JP7681038B2 - Ｂｔｋ阻害因子とｅ３リガーゼリガンドとのコンジュゲーションによるブルトンチロシンキナーゼ（ｂｔｋ）の分解及び使用方法 - Google Patents

Ｂｔｋ阻害因子とｅ３リガーゼリガンドとのコンジュゲーションによるブルトンチロシンキナーゼ（ｂｔｋ）の分解及び使用方法 Download PDF

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JP7681038B2
JP7681038B2 JP2022554565A JP2022554565A JP7681038B2 JP 7681038 B2 JP7681038 B2 JP 7681038B2 JP 2022554565 A JP2022554565 A JP 2022554565A JP 2022554565 A JP2022554565 A JP 2022554565A JP 7681038 B2 JP7681038 B2 JP 7681038B2
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mmol
phenyl
tert
butyl
piperidin
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JP2023523130A (ja
JP2023523130A5 (https=
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ヘシャン ワン
バイリン レイ
チャンシン フオ
ドンキン ソン
ジエ チェン
ジーウェイ ワン
ユチェン ワン
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BeOne Medicines Ltd
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BeOne Medicines Ltd
Beigene Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • A61K31/495—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
    • 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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicinal Preparation (AREA)
JP2022554565A 2020-04-30 2021-04-29 Ｂｔｋ阻害因子とｅ３リガーゼリガンドとのコンジュゲーションによるブルトンチロシンキナーゼ（ｂｔｋ）の分解及び使用方法 Active JP7681038B2 (ja)

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JP2025078734A JP2025122005A (ja) 2020-04-30 2025-05-09 Ｂｔｋ阻害因子とｅ３リガーゼリガンドとのコンジュゲーションによるブルトンチロシンキナーゼ（ｂｔｋ）の分解及び使用方法

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CN2020088322 2020-04-30
CNPCT/CN2020/088322 2020-04-30
CN2021085369 2021-04-02
CNPCT/CN2021/085369 2021-04-02
PCT/CN2021/090898 WO2021219070A1 (en) 2020-04-30 2021-04-29 Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use

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JP2023523130A JP2023523130A (ja) 2023-06-02
JP2023523130A5 JP2023523130A5 (https=) 2024-05-09
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JP2025078734A Pending JP2025122005A (ja) 2020-04-30 2025-05-09 Ｂｔｋ阻害因子とｅ３リガーゼリガンドとのコンジュゲーションによるブルトンチロシンキナーゼ（ｂｔｋ）の分解及び使用方法

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US (1) US20230167118A1 (https=)
EP (1) EP4146655A4 (https=)
JP (2) JP7681038B2 (https=)
KR (1) KR20230003161A (https=)
CN (4) CN116589466B (https=)
AU (1) AU2021264916A1 (https=)
BR (1) BR112022019014A2 (https=)
CA (1) CA3172498A1 (https=)
IL (1) IL297664A (https=)
MX (1) MX2022013407A (https=)
TW (1) TWI902789B (https=)
WO (1) WO2021219070A1 (https=)
ZA (1) ZA202209962B (https=)

