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EA201290184A1 - Бензодиазепиновый ингибитор бромодомена - Google Patents

Бензодиазепиновый ингибитор бромодомена

Info

Publication number
EA201290184A1
EA201290184A1 EA201290184A EA201290184A EA201290184A1 EA 201290184 A1 EA201290184 A1 EA 201290184A1 EA 201290184 A EA201290184 A EA 201290184A EA 201290184 A EA201290184 A EA 201290184A EA 201290184 A1 EA201290184 A1 EA 201290184A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitor
bromodomene
benzodiazepinum
compounds
therapy
Prior art date
Application number
EA201290184A
Other languages
English (en)
Other versions
EA023441B1 (ru
Inventor
Джеймс Бэйли
Ромэн Люк Мари Госмини
Оливье Миргюэ
Джейсон Уизерингтон
Original Assignee
ГЛАКСОСМИТКЛАЙН ЭлЭлСи
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
Priority claimed from GB0919433A external-priority patent/GB0919433D0/en
Priority claimed from GBGB1010509.6A external-priority patent/GB201010509D0/en
Priority claimed from PCT/EP2010/061518 external-priority patent/WO2011054553A1/en
Priority claimed from GBGB1014231.3A external-priority patent/GB201014231D0/en
Application filed by ГЛАКСОСМИТКЛАЙН ЭлЭлСи filed Critical ГЛАКСОСМИТКЛАЙН ЭлЭлСи
Publication of EA201290184A1 publication Critical patent/EA201290184A1/ru
Publication of EA023441B1 publication Critical patent/EA023441B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Предложены бензодиазепиновые соединения формулы (I)и их соли, фармацевтические композиции, содержащие такие соединения, и их применение в терапии, в частности в лечении заболеваний или состояний, для которых показан ингибитор бромодомена.
EA201290184A 2009-11-05 2010-11-03 Бензодиазепиновый ингибитор бромодомена EA023441B1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0919433A GB0919433D0 (en) 2009-11-05 2009-11-05 Novel compounds
GBGB1010509.6A GB201010509D0 (en) 2010-06-22 2010-06-22 Novel compounds
PCT/EP2010/061518 WO2011054553A1 (en) 2009-11-05 2010-08-06 Benzodiazepine bromodomain inhibitor
GBGB1014231.3A GB201014231D0 (en) 2010-08-25 2010-08-25 Novel compounds
PCT/EP2010/066697 WO2011054845A1 (en) 2009-11-05 2010-11-03 Benzodiazepine bromodomain inhibitor

Publications (2)

Publication Number Publication Date
EA201290184A1 true EA201290184A1 (ru) 2012-12-28
EA023441B1 EA023441B1 (ru) 2016-06-30

Family

ID=43969589

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201290184A EA023441B1 (ru) 2009-11-05 2010-11-03 Бензодиазепиновый ингибитор бромодомена

Country Status (23)

Country Link
US (3) US9102677B2 (ru)
EP (2) EP3050885B1 (ru)
JP (3) JP5702396B2 (ru)
KR (1) KR20120097508A (ru)
CN (1) CN102781943B (ru)
AU (1) AU2010317096B2 (ru)
BR (1) BR112012010705A2 (ru)
CA (1) CA2779423C (ru)
CY (1) CY1117424T1 (ru)
DK (1) DK2496582T3 (ru)
EA (1) EA023441B1 (ru)
ES (2) ES2654423T3 (ru)
HK (1) HK1221221A1 (ru)
HR (1) HRP20160253T1 (ru)
HU (1) HUE026967T2 (ru)
IL (2) IL219253A (ru)
ME (1) ME02356B (ru)
MX (1) MX341212B (ru)
PL (1) PL2496582T3 (ru)
RS (1) RS54645B1 (ru)
SI (1) SI2496582T1 (ru)
SM (1) SMT201600104B (ru)
WO (1) WO2011054845A1 (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2697393C2 (ru) * 2014-10-02 2019-08-14 ГлаксоСмитКлайн Интеллекчуал Проперти (N 2) Лимитед Кристаллическая твердая форма соли бензолсульфоновой кислоты и 2-[(4S)-6-(4-хлорфенил)-1-метил-8-(метилокси)-4H-[1,2,4]триазоло[4,3-a][1,4]бензодиазепин-4-ил]-N-этилацетамида, способ ее получения и фармацевтическая композиция, содержащая ее

