CN113166103A - Egfr抑制剂及其应用 - Google Patents

Egfr抑制剂及其应用 Download PDF

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CN113166103A
CN113166103A CN202080006242.5A CN202080006242A CN113166103A CN 113166103 A CN113166103 A CN 113166103A CN 202080006242 A CN202080006242 A CN 202080006242A CN 113166103 A CN113166103 A CN 113166103A
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compound
reaction
amino
group
radical
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CN113166103B (zh
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刘磊
谷晓辉
刘扬
诸舜伟
薛黎婷
于晓虹
张国宝
唐任宏
任晋生
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Jiangsu Simcere Pharmaceutical 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

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  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
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Abstract

本发明涉及作为第四代(T790M/C797S突变)EGFR激酶抑制剂及其医药用途，具体公开了式(I)所示化合物或其药学上可接受的盐。本发明化合物在EGFR Del19/T790M/C797S和L858R/T790M/C797S异常突变引起的疾病上有着较好的疗效。
Figure DDA0003068611530000011

Description

PCT国内申请，说明书已公开。

Claims (37)

  1. PCT国内申请，权利要求书已公开。
CN202080006242.5A 2019-04-26 2020-04-24 Egfr抑制剂及其应用 Active CN113166103B (zh)

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CN2019103459638 2019-04-26
CN201910345963 2019-04-26
CN201910810507 2019-08-29
CN2019108105076 2019-08-29
PCT/CN2020/086871 WO2020216371A1 (zh) 2019-04-26 2020-04-24 Egfr抑制剂及其应用

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Cited By (2)

* 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
CN115536699A (zh) * 2022-12-01 2022-12-30 北京鑫开元医药科技有限公司 一种新型EGFR-TKIs、制备方法、药物组合物及其应用

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WO2021098883A1 (zh) * 2019-11-21 2021-05-27 浙江同源康医药股份有限公司 用作egfr激酶抑制剂的化合物及其应用
CN114728932A (zh) * 2019-11-29 2022-07-08 江苏先声药业有限公司 作为egfr激酶抑制剂的多芳基化合物
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
WO2021244502A1 (zh) * 2020-06-03 2021-12-09 江苏先声药业有限公司 多芳基化合物及应用
CN115697996A (zh) * 2020-06-08 2023-02-03 南京红云生物科技有限公司 烯基嘧啶类化合物、其制备方法与应用
WO2022100688A1 (zh) * 2020-11-13 2022-05-19 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
WO2022171123A1 (en) * 2021-02-10 2022-08-18 Beigene, Ltd. Egfr degraders and methods of use
US20240228458A1 (en) * 2021-04-01 2024-07-11 Therapex Co., Ltd. Pyrimidine derivative having protein kinase inhibitory activity, and therapeutic pharmaceutical composition comprising same
WO2023020600A1 (zh) * 2021-08-19 2023-02-23 贝达药业股份有限公司 Egfr抑制剂的盐、晶型及其组合物和应用
WO2023061434A1 (zh) * 2021-10-14 2023-04-20 齐鲁制药有限公司 一种三环化合物的用途
WO2023061433A1 (zh) * 2021-10-14 2023-04-20 齐鲁制药有限公司 一种egfr抑制剂的多晶型
CN116063307A (zh) * 2021-10-29 2023-05-05 中国药科大学 Shp2与cdk4/6双靶点抑制化合物合成及其制备方法与应用
WO2023138607A1 (en) * 2022-01-18 2023-07-27 Beigene , Ltd. Degradation of (egfr) by conjugation of egfr inhibitors with e3 ligase ligand and methods of use
CN115073364B (zh) * 2022-06-20 2024-04-05 上海毕得医药科技股份有限公司 一种6-硝基吡啶-3-醇的制备方法
WO2024046405A1 (zh) * 2022-09-01 2024-03-07 齐鲁制药有限公司 一种egfr激酶抑制剂的用途
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof

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WO2012051587A1 (en) * 2010-10-14 2012-04-19 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in egfr-driven cancers
WO2013169401A1 (en) * 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CN106699810A (zh) * 2015-11-17 2017-05-24 清华大学 一种含氮杂环化合物及其制备方法与在抑制激酶活性中的应用
WO2017086829A1 (ru) * 2015-11-19 2017-05-26 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") Дихлорацетаты замещенных n4-[2-(диметилфосфиноил) фенил]-n2-(2-метокси-4-пиперидин-1-илфенил)-5-хлорпиримидин-2,4-диаминов в качестве модуляторов alk и egfr, предназначенных для лечения рака
WO2017086832A1 (ru) * 2015-11-19 2017-05-26 Акционерное Общество "Р-Фарм" (Ао "Р-Фарм") Замещенные n2-(4-амино-2-метокси-фенил)- n4-[2-(диметилфосфиноил)-фенил]- 5-хлор-пиримидин-2,4-диамины в качестве модуляторов alk и egfr, предназначенные для лечения рака
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

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* Cited by examiner, † Cited by third party
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WO2012051587A1 (en) * 2010-10-14 2012-04-19 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in egfr-driven cancers
WO2013169401A1 (en) * 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CN106699810A (zh) * 2015-11-17 2017-05-24 清华大学 一种含氮杂环化合物及其制备方法与在抑制激酶活性中的应用
WO2017086829A1 (ru) * 2015-11-19 2017-05-26 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") Дихлорацетаты замещенных n4-[2-(диметилфосфиноил) фенил]-n2-(2-метокси-4-пиперидин-1-илфенил)-5-хлорпиримидин-2,4-диаминов в качестве модуляторов alk и egfr, предназначенных для лечения рака
WO2017086832A1 (ru) * 2015-11-19 2017-05-26 Акционерное Общество "Р-Фарм" (Ао "Р-Фарм") Замещенные n2-(4-амино-2-метокси-фенил)- n4-[2-(диметилфосфиноил)-фенил]- 5-хлор-пиримидин-2,4-диамины в качестве модуляторов alk и egfr, предназначенные для лечения рака
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)

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Cited By (2)

* 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
CN115536699A (zh) * 2022-12-01 2022-12-30 北京鑫开元医药科技有限公司 一种新型EGFR-TKIs、制备方法、药物组合物及其应用

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