AU2016361441B2 - Bicyclic BET bromodomain inhibitors and uses thereof - Google Patents

Bicyclic BET bromodomain inhibitors and uses thereof Download PDF

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Publication number
AU2016361441B2
AU2016361441B2 AU2016361441A AU2016361441A AU2016361441B2 AU 2016361441 B2 AU2016361441 B2 AU 2016361441B2 AU 2016361441 A AU2016361441 A AU 2016361441A AU 2016361441 A AU2016361441 A AU 2016361441A AU 2016361441 B2 AU2016361441 B2 AU 2016361441B2
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Prior art keywords
dimethylisoxazol
quinazolin
chlorobenzyl
amino
methyl
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AU2016361441A1 (en
Inventor
Ajit Jadhav
David J. Maloney
Jeffrey William STROVEL
Daniel Jason URBAN
Shyh Ming YANG
Makoto Yoshioka
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ConverGene LLC
US Department of Health and Human Services
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ConverGene LLC
Government of the United States of America
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Priority to AU2024201890A priority patent/AU2024201890A1/en
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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)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Toxicology (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Hematology (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)
AU2016361441A 2015-11-25 2016-11-23 Bicyclic BET bromodomain inhibitors and uses thereof Active AU2016361441B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2021209257A AU2021209257B2 (en) 2015-11-25 2021-07-28 Bicyclic BET bromodomain inhibitors and uses thereof
AU2024201890A AU2024201890A1 (en) 2015-11-25 2024-03-22 Bicyclic BET bromodomain inhibitors and uses thereof

Applications Claiming Priority (3)

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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

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AU2016361441A1 AU2016361441A1 (en) 2018-06-21
AU2016361441B2 true AU2016361441B2 (en) 2021-08-12

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AU2021209257A Active AU2021209257B2 (en) 2015-11-25 2021-07-28 Bicyclic BET bromodomain inhibitors and uses thereof
AU2024201890A Pending AU2024201890A1 (en) 2015-11-25 2024-03-22 Bicyclic BET bromodomain inhibitors and uses thereof

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Country Status (8)

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US (2) US10508106B2 (OSRAM)
EP (2) EP3380469B1 (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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CN108314680A (zh) * 2017-01-16 2018-07-24 凯惠科技发展(上海)有限公司 一种含芳环化合物、其制备方法、药物组合物及应用
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
EP3620164A1 (en) * 2018-09-05 2020-03-11 Genoscience Pharma SAS Substituted 2,4 diamino-quinoline as new medicament for fibrosis, autophagy and cathepsins b (ctsb), l (ctsl) and d (ctsd) related diseases
EP4424379A3 (en) 2019-04-24 2024-10-30 Convergene Llc Small molecule bromodomain inhibitors and uses thereof
BR112021022099A2 (pt) * 2019-05-31 2021-12-28 Chiesi Farm Spa Derivados de amino quinazolina como inibidores de p2x3
BR112021020279A2 (pt) * 2019-05-31 2021-12-14 Chiesi Farm Spa Derivados de piridopirimidinas como inibidores de p2x3
WO2022083657A1 (zh) * 2020-10-20 2022-04-28 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
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
EP4291195A4 (en) * 2021-02-11 2025-07-09 Medical College Wisconsin Inc SMALL MOLECULE INHIBITORS OF PBRM1-BD2
WO2022199670A1 (zh) * 2021-03-26 2022-09-29 南京明德新药研发有限公司 6-氨基甲酸酯取代的杂芳环衍生物
WO2024043319A1 (ja) * 2022-08-26 2024-02-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 抗体薬物複合体
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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