JP2013544847A5 - - Google Patents

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JP2013544847A5
JP2013544847A5 JP2013542202A JP2013542202A JP2013544847A5 JP 2013544847 A5 JP2013544847 A5 JP 2013544847A5 JP 2013542202 A JP2013542202 A JP 2013542202A JP 2013542202 A JP2013542202 A JP 2013542202A JP 2013544847 A5 JP2013544847 A5 JP 2013544847A5
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cancer
pharmaceutical composition
hydrogen
lymphoma
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JP2013542202A 2010-12-02 2011-12-02 ブロモドメイン阻害剤およびその使用 Active JP5850944B2 (ja)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US41911910P 2010-12-02 2010-12-02
US61/419,119 2010-12-02
US201161451332P 2011-03-10 2011-03-10
US61/451,322 2011-03-10
US201161482473P 2011-05-04 2011-05-04
US61/482,473 2011-05-04
US201161540725P 2011-09-29 2011-09-29
US201161540788P 2011-09-29 2011-09-29
US61/540,788 2011-09-29
US61/540,725 2011-09-29
PCT/US2011/063046 WO2012075383A2 (en) 2010-12-02 2011-12-02 Bromodomain inhibitors and uses thereof

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JP2013544847A JP2013544847A (ja) 2013-12-19
JP2013544847A5 true JP2013544847A5 (enExample) 2015-01-22
JP5850944B2 JP5850944B2 (ja) 2016-02-03

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EP (1) EP2646446B1 (enExample)
JP (1) JP5850944B2 (enExample)
KR (1) KR101871013B1 (enExample)
CN (1) CN103415525B (enExample)
AR (1) AR084070A1 (enExample)
AU (1) AU2011336417B2 (enExample)
BR (1) BR112013013167B1 (enExample)
CA (1) CA2818187C (enExample)
CY (1) CY1116578T1 (enExample)
DK (1) DK2646446T3 (enExample)
EA (1) EA022645B1 (enExample)
ES (1) ES2545117T3 (enExample)
HR (1) HRP20150858T1 (enExample)
HU (1) HUE025321T2 (enExample)
IL (1) IL226331A (enExample)
MX (1) MX2013006214A (enExample)
NZ (1) NZ611964A (enExample)
PL (1) PL2646446T3 (enExample)
PT (1) PT2646446E (enExample)
RS (1) RS54175B1 (enExample)
SG (1) SG190739A1 (enExample)
SI (1) SI2646446T1 (enExample)
TW (1) TWI572607B (enExample)
WO (1) WO2012075383A2 (enExample)
ZA (1) ZA201303776B (enExample)

Families Citing this family (149)

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Publication number Priority date Publication date Assignee Title
US8053440B2 (en) 2007-02-01 2011-11-08 Resverlogix Corporation Compounds for the prevention and treatment of cardiovascular diseases
CA2992231C (en) 2009-03-18 2022-03-29 Resverlogix Corp. Phenyl-quinazolin-4(3h)-one and phenyl-pyrido[2,3-d]pyrimidin-4(3h)-one derivatives and compositions thereof useful as anti-inflammatory agents
PL2571503T3 (pl) 2010-05-14 2015-06-30 Dana Farber Cancer Inst Inc Kompozycje i sposoby leczenia nowotworu, choroby zapalnej i innych zaburzeń
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
EP2571875A4 (en) 2010-05-14 2013-10-30 Dana Farber Cancer Inst Inc CONTRACEPTIVE COMPOSITIONS FOR MEN AND METHODS OF USE THEREOF
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
US8912221B2 (en) * 2010-12-27 2014-12-16 Hoffmann-La Roche Inc. Biaryl amide derivatives
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
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
HRP20191587T1 (hr) 2011-11-01 2019-12-13 Resverlogix Corp Formulacije s trenutnim oslobađanjem za oralnu primjenu supstituiranih kinazolinona
WO2013106643A2 (en) 2012-01-12 2013-07-18 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
WO2013185284A1 (en) * 2012-06-12 2013-12-19 Abbott Laboratories Pyridinone and pyridazinone derivatives
EA201590356A1 (ru) 2012-08-16 2015-07-30 Байер Фарма Акциенгезельшафт 2,3-бензодиазепины
ES2625959T3 (es) 2012-09-28 2017-07-21 Bayer Pharma Aktiengesellschaft 5-Aril-triazolo-azepinas inhibidoras de la proteína BET
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
US9271978B2 (en) 2012-12-21 2016-03-01 Zenith Epigenetics Corp. Heterocyclic compounds as bromodomain inhibitors
AP2015008673A0 (en) * 2013-02-19 2015-08-31 Bayer Pharma Aktiengesellchaft Bicyclo 2,3-benzodiazepines and spirocyclically substituted 2,3-benzodiazepines
US20150376196A1 (en) 2013-02-22 2015-12-31 Bayer Pharma Aktiengesellschaft 4-substituted pyrrolo- and pyrazolo-diazepines
EP2958922A1 (de) 2013-02-22 2015-12-30 Bayer Pharma Aktiengesellschaft Pyrrolo- und pyrazolo-triazolodiazepine als bet-proteininhibitoren zur behandlung von hyper-proliferativen erkrankungen
