CN115989230A - 吡唑[1,5-a]吡啶类化合物及其制备方法与应用 - Google Patents

吡唑[1,5-a]吡啶类化合物及其制备方法与应用 Download PDF

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CN115989230A
CN115989230A CN202180047203.4A CN202180047203A CN115989230A CN 115989230 A CN115989230 A CN 115989230A CN 202180047203 A CN202180047203 A CN 202180047203A CN 115989230 A CN115989230 A CN 115989230A
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compound
alkyl
ret
pharmaceutically acceptable
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罗会兵
周华勇
李庆
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Shanghai Allist Medicine Polytron Technologies Inc
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Shanghai Allist Medicine Polytron Technologies Inc
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明涉及下述通式(I)所示的吡唑[1，5‑a]吡啶类化合物、其制备方法、药物组合物及应用，式中R1、R2、R3、R4、R5、X、Y、Z如说明书中所定义。本发明所述吡唑[1，5‑a]吡啶类化合物能够有效抑制野生型RET、突变型RET特别是G810R突变型RET、以及KIF5B‑RET和CCDC6‑RET等RET融合，且安全性好，可用于治疗由RET介导的疾病，例如癌症和肠易激综合征。
Figure DDA0004030764770000011

Description

PCT国内申请，说明书已公开。

Claims (23)

  1. PCT国内申请，权利要求书已公开。
CN202180047203.4A 2020-07-01 2021-06-30 吡唑[1,5-a]吡啶类化合物及其制备方法与应用 Pending CN115989230A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2020106251193 2020-07-01
CN202010625119.3A CN113880865A (zh) 2020-07-01 2020-07-01 吡唑[1,5-a]吡啶类化合物及其制备方法与应用
PCT/CN2021/103358 WO2022002097A1 (zh) 2020-07-01 2021-06-30 吡唑[1，5-a]吡啶类化合物及其制备方法与应用

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CN115989230A true CN115989230A (zh) 2023-04-18

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WO2021088911A1 (zh) * 2019-11-08 2021-05-14 杭州邦顺制药有限公司 作为ret激酶抑制剂的3、6二氮杂双环[3.1.1]庚烷衍生物
WO2023143486A1 (zh) * 2022-01-29 2023-08-03 深圳众格生物科技有限公司 化合物的盐、晶型、溶剂合物及水合物

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TWI704148B (zh) * 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
TWI783057B (zh) * 2017-10-10 2022-11-11 美商絡速藥業公司 製備6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈的方法
EP3891148A4 (en) * 2018-12-07 2022-09-07 Sunshine Lake Pharma Co., Ltd. RET INHIBITOR, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
WO2020114487A1 (en) * 2018-12-07 2020-06-11 Sunshine Lake Pharma Co., Ltd. Ret inhibitors, pharmaceutical compositions and uses thereof
US20220259201A1 (en) * 2019-05-14 2022-08-18 Shanghai Hansoh Biomedical Co., Ltd. Inhibitor containing bicyclic derivative, preparation method therefor and use thereof
WO2021088911A1 (zh) * 2019-11-08 2021-05-14 杭州邦顺制药有限公司 作为ret激酶抑制剂的3、6二氮杂双环[3.1.1]庚烷衍生物
CN112939967A (zh) * 2019-12-11 2021-06-11 深圳晶泰科技有限公司 吡唑并[1,5-a]吡啶类化合物及其制备方法和应用

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