[go: up one dir, main page]

EA201390803A1 - Ингибиторы бромодомена и их применение - Google Patents

Ингибиторы бромодомена и их применение

Info

Publication number
EA201390803A1
EA201390803A1 EA201390803A EA201390803A EA201390803A1 EA 201390803 A1 EA201390803 A1 EA 201390803A1 EA 201390803 A EA201390803 A EA 201390803A EA 201390803 A EA201390803 A EA 201390803A EA 201390803 A1 EA201390803 A1 EA 201390803A1
Authority
EA
Eurasian Patent Office
Prior art keywords
bromodomain inhibitors
compounds
inhibitors
compositions
bromodomens
Prior art date
Application number
EA201390803A
Other languages
English (en)
Other versions
EA022645B1 (ru
Inventor
Брайан К. Албрехт
Джеймс Эдмунд Аудиа
Александре Коте
Виктор С. Гейлинг
Жан-кристоф Харманж
Майкл С. Хьюит
Ив Леблан
Кристофер Г. Навесчук
Александер М. Тейлор
Риши Г. Васуани
Original Assignee
Констеллейшен Фармасьютикалс, Инк.
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 Констеллейшен Фармасьютикалс, Инк. filed Critical Констеллейшен Фармасьютикалс, Инк.
Publication of EA201390803A1 publication Critical patent/EA201390803A1/ru
Publication of EA022645B1 publication Critical patent/EA022645B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4702—Regulators; Modulating activity

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Zoology (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Изобретение относится к соединениям, применимым в качестве ингибиторов бромодоменсодержащих белков. В изобретении представлены также фармацевтически приемлемые композиции, включающие соединения по изобретению, и способы применения этих композиций при лечении различных расстройств.
EA201390803A 2010-12-02 2011-12-02 Ингибиторы бромодомена и их применение EA022645B1 (ru)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US41911910P 2010-12-02 2010-12-02
US201161451332P 2011-03-10 2011-03-10
US201161482473P 2011-05-04 2011-05-04
US201161540725P 2011-09-29 2011-09-29
US201161540788P 2011-09-29 2011-09-29
PCT/US2011/063046 WO2012075383A2 (en) 2010-12-02 2011-12-02 Bromodomain inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
EA201390803A1 true EA201390803A1 (ru) 2013-09-30
EA022645B1 EA022645B1 (ru) 2016-02-29

Family

ID=46235164

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201390803A EA022645B1 (ru) 2010-12-02 2011-12-02 Ингибиторы бромодомена и их применение

Country Status (26)

Country Link
US (2) US8796261B2 (ru)
EP (1) EP2646446B1 (ru)
JP (1) JP5850944B2 (ru)
KR (1) KR101871013B1 (ru)
CN (1) CN103415525B (ru)
AR (1) AR084070A1 (ru)
AU (1) AU2011336417B2 (ru)
BR (1) BR112013013167B1 (ru)
CA (1) CA2818187C (ru)
CY (1) CY1116578T1 (ru)
DK (1) DK2646446T3 (ru)
EA (1) EA022645B1 (ru)
ES (1) ES2545117T3 (ru)
HR (1) HRP20150858T1 (ru)
HU (1) HUE025321T2 (ru)
IL (1) IL226331A (ru)
MX (1) MX2013006214A (ru)
NZ (1) NZ611964A (ru)
PL (1) PL2646446T3 (ru)
PT (1) PT2646446E (ru)
RS (1) RS54175B1 (ru)
SG (1) SG190739A1 (ru)
SI (1) SI2646446T1 (ru)
TW (1) TWI572607B (ru)
WO (1) WO2012075383A2 (ru)
ZA (1) ZA201303776B (ru)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11458123B2 (en) 2016-11-01 2022-10-04 Arvinas Operations, Inc. Tau-protein targeting PROTACs and associated methods of use
RU2805523C2 (ru) * 2016-11-01 2023-10-18 Эрвинэс, Инк. Protac, целенаправленно воздействующие на тау-белок, и связанные с ними способы применения
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated

Families Citing this family (147)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101444489B1 (ko) 2007-02-01 2014-09-24 리스버로직스 코퍼레이션 심혈관 질환을 예방 및 치료하기 위한 화합물
KR101841003B1 (ko) 2009-03-18 2018-03-22 리스버로직스 코퍼레이션 신규한 소염제
CA2799420C (en) 2010-05-14 2018-10-02 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating neoplasia, inflammatory disease and other disorders
CA2799381A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Male contraceptive compositions and methods of use
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
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
US8912221B2 (en) * 2010-12-27 2014-12-16 Hoffmann-La Roche Inc. Biaryl amide derivatives
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
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
US9610251B2 (en) 2011-11-01 2017-04-04 Resverlogix Corp. Pharmaceutical compositions for substituted quinazolinones
WO2013106643A2 (en) 2012-01-12 2013-07-18 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
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
HK1208681A1 (en) * 2012-06-12 2016-03-11 Abbvie Inc. Pyridinone and pyridazinone derivatives
AU2013304146A1 (en) * 2012-08-16 2015-02-26 Bayer Pharma Aktiengesellschaft 2,3-benzodiazepines
WO2014048945A1 (de) 2012-09-28 2014-04-03 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische 5-aryl-triazolo-azepine
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
WO2014096965A2 (en) * 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors
AP2015008673A0 (en) * 2013-02-19 2015-08-31 Bayer Pharma Aktiengesellchaft Bicyclo 2,3-benzodiazepines and spirocyclically substituted 2,3-benzodiazepines
EP2958922A1 (de) 2013-02-22 2015-12-30 Bayer Pharma Aktiengesellschaft Pyrrolo- und pyrazolo-triazolodiazepine als bet-proteininhibitoren zur behandlung von hyper-proliferativen erkrankungen
CN105164135A (zh) 2013-02-22 2015-12-16 拜耳医药股份有限公司 4-取代的吡咯并二氮杂卓和吡唑并二氮杂卓
CA2902225A1 (en) * 2013-02-28 2014-09-04 Washington University Methods of treatment of human cytomegalovirus infection and diseases with bromodomain inhibitors
JP2016516701A (ja) * 2013-03-11 2016-06-09 アッヴィ・インコーポレイテッド 縮合四環系ブロモドメイン阻害剤
CA2903463A1 (en) 2013-03-11 2014-10-09 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
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
EP2970282B1 (en) 2013-03-15 2019-08-21 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
EP2989096B1 (en) 2013-04-26 2019-04-10 BeiGene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
TWI527811B (zh) 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
US8975417B2 (en) * 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
CA2913741A1 (en) * 2013-05-28 2014-12-04 The Brigham And Women's Hospital, Inc. Bet inhibition therapy for heart disease
CN105263934B (zh) * 2013-05-28 2017-09-08 诺华股份有限公司 作为bet抑制剂的吡唑并‑吡咯烷‑4‑酮衍生物及其在治疗疾病中的用途
ES2806135T3 (es) 2013-06-21 2021-02-16 Zenith Epigenetics Ltd Nuevos inhibidores de bromodominios bicíclicos
US9636328B2 (en) 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
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
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
RU2016105108A (ru) 2013-07-25 2017-08-30 Дана-Фарбер Кэнсер Инститьют, Инк. Ингибиторы факторов транскрипции и их применение
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
EP3027194A1 (en) * 2013-08-01 2016-06-08 Oncoethix GmbH Pharmaceutical formulation containing thienotriazolodiazepine compounds
WO2015018521A1 (en) * 2013-08-06 2015-02-12 Oncoethix Sa Method of treating diffuse large b-cell lymphoma (dlbcl) using a bet-bromodomain inhibitor
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
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US9994581B2 (en) 2013-12-10 2018-06-12 Abbvie Inc. Bromodomain inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EP3099677A4 (en) 2014-01-31 2017-07-26 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
CA2936256A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
WO2015121227A1 (de) * 2014-02-14 2015-08-20 Bayer Pharma Aktiengesellschaft 6,9-disubstituierte 1 -phenyl-3h-2,3-benzodiazepine und ihre verwendung als bromodomänen- inhibitoren
WO2015121268A1 (de) * 2014-02-14 2015-08-20 Bayer Pharma Aktiengesellschaft 1-phenyl-3h-2,3-benzodiazepine und ihre verwendung als bromodomänen-inhibitoren
JP2017071553A (ja) * 2014-02-25 2017-04-13 味の素株式会社 ヘテロ原子−メチレン−ヘテロ環構造を有する新規化合物