AU2014223990A1 (en) * 2013-02-28 2015-09-10 Washington University Methods of treatment of human cytomegalovirus infection and diseases with bromodomain inhibitors
WO2014164780A1 (en) * 2013-03-11 2014-10-09 Abbvie Inc. Fused tetracyclic bromodomain inhibitors
JP6401773B2 (ja) 2013-03-11 2018-10-10 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およびこれを用いる治療方法
EP2970330B1 (en) * 2013-03-12 2019-04-17 AbbVie Inc. Tetracyclic bromodomain inhibitors
US9714946B2 (en) 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
WO2014159837A1 (en) 2013-03-14 2014-10-02 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins
CA2903881C (en) 2013-03-15 2021-05-18 Incyte Corporation Tricyclic heterocycles as bet protein 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
US8975417B2 (en) * 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
ES2656471T3 (es) * 2013-05-28 2018-02-27 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona como inhibidores de BET y su uso en el tratamiento de enfermedades
JP2016520130A (ja) * 2013-05-28 2016-07-11 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 心臓疾患における新規治療戦略としてのbet阻害
CA2915622C (en) 2013-06-21 2020-08-18 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
US9855271B2 (en) 2013-07-31 2018-01-02 Zenith Epigenetics Ltd. Quinazolinones as bromodomain inhibitors
WO2015014998A1 (en) * 2013-08-01 2015-02-05 Oncoethix Sa Pharmaceutical formulation containing thienotriazolodiazepine compounds
CN105899212A (zh) * 2013-08-06 2016-08-24 翁科埃斯克斯有限公司 利用β溴结构域抑制剂治疗弥漫性大B细胞淋巴瘤(DLBCL)的方法
WO2015070020A2 (en) 2013-11-08 2015-05-14 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
WO2015081203A1 (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
CA2932040A1 (en) * 2013-12-10 2015-06-18 Abbvie Inc. Bromodomain inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
MX2016009976A (es) 2014-01-31 2016-11-15 Dana Farber Cancer Inst Inc Derivados de diazepam y sus usos.
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
KR20160115953A (ko) 2014-01-31 2016-10-06 다나-파버 캔서 인스티튜트 인크. 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도
WO2015121268A1 (de) * 2014-02-14 2015-08-20 Bayer Pharma Aktiengesellschaft 1-phenyl-3h-2,3-benzodiazepine und ihre verwendung als bromodomänen-inhibitoren
WO2015121227A1 (de) * 2014-02-14 2015-08-20 Bayer Pharma Aktiengesellschaft 6,9-disubstituierte 1 -phenyl-3h-2,3-benzodiazepine und ihre verwendung als bromodomänen- inhibitoren
JP2017071553A (ja) * 2014-02-25 2017-04-13 味の素株式会社 ヘテロ原子−メチレン−ヘテロ環構造を有する新規化合物
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
CA2940554A1 (en) 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
US20170027955A1 (en) * 2014-04-04 2017-02-02 Constellation Pharmaceuticals, Inc. Expression levels of bcl-xl, bcl2, bcl-w, and bad and cancer therapies
EP3129378B1 (en) * 2014-04-09 2019-06-26 Kainos Medicine, Inc. Bromodomain-inhibiting compounds and pharmaceutical composition comprising same for preventing or treating a cancer
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
DK3674302T3 (da) 2014-04-23 2023-04-03 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-oner og pyrazolo[3,4-c]pyridin-7(6h)-oner som inhibitorer af bet-proteiner
SG10201906842WA (en) 2014-05-29 2019-08-27 Entasis Therapeutics Ltd Fused, spirocyclic heteroaromatic compounds for the treatment of bacterial infections
CA2952526A1 (en) * 2014-06-18 2015-12-23 Bayer Pharma Aktiengesellschaft Bet-protein inhibiting 3,4-dihydropyrido[2,3-b]pyrazinones with meta-substituted aromatic amino- or ether groups
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
WO2015195863A1 (en) * 2014-06-20 2015-12-23 Constellation Pharmaceuticals, Inc. Hydrated 2-((4s)-6-(4-chlorophenyl)-1 -methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
CN106573915B (zh) * 2014-08-01 2020-12-25 纽韦卢森公司 针对布罗莫结构域有活性的化合物
CA2955077A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
WO2016022902A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
EP3194406B8 (en) 2014-09-15 2021-03-31 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
US10300073B2 (en) 2014-10-14 2019-05-28 The Regents Of The University Of California Use of CDK9 and BRD4 inhibitors to inhibit inflammation
MX376748B (es) 2014-10-27 2025-03-07 Tensha Therapeutics Inc Inhibidores del bromodominio.
