CN115348963A - 吡啶并嘧啶类化合物及其应用 - Google Patents

吡啶并嘧啶类化合物及其应用 Download PDF

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CN115348963A
CN115348963A CN202280001130.XA CN202280001130A CN115348963A CN 115348963 A CN115348963 A CN 115348963A CN 202280001130 A CN202280001130 A CN 202280001130A CN 115348963 A CN115348963 A CN 115348963A
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substituted
cycloalkyl
alkyl
membered heterocycloalkyl
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CN115348963B (zh
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丁克
张鑫
许芳
任小梅
陆小云
马大为
黄维雪
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Shanghai Institute of Organic Chemistry of CAS
Jinan University
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Shanghai Institute of Organic Chemistry of CAS
Jinan University
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

本发明提供了一种具有式(Ⅰ)所示结构的吡啶并嘧啶类化合物或者其药学上可接受的盐或者其立体异构体或者其前药分子，及其应用。本发明涉及的化合物可以高效、高选择性地降解细胞中的AKT3蛋白，而对AKT1/2无影响，从而能够显著抑制AKT3高表达介导的肿瘤细胞增殖，可用于制备与AKT3蛋白异常表达相关的癌症和其它相关疾病的治疗药物。

Description

PCT国内申请，说明书已公开。

Claims (27)

  1. PCT国内申请，权利要求书已公开。
CN202280001130.XA 2021-03-08 2022-03-07 吡啶并嘧啶类化合物及其应用 Active CN115348963B (zh)

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CN202110251924 2021-03-08
CN2021102519249 2021-03-08
PCT/CN2022/079597 WO2022188755A1 (zh) 2021-03-08 2022-03-07 吡啶并嘧啶类化合物及其应用

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JP (1) JP2024508901A (zh)
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WO2012065019A2 (en) * 2010-11-12 2012-05-18 Exelixis, Inc. Pyridopyrimidinone inhibitors of p13k alpha
WO2014079232A1 (zh) * 2012-11-22 2014-05-30 中国科学院广州生物医药与健康研究院 7-氧代吡啶并嘧啶类化合物及其药用组合物和应用
WO2014134308A1 (en) * 2013-03-01 2014-09-04 Amgen Inc. Substituted 7-oxo-pyrido [2, 3-d] pyrimidines and their use for the treatment of egfr / erbb2 related disorders
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WO2018233620A1 (zh) * 2017-06-21 2018-12-27 江苏恒瑞医药股份有限公司 SERD与CDK4/6抑制剂、PI3K/mTOR通路抑制剂的用途
CN109305967A (zh) * 2017-07-28 2019-02-05 中国科学院上海药物研究所 新型嘧啶并杂环类化合物及制备方法和用途
CN111297867A (zh) * 2020-03-31 2020-06-19 黄泳华 含有吡啶基氨基吡啶并嘧啶衍生物的组合物在制备用于治疗乳腺癌的药物中的用途

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RU2006121990A (ru) * 2003-11-21 2007-12-27 Эррэй Биофарма Инк. (Us) Ингибиторы протеинкиназ акт

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CN1422268A (zh) * 2000-03-06 2003-06-04 沃尼尔·朗伯公司 5－烷基吡啶并[2,3－d]嘧啶酪氨酸激酶抑制剂
WO2006021547A1 (de) * 2004-08-26 2006-03-02 Boehringer Ingelheim International Gmbh Pteridinone als plk (polo like kinase) inhibitoren
WO2012065019A2 (en) * 2010-11-12 2012-05-18 Exelixis, Inc. Pyridopyrimidinone inhibitors of p13k alpha
WO2014079232A1 (zh) * 2012-11-22 2014-05-30 中国科学院广州生物医药与健康研究院 7-氧代吡啶并嘧啶类化合物及其药用组合物和应用
WO2014134308A1 (en) * 2013-03-01 2014-09-04 Amgen Inc. Substituted 7-oxo-pyrido [2, 3-d] pyrimidines and their use for the treatment of egfr / erbb2 related disorders
CN107840846A (zh) * 2016-09-19 2018-03-27 郑州泰基鸿诺医药股份有限公司 一种含嘧啶环的化合物、egfr抑制剂及其应用
WO2018233620A1 (zh) * 2017-06-21 2018-12-27 江苏恒瑞医药股份有限公司 SERD与CDK4/6抑制剂、PI3K/mTOR通路抑制剂的用途
CN109305967A (zh) * 2017-07-28 2019-02-05 中国科学院上海药物研究所 新型嘧啶并杂环类化合物及制备方法和用途
CN111297867A (zh) * 2020-03-31 2020-06-19 黄泳华 含有吡啶基氨基吡啶并嘧啶衍生物的组合物在制备用于治疗乳腺癌的药物中的用途

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LUXI ZHANG, ET AL: "Characterization of the Novel Broad-Spectrum Kinase Inhibitor CTx-0294885 As an Affinity Reagent for Mass Spectrometry-Based Kinome Profiling", 《J. PROTEOME RES.》, vol. 12, no. 7, pages 3104 - 3116, XP055877826, DOI: 10.1021/pr3008495 *
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TIANFENG XU, ET AL: "C5-substituted pyrido[2,3-d]pyrimidin-7-ones as highly specific kinase inhibitors targeting the clinical resistance-related EGFR T790M mutant", 《MED. CHEM. COMMUN.》, vol. 6, no. 9, pages 1693 - 1697, XP055659229, DOI: 10.1039/C5MD00208G *

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CN115348963B (zh) 2024-04-19
KR20230148235A (ko) 2023-10-24
AU2022234998A1 (en) 2023-10-12
WO2022188755A1 (zh) 2022-09-15
EP4310084A1 (en) 2024-01-24
JP2024508901A (ja) 2024-02-28

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