MX362384B - Composiciones y metodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos. - Google Patents

Composiciones y metodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos.

Info

Publication number
MX362384B
MX362384B MX2015008841A MX2015008841A MX362384B MX 362384 B MX362384 B MX 362384B MX 2015008841 A MX2015008841 A MX 2015008841A MX 2015008841 A MX2015008841 A MX 2015008841A MX 362384 B MX362384 B MX 362384B
Authority
MX
Mexico
Prior art keywords
methods
compositions
disorders
inflammatory disease
treating neoplasia
Prior art date
Application number
MX2015008841A
Other languages
English (en)
Inventor
Elliott Bradner James
Qi Jun
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 MX362384B publication Critical patent/MX362384B/es

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Classifications

    • 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

Landscapes

  • 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)

Abstract

La invención presenta composiciones y métodos para tratar o prevenir una neoplasia. Más concretamente, la invención proporciona composiciones y métodos para alterar la interacción de un polipéptido de la familia BET que comprende un bromodominio con la cromatina (p. ej., alterar la interacción de un bromodominio con una modificación de lisina acetilada presente en una cola N-terminal de la histona).
MX2015008841A 2010-05-14 2011-05-16 Composiciones y metodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos. MX362384B (es)

Applications Claiming Priority (5)

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
PCT/US2011/036701 WO2011143669A2 (en) 2010-05-14 2011-05-16 Compositions and methods for treating neoplasia, inflammatory disease and other disorders

Publications (1)

Publication Number Publication Date
MX362384B true MX362384B (es) 2019-01-15

Family

ID=44915031

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2012013255A MX2012013255A (es) 2010-05-14 2011-05-16 Composiciones y metodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos.
MX2015008841A MX362384B (es) 2010-05-14 2011-05-16 Composiciones y metodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
MX2012013255A MX2012013255A (es) 2010-05-14 2011-05-16 Composiciones y metodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos.

Country Status (17)

Country Link
US (5) US8981083B2 (es)
EP (2) EP2902030B1 (es)
KR (1) KR101857599B1 (es)
CN (2) CN104311562B (es)
AU (1) AU2011252808B2 (es)
BR (2) BR112012029005A2 (es)
CA (1) CA2799420C (es)
DK (1) DK2571503T3 (es)
ES (2) ES2534521T3 (es)
HK (2) HK1183620A1 (es)
HU (1) HUE031073T2 (es)
IL (3) IL222993A (es)
MX (2) MX2012013255A (es)
PL (2) PL2902030T3 (es)
PT (1) PT2571503E (es)
SI (1) SI2902030T1 (es)
WO (1) WO2011143669A2 (es)

Families Citing this family (174)