TWI716367B (zh) * 2014-10-31 2021-01-21 麻省理工學院 用於常間回文重複序列叢集(crispr)之大量平行組合性基因學
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
EP3227281A4 (en) 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
HK1245248B (en) 2014-12-11 2020-05-15 恒翼生物医药(上海)股份有限公司 Substituted heterocycles as bromodomain inhibitors
HK1245247A1 (zh) 2014-12-17 2018-08-24 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
CN105985282B (zh) * 2015-01-28 2020-12-08 中国科学院广州生物医药与健康研究院 一种2-氧代-1,2-二氢苯并[cd]吲哚类化合物及其应用
EP3262045A1 (en) 2015-02-27 2018-01-03 The Regents of The University of Michigan 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors
US10111885B2 (en) 2015-03-13 2018-10-30 Resverlogix Corp. Compositions and therapeutic methods for the treatment of complement-associated diseases
KR102616762B1 (ko) 2015-03-18 2023-12-20 아비나스 오퍼레이션스, 인코포레이티드 타겟화된 단백질들의 향상된 분해를 위한 화합물들 및 방법들
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
MX376112B (es) * 2015-03-30 2025-03-07 Jubilant Biosys Ltd Derivados fusionados tricíclicos de 1-(ciclo)alquil piridin-2-ona como compuestos inhibidores de la familia bet de bromodominios, y el uso de los mismos en el tratamiento de trastornos proliferativos o cáncer.
PT3298021T (pt) 2015-05-18 2019-08-05 Tolero Pharmaceuticals Inc Pró-fármacos de alvocidib possuindo biodisponibilidade aumentada
WO2016196065A1 (en) 2015-05-29 2016-12-08 Genentech, Inc. Methods and compositions for assessing responsiveness of cancers to bet inhibitors
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP2018520124A (ja) 2015-06-26 2018-07-26 テンシャ セラピューティクス,インコーポレイテッド Nut正中線癌の治療
CA2988430A1 (en) * 2015-07-10 2017-01-19 Arvinas, Inc. Mdm2-based modulators of proteolysis and associated methods of use
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
WO2017040190A1 (en) 2015-08-28 2017-03-09 Constellation Pharmaceuticals, Inc. Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide
WO2017037567A1 (en) * 2015-09-03 2017-03-09 Pfizer Inc. Regulators of frataxin
HUE053912T2 (hu) * 2015-09-09 2021-07-28 Jubilant Biosys Ltd Triciklusos kondenzált prirdin-2-on száramazékok és azok alkalmazása BDR4 inhibitorként
KR20180049058A (ko) 2015-09-11 2018-05-10 다나-파버 캔서 인스티튜트 인크. 시아노 티에노트리아졸로디아제핀 및 그의 용도
JP2018526424A (ja) 2015-09-11 2018-09-13 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 アセトアミドチエノトリアゾロジアゼピンおよびこれらの使用
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
CN114957291A (zh) 2015-11-25 2022-08-30 达纳-法伯癌症研究所股份有限公司 二价溴结构域抑制剂及其用途
AU2017219627B2 (en) 2016-02-15 2021-08-05 The Regents Of The University Of Michigan Fused 1,4-oxazepines and related analogs as BET bromodomain inhibitors
AU2017246453A1 (en) 2016-04-06 2018-11-08 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
AU2017246452C1 (en) 2016-04-06 2021-06-03 The Regents Of The University Of Michigan MDM2 protein degraders
SG11201808729WA (en) 2016-04-12 2018-11-29 Univ Michigan Regents Bet protein degraders
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
DE102017005089A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one
CA3220957A1 (en) 2016-06-20 2017-12-28 Incyte Corporation Crystalline solid forms of a bet inhibitor
US11466028B2 (en) 2016-09-13 2022-10-11 The Regents Of The University Of Michigan Fused 1,4-oxazepines as BET protein degraders
CN110072866A (zh) 2016-09-13 2019-07-30 密执安大学评议会 作为bet蛋白降解剂的稠合的1,4-二氮杂*
WO2018075908A1 (en) * 2016-10-21 2018-04-26 University Of Miami Materials and methods for treating ophthalmic inflammation
