HK1189587A1 - 溴結構域蛋白抑制劑及其應用 - Google Patents

溴結構域蛋白抑制劑及其應用

Info

Publication number
HK1189587A1
HK1189587A1 HK14102658.3A HK14102658A HK1189587A1 HK 1189587 A1 HK1189587 A1 HK 1189587A1 HK 14102658 A HK14102658 A HK 14102658A HK 1189587 A1 HK1189587 A1 HK 1189587A1
Authority
HK
Hong Kong
Prior art keywords
bromodomain inhibitors
bromodomain
inhibitors
Prior art date
Application number
HK14102658.3A
Other languages
English (en)
Inventor
Brian K Albrecht
James Edmund Audia
Alexandre Cote
Victor S Gehling
Jean-Christophe Harmange
Michael C Hewitt
Yves Leblanc
Christopher G Nasveschuk
Alexander M Taylor
Rishi G Vaswani
Original Assignee
Constellation Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Constellation Pharmaceuticals Inc filed Critical Constellation Pharmaceuticals Inc
Publication of HK1189587A1 publication Critical patent/HK1189587A1/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/424Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4702Regulators; Modulating activity

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  • 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)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (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)
HK14102658.3A 2010-12-02 2014-03-17 溴結構域蛋白抑制劑及其應用 HK1189587A1 (zh)

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
US201161540788P 2011-09-29 2011-09-29
US201161540725P 2011-09-29 2011-09-29
PCT/US2011/063046 WO2012075383A2 (en) 2010-12-02 2011-12-02 Bromodomain inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
HK1189587A1 true HK1189587A1 (zh) 2014-06-13

Family

ID=46235164

Family Applications (1)

Application Number Title Priority Date Filing Date
HK14102658.3A HK1189587A1 (zh) 2010-12-02 2014-03-17 溴結構域蛋白抑制劑及其應用

Country Status (27)

Country Link
US (2) US8796261B2 (zh)
EP (1) EP2646446B1 (zh)
JP (1) JP5850944B2 (zh)
KR (1) KR101871013B1 (zh)
CN (1) CN103415525B (zh)
AR (1) AR084070A1 (zh)
AU (1) AU2011336417B2 (zh)
BR (1) BR112013013167B1 (zh)
CA (1) CA2818187C (zh)
CY (1) CY1116578T1 (zh)
DK (1) DK2646446T3 (zh)
EA (1) EA022645B1 (zh)
ES (1) ES2545117T3 (zh)
HK (1) HK1189587A1 (zh)
HR (1) HRP20150858T1 (zh)
HU (1) HUE025321T2 (zh)
IL (1) IL226331A (zh)
MX (1) MX2013006214A (zh)
NZ (1) NZ611964A (zh)
PL (1) PL2646446T3 (zh)
PT (1) PT2646446E (zh)
RS (1) RS54175B1 (zh)
SG (1) SG190739A1 (zh)
SI (1) SI2646446T1 (zh)
TW (1) TWI572607B (zh)
WO (1) WO2012075383A2 (zh)
ZA (1) ZA201303776B (zh)

