CY1117424T1 - Βενζοδιαζεπινικος αναστολεας bromodomain - Google Patents

Βενζοδιαζεπινικος αναστολεας bromodomain

Info

Publication number
CY1117424T1
CY1117424T1 CY20161100231T CY161100231T CY1117424T1 CY 1117424 T1 CY1117424 T1 CY 1117424T1 CY 20161100231 T CY20161100231 T CY 20161100231T CY 161100231 T CY161100231 T CY 161100231T CY 1117424 T1 CY1117424 T1 CY 1117424T1
Authority
CY
Cyprus
Prior art keywords
bromodomain
benzodiazepinic
suspension
compounds
therapeutics
Prior art date
Application number
CY20161100231T
Other languages
Greek (el)
English (en)
Inventor
James Bailey
Romain Luc Marie Gosmini
Olivier Mirguet
Jason Witherington
Original Assignee
Glaxosmithkline Llc
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 GBGB1014231.3A external-priority patent/GB201014231D0/en
Application filed by Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Publication of CY1117424T1 publication Critical patent/CY1117424T1/el

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)
CY20161100231T 2009-11-05 2016-03-18 Βενζοδιαζεπινικος αναστολεας bromodomain CY1117424T1 (el)

Applications Claiming Priority (4)

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
GBGB1014231.3A GB201014231D0 (en) 2010-08-25 2010-08-25 Novel compounds
EP10773325.5A EP2496582B1 (en) 2009-11-05 2010-11-03 Benzodiazepine bromodomain inhibitor

Publications (1)

Publication Number Publication Date
CY1117424T1 true CY1117424T1 (el) 2017-04-26

Family

ID=43969589

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20161100231T CY1117424T1 (el) 2009-11-05 2016-03-18 Βενζοδιαζεπινικος αναστολεας bromodomain

Country Status (23)

Country Link
US (3) US9102677B2 (enExample)
EP (2) EP2496582B1 (enExample)
JP (3) JP5702396B2 (enExample)
KR (1) KR20120097508A (enExample)
CN (1) CN102781943B (enExample)
AU (1) AU2010317096B2 (enExample)
BR (1) BR112012010705A2 (enExample)
CA (1) CA2779423C (enExample)
CY (1) CY1117424T1 (enExample)
DK (1) DK2496582T3 (enExample)
EA (1) EA023441B1 (enExample)
ES (2) ES2654423T3 (enExample)
HK (1) HK1221221A1 (enExample)
HR (1) HRP20160253T1 (enExample)
HU (1) HUE026967T2 (enExample)
IL (2) IL219253A (enExample)
ME (1) ME02356B (enExample)
MX (1) MX341212B (enExample)
PL (1) PL2496582T3 (enExample)
RS (1) RS54645B1 (enExample)
SI (1) SI2496582T1 (enExample)
SM (1) SMT201600104B (enExample)
WO (1) WO2011054845A1 (enExample)