EP3535265A4 (en) 2016-11-01 2020-07-08 Arvinas, Inc. PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE
DK3551634T3 (da) * 2016-12-12 2021-06-14 Union Therapeutics As Substituerede pyrazoloazepin-8-oner og anvendelse deraf som phosphodiesterasehæmmere
ES2875128T3 (es) * 2016-12-12 2021-11-08 Union Therapeutics As Pirazoloazepin-8-onas sustituidas y su uso como inhibidores de la fosfodiesterasa
US11028051B2 (en) 2016-12-13 2021-06-08 St. Jude Children's Research Hospital Tetrahydroquinoline-based bromodomain inhibitors
BR112019015484A2 (pt) 2017-01-31 2020-04-28 Arvinas Operations Inc ligantes de cereblon e compostos bifuncionais compreendendo os mesmos
EP3577120A1 (en) 2017-02-03 2019-12-11 The Regents of The University of Michigan Fused 1,4-diazepines as bet bromodomain inhibitors
JOP20190192A1 (ar) * 2017-03-01 2019-08-08 Glaxosmithkline Ip No 2 Ltd مشتقات بيرازول بوصفها مثبطات برومودومين
WO2018207881A1 (ja) * 2017-05-12 2018-11-15 武田薬品工業株式会社 複素環化合物
AU2018277958B8 (en) * 2017-05-31 2022-03-10 Ayumi Pharmaceutical Corporation 6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivative
JP7196160B2 (ja) 2017-09-12 2022-12-26 スミトモ ファーマ オンコロジー, インコーポレイテッド Mcl-1阻害剤アルボシジブを用いた、bcl-2阻害剤に対して非感受性である癌の治療レジメン
WO2019055444A1 (en) 2017-09-13 2019-03-21 The Regents Of The University Of Michigan DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS
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
JP2021512153A (ja) 2018-01-26 2021-05-13 イエール ユニバーシティ タンパク質分解のイミド系モジュレーターおよび使用方法
EP3819305A4 (en) 2018-07-04 2022-04-06 Mitsubishi Tanabe Pharma Corporation AMIDE COMPOUND WITH BET PROTEOLYSIS-INDUCING ACTIVITY AND MEDICAL USE THEREOF
CN112424200B (zh) 2018-07-25 2022-09-20 正大天晴药业集团股份有限公司 作为溴区结构域蛋白抑制剂的亚氨基砜类化合物、药物组合物及其医药用途
CA3120973A1 (en) 2018-11-27 2020-06-04 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2021091532A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
MX2021006205A (es) * 2018-11-27 2021-10-13 Constellation Pharmaceuticals Inc Metodos de tratamiento de trastornos mieloproliferativos.
KR20210099066A (ko) 2018-12-04 2021-08-11 스미토모 다이니폰 파마 온콜로지, 인크. 암의 치료를 위한 작용제로서 사용하기 위한 cdk9 억제제 및 그의 다형체
CN111518045A (zh) * 2019-02-02 2020-08-11 博诺康源(北京)药业科技有限公司 一种具有苯并七元环结构的化合物、其制备方法及用途
US11793802B2 (en) 2019-03-20 2023-10-24 Sumitomo Pharma Oncology, Inc. Treatment of acute myeloid leukemia (AML) with venetoclax failure
WO2020256739A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2020257644A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2021091535A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Treating myeloproliferative disorders with cpi-0610 and a jak inhibitor
CN112142711B (zh) * 2019-06-28 2022-03-29 中国科学院上海药物研究所 取代噻吩类化合物、其制备方法及其用途
CN114867727B (zh) 2019-07-17 2025-02-21 阿尔维纳斯运营股份有限公司 Tau蛋白靶向化合物及相关使用方法
EP4003342A1 (en) * 2019-07-29 2022-06-01 Constellation Pharmaceuticals, Inc. Compounds for use in treating neurological disorders
WO2021127443A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
AU2021215623A1 (en) 2020-02-06 2022-08-25 Mitsubishi Tanabe Pharma Corporation Sulfonamide or sulfinamide compound having effect of inducing BRD4 protein degradation and pharmaceutical use thereof
WO2021175432A1 (en) 2020-03-04 2021-09-10 Boehringer Ingelheim International Gmbh Method for administration of an anti cancer agent
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CA3185149A1 (en) 2020-06-23 2021-12-30 Genentech, Inc. Macrocyclic compounds and methods of use thereof
JP2023537715A (ja) 2020-08-04 2023-09-05 コンステレーション・ファーマシューティカルズ・インコーポレイテッド 血小板血症を治療するための2-((4s)-6-(4-クロロフェニル)-1-メチル-4h-ベンゾ[c]イソオキサゾロ[4,5-e]アゼピン-4-イル)アセトアミド
