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

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) EP2496582B1 (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
EP2081921B1 (en) 2006-07-10 2010-09-08 PAION UK Limited Short-acting benzodiazepine salts and their polymorphic forms
EP2496582B1 (en) * 2009-11-05 2016-01-27 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
BR112012029005A2 (pt) 2010-05-14 2016-07-26 Dana Farber Cancer Inst Inc composições e métodos de tratamento de neoplasia, doença inflamatória e outros distúrbios
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
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
EP2450039A1 (en) 2010-11-08 2012-05-09 PAION UK Ltd. Dosing regimen for sedation with CNS 7056 (Remimazolam)
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
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
WO2013033268A2 (en) * 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, 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
JP5989229B2 (ja) 2012-04-20 2016-09-07 アッヴィ・インコーポレイテッド イソインドロン誘導体
RS56660B1 (sr) * 2012-05-22 2018-03-30 Paion Uk Ltd Kompozicije koje sadrže benzodiazepine kratkotrajnog dejstva
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
US9624244B2 (en) 2012-06-06 2017-04-18 Constellation Pharmaceuticals, Inc. Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof
CN104718201A (zh) 2012-06-12 2015-06-17 艾伯维公司 吡啶酮和哒嗪酮衍生物
EA201590356A1 (ru) 2012-08-16 2015-07-30 Байер Фарма Акциенгезельшафт 2,3-бензодиазепины
JP2015524847A (ja) 2012-08-16 2015-08-27 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ 小細胞肺がんを治療するためのベンゾジアゼピン
JP6276277B2 (ja) * 2012-09-28 2018-02-07 バイエル ファーマ アクチエンゲゼルシャフト Ｂｅｔタンパク質阻害性の５−アリールトリアゾロアゼピン
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
EP2970285B1 (en) * 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
US9675697B2 (en) 2013-03-11 2017-06-13 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
CN108440528A (zh) * 2013-03-12 2018-08-24 艾伯维公司 四环布罗莫结构域抑制剂
CN105407894A (zh) * 2013-03-14 2016-03-16 康威基内有限公司 用于抑制含布罗莫结构域的蛋白质的方法和组合物
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
KR102355670B1 (ko) 2013-03-15 2022-02-08 인사이트 홀딩스 코포레이션 Bet 단백질 저해제로서의 삼환식 복소환
MX366623B (es) 2013-04-26 2019-07-16 Beigene Ltd 5-(3,5-dimetilisoxazol-4-il)indolina-2-onas sustituidas.
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
JP6461121B2 (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． 新規の二環式ブロモドメイン阻害剤
ES2661437T3 (es) 2013-06-21 2018-04-02 Zenith Epigenetics Corp. Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
US9975896B2 (en) 2013-07-25 2018-05-22 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
CA2929652A1 (en) 2013-11-08 2015-05-14 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015081203A1 (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
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
JP2017504653A (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 ジアミノピリミジンベンゼンスルホン誘導体およびその使用
US9695172B2 (en) 2014-01-31 2017-07-04 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
WO2015120393A1 (en) 2014-02-10 2015-08-13 Concert Pharmaceuticals, Inc. Substituted triazolobenzodiazepines
AU2015222887B2 (en) 2014-02-28 2019-06-27 The Regents Of The University Of Michigan 9H-pyrimido[4,5-b]indoles and related analogs as BET bromodomain inhibitors
US10925881B2 (en) 2014-02-28 2021-02-23 Tensha Therapeutics, Inc. Treatment of conditions associated with hyperinsulinaemia
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
ME03763B (me) 2014-04-23 2021-04-20 Incyte Corp 1h-pirrolo[2,3-c]piridin-7(6h)-oni i pirazolo[3,4-c]piridin-7(6h)-oni kao inhibitori bet proteina
CA2952526A1 (en) * 2014-06-18 2015-12-23 Bayer Pharma Aktiengesellschaft Bet-protein inhibiting 3,4-dihydropyrido[2,3-b]pyrazinones with meta-substituted aromatic amino- or ether groups
US9969747B2 (en) 2014-06-20 2018-05-15 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
RU2017104898A (ru) 2014-08-08 2018-09-10 Дана-Фарбер Кэнсер Инститьют, Инк. Дигидроптеридиноновые производные и их применения
EP3194406B8 (en) 2014-09-15 2021-03-31 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
SG11201703414VA (en) 2014-10-27 2017-05-30 Tensha Therapeutics Inc Bromodomain inhibitors
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
JP2017537946A (ja) 2014-12-11 2017-12-21 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置換複素環
WO2016097863A1 (en) 2014-12-17 2016-06-23 Zenith Epigenetics Corp. Inhibitors of bromodomains
US10307407B2 (en) 2015-02-27 2019-06-04 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
JP6785788B2 (ja) 2015-03-31 2020-11-18 エナンタ ファーマシューティカルズ インコーポレイテッド Ｆｘｒ／ｔｇｒ５アゴニストとしての胆汁酸誘導体およびその使用方法
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
CA2986441A1 (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
WO2016210275A1 (en) 2015-06-26 2016-12-29 Tensha Therapeutics, Inc. Treatment of nut midline carcinoma