Families Citing this family (140)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602007009128D1 (de) 2006-07-10 2010-10-21 Paion Uk Ltd Benzodiazepinsalze mit kurzzeitwirkung und polymorphe formen davon
KR20120097508A (ko) * 2009-11-05 2012-09-04 글락소스미스클라인 엘엘씨 벤조디아제핀 브로모도메인 억제제
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
US8981083B2 (en) 2010-05-14 2015-03-17 Dana Farber Cancer Institute, Inc. Compositions and methods for treating neoplasia, inflammatory disease and other disorders
MX373121B (es) 2010-05-14 2020-04-30 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
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
WO2012151512A2 (en) 2011-05-04 2012-11-08 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
CA2870931A1 (en) 2012-04-20 2013-10-24 Abbvie Inc. Isoindolone derivatives
GEAP201813666A (en) * 2012-05-22 2018-01-25 Paion Uk Ltd Compositions comprising short-acting benzodiazepines
US9624244B2 (en) 2012-06-06 2017-04-18 Constellation Pharmaceuticals, Inc. Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
AU2012382373A1 (en) 2012-06-12 2014-12-11 Abbvie Inc. Pyridinone and pyridazinone derivatives
CN104582708A (zh) * 2012-08-16 2015-04-29 葛兰素史克有限责任公司 用于治疗小细胞肺癌的苯并二氮*类
CA2881996A1 (en) 2012-08-16 2014-02-20 Bayer Pharma Aktiengesellschaft 2,3-benzodiazepines
EP2900672B1 (de) 2012-09-28 2017-02-22 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische 5-aryl-triazolo-azepine
WO2014096965A2 (en) 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors
AR094963A1 (es) 2013-03-04 2015-09-09 Ono Pharmaceutical Co Reacción de oxidación excelente en el índice de conversión
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
MX2015012158A (es) * 2013-03-11 2015-12-01 Abbvie Inc Inhibidores de bomodominio tetraciclicos fusionados.
WO2014139324A1 (en) * 2013-03-12 2014-09-18 Abbvie Inc. Tetracyclic bromodomain inhibitors
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
US9714946B2 (en) 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
CA2901083A1 (en) 2013-04-26 2014-10-30 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
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
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
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
KR20160072261A (ko) 2013-11-08 2016-06-22 다나-파버 캔서 인스티튜트 인크. 브로모도메인 및 엑스트라-말단 (bet) 단백질 저해제를 이용한 암 치료를 위한 조합 요법
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
KR20160111036A (ko) 2014-01-31 2016-09-23 다나-파버 캔서 인스티튜트 인크. 디아제판 유도체 및 그의 용도
MX2016009974A (es) 2014-01-31 2016-10-31 Dana Farber Cancer Inst Inc Derivados de diaminopirimidina bencensulfona y sus usos.
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
JP6526060B2 (ja) 2014-02-10 2019-06-05 コンサート ファーマシューティカルズ インコーポレイテッド 置換トリアゾロベンゾジアゼピン
US9580430B2 (en) 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
RU2722179C2 (ru) 2014-02-28 2020-05-28 Тэнша Терапеутикс, Инк. Лечение состояний, ассоциированных с гиперинсулинемией
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
UA119870C2 (uk) 2014-04-23 2019-08-27 Інсайт Корпорейшн 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET
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
CN106687463B (zh) 2014-06-20 2019-04-09 星座制药公司 一种乙酰胺类化合物的晶型
WO2016022970A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
EP3177626A4 (en) 2014-08-08 2017-12-27 Dana Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
BR112017006342A2 (pt) 2014-10-02 2017-12-19 Glaxosmithkline Ip No 2 Ltd composto de sal de ácido benzenossulfônico, forma em estado sólido cristalino, composição farmacêutica, produto farmacêutico de combinação, método de tratamento de doenças ou condições, uso de um composto de sal de ácido benzenossulfônico, e, processo para preparação de um composto de sal de ácido benzenossulfônico.
UA122130C2 (uk) 2014-10-27 2020-09-25 Тенша Терапеутікс, Інк. Інгібітори бромодомену
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
EP3227280B1 (en) 2014-12-01 2019-04-24 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
HK1245247A1 (zh) 2014-12-17 2018-08-24 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
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
SI3277286T1 (sl) 2015-03-31 2021-09-30 Enanta Pharmaceuticals, Inc. Derivati žolčne kisline kot antagonisti FXR/TGR5 in metode za njihovo uporabo
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
US10702527B2 (en) 2015-06-12 2020-07-07 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
AU2016283020A1 (en) 2015-06-26 2018-01-04 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
AU2016297024B2 (en) 2015-07-22 2021-03-04 Enanta Pharmaceuticals, Inc. Benzodiazepine derivatives as RSV inhibitors
US11306105B2 (en) 2015-09-11 2022-04-19 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof
JP2018526424A (ja) 2015-09-11 2018-09-13 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド アセトアミドチエノトリアゾロジアゼピンおよびこれらの使用
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
CR20180336A (es) 2015-11-25 2018-08-06 Dana Farber Cancer Inst Inc Inhibidores de bromodominio bivalentes y usos de los mismos
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