UY39610A (es) 2021-01-20 2022-08-31 Abbvie Inc Conjugados anticuerpo-fármaco anti-egfr
EP4337213A1 (en) 2021-05-11 2024-03-20 Constellation Pharmaceuticals, Inc. Use of pelabresib for treating anemias
KR102619332B1 (ko) * 2021-11-30 2024-01-02 주식회사 베노바이오 Bet 단백질을 저해하는 신규한 카르복스아마이드 리독스 유도체 및 이를 이용한 안과질환 예방 및 치료용 조성물
CA3249832A1 (en) 2022-01-31 2023-08-03 Constellation Pharmaceuticals, Inc. ANHYDROUS CRYSTALLINE FORMS OF 2-((4S)-6-(4-CHLOROPHENYL)-1-METHYL-4H-BENZO[C]ISOXAZOLO[4,5-E]AZEPINE-4-YL)ACETAMIDE
EP4511119A1 (en) 2022-04-19 2025-02-26 Nuevolution A/S Compounds active towards bromodomains
JP2025542349A (ja) 2022-12-20 2025-12-25 コンステレーション・ファーマシューティカルズ・インコーポレイテッド 比較的低リスクの骨髄異形成症候群を治療する方法
CN119708005A (zh) * 2023-09-27 2025-03-28 北京沐华生物科技有限责任公司 一类brd4蛋白降解剂化合物及其制备方法和应用
WO2025137396A1 (en) * 2023-12-20 2025-06-26 Constellation Pharmaceuticals, Inc. Synthesis of bromodomain inhibitors

Family Cites Families (140)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3523939A (en) 1967-07-03 1970-08-11 Hoffmann La Roche 5-(2,6-disubstituted phenyl)-1,4-benzodiazepines and methods for their preparation
CH498846A (de) 1967-08-09 1970-11-15 Hoffmann La Roche Verfahren zur Herstellung von Benzodiazepin-Derivaten
US3781289A (en) 1971-02-09 1973-12-25 Upjohn Co 7-chloro-1-methyl-5-phenyl-s-triazolo (4,3-a)quinolines
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
DE2242918A1 (de) 1971-09-15 1973-03-22 Upjohn Co Neue 4-amino-s-triazolo eckige klammer auf 4,3-a eckige klammer zu eckige klammer auf 1,4 eckige klammer zu benzodiazepine
US3903103A (en) 1971-09-15 1975-09-02 Upjohn Co 4-Amino-s-triazolo-{8 4,3-a{9 {8 1,4{9 benzodiazepine
US3886141A (en) 1971-10-07 1975-05-27 Hoffmann La Roche Preparation of 5-pyridyl benzodiazepine utilizing hexamethylenetetramine
BE795790A (fr) 1972-02-22 1973-08-22 Upjohn Co Dibenzo-triazolo-azepine
US4155904A (en) 1973-02-08 1979-05-22 Schering Corporation Process for the preparation of 1,4-benzo-diazepines and 1,4-benzodiazepinones
FR2220257A1 (en) 1973-03-09 1974-10-04 Lipha 5,6-Dihydro-(4H)-s-triazolo-(4,3-a) (1,5)benzodiazepines - as antiinflam-matory and analgesic agents without tranquillising effects
IE38931B1 (en) 1973-03-09 1978-07-05 Lipha Triazolobenzodiazepines
US3966736A (en) 1975-04-07 1976-06-29 The Upjohn Company 2,9-Dihydro-3H-pyrido[3,2-c]-s-triazolo[4,3-a][1,5]-benzodiazepin-3-ones
AT350056B (de) 1975-11-04 1979-05-10 Degussa Verfahren zur herstellung von neuen pyrido- (2,3-f)-(1,4)-diazepinen, deren optischen isomeren und salzen
DE2640599A1 (de) 1976-09-09 1978-03-16 Scherico Ltd Verfahren zur herstellung von 1,4- benzodiazepinen
CA1152066A (en) 1980-02-08 1983-08-16 Hoffmann-La Roche Limited Benzodiazepine derivatives
CA1157855A (en) 1980-07-31 1983-11-29 Albert E. Fischli Benzodiazepine derivatives
CA1163266A (en) 1980-07-31 1984-03-06 Albert E. Fischli Benzodiazepine derivatives
US4455307A (en) 1982-01-04 1984-06-19 The Upjohn Company Antihypertensive use of triazolobenzodiazepines
US5004741A (en) 1984-06-26 1991-04-02 Merck & Co., Inc. Methods of antagonizing CCK or gastrin with benzodiazepine analogs
US4820834A (en) 1984-06-26 1989-04-11 Merck & Co., Inc. Benzodiazepine analogs
US4663321A (en) 1984-06-26 1987-05-05 Merck & Co., Inc. Triazolobenzodiazepines and pharmaceutical use
ATE86256T1 (de) 1987-05-28 1993-03-15 Yoshitomi Pharmaceutical Thieno(triazolo)diazepinverbindungen, und medizinische verwendung derselben.
