HK1212627A1 - 用於治療瘤形成的噻吩並***並二氮雜䓬化合物 - Google Patents

用於治療瘤形成的噻吩並***並二氮雜䓬化合物

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Publication number
HK1212627A1
HK1212627A1 HK16100664.7A HK16100664A HK1212627A1 HK 1212627 A1 HK1212627 A1 HK 1212627A1 HK 16100664 A HK16100664 A HK 16100664A HK 1212627 A1 HK1212627 A1 HK 1212627A1
Authority
HK
Hong Kong
Prior art keywords
treating neoplasia
thienotriazolodiazepine compounds
thienotriazolodiazepine
compounds
neoplasia
Prior art date
Application number
HK16100664.7A
Other languages
English (en)
Inventor
Elliott James Bradner
Jun Qi
Original Assignee
Dana Farber Cancer Inst 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 Dana Farber Cancer Inst Inc filed Critical Dana Farber Cancer Inst Inc
Publication of HK1212627A1 publication Critical patent/HK1212627A1/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic 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
    • C07D495/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pyridine Compounds (AREA)
HK16100664.7A 2010-05-14 2016-01-21 用於治療瘤形成的噻吩並***並二氮雜䓬化合物 HK1212627A1 (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US33499110P 2010-05-14 2010-05-14
US37074510P 2010-08-04 2010-08-04
US37586310P 2010-08-22 2010-08-22
US201161467376P 2011-03-24 2011-03-24

Publications (1)

Publication Number Publication Date
HK1212627A1 true HK1212627A1 (zh) 2016-06-17

Family

ID=44915031

Family Applications (2)

Application Number Title Priority Date Filing Date
HK13110647.1A HK1183620A1 (zh) 2010-05-14 2013-09-16 用於治療瘤形成、炎性疾病和其他疾病的組合物及其用途
HK16100664.7A HK1212627A1 (zh) 2010-05-14 2016-01-21 用於治療瘤形成的噻吩並***並二氮雜䓬化合物

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HK13110647.1A HK1183620A1 (zh) 2010-05-14 2013-09-16 用於治療瘤形成、炎性疾病和其他疾病的組合物及其用途

Country Status (17)

Country Link
US (5) US8981083B2 (zh)
EP (2) EP2902030B1 (zh)
KR (1) KR101857599B1 (zh)
CN (2) CN103037865B (zh)
AU (1) AU2011252808B2 (zh)
BR (2) BR112012029005A2 (zh)
CA (1) CA2799420C (zh)
DK (1) DK2571503T3 (zh)
ES (2) ES2606958T3 (zh)
HK (2) HK1183620A1 (zh)
HU (1) HUE031073T2 (zh)
IL (3) IL222993A (zh)
MX (2) MX362384B (zh)
PL (2) PL2571503T3 (zh)
PT (1) PT2571503E (zh)
SI (1) SI2902030T1 (zh)
WO (1) WO2011143669A2 (zh)

Families Citing this family (173)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
US9301962B2 (en) 2010-05-14 2016-04-05 Baylor College Of Medicine Male contraceptive compositions and methods of use
HUE031073T2 (en) * 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
EP2569434B1 (en) 2010-05-14 2019-09-04 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia and related disorders
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
US9422292B2 (en) 2011-05-04 2016-08-23 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
WO2013074986A1 (en) 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
EP2802608A4 (en) 2012-01-12 2015-08-05 Univ Yale COMPOUNDS AND METHODS FOR ENHANCED DEGRADATION OF TARGET PROTEINS AND OTHER POLYPEPTIDES BY E3 UBIQUITIN LIGASE
AU2013225592B2 (en) * 2012-02-27 2017-11-09 British Columbia Cancer Agency Branch Reprogramming effector protein interactions to correct epigenetic defects in cancer
EP2864336B1 (en) 2012-06-06 2016-11-23 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
JP2015522259A (ja) 2012-06-14 2015-08-06 ホワイトヘッド・インスティテュート・フォー・バイオメディカル・リサーチ 化学実体とそれらの標的分子の間の相互作用を評価するゲノム全域法
