CN112469713A - 芳基磷氧化物类衍生物抑制剂、其制备方法和应用 - Google Patents

芳基磷氧化物类衍生物抑制剂、其制备方法和应用 Download PDF

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CN112469713A
CN112469713A CN202080004102.4A CN202080004102A CN112469713A CN 112469713 A CN112469713 A CN 112469713A CN 202080004102 A CN202080004102 A CN 202080004102A CN 112469713 A CN112469713 A CN 112469713A
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alkyl
substituted
cycloalkyl
halogen
unsubstituted
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CN112469713B (zh
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高鹏
王少宝
孙广俊
修文华
谭松良
蔡家强
包如迪
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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    • 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
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明涉及芳基磷氧化物类衍生物抑制剂、其制备方法和应用。特别地，本发明涉及通式(IA)所示的化合物、其制备方法及含有该化合物的药物组合物，及其作为EGFR抑制剂在治疗癌症相关疾病中的用途。

Description

PCT国内申请，说明书已公开。

Claims (30)

  1. PCT国内申请，权利要求书已公开。
CN202080004102.4A 2019-06-21 2020-06-22 芳基磷氧化物类衍生物抑制剂、其制备方法和应用 Active CN112469713B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
CN2019105449274 2019-06-21
CN201910544927 2019-06-21
CN201910927802X 2019-09-27
CN201910927802 2019-09-27
CN202010033871 2020-01-13
CN2020100338719 2020-01-13
CN202010334631 2020-04-24
CN2020103346312 2020-04-24
PCT/CN2020/097362 WO2020253860A1 (zh) 2019-06-21 2020-06-22 芳基磷氧化物类衍生物抑制剂、其制备方法和应用

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CN112469713A true CN112469713A (zh) 2021-03-09
CN112469713B CN112469713B (zh) 2023-09-01

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Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111410667A (zh) * 2019-01-08 2020-07-14 武汉宇科源医药生物科技有限公司 新型(1,2,4)三唑并(1,5-a)吡啶基磷氧化物及其用途
CN112168820B (zh) * 2019-07-05 2023-09-29 中国科学院生物物理研究所 SRCAP ATPase抑制剂在结直肠癌治疗中的应用
AU2020385527B2 (en) * 2019-11-21 2023-04-13 Tyk Medicines, Inc. Compound used as EGFR kinase inhibitor and use thereof
CN113717156B (zh) * 2020-05-25 2023-05-09 南京红云生物科技有限公司 Egfr抑制剂、其制备方法及用途
CN115715289A (zh) * 2020-06-03 2023-02-24 江苏先声药业有限公司 多芳基化合物及应用
CN116438172A (zh) * 2020-11-13 2023-07-14 南京红云生物科技有限公司 Hpk1激酶调节剂、其制备方法与应用
CN116234556A (zh) * 2020-12-18 2023-06-06 江苏豪森药业集团有限公司 一种芳基磷氧化物类衍生物自由碱的晶型及其制备方法和应用
WO2022146027A1 (ko) * 2020-12-29 2022-07-07 주식회사 비투에스바이오 헤테로아릴 유도체 화합물 및 이의 용도
WO2022227032A1 (en) * 2021-04-30 2022-11-03 Beigene (Beijing) Co., Ltd. Egfr degraders and associated methods of use
WO2022271630A1 (en) * 2021-06-22 2022-12-29 Blueprint Medicines Corporation Egfr inhibitors
WO2022271749A1 (en) * 2021-06-22 2022-12-29 Blueprint Medicines Corporation Heterocyclic egfr inhibitors for use in the treatment of cancer
CN117836286A (zh) * 2021-06-22 2024-04-05 缆图药品公司 用于治疗癌症的杂环egfr抑制剂
CN117858872A (zh) * 2021-06-22 2024-04-09 缆图药品公司 用于治疗癌症的杂环egfr抑制剂
EP4367112A1 (en) 2021-07-09 2024-05-15 Plexium, Inc. Aryl compounds and pharmaceutical compositions that modulate ikzf2
WO2023011610A1 (zh) * 2021-08-06 2023-02-09 南京红云生物科技有限公司 苯并二噁烷类化合物、其制备方法与应用
CN116178433A (zh) * 2021-11-26 2023-05-30 南京正大天晴制药有限公司 Axl激酶抑制剂的盐及其制备方法和用途
CN116178434A (zh) * 2021-11-26 2023-05-30 南京正大天晴制药有限公司 Axl激酶抑制剂的单对甲苯磺酸盐及其晶型
WO2024005516A1 (ko) * 2022-06-28 2024-01-04 보로노이 주식회사 헤테로아릴 유도체 화합물 및 이의 용도
KR20240046408A (ko) * 2022-09-30 2024-04-09 주식회사 테라펙스 단백질 키나아제 저해 활성을 갖는 피리미딘 유도체 및 이를 포함하는 치료용 약학 조성물