MC1999A1 (fr) 1987-12-18 1990-01-26 Hoffmann La Roche Composes tricycliques
US4959361A (en) 1987-12-18 1990-09-25 Hoffmann-La Roche Inc. Triazolo(4,3-A)(1,4)benzodiazepines and thieno (3,2-F)(1,2,4)triazolo(4,3-A)(1,4)diazepine compounds which have useful activity as platelet activating factor (PAF) antagonists
EP0348523A4 (en) 1987-12-22 1991-10-09 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compounds and their medicinal use
CA1324863C (en) 1988-01-30 1993-11-30 Minoru Moriwaki Thienotriazolodiazepine compounds and pharmaceutical uses thereof
CA1322367C (en) 1988-05-17 1993-09-21 Yoshitomi Pharmaceutical Industries Ltd. Thienotriazolodiazepine compounds and pharmaceutical uses thereof
US5382579A (en) 1988-10-31 1995-01-17 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
FI95708C (fi) 1988-10-31 1996-03-11 Eisai Co Ltd Analogiamenetelmä 1,4-diatsepiinijohdannaisen ja sen farmaseuttisesti sopivan suolan valmistamiseksi
US5221671A (en) 1988-10-31 1993-06-22 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
DE3936828A1 (de) 1988-11-06 1990-05-10 Boehringer Ingelheim Kg Neue hetrazepine
DE4006471A1 (de) 1989-03-03 1990-09-06 Boehringer Ingelheim Kg Neue thienodiazepine
CA2020806A1 (en) 1989-07-12 1991-01-13 Karl-Heinz Weber Thienodiazepine derivatives
JPH0374328A (ja) 1989-08-04 1991-03-28 Warner Lambert Co 薬学的活性を有する中枢コレシストキニン拮抗剤
US5175159A (en) 1989-10-05 1992-12-29 Merck & Co., Inc. 3-substituted-1,4-benzodiazepines as oxytocin antagonists
IL96613A0 (en) 1989-12-18 1991-09-16 Merck & Co Inc Pharmaceutical compositions containing benzodiazepine analogs
CA2032427A1 (en) 1989-12-18 1991-06-19 Mark G. Bock Benzodiazepines analogs
WO1994006801A1 (fr) 1990-05-23 1994-03-31 Yoshitomi Pharmaceutical Industries, Ltd. Compose de thienodiazepine et son utilisation comme medicament
JP2959591B2 (ja) 1990-05-23 1999-10-06 吉富製薬株式会社 チエノトリアゾロジアゼピン化合物
DE4027470A1 (de) 1990-08-30 1992-03-05 Boehringer Ingelheim Kg Neue hetrazepinoide amide
JP2959598B2 (ja) 1990-10-12 1999-10-06 吉富製薬株式会社 光学活性なチエノトリアゾロジアゼピン化合物
US5206234A (en) 1990-10-22 1993-04-27 Merck & Co., Inc. Benzolactam analogs as antagonists of cck
CA2056809A1 (en) 1990-12-07 1992-06-08 Mark G. Bock Benzodiazepine analogs
DE4101146A1 (de) 1991-01-16 1992-07-23 Boehringer Ingelheim Kg Neue in 6-position substituierte diazepine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DE4107521A1 (de) 1991-03-08 1992-09-10 Boehringer Ingelheim Kg Neue acylaminosubstituierte hetrazepine
US5683998A (en) 1991-04-23 1997-11-04 Toray Industries, Inc. Tricyclic triazolo derivatives, processes for producing the same and the uses of the same
US5185331A (en) 1991-05-14 1993-02-09 Merck & Co., Inc. Triazolobenzodiazepines
CA2071092A1 (en) 1991-06-14 1992-12-15 Roger M. Freidinger 1,4-benzodiazepines with 5-membered heterocyclic rings
GB9117852D0 (en) 1991-08-19 1991-10-09 Merck Sharp & Dohme Therapeutic agents
US5153191A (en) 1991-08-20 1992-10-06 Warner-Lambert Company Cholecystokinin antagonists useful for treating depression
DE4128581A1 (de) 1991-08-28 1993-03-04 Boehringer Ingelheim Kg Verwendung von paf-antagonisten hetrazepinoider struktur zur behandlung der allergischen rhinitis
CA2097285C (en) 1991-09-30 2000-03-14 Yoichi Naka Thienodiazepine compounds and their use
US5593988A (en) 1991-10-11 1997-01-14 Yoshitomi Pharmaceutical Industries, Ltd. Therapeutic agent for osteoporosis and diazepine compound
ATE191345T1 (de) 1991-12-11 2000-04-15 Yoshitomi Pharmaceutical Arzneimittel zur behandlung von autoimmunerkrankungen
EP0617621A4 (en) 1991-12-20 1995-04-05 Merck Sharp & Dohme CENTRAL CHOLECYSTOKININE ANTAGONISTS WITH PHARMACEUTICAL EFFECTIVENESS.
