TWI602820B - 溴域抑制劑及其用途 - Google Patents

溴域抑制劑及其用途 Download PDF

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Publication number
TWI602820B
TWI602820B TW102119106A TW102119106A TWI602820B TW I602820 B TWI602820 B TW I602820B TW 102119106 A TW102119106 A TW 102119106A TW 102119106 A TW102119106 A TW 102119106A TW I602820 B TWI602820 B TW I602820B
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TW
Taiwan
Prior art keywords
cancer
compound
group
methyl
mmol
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TW102119106A
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English (en)
Chinese (zh)
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TW201402580A (zh
Inventor
布萊恩Ｋ 艾爾布列希
麥可 查爾斯 希威特
維克特Ｓ 吉林
李希Ｇ 瓦思瓦尼
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星宿藥物公司
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    • 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
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW102119106A 2012-06-06 2013-05-30 溴域抑制劑及其用途 TWI602820B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261656205P 2012-06-06 2012-06-06

Publications (2)

Publication Number Publication Date
TW201402580A TW201402580A (zh) 2014-01-16
TWI602820B true TWI602820B (zh) 2017-10-21

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
TW102119106A TWI602820B (zh) 2012-06-06 2013-05-30 溴域抑制劑及其用途

Country Status (19)

Country Link
US (2) US9493483B2 (OSRAM)
EP (1) EP2859000B1 (OSRAM)
JP (1) JP6154004B2 (OSRAM)
KR (1) KR20150023562A (OSRAM)
CN (1) CN104428304B (OSRAM)
AR (1) AR091285A1 (OSRAM)
AU (1) AU2013271569B2 (OSRAM)
BR (1) BR112014030165A2 (OSRAM)
CA (1) CA2874774C (OSRAM)
EA (1) EA026894B1 (OSRAM)
ES (1) ES2632774T3 (OSRAM)
IL (1) IL235844A (OSRAM)
IN (1) IN2014DN10386A (OSRAM)
MX (1) MX360598B (OSRAM)
NZ (1) NZ702458A (OSRAM)
SG (1) SG11201407900WA (OSRAM)
TW (1) TWI602820B (OSRAM)
WO (1) WO2013184876A1 (OSRAM)
ZA (1) ZA201408720B (OSRAM)

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WO2013184878A1 (en) 2012-06-06 2013-12-12 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
CN105263919A (zh) 2013-02-19 2016-01-20 拜耳医药股份有限公司 二环2,3-苯并二氮杂*和螺环取代的2,3-苯并二氮杂*
JP2016513117A (ja) 2013-02-22 2016-05-12 バイエル ファーマ アクチエンゲゼルシャフト 過剰増殖性疾患を治療するためのｂｅｔタンパク質阻害剤としてのピロロ−およびピラゾロ−トリアゾロジアゼピン類
WO2014128111A1 (de) 2013-02-22 2014-08-28 Bayer Pharma Aktiengesellschaft 4-substituierte pyrrolo- und pyrazolo-diazepine
ES2909778T3 (es) 2013-03-15 2022-05-10 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de proteína BET para su uso en el tratamiento de una enfermedad proliferativa en combinación con un inhibidor de Janus quinasas
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein 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
SG10201809353TA (en) 2014-04-23 2018-11-29 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
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
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
AR105124A1 (es) 2015-06-26 2017-09-06 Tensha Therapeutics Inc Tratamiento de carcinoma de la línea media nut
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
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
EP3397640B1 (en) 2015-12-29 2021-08-04 INSERM - Institut National de la Santé et de la Recherche Médicale Xanthine derivative inhibitors of bet proteins
TWI830533B (zh) 2016-06-20 2024-01-21 美商英塞特公司 Ｂｅｔ抑制劑之結晶固體形式
US20180325931A1 (en) 2017-01-21 2018-11-15 Ningbo Zhiming Biotechnology Co., Ltd. Use of paeoniflorin-6'-o-benzenesulfonate in treatment of sjögren's syndrome
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
KR102026243B1 (ko) * 2018-01-19 2019-09-27 연세대학교 산학협력단 백혈병 치료용 약학적 조성물
SI3778573T1 (sl) 2018-03-30 2024-08-30 Kyowa Kirin Co., Ltd., Spojina s protirakavim delovanjem
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
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

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