EP3110424A1 (en) 2014-02-28 2017-01-04 Tensha Therapeutics, Inc. Treatment of conditions associated with hyperinsulinaemia
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
WO2015153871A2 (en) * 2014-04-04 2015-10-08 Constellation Pharmaceuticals, Inc. EXPRESSION LEVELS OF BCL-xL, BCL2, BCL-w, AND BAD AND CANCER THERAPIES
WO2015156601A1 (en) * 2014-04-09 2015-10-15 Kainos Medicine, Inc. Bromodomain-inhibiting compounds and pharmaceutical composition comprising same for preventing or treating a cancer
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
PL3674302T3 (pl) 2014-04-23 2023-07-24 Incyte Holdings Corporation 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET
SG11201609404SA (en) 2014-05-29 2016-12-29 Entasis Therapeutics Ltd Fused, spirocyclic heteroaromatic compounds for the treatment of bacterial infections
JP2017519760A (ja) * 2014-06-18 2017-07-20 バイエル ファーマ アクチエンゲゼルシャフト ＢＥＴ−タンパク質を阻害するメタ位置換芳香族アミノ又はエーテル基を有する３，４−ジヒドロピリド［２，３−ｂ］ピラジノン類
WO2015195863A1 (en) * 2014-06-20 2015-12-23 Constellation Pharmaceuticals, Inc. Hydrated 2-((4s)-6-(4-chlorophenyl)-1 -methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
CA2952830C (en) * 2014-06-20 2022-11-01 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
CN106573915B (zh) * 2014-08-01 2020-12-25 纽韦卢森公司 针对布罗莫结构域有活性的化合物
KR20170032473A (ko) 2014-08-08 2017-03-22 다나-파버 캔서 인스티튜트 인크. 디아제판 유도체 및 그의 용도
MX2017001757A (es) 2014-08-08 2017-05-30 Dana Farber Cancer Inst Inc Derivados de dihidropteridinona y sus usos.
TWI712603B (zh) 2014-09-15 2020-12-11 美商英塞特公司 作為ｂｅｔ蛋白抑制劑之三環雜環
WO2016061144A1 (en) 2014-10-14 2016-04-21 The Regents Of The University Of California Use of cdk9 and brd4 inhibitors to inhibit inflammation
UA122130C2 (uk) 2014-10-27 2020-09-25 Тенша Терапеутікс, Інк. Інгібітори бромодомену
US20190100769A1 (en) * 2014-10-31 2019-04-04 Massachusetts Institute Of Technology Massively parallel combinatorial genetics for crispr
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
HK1245248B (en) 2014-12-11 2020-05-15 恒翼生物医药(上海)股份有限公司 Substituted heterocycles as bromodomain inhibitors
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. Inhibitors of bromodomains
CN111662226B (zh) * 2015-01-28 2022-03-18 中国科学院广州生物医药与健康研究院 一种2-氧代-1,2-二氢苯并[cd]吲哚类化合物
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
CN107530356A (zh) 2015-03-13 2018-01-02 雷斯韦洛吉克斯公司 用于治疗补体相关疾病之组合物及治疗方法
EP4414369A3 (en) 2015-03-18 2024-10-16 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
CN107548393B (zh) * 2015-03-30 2021-03-02 朱比兰特生物系统有限公司 适用于治疗癌症的1-(环)烷基吡啶-2-酮的三环稠合衍生物
DK3527574T3 (da) 2015-05-18 2022-06-27 Sumitomo Pharma Oncology Inc Alvocidib-prodrugs, der har øget biotilgængelighed
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
WO2016210275A1 (en) 2015-06-26 2016-12-29 Tensha Therapeutics, Inc. Treatment of nut midline carcinoma
AU2016291578C1 (en) * 2015-07-10 2021-07-15 Arvinas Operations, Inc. MDM2-based modulators of proteolysis and associated methods of use
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
WO2017040190A1 (en) 2015-08-28 2017-03-09 Constellation Pharmaceuticals, Inc. Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide
WO2017037567A1 (en) * 2015-09-03 2017-03-09 Pfizer Inc. Regulators of frataxin
CA2997531A1 (en) 2015-09-09 2017-03-16 Jubilant Biosys Limited Tricyclic fused pyridin-2-one derivatives and their use as brd4 inhibitors
MX2018003030A (es) 2015-09-11 2018-04-11 Dana Farber Cancer Inst Inc Acetamida tienotriazolodiazepinas y usos de las mismas.
KR20180049058A (ko) * 2015-09-11 2018-05-10 다나-파버 캔서 인스티튜트 인크. 시아노 티에노트리아졸로디아제핀 및 그의 용도
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
JP7385356B2 (ja) 2015-11-25 2023-11-22 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド 二価ブロモドメインインヒビターおよびそれらの使用
JP6967522B2 (ja) 2016-02-15 2021-11-17 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｂｅｔブロモドメイン阻害剤としての融合１，４−オキサゼピンおよび関連類似体
CN109311900A (zh) 2016-04-06 2019-02-05 密执安大学评议会 用于配体依赖性靶蛋白质降解的单官能中间体
KR102387316B1 (ko) 2016-04-06 2022-04-15 더 리젠츠 오브 더 유니버시티 오브 미시간 Mdm2 단백질 분해제
CA3020541A1 (en) 2016-04-12 2017-10-19 The Regents Of The University Of Michigan Bet protein degraders
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
HRP20230466T1 (hr) 2016-06-20 2023-07-21 Incyte Corporation Kristalni čvrsti oblici bet inhibitora