ES2882066T3 (es) 2016-02-15 2021-12-01 Univ Michigan Regents 1,4-oxazepinas fusionadas y análogos relacionados como inhibidores de bromodominio BET
CN113788818A (zh) 2016-04-06 2021-12-14 密执安大学评议会 Mdm2蛋白质降解剂
AU2017246453A1 (en) 2016-04-06 2018-11-08 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
BR112018070859A2 (pt) 2016-04-12 2019-02-05 Univ Michigan Regents degradantes da proteína de bet
RS60302B1 (sr) 2016-04-15 2020-07-31 Abbvie Inc Inhibitori bromodomena
US10080742B2 (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
WO2017189652A1 (en) 2016-04-26 2017-11-02 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
AU2017281286B2 (en) 2016-06-20 2021-05-20 Incyte Corporation Crystalline solid forms of a bet inhibitor
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
US10975093B2 (en) 2016-09-13 2021-04-13 The Regents Of The University Of Michigan Fused 1,4-diazepines as BET protein degraders
CN110062759B (zh) 2016-09-13 2022-05-24 密执安大学评议会 作为bet蛋白降解剂的稠合的1,4-氧氮杂䓬
EP3523298A4 (en) 2016-10-04 2020-06-24 Enanta Pharmaceuticals, Inc. ISOXAZOLANALOGA AS FXR AGONISTS AND METHOD FOR USE THEREOF
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
WO2018144789A1 (en) 2017-02-03 2018-08-09 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet bromodomain inhibitors
AU2018221820B2 (en) 2017-02-16 2023-11-02 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
WO2018226801A1 (en) 2017-06-07 2018-12-13 Enanta Pharmaceuticals, Inc. Aryldiazepine derivatives as rsv inhibitors
WO2019006291A1 (en) 2017-06-30 2019-01-03 Enanta Pharmaceuticals, Inc. HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
WO2019006295A1 (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
WO2019067864A1 (en) 2017-09-29 2019-04-04 Enanta Pharmaceuticals, Inc. PHARMACEUTICAL AGENTS IN COMBINATION AS INHIBITORS OF RSV
WO2019094920A1 (en) 2017-11-13 2019-05-16 Enanta Pharmaceuticals, Inc. Azepin-2-one derivatives as rsv inhibitors
MX394621B (es) 2017-11-13 2025-03-24 Enanta Pharm Inc Procesos para la resolucion de los derivados de la benzodiazepina-2-ona y de la benzoazepin-2-ona
US10689391B2 (en) 2017-12-12 2020-06-23 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
EP4342543A3 (en) 2018-09-11 2024-06-19 F. Hoffmann-La Roche AG Tert-butyl (s)-2-(4-(phenyl)-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a] [1,4]diazepin-6-yl) acetate derivatives and related compounds as bromodomain brd4 inhibitors for treating cancer
US20220177490A1 (en) * 2019-03-07 2022-06-09 Medshine Discovery Inc. Compounds having both effects of bet bromodomain protein inhibition and pd-l1 gene regulation
JP7558189B2 (ja) 2019-03-18 2024-09-30 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 Ｒｓｖ阻害剤としてのベンゾジアゼピン誘導体
US11179400B2 (en) 2019-04-09 2021-11-23 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
CA3153297A1 (en) 2019-10-04 2021-04-08 Adam SZYMANIAK Antiviral heterocyclic compounds
US11505558B1 (en) 2019-10-04 2022-11-22 Enanta Pharmaceuticals, Inc. Antiviral heterocyclic compounds
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
KR20230026461A (ko) 2020-06-23 2023-02-24 제넨테크, 인크. 거대고리 화합물 및 이의 사용 방법
US11534439B2 (en) 2020-07-07 2022-12-27 Enanta Pharmaceuticals, Inc. Dihydroquinoxaline and dihydropyridopyrazine derivatives as RSV inhibitors
US11945824B2 (en) 2020-10-19 2024-04-02 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as anti-viral agents
GB202016977D0 (en) 2020-10-26 2020-12-09 In4Derm Ltd Compounds
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
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
WO2022182861A1 (en) 2021-02-26 2022-09-01 Enanta Pharmaceuticals, Inc. Antiviral heterocyclic compounds
US20240308998A1 (en) 2021-06-29 2024-09-19 Tay Therapeutics Limited Pyrrolopyridone derivatives useful in the treatment of cancer
AR129003A1 (es) 2022-04-07 2024-07-03 Enanta Pharm Inc Compuestos heterocíclicos antivirales
CN119365455A (zh) 2022-04-19 2025-01-24 纽韦卢森公司 对溴结构域有活性的化合物
WO2023211997A1 (en) 2022-04-27 2023-11-02 Enanta Pharmaceuticals, Inc. Antiviral compounds
EP4558224A1 (en) 2022-07-21 2025-05-28 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
JP2840454B2 (ja) 1993-11-22 1998-12-24 メルク エンド カンパニー インコーポレーテッド ベンゾジアゼピン類
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
AU694278B2 (en) * 1994-11-18 1998-07-16 Japan Tobacco Inc. Osteoporosis remedy and triazepine compound
CN1227555A (zh) * 1996-06-12 1999-09-01 日本烟草产业株式会社 细胞因子生成抑制剂、三氮䓬化合物及其中间体
PT989131E (pt) 1996-09-13 2003-03-31 Mitsubishi Pharma Corp Compostos de trienotriazolodiazepina e suas utilizacoes com fins medicinais
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
PL1699512T3 (pl) 2003-11-03 2012-11-30 Glaxo Group Ltd Urządzenie do dozowania płynów
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
EP1887008B1 (en) 2005-05-30 2021-04-21 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and a medicinal use thereof
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 ANTITUMORAL MEDIUM
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
MY160456A (en) 2009-11-05 2017-03-15 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
KR20120097508A (ko) * 2009-11-05 2012-09-04 글락소스미스클라인 엘엘씨 벤조디아제핀 브로모도메인 억제제