DE4200610A1 (de) 1992-01-13 1993-07-15 Boehringer Ingelheim Kg Verwendung von paf-antagonisten zur behandlung der dysmenorrhea
EP0636123A1 (en) 1992-03-24 1995-02-01 MERCK SHARP & DOHME LTD. 3-ureido substituted benzodiazepin-2-ones having cholecystokinin and/or gastrin antagonistic activity and their use in therapy
DE4219659A1 (de) 1992-06-16 1993-12-23 Boehringer Ingelheim Kg Die Verwendung von PAF-Antagonisten in Kombination mit Anticholinergika
EP0661284A1 (en) 1992-09-18 1995-07-05 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
JP3223290B2 (ja) 1992-11-10 2001-10-29 日本電信電話株式会社 マイクロ回転体およびその製造方法
US5302590A (en) 1992-12-18 1994-04-12 Hoffmann-La Roche Inc. Compounds useful as dual antagonists of platelet activating factor and leukotriene D4
WO1994022872A1 (fr) 1993-03-30 1994-10-13 Yoshitomi Pharmaceutical Industries, Ltd. Inhibiteur d'adhesion cellulaire et compose a base de thienotriazolodiazepine
EP0763537A3 (en) 1993-05-14 1997-10-22 Genentech Inc Non-peptides farnesyl transfer inhibitors
US5869483A (en) 1993-07-29 1999-02-09 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US5516774A (en) 1993-07-29 1996-05-14 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5733905A (en) 1993-07-29 1998-03-31 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5760031A (en) 1993-07-29 1998-06-02 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
WO1995014694A1 (en) 1993-11-22 1995-06-01 Merck & Co., Inc. Benzodiazepines
ES2156933T3 (es) 1993-12-28 2001-08-01 Meiji Seika Co Derivados triciclicos de benzazepina y benzotiazepina.
US5739129A (en) 1994-04-14 1998-04-14 Glaxo Wellcome Inc. CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
JPH09511998A (ja) 1994-04-15 1997-12-02 グラクソ、ウェルカム、インコーポレーテッド 1,4 − ベンゾジアゼピン化合物を用いたコレシストキニンアゴニスト活性の誘導方法
EP0906907B1 (en) 1995-09-21 2002-03-06 Institute of Medicinal Molecular Design, Inc. Compounds potentiating retinoid
IL127516A0 (en) 1996-06-12 1999-10-28 Japan Tobacco Inc A cytokine production inhibitor
AU716490B2 (en) 1996-09-13 2000-02-24 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compounds and pharmaceutical use thereof
ZA9711537B (en) 1996-12-23 1998-06-25 Athena Neurosciences Inc Eli L Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ß-amyloid peptide release and/or its synthesis by use of such compounds.
WO1998058930A1 (en) 1997-06-25 1998-12-30 Nikken Chemicals Co., Ltd. Triazolo-1,4-diazepine compounds and medicinal composition containing the same
JP4204657B2 (ja) 1997-12-05 2009-01-07 有限会社ケムフィズ 糖尿病の予防・治療剤
JPH11228576A (ja) 1997-12-10 1999-08-24 Japan Tobacco Inc アポトーシス抑制剤
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
PE20000944A1 (es) 1998-07-31 2000-09-20 Lilly Co Eli Derivados de sulfonamida
BR9913226A (pt) 1998-09-01 2001-05-22 Innogenetics Nv Benzodiazepinas e derivados de benzotiazepinas e peptìdios de hbsag ligados a anexinas, suas composições e uso
US6277844B1 (en) * 1998-09-14 2001-08-21 Sydney Spector Compound for selective treatment of malignant cells by inhibiting cell cycle progression, decreasing Bcl2, and increasing apoptosis
WO2000054778A1 (fr) 1999-03-12 2000-09-21 Welfide Corporation Agents preventifs ou therapeutiques des dermatoses inflammatoires
FR2791980B1 (fr) 1999-04-09 2001-07-06 Sod Conseils Rech Applic Pyrido-thieno-diazepines, leur procede de preparation, et les compositions pharmaceutiques les contenant
GB9911152D0 (en) 1999-05-14 1999-07-14 Glaxo Group Ltd Short-acting benzodiazepines
US7160880B1 (en) 1999-05-14 2007-01-09 Cenes Limited Short-acting benzodiazepines
JP2003518494A (ja) 1999-12-29 2003-06-10 グラクソ グループ リミテッド アネキシンおよび軟骨ホメオスタシスのモジュレーターに関係する方法と組成物
CA2412776C (en) 2000-06-16 2011-03-15 Mitsubishi Pharma Corporation Compositions controlling release ph range and/or speed
NZ529582A (en) 2001-06-07 2006-10-27 Neuro3D Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses thereof
EP1481977A4 (en) 2002-03-01 2006-02-01 Astellas Pharma Inc NITROGENIC HETEROCYCLIC COMPOUND
ES2315546T3 (es) 2002-10-30 2009-04-01 Via Pharmaceuticals, Inc. Inhibidores delas fosfodiesterasas de los nucleotidos ciclicos, que presentan una estructura de benzodiazepina, y su uso en terapia.