JP6765622B2 (ja) 2015-07-17 2020-10-07 日本光電工業株式会社 救命支援装置
RU2738232C2 (ru) 2015-07-22 2020-12-09 Энанта Фармасьютикалс, Инк. Производные бензодиазепина как ингибиторы rsv
RU2018112953A (ru) 2015-09-11 2019-10-14 Дана-Фарбер Кэнсер Инститьют, Инк. Ацетамидтиенотриазолодиазепины и пути их применения
SG10202007090UA (en) 2015-09-11 2020-08-28 Dana Farber Cancer Inst Inc Cyano thienotriazolodiazepines and uses thereof
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
KR20180081809A (ko) 2015-11-25 2018-07-17 다나-파버 캔서 인스티튜트 인크. 2가 브로모도메인 억제제 및 그의 용도
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
CN108699077B (zh) 2016-01-15 2021-03-02 英安塔制药有限公司 作为rsv抑制剂的杂环化合物
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
WO2017176958A1 (en) 2016-04-06 2017-10-12 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
KR102387316B1 (ko) 2016-04-06 2022-04-15 더 리젠츠 오브 더 유니버시티 오브 미시간 Mdm2 단백질 분해제
KR20180132861A (ko) 2016-04-12 2018-12-12 더 리젠츠 오브 더 유니버시티 오브 미시간 Bet 단백질 분해제
DK3442972T3 (da) 2016-04-15 2020-04-27 Abbvie Inc Bromdomænehæmmere
US10080741B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
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
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
PE20190623A1 (es) 2016-06-20 2019-04-26 Incyte Corp Formas solidas cristalinas de un inhibidor de bet
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
EP3490552B1 (en) 2016-07-26 2022-11-23 University of Southern California Selective bromodomain inhibition of fungal bdf1
WO2018052945A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
JP7035027B2 (ja) 2016-09-13 2022-03-14 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｂｅｔタンパク質分解物質としての縮合１，４－ジアゼピン
JP2019537557A (ja) 2016-10-04 2019-12-26 エナンタ ファーマシューティカルズ インコーポレイテッド Ｆｘｒアゴニストとしてのイソキサゾール類似体およびその使用方法
US10597391B2 (en) 2016-10-26 2020-03-24 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof
JP2019534306A (ja) 2016-11-10 2019-11-28 羅欣薬業（上海）有限公司Ｌｕｏｘｉｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ（Ｓｈａｎｇｈａｉ） Ｃｏ．， Ｌｔｄ． 窒素含有大員環系化合物、その製造方法、薬物組成物および使用
WO2018129287A1 (en) * 2017-01-06 2018-07-12 Enanta Pharmaceuticals, Inc. Heteroaryldiazepine derivatives as rsv inhibitors
US11046709B2 (en) 2017-02-03 2021-06-29 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
WO2019055444A1 (en) 2017-09-13 2019-03-21 The Regents Of The University Of Michigan DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS
US11312726B2 (en) * 2017-09-22 2022-04-26 Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. Thienodiazepine derivatives and application thereof
CN111386118B (zh) 2017-09-29 2023-05-09 英安塔制药有限公司 作为rsv抑制剂的组合药物剂
US10647711B2 (en) 2017-11-13 2020-05-12 Enanta Pharmaceuticals, Inc. Azepin-2-one derivatives as RSV inhibitors
MX2020004917A (es) 2017-11-13 2020-08-06 Enanta Pharm Inc Procesos para la resolucion de los derivados de la benzodiazepina-2-ona y de la benzoazepin-2-ona.
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
WO2019199908A1 (en) 2018-04-11 2019-10-17 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as rsv inhibitors
CN113631559B (zh) * 2019-03-07 2023-05-23 南京明德新药研发有限公司 同时具有BET Bromodomain蛋白抑制和PD-L1基因调控作用的化合物
SG11202110137VA (en) 2019-03-18 2021-10-28 Enanta Pharm Inc Benzodiazepine derivatives as rsv inhibitors
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
WO2020231917A1 (en) 2019-05-13 2020-11-19 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
AR122707A1 (es) 2020-06-23 2022-09-28 Genentech Inc Compuestos macrocíclicos y métodos de uso de los mismos
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
KR20230161976A (ko) 2021-02-26 2023-11-28 이난타 파마슈티칼스, 인코포레이티드 항바이러스성 헤테로사이클릭 화합물
IL309651A (en) 2021-06-29 2024-02-01 Tay Therapeutics Ltd History Pyrolopyridone is useful in the treatment of cancer
WO2023205251A1 (en) 2022-04-19 2023-10-26 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
US5593988A (en) 1991-10-11 1997-01-14 Yoshitomi Pharmaceutical Industries, Ltd. 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
AU686715B2 (en) 1993-11-22 1998-02-12 Merck & Co., Inc. Tricyclic benzodiazepinyl amide derivatives as amtiarrhythmics
US5807850A (en) 1994-11-18 1998-09-15 Japan Tobacco, Inc. 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
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.
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
PT1699512E (pt) 2003-11-03 2012-09-11 Glaxo Group Ltd Dispositivo distribuidor de fluido
CN1739788A (zh) 2004-03-31 2006-03-01 新加坡国立大学 Trip－br功能的调节和治疗增殖性紊乱的方法
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
JP5478262B2 (ja) 2007-12-28 2014-04-23 田辺三菱製薬株式会社 抗癌剤
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP2496582B1 (en) * 2009-11-05 2016-01-27 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
ES2652304T3 (es) 2009-11-05 2018-02-01 Glaxosmithkline Llc Compuesto de benzodiacepina novedoso

