CN110446712A - 作为A2A受体抑制剂的[1,2,4]三唑并[1,5-c]嘧啶衍生物 - Google Patents

作为A2A受体抑制剂的[1,2,4]三唑并[1,5-c]嘧啶衍生物 Download PDF

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Publication number
CN110446712A
CN110446712A CN201880020259.9A CN201880020259A CN110446712A CN 110446712 A CN110446712 A CN 110446712A CN 201880020259 A CN201880020259 A CN 201880020259A CN 110446712 A CN110446712 A CN 110446712A
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compound
pharmaceutically acceptable
isomer
acceptable salt
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CN110446712B (zh
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陈新海
于衍新
陈鑫德
张丽
陈兆国
谢程
王校飞
吴灵慧
胡国平
黎健
陈曙辉
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Yingnuohu Pharmaceutical Hangzhou Co ltd
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Medshine Discovery Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

式(Ⅰ)所示化合物、其异构体或其药学上可接受的盐，以及其在制备治疗与A2A受体相关疾病药物中的应用，其中R1、R2、R3、环A、环B、n和m为如本文中定义的。

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。
CN201880020259.9A 2017-04-07 2018-04-08 作为A2A受体抑制剂的[1,2,4]三唑并[1,5-c]嘧啶衍生物 Active CN110446712B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN2017102245539 2017-04-07
CN201710224553 2017-04-07
CN2017107378715 2017-08-24
CN201710737871 2017-08-24
CN201810129208 2018-02-08
CN2018101292081 2018-02-08
PCT/CN2018/082119 WO2018184590A1 (zh) 2017-04-07 2018-04-08 作为A 2A受体抑制剂的[1,2,4]三唑并[1,5-c]嘧啶衍生物

Publications (2)

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CN110446712A true CN110446712A (zh) 2019-11-12
CN110446712B CN110446712B (zh) 2021-09-14

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US (1) US11117899B2 (zh)
EP (1) EP3611174B1 (zh)
JP (1) JP7065113B2 (zh)
CN (1) CN110446712B (zh)
DK (1) DK3611174T3 (zh)
ES (1) ES2919474T3 (zh)
PL (1) PL3611174T3 (zh)
PT (1) PT3611174T (zh)
WO (1) WO2018184590A1 (zh)

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CN112279852A (zh) * 2018-09-12 2021-01-29 迪哲(江苏)医药股份有限公司 三唑并-嘧啶化合物和其用途
CN112384515A (zh) * 2018-02-27 2021-02-19 因赛特公司 作为a2a/a2b抑制剂的咪唑并嘧啶和三唑并嘧啶
CN109535161B (zh) * 2017-09-22 2021-09-03 江苏恒瑞医药股份有限公司 三唑并嘧啶类衍生物、其制备方法及其在医药上的应用

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US11649239B2 (en) 2018-04-28 2023-05-16 Medshine Discovery Inc. Crystal form a of (5-amino-8-(2-methyl-6-(trifluoromethyl)pyridin-4-yl)-7-phenyl-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)methanol (compound 1)
US11168089B2 (en) 2018-05-18 2021-11-09 Incyte Corporation Fused pyrimidine derivatives as A2A / A2B inhibitors
CN113166153A (zh) * 2018-07-05 2021-07-23 因赛特公司 作为a2a/a2b抑制剂的稠合吡嗪衍生物
WO2020106558A1 (en) 2018-11-20 2020-05-28 Merck Sharp & Dohme Corp. Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
US20220040184A1 (en) 2018-11-20 2022-02-10 Merck Sharp Dohme Corp. Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
JP7241871B2 (ja) 2018-11-30 2023-03-17 メルク・シャープ・アンド・ドーム・エルエルシー アデノシン受容体拮抗薬としての９－置換されたアミノトリアゾロキナゾリン誘導体、医薬組成物及びそれらの使用
BR112021009880A2 (pt) * 2018-11-30 2021-08-17 Tuojie Biotech (Shanghai) Co., Ltd. pirimidina e derivado de heterociclo de nitrogênio de cinco membros, método de preparação para os mesmos e usos médicos dos mesmos
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
CN111848625B (zh) * 2019-04-24 2022-07-26 江苏恒瑞医药股份有限公司 一种杂芳基并[4,3-c]嘧啶-5-胺类化合物的制备方法及中间体
WO2021041360A1 (en) * 2019-08-26 2021-03-04 Incyte Corporation Triazolopyrimidines as a2a / a2b inhibitors
WO2021156439A1 (en) 2020-02-06 2021-08-12 Astrazeneca Ab Triazole compounds as adenosine receptor antagonists
JP7429799B2 (ja) 2020-02-18 2024-02-08 ギリアード サイエンシーズ， インコーポレイテッド 抗ウイルス化合物
TWI775313B (zh) 2020-02-18 2022-08-21 美商基利科學股份有限公司 抗病毒化合物
TW202322824A (zh) 2020-02-18 2023-06-16 美商基利科學股份有限公司 抗病毒化合物
EP4323362A1 (en) 2021-04-16 2024-02-21 Gilead Sciences, Inc. Methods of preparing carbanucleosides using amides
US12116380B2 (en) 2021-08-18 2024-10-15 Gilead Sciences, Inc. Phospholipid compounds and methods of making and using the same

