CN113557236A - 一种双功能免疫调节剂及其在药学上可接受的盐、药物组合物 - Google Patents

一种双功能免疫调节剂及其在药学上可接受的盐、药物组合物 Download PDF

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CN113557236A
CN113557236A CN202080018398.5A CN202080018398A CN113557236A CN 113557236 A CN113557236 A CN 113557236A CN 202080018398 A CN202080018398 A CN 202080018398A CN 113557236 A CN113557236 A CN 113557236A
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compound
substituted
bifunctional
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cancer
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CN113557236B (zh
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唐士兵
曾少高
米琦·丹尼尔·托特雷拉
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Guangzhou Institute of Biomedicine and Health of CAS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Communicable Diseases (AREA)
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  • Biomedical Technology (AREA)
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  • Immunology (AREA)
  • Molecular Biology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

一种双功能免疫调节剂及其在药学上可接受的盐、药物组合物,所述调节剂具有如式I所示结构。双功能免疫调节剂包含同时阻断PD‑1/PD‑L1相互作用的苄苯醚类分子骨架和阻断TGF‑β信号通路的4‑(4‑吡唑)喹啉分子骨架,二者通过分子链片段相连接。因此,双功能免疫调节剂可同时阻断PD‑1/PD‑L1相互作用和TGF‑β信号通路。

Description

PCT国内申请,说明书已公开。

Claims (15)

  1. PCT国内申请,权利要求书已公开。
CN202080018398.5A 2019-06-10 2020-06-05 一种双功能免疫调节剂及其在药学上可接受的盐、药物组合物 Active CN113557236B (zh)

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CN201910497925 2019-06-10
CN2019104979254 2019-06-10
PCT/CN2020/094580 WO2020248908A1 (zh) 2019-06-10 2020-06-05 一种双功能免疫调节剂及其在药学上可接受的盐、药物组合物

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CN113307779B (zh) * 2021-05-25 2023-04-21 中国药科大学 杂环取代联苯类化合物、制备方法及用途

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1337950A (zh) * 1999-01-08 2002-02-27 日本烟草产业株式会社 2-氧代喹啉化合物及其药物用途
US20100254899A1 (en) * 2007-02-27 2010-10-07 The United States Of America, As Represented By The Secretary, Dept Of Health And Human Services Radiolabeled affibody molecules
CN105705489A (zh) * 2013-09-04 2016-06-22 百时美施贵宝公司 用作免疫调节剂的化合物
CN109305934A (zh) * 2018-08-07 2019-02-05 成都海博锐药业有限公司 苯醚类衍生物及可药用盐、医药上的用途
CN109824621A (zh) * 2019-03-28 2019-05-31 中国药科大学 噁二唑类和噻二唑类化合物及其制备方法和用途

Family Cites Families (6)

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Publication number Priority date Publication date Assignee Title
DE60221392T2 (de) * 2001-05-24 2008-04-17 Eli Lilly And Co., Indianapolis Neue pyrrolderivate als pharmazeutische mittel
UA80571C2 (en) * 2002-11-22 2007-10-10 Lilly Co Eli Quinolinyl-pyrrolopyrazoles
US8871744B2 (en) * 2010-07-21 2014-10-28 B & G Partyers, LLC Compounds and methods for selectively targeting tumor-associated mucins
US9850225B2 (en) * 2014-04-14 2017-12-26 Bristol-Myers Squibb Company Compounds useful as immunomodulators
US10167334B2 (en) * 2015-04-03 2019-01-01 Xoma Technology Ltd. Treatment of cancer using anti-TGF-BETA and PD-1 antibodies
US10745382B2 (en) * 2015-10-15 2020-08-18 Bristol-Myers Squibb Company Compounds useful as immunomodulators

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1337950A (zh) * 1999-01-08 2002-02-27 日本烟草产业株式会社 2-氧代喹啉化合物及其药物用途
US20100254899A1 (en) * 2007-02-27 2010-10-07 The United States Of America, As Represented By The Secretary, Dept Of Health And Human Services Radiolabeled affibody molecules
CN105705489A (zh) * 2013-09-04 2016-06-22 百时美施贵宝公司 用作免疫调节剂的化合物
CN109305934A (zh) * 2018-08-07 2019-02-05 成都海博锐药业有限公司 苯醚类衍生物及可药用盐、医药上的用途
CN109824621A (zh) * 2019-03-28 2019-05-31 中国药科大学 噁二唑类和噻二唑类化合物及其制备方法和用途

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