CN112334475B - Bcl6抑制剂 - Google Patents

Bcl6抑制剂 Download PDF

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Publication number
CN112334475B
CN112334475B CN201980039513.4A CN201980039513A CN112334475B CN 112334475 B CN112334475 B CN 112334475B CN 201980039513 A CN201980039513 A CN 201980039513A CN 112334475 B CN112334475 B CN 112334475B
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Prior art keywords
amino
chloro
quinolin
methyl
oxazepine
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CN201980039513.4A
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Chinese (zh)
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CN112334475A (zh
Inventor
本杰明·理查德·贝莱妮
贵明·杰克·张
欧文·亚历山大·戴维斯
斯文·霍尔德
罗斯玛丽·哈克威尔
加文·柯利
米尔科·梅尼科尼
阿尔菲·布伦南
马修·加思·劳埃德
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Cancer Research Institute Royal Cancer Hospital
Cancer Research Technology Ltd
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Cancer Research Institute 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 Cancer Research Institute Royal Cancer Hospital, Cancer Research Technology Ltd filed Critical Cancer Research Institute Royal Cancer Hospital
Priority to CN202411445401.8A priority Critical patent/CN119330979A/zh
Publication of CN112334475A publication Critical patent/CN112334475A/zh
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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)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
CN201980039513.4A 2018-04-13 2019-04-12 Bcl6抑制剂 Active CN112334475B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202411445401.8A CN119330979A (zh) 2018-04-13 2019-04-12 作为bcl6抑制剂的化合物及其制备方法

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
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
CN202411445401.8A Division CN119330979A (zh) 2018-04-13 2019-04-12 作为bcl6抑制剂的化合物及其制备方法

Publications (2)

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CN112334475A CN112334475A (zh) 2021-02-05
CN112334475B true CN112334475B (zh) 2024-10-29

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CN201980039513.4A Active CN112334475B (zh) 2018-04-13 2019-04-12 Bcl6抑制剂
CN202411445401.8A Pending CN119330979A (zh) 2018-04-13 2019-04-12 作为bcl6抑制剂的化合物及其制备方法

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Country Status (16)

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US (3) US11512095B2 (OSRAM)
EP (3) EP4729127A2 (OSRAM)
JP (2) JP7493454B2 (OSRAM)
KR (2) KR20250105504A (OSRAM)
CN (2) CN112334475B (OSRAM)
AU (2) AU2019253510B2 (OSRAM)
BR (1) BR112020020832A2 (OSRAM)
CA (1) CA3095371A1 (OSRAM)
DK (1) DK3774817T3 (OSRAM)
ES (2) ES2939776T3 (OSRAM)
HR (1) HRP20230120T1 (OSRAM)
IL (2) IL296734B2 (OSRAM)
MX (2) MX2020010805A (OSRAM)
PT (1) PT3774817T (OSRAM)
SG (1) SG11202009735QA (OSRAM)
WO (1) WO2019197842A1 (OSRAM)

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GB201914860D0 (en) * 2019-10-14 2019-11-27 Cancer Research Tech Ltd Inhibitor compounds
US12310975B2 (en) * 2019-10-17 2025-05-27 Arvinas Operations, Inc. Modulators of BCL6 proteolysis and associated methods of use
CA3214806A1 (en) 2021-04-16 2022-10-20 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
CR20250001A (es) 2022-06-06 2025-05-14 Treeline Biosciences Inc Degradadores bifuncionales de bcl6 de quinolona tricíclica
JP2025525324A (ja) 2022-06-13 2025-08-05 ツリーライン バイオサイエンシズ インコーポレイテッド 1,8-ナフチリジン-2-オンヘテロ二官能性bcl6分解剤
AU2023292893A1 (en) 2022-06-13 2025-01-02 Treeline Biosciences, Inc. Quinolone bcl6 bifunctional degraders
JP2025524835A (ja) * 2022-07-19 2025-08-01 ダナ-ファーバー キャンサー インスティテュート,インコーポレイテッド キノキサリンジオンおよびピリド[2,3-b]ピラジン-2,3-ジオンb細胞リンパ腫6(bcl6)分解剤ならびにその使用
CN120813582A (zh) * 2023-03-17 2025-10-17 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
WO2025049964A1 (en) * 2023-09-01 2025-03-06 Treeline Biosciences, Inc. Bcl6 bifunctional degraders
AU2024331309A1 (en) * 2023-09-01 2026-03-19 Treeline Biosciences, Inc. Tricyclic quinolone 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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HRP20230120T1 (hr) 2023-06-09
ES2939776T3 (es) 2023-04-26
IL277778B2 (en) 2023-03-01
JP7493454B2 (ja) 2024-05-31
AU2023263501B2 (en) 2026-01-08
CA3095371A1 (en) 2019-10-17
KR102830237B1 (ko) 2025-07-07
IL277778B (en) 2022-11-01
AU2019253510A1 (en) 2020-10-22
MX2023004920A (es) 2023-05-16
EP4201939C0 (en) 2025-12-31
DK3774817T3 (da) 2023-02-13
IL277778A (en) 2020-11-30
EP4201939B1 (en) 2025-12-31
KR20250105504A (ko) 2025-07-08
ES3060268T3 (en) 2026-03-25
CN112334475A (zh) 2021-02-05
US11512095B2 (en) 2022-11-29
US20230287003A1 (en) 2023-09-14
EP3774817A1 (en) 2021-02-17
EP3774817B1 (en) 2022-12-07
PT3774817T (pt) 2023-03-09
AU2023263501A1 (en) 2023-11-30
IL296734B1 (en) 2025-02-01
BR112020020832A2 (pt) 2021-01-19
IL296734B2 (en) 2025-06-01
EP4729127A2 (en) 2026-04-22
US12486285B2 (en) 2025-12-02
SG11202009735QA (en) 2020-10-29
US20210163497A1 (en) 2021-06-03
JP2021521165A (ja) 2021-08-26
EP4201939A1 (en) 2023-06-28
US20260042776A1 (en) 2026-02-12
AU2019253510B2 (en) 2023-08-10
KR20200144109A (ko) 2020-12-28
IL296734A (en) 2022-11-01
MX2020010805A (es) 2021-01-29
JP2024119835A (ja) 2024-09-03
WO2019197842A1 (en) 2019-10-17
CN119330979A (zh) 2025-01-21
JP7855637B2 (ja) 2026-05-08

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