JP7129973B2 - ブロモドメイン阻害剤 - Google Patents

ブロモドメイン阻害剤 Download PDF

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Publication number
JP7129973B2
JP7129973B2 JP2019521064A JP2019521064A JP7129973B2 JP 7129973 B2 JP7129973 B2 JP 7129973B2 JP 2019521064 A JP2019521064 A JP 2019521064A JP 2019521064 A JP2019521064 A JP 2019521064A JP 7129973 B2 JP7129973 B2 JP 7129973B2
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Prior art keywords
pharmaceutical composition
compound
cancer
methylisoquinolin
methylsulfonylphenyl
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JP2019521064A
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Japanese (ja)
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JP2019535671A (ja
JP2019535671A5 (zh
Inventor
ジュアン マヌエル ベタンコート
ジェフリー アラン スタッフォード
ライアン スタンフィールド
ジェームズ マーヴィン ヴィール
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セルジーン クオンティセル リサーチ,インク.
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Publication of JP2019535671A publication Critical patent/JP2019535671A/ja
Publication of JP2019535671A5 publication Critical patent/JP2019535671A5/ja
Priority to JP2022066855A priority Critical patent/JP2022095897A/ja
Application granted granted Critical
Publication of JP7129973B2 publication Critical patent/JP7129973B2/ja
Priority to JP2024021416A priority patent/JP2024056905A/ja
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    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • A61K9/1694Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24Oxygen atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
JP2019521064A 2016-10-20 2017-10-19 ブロモドメイン阻害剤 Active JP7129973B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2022066855A JP2022095897A (ja) 2016-10-20 2022-04-14 ブロモドメイン阻害剤
JP2024021416A JP2024056905A (ja) 2016-10-20 2024-02-15 ブロモドメイン阻害剤

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662410756P 2016-10-20 2016-10-20
US62/410,756 2016-10-20
PCT/US2017/057439 WO2018075796A1 (en) 2016-10-20 2017-10-19 Bromodomain inhibitor

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2022066855A Division JP2022095897A (ja) 2016-10-20 2022-04-14 ブロモドメイン阻害剤

Publications (3)

Publication Number Publication Date
JP2019535671A JP2019535671A (ja) 2019-12-12
JP2019535671A5 JP2019535671A5 (zh) 2020-10-22
JP7129973B2 true JP7129973B2 (ja) 2022-09-02

Family

ID=62019669

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2019521064A Active JP7129973B2 (ja) 2016-10-20 2017-10-19 ブロモドメイン阻害剤
JP2022066855A Pending JP2022095897A (ja) 2016-10-20 2022-04-14 ブロモドメイン阻害剤
JP2024021416A Pending JP2024056905A (ja) 2016-10-20 2024-02-15 ブロモドメイン阻害剤

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2022066855A Pending JP2022095897A (ja) 2016-10-20 2022-04-14 ブロモドメイン阻害剤
JP2024021416A Pending JP2024056905A (ja) 2016-10-20 2024-02-15 ブロモドメイン阻害剤

Country Status (7)

Country Link
EP (1) EP3528810A4 (zh)
JP (3) JP7129973B2 (zh)
CN (1) CN110099685A (zh)
AR (1) AR109859A1 (zh)
AU (1) AU2017345468B2 (zh)
TW (1) TW201821062A (zh)
WO (1) WO2018075796A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10702517B2 (en) 2015-04-22 2020-07-07 Celgene Quanticel Research, Inc. Bromodomain inhibitor
TW201642860A (zh) * 2015-04-22 2016-12-16 塞爾基因定量細胞研究公司 布羅莫結構域抑制劑
BR112021001019A2 (pt) * 2018-07-23 2021-04-13 Celgene Quanticel Research, Inc. Processo para a preparação de inibidor de bromodomínio

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015058160A1 (en) 2013-10-18 2015-04-23 Quanticel Pharmaceuticals, Inc. Bromodomain inhibitors
WO2015078929A1 (en) 2013-11-27 2015-06-04 Oncoethix Sa Method of treating leukemia using pharmaceutical formulation containing thienotriazolodiazepine compounds
JP2016529246A (ja) 2013-08-06 2016-09-23 オンコエシックス ゲーエムベーハー Betブロモドメイン阻害剤を用いるびまん性大細胞型b細胞性リンパ腫(dlbcl)の治療方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ20022332A3 (cs) * 2000-01-07 2003-01-15 Transform Pharmaceuticals, Inc. Sestava vzorků
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US9884806B2 (en) * 2013-08-30 2018-02-06 Icahn School Of Medicine At Mount Sinai Cyclic vinylogous amides as bromodomain inhibitors
TW201642860A (zh) * 2015-04-22 2016-12-16 塞爾基因定量細胞研究公司 布羅莫結構域抑制劑
CN105732624B (zh) * 2016-01-28 2019-08-02 中国药科大学 吡咯[4,3,2-de]喹啉-2(1H)-酮类BRD4蛋白抑制剂的制备方法及其用途

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016529246A (ja) 2013-08-06 2016-09-23 オンコエシックス ゲーエムベーハー Betブロモドメイン阻害剤を用いるびまん性大細胞型b細胞性リンパ腫(dlbcl)の治療方法
WO2015058160A1 (en) 2013-10-18 2015-04-23 Quanticel Pharmaceuticals, Inc. Bromodomain inhibitors
WO2015078929A1 (en) 2013-11-27 2015-06-04 Oncoethix Sa Method of treating leukemia using pharmaceutical formulation containing thienotriazolodiazepine compounds

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
森部久仁一、山本恵司,非晶質医薬品の調製と評価,低温生物工学会誌,2005年,Vol.51, No.1,p.19-24
難水溶性薬物の経口製剤化技術最前線,株式会社シーエムシー出版,2016年07月,p.64,127-135

Also Published As

Publication number Publication date
JP2022095897A (ja) 2022-06-28
AU2017345468A1 (en) 2019-06-06
AU2017345468B2 (en) 2022-06-02
WO2018075796A1 (en) 2018-04-26
JP2019535671A (ja) 2019-12-12
AR109859A1 (es) 2019-01-30
CN110099685A (zh) 2019-08-06
EP3528810A4 (en) 2020-06-17
TW201821062A (zh) 2018-06-16
EP3528810A1 (en) 2019-08-28
JP2024056905A (ja) 2024-04-23

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