* 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
BR112012029057A2 (pt) 2010-05-14 2020-10-13 Dana-Farber Cancer Institute, Inc. composições e métodos de tratamento de leucemia
EP2902030B1 (en) * 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
CA2799381A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Male contraceptive compositions and methods of use
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
WO2012174487A2 (en) 2011-06-17 2012-12-20 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
JP6106685B2 (ja) 2011-11-17 2017-04-05 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 C−jun−n−末端キナーゼ(jnk)の阻害剤
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
CN117736134A (zh) 2012-01-12 2024-03-22 耶鲁大学 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法
EP2819662B1 (en) * 2012-02-27 2019-04-10 British Columbia Cancer Agency Branch Reprogramming effector protein interactions to correct epigenetic defects in cancer
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
EP2861988B1 (en) 2012-06-14 2019-05-22 The Whitehead Institute for Biomedical Research Genome-wide method of assessing interactions between chemical entities and their target molecules
EP2861255B1 (en) 2012-06-19 2019-10-09 The Broad Institute, Inc. Diagnostic and treatment methods in subjects having or at risk of developing resistance to cancer therapy
CA2877434A1 (en) * 2012-06-25 2014-01-03 Oncoethix Sa Method of treating lymphoma using thienotriazolodiazepine compounds
US9610332B2 (en) 2012-07-18 2017-04-04 Massachusetts Institute Of Technology Compositions and methods for modulating BRD4 bioactivity
US9890147B2 (en) 2012-08-16 2018-02-13 Bayer Pharma Aktiengesellshaft 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)
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
CA2895905A1 (en) 2012-12-21 2014-06-26 Zenith Epigenetics Corp. Novel heterocyclic compounds as bromodomain inhibitors
CA2896053A1 (en) 2012-12-21 2014-06-26 Ocata Therapeutics, Inc. Methods for production of platelets from pluripotent stem cells and compositions thereof
MA38346B1 (fr) 2013-02-19 2019-05-31 Bayer Pharma AG 2,3-benzodiazépines bicyclo- et spirocyclosubstituées
US20150376196A1 (en) 2013-02-22 2015-12-31 Bayer Pharma Aktiengesellschaft 4-substituted pyrrolo- and pyrazolo-diazepines
CA2901799A1 (en) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft Pyrrolo- and pyrazolo-triazolodiazepines as bet-protein inhibitors for treating hyperproliferative diseases
WO2014134583A2 (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
SG10201707487VA (en) 2013-03-15 2017-10-30 Incyte Corp Tricyclic heterocycles as bet protein inhibitors
JP6388915B2 (ja) 2013-04-26 2018-09-12 ベイジーン,リミテッド 置換5−(3,5−ジメチルイソオキサゾール−4−イル)インドリン−2−オン
CA2913741A1 (en) * 2013-05-28 2014-12-04 The Brigham And Women's Hospital, Inc. Bet inhibition therapy for heart disease
JP6461118B2 (ja) 2013-06-21 2019-01-30 ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. ブロモドメイン阻害剤としての新規の置換された二環式化合物
NZ714669A (en) 2013-06-21 2021-07-30 Zenith Epigenetics Ltd Novel bicyclic bromodomain inhibitors
SG11201510678TA (en) * 2013-06-28 2016-01-28 Abbvie Inc Bromodomain inhibitors
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
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
EA201690087A1 (ru) 2013-07-31 2016-08-31 Зенит Эпидженетикс Корп. Новые квиназолиноны как ингибиторы бромодомена
WO2015018523A1 (en) * 2013-08-06 2015-02-12 Oncoethix Sa A novel bet-brd inhibitor for treatment of solid tumors
WO2015018521A1 (en) * 2013-08-06 2015-02-12 Oncoethix Sa 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)
WO2015031741A1 (en) 2013-08-30 2015-03-05 Concert Pharmaceuticals, Inc. Deuterated derivatives of a thienotriazolodiazapine bromodomain-containing protein inhibitor
EP3057955B1 (en) 2013-10-18 2018-04-11 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
US11446309B2 (en) 2013-11-08 2022-09-20 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
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
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
CN105960239A (zh) 2013-11-27 2016-09-21 翁科埃斯克斯有限公司 利用含有噻吩并三唑并二氮杂*化合物的药物制剂治疗白血病的方法