Families Citing this family (135)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2081921T3 (da) 2006-07-10 2011-01-03 Paion Uk Ltd Korttidsvirkende benzodiazepinsalte og deres polymorfe former
SI2496582T1 (sl) * 2009-11-05 2016-04-29 Glaxosmithkline Llc Corporation Service Company Benzodiazepinski inhibitor bromodomene
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
ES2534521T3 (es) 2010-05-14 2015-04-23 Dana-Farber Cancer Institute, Inc. Composiciones y su uso en el tratamiento de neoplasia, enfermedades inflamatorias y otras enfermedades
CN103154246B (zh) 2010-05-14 2015-11-25 达那-法伯癌症研究所 用于治疗白血病的组合物和方法
CN103180318B (zh) 2010-05-14 2017-05-10 达那-法伯癌症研究所 雄性避孕组合物以及使用方法
EP2450039A1 (en) 2010-11-08 2012-05-09 PAION UK Ltd. Dosing regimen for sedation with CNS 7056 (Remimazolam)
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
US9328117B2 (en) 2011-06-17 2016-05-03 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) * 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033270A2 (en) * 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
CN104334526A (zh) 2012-04-20 2015-02-04 艾伯维公司 异吲哚酮衍生物
EP2852389B1 (en) * 2012-05-22 2017-10-18 Paion UK Limited Compositions comprising short-acting benzodiazepines
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
BR112014031068A2 (pt) 2012-06-12 2017-06-27 Abbvie Inc derivados piridinona e piridazinona
EP2885286B1 (de) 2012-08-16 2017-03-22 Bayer Pharma Aktiengesellschaft 2,3-benzodiazepine
CA2880578A1 (en) * 2012-08-16 2014-02-20 Glaxosmithkline Llc Benzodiazepines for treating small cell lung cancer
EP2900672B1 (de) * 2012-09-28 2017-02-22 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische 5-aryl-triazolo-azepine
CN105073744B (zh) 2012-12-21 2019-11-08 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新型杂环化合物
AR094963A1 (es) 2013-03-04 2015-09-09 Ono Pharmaceutical Co Reacción de oxidación excelente en el índice de conversión
JP6401773B2 (ja) 2013-03-11 2018-10-10 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｂｅｔブロモドメイン阻害剤およびこれを用いる治療方法
US8980879B2 (en) * 2013-03-11 2015-03-17 Abbvie Inc. Bromodomain inhibitors
PE20151788A1 (es) * 2013-03-12 2015-12-20 Abbvie Inc Inhibidores de bromodominios tetraciclicos
WO2014159837A1 (en) * 2013-03-14 2014-10-02 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
ES2909778T3 (es) 2013-03-15 2022-05-10 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de proteína BET para su uso en el tratamiento de una enfermedad proliferativa en combinación con un inhibidor de Janus quinasas
EP2989096B1 (en) 2013-04-26 2019-04-10 BeiGene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
CN104146970A (zh) * 2013-05-05 2014-11-19 王元青 治疗精神疾病的冻干粉针剂
CN103202815B (zh) * 2013-05-05 2014-09-24 李友香 治疗精神疾病的注射剂
CN105473581B (zh) 2013-06-21 2019-04-23 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新取代的双环化合物
BR112015031073B1 (pt) 2013-06-21 2022-11-29 Zenith Epigenetics Ltd Compostos inibidores bicíclicos de bromodomínio e composição farmacêutica contendo os referidos compostos
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
JP2016531113A (ja) 2013-07-25 2016-10-06 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 転写因子の阻害剤およびその使用
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
RU2016122654A (ru) 2013-11-08 2017-12-14 Дана-Фарбер Кэнсер Инститьют, Инк. Комбинированная терапия злокачественной опухоли с использованием ингибиторов бромодоменового и экстратерминального (вет) белка
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
GB201320994D0 (en) * 2013-11-28 2014-01-15 Univ Dundee Enzyme function probes
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
RU2016134941A (ru) 2014-01-31 2018-03-01 Дана-Фарбер Кансер Институт, Инк. Производные диазепана и их применения
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
MX2016009974A (es) 2014-01-31 2016-10-31 Dana Farber Cancer Inst Inc Derivados de diaminopirimidina bencensulfona y sus usos.
US9694017B2 (en) 2014-02-10 2017-07-04 Concert Pharmaceuticals, Inc. Substituted triazolobenzodiazepines
CA2940472A1 (en) 2014-02-28 2015-09-03 Tensha Therapeutics, Inc. Treatment of conditions associated with hyperinsulinaemia