CA3036834A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-oxazepines as bet protein degraders
ES2857743T3 (es) 2016-09-13 2021-09-29 Univ Michigan Regents 1,4-diazepinas fusionadas como degradadores de proteína BET
WO2018075908A1 (en) * 2016-10-21 2018-04-26 University Of Miami Materials and methods for treating ophthalmic inflammation
RU2762279C2 (ru) * 2016-12-12 2021-12-17 Юнион Терапьютикс А/С Замещенные пиразолоазепин-4-оны и их применение в качестве ингибиторов фосфодиэстеразы
JP6850887B2 (ja) * 2016-12-12 2021-03-31 レオ ファーマ アクティーゼルスカブ 置換ピラゾロアゼピン−８−オンおよびそれらのホスホジエステラーゼ阻害剤としての使用
US11028051B2 (en) 2016-12-13 2021-06-08 St. Jude Children's Research Hospital Tetrahydroquinoline-based bromodomain inhibitors
JP2020506922A (ja) 2017-01-31 2020-03-05 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物
WO2018144789A1 (en) 2017-02-03 2018-08-09 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet bromodomain inhibitors
JOP20190192A1 (ar) * 2017-03-01 2019-08-08 Glaxosmithkline Ip No 2 Ltd مشتقات بيرازول بوصفها مثبطات برومودومين
WO2018207881A1 (ja) * 2017-05-12 2018-11-15 武田薬品工業株式会社 複素環化合物
AU2018277958B8 (en) * 2017-05-31 2022-03-10 Ayumi Pharmaceutical Corporation 6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivative
JP7196160B2 (ja) 2017-09-12 2022-12-26 スミトモ ファーマ オンコロジー， インコーポレイテッド Ｍｃｌ－１阻害剤アルボシジブを用いた、ｂｃｌ－２阻害剤に対して非感受性である癌の治療レジメン
WO2019055444A1 (en) 2017-09-13 2019-03-21 The Regents Of The University Of Michigan DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS
EP3707139B1 (en) 2017-11-06 2022-02-16 Centre National de la Recherche Scientifique Xanthine derivatives and uses thereof as inhibitors of bromodomains of bet proteins
WO2019148055A1 (en) 2018-01-26 2019-08-01 Yale University Imide-based modulators of proteolysis and methods of use
WO2020009176A1 (ja) 2018-07-04 2020-01-09 田辺三菱製薬株式会社 Ｂｅｔ蛋白質分解誘導作用を有するアミド化合物及びその医薬としての用途
CN115716827A (zh) 2018-07-25 2023-02-28 正大天晴药业集团股份有限公司 作为溴区结构域蛋白抑制剂的亚氨基砜类化合物、药物组合物及其医药用途
BR112021010134A2 (pt) * 2018-11-27 2021-08-24 Constellation Pharmaceuticals, Inc. Métodos de tratamento de transtornos mieloproliferativos
MX2021006205A (es) * 2018-11-27 2021-10-13 Constellation Pharmaceuticals Inc Metodos de tratamiento de trastornos mieloproliferativos.
WO2021091532A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2020117988A1 (en) 2018-12-04 2020-06-11 Tolero Pharmaceuticals, Inc. Cdk9 inhibitors and polymorphs thereof for use as agents for treatment of cancer
CN111518045A (zh) * 2019-02-02 2020-08-11 博诺康源(北京)药业科技有限公司 一种具有苯并七元环结构的化合物、其制备方法及用途
WO2020191326A1 (en) 2019-03-20 2020-09-24 Sumitomo Dainippon Pharma Oncology, Inc. Treatment of acute myeloid leukemia (aml) with venetoclax failure
WO2020257644A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2021091535A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Treating myeloproliferative disorders with cpi-0610 and a jak inhibitor
WO2020256739A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
CN112142711B (zh) * 2019-06-28 2022-03-29 中国科学院上海药物研究所 取代噻吩类化合物、其制备方法及其用途
JP2022542421A (ja) * 2019-07-29 2022-10-03 コンステレーション・ファーマシューティカルズ・インコーポレイテッド 神経障害の治療に使用するための化合物
CR20220353A (es) 2019-12-19 2022-10-20 Arvinas Operations Inc Compuestos y métodos para la degradación dirigida del receptor de andrógenos
CN115087658B (zh) 2020-02-06 2025-02-28 田边三菱制药株式会社 具有诱导brd4蛋白质分解作用的磺酰胺或亚磺酰胺化合物及其药物用途
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
WO2022031686A1 (en) 2020-08-04 2022-02-10 Constellation Pharmaceuticals, Inc. 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide for treating thrombocythemia
AR124681A1 (es) 2021-01-20 2023-04-26 Abbvie Inc Conjugados anticuerpo-fármaco anti-egfr
CN117320725A (zh) 2021-05-11 2023-12-29 星座制药公司 Pelabresib用于治疗贫血的用途
KR102619331B1 (ko) * 2021-11-30 2023-12-29 주식회사 베노바이오 Bet 단백질을 저해하는 신규한 카르복스아마이드 리독스 유도체 및 이를 이용한 안과질환 예방 및 치료용 조성물
KR20240144976A (ko) 2022-01-31 2024-10-04 콘스텔레이션 파마슈티칼스, 인크. 2-((4s)-6-(4-클로로페닐)-1-메틸-4h-벤조[c]이소옥사졸로[4,5-e]아제핀-4-일)아세트아미드의무수 결정질 형태
US20250382308A1 (en) 2022-04-19 2025-12-18 Nuevolution A/S Compounds active towards bromodomains
WO2024137713A1 (en) 2022-12-20 2024-06-27 Constellation Pharmaceuticals, Inc. Methods for treating lower risk myelodysplastic syndrome
WO2025067451A1 (zh) * 2023-09-27 2025-04-03 北京沐华生物科技有限责任公司 一类brd4蛋白降解剂化合物及其制备方法和应用
WO2025137396A1 (en) * 2023-12-20 2025-06-26 Constellation Pharmaceuticals, Inc. Synthesis of bromodomain inhibitors