US9763956B2 (en) 2012-06-19 2017-09-19 The Broad Institute, Inc. Diagnostic and treatment methods in subjects having or at risk of developing resistance to cancer therapy
CN105050605A (zh) * 2012-06-25 2015-11-11 翁科埃蒂克斯股份公司 使用噻吩并***并二氮杂*化合物治疗淋巴瘤的方法
WO2014015175A1 (en) * 2012-07-18 2014-01-23 Massachusetts Institute Of Technology Compositions and methods for modulating brd4 bioactivity
CA2881996A1 (en) 2012-08-16 2014-02-20 Bayer Pharma Aktiengesellschaft 2,3-benzodiazepines
ES2625959T3 (es) 2012-09-28 2017-07-21 Bayer Pharma Aktiengesellschaft 5-Aril-triazolo-azepinas inhibidoras de la proteína BET
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
CA3177929A1 (en) 2012-12-21 2014-06-26 Astellas Institute For Regenerative Medicine Methods for production of platelets from pluripotent stem cells and compositions thereof
KR20150096794A (ko) 2012-12-21 2015-08-25 제니쓰 에피제네틱스 코포레이션 브로모도메인 저해제로서의 신규한 헤테로사이클릭 화합물
WO2014128067A1 (de) 2013-02-19 2014-08-28 Bayer Pharma Aktiengesellschaft Bicyclo- und spirocyclisch substituierte 2,3-benzodiazepine
CN105164135A (zh) 2013-02-22 2015-12-16 拜耳医药股份有限公司 4-取代的吡咯并二氮杂卓和吡唑并二氮杂卓
US20160009725A1 (en) * 2013-02-22 2016-01-14 Bayer Pharma Aktiengesellschaft Pyrrolo- and pyrazolo-triazolodiazepines as bet-protein inhibitors for treating hyperproliferative diseases
CA2902225A1 (en) * 2013-02-28 2014-09-04 Washington University Methods of treatment of human cytomegalovirus infection and diseases with bromodomain inhibitors
AU2014249192B2 (en) 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
US9714946B2 (en) * 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
EP2970282B1 (en) 2013-03-15 2019-08-21 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
CA2901083A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
CA2913741A1 (en) * 2013-05-28 2014-12-04 The Brigham And Women's Hospital, Inc. Bet inhibition therapy for heart disease
US9636328B2 (en) 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
CN109939113B (zh) 2013-06-21 2022-02-15 恒翼生物医药科技(上海)有限公司 双环溴结构域抑制剂
CN105518007A (zh) * 2013-06-28 2016-04-20 艾伯维公司 布罗莫结构域抑制剂
AR096758A1 (es) * 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
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
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
KR20160034379A (ko) 2013-07-25 2016-03-29 다나-파버 캔서 인스티튜트 인크. 전사 인자의 억제제 및 그의 용도
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
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)
WO2015018523A1 (en) * 2013-08-06 2015-02-12 Oncoethix Sa A novel bet-brd inhibitor for treatment of solid tumors
KR20160037201A (ko) * 2013-08-06 2016-04-05 온코에틱스 게엠베하 Bet-브로모도메인 억제제를 사용한 미만성 거대 b-세포 림프종 (dlbcl)의 치료 방법
US9676790B2 (en) 2013-08-30 2017-06-13 Concert Pharmaceuticals, Inc. Substituted thienotriazolodiazapines
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
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
WO2015081189A1 (en) 2013-11-26 2015-06-04 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
JP2016538310A (ja) 2013-11-27 2016-12-08 オンコエシックス ゲーエムベーハー チエノトリアゾロジアゼピン化合物を含む医薬製剤を用いる白血病の治療方法
US9820992B2 (en) 2013-11-27 2017-11-21 Merck Sharp & Dohme Corp. Method of treating non-small-cell lung cancer using pharmaceutical formulation containing thienotriazolodiazepine compounds
WO2015078931A1 (en) * 2013-11-27 2015-06-04 Oncoethix Sa Method of treating neuroblastomas using thienotriazolodiazepine compounds
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
US20170007595A1 (en) * 2014-01-24 2017-01-12 The Brigham And Women's Hospital, Inc. Nsd3 inhibitors for treatment of cancers