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
WO2015112809A2 (en) * 2014-01-24 2015-07-30 The Brigham And Women's Hospital, Inc. Nsd3 inhibitors for treatment of cancers
MX2016009976A (es) 2014-01-31 2016-11-15 Dana Farber Cancer Inst Inc Derivados de diazepam y sus usos.
RU2016134947A (ru) 2014-01-31 2018-03-01 Дана-Фарбер Кансер Институт, Инк. Производные диаминопиримидин бензолсульфона и их применение
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
CN106459056A (zh) 2014-02-10 2017-02-22 康塞特医药品公司 经取代的三唑苯二氮卓
CN107074861A (zh) 2014-02-28 2017-08-18 密执安大学评议会 作为bet溴结构域抑制剂的9h嘧啶并[4,5‑b]吲哚和相关类似物
WO2015131113A1 (en) * 2014-02-28 2015-09-03 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
KR20220101015A (ko) * 2014-04-14 2022-07-18 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
SG11201608843TA (en) 2014-04-23 2016-11-29 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
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
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
AU2015252844A1 (en) * 2014-05-02 2016-11-03 Kay NOEL Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds
RU2016147946A (ru) 2014-05-08 2018-06-08 Онкоэтикс Гмбх Способ лечения трижды негативного рака молочной железы с использованием тиенотриазолодиазепиновых соединений
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
JP2017526741A (ja) 2014-08-08 2017-09-14 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
JP2017525759A (ja) 2014-08-08 2017-09-07 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 ジヒドロプテリジノン誘導体およびその使用
JP2017529332A (ja) * 2014-08-28 2017-10-05 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組成物を用いる急性骨髄性白血病又は急性リンパ性白血病の治療方法
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
WO2016069578A1 (en) * 2014-10-27 2016-05-06 Tensha Therapeutics, Inc. Bromodomain inhibitors
BR112017009671A2 (pt) 2014-11-06 2017-12-26 Dana Farber Cancer Inst Inc inibidores de ezh2 e usos destes
JP6938154B2 (ja) * 2014-11-07 2021-09-22 国立大学法人大阪大学 未分化細胞が除去された分化誘導細胞集団、その利用及びその製造方法
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
KR20170101913A (ko) * 2014-12-05 2017-09-06 에이치 리 모피트 캔서 센터 앤드 리서어치 인스티튜트 아이엔씨 암 면역치료의 보조제로서의 브로모도메인 억제제
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
US10870651B2 (en) 2014-12-23 2020-12-22 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
CN107257800B (zh) 2014-12-23 2020-06-30 达纳-法伯癌症研究所股份有限公司 通过双功能分子诱导靶蛋白降解的方法
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
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
KR20230175343A (ko) 2015-03-18 2023-12-29 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
JP6861166B2 (ja) 2015-03-27 2021-04-21 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 サイクリン依存性キナーゼの阻害剤
WO2016176335A1 (en) 2015-04-27 2016-11-03 Concert Pharmaceuticals, Inc. Deuterated otx-015
WO2016179222A1 (en) * 2015-05-04 2016-11-10 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
KR102691931B1 (ko) * 2015-06-04 2024-08-05 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드계 조절인자 및 관련된 이용 방법
WO2016201370A1 (en) 2015-06-12 2016-12-15 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
JP2018526430A (ja) * 2015-07-10 2018-09-13 アルヴィナス・インコーポレイテッド タンパク質分解のmdm2系修飾因子および関連の使用方法
US11666580B2 (en) 2015-08-10 2023-06-06 Dana-Farber Cancer Institute, Inc. Mechanism of resistance to bet bromodomain inhibitors
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, 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
BR112018004617A2 (pt) 2015-09-11 2018-09-25 Dana Farber Cancer Inst Inc acetamida tienotriazoldiazepinas e usos das mesmas
RU2750164C2 (ru) 2015-09-11 2021-06-22 Дана-Фарбер Кэнсер Инститьют, Инк. Цианотиенотриазолодиазепины и пути их применения
EP3355922A2 (en) * 2015-10-02 2018-08-08 Dana Farber Cancer Institute, Inc. Combination therapy of bromodomain inhibitors and checkpoint blockade
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CR20180336A (es) 2015-11-25 2018-08-06 Dana Farber Cancer Inst Inc Inhibidores de bromodominio bivalentes y usos de los mismos
WO2017142881A1 (en) 2016-02-15 2017-08-24 The Regents Of The University Of Michigan Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors
