JP7202315B2 - ベンズイミダゾロン由来のｂｃｌ６阻害剤 - Google Patents

ベンズイミダゾロン由来のｂｃｌ６阻害剤 Download PDF

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JP7202315B2
JP7202315B2 JP2019565443A JP2019565443A JP7202315B2 JP 7202315 B2 JP7202315 B2 JP 7202315B2 JP 2019565443 A JP2019565443 A JP 2019565443A JP 2019565443 A JP2019565443 A JP 2019565443A JP 7202315 B2 JP7202315 B2 JP 7202315B2
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methyl
amino
chloro
hydroxy
alkyl
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JP2020521771A (ja
Inventor
ベンジャミン・リチャード・ベレーニー
マイケル・キース・カーター
クワイ・ミン・ジャック・チュン
オーウェン・アレクサンダー・デイヴィス
スウェン・ヘルダー
マシュー・ガース・ロイド
アナ・ヴァレラ・ロドリゲス
ハンナ・ウッドワード
パオロ・イノチェンチ
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Cancer Research Technology Ltd
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Cancer Research Technology Ltd
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Priority claimed from GBGB1708502.8A external-priority patent/GB201708502D0/en
Priority claimed from GBGB1806130.9A external-priority patent/GB201806130D0/en
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Publication of JP2020521771A publication Critical patent/JP2020521771A/ja
Priority to JP2022207230A priority Critical patent/JP7534379B2/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26—Oxygen atoms
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
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    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
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    • 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
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    • 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
    • C07D471/08—Bridged systems
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    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • 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)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2019565443A 2017-05-26 2018-05-25 ベンズイミダゾロン由来のｂｃｌ６阻害剤 Active JP7202315B2 (ja)

Priority Applications (1)

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JP2022207230A JP7534379B2 (ja) 2017-05-26 2022-12-23 ベンズイミダゾロン由来のｂｃｌ６阻害剤

Applications Claiming Priority (5)

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GB1708502.8 2017-05-26
GBGB1708502.8A GB201708502D0 (en) 2017-05-26 2017-05-26 Inhibitor compounds
GBGB1806130.9A GB201806130D0 (en) 2018-04-13 2018-04-13 Inhibitor compounds
GB1806130.9 2018-04-13
PCT/GB2018/051447 WO2018215801A1 (en) 2017-05-26 2018-05-25 Benzimidazolone derived inhibitors of bcl6

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JP7202315B2 true JP7202315B2 (ja) 2023-01-11

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US (2) US12110286B2 (enExample)
EP (2) EP3630291B9 (enExample)
JP (2) JP7202315B2 (enExample)
KR (2) KR102628675B1 (enExample)
CN (2) CN111163839B (enExample)
AU (2) AU2018274723B2 (enExample)
CA (1) CA3065005A1 (enExample)
ES (1) ES2975690T3 (enExample)
IL (2) IL302300B1 (enExample)
MX (1) MX2023005636A (enExample)
WO (1) WO2018215801A1 (enExample)
ZA (1) ZA202405646B (enExample)

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JP2023052069A (ja) * 2017-05-26 2023-04-11 キャンサー・リサーチ・テクノロジー・リミテッド ベンズイミダゾロン由来のｂｃｌ６阻害剤
US12486285B2 (en) 2018-04-13 2025-12-02 Cancer Research Technology Limited BCL6 inhibitors
US12528826B2 (en) 2019-10-14 2026-01-20 Cancer Research Technology Limited [1,4]oxazepino[2,3-c]quinolinone derivatives as BCL6 inhibitors

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US12454520B2 (en) 2018-07-06 2025-10-28 Kymera Therapeutics, Inc. Protein degraders and uses thereof
GB201819126D0 (en) * 2018-11-23 2019-01-09 Cancer Research Tech Ltd Inhibitor compounds
AU2019389174A1 (en) 2018-11-30 2021-07-01 Kymera Therapeutics, Inc. Irak degraders and uses thereof
KR102922115B1 (ko) 2019-04-09 2026-02-04 누릭스 테라퓨틱스 인코포레이티드 Cbl-b 억제용의 3-치환된 피페리딘 화합물, 및 암 백신 및/또는 종양용해 바이러스와 조합된 cbl-b 억제제의 용도
PH12022500002A1 (en) 2019-06-28 2023-04-03 Kymera Therapeutics Inc Irak degraders and uses thereof
GB201909573D0 (en) 2019-07-03 2019-08-14 Cancer Research Tech Ltd Modulation of T cell cytotoxicity and related therapy
US12558427B2 (en) 2019-07-17 2026-02-24 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
US12653809B2 (en) 2019-07-30 2026-06-16 Nurix Therapeutics, Inc. Urea, amide, and substituted heteroaryl compounds for CBL-B inhibition
MX2022004526A (es) 2019-10-17 2022-07-21 Arvinas Operations Inc Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6.
WO2021119159A1 (en) 2019-12-10 2021-06-17 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CA3161878A1 (en) 2019-12-17 2021-06-24 Matthew M. Weiss Irak degraders and uses thereof
EP4161521A4 (en) 2020-06-03 2024-07-10 Kymera Therapeutics, Inc. DEUTERED IRAQ DEGRADERS AND USES THEREOF
CA3192868A1 (en) * 2020-09-24 2022-03-31 Auckland Uniservices Limited Novel aminopyridines and their use in treating cancer
AR124547A1 (es) 2020-12-30 2023-04-05 Kymera Therapeutics Inc Degradadores de irak y sus usos
WO2022174268A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
US12016860B2 (en) 2021-04-08 2024-06-25 Nurix Therapeutics, Inc. Combination therapies with Cbl-b inhibitor compounds
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
JP2024540080A (ja) 2021-10-29 2024-10-31 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ４分解剤およびその合成
EP4463166A4 (en) * 2022-01-14 2025-12-31 Kymera Therapeutics Inc IRAQ4 DEGRADATION AGENTS AND THEIR USES
EP4472967A4 (en) 2022-01-31 2026-04-15 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
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
KR20250023483A (ko) 2022-06-13 2025-02-18 트리라인 바이오사이언시스, 인크. 퀴놀론 bcl6 이작용성 분해제
AU2023295387A1 (en) 2022-06-13 2025-01-09 Treeline Biosciences, Inc. 1,8-naphthyridin-2-one heterobifunctional bcl6 degraders
JP2025534769A (ja) * 2022-10-17 2025-10-17 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 Ｂｃｌ６のアルキルアミン含有小分子分解剤
EP4626884A1 (en) 2022-11-30 2025-10-08 Blueprint Medicines Corporation N-phenyl-pyrazolo[1,5-a]pyridine-3-carboxamide derivatives as wild type c-kit kinase inhibitors for the treatment of urticaria
WO2024191788A1 (en) * 2023-03-10 2024-09-19 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof

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