JP7493454B2 - Bcl6阻害剤 - Google Patents

Bcl6阻害剤 Download PDF

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Publication number
JP7493454B2
JP7493454B2 JP2020555420A JP2020555420A JP7493454B2 JP 7493454 B2 JP7493454 B2 JP 7493454B2 JP 2020555420 A JP2020555420 A JP 2020555420A JP 2020555420 A JP2020555420 A JP 2020555420A JP 7493454 B2 JP7493454 B2 JP 7493454B2
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Prior art keywords
amino
chloro
oxazepino
quinolin
methyl
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Japanese (ja)
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JP2021521165A5 (enExample
JP2021521165A (ja
Inventor
ベンジャミン・リチャード・ベレニー
クワイ・ミン・ジャック・チュン
オーウェン・アレクサンダー・デイビス
スウェン・ヘルダー
ローズマリー・ハックベイル
ギャビン・コリー
ミルコ・メニコーニ
アルフィー・ブレナン
マシュー・ガース・ロイド
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The Institute of Cancer Research: Royal Cancer Hospital
Cancer Research Technology Ltd
Original Assignee
The Institute of Cancer Research: Royal Cancer Hospital
Cancer Research Technology Ltd
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Priority claimed from GBGB1806132.5A external-priority patent/GB201806132D0/en
Priority claimed from GBGB1819136.1A external-priority patent/GB201819136D0/en
Application filed by The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Ltd filed Critical The Institute of Cancer Research: Royal Cancer Hospital
Publication of JP2021521165A publication Critical patent/JP2021521165A/ja
Publication of JP2021521165A5 publication Critical patent/JP2021521165A5/ja
Priority to JP2024082277A priority Critical patent/JP7855637B2/ja
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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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D498/08—Bridged systems
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/14—Ortho-condensed systems
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2020555420A 2018-04-13 2019-04-12 Bcl6阻害剤 Active JP7493454B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024082277A JP7855637B2 (ja) 2018-04-13 2024-05-21 Bcl6阻害剤

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB1806132.5A GB201806132D0 (en) 2018-04-13 2018-04-13 Inhibitor coumpounds
GB1806132.5 2018-04-13
GBGB1819136.1A GB201819136D0 (en) 2018-11-23 2018-11-23 Inhibitor compounds
GB1819136.1 2018-11-23
PCT/GB2019/051058 WO2019197842A1 (en) 2018-04-13 2019-04-12 Bcl6 inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2024082277A Division JP7855637B2 (ja) 2018-04-13 2024-05-21 Bcl6阻害剤

Publications (3)

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JP2021521165A JP2021521165A (ja) 2021-08-26
JP2021521165A5 JP2021521165A5 (enExample) 2022-02-07
JP7493454B2 true JP7493454B2 (ja) 2024-05-31

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JP2020555420A Active JP7493454B2 (ja) 2018-04-13 2019-04-12 Bcl6阻害剤
JP2024082277A Active JP7855637B2 (ja) 2018-04-13 2024-05-21 Bcl6阻害剤

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US (3) US11512095B2 (enExample)
EP (3) EP3774817B1 (enExample)
JP (2) JP7493454B2 (enExample)
KR (2) KR102830237B1 (enExample)
CN (2) CN119330979A (enExample)
AU (2) AU2019253510B2 (enExample)
BR (1) BR112020020832A2 (enExample)
CA (1) CA3095371A1 (enExample)
DK (1) DK3774817T3 (enExample)
ES (2) ES2939776T3 (enExample)
HR (1) HRP20230120T1 (enExample)
IL (2) IL296734B2 (enExample)
MX (2) MX2020010805A (enExample)
PT (1) PT3774817T (enExample)
SG (1) SG11202009735QA (enExample)
WO (1) WO2019197842A1 (enExample)

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CN118388454A (zh) 2021-04-16 2024-07-26 阿尔维纳斯运营股份有限公司 Bcl6蛋白水解的调节剂和其相关使用方法
CA3251059A1 (en) 2022-05-02 2023-11-09 The Board Of Trustees Of The Leland Stanford Junior University Compositions, systems and methods for modulating a target gene
WO2023240038A1 (en) 2022-06-06 2023-12-14 Treeline Biosciences, Inc. Tricyclic quinolone bcl6 bifunctional degraders
AU2023295387A1 (en) 2022-06-13 2025-01-09 Treeline Biosciences, Inc. 1,8-naphthyridin-2-one heterobifunctional bcl6 degraders
KR20250023483A (ko) 2022-06-13 2025-02-18 트리라인 바이오사이언시스, 인크. 퀴놀론 bcl6 이작용성 분해제
EP4558487A1 (en) * 2022-07-19 2025-05-28 Dana-Farber Cancer Institute, Inc. Quinoxalinedione and pyrido [2, 3-b]pyrazine-2, 3-dione b cell lymphoma 6 (bcl6) degraders and uses thereof
WO2024193464A1 (zh) * 2023-03-17 2024-09-26 西藏海思科制药有限公司 一种含氮三并环衍生物及其在医药上的应用
TW202525814A (zh) * 2023-09-01 2025-07-01 美商樹線生物科學公司 三環喹啉酮bcl6雙功能降解劑
AU2024331602A1 (en) * 2023-09-01 2026-03-19 Treeline Biosciences, Inc. Bcl6 bifunctional degraders
CN120987969A (zh) * 2024-05-21 2025-11-21 中国药科大学 一类蛋白靶向降解嵌合体及其用途
WO2026128820A1 (en) * 2024-12-13 2026-06-18 Treeline Biosciences, Inc. Methods of treating cancer using an ezh2 inhibitor and a tricyclic quinolone heterobifunctional degrader of bcl6
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CN119330979A (zh) 2025-01-21
IL277778B2 (en) 2023-03-01
CN112334475A (zh) 2021-02-05
JP7855637B2 (ja) 2026-05-08
EP3774817A1 (en) 2021-02-17
DK3774817T3 (da) 2023-02-13
JP2024119835A (ja) 2024-09-03
EP4729127A2 (en) 2026-04-22
AU2023263501B2 (en) 2026-01-08
PT3774817T (pt) 2023-03-09
WO2019197842A1 (en) 2019-10-17
SG11202009735QA (en) 2020-10-29
AU2023263501A1 (en) 2023-11-30
US20230287003A1 (en) 2023-09-14
HRP20230120T1 (hr) 2023-06-09
KR102830237B1 (ko) 2025-07-07
US12486285B2 (en) 2025-12-02
EP4201939C0 (en) 2025-12-31
IL296734B2 (en) 2025-06-01
ES2939776T3 (es) 2023-04-26
US20260042776A1 (en) 2026-02-12
BR112020020832A2 (pt) 2021-01-19
EP4729127A3 (en) 2026-08-12
US20210163497A1 (en) 2021-06-03
MX2023004920A (es) 2023-05-16
AU2019253510B2 (en) 2023-08-10
JP2021521165A (ja) 2021-08-26
IL296734A (en) 2022-11-01
MX2020010805A (es) 2021-01-29
KR20250105504A (ko) 2025-07-08
US11512095B2 (en) 2022-11-29
IL296734B1 (en) 2025-02-01
EP4201939A1 (en) 2023-06-28
KR20200144109A (ko) 2020-12-28
AU2019253510A1 (en) 2020-10-22
CA3095371A1 (en) 2019-10-17
EP3774817B1 (en) 2022-12-07
EP4201939B1 (en) 2025-12-31
ES3060268T3 (en) 2026-03-25
IL277778B (en) 2022-11-01
CN112334475B (zh) 2024-10-29
IL277778A (en) 2020-11-30

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