KR102830237B1 - Bcl6 저해제 - Google Patents

Bcl6 저해제 Download PDF

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Publication number
KR102830237B1
KR102830237B1 KR1020207032149A KR20207032149A KR102830237B1 KR 102830237 B1 KR102830237 B1 KR 102830237B1 KR 1020207032149 A KR1020207032149 A KR 1020207032149A KR 20207032149 A KR20207032149 A KR 20207032149A KR 102830237 B1 KR102830237 B1 KR 102830237B1
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amino
chloro
oxazepino
quinolin
methyl
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KR20200144109A (ko
Inventor
벤자민 리처드 벨레니
콰이 밍 잭 청
오웬 알렉산더 데이비스
스벤 횔더
로즈마리 후크베일
게빈 콜리
미르코 메니코니
알피 브렌넨
매튜 가쓰 로이드
Original Assignee
캔써 리서치 테크놀로지 리미티드
디 인스티튜트 오브 캔서 리서치:로얄 캔서 하스피틀
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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 캔써 리서치 테크놀로지 리미티드, 디 인스티튜트 오브 캔서 리서치:로얄 캔서 하스피틀 filed Critical 캔써 리서치 테크놀로지 리미티드
Priority to KR1020257022060A priority Critical patent/KR20250105504A/ko
Publication of KR20200144109A publication Critical patent/KR20200144109A/ko
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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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/54Heterocyclic 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
    • A61K31/542Heterocyclic 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
    • 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
    • A61K31/553Heterocyclic 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
    • 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
    • A61K31/554Heterocyclic 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
    • 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
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • 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
    • C07D498/08Bridged systems
    • 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
    • C07D498/12Heterocyclic 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
    • C07D498/14Ortho-condensed systems
    • 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
    • C07D498/12Heterocyclic 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
    • C07D498/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
KR1020207032149A 2018-04-13 2019-04-12 Bcl6 저해제 Active KR102830237B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020257022060A KR20250105504A (ko) 2018-04-13 2019-04-12 Bcl6 저해제

Applications Claiming Priority (5)

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

Related Child Applications (1)

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KR1020257022060A Division KR20250105504A (ko) 2018-04-13 2019-04-12 Bcl6 저해제

Publications (2)

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KR20200144109A KR20200144109A (ko) 2020-12-28
KR102830237B1 true KR102830237B1 (ko) 2025-07-07

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KR1020207032149A Active KR102830237B1 (ko) 2018-04-13 2019-04-12 Bcl6 저해제
KR1020257022060A Pending KR20250105504A (ko) 2018-04-13 2019-04-12 Bcl6 저해제

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Country Status (16)

Country Link
US (3) US11512095B2 (https=)
EP (3) EP4729127A2 (https=)
JP (2) JP7493454B2 (https=)
KR (2) KR102830237B1 (https=)
CN (2) CN119330979A (https=)
AU (2) AU2019253510B2 (https=)
BR (1) BR112020020832A2 (https=)
CA (1) CA3095371A1 (https=)
DK (1) DK3774817T3 (https=)
ES (2) ES3060268T3 (https=)
HR (1) HRP20230120T1 (https=)
IL (2) IL296734B2 (https=)
MX (2) MX2020010805A (https=)
PT (1) PT3774817T (https=)
SG (1) SG11202009735QA (https=)
WO (1) WO2019197842A1 (https=)

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CN115397821B (zh) * 2019-10-17 2024-09-03 阿尔维纳斯运营股份有限公司 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子
CN117279910A (zh) 2021-04-16 2023-12-22 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
MA69177B1 (fr) 2022-06-06 2026-03-31 Treeline Biosciences, Inc. Agents de dégradation bifonctionnels de quinolone-bcl6 tricycliques
EP4536658A1 (en) 2022-06-13 2025-04-16 Treeline Biosciences, Inc. 1,8-naphthyridin-2-one heterobifunctional bcl6 degraders
WO2023244918A1 (en) 2022-06-13 2023-12-21 Treeline Biosciences, Inc. Quinolone bcl6 bifunctional degraders
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
WO2025050016A1 (en) * 2023-09-01 2025-03-06 Treeline Biosciences, Inc. Tricyclic quinolone bcl6 bifunctional degraders
WO2025049964A1 (en) * 2023-09-01 2025-03-06 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

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WO2014135474A1 (en) 2013-03-05 2014-09-12 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
WO2014204859A2 (en) 2013-06-17 2014-12-24 Melnick Ari Bcl6 inhibitors as anticancer agents
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WO2018215798A1 (en) 2017-05-26 2018-11-29 Cancer Research Technology Limited 2-quinolone derived inhibitors of bcl6

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DK3774817T3 (da) 2023-02-13
JP2021521165A (ja) 2021-08-26
AU2023263501A1 (en) 2023-11-30
ES2939776T3 (es) 2023-04-26
IL277778A (en) 2020-11-30
IL296734B1 (en) 2025-02-01
MX2020010805A (es) 2021-01-29
US12486285B2 (en) 2025-12-02
EP4201939B1 (en) 2025-12-31
IL296734A (en) 2022-11-01
PT3774817T (pt) 2023-03-09
AU2019253510B2 (en) 2023-08-10
US20260042776A1 (en) 2026-02-12
JP2024119835A (ja) 2024-09-03
CN112334475A (zh) 2021-02-05
EP3774817B1 (en) 2022-12-07
IL277778B (en) 2022-11-01
KR20200144109A (ko) 2020-12-28
HRP20230120T1 (hr) 2023-06-09
EP4201939C0 (en) 2025-12-31
IL277778B2 (en) 2023-03-01
EP4201939A1 (en) 2023-06-28
EP4729127A2 (en) 2026-04-22
JP7493454B2 (ja) 2024-05-31
AU2019253510A1 (en) 2020-10-22
US20210163497A1 (en) 2021-06-03
MX2023004920A (es) 2023-05-16
KR20250105504A (ko) 2025-07-08
US20230287003A1 (en) 2023-09-14
US11512095B2 (en) 2022-11-29
CN112334475B (zh) 2024-10-29
SG11202009735QA (en) 2020-10-29
AU2023263501B2 (en) 2026-01-08
BR112020020832A2 (pt) 2021-01-19
EP3774817A1 (en) 2021-02-17
IL296734B2 (en) 2025-06-01
WO2019197842A1 (en) 2019-10-17
ES3060268T3 (en) 2026-03-25
CA3095371A1 (en) 2019-10-17
CN119330979A (zh) 2025-01-21

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