Families Citing this family (144)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2118074T3 (pl) 2007-02-01 2014-06-30 Resverlogix Corp Związki chemiczne do celów profilaktyki i leczenia chorób układu sercowo-naczyniowego
US9238640B2 (en) 2009-03-18 2016-01-19 Resverlogix Corp. Anti-inflammatory agents
EP2569434B1 (en) 2010-05-14 2019-09-04 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia and related disorders
HUE031073T2 (en) 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
US9301962B2 (en) 2010-05-14 2016-04-05 Baylor College Of Medicine Male contraceptive compositions and methods of use
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (es) * 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
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
EP2721031B1 (en) 2011-06-17 2016-01-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
HUE044986T2 (hu) 2011-11-01 2019-11-28 Resverlogix Corp Orális, azonnali felszabadulású készítmények szubsztituált kinazolinonokhoz
EP2802608A4 (en) 2012-01-12 2015-08-05 Univ Yale COMPOUNDS AND METHODS FOR ENHANCED DEGRADATION OF TARGET PROTEINS AND OTHER POLYPEPTIDES BY 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
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
EP2858982A4 (en) * 2012-06-12 2015-11-11 Abbvie Inc PYRIDINONE AND PYRIDAZINONE DERIVATIVES
CA2881996A1 (en) 2012-08-16 2014-02-20 Bayer Pharma Aktiengesellschaft 2,3-benzodiazepines
ES2625959T3 (es) 2012-09-28 2017-07-21 Bayer Pharma Aktiengesellschaft 5-Aril-triazolo-azepinas inhibidoras de la proteína BET
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
KR20150096794A (ko) * 2012-12-21 2015-08-25 제니쓰 에피제네틱스 코포레이션 브로모도메인 저해제로서의 신규한 헤테로사이클릭 화합물
WO2014128067A1 (de) * 2013-02-19 2014-08-28 Bayer Pharma Aktiengesellschaft Bicyclo- und spirocyclisch substituierte 2,3-benzodiazepine
US20160009725A1 (en) 2013-02-22 2016-01-14 Bayer Pharma Aktiengesellschaft Pyrrolo- and pyrazolo-triazolodiazepines as bet-protein inhibitors for treating hyperproliferative diseases
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
TW201444843A (zh) * 2013-03-11 2014-12-01 Abbvie Inc 溴區結構域蛋白抑制劑
AU2014249192B2 (en) 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
MX363913B (es) * 2013-03-12 2019-04-08 Abbvie Inc Inhibidores de bromodominio tetraciclicos.
EP2968360B1 (en) 2013-03-14 2021-01-20 ConverGene LLC Quinolinone derivatives for the inhibition of bromodomain-containing proteins
US9714946B2 (en) 2013-03-14 2017-07-25 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
CA2901083A1 (en) 2013-04-26 2014-10-30 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
US9624247B2 (en) * 2013-05-28 2017-04-18 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
US9636328B2 (en) 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
CN109939113B (zh) 2013-06-21 2022-02-15 恒翼生物医药科技(上海)有限公司 双环溴结构域抑制剂
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
KR20160034379A (ko) 2013-07-25 2016-03-29 다나-파버 캔서 인스티튜트 인크. 전사 인자의 억제제 및 그의 용도
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
WO2015014998A1 (en) * 2013-08-01 2015-02-05 Oncoethix Sa Pharmaceutical formulation containing thienotriazolodiazepine compounds
KR20160037201A (ko) * 2013-08-06 2016-04-05 온코에틱스 게엠베하 Bet-브로모도메인 억제제를 사용한 미만성 거대 b-세포 림프종 (dlbcl)의 치료 방법
WO2015070020A2 (en) 2013-11-08 2015-05-14 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (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
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
AU2014361381A1 (en) * 2013-12-10 2016-06-16 Abbvie Inc. Bromodomain inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
WO2015117083A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
CA2936865A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
EP3099693A4 (en) 2014-01-31 2017-08-16 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