Family Cites Families (140)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3523939A (en) 1967-07-03 1970-08-11 Hoffmann La Roche 5-(2,6-disubstituted phenyl)-1,4-benzodiazepines and methods for their preparation
CH498846A (de) 1967-08-09 1970-11-15 Hoffmann La Roche Verfahren zur Herstellung von Benzodiazepin-Derivaten
US3781289A (en) 1971-02-09 1973-12-25 Upjohn Co 7-chloro-1-methyl-5-phenyl-s-triazolo (4,3-a)quinolines
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
US3903103A (en) 1971-09-15 1975-09-02 Upjohn Co 4-Amino-s-triazolo-{8 4,3-a{9 {8 1,4{9 benzodiazepine
DE2242918A1 (de) 1971-09-15 1973-03-22 Upjohn Co Neue 4-amino-s-triazolo eckige klammer auf 4,3-a eckige klammer zu eckige klammer auf 1,4 eckige klammer zu benzodiazepine
US3886141A (en) 1971-10-07 1975-05-27 Hoffmann La Roche Preparation of 5-pyridyl benzodiazepine utilizing hexamethylenetetramine
BE795790A (fr) 1972-02-22 1973-08-22 Upjohn Co Dibenzo-triazolo-azepine
US4155904A (en) 1973-02-08 1979-05-22 Schering Corporation Process for the preparation of 1,4-benzo-diazepines and 1,4-benzodiazepinones
IE38931B1 (en) 1973-03-09 1978-07-05 Lipha Triazolobenzodiazepines
FR2220257A1 (en) 1973-03-09 1974-10-04 Lipha 5,6-Dihydro-(4H)-s-triazolo-(4,3-a) (1,5)benzodiazepines - as antiinflam-matory and analgesic agents without tranquillising effects
US3966736A (en) 1975-04-07 1976-06-29 The Upjohn Company 2,9-Dihydro-3H-pyrido[3,2-c]-s-triazolo[4,3-a][1,5]-benzodiazepin-3-ones
AT350056B (de) 1975-11-04 1979-05-10 Degussa Verfahren zur herstellung von neuen pyrido- (2,3-f)-(1,4)-diazepinen, deren optischen isomeren und salzen
DE2640599A1 (de) 1976-09-09 1978-03-16 Scherico Ltd Verfahren zur herstellung von 1,4- benzodiazepinen
CA1152066A (en) 1980-02-08 1983-08-16 Hoffmann-La Roche Limited Benzodiazepine derivatives
CA1157855A (en) 1980-07-31 1983-11-29 Albert E. Fischli Benzodiazepine derivatives
CA1163266A (en) 1980-07-31 1984-03-06 Albert E. Fischli Benzodiazepine derivatives
US4455307A (en) 1982-01-04 1984-06-19 The Upjohn Company Antihypertensive use of triazolobenzodiazepines
US4820834A (en) 1984-06-26 1989-04-11 Merck & Co., Inc. Benzodiazepine analogs
US5004741A (en) 1984-06-26 1991-04-02 Merck & Co., Inc. Methods of antagonizing CCK or gastrin with benzodiazepine analogs
US4663321A (en) 1984-06-26 1987-05-05 Merck & Co., Inc. Triazolobenzodiazepines and pharmaceutical use
DE3878833T2 (de) 1987-05-28 1993-06-09 Yoshitomi Pharmaceutical Thieno(triazolo)diazepinverbindungen, und medizinische verwendung derselben.
MC1999A1 (fr) 1987-12-18 1990-01-26 Hoffmann La Roche Composes tricycliques
US4959361A (en) 1987-12-18 1990-09-25 Hoffmann-La Roche Inc. Triazolo(4,3-A)(1,4)benzodiazepines and thieno (3,2-F)(1,2,4)triazolo(4,3-A)(1,4)diazepine compounds which have useful activity as platelet activating factor (PAF) antagonists
EP0348523A4 (en) 1987-12-22 1991-10-09 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compounds and their medicinal use
CA1324863C (en) 1988-01-30 1993-11-30 Minoru Moriwaki Thienotriazolodiazepine compounds and pharmaceutical uses thereof
CA1322367C (en) 1988-05-17 1993-09-21 Yoshitomi Pharmaceutical Industries Ltd. Thienotriazolodiazepine compounds and pharmaceutical uses thereof
US5382579A (en) 1988-10-31 1995-01-17 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
US5221671A (en) 1988-10-31 1993-06-22 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
FI95708C (fi) 1988-10-31 1996-03-11 Eisai Co Ltd Analogiamenetelmä 1,4-diatsepiinijohdannaisen ja sen farmaseuttisesti sopivan suolan valmistamiseksi
DE3936828A1 (de) 1988-11-06 1990-05-10 Boehringer Ingelheim Kg Neue hetrazepine
DE4006471A1 (de) 1989-03-03 1990-09-06 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
ATE119040T1 (de) 1989-08-04 1995-03-15 Merck Sharp & Dohme Zentrale cholecystokinin-antagonisten zur behandlung von psychiatrischen krankheiten.
US5175159A (en) 1989-10-05 1992-12-29 Merck & Co., Inc. 3-substituted-1,4-benzodiazepines as oxytocin antagonists
CA2032427A1 (en) 1989-12-18 1991-06-19 Mark G. Bock Benzodiazepines analogs
IL96613A0 (en) 1989-12-18 1991-09-16 Merck & Co Inc Pharmaceutical compositions containing benzodiazepine analogs
JP2959591B2 (ja) 1990-05-23 1999-10-06 吉富製薬株式会社 チエノトリアゾロジアゼピン化合物
WO1994006801A1 (fr) 1990-05-23 1994-03-31 Yoshitomi Pharmaceutical Industries, Ltd. Compose de thienodiazepine et son utilisation comme medicament
DE4027470A1 (de) 1990-08-30 1992-03-05 Boehringer Ingelheim Kg Neue hetrazepinoide amide
JP2959598B2 (ja) 1990-10-12 1999-10-06 吉富製薬株式会社 光学活性なチエノトリアゾロジアゼピン化合物
US5206234A (en) 1990-10-22 1993-04-27 Merck & Co., Inc. Benzolactam analogs as antagonists of cck
CA2056809A1 (en) 1990-12-07 1992-06-08 Mark G. Bock Benzodiazepine analogs