CA2936865A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
WO2015117083A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
EP3099693A4 (en) 2014-01-31 2017-08-16 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
CN106459056A (zh) 2014-02-10 2017-02-22 康塞特医药品公司 经取代的***苯二氮卓
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
AU2015222805B2 (en) * 2014-02-28 2020-05-21 Tensha Therapeutics, Inc. Treatment of conditions associated with hyperinsulinaemia
WO2015144636A1 (en) 2014-03-24 2015-10-01 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of t-cell acute lymphoblastic leukemias
US9884874B2 (en) 2014-04-09 2018-02-06 Kainos Medicine, Inc. Bromodomain-inhibiting compounds and pharmaceutical composition comprising same for preventing or treating a cancer
US20160058872A1 (en) * 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
KR20210132233A (ko) * 2014-04-14 2021-11-03 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
MY180775A (en) 2014-04-23 2020-12-09 Incyte Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
KR20160145833A (ko) * 2014-05-02 2016-12-20 온코에틱스 게엠베하 티에노트리아졸로디아제핀 화합물을 사용한 급성 골수성 백혈병 및/또는 급성 림프아구성 백혈병의 치료 방법
US20170095484A1 (en) * 2014-05-02 2017-04-06 Oncoethix Gmbh Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or alk+non-small cell lung cancer using thienotriazolodiazepine compounds
BR112016026046A8 (pt) 2014-05-08 2021-07-20 Oncoethix Gmbh uso de compostos de tienotriazolodiazepina
BR112016029012A2 (pt) 2014-06-13 2017-08-22 Oncoethix Gmbh método de tratamento de câncer de pulmão de células não pequenas e/ou câncer de pulmão de células pequenas usando compostos de tienotriazolodiazepina
EP3157928B1 (en) 2014-06-20 2019-02-13 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
CA2955077A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
CN106715437A (zh) 2014-08-08 2017-05-24 达纳-法伯癌症研究所股份有限公司 二氮杂环庚烷衍生物及其用途
EP3185871A1 (en) * 2014-08-28 2017-07-05 Oncoethix GmbH Methods of treating acute myeloid leukemia or acute lymphoid leukemia using pharmaceutical compositions containing thienotriazolodiazepine compounds
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
BR112017008714A2 (pt) 2014-10-27 2017-12-19 Tensha Therapeutics Inc inibidores de bromodomínio
WO2016073956A1 (en) 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
SG11201703544QA (en) * 2014-11-07 2017-06-29 Univ Osaka Differentiation-induced cell population from which undifferentiated cells have been removed, use of same, and method for producing same
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
CA2969417A1 (en) * 2014-12-05 2016-06-09 H. Lee Moffitt Cancer Center And Research Institute, Inc. Bromodomain inhibitor as adjuvant in cancer immunotherapy
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
EP3233846A4 (en) 2014-12-17 2018-07-18 Zenith Epigenetics Ltd. Inhibitors of bromodomains
JP6815318B2 (ja) 2014-12-23 2021-01-20 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 二官能性分子によって標的化タンパク質分解を誘導する方法
CA2972239A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CN104610255B (zh) * 2015-01-28 2017-01-18 常州工程职业技术学院 含有异噁唑骨架的[1,2‑a]咪唑并吡啶类衍生物的合成方法
WO2016138332A1 (en) 2015-02-27 2016-09-01 The Regents Of The University Of Michigan 9h-pyrimido [4,5-b] indoles as bet bromodomain inhibitors
EP3270917A4 (en) 2015-03-18 2018-08-08 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
