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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Prior art keywords
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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    • 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)
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
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
KR1020257022060A Division KR20250105504A (ko) 2018-04-13 2019-04-12 Bcl6 저해제

Publications (2)

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

Family

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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

Family Applications After (1)

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

Country Status (16)

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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
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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
WO2026128853A1 (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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WO2001094341A1 (en) 2000-06-06 2001-12-13 Astrazeneca Ab Quinazoline derivatives for the treatment of tumours
WO2014135474A1 (en) 2013-03-05 2014-09-12 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
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WO2018215801A1 (en) 2017-05-26 2018-11-29 Cancer Research Technology Limited Benzimidazolone derived inhibitors 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
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
JP7493454B2 (ja) 2024-05-31
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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