CA3019342A1 (en) 2016-03-30 2017-10-05 Wisconsin Alumni Research Foundation Methods and compositions for modulating frataxin expression
US11192898B2 (en) 2016-04-06 2021-12-07 The Regents Of The University Of Michigan MDM2 protein degraders
CA3020281A1 (en) 2016-04-06 2017-10-12 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
RU2752677C2 (ru) 2016-04-12 2021-07-29 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган Деструкторы белка вет
MA44674B1 (fr) 2016-04-15 2020-06-30 Abbvie Inc Inhibiteurs de bromodomaine
EP3445365A4 (en) 2016-04-22 2019-10-16 Dana-Farber Cancer Institute, Inc. EZH2 INHIBITORS AND USES THEREOF
EP3454856B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-LINKED C3-GLUTARIMIDE DEGRONIMERS FOR THE DEGRADATION OF TARGET PROTEINS
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
DE102017005089A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
IL263824B2 (en) 2016-06-20 2023-10-01 Incyte Corp Crystals in solid form in the presence of an inhibitor
WO2018002290A1 (en) 2016-07-01 2018-01-04 Centre National De La Recherche Scientifique (Cnrs) Amplifying beta cell differentiation with small molecules bet (bromodomain and extraterminal family of bromodomain-containing proteins) inhibitors
WO2018052945A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
EP3858837A1 (en) 2016-09-13 2021-08-04 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
EP3555059A1 (en) * 2016-12-16 2019-10-23 H. Hoffnabb-La Roche Ag Process for the manufacture of diazepine derivatives
US11046709B2 (en) 2017-02-03 2021-06-29 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
US11098043B2 (en) 2017-07-14 2021-08-24 University Of Massachusetts Certain imidazopyridines as cyclic AMP response element binding (CREB) binding protein (CBP) inhibitors and uses thereof
EP3658584A1 (en) 2017-07-26 2020-06-03 H. Hoffnabb-La Roche Ag Combination therapy with a bet inhibitor, a bcl-2 inhibitor and an anti-cd20 antibody
EP3658188A1 (en) * 2017-07-26 2020-06-03 H. Hoffnabb-La Roche Ag Combination therapy with a bet inhibitor and a bcl-2 inhibitor
EP3679027A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Dihydrobenzimidazolones
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
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
CN108084193A (zh) * 2017-12-19 2018-05-29 郭守东 一种brd4蛋白抑制剂
CN108129484B (zh) * 2017-12-19 2021-04-27 郭守东 杂芳环衍生物
US11220515B2 (en) 2018-01-26 2022-01-11 Yale University Imide-based modulators of proteolysis and associated methods of use
WO2019191112A1 (en) 2018-03-26 2019-10-03 C4 Therapeutics, Inc. Cereblon binders for the degradation of ikaros
CN112312904A (zh) 2018-04-16 2021-02-02 C4医药公司 螺环化合物
WO2019201882A1 (en) 2018-04-18 2019-10-24 F. Hoffmann-La Roche Ag Combination therapy with a bet inhibitor and a proteasome inhibitor
MX2020013608A (es) 2018-06-13 2021-03-09 Worg Pharmaceuticals Hangzhou Co Ltd Preparacion de derivados de triazepina condensados y su uso como inhibidores de bet.
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
KR20210038921A (ko) 2018-07-25 2021-04-08 치아타이 티안큉 파마수티컬 그룹 주식회사 브로모도메인 단백질 억제제로서의 설폭시민 화합물과 약학적 조성물 및 이의 의학적 용도
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
WO2020086858A1 (en) 2018-10-24 2020-04-30 Genentech, Inc. 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
EP4051283A4 (en) * 2019-11-01 2024-03-27 The Regents of the University of California P53 MODULATORS AND USES THEREOF
US11883393B2 (en) 2019-12-19 2024-01-30 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
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
TW202219056A (zh) 2020-06-23 2022-05-16 美商建南德克公司 巨環化合物及其使用方法
WO2022046682A1 (en) * 2020-08-26 2022-03-03 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
EP4401715A1 (en) 2021-09-17 2024-07-24 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
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
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
EP0407955A1 (de) 1989-07-12 1991-01-16 Boehringer Ingelheim Kg Neue Hetrazepine mit PAF-antagonistischer Wirkung, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
