CN116134028A - 一种具有降解btk激酶的化合物及其制备方法和药学上的应用 - Google Patents

一种具有降解btk激酶的化合物及其制备方法和药学上的应用 Download PDF

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Publication number
CN116134028A
CN116134028A CN202180047615.8A CN202180047615A CN116134028A CN 116134028 A CN116134028 A CN 116134028A CN 202180047615 A CN202180047615 A CN 202180047615A CN 116134028 A CN116134028 A CN 116134028A
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China
Prior art keywords
substituted
cyclopentyl
azetidinyl
cyclohexyl
pyrimidin
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Pending
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CN202180047615.8A
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English (en)
Inventor
张晨
廖雨亭
王健民
程新帆
陈孝刚
邹思佳
袁帅
叶飞
唐平明
祝国智
黄正刚
吴守涛
李瑶
倪佳
严庞科
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Tibet Haisike Pharmaceutical Co ltd
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Sichuan Haisco Pharmaceutical Co Ltd
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Publication of CN116134028A publication Critical patent/CN116134028A/zh
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

本发明涉及一种通式(I)所述的化合物或者其立体异构体、溶剂化物、前药、代谢产物、药学上可接受的盐或共晶，及其中间体和制备方法，以及在BTK相关疾病如肿瘤或自身免疫系统疾病中的用途。B‑L‑K(I)。

Description

PCT国内申请，说明书已公开。

Claims (26)

  1. PCT国内申请，权利要求书已公开。
CN202180047615.8A 2020-07-07 2021-07-07 一种具有降解btk激酶的化合物及其制备方法和药学上的应用 Pending CN116134028A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN202010644112 2020-07-07
CN2020106441126 2020-07-07
CN202011237752 2020-11-10
CN2020112377521 2020-11-10
PCT/CN2021/104905 WO2022007824A1 (zh) 2020-07-07 2021-07-07 一种具有降解btk激酶的化合物及其制备方法和药学上的应用

Publications (1)

Publication Number Publication Date
CN116134028A true CN116134028A (zh) 2023-05-16

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CN202180047615.8A Pending CN116134028A (zh) 2020-07-07 2021-07-07 一种具有降解btk激酶的化合物及其制备方法和药学上的应用

Country Status (5)

Country Link
US (1) US20230248833A1 (zh)
EP (1) EP4180432A1 (zh)
CN (1) CN116134028A (zh)
TW (1) TW202216715A (zh)
WO (1) WO2022007824A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117377675A (zh) * 2021-06-01 2024-01-09 正大天晴药业集团股份有限公司 含有并环或螺环的布鲁顿酪氨酸激酶降解剂
WO2023072270A1 (zh) * 2021-10-29 2023-05-04 百极弘烨(南通)医药科技有限公司 Protac化合物、含其的药物组合物及其制备方法和应用
CN114292270B (zh) * 2021-12-16 2023-05-05 南方医科大学 一种btk抑制剂及其制备方法与应用
CN114560757B (zh) * 2022-03-04 2023-09-26 上海凌凯医药科技有限公司 一种二芳基醚化合物的制备方法
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

Family Cites Families (11)

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WO2017197056A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Bromodomain targeting degronimers for target protein degradation
AU2017314178B2 (en) 2016-08-16 2021-11-18 Beigene Switzerland Gmbh Crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
EP3538526B1 (en) 2016-11-08 2024-04-10 Bristol-Myers Squibb Company Cyclobutane- and azetidine-containing mono and spirocyclic compounds as alpha v integrin inhibitors
WO2019127008A1 (zh) * 2017-12-26 2019-07-04 清华大学 一种靶向降解btk的化合物及其应用
CN110627796B (zh) 2018-06-21 2022-07-12 北京越之康泰生物医药科技有限公司 含氮杂环类衍生物及其在医药上的应用
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
JP2022534650A (ja) 2019-05-31 2022-08-03 海思科医▲薬▼有限公司 Ｂｔｋ阻害薬環誘導体、その調製方法及びその医薬品適用
WO2020252397A1 (en) * 2019-06-12 2020-12-17 Baylor College Of Medicine Small molecule proteolysis-targeting chimeras and methods of use thereof
CN114174299A (zh) * 2019-07-26 2022-03-11 百济神州有限公司 通过btk抑制剂与e3连接酶配体缀合对布鲁顿氏酪氨酸激酶(btk)的降解以及使用方法
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
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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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EP4180432A1 (en) 2023-05-17
US20230248833A1 (en) 2023-08-10
WO2022007824A1 (zh) 2022-01-13
TW202216715A (zh) 2022-05-01

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