DE4101146A1 (de) 1991-01-16 1992-07-23 Boehringer Ingelheim Kg Neue in 6-position substituierte diazepine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DE4107521A1 (de) 1991-03-08 1992-09-10 Boehringer Ingelheim Kg Neue acylaminosubstituierte hetrazepine
US5683998A (en) 1991-04-23 1997-11-04 Toray Industries, Inc. Tricyclic triazolo derivatives, processes for producing the same and the uses of the same
US5185331A (en) 1991-05-14 1993-02-09 Merck & Co., Inc. Triazolobenzodiazepines
CA2071092A1 (en) 1991-06-14 1992-12-15 Roger M. Freidinger 1,4-benzodiazepines with 5-membered heterocyclic rings
GB9117852D0 (en) 1991-08-19 1991-10-09 Merck Sharp & Dohme Therapeutic agents
US5153191A (en) 1991-08-20 1992-10-06 Warner-Lambert Company Cholecystokinin antagonists useful for treating depression
DE4128581A1 (de) 1991-08-28 1993-03-04 Boehringer Ingelheim Kg Verwendung von paf-antagonisten hetrazepinoider struktur zur behandlung der allergischen rhinitis
EP0559891B1 (en) 1991-09-30 2000-01-12 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and its use
WO1993007129A1 (fr) 1991-10-11 1993-04-15 Yoshitomi Pharmaceutical Industries, Ltd. Medicament utilise pour traiter l'osteoporose et compose de diazepine
WO1993012117A1 (en) 1991-12-11 1993-06-24 Yoshitomi Pharmaceutical Industries, Ltd. Immunosuppressive agent
WO1993012791A1 (en) 1991-12-20 1993-07-08 Merck Sharp & Dohme Limited Central cholecystokinin antagonists having pharmaceutical activity
DE4200610A1 (de) 1992-01-13 1993-07-15 Boehringer Ingelheim Kg Verwendung von paf-antagonisten zur behandlung der dysmenorrhea
EP0636123A1 (en) 1992-03-24 1995-02-01 MERCK SHARP & DOHME LTD. 3-ureido substituted benzodiazepin-2-ones having cholecystokinin and/or gastrin antagonistic activity and their use in therapy
DE4219659A1 (de) 1992-06-16 1993-12-23 Boehringer Ingelheim Kg Die Verwendung von PAF-Antagonisten in Kombination mit Anticholinergika
EP0661284A1 (en) * 1992-09-18 1995-07-05 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
JP3223290B2 (ja) 1992-11-10 2001-10-29 日本電信電話株式会社 マイクロ回転体およびその製造方法
US5302590A (en) 1992-12-18 1994-04-12 Hoffmann-La Roche Inc. Compounds useful as dual antagonists of platelet activating factor and leukotriene D4
EP0692483A1 (en) 1993-03-30 1996-01-17 Yoshitomi Pharmaceutical Industries, Ltd. Cell adhesion inhibitor and thienotriazolodiazepine compound
WO1994026723A2 (en) 1993-05-14 1994-11-24 Genentech, Inc. ras FARNESYL TRANSFERASE INHIBITORS
US5760031A (en) 1993-07-29 1998-06-02 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US5869483A (en) 1993-07-29 1999-02-09 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US5516774A (en) 1993-07-29 1996-05-14 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5733905A (en) 1993-07-29 1998-03-31 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
AU686715B2 (en) 1993-11-22 1998-02-12 Merck & Co., Inc. Tricyclic benzodiazepinyl amide derivatives as amtiarrhythmics
ES2156933T3 (es) 1993-12-28 2001-08-01 Meiji Seika Co Derivados triciclicos de benzazepina y benzotiazepina.
US5739129A (en) 1994-04-14 1998-04-14 Glaxo Wellcome Inc. CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
US5795887A (en) 1994-04-15 1998-08-18 Glaxo Wellcome Inc. Method of inducing cholecystokinin agonist activity using 1,4- Benzodiazepine compounds
KR100484294B1 (ko) 1995-09-21 2005-09-09 가부시키가이샤 이야쿠 분지 셋케이 겐쿠쇼 레티노이드작용증강성화합물
PL330635A1 (en) * 1996-06-12 1999-05-24 Japan Tobacco Inc Inhibitor of cytokin production, triazepin compound and intermediate compounds used for obtaining the last mentioned one
EP0989131B1 (en) * 1996-09-13 2002-11-13 Mitsubishi Pharma Corporation Thienotriazolodiazepine compounds and medicinal uses thereof
AU749658C (en) 1996-12-23 2004-04-29 Elan Pharmaceuticals, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
US6433167B1 (en) 1997-06-25 2002-08-13 Nikken Chemicals Co., Ltd. Triazolo-1,4-diazepine compounds and medicinal composition containing the same
JP4204657B2 (ja) 1997-12-05 2009-01-07 有限会社ケムフィズ 糖尿病の予防・治療剤
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
PE20000944A1 (es) 1998-07-31 2000-09-20 Lilly Co Eli Derivados de sulfonamida
EP1107983A2 (en) 1998-09-01 2001-06-20 Innogenetics N.V. Benzodiazepine and benzothiazepine derivatives and hbsag peptides binding to annexins, their compositions and use
US6277844B1 (en) * 1998-09-14 2001-08-21 Sydney Spector Compound for selective treatment of malignant cells by inhibiting cell cycle progression, decreasing Bcl2, and increasing apoptosis
WO2000054778A1 (fr) 1999-03-12 2000-09-21 Welfide Corporation Agents preventifs ou therapeutiques des dermatoses inflammatoires
FR2791980B1 (fr) 1999-04-09 2001-07-06 Sod Conseils Rech Applic Pyrido-thieno-diazepines, leur procede de preparation, et les compositions pharmaceutiques les contenant
GB9911152D0 (en) 1999-05-14 1999-07-14 Glaxo Group Ltd Short-acting benzodiazepines
