CA2874774C - Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof - Google Patents

Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof Download PDF

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Publication number
CA2874774C
CA2874774C CA2874774A CA2874774A CA2874774C CA 2874774 C CA2874774 C CA 2874774C CA 2874774 A CA2874774 A CA 2874774A CA 2874774 A CA2874774 A CA 2874774A CA 2874774 C CA2874774 C CA 2874774C
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cancer
compound
alkyl
pharmaceutically acceptable
mmol
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French (fr)
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CA2874774A1 (en
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Brian K. Albrecht
Michael Charles Hewitt
Victor S. Gehling
Rishi G. Vaswani
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Constellation Pharmaceuticals Inc
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Constellation Pharmaceuticals Inc
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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
    • 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
    • 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
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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

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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)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Hematology (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)
CA2874774A 2012-06-06 2013-06-06 Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof Active CA2874774C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261656205P 2012-06-06 2012-06-06
US61/656,205 2012-06-06
PCT/US2013/044444 WO2013184876A1 (en) 2012-06-06 2013-06-06 Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
CA2874774A1 CA2874774A1 (en) 2013-12-12
CA2874774C true CA2874774C (en) 2022-10-04

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CA2874774A Active CA2874774C (en) 2012-06-06 2013-06-06 Benzo [c] isoxazoloazepine bromodomain inhibitors and uses thereof

Country Status (19)

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

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EP2864336B1 (en) 2012-06-06 2016-11-23 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
JP2016511247A (ja) 2013-02-19 2016-04-14 バイエル ファーマ アクチエンゲゼルシャフト ビシクロ2,3−ベンゾジアゼピン類及びスピロ環式置換2,3−ベンゾジアゼピン類
US20150376196A1 (en) 2013-02-22 2015-12-31 Bayer Pharma Aktiengesellschaft 4-substituted pyrrolo- and pyrazolo-diazepines
CN105189514A (zh) 2013-02-22 2015-12-23 拜耳医药股份有限公司 作为bet-蛋白抑制剂用于治疗过度增殖性疾病的吡咯并-和吡唑并-三唑并二氮杂卓
ES2755827T3 (es) 2013-03-15 2020-04-23 Incyte Holdings Corp Heterciclos tricíclicos como inhibidores de proteína BET
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EP3125896A2 (en) * 2014-04-04 2017-02-08 Constellation Pharmaceuticals, Inc. EXPRESSION LEVELS OF BCL-xL, BCL2, BCL-w, AND BAD AND CANCER THERAPIES
RS64231B1 (sr) 2014-04-23 2023-06-30 Incyte Holdings Corp 1h-pirolo[2,3-c]piridin-7(6h)-on i pirazolo[3,4-c]piridin-7(6h)-on kao inhibitori bet proteina
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
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
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
RS61803B1 (sr) * 2015-09-09 2021-06-30 Jubilant Biosys Ltd Triciklični fuzioni piridin-2-on derivati i njihova upotreba kao inhibitora brd4
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
WO2017114843A1 (en) 2015-12-29 2017-07-06 INSERM (Institut National de la Santé et de la Recherche Médicale) Xanthine derivative inhibitors of bet proteins
PE20190623A1 (es) 2016-06-20 2019-04-26 Incyte Corp Formas solidas cristalinas de un inhibidor de bet
WO2018133139A1 (zh) 2017-01-21 2018-07-26 宁波知明生物科技有限公司 芍药苷-6'-o-苯磺酸酯在治疗干燥综合征的应用
CA3081753A1 (en) 2017-11-06 2019-05-09 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
US11629152B2 (en) 2018-03-30 2023-04-18 Kyowa Kirin Co., Ltd. Compound with anticancer activity
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
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