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1293665A (zh) * 1998-02-18 2001-05-02 神经研究公司 新化合物及其用作阳性ampa受体调节剂
CN1697830A (zh) * 2002-03-15 2005-11-16 诺瓦提斯公司 嘧啶衍生物
CN1852900A (zh) * 2003-09-18 2006-10-25 诺瓦提斯公司 可用于治疗增殖性病症的2,4－二(苯基氨基)嘧啶类
CN1882578A (zh) * 2003-09-16 2006-12-20 诺瓦提斯公司 作为zap－70和/或syk抑制剂的2,4－二(杂)芳基氨基嘧啶衍生物
WO2007120596A1 (en) * 2006-04-12 2007-10-25 Wyeth DIHYDRO[1,4]DIOXINO[2,3-e]INDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS
CN101730692A (zh) * 2007-03-15 2010-06-09 先灵公司 用作葡聚糖合成酶抑制剂的哒嗪酮衍生物
CN103153064A (zh) * 2010-10-14 2013-06-12 阿里亚德医药股份有限公司 抑制egfr导致的癌症中细胞增殖的方法
WO2019015655A1 (zh) * 2017-07-19 2019-01-24 正大天晴药业集团股份有限公司 作为egfr激酶抑制剂的芳基磷氧化合物

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6939874B2 (en) * 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
EP2154967B9 (en) * 2007-04-16 2014-07-23 Hutchison Medipharma Enterprises Limited Pyrimidine derivatives
CN106831730B (zh) * 2017-01-11 2019-11-26 温州医科大学 一种取代的二氨基嘧啶类化合物及其在制备抗恶性肿瘤药物中的用途
TWI702205B (zh) * 2017-10-06 2020-08-21 俄羅斯聯邦商拜奧卡德聯合股份公司 表皮生長因子受體抑制劑
CN108101926B (zh) * 2018-02-07 2019-12-13 郑州大学 含喹啉酮的嘧啶并五元杂环类化合物、制备方法及其应用
CN111410667A (zh) * 2019-01-08 2020-07-14 武汉宇科源医药生物科技有限公司 新型(1,2,4)三唑并(1,5-a)吡啶基磷氧化物及其用途

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1293665A (zh) * 1998-02-18 2001-05-02 神经研究公司 新化合物及其用作阳性ampa受体调节剂
CN1697830A (zh) * 2002-03-15 2005-11-16 诺瓦提斯公司 嘧啶衍生物
CN1882578A (zh) * 2003-09-16 2006-12-20 诺瓦提斯公司 作为zap－70和/或syk抑制剂的2,4－二(杂)芳基氨基嘧啶衍生物
CN1852900A (zh) * 2003-09-18 2006-10-25 诺瓦提斯公司 可用于治疗增殖性病症的2,4－二(苯基氨基)嘧啶类
WO2007120596A1 (en) * 2006-04-12 2007-10-25 Wyeth DIHYDRO[1,4]DIOXINO[2,3-e]INDAZOLE DERIVATIVES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS
CN101730692A (zh) * 2007-03-15 2010-06-09 先灵公司 用作葡聚糖合成酶抑制剂的哒嗪酮衍生物
CN103153064A (zh) * 2010-10-14 2013-06-12 阿里亚德医药股份有限公司 抑制egfr导致的癌症中细胞增殖的方法
WO2019015655A1 (zh) * 2017-07-19 2019-01-24 正大天晴药业集团股份有限公司 作为egfr激酶抑制剂的芳基磷氧化合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
STN检索: "RN1824373-78-5", 《STN》 *

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CN112513029B (zh) 2023-10-24
WO2020253862A1 (zh) 2020-12-24
WO2020253860A1 (zh) 2020-12-24
CN112469713B (zh) 2023-09-01
CN112513029A (zh) 2021-03-16
TW202115042A (zh) 2021-04-16

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