CN114206872A - 咪唑并[2,1-f][1,2,4]三嗪-4-胺衍生物作为tlr8激动剂 - Google Patents

咪唑并[2,1-f][1,2,4]三嗪-4-胺衍生物作为tlr8激动剂 Download PDF

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Publication number
CN114206872A
CN114206872A CN202080055549.4A CN202080055549A CN114206872A CN 114206872 A CN114206872 A CN 114206872A CN 202080055549 A CN202080055549 A CN 202080055549A CN 114206872 A CN114206872 A CN 114206872A
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alkyl
heterocyclyl
imidazo
optionally substituted
piperidin
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张国良
苗建壮
王策
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Beigene Ltd
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Beigene Ltd
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    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/08—Antiallergic agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

本发明公开了用作TLR8激动剂的咪唑并[2,1‑f][1,2,4]三嗪‑4‑胺衍生物或其立体异构体或其药学上可接受的盐，以及包含其的药物组合物。本发明还公开了使用咪唑并[2,1‑f][1,2,4]三嗪‑4‑胺衍生物或其立体异构体或其药学上可接受的盐作为TLR8激动剂来治疗癌症的方法。

Description

PCT国内申请，说明书已公开。

Claims (21)

  1. PCT国内申请，权利要求书已公开。
CN202080055549.4A 2019-08-02 2020-07-31 咪唑并[2,1-f][1,2,4]三嗪-4-胺衍生物作为tlr8激动剂 Pending CN114206872A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
CN2019099147 2019-08-02
CNPCT/CN2019/099147 2019-08-02
CN2019109398163 2019-09-30
CN201910939816 2019-09-30
CN2019112045237 2019-11-29
CN201911204523 2019-11-29
CN2020100759506 2020-01-22
CN202010075950 2020-01-22
PCT/CN2020/106190 WO2021023105A1 (zh) 2019-08-02 2020-07-31 咪唑并[2,1-f][1,2,4]三嗪-4-胺衍生物作为tlr8激动剂

Publications (1)

Publication Number Publication Date
CN114206872A true CN114206872A (zh) 2022-03-18

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
CN202080055549.4A Pending CN114206872A (zh) 2019-08-02 2020-07-31 咪唑并[2,1-f][1,2,4]三嗪-4-胺衍生物作为tlr8激动剂
CN202010758378.3A Pending CN112321590A (zh) 2019-08-02 2020-07-31 咪唑并[2,1-f][1,2,4]三嗪-4-胺衍生物作为tlr8激动剂

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CN202010758378.3A Pending CN112321590A (zh) 2019-08-02 2020-07-31 咪唑并[2,1-f][1,2,4]三嗪-4-胺衍生物作为tlr8激动剂

Country Status (7)

Country Link
US (1) US20220289752A1 (zh)
EP (1) EP4008720A4 (zh)
JP (1) JP2022542269A (zh)
KR (1) KR20220041838A (zh)
CN (2) CN114206872A (zh)
TW (1) TW202115078A (zh)
WO (1) WO2021023105A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4385985A1 (en) 2021-08-11 2024-06-19 Xizang Haisco Pharmaceutical Co., Ltd. Heterocyclic derivative, and composition and pharmaceutical use thereof
WO2023125681A1 (en) * 2021-12-29 2023-07-06 Beigene, Ltd. Heterocyclic compounds
WO2023125121A1 (zh) * 2021-12-30 2023-07-06 四川科伦博泰生物医药股份有限公司 一类三并环化合物、其制备方法及用途

Citations (1)

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CN105367576A (zh) * 2014-08-15 2016-03-02 正大天晴药业集团股份有限公司 作为tlr7激动剂的吡咯并嘧啶化合物

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EP2396328A2 (en) * 2009-02-11 2011-12-21 The Regents of The University of California Toll-like receptor modulators and treatment of diseases
JO3407B1 (ar) * 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
BR112017002811B1 (pt) 2014-08-15 2022-09-06 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Compostos de pirrolopirimidina usados como agonista de tlr7 e seu uso, composição farmacêutica e kit
CN105732635A (zh) * 2014-12-29 2016-07-06 南京明德新药研发股份有限公司 一类Toll样受体7激动剂
AR108875A1 (es) * 2016-06-24 2018-10-03 Incyte Corp COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
CN108069969B (zh) * 2016-11-11 2020-09-18 南京海璞医药科技有限公司 含氮杂环化合物、制备方法、中间体、药物组合物和应用
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KR20210125025A (ko) * 2019-02-07 2021-10-15 베이진 엘티디 Tlr7 작용제로서의 이미다조[2,1-f][1,2,4]트리아진-4-아민 유도체

Patent Citations (1)

* Cited by examiner, † Cited by third party
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Non-Patent Citations (1)

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Title
SALUNKE D.B.等: "Structure−Activity Relationships in Human Toll-like Receptor 8‑Active 2,3-Diamino-furo[2,3‑c]pyridines", JOURNAL OF MEDICINAL CHEMISTRY, vol. 55, no. 18, pages 8137, XP055195425, DOI: 10.1021/jm301066h *

Also Published As

Publication number Publication date
EP4008720A1 (en) 2022-06-08
CN112321590A (zh) 2021-02-05
JP2022542269A (ja) 2022-09-30
KR20220041838A (ko) 2022-04-01
TW202115078A (zh) 2021-04-16
EP4008720A4 (en) 2023-08-02
US20220289752A1 (en) 2022-09-15
WO2021023105A1 (zh) 2021-02-11

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