CA3006300C - Bicyclic bet bromodomain inhibitors and uses thereof - Google Patents

Bicyclic bet bromodomain inhibitors and uses thereof Download PDF

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Publication number
CA3006300C
CA3006300C CA3006300A CA3006300A CA3006300C CA 3006300 C CA3006300 C CA 3006300C CA 3006300 A CA3006300 A CA 3006300A CA 3006300 A CA3006300 A CA 3006300A CA 3006300 C CA3006300 C CA 3006300C
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alkyl
membered
heteroaryl
optionally
group
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French (fr)
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CA3006300A1 (en
Inventor
Jeffrey William STROVEL
Makoto Yoshioka
David J. Maloney
Shyh Ming YANG
Ajit Jadhav
Daniel Jason URBAN
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ConverGene LLC
US Department of Health and Human Services
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ConverGene LLC
US Department of Health and Human Services
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P39/00—General protective or antinoxious agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Toxicology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyridine Compounds (AREA)
CA3006300A 2015-11-25 2016-11-23 Bicyclic bet bromodomain inhibitors and uses thereof Active CA3006300C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562259894P 2015-11-25 2015-11-25
US62/259,894 2015-11-25
PCT/US2016/063485 WO2017091661A1 (en) 2015-11-25 2016-11-23 Bicyclic bet bromodomain inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
CA3006300A1 CA3006300A1 (en) 2017-06-01
CA3006300C true CA3006300C (en) 2024-02-27

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CA3006300A Active CA3006300C (en) 2015-11-25 2016-11-23 Bicyclic bet bromodomain inhibitors and uses thereof

Country Status (8)

Country Link
US (2) US10508106B2 (OSRAM)
EP (2) EP4050005B1 (OSRAM)
JP (2) JP6882289B2 (OSRAM)
CN (2) CN109641886B (OSRAM)
AU (3) AU2016361441B2 (OSRAM)
CA (1) CA3006300C (OSRAM)
ES (2) ES2918589T3 (OSRAM)
WO (1) WO2017091661A1 (OSRAM)

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CN109111426B (zh) * 2017-06-23 2021-12-14 中国科学院上海药物研究所 一类稠合双环杂芳基或芳基化合物，及其用途
WO2019201296A1 (zh) * 2018-04-18 2019-10-24 南京明德新药研发有限公司 作为rho激酶抑制剂的吡唑类化合物
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CN117279914A (zh) * 2021-01-29 2023-12-22 南京再明医药有限公司 Sos1抑制剂及其制备方法和应用
WO2022171018A1 (zh) * 2021-02-09 2022-08-18 苏州泽璟生物制药股份有限公司 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用
CA3211053A1 (en) * 2021-02-11 2022-08-18 The Medical College Of Wisconsin, Inc. Small molecule inhibitors of pbrm1-bd2
JP2024511507A (ja) * 2021-03-26 2024-03-13 メッドシャイン ディスカバリー インコーポレイテッド ６－カルバメート置換複素芳香環誘導体
TW202416953A (zh) * 2022-08-26 2024-05-01 日商衛材R&D企管股份有限公司 抗體藥物複合物
WO2024235225A1 (zh) * 2023-05-15 2024-11-21 苏州泽璟生物制药股份有限公司 取代嘧啶并环类抑制剂及其制备方法和应用
WO2025209570A1 (zh) * 2024-04-03 2025-10-09 北京大学 Bet抑制剂及其应用

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Also Published As

Publication number Publication date
AU2016361441B2 (en) 2021-08-12
CN115806550B (zh) 2025-11-28
CA3006300A1 (en) 2017-06-01
ES2918589T3 (es) 2022-07-19
US20200223836A1 (en) 2020-07-16
AU2016361441A1 (en) 2018-06-21
CN109641886A (zh) 2019-04-16
JP7112567B2 (ja) 2022-08-03
US11028079B2 (en) 2021-06-08
CN109641886B (zh) 2022-11-18
JP2019501140A (ja) 2019-01-17
AU2021209257A1 (en) 2021-08-19
WO2017091661A1 (en) 2017-06-01
EP4050005B1 (en) 2024-12-25
AU2024201890A1 (en) 2024-05-16
AU2021209257B2 (en) 2023-12-21
JP6882289B2 (ja) 2021-06-02
ES3011058T3 (en) 2025-04-07
CN115806550A (zh) 2023-03-17
US10508106B2 (en) 2019-12-17
EP3380469A1 (en) 2018-10-03
JP2021119188A (ja) 2021-08-12
US20180305344A1 (en) 2018-10-25
EP3380469B1 (en) 2022-03-16
EP4050005A1 (en) 2022-08-31

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