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
EP0638560A4 (en) 1991-10-11 1995-03-29 Yoshitomi Pharmaceutical MEDICINE FOR OSTEOPOROSIS AND DIAZEPINE COMPOUND *.
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
WO1995032963A1 (fr) 1994-06-01 1995-12-07 Yoshitomi Pharmaceutical Industries, Ltd. Compose de thienylazole et compose de thienotriazolodiazepine
DK0801651T3 (da) 1995-01-06 2001-10-22 Hoffmann La Roche Hydroxymethyl-imidazodiazepiner og deres estere
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
CA2230477A1 (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
EA001732B1 (ru) * 1996-09-13 2001-08-27 Велфайд Корпорейшн Тиенотриазолодиазепиновые соединения и лекарственное средство
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
EE200100603A (et) 1999-05-14 2003-02-17 Imclone Systems Incorporated Inimese refraktaarsete kasvajate ravi epidermaalse kasvufaktori retseptori antagonistidega
US7589167B2 (en) * 2000-02-22 2009-09-15 J. David Gladstone Institutes ZA loops of bromodomains
AU2001264303A1 (en) 2000-06-16 2001-12-24 Mitsubishi Pharma Corporation Compositions controlling release ph range and/or speed
US6552037B2 (en) 2000-06-30 2003-04-22 Neurogen Corporation 2-Substituted imidazo[1,2-A]pyridine derivatives
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
MXPA05009151A (es) 2003-02-27 2005-10-20 Abbott Lab Inhibidores de cinasa heterociclica.
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US20070111933A1 (en) 2003-06-02 2007-05-17 Kopchick John J Diagnosis and treatment methods related to aging, especially of liver
WO2005002526A2 (en) 2003-07-01 2005-01-13 President And Fellows Of Harvard College Method and compositions for treatment of viral infections
CN100584832C (zh) 2003-09-18 2010-01-27 诺瓦提斯公司 可用于治疗增殖性病症的2,4-二(苯基氨基)嘧啶类
EP1528056A1 (en) 2003-10-29 2005-05-04 Academisch Ziekenhuis bij de Universiteit van Amsterdam Deoxynojirimycin analogues and their uses as glucosylceramidase inhibitors
US7759485B2 (en) 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
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
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
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
CA2617589A1 (en) 2005-08-03 2007-02-08 Boehringer Ingelheim International Gmbh Dihydropteridinones in the treatment of respiratory diseases
US7528143B2 (en) 2005-11-01 2009-05-05 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
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007056117A1 (en) 2005-11-04 2007-05-18 Wyeth Antineoplastic combinations of temsirolimus and sunitinib malate
KR20080083680A (ko) 2005-12-23 2008-09-18 스미스클라인 비참 코포레이션 오로라 키나제의 아자인돌 억제제
CN101370807B (zh) 2006-01-17 2011-08-31 弗·哈夫曼-拉罗切有限公司 可用于经由gaba受体治疗阿尔茨海默病的芳基-异唑-4-基-咪唑并[1,2-a]吡啶
DE602007008837D1 (de) 2006-02-14 2010-10-14 Vertex Pharma Als protein-kinase-inhibitoren nutzbare dyhydrodiazepine
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
RU2478635C2 (ru) 2006-10-19 2013-04-10 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Гетероарильные соединения, содержащие их композиции и способы лечения с применением этих соединений
WO2008066887A2 (en) 2006-11-30 2008-06-05 Albert Einstein College Of Medicine Of Yeshiva University Small molecule inhibitors of bcl6
EP2474525B1 (en) 2006-12-26 2020-04-15 Lantheus Medical Imaging, Inc. Ligands for imaging cardiac innervation
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
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
CA2717529A1 (en) 2008-03-11 2009-09-17 Cellzome Limited 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
AU2009309691B2 (en) 2008-10-30 2015-04-02 Circomed Llc Thienotriazolodiazepine derivatives active on apo A
EP3255047B1 (en) 2009-01-06 2021-06-30 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and uses in 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
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
WO2011054845A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
KR101424989B1 (ko) 2009-11-05 2014-07-31 글락소스미스클라인 엘엘씨 벤조디아제핀 브로모도메인 억제제