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CN116589466B (zh) * 2020-04-30 2025-08-15 百济神州有限公司 通过缀合btk抑制剂与e3连接酶配体降解布鲁顿氏酪氨酸激酶(btk)及其使用方法
CN116981675A (zh) * 2020-12-31 2023-10-31 百济神州有限公司 通过布鲁顿氏酪氨酸激酶（btk）抑制剂与e3连接酶配体的缀合降解btk和使用方法
AU2022270089A1 (en) * 2021-05-03 2023-11-16 Nurix Therapeutics, Inc. Compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use
TW202309039A (zh) * 2021-05-05 2023-03-01 美商百健Ｍａ公司 用於靶向布魯頓氏酪胺酸激酶降解之化合物
KR20240020735A (ko) 2021-05-07 2024-02-15 카이메라 쎄라퓨틱스 인코포레이티드 Cdk2 분해제 및 그 용도
JP2024525181A (ja) * 2021-06-21 2024-07-10 ベイジーン スウィッツァーランド ゲーエムベーハー （ｒ）－グルタルイミドｃｒｂｎリガンド及び使用方法
KR20240128831A (ko) 2021-12-30 2024-08-27 베이진 스위찰랜드 게엠베하 브루톤 티로신 키나아제(btk) 억제제와 e3 리가아제 리간드의 접합에 의한 btk의 분해 및 사용 방법
WO2023125907A1 (en) * 2021-12-30 2023-07-06 Beigene, Ltd. Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
JP7805983B2 (ja) 2022-03-22 2026-01-26 アッヴィ・インコーポレイテッド ブルトン型チロシンキナーゼを分解するためのピリミジン
WO2024169871A1 (zh) * 2023-02-17 2024-08-22 江苏威凯尔医药科技有限公司 Btk抑制剂及其用途
CN118946561A (zh) * 2023-03-10 2024-11-12 标新生物医药科技(上海)有限公司 新颖的e3泛素连接酶配体、蛋白降解剂及其应用
CN117126133A (zh) * 2023-08-14 2023-11-28 中国海洋大学 一种化合物及其用途
TW202532078A (zh) * 2024-02-09 2025-08-16 瑞士商百濟神州瑞士有限責任公司 用嵌合降解活化化合物治療b細胞增殖性病症
CN120623148A (zh) * 2024-03-11 2025-09-12 北京深势科技有限公司 一种c-Myc降解剂及其制备方法和用途
WO2025218772A1 (en) * 2024-04-19 2025-10-23 Beigene (Suzhou) Co., Ltd. Solid forms comprising a bruton's tyrosine kinase degrader and uses therefor
WO2025232885A1 (en) * 2024-05-10 2025-11-13 Beigene (Suzhou) Co., Ltd. Preparation method of a bruton's tyrosine kinase degrader thereof
WO2026012424A1 (zh) * 2024-07-10 2026-01-15 江苏恒瑞医药股份有限公司 一种杂芳基类化合物、其制备方法及其在医药上的应用
CN121405700A (zh) * 2024-07-26 2026-01-27 苏州亚盛药业有限公司 Btk降解剂及其用途

Citations (4)

* Cited by examiner, † Cited by third party
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WO2013157021A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
JP2015535226A (ja) 2012-10-26 2015-12-10 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ブルートンチロシンキナーゼの阻害剤
WO2019186358A1 (en) 2018-03-26 2019-10-03 Novartis Ag 3-hydroxy-n-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)pyrrolidine-1-carboxamide derivatives
WO2019186343A1 (en) 2018-03-26 2019-10-03 Novartis Ag N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives

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EP3444251B1 (en) * 2013-12-11 2023-06-07 Biogen MA Inc. Biaryl compounds useful for the treatment of human diseases in oncology, neurology and immunology
CN116589466B (zh) * 2020-04-30 2025-08-15 百济神州有限公司 通过缀合btk抑制剂与e3连接酶配体降解布鲁顿氏酪氨酸激酶(btk)及其使用方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013157021A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
JP2015535226A (ja) 2012-10-26 2015-12-10 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ブルートンチロシンキナーゼの阻害剤
WO2019186358A1 (en) 2018-03-26 2019-10-03 Novartis Ag 3-hydroxy-n-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)pyrrolidine-1-carboxamide derivatives
WO2019186343A1 (en) 2018-03-26 2019-10-03 Novartis Ag N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives

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IL297664A (en) 2022-12-01
CA3172498A1 (en) 2021-11-04
CN115485278A (zh) 2022-12-16
TWI902789B (zh) 2025-11-01
JP2023523130A (ja) 2023-06-02
MX2022013407A (es) 2022-11-14
EP4146655A1 (en) 2023-03-15
BR112022019014A2 (pt) 2022-11-29
EP4146655A4 (en) 2024-07-31
ZA202209962B (en) 2023-05-31
JP2025122005A (ja) 2025-08-20
CN121159541A (zh) 2025-12-19
TW202142542A (zh) 2021-11-16
WO2021219070A1 (en) 2021-11-04
CN116589467A (zh) 2023-08-15
CN116589466A (zh) 2023-08-15
AU2021264916A1 (en) 2022-11-03
CN116589466B (zh) 2025-08-15
US20230167118A1 (en) 2023-06-01
KR20230003161A (ko) 2023-01-05

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