US7160880B1 (en) 1999-05-14 2007-01-09 Cenes Limited Short-acting benzodiazepines
DE60015392D1 (de) 1999-12-29 2004-12-02 Glaxo Group Ltd Verwendung von annexin-modulatoren zur herstellung eines medikaments zur behandlung und/oder vorbeugung von arthritis und arthritischen erkrankungen
WO2001095912A1 (fr) 2000-06-16 2001-12-20 Mitsubishi Pharma Corporation Compositions permettant de reguler la plage et/ou la vitesse de liberation du ph
JP2005503356A (ja) 2001-06-07 2005-02-03 ニューロ３デー 環状ヌクレオチドホスホジエステラーゼ阻害剤、その製造および使用
EP1481977A4 (en) 2002-03-01 2006-02-01 Astellas Pharma Inc NITROGENIC HETEROCYCLIC COMPOUND
JP2006509832A (ja) 2002-10-30 2006-03-23 ニューロ３デー サイクリックヌクレオチドホスホジエステラーゼ阻害剤、その調製及び使用
US7482337B2 (en) 2002-11-08 2009-01-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
DE10251927A1 (de) 2002-11-08 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
RU2005122484A (ru) 2002-12-18 2006-01-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Композиции, используемые в качестве ингибиторов протеинкиназ
US7119088B2 (en) 2003-02-19 2006-10-10 Pfizer Inc. Triazole compounds useful in therapy
EP1640010A1 (en) 2003-07-01 2006-03-29 Astellas Pharma Inc. Agent inducing increase in bone mass
WO2005099759A1 (ja) 2004-04-16 2005-10-27 Institute Of Medicinal Molecular Design. Inc. 動脈硬化症の予防及び／又は治療のための医薬
KR20070103352A (ko) 2004-10-05 2007-10-23 파이오니아 가부시키가이샤 오디오 랙
US8044042B2 (en) * 2005-05-30 2011-10-25 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and medicinal use thereof
US7947678B2 (en) 2005-07-29 2011-05-24 Merck Sharp & Dohme Corp. Heterocyclic benzodiazepine CGRP receptor antagonists
CA2627757A1 (en) 2005-10-26 2007-05-03 The Regents Of The University Of Michigan Therapeutic compositions and methods
US20070105844A1 (en) 2005-10-26 2007-05-10 Regents Of The University Of Michigan Therapeutic compositions and methods
DE102005061840A1 (de) 2005-12-23 2007-06-28 Merck Patent Gmbh Triazolderivate
CN101541768A (zh) 2006-08-25 2009-09-23 日本化学医药株式会社 P2x4受体拮抗剂
WO2008109856A2 (en) 2007-03-07 2008-09-12 Xenon Pharmaceuticals Inc. Methods of using diazepinone compounds in treating sodium channel-mediated diseases or conditions
US20090111780A1 (en) 2007-10-31 2009-04-30 Everett Laboratories, Inc. Compositions and methods for treatment of ear canal infection and inflammation
ITFI20070288A1 (it) 2007-12-21 2009-06-22 A I L Firenze Sezione Autonoma Inibitori delle deacetilasi istoniche
WO2009084693A1 (ja) * 2007-12-28 2009-07-09 Mitsubishi Tanabe Pharma Corporation 抗癌剤
WO2009152589A1 (en) 2008-06-17 2009-12-23 Universidade Federal De Minas Gerais-Ufmg Use of paf receptor for treating infections caused by flaviviridae
CN102076691A (zh) 2008-06-23 2011-05-25 维泰克斯制药公司 蛋白激酶抑制剂
CA2741934C (en) 2008-10-30 2016-09-13 Circomed Llc Thienotriazolodiazepine derivatives active on apo a
WO2010121164A2 (en) 2009-04-17 2010-10-21 The Regents Of The University Of Michigan 1,4-benzodiazepinone compounds and their use in treating cancer
EP2427451B1 (en) 2009-05-07 2019-03-20 PRISM BioLab Co., Ltd. Alpha helix mimetics and methods relating thereto
JP5442021B2 (ja) 2009-09-28 2014-03-12 日本曹達株式会社 含窒素ヘテロ環化合物およびその塩ならびに農園芸用殺菌剤
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
BR112012010705A2 (pt) 2009-11-05 2016-03-29 Glaxosmithkline Llc composto, composição farmacêutica, produto farmacêutico combinado, uso de um composto, e, métodos para tratar uma doença ou condição, e para inibir um bromodomínio
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
PH12012500894A1 (en) 2009-11-05 2022-03-09 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
WO2011054851A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Novel process
US8765920B2 (en) 2009-12-23 2014-07-01 The Scripps Research Institute Tyrosine bioconjugation through aqueous Ene-like reactions
US8541407B2 (en) 2010-03-31 2013-09-24 Arqule, Inc. Substituted benzo-pyrido-triazolo-diazepine compounds
CA2799381A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Male contraceptive compositions and methods of use
WO2011143660A2 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
CA2799420C (en) 2010-05-14 2018-10-02 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating neoplasia, inflammatory disease and other disorders
EP2569429A4 (en) 2010-05-14 2013-09-25 Dana Farber Cancer Inst Inc COMPOSITIONS AND METHODS FOR MODULATING METABOLISM
US9085582B2 (en) 2010-06-22 2015-07-21 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
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
US9422292B2 (en) 2011-05-04 2016-08-23 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
US10071129B2 (en) 2011-08-30 2018-09-11 Whitehead Institute For Biomedical Research Dana-Farber Cancer Institute, Inc. Method for identifying bromodomain inhibitors
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
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

