CN110461846A - 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物 - Google Patents

一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物 Download PDF

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CN110461846A
CN110461846A CN201880004080.4A CN201880004080A CN110461846A CN 110461846 A CN110461846 A CN 110461846A CN 201880004080 A CN201880004080 A CN 201880004080A CN 110461846 A CN110461846 A CN 110461846A
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cycloalkyl
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CN110461846B (zh
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舒永志
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Shanghai Meizer Pharmaceuticals Co ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Immunology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的式I化合物，其具有很好的Btk抑制活性并能将Btk降解，可以用于制备治疗间Btk活性相关的疾病的药物。(I)

Description

PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN201880004080.4A 2017-09-03 2018-09-02 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物 Active CN110461846B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201710783076X 2017-09-03
CN201710783076.XA CN109422752B (zh) 2017-09-03 2017-09-03 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物
PCT/CN2018/103710 WO2019042445A1 (zh) 2017-09-03 2018-09-02 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物

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CN110461846A true CN110461846A (zh) 2019-11-15
CN110461846B CN110461846B (zh) 2023-01-06

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CN201880004080.4A Active CN110461846B (zh) 2017-09-03 2018-09-02 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物

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US (2) US11155561B2 (zh)
EP (1) EP3677584A4 (zh)
JP (1) JP2020532552A (zh)
CN (2) CN109422752B (zh)
WO (1) WO2019042445A1 (zh)

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CN109422733A (zh) * 2017-09-03 2019-03-05 上海美志医药科技有限公司 一类抑制并降解酪氨酸蛋白激酶alk的化合物
JP2021512059A (ja) * 2018-01-29 2021-05-13 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 ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｂｔｋの分解および使用方法
WO2020177657A1 (zh) * 2019-03-02 2020-09-10 上海美志医药科技有限公司 一类具有降解Btk活性的化合物
SG11202110085TA (en) * 2019-05-31 2021-10-28 Sichuan Haisco Pharmaceutical Co Ltd Btk inhibitor ring derivative, preparation method therefor and pharmaceutical application thereof
CN112010858B (zh) * 2019-05-31 2023-07-18 四川海思科制药有限公司 一种btk抑制剂及其制备方法和药学上的应用
WO2020252397A1 (en) * 2019-06-12 2020-12-17 Baylor College Of Medicine Small molecule proteolysis-targeting chimeras and methods of use thereof
CN110724143B (zh) * 2019-10-09 2021-03-23 清华大学 一种靶向btk蛋白降解化合物的制备及其在治疗自身免疫系统疾病与肿瘤中的应用
CN110845500B (zh) * 2019-10-09 2021-05-11 清华大学 靶向btk降解化合物在治疗自身免疫系统疾病中的应用
CN112979656A (zh) * 2019-12-12 2021-06-18 上海美志医药科技有限公司 一类靶向降解btk蛋白的化合物
US20240018147A1 (en) * 2020-09-09 2024-01-18 Haisco Pharmaceuticals Pte. Ltd. Salt of compound for degrading btk, crystal form thereof, and use thereof in medicine
CN114478532A (zh) * 2020-10-26 2022-05-13 上海美志医药科技有限公司 靶向降解Btk的化合物及其抗肿瘤用途
CN115304606B (zh) * 2021-06-21 2024-04-19 清华大学 一种同时靶向btk和gspt1蛋白的降解剂
CN115521313B (zh) * 2021-06-24 2023-11-03 山东大学 一种降解btk蛋白的化合物及其制备方法和应用
CA3223447A1 (en) * 2021-06-25 2022-12-29 Korea Research Institute Of Chemical Technology Novel bifunctional heterocyclic compound having btk degradation function via ubiquitin proteasome pathway, and use thereof
WO2023284703A1 (zh) * 2021-07-15 2023-01-19 标新生物医药科技(上海)有限公司 基于布鲁顿酪氨酸激酶配体设计的蛋白降解化合物及其应用
CN115785099A (zh) * 2021-09-13 2023-03-14 上海美志医药科技有限公司 具有降解酪氨酸蛋白激酶Btk活性的化合物及其应用
CN114409658B (zh) * 2022-04-02 2022-06-07 水木未来(北京)科技有限公司 一种同时调节btk和ikzf3的双功能化合物
WO2023227080A1 (zh) * 2022-05-25 2023-11-30 百极弘烨(南通)医药科技有限公司 一种protac化合物、含其的药物组合物及其制备方法和应用

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US11155561B2 (en) 2021-10-26
EP3677584A4 (en) 2021-04-07
CN109422752B (zh) 2023-04-07
WO2019042445A1 (zh) 2019-03-07
EP3677584A1 (en) 2020-07-08
JP2020532552A (ja) 2020-11-12
CN110461846B (zh) 2023-01-06
CN109422752A (zh) 2019-03-05
US20200199132A1 (en) 2020-06-25
US20210363148A1 (en) 2021-11-25

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