Also Published As

Publication number Publication date
AU2010317096B2 (en) 2015-03-26
EP3050885A1 (en) 2016-08-03
JP2013510123A (ja) 2013-03-21
ES2564318T3 (es) 2016-03-21
JP5702396B2 (ja) 2015-04-15
US20120252781A1 (en) 2012-10-04
HRP20160253T1 (hr) 2016-04-08
JP2015143232A (ja) 2015-08-06
EA201290184A1 (ru) 2012-12-28
HUE026967T2 (en) 2016-07-28
AU2010317096A1 (en) 2012-05-31
SMT201600104B (it) 2016-04-29
US9598420B2 (en) 2017-03-21
DK2496582T3 (en) 2016-03-21
RS54645B1 (sr) 2016-08-31
JP2017039738A (ja) 2017-02-23
US20150299210A1 (en) 2015-10-22
KR20120097508A (ko) 2012-09-04
CN102781943A (zh) 2012-11-14
EP2496582B1 (en) 2016-01-27
EP3050885B1 (en) 2017-10-18
WO2011054845A1 (en) 2011-05-12
IL219253A (en) 2015-11-30
CN102781943B (zh) 2016-10-05
MX341212B (es) 2016-08-11
IL239625A0 (en) 2015-08-31
MX2012005296A (es) 2012-06-19
SI2496582T1 (sl) 2016-04-29
HK1221221A1 (en) 2017-05-26
ME02356B (me) 2016-06-20
BR112012010705A2 (pt) 2016-03-29
IL219253A0 (en) 2012-06-28
PL2496582T3 (pl) 2016-08-31
ES2654423T3 (es) 2018-02-13
EP2496582A1 (en) 2012-09-12
CA2779423C (en) 2018-08-14
EA023441B1 (ru) 2016-06-30
US9102677B2 (en) 2015-08-11
US20170145021A1 (en) 2017-05-25
CA2779423A1 (en) 2011-05-12
IL239625B (en) 2018-05-31