AU2015222805B2 (en) 2014-02-28 2020-05-21 Tensha Therapeutics, Inc. Treatment of conditions associated with hyperinsulinaemia
JP2017511801A (ja) 2014-02-28 2017-04-27 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9H−ピリミド[4,5−b]インドールおよび関連類似体
EP3125896A2 (en) * 2014-04-04 2017-02-08 Constellation Pharmaceuticals, Inc. EXPRESSION LEVELS OF BCL-xL, BCL2, BCL-w, AND BAD AND CANCER THERAPIES
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
MY180775A (en) 2014-04-23 2020-12-09 Incyte Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
WO2015181637A1 (en) 2014-05-29 2015-12-03 Entasis Therapeutics Limited Fused, spirocyclic heteroaromatic compounds for the treatment of bacterial infections
WO2015193219A1 (de) * 2014-06-18 2015-12-23 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische 3,4-dihydropyrido[2,3-b]pyrazinone mit meta-substituierter aromatischer amino- oder ethergruppe
EP3157928B1 (en) * 2014-06-20 2019-02-13 Constellation Pharmaceuticals, Inc. Crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
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
SG10201900631TA (en) * 2014-08-01 2019-02-27 Nuevolution As Compounds active towards bromodomains
CN106715437A (zh) 2014-08-08 2017-05-24 达纳-法伯癌症研究所股份有限公司 二氮杂环庚烷衍生物及其用途
CA2955077A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
JP6599979B2 (ja) 2014-09-15 2019-10-30 インサイト・コーポレイション Betタンパク質阻害剤として用いるための三環式複素環化合物
CA3000633C (en) 2014-10-14 2023-10-03 The Regents Of The University Of California Use of cdk9 and brd4 inhibitors to inhibit inflammation
BR112017008714A2 (pt) 2014-10-27 2017-12-19 Tensha Therapeutics Inc inibidores de bromodomínio
CN107429246B (zh) * 2014-10-31 2021-06-01 麻省理工学院 用于crispr的大规模并行组合遗传学
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
CA2966449A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
EP3233846A4 (en) 2014-12-17 2018-07-18 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
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
CN114984016A (zh) 2015-03-13 2022-09-02 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
EP3270917A4 (en) 2015-03-18 2018-08-08 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
DK3277683T3 (en) * 2015-03-30 2022-05-02 Jubilant Biosys Ltd Tricyklisk sammensmeltet afledt af 1-(cyklo)alkyl pyridin-2-one nyttig til behandling af kræft
WO2016196065A1 (en) 2015-05-29 2016-12-08 Genentech, Inc. Methods and compositions for assessing responsiveness of cancers to bet inhibitors
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
MA42249A (fr) 2015-06-26 2018-05-02 Tensha Therapeutics Inc Traitement de carcinome de la ligne médiane nut
KR20180035828A (ko) * 2015-07-10 2018-04-06 아비나스 인코포레이티드 단백질 분해의 mdm2계 조절인자 및 관련된 이용 방법
WO2017030814A1 (en) * 2015-08-19 2017-02-23 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
ES2866073T3 (es) 2015-09-09 2021-10-19 Jubilant Biosys Ltd Derivados tricíclicos fusionados de piridin-2-ona y su uso como inhibidores de BRD4
WO2017044849A1 (en) 2015-09-11 2017-03-16 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof
PE20181086A1 (es) 2015-09-11 2018-07-05 Dana Farber Cancer Inst Inc Acetamida tienotrizolodiazepinas y usos de las mismas
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
SG10201913450PA (en) 2015-11-25 2020-03-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
CN109071562B (zh) 2016-02-15 2022-03-22 密执安大学评议会 作为bet溴结构域抑制剂的稠合1,4-氧氮杂䓬和相关类似物
SG11201808728QA (en) 2016-04-06 2018-11-29 Univ Michigan Regents Mdm2 protein degraders
US10759808B2 (en) 2016-04-06 2020-09-01 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
US10633386B2 (en) 2016-04-12 2020-04-28 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
EP4234554A3 (en) 2016-06-20 2023-12-27 Incyte Corporation Crystalline solid forms of a bet inhibitor
WO2018052949A1 (en) 2016-09-13 2018-03-22 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet protein degraders