EP3273966B1 (en) 2015-03-27 2023-05-03 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2016176335A1 (en) 2015-04-27 2016-11-03 Concert Pharmaceuticals, Inc. Deuterated otx-015
US20180346988A1 (en) * 2015-05-04 2018-12-06 The Brigham And Women's Hospital, Inc. Znf532 for diagnosis and treatment of cancer
WO2016196065A1 (en) 2015-05-29 2016-12-08 Genentech, Inc. Methods and compositions for assessing responsiveness of cancers to bet inhibitors
JP6873433B2 (ja) * 2015-06-04 2021-05-19 アルヴィナス・オペレーションズ・インコーポレイテッド タンパク質分解のイミド系修飾因子および関連の使用方法
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
MA42249A (fr) 2015-06-26 2018-05-02 Tensha Therapeutics Inc Traitement de carcinome de la ligne médiane nut
WO2017007612A1 (en) 2015-07-07 2017-01-12 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
KR20180035828A (ko) * 2015-07-10 2018-04-06 아비나스 인코포레이티드 단백질 분해의 mdm2계 조절인자 및 관련된 이용 방법
WO2017027571A1 (en) 2015-08-10 2017-02-16 Dana-Farber Cancer Institute, Inc. Mechanism of resistance to bet bromodomain inhibitors
WO2017030814A1 (en) 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
WO2017037567A1 (en) * 2015-09-03 2017-03-09 Pfizer Inc. Regulators of frataxin
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
PE20181086A1 (es) 2015-09-11 2018-07-05 Dana Farber Cancer Inst Inc Acetamida tienotrizolodiazepinas y usos de las mismas
WO2017044849A1 (en) 2015-09-11 2017-03-16 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof
JP2018530554A (ja) * 2015-10-02 2018-10-18 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 ブロモドメイン阻害薬及びチェックポイント阻害薬による併用療法
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
SG10201913450PA (en) 2015-11-25 2020-03-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
CN109071562B (zh) * 2016-02-15 2022-03-22 密执安大学评议会 作为bet溴结构域抑制剂的稠合1,4-氧氮杂䓬和相关类似物
CA3019342A1 (en) 2016-03-30 2017-10-05 Wisconsin Alumni Research Foundation Methods and compositions for modulating frataxin expression
SG11201808728QA (en) 2016-04-06 2018-11-29 Univ Michigan Regents Mdm2 protein degraders
US10759808B2 (en) 2016-04-06 2020-09-01 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
US10633386B2 (en) 2016-04-12 2020-04-28 The Regents Of The University Of Michigan BET protein degraders
RU2741808C2 (ru) 2016-04-15 2021-01-28 Эббви Инк. Ингибиторы бромодомена
US10633371B2 (en) 2016-04-22 2020-04-28 Dana-Farber Cancer Institute, Inc. EZH2 inhibitors and uses thereof
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
EP3454856A4 (en) 2016-05-10 2019-12-25 C4 Therapeutics, Inc. HETEROCYCLIC DEGRONIMERS FOR TARGET PROTEIN REDUCTION
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
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
EP4234554A3 (en) 2016-06-20 2023-12-27 Incyte Corporation Crystalline solid forms of a bet inhibitor
EP3478824A1 (en) 2016-07-01 2019-05-08 Centre National de la Recherche Scientifique - CNRS Amplifying beta cell differentiation with small molecules bet (bromodomain and extraterminal family of bromodomain-containing proteins) inhibitors
US11466028B2 (en) 2016-09-13 2022-10-11 The Regents Of The University Of Michigan Fused 1,4-oxazepines as BET protein degraders
WO2018052949A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet protein degraders
WO2018064589A1 (en) 2016-09-29 2018-04-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation using a mutant e3 ubiquitin ligase
MX2019006956A (es) * 2016-12-16 2019-08-01 Hoffmann La Roche Proceso para la fabricacion de derivados de diazepina.