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

Also Published As

Publication number Publication date
BR112012010705A2 (pt) 2016-03-29
ES2654423T3 (es) 2018-02-13
AU2010317096B2 (en) 2015-03-26
EP2496582B1 (en) 2016-01-27
EP3050885B1 (en) 2017-10-18
SI2496582T1 (sl) 2016-04-29
US20120252781A1 (en) 2012-10-04
MX2012005296A (es) 2012-06-19
US9598420B2 (en) 2017-03-21
ME02356B (me) 2016-06-20
EP3050885A1 (en) 2016-08-03
JP5702396B2 (ja) 2015-04-15
HUE026967T2 (en) 2016-07-28
ES2564318T3 (es) 2016-03-21
IL239625B (en) 2018-05-31
RS54645B1 (en) 2016-08-31
CA2779423A1 (en) 2011-05-12
JP2015143232A (ja) 2015-08-06
JP2017039738A (ja) 2017-02-23
HRP20160253T1 (hr) 2016-04-08
CA2779423C (en) 2018-08-14
AU2010317096A1 (en) 2012-05-31
IL219253A0 (en) 2012-06-28
KR20120097508A (ko) 2012-09-04
CN102781943A (zh) 2012-11-14
US20170145021A1 (en) 2017-05-25
IL239625A0 (en) 2015-08-31
JP2013510123A (ja) 2013-03-21
HK1221221A1 (zh) 2017-05-26
DK2496582T3 (en) 2016-03-21
US9102677B2 (en) 2015-08-11
SMT201600104B (it) 2016-04-29
CN102781943B (zh) 2016-10-05
PL2496582T3 (pl) 2016-08-31
IL219253A (en) 2015-11-30
CY1117424T1 (el) 2017-04-26
WO2011054845A1 (en) 2011-05-12
EA023441B1 (ru) 2016-06-30
US20150299210A1 (en) 2015-10-22
EP2496582A1 (en) 2012-09-12
MX341212B (es) 2016-08-11

Similar Documents

Publication Publication Date Title
EA201290184A1 (ru) Бензодиазепиновый ингибитор бромодомена
EA201290183A1 (ru) Бензодиазепиновый ингибитор бромодомена
EA201300684A1 (ru) Производные 6-амино-2-фениламино-1н-бензимидазол-5-карбоксамида и их применение в качестве ингибиторов микросомной простагландин-е2-синтазы-1
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
EA201170508A1 (ru) Производные 1-амино-2-циклобутилэтилбороновой кислоты
EA201500278A1 (ru) Пиразолилхиназолиновые ингибиторы киназы
EA201270666A1 (ru) Соединения и фармацевтические композиции для снижения уровня мочевой кислоты
EA201101583A1 (ru) Ингибиторы pi3 киназы или mtor
EA201170531A1 (ru) Соединения на основе пиридина и пиримидина в качестве ингибиторов сигнального пути wnt для лечения рака
UA109010C2 (en) MORPHOLINOPYRIMIDINES AND THEIR APPLICATIONS IN THERAPY
EA201390772A1 (ru) Новые соли и полиморфные формы афатиниба
EA201391720A1 (ru) Замещенные диоксопиперидинилфталимидные производные
EA201390803A1 (ru) Ингибиторы бромодомена и их применение
EA201070247A1 (ru) Ингибиторы протеасом
EA201190217A1 (ru) Замещенные 2-ацетамидо-5-арил-1,2,4-триазолоны и их применение
EA201100030A1 (ru) Пиразольные соединения 436
EA201101192A1 (ru) Фармацевтическая композиция, включающая производные глюкопиранозилдифенилметана, фармацевтическая дозированная форма, содержащая указанные производные, способ их получения и применения для улучшения гликемического контроля у пациентов
EA201170832A1 (ru) Пуриновые соединения
EA201100391A1 (ru) Соединения, ингибирующие активность семикарбазид-чувствительной аминооксидазы
EA200801997A1 (ru) Новые соединения
EA201070327A1 (ru) Катехоламиновые производные и их пролекарства
JO3007B1 (ar) مركبات و تركيبات كمثبطات كيناز بروتين
EA201101435A1 (ru) Имидазотиадиазолы для применения в качестве ингибиторов киназ
EA201291099A1 (ru) Новые иммуномодуляторные и противовоспалительные соединения
EA201101533A1 (ru) Гетероциклические соединения в качестве ингибиторов mek

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM