CN114761020A - (5r)-5-羟基雷公藤内酯醇在制备药物中的应用 - Google Patents

(5r)-5-羟基雷公藤内酯醇在制备药物中的应用 Download PDF

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Publication number
CN114761020A
CN114761020A CN201880089248.6A CN201880089248A CN114761020A CN 114761020 A CN114761020 A CN 114761020A CN 201880089248 A CN201880089248 A CN 201880089248A CN 114761020 A CN114761020 A CN 114761020A
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aids
immune
cells
immune activation
activation
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CN201880089248.6A
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刘彦君
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Dunshan Medical Technology (Shenzhen) Co.,Ltd.
Shanghai Pharmaceuticals Holding Co Ltd
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Shanghai Pharmaceuticals Holding Co Ltd
Peking Union Medical College Hospital Chinese Academy of Medical Sciences
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Publication of CN114761020A publication Critical patent/CN114761020A/zh
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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
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • 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
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

本发明公开了(5R)‑5‑羟基雷公藤内酯醇在制备药物中的应用,特别是在制备治疗和/或预防艾滋病异常免疫激活、或者艾滋病异常免疫激活相关的免疫重建不全的药物中的应用。本发明使用(5R)‑5‑羟基雷公藤内酯醇(T8)进行实验后发现,其在艾滋病异常免疫激活、或者艾滋病异常免疫激活相关的免疫重建不全中具有免疫抑制活性,且表现为效率高、毒性低,具有很好的安全治疗指数。

Description

PCT国内申请,说明书已公开。

Claims (9)

  1. PCT国内申请,权利要求书已公开。
CN201880089248.6A 2018-02-13 2018-12-14 (5r)-5-羟基雷公藤内酯醇在制备药物中的应用 Pending CN114761020A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2018101491494 2018-02-13
CN201810149149 2018-02-13
PCT/CN2018/121201 WO2019157854A1 (zh) 2018-02-13 2018-12-14 (5r)-5-羟基雷公藤内酯醇在制备药物中的应用

Publications (1)

Publication Number Publication Date
CN114761020A true CN114761020A (zh) 2022-07-15

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Family Applications (2)

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CN201811532917.0A Withdrawn CN109394771A (zh) 2018-02-13 2018-12-14 (5r)-5-羟基雷公藤内酯醇在制备药物中的应用
CN201880089248.6A Pending CN114761020A (zh) 2018-02-13 2018-12-14 (5r)-5-羟基雷公藤内酯醇在制备药物中的应用

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CN201811532917.0A Withdrawn CN109394771A (zh) 2018-02-13 2018-12-14 (5r)-5-羟基雷公藤内酯醇在制备药物中的应用

Country Status (7)

Country Link
US (1) US20210052541A1 (zh)
EP (1) EP3753564A4 (zh)
JP (1) JP2021513554A (zh)
CN (2) CN109394771A (zh)
BR (1) BR112020016473A2 (zh)
WO (1) WO2019157854A1 (zh)
ZA (1) ZA202005671B (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111821295A (zh) * 2019-04-15 2020-10-27 中国科学院上海药物研究所 (5r)-5-羟基雷公藤内酯醇在制备治疗和/或预防皮肤炎症药物中的应用
CN111202738A (zh) * 2020-02-10 2020-05-29 复旦大学附属中山医院 (5r)-5-羟基雷公藤内酯醇在制备脓毒症治疗药物中的用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1511838A (zh) * 2002-12-27 2004-07-14 �й���ѧԺ�Ϻ�ҩ���о��� 雷公藤内酯醇衍生物及其应用
CN103083334A (zh) * 2012-12-20 2013-05-08 李太生 雷公藤多甙在hiv/aids患者中对治疗免疫重建不全及非aids相关疾病与免疫重建不全的新用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1511838A (zh) * 2002-12-27 2004-07-14 �й���ѧԺ�Ϻ�ҩ���о��� 雷公藤内酯醇衍生物及其应用
CN103083334A (zh) * 2012-12-20 2013-05-08 李太生 雷公藤多甙在hiv/aids患者中对治疗免疫重建不全及非aids相关疾病与免疫重建不全的新用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ZHOU, R 等.: "Inhibition of inducible nitric-oxide synthase expression by (5R)-5- hydroxytriptolide in interferon-γ- and bacterial lipopolysaccharide-stimulated macrophages.", JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS., vol. 316, no. 1, pages 121 - 128, XP055631810, DOI: 10.1124/jpet.105.093179 *

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Publication number Publication date
US20210052541A1 (en) 2021-02-25
CN109394771A (zh) 2019-03-01
WO2019157854A1 (zh) 2019-08-22
EP3753564A4 (en) 2021-11-10
BR112020016473A2 (pt) 2020-12-15
JP2021513554A (ja) 2021-05-27
EP3753564A1 (en) 2020-12-23
ZA202005671B (en) 2021-09-29

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