WO2018144789A1 (en) 2017-02-03 2018-08-09 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet bromodomain inhibitors
WO2018183679A1 (en) 2017-03-29 2018-10-04 Wisconsin Alumni Research Foundation Methods and compositions for modulating gene expression
WO2018237026A1 (en) 2017-06-20 2018-12-27 C4 Therapeutics, Inc. N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS
WO2019014514A1 (en) 2017-07-14 2019-01-17 University Of Massachusetts HETEROCYCLIC COMPOUNDS AND USES THEREOF
EP3658188A1 (en) 2017-07-26 2020-06-03 H. Hoffnabb-La Roche Ag Combination therapy with a bet inhibitor and a bcl-2 inhibitor
CN110869391A (zh) 2017-07-26 2020-03-06 豪夫迈·罗氏有限公司 用BET抑制剂,Bcl-2抑制剂和抗CD20抗体的组合疗法
CN111278816B (zh) 2017-09-04 2024-03-15 C4医药公司 二氢喹啉酮
CN118206529A (zh) 2017-09-04 2024-06-18 C4医药公司 二氢苯并咪唑酮
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
WO2019055444A1 (en) 2017-09-13 2019-03-21 The Regents Of The University Of Michigan DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS
CN109503618A (zh) * 2017-09-14 2019-03-22 成都海创药业有限公司 一种brd4抑制剂
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
CN108129484B (zh) * 2017-12-19 2021-04-27 郭守东 杂芳环衍生物
CN108084193A (zh) * 2017-12-19 2018-05-29 郭守东 一种brd4蛋白抑制剂
WO2019148055A1 (en) 2018-01-26 2019-08-01 Yale University Imide-based modulators of proteolysis and methods of use
JP2021519337A (ja) 2018-03-26 2021-08-10 シー4 セラピューティクス, インコーポレイテッド Ikarosの分解のためのセレブロン結合剤
EP3781156A4 (en) 2018-04-16 2022-05-18 C4 Therapeutics, Inc. SPIROCYCLIC COMPOUNDS
CN111989092A (zh) 2018-04-18 2020-11-24 豪夫迈·罗氏有限公司 Bet抑制剂和蛋白酶体抑制剂的联合治疗
KR20210020889A (ko) 2018-06-13 2021-02-24 디블라이 아게 응축된 트리아제핀 유도체의 제조 및 이의 bet 억제제로서 용도
CN108743591A (zh) * 2018-07-17 2018-11-06 苏州大学 用于治疗癌症的药物组合物及其应用
CA3106733A1 (en) 2018-07-25 2020-01-30 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Sulfoximine compound as bromodomain protein inhibitor and pharmaceutical composition and medical use thereof
CN113164495A (zh) * 2018-10-09 2021-07-23 加利福尼亚大学董事会 E3连接酶的共价靶向
EP3870235A1 (en) 2018-10-24 2021-09-01 F. Hoffmann-La Roche AG Conjugated chemical inducers of degradation and methods of use
WO2020132561A1 (en) 2018-12-20 2020-06-25 C4 Therapeutics, Inc. Targeted protein degradation
WO2020169698A1 (en) 2019-02-21 2020-08-27 F. Hoffmann-La Roche Ag Sensitization of cancer cells to tnf by bet inhibition
KR102201902B1 (ko) * 2019-04-22 2021-01-11 건국대학교 글로컬산학협력단 암을 진단하기 위한 마커인 sox9 및 brd4, 및 이들을 이용한 암 예측 방법
WO2020234445A1 (en) 2019-05-23 2020-11-26 F. Hoffmann-La Roche Ag Combination therapy with a bet inhibitor and a bcl-2 inhibitor
WO2021048852A1 (en) 2019-09-11 2021-03-18 Yeda Research And Development Co. Ltd. Methods of treating breast cancer
US20230145782A1 (en) * 2019-11-01 2023-05-11 The Regents Of The University Of California p53 MODULATORS AND USES THEREOF
PE20221582A1 (es) 2019-12-19 2022-10-06 Arvinas Operations Inc Compuestos y metodos para la degradacion dirigida de receptor de androgenos
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
CN111529533B (zh) * 2020-06-05 2021-06-11 南华大学附属第一医院 溴结构域蛋白4抑制剂jq1或其衍生物在制备治疗脓毒症肠屏障损伤药物中的应用
AU2021297799A1 (en) 2020-06-23 2022-12-22 Genentech, Inc. Macrocyclic compounds and methods of use thereof
US20230310452A1 (en) * 2020-08-26 2023-10-05 Mdi Biological Laboratory Bromodomain and extra terminal domain (bet) inhibitor compositions and methods thereof for use as anti-aging agents
WO2022236173A1 (en) * 2021-05-07 2022-11-10 Mayo Foundation For Medical Education And Research Treating liver disease
WO2023041744A1 (en) 2021-09-17 2023-03-23 Institut Curie Bet inhibitors for treating pab1 deficient cancer
WO2023205251A1 (en) 2022-04-19 2023-10-26 Nuevolution A/S Compounds active towards bromodomains

Family Cites Families (132)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ATE86256T1 (de) 1987-05-28 1993-03-15 Yoshitomi Pharmaceutical Thieno(triazolo)diazepinverbindungen, und medizinische verwendung derselben.
