosylceramidase inhibitors
US20060074088A1 (en) 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US7759485B2 (en) 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
CN1759834B (zh) 2004-09-17 2010-06-23 中国医学科学院医药生物技术研究所 黄连素或其与辛伐他汀联合在制备用于预防或治疗与血脂有关疾病或症状的产品中用途
JP5159305B2 (ja) * 2005-05-30 2013-03-06 田辺三菱製薬株式会社 チエノトリアゾロジアゼピン化合物及びその医薬としての用途
DK1951684T3 (en) 2005-11-01 2016-10-24 Targegen Inc BIARYLMETAPYRIMIDIN kinase inhibitors
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
TW200803842A (en) 2005-11-04 2008-01-16 Wyeth Corp Antineoplastic combinations of temsirolimus and sunitinib malate
KR20080083680A (ko) 2005-12-23 2008-09-18 스미스클라인 비참 코포레이션 오로라 키나제의 아자인돌 억제제
KR101062583B1 (ko) 2006-01-17 2011-09-06 에프. 호프만-라 로슈 아게 Ｇａｂａ 수용체에 의해 알츠하이머병의 치료에 유용한아릴-아이속사졸-4-일-이미다조[1,2-ａ]피리딘
KR20080095902A (ko) 2006-02-14 2008-10-29 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로서 유용한 디하이드로디아제핀
US20070218135A1 (en) 2006-03-14 2007-09-20 Glenmark Pharmaceuticals Limited Sustained release matrix pharmaceutical composition
DE602007008553D1 (de) 2006-05-03 2010-09-30 Novartis Ag Verwendung von organischen verbindungen
US7621117B2 (en) 2006-06-19 2009-11-24 Pratt & Whitney Canada Corp. Apparatus and method for controlling engine windmilling
MX2009004077A (es) 2006-10-19 2009-05-05 Signal Pharm Llc Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas.
US7624617B2 (en) 2006-11-21 2009-12-01 Asml Netherlands B.V. Gas analyzing system, lithographic apparatus and method of improving a sensitivity of a gas analyzing system
US8338464B2 (en) 2006-11-30 2012-12-25 Albert Einstein College Of Medicine Of Yeshiva University Small molecule inhibitors of BCL6
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Ｂｒｄ２ブロモドメイン結合剤
WO2008137081A1 (en) 2007-05-02 2008-11-13 The Trustees Of Columbia University In The City Of New York Substituted ( 5, 6 ) -dihydronaphraalenyl compounds as reversible male contraceptives
KR20080107050A (ko) 2007-06-05 2008-12-10 울산대학교 산학협력단 항-ｃｄ１３７ 단일클론 항체를 포함하는 만성이식편대숙주 질환의 예방 또는 치료용 약학적 조성물
WO2009080638A2 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
KR101600634B1 (ko) 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 항암제
EP2276747A1 (en) 2008-03-11 2011-01-26 Cellzome Limited Sulfonamides as zap-70 inhibitors
USPP20436P2 (en) 2008-04-10 2009-10-20 Driscoll Strawberry Associates, Inc. Blueberry plant named ‘DrisBlueThree’
WO2010015340A1 (en) 2008-08-06 2010-02-11 Bayer Schering Pharma Aktiengesellschaft Daa-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment
AU2009309691B2 (en) 2008-10-30 2015-04-02 Circomed Llc Thienotriazolodiazepine derivatives active on apo A
EP2379559B1 (en) 2009-01-06 2017-10-25 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
CN102341394B (zh) 2009-01-23 2015-04-15 武田药品工业株式会社 聚(adp-核糖)聚合酶(parp)抑制剂
EP2488548A1 (en) 2009-10-14 2012-08-22 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung A low density lipoprotein-related protein 1 splice variant as cancer marker
ES2652304T3 (es) 2009-11-05 2018-02-01 Glaxosmithkline Llc Compuesto de benzodiacepina novedoso
US9102677B2 (en) 2009-11-05 2015-08-11 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
DE102009046518A1 (de) 2009-11-09 2011-05-12 Robert Bosch Gmbh Speicheranordnung
WO2011101369A1 (en) 2010-02-17 2011-08-25 Boehringer Ingelheim International Gmbh Dihydropteridinones, method for production and use thereof
WO2011162845A1 (en) 2010-03-26 2011-12-29 Rolls-Royce North American Technologies, Inc. Adaptive fan system for a variable cycle turbofan engine
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
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
EP2902030B1 (en) 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
JP5844358B2 (ja) 2010-06-22 2016-01-13 グラクソスミスクライン エルエルシー ベンゾトリアゾロジアゼピン化合物を含むブロモドメイン阻害剤
WO2011163647A2 (en) 2010-06-25 2011-12-29 Shire Human Genetic Therapies, Inc. Methods and compositions for cns delivery of heparan n-sulfatase
US20120014979A1 (en) 2010-07-16 2012-01-19 Alexander Dent Use of bcl6 inhibitors for treating autoimmune diseases
TWI549955B (zh) 2010-08-04 2016-09-21 達納 法柏癌症學院有限公司 治療腫瘤形成、發炎疾病及其他病症之組成物及方法
DK2621282T3 (da) 2010-09-28 2020-05-04 Univ California Gaba-agonister i behandlingen af forstyrrelser forbundet med metabolisk syndrom og gaba-kombinationer i behandling eller profylakse af type i diabetes
