CN107835811A - 苯胺嘧啶衍生物及其用途 - Google Patents

苯胺嘧啶衍生物及其用途 Download PDF

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Publication number
CN107835811A
CN107835811A CN201680041201.3A CN201680041201A CN107835811A CN 107835811 A CN107835811 A CN 107835811A CN 201680041201 A CN201680041201 A CN 201680041201A CN 107835811 A CN107835811 A CN 107835811A
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China
Prior art keywords
methyl
amino
compound
pyrimidine
imidazoles
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CN201680041201.3A
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CN107835811B (zh
Inventor
朱岩
赵娜
商现星
胡远东
彭勇
张慧
刘波
罗鸿
韩永信
杨玲
徐宏江
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Shouyao Holdings Beijing Co Ltd
Original Assignee
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Shouyao Holdings Beijing Co Ltd
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Publication of CN107835811A publication Critical patent/CN107835811A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

本公开涉及作为EGFR抑制剂的苯胺嘧啶衍生物或其药学上可接受的盐，具体涉及式（Ⅰ）所示化合物或其药学上可接受的盐、其药物组合物、及其用于治疗EGFR介导的疾病的方法和用途。

Description

PCT国内申请，说明书已公开。

Claims (12)

  1. PCT国内申请，权利要求书已公开。
CN201680041201.3A 2015-07-16 2016-07-15 苯胺嘧啶衍生物及其用途 Active CN107835811B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510419018 2015-07-16
CN201510419018X 2015-07-16
PCT/CN2016/090149 WO2017008761A1 (zh) 2015-07-16 2016-07-15 苯胺嘧啶衍生物及其用途

Publications (2)

Publication Number Publication Date
CN107835811A true CN107835811A (zh) 2018-03-23
CN107835811B CN107835811B (zh) 2019-11-08

Family

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Country Status (11)

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US (1) US10329277B2 (zh)
EP (1) EP3323817B1 (zh)
JP (1) JP6970081B2 (zh)
KR (1) KR102666414B1 (zh)
CN (1) CN107835811B (zh)
AU (1) AU2016292450B2 (zh)
CA (1) CA2992317A1 (zh)
HK (1) HK1250164A1 (zh)
RU (1) RU2734849C2 (zh)
TW (1) TWI739753B (zh)
WO (1) WO2017008761A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114026090A (zh) * 2019-07-04 2022-02-08 微境生物医药科技(上海)有限公司 一类抑制egfr激酶的化合物及其制备方法和用途

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111170999B (zh) * 2014-10-11 2023-06-30 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用
CN111170998B (zh) 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
KR20180105161A (ko) 2016-01-07 2018-09-27 씨에스 파마테크 리미티드 Egfr 티로신 키나제의 임상적으로 중요한 돌연변이체의 선택적 억제제
CN107540661A (zh) * 2016-06-24 2018-01-05 正大天晴药业集团股份有限公司 作为egfr抑制剂的苯胺嘧啶化合物的结晶
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
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
WO2020245208A1 (en) 2019-06-04 2020-12-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use

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WO2011140338A1 (en) * 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CN103702990A (zh) * 2011-07-27 2014-04-02 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症
CN105085489A (zh) * 2014-11-05 2015-11-25 上海页岩科技有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
CN106117185A (zh) * 2015-08-31 2016-11-16 广州科擎新药开发有限公司 2,4‑二含氮基团取代嘧啶类化合物及其制备方法和应用

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MXPA02003436A (es) 1999-10-07 2002-08-20 Amgen Inc Inhibidores de triazina cinasa.
CA2400447C (en) 2000-02-17 2008-04-22 Amgen Inc. Kinase inhibitors
HN2005000795A (es) * 2004-10-15 2010-08-19 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
WO2011053476A1 (en) * 2009-11-02 2011-05-05 Abbott Laboratories Imidazopyridines as a novel scaffold for multi-targeted kinase inhibition
BR112012011109A2 (pt) * 2009-11-12 2019-09-24 Selvita S A um composto um processo para sua preparação uma composição farmaceutica uso de um composto um metodo modular ou regular serina treonina quinases
CN104761544B (zh) * 2014-01-03 2019-03-15 北京轩义医药科技有限公司 Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011140338A1 (en) * 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CN103702990A (zh) * 2011-07-27 2014-04-02 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症
CN105085489A (zh) * 2014-11-05 2015-11-25 上海页岩科技有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
CN106117185A (zh) * 2015-08-31 2016-11-16 广州科擎新药开发有限公司 2,4‑二含氮基团取代嘧啶类化合物及其制备方法和应用

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114026090A (zh) * 2019-07-04 2022-02-08 微境生物医药科技(上海)有限公司 一类抑制egfr激酶的化合物及其制备方法和用途
CN114026090B (zh) * 2019-07-04 2023-01-06 微境生物医药科技(上海)有限公司 一类抑制egfr激酶的化合物及其制备方法和用途

Also Published As

Publication number Publication date
WO2017008761A1 (zh) 2017-01-19
HK1250164A1 (zh) 2018-11-30
RU2018102963A (ru) 2019-08-16
EP3323817A4 (en) 2019-04-10
KR20180030190A (ko) 2018-03-21
CN107835811B (zh) 2019-11-08
RU2018102963A3 (zh) 2019-12-24
EP3323817A1 (en) 2018-05-23
US10329277B2 (en) 2019-06-25
EP3323817B1 (en) 2022-10-19
TW201703768A (zh) 2017-02-01
US20180208581A1 (en) 2018-07-26
JP6970081B2 (ja) 2021-11-24
KR102666414B1 (ko) 2024-05-17
JP2018520190A (ja) 2018-07-26
CA2992317A1 (en) 2017-01-19
RU2734849C2 (ru) 2020-10-23
AU2016292450B2 (en) 2021-03-25
AU2016292450A1 (en) 2018-02-15
TWI739753B (zh) 2021-09-21

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