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
US5223409A (en) 1988-09-02 1993-06-29 Protein Engineering Corp. Directed evolution of novel binding proteins
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
YU133090A (sh) 1989-07-12 1993-10-20 Boehringer Ingelheim Kg. Novi heteroazepini s paf-antaganostičnim učinkom in postopek za njihovo pripravo
JPH0396299A (ja) 1989-09-08 1991-04-22 Asahi Tec Corp ブラウン管等の電磁遮へい装置
DE4010528A1 (de) 1990-04-02 1991-10-17 Boehringer Ingelheim Kg Praeparativ chromatographisches trennverfahren zur herstellung enantiomerenreiner hetrazepine
CA2120939A1 (en) 1991-10-11 1993-04-15 Tetsuya Tahara Therapeutic agent for osteoporosis and diazepine compound
EP0661284A1 (en) 1992-09-18 1995-07-05 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
WO1994022872A1 (en) 1993-03-30 1994-10-13 Yoshitomi Pharmaceutical Industries, Ltd. Cell adhesion inhibitor and thienotriazolodiazepine compound
WO1995032963A1 (fr) 1994-06-01 1995-12-07 Yoshitomi Pharmaceutical Industries, Ltd. Compose de thienylazole et compose de thienotriazolodiazepine
ES2159714T3 (es) 1995-01-06 2001-10-16 Hoffmann La Roche Hidroximetil-imidazodiazepinas y sus esteres.
US5978740A (en) 1995-08-09 1999-11-02 Vertex Pharmaceuticals Incorporated Molecules comprising a calcineurin-like binding pocket and encoded data storage medium capable of graphically displaying them
WO1997009048A1 (en) 1995-09-09 1997-03-13 F. Hoffmann-La Roche Ag Use of a thienotriazolodiazepine to increase apolipoprotein a-i levels
EP0934940A1 (en) * 1996-06-12 1999-08-11 Japan Tobacco Inc. Cytokine production inhibitors, triazepine compounds, and intermediates thereof
ES2182108T3 (es) * 1996-09-13 2003-03-01 Mitsubishi Pharma Corp Compuestos de tienotriazolodiazepina y usos medicinales de los mismos.
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
US6183121B1 (en) 1997-08-14 2001-02-06 Vertex Pharmaceuticals Inc. Hepatitis C virus helicase crystals and coordinates that define helicase binding pockets
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
KR20000016732A (en) 1998-12-12 2000-03-25 Japan Tobacco Inc Cytokine production inhibitors, triazepine compounds, and intermediates thereof
CA2373815A1 (en) 1999-05-14 2000-11-23 Imclone Systems Incorporated Treatment of refractory human tumors with epidermal growth factor receptor antagonists
US7589167B2 (en) * 2000-02-22 2009-09-15 J. David Gladstone Institutes ZA loops of bromodomains
EP1297836A4 (en) 2000-06-16 2007-06-13 Mitsubishi Pharma Corp COMPOSITIONS FOR CHECKING RELEASE, PH AREA AND / OR SPEED
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
KR20050106465A (ko) 2003-02-27 2005-11-09 아보트 러보러터리즈 헤테로사이클릭 키나제 억제제
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
AU2004251654A1 (en) 2003-06-02 2005-01-06 Icoria, Inc. Use of genes differentially expressed during aging of liver for treatment and diagnosis
WO2005002526A2 (en) 2003-07-01 2005-01-13 President And Fellows Of Harvard College Method and compositions for treatment of viral infections
EP1663992A1 (en) 2003-09-18 2006-06-07 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
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US7759485B2 (en) 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
US20060074088A1 (en) 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
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
US8624027B2 (en) 2005-05-12 2014-01-07 Abbvie Inc. Combination therapy for treating cancer and diagnostic assays for use therein
US8044042B2 (en) 2005-05-30 2011-10-25 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and medicinal use thereof
JP2009503014A (ja) 2005-08-03 2009-01-29 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 呼吸器系疾患の治療におけるジヒドロプテリジノン
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
NZ592990A (en) 2005-11-01 2013-01-25 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
AR058505A1 (es) 2005-11-04 2008-02-06 Wyeth Corp Combinaciones antineoplasicas de temsirolimus y malato de sunitinib
MX2008008320A (es) 2005-12-23 2008-09-03 Smithkline Beecham Corp Inhibidores de azaindol de aurora cinasas.