US11466028B2 (en) 2016-09-13 2022-10-11 The Regents Of The University Of Michigan Fused 1,4-oxazepines as BET protein degraders
WO2018075908A1 (en) * 2016-10-21 2018-04-26 University Of Miami Materials and methods for treating ophthalmic inflammation
CA3209295A1 (en) 2016-11-01 2018-06-07 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
CN110099905B (zh) * 2016-12-12 2024-06-14 联合疗法公司 取代的吡唑并氮杂䓬-8-酮类及其作为磷酸二酯酶抑制剂的用途
RU2762279C2 (ru) * 2016-12-12 2021-12-17 Юнион Терапьютикс А/С Замещенные пиразолоазепин-4-оны и их применение в качестве ингибиторов фосфодиэстеразы
US11028051B2 (en) 2016-12-13 2021-06-08 St. Jude Children's Research Hospital Tetrahydroquinoline-based bromodomain inhibitors
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
CA3064845A1 (en) 2017-05-31 2018-12-06 Ayumi Pharmaceutical Corporation 6h-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivatives
WO2019055579A1 (en) 2017-09-12 2019-03-21 Tolero Pharmaceuticals, Inc. TREATMENT REGIME FOR CANCERS THAT ARE INSENSITIVE TO BCL-2 INHIBITORS USING THE MCL-1 ALVOCIDIB INHIBITOR
WO2019055444A1 (en) 2017-09-13 2019-03-21 The Regents Of The University Of Michigan DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS
US11180510B2 (en) 2017-11-06 2021-11-23 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
CN112543764B (zh) 2018-07-04 2024-05-10 田边三菱制药株式会社 具有bet蛋白水解诱导作用的酰胺化合物及其医药应用
CA3106733A1 (en) 2018-07-25 2020-01-30 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Sulfoximine compound as bromodomain protein inhibitor and pharmaceutical composition and medical use thereof
WO2020112939A1 (en) 2018-11-27 2020-06-04 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
SG11202105279SA (en) 2018-11-27 2021-06-29 Constellation Pharmaceuticals Inc Methods of treating myeloproliferative disorders
WO2021091532A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
US11034710B2 (en) 2018-12-04 2021-06-15 Sumitomo Dainippon Pharma Oncology, 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
US11793802B2 (en) 2019-03-20 2023-10-24 Sumitomo Pharma Oncology, Inc. Treatment of acute myeloid leukemia (AML) with venetoclax failure
WO2021091535A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Treating myeloproliferative disorders with cpi-0610 and a jak inhibitor
WO2020257644A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
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
WO2021011913A1 (en) 2019-07-17 2021-01-21 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
CA3149095A1 (en) * 2019-07-29 2021-02-04 Constellation Pharmaceuticals, Inc. Alpha-amino amide compounds for use in treating neurological disorders
PE20221582A1 (es) 2019-12-19 2022-10-06 Arvinas Operations Inc Compuestos y metodos para la degradacion dirigida de receptor de androgenos
CA3168824A1 (en) 2020-02-06 2021-08-12 Mitsubishi Tanabe Pharma Corporation Sulfonamide or sulfinamide compound having effect of inducing brd4 protein degradation and pharmaceutical use thereof
WO2021175432A1 (en) 2020-03-04 2021-09-10 Boehringer Ingelheim International Gmbh Method for administration of an anti cancer agent
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
AU2021297799A1 (en) 2020-06-23 2022-12-22 Genentech, Inc. Macrocyclic compounds and methods of use thereof
CA3188245A1 (en) 2020-08-04 2022-02-10 Adrian SENDEROWICZ 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
KR20240005881A (ko) 2021-05-11 2024-01-12 콘스텔레이션 파마슈티칼스, 인크. 빈혈 치료를 위한 펠라브레시브의 용도
KR102619332B1 (ko) * 2021-11-30 2024-01-02 주식회사 베노바이오 Bet 단백질을 저해하는 신규한 카르복스아마이드 리독스 유도체 및 이를 이용한 안과질환 예방 및 치료용 조성물
WO2023147149A1 (en) 2022-01-31 2023-08-03 Constellation Pharmaceuticals, Inc. Anhydrous crystalline forms of 2-((4s)-6-(4-chlorophenyl)-1-methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide
WO2023205251A1 (en) 2022-04-19 2023-10-26 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