CA2940554A1 (en) 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
DK3129378T3 (da) * 2014-04-09 2019-10-07 Kainos Medicine Inc Bromdomæne-hæmmende forbindelser og farmaceutisk sammensætning omfattende disse til forebyggelse eller behandling af en cancer
EP3134403B1 (en) 2014-04-23 2020-02-12 Incyte Corporation 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
US20170121322A1 (en) * 2014-06-18 2017-05-04 Bayer Pharma Aktiengesellschaft Bet-protein inhibiting 3,4-dihydropyrido[2,3-b]pyrazinones with meta-substituted aromatic amino- or ether groups
DK3157928T3 (da) 2014-06-20 2019-05-20 Constellation Pharmaceuticals Inc Krystallinske former af 2-((4s)-6-(4-chlorphenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamid
EP3177147A4 (en) 2014-08-08 2018-01-24 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
WO2016022902A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
EP3194406B8 (en) 2014-09-15 2021-03-31 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
KR20170068597A (ko) 2014-10-27 2017-06-19 텐샤 세러퓨틱스 인코포레이티드 브로모도메인 저해제
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
EP3227281A4 (en) 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
EP3230277B1 (en) 2014-12-11 2019-09-18 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
WO2016097863A1 (en) 2014-12-17 2016-06-23 Zenith Epigenetics Corp. Inhibitors of bromodomains
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
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
WO2016161003A1 (en) 2015-03-31 2016-10-06 Enanta Phamraceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
WO2016171470A1 (en) * 2015-04-21 2016-10-27 Kainos Medicine, Inc. Bromodomain-inhibiting compounds and methods to prevent or treat a cancer
WO2016196065A1 (en) 2015-05-29 2016-12-08 Genentech, Inc. Methods and compositions for assessing responsiveness of cancers to bet inhibitors
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
MX2017016337A (es) 2015-06-26 2018-11-22 Tensha Therapeutics Inc Tratamiento de carcinoma de linea media nut.
JP6765622B2 (ja) 2015-07-17 2020-10-07 日本光電工業株式会社 救命支援装置
KR102667914B1 (ko) 2015-07-22 2024-05-21 이난타 파마슈티칼스, 인코포레이티드 Rsv 저해제로서의 벤조다이아제핀 유도체
MX2018003031A (es) 2015-09-11 2018-08-01 Dana Farber Cancer Inst Inc Ciano tienotriazolpirazinas y usos de las mismas.
EP3347020A4 (en) 2015-09-11 2019-08-14 Dana-Farber Cancer Institute, Inc. ACETAMIDE THIENOTRIAZOLDIAZEPINES AND USES THEREOF
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
US10913752B2 (en) 2015-11-25 2021-02-09 Dana-Farber Cancer Institute, Inc. Bivalent bromodomain inhibitors and uses thereof
CN106892924B (zh) * 2015-12-17 2021-01-08 四川科伦博泰生物医药股份有限公司 短效苯并二氮*衍生物、其制备方法及其用途
EP3402799B1 (en) 2016-01-15 2022-05-04 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as rsv inhibitors
CA3014644A1 (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
CA3020281A1 (en) 2016-04-06 2017-10-12 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
CN109415336B (zh) 2016-04-06 2023-08-29 密执安大学评议会 Mdm2蛋白质降解剂
SG11201808729WA (en) 2016-04-12 2018-11-29 Univ Michigan Regents Bet protein degraders
ES2793239T3 (es) 2016-04-15 2020-11-13 Abbvie Inc Inhibidores del bromodominio
WO2017189663A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10080742B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10080741B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
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
CN109715625B (zh) 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
CN107629057B (zh) * 2016-07-19 2020-03-27 上海勋和医药科技有限公司 Bet蛋白抑制剂及其应用
US10918647B2 (en) 2016-07-26 2021-02-16 University Of Southern California Selective bromodomain inhibition of fungal Bdf1
EP3512853B1 (en) 2016-09-13 2020-12-23 The Regents of The University of Michigan Fused 1,4-diazepines as bet protein degraders
US11466028B2 (en) 2016-09-13 2022-10-11 The Regents Of The University Of Michigan Fused 1,4-oxazepines as BET protein degraders
EP3523298A4 (en) 2016-10-04 2020-06-24 Enanta Pharmaceuticals, Inc. ISOXAZOLANALOGA AS FXR AGONISTS AND METHOD FOR USE THEREOF
WO2018081285A1 (en) 2016-10-26 2018-05-03 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as fxr agonists and methods of use thereof