RU2426732C2 (ru) 2006-01-17 2011-08-20 Ф. Хоффманн-Ля Рош Аг АРИЛ-ИЗОКСАЗОЛ-4-ИЛ-ИМИДАЗО[1,2-a]ПИРИДИН, ПРИГОДНЫЙ ДЛЯ ЛЕЧЕНИЯ БОЛЕЗНИ АЛЬЦГЕЙМЕРА ЧЕРЕЗ ПОСРЕДСТВО GABA-РЕЦЕПТОРОВ
JP5243970B2 (ja) 2006-02-14 2013-07-24 バーテックス ファーマシューティカルズ インコーポレイテッド タンパク質キナーゼの阻害剤として有用なジヒドロジアゼピン
US20070218135A1 (en) 2006-03-14 2007-09-20 Glenmark Pharmaceuticals Limited Sustained release matrix pharmaceutical composition
JP2009535425A (ja) 2006-05-03 2009-10-01 ノバルティス アクチエンゲゼルシャフト 有機化合物の使用
EP2078016B1 (en) 2006-10-19 2012-02-01 Signal Pharmaceuticals LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
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
KR101810348B1 (ko) 2006-12-26 2017-12-18 랜티우스 메디컬 이메징, 인크. 심장 신경 분포의 영상화를 위한 리간드
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
EP2234986A2 (en) 2007-12-20 2010-10-06 Cellzome Limited Sulfamides as zap-70 inhibitors
WO2009084693A1 (ja) * 2007-12-28 2009-07-09 Mitsubishi Tanabe Pharma Corporation 抗癌剤
US20110098288A1 (en) 2008-03-11 2011-04-28 Jeremy Major Sulfonamides as zap-70 inhibitors
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
ES2448567T3 (es) 2008-10-30 2014-03-14 Circomed Llc Derivados de la tienotriazoldiazepina activos en apo A
JP5908728B2 (ja) 2009-01-06 2016-04-26 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 ピリミド−ジアゼピノンキナーゼ骨格化合物及び疾患を治療する方法
US7928105B2 (en) 2009-01-23 2011-04-19 Takeda Pharmaceutical Company Limited Substituted 6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-ones
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
AU2010314395B2 (en) 2009-11-05 2015-04-09 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
ES2564318T3 (es) 2009-11-05 2016-03-21 Glaxosmithkline Llc Inhibidor de bromodominio de benzodiazepina
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP2536725B1 (en) 2010-02-17 2015-10-28 Boehringer Ingelheim International GmbH Dihydropteridinones, method for production and use thereof
HUE031073T2 (en) 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
EP2569434B1 (en) 2010-05-14 2019-09-04 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia and related disorders
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
JP5715241B2 (ja) 2010-05-14 2015-05-07 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 新生物、炎症性疾患、およびその他の障害を治療するための組成物および方法
US9301962B2 (en) 2010-05-14 2016-04-05 Baylor College Of Medicine Male contraceptive compositions and methods of use
ES2526671T3 (es) 2010-06-22 2015-01-14 Glaxosmithkline Llc Compuestos de benzotriazoldiazepina inhibidores de bromodominios
JP6073783B2 (ja) 2010-06-25 2017-02-01 シャイアー ヒューマン ジェネティック セラピーズ インコーポレイテッド ヘパランn−スルファターゼのcns送達のための方法および組成物
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
CN103228142A (zh) 2010-09-28 2013-07-31 加利福尼亚大学董事会 治疗代谢综合征相关疾病的gaba激动剂和治疗或预防i型糖尿病的gaba组合
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
US20130004481A1 (en) 2011-01-12 2013-01-03 Boehringer Ingelheim International Gmbh Anticancer therapy
EP2677865A4 (en) 2011-02-23 2015-04-22 Icahn School Med Mount Sinai BROMODOMAIN INHIBITORS AS MODULATORS OF GENE EXPRESSION
JP2014511389A (ja) 2011-02-28 2014-05-15 エピザイム インコーポレイテッド 置換6,5−縮合二環式ヘテロアリール化合物
EP2741784B1 (en) 2011-03-02 2017-05-17 Board Of Regents, The University Of Texas System Tusc2 therapies
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
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