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EP0976753A1 (en) * 1997-03-24 2000-02-02 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES
WO2004092173A2 (en) * 2003-04-09 2004-10-28 Biogen Idec Ma Inc. A2a adenosine receptor antagonists
EP1544200A1 (en) * 2002-09-24 2005-06-22 Kyowa Hakko Kogyo Co., Ltd. 1,2,4 -TRIAZOLO 1,5-c PYRIMIDINE DERIVATIVE
CN109535161A (zh) * 2017-09-22 2019-03-29 江苏恒瑞医药股份有限公司 三唑并嘧啶类衍生物、其制备方法及其在医药上的应用

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TWI330183B (zh) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
PE20030739A1 (es) 2001-11-30 2003-08-28 Schering Corp Antagonistas del receptor de adenosina a2a
IL303087B1 (en) * 2018-02-27 2024-08-01 Incyte Corp Midazopyrimidines and triazolopyrimidines as A2A /A2B inhibitors
CN109535162B (zh) 2018-12-13 2020-03-24 浙江圣达生物药业股份有限公司 一种n-对氨基苯甲酰谷氨酰叶酸的制备方法

Patent Citations (4)

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EP0976753A1 (en) * 1997-03-24 2000-02-02 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES
EP1544200A1 (en) * 2002-09-24 2005-06-22 Kyowa Hakko Kogyo Co., Ltd. 1,2,4 -TRIAZOLO 1,5-c PYRIMIDINE DERIVATIVE
WO2004092173A2 (en) * 2003-04-09 2004-10-28 Biogen Idec Ma Inc. A2a adenosine receptor antagonists
CN109535161A (zh) * 2017-09-22 2019-03-29 江苏恒瑞医药股份有限公司 三唑并嘧啶类衍生物、其制备方法及其在医药上的应用

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109535161B (zh) * 2017-09-22 2021-09-03 江苏恒瑞医药股份有限公司 三唑并嘧啶类衍生物、其制备方法及其在医药上的应用
CN112384515A (zh) * 2018-02-27 2021-02-19 因赛特公司 作为a2a/a2b抑制剂的咪唑并嘧啶和三唑并嘧啶
CN112279852A (zh) * 2018-09-12 2021-01-29 迪哲(江苏)医药股份有限公司 三唑并-嘧啶化合物和其用途
US11629147B2 (en) 2018-09-12 2023-04-18 Dizal (Jiangsu) Pharmaceutical Co., Ltd. Triazolo-pyrimidine compounds and uses thereof

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JP2020516606A (ja) 2020-06-11
DK3611174T3 (da) 2022-07-04
PT3611174T (pt) 2022-07-07
US11117899B2 (en) 2021-09-14
EP3611174A1 (en) 2020-02-19
PL3611174T3 (pl) 2022-08-08
EP3611174A4 (en) 2020-09-09
WO2018184590A1 (zh) 2018-10-11
US20200131184A1 (en) 2020-04-30
CN110446712B (zh) 2021-09-14
ES2919474T3 (es) 2022-07-26
EP3611174B1 (en) 2022-06-08
JP7065113B2 (ja) 2022-05-11

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Address after: No. 291 Fucheng Road, Xiasha Street, Qiantang District, Hangzhou City, Zhejiang Province, China, and 1-1210, Heda Pharmaceutical Valley Center

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