CN115087641A - 2-氨基嘧啶类化合物及其药物组合物和应用 - Google Patents

2-氨基嘧啶类化合物及其药物组合物和应用 Download PDF

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Publication number
CN115087641A
CN115087641A CN202180005255.5A CN202180005255A CN115087641A CN 115087641 A CN115087641 A CN 115087641A CN 202180005255 A CN202180005255 A CN 202180005255A CN 115087641 A CN115087641 A CN 115087641A
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substituted
pharmaceutically acceptable
alkyl
tautomer
stereoisomer
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CN115087641B (zh
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丁克
李姗
张章
司鸿飞
涂正超
任小梅
雷冲
唐霞
高悦译
陈成斌
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Guangzhou Lixin Biotechnology Co ltd
Jinan University
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Guangzhou Lixin Pharmaceuticals Co ltd
Jinan University
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • 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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

本发明提供了一种具有式(Ⅰ)所示结构的2‑氨基嘧啶类化合物或者其药学上可接受的盐、同位素衍生物、溶剂化物，或者其立体异构体、几何异构体、互变异构体，或者其前药分子、代谢产物，及其药用组合物和应用。本发明涉及的化合物可以高效、高选择性地抑制Janus Kinase 3(JAK3)的激酶活性，对多种血液肿瘤细胞(尤其是人急性髓系白血病细胞U937细胞)和实体瘤细胞均具有较强的信号抑制作用和细胞增殖抑制作用，可用于制备抗肿瘤药物，并且可以用于制备防治炎症性疾病的药物。

Description

PCT国内申请，说明书已公开。

Claims (23)

  1. PCT国内申请，权利要求书已公开。
CN202180005255.5A 2021-01-11 2021-12-31 2-氨基嘧啶类化合物及其药物组合物和应用 Active CN115087641B (zh)

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CN202110032031 2021-01-11
CN2021100320315 2021-01-11
PCT/CN2021/143765 WO2022148317A1 (zh) 2021-01-11 2021-12-31 2-氨基嘧啶类化合物及其药物组合物和应用

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CN115087641A true CN115087641A (zh) 2022-09-20
CN115087641B CN115087641B (zh) 2024-06-18

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US (1) US20230348487A1 (zh)
EP (1) EP4279486A1 (zh)
JP (1) JP2024502163A (zh)
CN (1) CN115087641B (zh)
AU (1) AU2021416682B2 (zh)
WO (1) WO2022148317A1 (zh)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102083800A (zh) * 2008-06-27 2011-06-01 阿维拉制药公司 杂芳基化合物和其用途
CN104144915A (zh) * 2012-02-28 2014-11-12 安斯泰来制药有限公司 含氮芳香族杂环化合物
WO2015148867A1 (en) * 2014-03-28 2015-10-01 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN104974140A (zh) * 2014-04-14 2015-10-14 上海海雁医药科技有限公司 2,3,4,6-四取代苯-1,5-二胺衍生物、其制法与医药上的用途
CN108309959A (zh) * 2018-02-06 2018-07-24 宁波新靶生物医药科技有限公司 N或o或c-二芳基取代衍生物的合成及其药学应用

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060270694A1 (en) * 2005-05-03 2006-11-30 Rigel Pharmaceuticals, Inc. JAK kinase inhibitors and their uses
UA109412C2 (uk) * 2005-11-01 2015-08-25 5-метил-n2-[4-(4-метилпіперазин-1-іл)феніл]-піримідин-2,4-діамін та його застосування в способі одержання сполуки
WO2015094803A1 (en) * 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN106478651B (zh) * 2015-08-31 2019-07-09 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
CN110317176A (zh) * 2019-07-04 2019-10-11 沈阳药科大学 2-氨基嘧啶类化合物及其用途

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102083800A (zh) * 2008-06-27 2011-06-01 阿维拉制药公司 杂芳基化合物和其用途
CN104144915A (zh) * 2012-02-28 2014-11-12 安斯泰来制药有限公司 含氮芳香族杂环化合物
WO2015148867A1 (en) * 2014-03-28 2015-10-01 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN104974140A (zh) * 2014-04-14 2015-10-14 上海海雁医药科技有限公司 2,3,4,6-四取代苯-1,5-二胺衍生物、其制法与医药上的用途
CN108309959A (zh) * 2018-02-06 2018-07-24 宁波新靶生物医药科技有限公司 N或o或c-二芳基取代衍生物的合成及其药学应用

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EP4279486A1 (en) 2023-11-22
US20230348487A1 (en) 2023-11-02
AU2021416682B2 (en) 2024-01-11
WO2022148317A1 (zh) 2022-07-14
CN115087641B (zh) 2024-06-18
JP2024502163A (ja) 2024-01-17
AU2021416682A1 (en) 2023-07-06

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