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11458123B2 (en) 2016-11-01 2022-10-04 Arvinas Operations, Inc. Tau-protein targeting PROTACs and associated methods of use
RU2805523C2 (ru) * 2016-11-01 2023-10-18 Эрвинэс, Инк. Protac, целенаправленно воздействующие на тау-белок, и связанные с ними способы применения
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated

Also Published As

Publication number Publication date
SG190739A1 (en) 2013-07-31
IL226331A (en) 2015-09-24
EP2646446A4 (en) 2014-04-23
NZ611964A (en) 2015-01-30
MX2013006214A (es) 2014-10-17
EP2646446B1 (en) 2015-05-13
PT2646446E (pt) 2015-09-24
AU2011336417B2 (en) 2016-09-29
WO2012075383A3 (en) 2012-08-16
BR112013013167A8 (pt) 2021-05-18
HK1189587A1 (en) 2014-06-13
IL226331A0 (en) 2013-07-31
PL2646446T3 (pl) 2015-10-30
CA2818187A1 (en) 2012-06-07
BR112013013167A2 (pt) 2017-10-31
AU2011336417A1 (en) 2013-07-04
BR112013013167B1 (pt) 2021-12-07
HUE025321T2 (en) 2016-02-29
KR101871013B1 (ko) 2018-07-20
US20120157428A1 (en) 2012-06-21
US9522920B2 (en) 2016-12-20
AR084070A1 (es) 2013-04-17
WO2012075383A2 (en) 2012-06-07
JP5850944B2 (ja) 2016-02-03
RS54175B1 (sr) 2015-12-31
TWI572607B (zh) 2017-03-01
KR20130125378A (ko) 2013-11-18
EA022645B1 (ru) 2016-02-29
HRP20150858T1 (hr) 2015-09-25
JP2013544847A (ja) 2013-12-19
CN103415525A (zh) 2013-11-27
US20140371206A1 (en) 2014-12-18
CN103415525B (zh) 2016-05-18
CA2818187C (en) 2018-10-23
EP2646446A2 (en) 2013-10-09
DK2646446T3 (en) 2015-08-10
ZA201303776B (en) 2014-11-26
SI2646446T1 (sl) 2015-09-30
CY1116578T1 (el) 2017-03-15
ES2545117T3 (es) 2015-09-08
US8796261B2 (en) 2014-08-05
TW201305182A (zh) 2013-02-01

Similar Documents

Publication Publication Date Title
EA201390803A1 (ru) Ингибиторы бромодомена и их применение
EA201492216A1 (ru) Ингибиторы бромодомена и их применение
CY1124311T1 (el) Παρεμποδιστες dna-pk
WO2012174487A3 (en) Bromodomain inhibitors and uses thereof
WO2012151512A3 (en) Bromodomain inhibitors and uses thereof
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
EA201290980A1 (ru) Производные 1-амино-2-циклопропилэтилбороновой кислоты
EA201270722A1 (ru) Формы рифаксимина и их применение
EA201391285A1 (ru) Производные тетрагидрохинолина, полезные в качестве ингибиторов бромодомена
MX2015012502A (es) Inhibidores de proteina cinasa dependiente de adn.
EA201201201A1 (ru) Новые ингибиторы rock
EA201391719A1 (ru) Хиназолиновые производные для лечения вирусных инфекций и дальнейших заболеваний
EA201291336A1 (ru) Замещенные 5-фтор-1н-пиразолопиридины и их применение
EA201370018A1 (ru) Составы рифаксимина и их применение
MX2015011898A (es) Compuestos de pirazolo y usos de los mismos.
EA033374B1 (ru) Твердые фармацевтические композиции, содержащие энзалутамид, и способ лечения
EA201992133A1 (ru) Производные пиперидино-пиримидина для лечения вирусных инфекций
EA201590343A1 (ru) Алкилпиримидиновые производные для лечения вирусных инфекций и дальнейших заболеваний
EA201300471A1 (ru) Замещенные 6-аминоникотинамиды в качестве модуляторов kcnq2/3
EA201490471A1 (ru) Пиридазиноновые соединения и их применение в качестве ингибиторов daao
EA201691070A1 (ru) Новые трициклические соединения в качестве противораковых средств
EA201591166A1 (ru) Ингибиторы аутотаксина
EA201491617A1 (ru) Соединения для лечения спинальной мышечной атрофии
EA201291034A1 (ru) АПТАМЕРЫ К β-NGF И ИХ ПРИМЕНЕНИЕ ПРИ ЛЕЧЕНИИ B-NGF-ОПОСРЕДОВАННЫХ ЗАБОЛЕВАНИЙ И РАССТРОЙСТВ
EA201290860A1 (ru) Лечение ревматоидного артрита комбинацией лаквинимода и метотрексата