US10071129B2 (en) 2011-08-30 2018-09-11 Whitehead Institute For Biomedical Research Dana-Farber Cancer Institute, Inc. Method for identifying bromodomain inhibitors
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
CN104203267A (zh) 2012-02-17 2014-12-10 安迅生物制药公司 用于治疗流感和副流感患者的方法、化合物和组合物
WO2013148197A1 (en) 2012-03-28 2013-10-03 The J. David Gladstone Institutes Compositions and methods for reactivating latent immunodeficiency virus
US9763956B2 (en) 2012-06-19 2017-09-19 The Broad Institute, Inc. Diagnostic and treatment methods in subjects having or at risk of developing resistance to cancer therapy
CN104968334B (zh) 2012-09-28 2018-09-14 翁科埃斯克斯有限公司 包含噻吩并***并二氮杂卓化合物的药物制剂
US9567301B2 (en) 2012-11-02 2017-02-14 Dana-Farber Cancer Institute, Inc. Pyrrol-1-yl benzoic acid derivatives useful as myc inhibitors
US20160009725A1 (en) 2013-02-22 2016-01-14 Bayer Pharma Aktiengesellschaft Pyrrolo- and pyrazolo-triazolodiazepines as bet-protein inhibitors for treating hyperproliferative diseases
CN105164135A (zh) 2013-02-22 2015-12-16 拜耳医药股份有限公司 4-取代的吡咯并二氮杂卓和吡唑并二氮杂卓
CA2902225A1 (en) 2013-02-28 2014-09-04 Washington University Methods of treatment of human cytomegalovirus infection and diseases with bromodomain inhibitors
US9714946B2 (en) 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
BR112015023184A2 (pt) 2013-03-15 2017-11-21 Constellation Pharmaceuticals Inc método para o tratamento de uma doença, inibidor e seu uso, composição, método de identificação de um composto e método para inibir a produção de il-4, il-5 e il-13
CA2913741A1 (en) 2013-05-28 2014-12-04 The Brigham And Women's Hospital, Inc. Bet inhibition therapy for heart disease
DE102013106353B4 (de) 2013-06-18 2018-06-28 Tdk Corporation Verfahren zum Aufbringen einer strukturierten Beschichtung auf ein Bauelement
KR20160034379A (ko) 2013-07-25 2016-03-29 다나-파버 캔서 인스티튜트 인크. 전사 인자의 억제제 및 그의 용도
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)
KR20160037201A (ko) 2013-08-06 2016-04-05 온코에틱스 게엠베하 Bet-브로모도메인 억제제를 사용한 미만성 거대 b-세포 림프종 (dlbcl)의 치료 방법
WO2015023938A1 (en) 2013-08-16 2015-02-19 Rana Therapeutics, Inc. Epigenetic regulators of frataxin
JP6663852B2 (ja) 2013-09-19 2020-03-13 デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド Bh3プロファイリングの方法
WO2015054642A2 (en) 2013-10-11 2015-04-16 Genentech, Inc. Use of cbp/ep300 bromodomain inhibitors for cancer immunotherapy
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
WO2015081284A1 (en) 2013-11-26 2015-06-04 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
WO2015117083A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
CA2936865A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
EP3099693A4 (en) 2014-01-31 2017-08-16 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
AU2015222805B2 (en) 2014-02-28 2020-05-21 Tensha Therapeutics, Inc. Treatment of conditions associated with hyperinsulinaemia
BR112017008714A2 (pt) 2014-10-27 2017-12-19 Tensha Therapeutics Inc inibidores de bromodomínio
CA2969417A1 (en) 2014-12-05 2016-06-09 H. Lee Moffitt Cancer Center And Research Institute, Inc. Bromodomain inhibitor as adjuvant in cancer immunotherapy
MA42249A (fr) 2015-06-26 2018-05-02 Tensha Therapeutics Inc Traitement de carcinome de la ligne médiane nut
JP2018530554A (ja) 2015-10-02 2018-10-18 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 ブロモドメイン阻害薬及びチェックポイント阻害薬による併用療法

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