Family Cites Families (142)

* 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
US3709898A (en) 1971-02-09 1973-01-09 Upjohn Co Process for the production of triazolobenzodiazepines and intermediates
US3781289A (en) 1971-02-09 1973-12-25 Upjohn Co 7-chloro-1-methyl-5-phenyl-s-triazolo (4,3-a)quinolines
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
US4663321A (en) 1984-06-26 1987-05-05 Merck & Co., Inc. Triazolobenzodiazepines and pharmaceutical use
US5004741A (en) 1984-06-26 1991-04-02 Merck & Co., Inc. Methods of antagonizing CCK or gastrin with benzodiazepine analogs
ATE86256T1 (de) 1987-05-28 1993-03-15 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
WO1989005812A1 (en) 1987-12-22 1989-06-29 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
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
US5382579A (en) 1988-10-31 1995-01-17 Eisai Co., Ltd. Triazolo-1,4-diazepine derivatives and their use in pharmaceuticals
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
YU133090A (sh) 1989-07-12 1993-10-20 Boehringer Ingelheim Kg. Novi heteroazepini s paf-antaganostičnim učinkom in postopek za njihovo pripravo
JPH0374328A (ja) 1989-08-04 1991-03-28 Warner Lambert Co 薬学的活性を有する中枢コレシストキニン拮抗剤
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
JP2971902B2 (ja) 1990-03-15 1999-11-08 エーザイ株式会社 トリアゾロ―1,4―ジアゼピン系化合物
JP2971901B2 (ja) 1990-03-15 1999-11-08 エーザイ株式会社 トリアゾロ―1,4―ジアゼピン系化合物
WO1994006801A1 (en) 1990-05-23 1994-03-31 Yoshitomi Pharmaceutical Industries, Ltd. Thienodiazepine compound and medicinal use thereof
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
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
EP0523846A3 (en) 1991-06-14 1993-03-17 Merck & Co. Inc. 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
DE69131907T2 (de) 1991-09-30 2000-06-15 Yoshitomi Pharmaceutical Thienodiazepinverbindungen und ihre verwendung
CA2120939A1 (en) 1991-10-11 1993-04-15 Tetsuya Tahara Therapeutic agent for osteoporosis and diazepine compound
WO1993012117A1 (fr) 1991-12-11 1993-06-24 Yoshitomi Pharmaceutical Industries, Ltd. Agent immunosuppresseur
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
AU670431B2 (en) 1992-03-24 1996-07-18 Merck Sharp & Dohme Limited 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
WO1994022872A1 (en) 1993-03-30 1994-10-13 Yoshitomi Pharmaceutical Industries, Ltd. Cell adhesion inhibitor and thienotriazolodiazepine compound
AU6909194A (en) 1993-05-14 1994-12-12 Board Of Regents, The University Of Texas System Preparation of n-cyanodithioimino-carbonates and 3-mercapto-5-amino-1h-1,2,4-triazole
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
US5760031A (en) 1993-07-29 1998-06-02 American Cyanamid Company Tricyclic benzazepine vasopressin antagonists
US5679672A (en) 1993-11-22 1997-10-21 Merck & Co., Inc. Benzodiazepines
JP3290664B2 (ja) 1993-12-28 2002-06-10 明治製菓株式会社 3環性ベンゾアゼピンおよびベンゾチアゼピン誘導体
US5739129A (en) 1994-04-14 1998-04-14 Glaxo Wellcome Inc. CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
JPH09511998A (ja) 1994-04-15 1997-12-02 グラクソ、ウェルカム、インコーポレーテッド 1,4 − ベンゾジアゼピン化合物を用いたコレシストキニンアゴニスト活性の誘導方法
CN1121395C (zh) 1995-09-21 2003-09-17 药物分子设计研究所株式会社 类视色素作用增强性化合物
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.
WO1998028268A2 (en) 1996-12-23 1998-07-02 Elan Pharmaceuticals, Inc. CYCLOALKYL, LACTAM, LACTONE AND RELATED COMPOUNDS AS β-AMYLOID PEPTIDE RELEASE INHIBITORS
EP0995752A4 (en) 1997-06-25 2001-08-16 Nikken Chemicals Co Ltd TRIAZOLO-1,4-DIAZEPINE COMPOUNDS AND MEDICINAL COMPOSITION CONTAINING THEM
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
WO2000012547A2 (en) 1998-09-01 2000-03-09 Innogenetics N.V. Benzodiazepines and benzothiazepines 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
