CN109952305A - 哌嗪并杂芳基类衍生物、其制备方法及其在医药上的应用 - Google Patents

哌嗪并杂芳基类衍生物、其制备方法及其在医药上的应用 Download PDF

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CN109952305A
CN109952305A CN201880004423.7A CN201880004423A CN109952305A CN 109952305 A CN109952305 A CN 109952305A CN 201880004423 A CN201880004423 A CN 201880004423A CN 109952305 A CN109952305 A CN 109952305A
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alkyl
compound
heteroaryl
aryl
heterocycle
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CN109952305B (zh
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李心
何威
陈阳
贺峰
陶维康
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Shanghai Hengrui Pharmaceutical Co Ltd
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    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Abstract

本发明涉及哌嗪并杂芳基类衍生物、其制备方法及其在医药上的应用。特别地，本发明涉及通式(I)所示的哌嗪并杂芳基类衍生物、其制备方法、含有该衍生物的药物组合物，以及其作为衣壳蛋白抑制剂，特别是在预防和/或治疗乙型肝炎、流感、疱疹和艾滋病等疾病中的用途。其中通式(I)中的各基团的定义与说明书中的定义相同。

Description

PCT国内申请，说明书已公开。

Claims (19)

  1. PCT国内申请，权利要求书已公开。
CN201880004423.7A 2017-07-27 2018-07-26 哌嗪并杂芳基类衍生物、其制备方法及其在医药上的应用 Active CN109952305B (zh)

Applications Claiming Priority (5)

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CN2017106217449 2017-07-27
CN201710621744 2017-07-27
CN201711058986 2017-11-01
CN2017110589868 2017-11-01
PCT/CN2018/097170 WO2019020070A1 (zh) 2017-07-27 2018-07-26 哌嗪并杂芳基类衍生物、其制备方法及其在医药上的应用

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CN109952305B CN109952305B (zh) 2022-06-21

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US (1) US11247998B2 (zh)
EP (1) EP3660018A4 (zh)
JP (1) JP2020528062A (zh)
KR (1) KR20200032702A (zh)
CN (1) CN109952305B (zh)
AU (1) AU2018305614B2 (zh)
BR (1) BR112020001299A2 (zh)
CA (1) CA3070004A1 (zh)
RU (1) RU2745431C1 (zh)
WO (1) WO2019020070A1 (zh)
ZA (1) ZA201908609B (zh)

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CN113039186A (zh) * 2018-11-02 2021-06-25 艾库里斯有限及两合公司 抗乙型肝炎病毒HBV的脲6,7-二氢-4H-吡唑并[1,5-a]吡嗪活性剂
CN114146582A (zh) * 2021-11-30 2022-03-08 南京工业大学 一种氟化zif-90改性pdms膜的制备方法

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UY38436A (es) * 2018-11-02 2020-05-29 Aicuris Gmbh & Co Kg Nuevas 6,7-dihidro-4h-pirazolo[1,5-a] pirazinindol-2-carboxamidas activas contra el virus de la hepatitis b (vhb)
CN111484497B (zh) * 2019-01-25 2021-07-02 江苏恒瑞医药股份有限公司 咪唑并[1,5-a]吡嗪类衍生物的可药用盐、晶型及其制备方法
CN111484498B (zh) * 2019-01-25 2021-05-14 江苏恒瑞医药股份有限公司 咪唑并[1,5-a]吡嗪类化合物的晶型及其制备方法
AU2020210998A1 (en) * 2019-01-25 2021-09-16 Jiangsu Hengrui Medicine Co., Ltd. Crystal form of 1,2,3-triazolo(1,5-a)pyrazines derivative and preparation method for crystal form
US20220227789A1 (en) 2019-04-30 2022-07-21 Aicuris Gmbh & Co. Kg Novel indolizine-2-carboxamides active against the hepatitis b virus (hbv)
JP2022531199A (ja) 2019-04-30 2022-07-06 アイクリス ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト Ｂ型肝炎ウイルス（ｈｂｖ）に対し活性な新規のフェニル及びピリジル尿素
AU2020267015A1 (en) 2019-04-30 2021-12-23 Aicuris Gmbh & Co. Kg Novel indole-2-carboxamides active against the hepatitis B virus (HBV)
SG11202111493WA (en) 2019-04-30 2021-11-29 Aicuris Gmbh & Co Kg Novel oxalyl piperazines active against the hepatitis b virus (hbv)
CN112778299B (zh) * 2019-11-04 2023-07-14 江苏恒瑞医药股份有限公司 哌嗪脲基类衍生物、其制备方法及其在医药上的应用
WO2022022613A1 (zh) * 2020-07-29 2022-02-03 江苏恒瑞医药股份有限公司 一种三氮唑并[1，5-a]吡嗪制备方法及其应用
CN114057745A (zh) * 2020-07-29 2022-02-18 江苏恒瑞医药股份有限公司 一种三氮唑并[1,5-a]吡嗪制备方法及其应用
US11845752B2 (en) 2020-10-15 2023-12-19 Aligos Therapeutics, Inc. Substituted imidazo[1,5-a]pyrazines for the treatment of hepatitis B
WO2022166778A1 (zh) * 2021-02-04 2022-08-11 江苏恒瑞医药股份有限公司 一种衣壳蛋白抑制剂的药物组合物及其制备方法

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CN113039186A (zh) * 2018-11-02 2021-06-25 艾库里斯有限及两合公司 抗乙型肝炎病毒HBV的脲6,7-二氢-4H-吡唑并[1,5-a]吡嗪活性剂
CN114146582A (zh) * 2021-11-30 2022-03-08 南京工业大学 一种氟化zif-90改性pdms膜的制备方法

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AU2018305614A1 (en) 2020-03-05
EP3660018A1 (en) 2020-06-03
AU2018305614B2 (en) 2022-05-12
ZA201908609B (en) 2022-07-27
EP3660018A4 (en) 2021-04-21
CA3070004A1 (en) 2019-01-31
US20200157111A1 (en) 2020-05-21
KR20200032702A (ko) 2020-03-26
BR112020001299A2 (pt) 2020-07-28
RU2745431C1 (ru) 2021-03-25
CN109952305B (zh) 2022-06-21
WO2019020070A1 (zh) 2019-01-31
US11247998B2 (en) 2022-02-15
JP2020528062A (ja) 2020-09-17

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