Similar Documents

Publication Publication Date Title
CY1117424T1 (el) Βενζοδιαζεπινικος αναστολεας bromodomain
CY1124928T1 (el) Αναστολεις πυραζολυλο κινοξαλινο κινασης
CY1124068T1 (el) Στερεες μορφες ενος εκλεκτικου αναστολεα cdk4/6
CY1122266T1 (el) Ενωσεις 3-αμινοκυκλοαλκυλιου ως ror-gamma-t αναστολεις και χρησεις αυτων
CY1124000T1 (el) Υποκατεστημενες 5-φθορο-1η-πυραζολοπυριδινες σε κρυσταλλικη μορφη
CY1120031T1 (el) Αποπτωτικοι υποκινητες ν-ακυλοσουλφοναμιδης
BR112015022861A2 (pt) inibidores de bromodomínio
CY1117143T1 (el) Νεα καρβονυλιωμενα (αζα)κυκλοεξανια ως προσδετες του d3 υποδοχεα ντοπαμινης
CY1121150T1 (el) Νευροδραστικα 19-αλκοξυ-17-υποκατεστημενα στεροειδη, χρησιμα σε μεθοδους θεραπειας
CY1118156T1 (el) Ενωσεις αντιστροφης αμιδης ως αναστολεις δεακετυλασης πρωτεϊνων και μεθοδοι χρησης αυτων
CY1114988T1 (el) Βενζοδιαζεπινη αναστολεας bromodomain
EA201300684A1 (ru) Производные 6-амино-2-фениламино-1н-бензимидазол-5-карбоксамида и их применение в качестве ингибиторов микросомной простагландин-е2-синтазы-1
CY1117962T1 (el) Υδροχλωρικο αλας 4-[2-[[5-μεθυλο-1-(2- ναφθαλενυλο)-1η- πυραζολ-3-υλ]οξυ]αιθυλο] μορφολινης
CL2011000589A1 (es) Compuestos derivados de pirrolidin-2-carboxamida, inhibidores de la interaccion p53-mdm2; composicion farmaceutica que los comprende; y su uso en la preparacion de medicamentos utiles para el tratamiento del cancer.
BR112015022674A2 (pt) inibidores de bromodomínio
CY1119123T1 (el) Δις-αρυλοσυζευγμενες αρυλοτριαζολονες και η χρηση τους
CY1109656T1 (el) Υποκατεστημενα παραγωγα μορφολινης και θειομορφολινης
UA110612C2 (uk) Похідні 1-аміно-2-циклопропілетилборонової кислоти
EA201270730A1 (ru) ИНГИБИТОРЫ КИНАЗЫ Cdc7 И ИХ ПРИМЕНЕНИЕ
EA201200049A1 (ru) 1,3-дизамещенные производные имидазолидин-2-она в качестве ингибиторов cyp 17
EA201390908A1 (ru) Производные бицикло[3.2.1]октиламида и их применение
UA109010C2 (en) Morpholino pyrividines and their use in therapy
CY1111454T1 (el) Παραγωγα φαινυλο-πυραζολιου ως συνδετες υποδοχεα μη στεροειδων γλυκοκορτικοειδων
CY1112558T1 (el) Ενωσεις ν-μεθυλαμινομεθυλο ισοϊνδολης και συνθεσεις που τις περιλαμβανουν και μεθοδοι χρησης τους
CY1119730T1 (el) Παραγωγα καρβοξυλικου οξεος πυρρολιδινης ως αγωνιστες του συζευγμενου με πρωτεϊνή-g υποδοχεα 43 (gpr43), φαρμακευτικη συνθεση και μεθοδοι για χρηση στην αντιμετωπιση μεταβολικων διαταραχων