CN114025763A - 腺苷类化合物、其可药用盐或其立体异构体及用途 - Google Patents

腺苷类化合物、其可药用盐或其立体异构体及用途 Download PDF

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Publication number
CN114025763A
CN114025763A CN202080044278.2A CN202080044278A CN114025763A CN 114025763 A CN114025763 A CN 114025763A CN 202080044278 A CN202080044278 A CN 202080044278A CN 114025763 A CN114025763 A CN 114025763A
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pharmaceutically acceptable
substituted
membered
stereoisomer
compound
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CN114025763B (zh
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钟武
张珉
周辛波
樊士勇
李松
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Academy of Military Medical Sciences AMMS of PLA
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Academy of Military Medical Sciences AMMS of PLA
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/167—Purine radicals with ribosyl as the saccharide radical

Abstract

本发明为式I所示的化合物或其可药用盐、其立体异构体、其药学可接受的水合物或溶剂合物、其药学可接受的酯，其中，R选自杂芳基、取代的杂芳基、芳基、取代的芳基、环烷基、取代的环烷基、烷基和取代的烷基，其中，所述取代各自独立地为被一个或多个羟基亚烷基所取代。本发明化合物或其可药用盐、其立体异构体、其药学可接受的水合物或溶剂合物、其药学可接受的酯对A2A腺苷受体具有激动活性，能提高血脑屏障的通透性，促进跨血脑屏障递送药物，还能预防或治疗与A2A腺苷受体激动活性相关的疾病。

Description

PCT国内申请，说明书已公开。

Claims (16)

  1. PCT国内申请，权利要求书已公开。
CN202080044278.2A 2019-06-21 2020-06-22 腺苷类化合物、其可药用盐或其立体异构体及用途 Active CN114025763B (zh)

Applications Claiming Priority (3)

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CN2019105421207 2019-06-21
CN201910542120 2019-06-21
PCT/CN2020/097392 WO2020253866A1 (zh) 2019-06-21 2020-06-22 腺苷类化合物、其可药用盐或其立体异构体及用途

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CN114025763B CN114025763B (zh) 2023-09-12

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US (1) US20220332750A1 (zh)
EP (1) EP3988100A4 (zh)
JP (1) JP2022538409A (zh)
CN (1) CN114025763B (zh)
WO (1) WO2020253866A1 (zh)

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CN101068825A (zh) * 2004-08-02 2007-11-07 弗吉尼亚大学专利基金会 具有a2a激动剂活性的具有修饰的5＇－核糖基团的2－丙炔基腺苷类似物
JP2008285478A (ja) * 2007-04-16 2008-11-27 Santen Pharmaceut Co Ltd アデノシンａ２ａ受容体アゴニストを有効成分として含有する緑内障治療剤
WO2009114533A2 (en) * 2008-03-10 2009-09-17 Cornell University Modulation of blood brain barrier permeability
CN102470129A (zh) * 2009-07-09 2012-05-23 Cbt发展有限公司 作为药物使用的组合制剂
CN103221535A (zh) * 2010-09-16 2013-07-24 康奈尔大学 腺苷受体信号转导调节血脑屏障通透性的用途
CN104211666A (zh) * 2013-05-31 2014-12-17 中国人民解放军军事医学科学院毒物药物研究所 2,3-环氧丁二酰胺类化合物、其制备方法和用途
CN104582709A (zh) * 2012-08-01 2015-04-29 路易斯与克拉克药品公司 作为a2a激动剂的n-烷基2-(双取代的)炔基腺苷-5’-糖醛酰胺
US20180030453A1 (en) * 2015-02-19 2018-02-01 St. Jude Children's Research Hospital, Inc. Method for improving learning
CN109125728A (zh) * 2018-10-24 2019-01-04 东南大学 基于细胞载药技术控制磁性纳米颗粒无创入脑的方法

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1538972A (zh) * 2001-08-08 2004-10-20 CVҽҩ���޹�˾ 腺苷a3受体激动剂
CN101068825A (zh) * 2004-08-02 2007-11-07 弗吉尼亚大学专利基金会 具有a2a激动剂活性的具有修饰的5＇－核糖基团的2－丙炔基腺苷类似物
JP2008285478A (ja) * 2007-04-16 2008-11-27 Santen Pharmaceut Co Ltd アデノシンａ２ａ受容体アゴニストを有効成分として含有する緑内障治療剤
WO2009114533A2 (en) * 2008-03-10 2009-09-17 Cornell University Modulation of blood brain barrier permeability
CN102470129A (zh) * 2009-07-09 2012-05-23 Cbt发展有限公司 作为药物使用的组合制剂
CN103221535A (zh) * 2010-09-16 2013-07-24 康奈尔大学 腺苷受体信号转导调节血脑屏障通透性的用途
CN104582709A (zh) * 2012-08-01 2015-04-29 路易斯与克拉克药品公司 作为a2a激动剂的n-烷基2-(双取代的)炔基腺苷-5’-糖醛酰胺
CN104211666A (zh) * 2013-05-31 2014-12-17 中国人民解放军军事医学科学院毒物药物研究所 2,3-环氧丁二酰胺类化合物、其制备方法和用途
US20180030453A1 (en) * 2015-02-19 2018-02-01 St. Jude Children's Research Hospital, Inc. Method for improving learning
CN109125728A (zh) * 2018-10-24 2019-01-04 东南大学 基于细胞载药技术控制磁性纳米颗粒无创入脑的方法

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
MIN ZHANG，等: "Design, synthesis and biological evaluation of 2-hydrazinyladenosine derivatives as A2A adenosine receptor ligands", 《EUR J MED CHEM.》, pages 310 - 324 *
SADHANA JACKSON，等: "The effect of regadenoson on the integrity of the human blood-brain barrier, a pilot study", 《J NEUROONCOL.》, vol. 132, no. 3, pages 513 - 519, XP036262454, DOI: 10.1007/s11060-017-2404-1 *
VAN DER PLOEG，等: "Functional characterization of adenosine A2 receptors in Jurkat cells and PC12 cells using adenosine receptor agonists", 《NAUNYN-SCHMIEDEBERG\'S ARCHIVES OF PHARMACOLOGY》, vol. 353, no. 3, pages 250 - 260, XP000978323, DOI: 10.1007/BF00168626 *
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Also Published As

Publication number Publication date
US20220332750A1 (en) 2022-10-20
EP3988100A1 (en) 2022-04-27
CN114025763B (zh) 2023-09-12
WO2020253866A1 (zh) 2020-12-24
EP3988100A4 (en) 2023-07-26
JP2022538409A (ja) 2022-09-02

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