DE10251927A1 (de) 2002-11-08 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
US7482337B2 (en) 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
AU2003297161B8 (en) 2002-12-18 2011-03-31 Vertex Pharmaceuticals Incorporated Triazolopyridazines as protein kinases inhibitors
US7119088B2 (en) 2003-02-19 2006-10-10 Pfizer Inc. Triazole compounds useful in therapy
JPWO2005002590A1 (ja) 2003-07-01 2006-08-10 アステラス製薬株式会社 骨量増加誘導剤
WO2005099759A1 (ja) 2004-04-16 2005-10-27 Institute Of Medicinal Molecular Design. Inc. 動脈硬化症の予防及び/又は治療のための医薬
JP4494414B2 (ja) 2004-10-05 2010-06-30 パイオニア株式会社 オーディオラック
EP1887008B1 (en) 2005-05-30 2021-04-21 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and a medicinal use thereof
CA2615463A1 (en) 2005-07-29 2007-02-08 Merck & Co., Inc. Heterocyclic benzodiazepine cgrp receptor antagonists
JP2009513644A (ja) 2005-10-26 2009-04-02 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 治療組成物および方法
US20070105844A1 (en) 2005-10-26 2007-05-10 Regents Of The University Of Michigan Therapeutic compositions and methods
DE102005061840A1 (de) 2005-12-23 2007-06-28 Merck Patent Gmbh Triazolderivate
JPWO2008023847A1 (ja) 2006-08-25 2010-01-14 日本ケミファ株式会社 P2x4受容体拮抗剤
WO2008109856A2 (en) 2007-03-07 2008-09-12 Xenon Pharmaceuticals Inc. Methods of using diazepinone compounds in treating sodium channel-mediated diseases or conditions
US20090111780A1 (en) 2007-10-31 2009-04-30 Everett Laboratories, Inc. Compositions and methods for treatment of ear canal infection and inflammation
ITFI20070288A1 (it) 2007-12-21 2009-06-22 A I L Firenze Sezione Autonoma Inibitori delle deacetilasi istoniche
CA2710740C (en) * 2007-12-28 2016-07-19 Shinji Miyoshi Thienotriazolodiazepine compound as antitumor agent
EP2349257B1 (en) 2008-06-17 2013-11-27 Universidade Federal de Minas Gerais-UFMG Use of paf receptor for treating infections caused by flaviviridae
KR20110033239A (ko) 2008-06-23 2011-03-30 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제
KR101633742B1 (ko) 2008-10-30 2016-06-27 써코메드 엘엘씨 아포 a에 활성인 티에노트리아졸로디아제핀 유도체
US8604023B2 (en) 2009-04-17 2013-12-10 The Regents Of The University Of Michigan 1,4-benzodiazepinone compounds and their use in treating cancer
CN102482258B (zh) 2009-05-07 2014-06-25 株式会社棱镜制药 α-螺旋模拟物和与其相关的方法
WO2011037128A1 (ja) 2009-09-28 2011-03-31 日本曹達株式会社 含窒素ヘテロ環化合物およびその塩ならびに農園芸用殺菌剤
GB0919431D0 (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
BR112012010705A2 (pt) 2009-11-05 2016-03-29 Glaxosmithkline Llc composto, composição farmacêutica, produto farmacêutico combinado, uso de um composto, e, métodos para tratar uma doença ou condição, e para inibir um bromodomínio
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ES2539964T3 (es) 2009-11-05 2015-07-07 Glaxosmithkline Llc Procedimiento novedoso
ME02360B (me) 2009-11-05 2016-06-20 Glaxosmithkline Llc Inhibitor bromodomena benzodiazepina
CA2785410A1 (en) 2009-12-23 2011-06-30 Carlos F. Barbas, Iii Tyrosine bioconjugation through aqueous ene-like reactions
WO2011123678A2 (en) 2010-03-31 2011-10-06 Arqule, Inc. Substituted benzo-pyrido-triazolo-diazepine compounds
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
EP2571875A4 (en) 2010-05-14 2013-10-30 Dana Farber Cancer Inst Inc CONTRACEPTIVE COMPOSITIONS FOR MEN AND METHODS OF USE THEREOF
PL2571503T3 (pl) 2010-05-14 2015-06-30 Dana Farber Cancer Inst Inc Kompozycje i sposoby leczenia nowotworu, choroby zapalnej i innych zaburzeń
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
US9085582B2 (en) 2010-06-22 2015-07-21 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
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
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
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
TWI602820B (zh) * 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof

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