EP3539960A4 (en) 2016-11-10 2020-03-18 Luoxin Pharmaceutical (Shanghai) Co., Ltd. NITROGEN MACROCYCLIC COMPOUND, ITS PREPARATION METHOD, ITS PHARMACEUTICAL COMPOSITION AND ITS APPLICATION
US10398706B2 (en) 2017-01-06 2019-09-03 Enanta Pharmaceuticals, Inc. Heteroaryldiazepine derivatives as RSV inhibitors
EP3577120A1 (en) 2017-02-03 2019-12-11 The Regents of The University of Michigan Fused 1,4-diazepines as bet bromodomain inhibitors
WO2018152413A1 (en) 2017-02-16 2018-08-23 Enanta Pharmaceuticals, Inc. Processes for the preparation of benzodiazepine derivatives
CN108727380A (zh) * 2017-04-13 2018-11-02 中国科学院上海药物研究所 一种brd4抑制剂及其制备和应用
CN110418791B (zh) * 2017-04-28 2022-07-01 四川科伦博泰生物医药股份有限公司 包含苯并二氮䓬类化合物的注射用组合物及其制备方法
CN108948018B (zh) * 2017-05-17 2021-03-30 四川科伦博泰生物医药股份有限公司 苯并二氮*衍生物及其盐和相关晶体形式、制备方法和用途
US10752598B2 (en) 2017-06-07 2020-08-25 Enanta Pharmaceuticals, Inc. Aryldiazepine derivatives as RSV inhibitors
US11091501B2 (en) 2017-06-30 2021-08-17 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
WO2019006291A1 (en) 2017-06-30 2019-01-03 Enanta Pharmaceuticals, Inc. HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
US11267822B2 (en) 2017-09-13 2022-03-08 The Regents Of The University Of Michigan BET bromodomain protein degraders with cleavable linkers
JP7417519B2 (ja) * 2017-09-22 2024-01-18 石薬集団中奇制薬技術（石家庄）有限公司 チエノジアゼピン誘導体とその応用
EP3687543B1 (en) 2017-09-29 2024-03-20 Enanta Pharmaceuticals, Inc. Combinations of pharmaceutical agents as rsv inhibitors
US10647711B2 (en) 2017-11-13 2020-05-12 Enanta Pharmaceuticals, Inc. Azepin-2-one derivatives as RSV inhibitors
KR102634720B1 (ko) 2017-11-13 2024-02-06 이난타 파마슈티칼스, 인코포레이티드 벤조디아제핀-2-온 및 벤조아제핀-2-온 유도체의 분할 방법
WO2019118571A1 (en) 2017-12-12 2019-06-20 Enanta Pharmaceuticals, Inc. Isoxazole analogs as fxr agonists and methods of use thereof
WO2019160813A1 (en) 2018-02-14 2019-08-22 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10975094B2 (en) 2018-04-11 2021-04-13 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
EP3936507A4 (en) * 2019-03-07 2022-11-23 Medshine Discovery Inc. COMPOUNDS WITH BOTH EFFECTS OF BET BROMOMAIN PROTEIN INHIBITION AND PD-L1 GENE REGULATION
MX2021011144A (es) 2019-03-18 2022-01-18 Enanta Pharm Inc Derivados de las benzodiazepinas como inhibidores del vsr.
WO2020210246A1 (en) 2019-04-09 2020-10-15 Enanta Pharmaceuticals, Inc, Heterocyclic compounds as rsv inhibitors
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds
US11555032B2 (en) 2019-05-13 2023-01-17 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US11505558B1 (en) 2019-10-04 2022-11-22 Enanta Pharmaceuticals, Inc. Antiviral heterocyclic compounds
KR20220101083A (ko) 2019-10-04 2022-07-19 이난타 파마슈티칼스, 인코포레이티드 항바이러스 헤테로사이클릭 화합물
PT116050B (pt) * 2020-01-09 2022-06-15 Hovione Farm S A Conjugados fármaco-ligando e inibidores das proteínas da família bromodomínio e domínio extraterminal -(bet) modificados
UY39032A (es) 2020-01-24 2021-07-30 Enanta Pharm Inc Compuestos heterocíclicos como agentes antivirales
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
AU2021297799A1 (en) 2020-06-23 2022-12-22 Genentech, Inc. Macrocyclic compounds and methods of use thereof
US11534439B2 (en) 2020-07-07 2022-12-27 Enanta Pharmaceuticals, Inc. Dihydroquinoxaline and dihydropyridopyrazine derivatives as RSV inhibitors
WO2022086840A1 (en) 2020-10-19 2022-04-28 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as anti-viral agents
GB202016977D0 (en) 2020-10-26 2020-12-09 In4Derm Ltd Compounds
CN112358483A (zh) * 2020-11-09 2021-02-12 中国药科大学 一类新型苯并二氮*类化合物、其制备方法及其用途
CN114456171A (zh) * 2020-11-09 2022-05-10 中国药科大学 一类用于镇静催眠的苯并二氮䓬类药物、其制备方法及应用
CA3173354A1 (en) 2021-02-26 2022-09-01 Adam SZYMANIAK A 2,3-dihydrofuro[2,3-c]pyridine-3-carboxamide compound and its antiviral use
CA3224302A1 (en) 2021-06-29 2023-01-05 Tay Therapeutics Limited Pyrrolopyridone derivatives useful in the treatment of cancer
AU2023255396A1 (en) 2022-04-19 2024-10-24 Nuevolution A/S Compounds active towards bromodomains
WO2024018423A1 (en) 2022-07-21 2024-01-25 Tay Therapeutics Limited Pyrroles and imidazoles as bet protein inhibitors

