CN106661000A - Egfr抑制剂及其制备和应用 - Google Patents

Egfr抑制剂及其制备和应用 Download PDF

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CN106661000A
CN106661000A CN201580045311.2A CN201580045311A CN106661000A CN 106661000 A CN106661000 A CN 106661000A CN 201580045311 A CN201580045311 A CN 201580045311A CN 106661000 A CN106661000 A CN 106661000A
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compound
methyl
formula
amino
pyrimidine
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CN201580045311.2A
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CN106661000B (zh
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危明松
孙广俊
谭松良
高鹏
王少宝
修文华
张福军
包如迪
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
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Lianyungang Hongchuang Pharmaceutical Co ltd
Shanghai Hansoh Biomedical Co Ltd
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Priority to CN201910210386.1A priority Critical patent/CN111171000B/zh
Priority to CN201910210387.6A priority patent/CN111187221B/zh
Priority to CN202311029815.8A priority patent/CN117069700A/zh
Priority to CN202311339167.6A priority patent/CN117402143A/zh
Priority to CN201910208542.0A priority patent/CN111170999B/zh
Priority to CN202311030017.7A priority patent/CN117050062A/zh
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    • A—HUMAN NECESSITIES
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    • 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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

一种如式(I)所示的4‑取代‑2‑(N‑(5‑取代烯丙酰胺基)苯基)氨基)嘧啶衍生物以及其作为EGFR抑制剂的制备和应用，该化合物具有抑制L858R EGFR突变体、T790M EGFR突变体和外显子19缺失激活突变体的活性，可以用来治疗单独或部分地由EGFR突变体活性介导疾病，在预防与治疗癌症尤其是非小细胞肺癌药物中的具有广泛应用。

Description

PCT国内申请，说明书已公开。

Claims (49)

  1. PCT国内申请，权利要求书已公开。
CN201580045311.2A 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用 Active CN106661000B (zh)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CN201910210386.1A CN111171000B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201910210387.6A CN111187221B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN202311029815.8A CN117069700A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN202311339167.6A CN117402143A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201910208542.0A CN111170999B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN202311030017.7A CN117050062A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用

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CN2014105342039 2014-10-11
CN201410534203 2014-10-11
PCT/CN2015/091189 WO2016054987A1 (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用

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CN202311030017.7A Division CN117050062A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201910210386.1A Division CN111171000B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201910208542.0A Division CN111170999B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201910210387.6A Division CN111187221B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN202311339167.6A Division CN117402143A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN202311029815.8A Division CN117069700A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用

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CN106661000A true CN106661000A (zh) 2017-05-10
CN106661000B CN106661000B (zh) 2019-04-09

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CN202311339167.6A Pending CN117402143A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201910210387.6A Active CN111187221B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201910208542.0A Active CN111170999B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201580045311.2A Active CN106661000B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201910210386.1A Active CN111171000B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN202311029815.8A Pending CN117069700A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN202311030017.7A Pending CN117050062A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用

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CN201910210387.6A Active CN111187221B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN201910208542.0A Active CN111170999B (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用

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CN202311029815.8A Pending CN117069700A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用
CN202311030017.7A Pending CN117050062A (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用

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CN (7) CN117402143A (zh)
AU (1) AU2015330506B2 (zh)
BR (1) BR112017006713B1 (zh)
CA (1) CA2959194A1 (zh)
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Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105384694A (zh) * 2014-08-22 2016-03-09 四川海思科制药有限公司 一种取代的氨基嘧啶衍生物及其制备方法和药物用途
CN106928150A (zh) * 2015-12-31 2017-07-07 恩瑞生物医药科技（上海）有限公司 丙烯酰胺苯胺衍生物及其药学上的应用
CN108017633A (zh) * 2018-01-30 2018-05-11 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺衍生物及应用
CN110652514A (zh) * 2018-06-29 2020-01-07 上海翰森生物医药科技有限公司 第三代egfr抑制剂的制药用途
CN110684016A (zh) * 2019-09-27 2020-01-14 上海应用技术大学 一种含氟的azd9291衍生物及其制备方法和应用
CN112645932A (zh) * 2016-03-22 2021-04-13 江苏豪森药业集团有限公司 Egfr抑制剂游离碱或其酸式盐的多晶型、其制备方法和应用
CN113387935A (zh) * 2021-07-23 2021-09-14 苏州雅深智慧科技有限公司 抑制三突变表皮生长因子受体酪氨酸激酶的化合物及用途
CN114605400A (zh) * 2019-03-19 2022-06-10 株式会社沃若诺伊 杂芳基衍生物、其制备方法、及含其作为有效成分的药物组合物

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CA2949793C (en) 2014-06-19 2024-02-27 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CN105085489B (zh) 2014-11-05 2019-03-01 益方生物科技（上海）有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
CN107406442B (zh) 2014-12-23 2021-08-17 达纳－法伯癌症研究所公司 作为egfr抑制剂的新的嘧啶和治疗病症的方法
CN106117185B (zh) 2015-08-31 2017-11-07 广州必贝特医药技术有限公司 2,4‑二含氮基团取代嘧啶类化合物及其制备方法和应用
CN106749193B (zh) * 2015-11-23 2020-11-20 南京圣和药业股份有限公司 吲唑取代的表皮生长因子受体抑制剂及其应用
KR20180105161A (ko) * 2016-01-07 2018-09-27 씨에스 파마테크 리미티드 Egfr 티로신 키나제의 임상적으로 중요한 돌연변이체의 선택적 억제제
WO2017119732A1 (en) 2016-01-08 2017-07-13 Samsung Electronics Co., Ltd. Electronic device and operating method thereof
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