JP5841548B2 (ja) 2010-02-17 2016-01-13 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 ジヒドロプテリジノン、その製造方法及び使用
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
BR112012029057A2 (pt) 2010-05-14 2020-10-13 Dana-Farber Cancer Institute, Inc. composições e métodos de tratamento de leucemia
EP2902030B1 (en) 2010-05-14 2016-09-14 Dana-Farber Cancer Institute, Inc. Thienotriazolodiazepine compounds for treating neoplasia
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
CA2799381A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Male contraceptive compositions and methods of use
WO2011161031A1 (en) 2010-06-22 2011-12-29 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
MX2013000320A (es) 2010-06-25 2013-06-05 Shire Human Genetic Therapies Composiciones y metodos para suministro al sistema nervioso central de heparan n-sulfatasa.
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
US20130004481A1 (en) 2011-01-12 2013-01-03 Boehringer Ingelheim International Gmbh Anticancer therapy
CA2828212A1 (en) 2011-02-23 2012-08-30 Shiraz Mujtaba Inhibitors of bromodomains as modulators of gene expression
WO2012118812A2 (en) 2011-02-28 2012-09-07 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2012119095A1 (en) 2011-03-02 2012-09-07 Board Of Regents, The University Of Texas System Fus1/tusc2 therapies
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
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
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
CN109529026A (zh) 2012-02-17 2019-03-29 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
EP2861255B1 (en) 2012-06-19 2019-10-09 The Broad Institute, Inc. Diagnostic and treatment methods in subjects having or at risk of developing resistance to cancer therapy
WO2014068402A2 (en) 2012-09-28 2014-05-08 Oncoethix Sa Pharmaceutical formulation containing thienotriazolodiazepine compounds
EP2917203B1 (en) 2012-11-02 2019-04-03 Dana-Farber Cancer Institute, Inc. Method for identifying myc inhibitors
CA2901799A1 (en) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft Pyrrolo- and pyrazolo-triazolodiazepines as bet-protein inhibitors for treating hyperproliferative diseases
US20150376196A1 (en) 2013-02-22 2015-12-31 Bayer Pharma Aktiengesellschaft 4-substituted pyrrolo- and pyrazolo-diazepines
WO2014134583A2 (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
JP2016519672A (ja) 2013-03-15 2016-07-07 ジェネンテック, インコーポレイテッド ブロモドメイン含有タンパク質brd7およびbrd9の阻害によるth2媒介性疾患の治療
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
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
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)
WO2015018521A1 (en) 2013-08-06 2015-02-12 Oncoethix Sa Method of treating diffuse large b-cell lymphoma (dlbcl) using a bet-bromodomain inhibitor
WO2015023938A1 (en) 2013-08-16 2015-02-19 Rana Therapeutics, Inc. Epigenetic regulators of frataxin
US10739333B2 (en) 2013-09-19 2020-08-11 Dana-Farber Cancer Institute, Inc. Methods of BH3 profiling
BR112016007891A2 (pt) 2013-10-11 2017-12-05 Constellation Pharmaceuticals Inc uso de inibidores de bromodomínio cbp/ep300 para imunoterapia do câncer
US11446309B2 (en) 2013-11-08 2022-09-20 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
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
MX2016009976A (es) 2014-01-31 2016-11-15 Dana Farber Cancer Inst Inc Derivados de diazepam y sus usos.
RU2016134947A (ru) 2014-01-31 2018-03-01 Дана-Фарбер Кансер Институт, Инк. Производные диаминопиримидин бензолсульфона и их применение
WO2015131113A1 (en) 2014-02-28 2015-09-03 Tensha Therapeutics, Inc. Treatment of conditions associated with hyperinsulinaemia
WO2016069578A1 (en) 2014-10-27 2016-05-06 Tensha Therapeutics, Inc. Bromodomain inhibitors
KR20170101913A (ko) 2014-12-05 2017-09-06 에이치 리 모피트 캔서 센터 앤드 리서어치 인스티튜트 아이엔씨 암 면역치료의 보조제로서의 브로모도메인 억제제
MA42249A (fr) 2015-06-26 2018-05-02 Tensha Therapeutics Inc Traitement de carcinome de la ligne médiane nut
EP3355922A2 (en) 2015-10-02 2018-08-08 Dana Farber Cancer Institute, Inc. Combination therapy of bromodomain inhibitors and checkpoint blockade

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