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1152066A (en) 1980-02-08 1983-08-16 Hoffmann-La Roche Limited Benzodiazepine derivatives
DE3610848A1 (de) * 1986-04-01 1987-10-15 Boehringer Ingelheim Kg Neue 1,4-diazepine
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
CA2120939A1 (en) 1991-10-11 1993-04-15 Tetsuya Tahara Therapeutic agent for osteoporosis and diazepine compound
JPH06128257A (ja) 1992-10-13 1994-05-10 Yoshitomi Pharmaceut Ind Ltd ピリドジアゼピン化合物
US5679672A (en) 1993-11-22 1997-10-21 Merck & Co., Inc. Benzodiazepines
CA2205173A1 (en) 1994-11-18 1996-05-30 Takeshi Nakamura Therapeutic agent for osteoporosis and triazepine compound
JP2622673B2 (ja) * 1994-11-18 1997-06-18 日本たばこ産業株式会社 骨粗鬆症治療薬およびトリアゼピン化合物
AU3106197A (en) 1996-06-12 1998-01-07 Japan Tobacco Inc. Cytokine production inhibitors, triazepine compounds, and intermediates there of
KR100338144B1 (ko) 1996-09-13 2002-05-24 가마쿠라 아키오 티에노트리아졸로디아제핀 화합물 및 그의 약제학적 용도
JPH11228576A (ja) * 1997-12-10 1999-08-24 Japan Tobacco Inc アポトーシス抑制剤
US6916995B2 (en) 2003-02-25 2005-07-12 Broadcom Corporation Optimization of routing layers and board space requirements for ball grid array package implementations including single and multi-layer routing
JP4641526B2 (ja) 2003-11-03 2011-03-02 グラクソ グループ リミテッド 流体分配デバイス
US7223733B2 (en) 2004-03-31 2007-05-29 National University Of Singapore Modulation of TRIP-Br function and method of treating proliferative disorders
GB0420970D0 (en) 2004-09-21 2004-10-20 Smithkline Beecham Corp Novel triazoloquinoline compounds
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
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Ｂｒｄ２ブロモドメイン結合剤
EP2239264A4 (en) 2007-12-28 2012-01-11 Mitsubishi Tanabe Pharma Corp ANTITUMOR AGENT
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
JP5524343B2 (ja) * 2009-11-05 2014-06-18 グラクソスミスクライン エルエルシー ベンゾジアゼピンブロモドメイン阻害剤
SI2496582T1 (sl) * 2009-11-05 2016-04-29 Glaxosmithkline Llc Corporation Service Company Benzodiazepinski inhibitor bromodomene
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2697393C2 (ru) * 2014-10-02 2019-08-14 ГлаксоСмитКлайн Интеллекчуал Проперти (N 2) Лимитед Кристаллическая твердая форма соли бензолсульфоновой кислоты и 2-[(4S)-6-(4-хлорфенил)-1-метил-8-(метилокси)-4H-[1,2,4]триазоло[4,3-a][1,4]бензодиазепин-4-ил]-N-этилацетамида, способ ее получения и фармацевтическая композиция, содержащая ее

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