CN115515949A - 新型氨基嘧啶类egfr抑制剂 - Google Patents

新型氨基嘧啶类egfr抑制剂 Download PDF

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CN115515949A
CN115515949A CN202180023325.XA CN202180023325A CN115515949A CN 115515949 A CN115515949 A CN 115515949A CN 202180023325 A CN202180023325 A CN 202180023325A CN 115515949 A CN115515949 A CN 115515949A
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cycloalkyl
radical
alkyl
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邓伟
郑善松
塞巴斯蒂安·安德烈·坎波斯
杨莹莹
田振华
郑庆梅
吴国胜
赵志威
李磊磊
付健民
赵树雍
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Qilu Pharmaceutical Co Ltd
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Qilu Pharmaceutical Co Ltd
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    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
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    • C07D403/10—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 linked by a carbon chain containing aromatic rings
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    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
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    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65615—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing a spiro condensed ring system of the formula where at least one of the atoms X or Y is a hetero atom, e.g. S
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Abstract

本发明提供了作为第四代EGFR(T790M/C797S突变)选择性抑制剂的新型氨基嘧啶类化合物，含有所述化合物的药物组合物、制备所述化合物的有用中间体以及利用本发明化合物治疗细胞增殖性疾病，例如癌症的方法。
Figure DDA0003855135040000011

Description

PCT国内申请，说明书已公开。

Claims (58)

  1. PCT国内申请，权利要求书已公开。
CN202180023325.XA 2020-03-23 2021-03-19 新型氨基嘧啶类egfr抑制剂 Pending CN115515949A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2020102086252 2020-03-23
CN202010208625 2020-03-23
CN202010984379X 2020-09-18
CN202010984379.XA CN112538072B (zh) 2019-09-21 2020-09-18 氨基嘧啶类egfr抑制剂
PCT/CN2021/081868 WO2021190417A1 (zh) 2020-03-23 2021-03-19 新型氨基嘧啶类egfr抑制剂

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CN115515949A true CN115515949A (zh) 2022-12-23

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US (1) US20230219986A1 (zh)
EP (1) EP4129996A4 (zh)
JP (1) JP2023518609A (zh)
CN (1) CN115515949A (zh)
WO (1) WO2021190417A1 (zh)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022199589A1 (zh) * 2021-03-23 2022-09-29 南京明德新药研发有限公司 嘧啶衍生物
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
WO2023106881A1 (ko) * 2021-12-09 2023-06-15 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규 헤테로 고리 치환 피리미딘 유도체 및 그를 포함하는 약학 조성물
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

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CN103501612B (zh) * 2011-05-04 2017-03-29 阿里亚德医药股份有限公司 抑制表皮生长因子受体导致的癌症中细胞增殖的化合物
WO2013029338A1 (en) * 2011-09-01 2013-03-07 Glaxo Group Limited Novel compounds
RU2606951C1 (ru) * 2015-11-19 2017-01-10 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") Дихлорацетаты замещенных N4-[2-(диметилфосфорил)фенил]-N2-(2-метокси-4-пиперидин-1-илфенил)-5-хлорпиримидин-2,4-диаминов в качестве модуляторов ALK и EGFR, предназначенных для лечения рака
RU2607371C1 (ru) * 2015-11-19 2017-01-10 Закрытое акционерное общество "Р-Фарм"(ЗАО "Р-Фарм") Замещенные N2-(4-амино-2-метоксифенил)-N4-[2-(диметилфосфорил)-фенил]-5-хлор-пиримидин-2,4-диамины в качестве модуляторов ALK и EGFR, предназначенные для лечения рака
US10647665B2 (en) * 2016-06-22 2020-05-12 Fudan University Biaryl urea derivative or salt thereof and preparation process and use for the same
WO2018108064A1 (zh) * 2016-12-13 2018-06-21 南京明德新药研发股份有限公司 作为第四代egfr激酶抑制剂的螺环芳基磷氧化合物
US20220259235A1 (en) * 2019-07-26 2022-08-18 Betta Pharmaceuticals Co., Ltd EGFR Inhibitor, Composition, and Preparation Method Therefor
CN112538072B (zh) * 2019-09-21 2024-02-06 齐鲁制药有限公司 氨基嘧啶类egfr抑制剂
KR102168179B1 (ko) * 2019-10-31 2020-10-20 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규한 헤테로 고리 치환 피리미딘 유도체 및 그를 포함하는 약제학적 조성물
CA3167899A1 (en) * 2020-02-14 2021-08-19 Xiangyong LIU Quinolyl phosphine oxide compound, and composition and application thereof
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
WO2022146027A1 (ko) * 2020-12-29 2022-07-07 주식회사 비투에스바이오 헤테로아릴 유도체 화합물 및 이의 용도

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US20230219986A1 (en) 2023-07-13
EP4129996A4 (en) 2023-07-12

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