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AU2012220620A1 (en) 2011-02-23 2013-10-03 Icahn School Of Medicine At Mount Sinai Inhibitors of bromodomains as modulators of gene expression
EP3323820B1 (en) 2011-02-28 2023-05-10 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2013019710A1 (en) 2011-07-29 2013-02-07 The Children's Hospital Of Philadelphia Compositions and methods for the treatment of hiv
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
FI20110279A7 (fi) 2011-08-29 2013-03-01 Outotec Oyj Menetelmä metallien talteenottamiseksi niitä sisältävästä materiaalista
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033420A1 (en) 2011-08-30 2013-03-07 Whitehead Institute For Biomedical Research Methods of downregulating translocated oncogene expression using bromodomain inhibitors
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
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
AU2013221230A1 (en) 2012-02-17 2014-10-02 Ansun Biopharma, Inc. Methods, compounds and compositions for treatment of parainfluenza virus in immunocompromised patients
US20150133434A1 (en) 2012-03-28 2015-05-14 The J. David Gladstone Institutes Compositions and Methods for Reactivating Latent Immunodeficiency Virus
WO2013192274A2 (en) 2012-06-19 2013-12-27 The Broad Institute, Inc. Diagnostic and treatment methods in subjects having or at risk of developing resistance to cancer therapy
EP2900221B1 (en) * 2012-09-28 2019-03-06 Oncoethix GmbH Pharmaceutical formulation containing thienotriazolodiazepine compounds
EP2917203B1 (en) 2012-11-02 2019-04-03 Dana-Farber Cancer Institute, Inc. Method for identifying myc inhibitors
WO2014128070A1 (de) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft Pyrrolo- und pyrazolo-triazolodiazepine als bet-proteininhibitoren zur behandlung von hyper-proliferativen erkrankungen
WO2014128111A1 (de) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft 4-substituierte pyrrolo- und pyrazolo-diazepine
JP2016510039A (ja) * 2013-02-28 2016-04-04 ワシントン・ユニバーシティＷａｓｈｉｎｇｔｏｎ Ｕｎｉｖｅｒｓｉｔｙ ブロモドメイン阻害剤によるヒトサイトメガロウイルス感染および疾患の治療方法
WO2014159392A1 (en) * 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
US20160024504A1 (en) 2013-03-15 2016-01-28 Constellation Pharmaceuticals, Inc. Treating th2-mediated diseases by inhibition of bromodomains
CN105358150A (zh) 2013-05-28 2016-02-24 达纳-法伯癌症研究所有限公司 用于心脏病的bet抑制疗法
CA2918910A1 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
EP3030242A1 (en) 2013-08-06 2016-06-15 Oncoethix GmbH Method of treating diffuse large b-cell lymphoma (dlbcl) using a bet-bromodomain inhibitor
WO2015018522A1 (en) 2013-08-06 2015-02-12 Oncoethix Sa Bet-bromodomain inhibitor shows synergism with several anti-cancer agents in pre-clinical models of diffuse large b-cell lymphoma (dlbcl)
US20160201063A1 (en) 2013-08-16 2016-07-14 Rana Therapeutics, Inc. Epigenetic regulators of frataxin
US10739333B2 (en) 2013-09-19 2020-08-11 Dana-Farber Cancer Institute, Inc. Methods of BH3 profiling
JP2016534044A (ja) 2013-10-11 2016-11-04 ジェネンテック， インコーポレイテッド 癌の免疫療法のためのｃｂｐ／ｅｐ３００ブロモドメインインヒビターの使用
EP3066101B1 (en) 2013-11-08 2020-07-29 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
WO2015081284A1 (en) 2013-11-26 2015-06-04 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
JP2017504650A (ja) 2014-01-31 2017-02-09 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジアゼパン誘導体およびその使用
JP2017504651A (ja) 2014-01-31 2017-02-09 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジアゼパン誘導体の使用
KR20160115953A (ko) 2014-01-31 2016-10-06 다나-파버 캔서 인스티튜트 인크. 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도
CN106456653A (zh) 2014-02-28 2017-02-22 腾沙治疗公司 高胰岛素血症相关病症的治疗
SG11201703414VA (en) 2014-10-27 2017-05-30 Tensha Therapeutics Inc Bromodomain inhibitors
CN107223057A (zh) 2014-12-05 2017-09-29 H·李·莫菲特癌症中心研究所公司 布罗莫结构域抑制剂作为癌症免疫治疗的补充剂
MX2017016337A (es) 2015-06-26 2018-11-22 Tensha Therapeutics Inc Tratamiento de carcinoma de linea media nut.
PE20181068A1 (es) 2015-10-02 2018-07-04 Dana Farber Cancer Inst Inc Terapia de combinacion de inhibidores de bromodominios y bloqueo de puntos de control

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