US7160880B1 (en) 1999-05-14 2007-01-09 Cenes Limited Short-acting benzodiazepines
GB9911152D0 (en) 1999-05-14 1999-07-14 Glaxo Group Ltd Short-acting benzodiazepines
JP2003518494A (ja) 1999-12-29 2003-06-10 グラクソ グループ リミテッド アネキシンおよび軟骨ホメオスタシスのモジュレーターに関係する方法と組成物
EP1297836A4 (en) 2000-06-16 2007-06-13 Mitsubishi Pharma Corp COMPOSITIONS FOR CHECKING RELEASE, PH AREA AND / OR SPEED
CA2446696A1 (fr) 2001-06-07 2002-12-12 Neuro3D Inhibiteurs des phosphodiesterases des nucleotides cycliques, preparation et utilisations de ces inhibiteurs
WO2003074525A1 (fr) 2002-03-01 2003-09-12 Yamanouchi Pharmaceutical Co., Ltd. Compose heterocyclique azote
AU2003288352A1 (en) 2002-10-30 2004-06-07 Centre National De La Recherche Scientifique (Cnrs) Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses
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
MXPA05006478A (es) 2002-12-18 2005-09-08 Vertex Pharma Triazolopiridazinas como inhibidores de proteinas cinasas.
WO2005002590A1 (ja) 2003-07-01 2005-01-13 Astellas Pharma Inc. 骨量増加誘導剤
US7119088B2 (en) 2003-02-19 2006-10-10 Pfizer Inc. Triazole compounds useful in therapy
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
CN101035450A (zh) 2004-10-05 2007-09-12 日本先锋公司 音频架
US8044042B2 (en) 2005-05-30 2011-10-25 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and medicinal use thereof
EP1912653B1 (en) 2005-07-29 2014-01-01 Merck Sharp & Dohme Corp. Heterocyclic benzodiazepine cgrp receptor antagonists
AU2006306347A1 (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
WO2008023847A1 (fr) 2006-08-25 2008-02-28 Nippon Chemiphar Co., Ltd. Antagoniste du récepteur p2x4
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
CN102123706B (zh) 2008-06-17 2013-08-14 米纳斯吉拉斯联合大学 血小板活化因子受体在治疗黄病毒科病毒引起的感染中的用途
CA2728830A1 (en) 2008-06-23 2010-01-21 Jean-Damien Charrier Protein kinase inhibitors
ES2448567T3 (es) 2008-10-30 2014-03-14 Circomed Llc Derivados de la tienotriazoldiazepina activos en apo A
US8604023B2 (en) 2009-04-17 2013-12-10 The Regents Of The University Of Michigan 1,4-benzodiazepinone compounds and their use in treating cancer
CN102482258B (zh) 2009-05-07 2014-06-25 株式会社棱镜制药 α-螺旋模拟物和与其相关的方法
KR101435729B1 (ko) 2009-09-28 2014-09-01 닛뽕소다 가부시키가이샤 함질소 헤테로 고리 화합물 및 그의 염, 그리고 농원예용 살균제
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
WO2011054851A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Novel process
AU2010314395B2 (en) 2009-11-05 2015-04-09 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
ES2564318T3 (es) 2009-11-05 2016-03-21 Glaxosmithkline Llc Inhibidor de bromodominio de benzodiazepina
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP2515914A4 (en) 2009-12-23 2013-09-11 Scripps Research Inst BIOCONJUGATION OF TYROSINE BY EYE REACTIONS IN AQUEOUS MEDIA
TW201201813A (en) 2010-03-31 2012-01-16 Arqule Inc Substituted benzo-pyrido-triazolo-diazepine compounds
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
EP2569434B1 (en) 2010-05-14 2019-09-04 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia and related disorders
HUE031073T2 (en) 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
US9301962B2 (en) 2010-05-14 2016-04-05 Baylor College Of Medicine Male contraceptive compositions and methods of use
ES2526671T3 (es) 2010-06-22 2015-01-14 Glaxosmithkline Llc Compuestos de benzotriazoldiazepina inhibidores de bromodominios
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
US9422292B2 (en) 2011-05-04 2016-08-23 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
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
TWI602820B (zh) * 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof

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