CN115175902A - 一类用作激酶抑制剂的化合物及其应用 - Google Patents
一类用作激酶抑制剂的化合物及其应用 Download PDFInfo
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- CN115175902A CN115175902A CN202180013936.6A CN202180013936A CN115175902A CN 115175902 A CN115175902 A CN 115175902A CN 202180013936 A CN202180013936 A CN 202180013936A CN 115175902 A CN115175902 A CN 115175902A
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- cycloalkyl
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- 125000000217 alkyl group Chemical group 0.000 claims description 76
- 229910052757 nitrogen Inorganic materials 0.000 claims description 68
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- 125000001188 haloalkyl group Chemical group 0.000 claims description 28
- 125000003118 aryl group Chemical group 0.000 claims description 26
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- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
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- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical class [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 35
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- LFZAGIJXANFPFN-UHFFFAOYSA-N N-[3-[4-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)piperidin-1-yl]-1-thiophen-2-ylpropyl]acetamide Chemical compound C(C)(C)C1=NN=C(N1C1CCN(CC1)CCC(C=1SC=CC=1)NC(C)=O)C LFZAGIJXANFPFN-UHFFFAOYSA-N 0.000 description 32
- 239000007864 aqueous solution Substances 0.000 description 32
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 30
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- VSCWAEJMTAWNJL-UHFFFAOYSA-K aluminium trichloride Chemical compound Cl[Al](Cl)Cl VSCWAEJMTAWNJL-UHFFFAOYSA-K 0.000 description 11
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- A61P35/00—Antineoplastic agents
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- 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
- C07D401/14—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 three or more hetero rings
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- C07—ORGANIC CHEMISTRY
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- 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
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- C07D—HETEROCYCLIC COMPOUNDS
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- C07D403/14—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 three or more hetero rings
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- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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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
- C07D471/04—Ortho-condensed systems
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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Abstract
式Ⅰ所示的激酶抑制剂的化合物或其药学上可以接受的盐、溶剂化物或前药。该化合物对EGFR和Her2外显子20插入突变、EGFR外显子19缺失和外显子21的L858R点突变具有良好的抑制活性。
Description
PCT国内申请,说明书已公开。
Claims (14)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
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CN2020101757917 | 2020-03-13 | ||
PCT/CN2021/080892 WO2021180238A1 (zh) | 2020-03-13 | 2021-03-15 | 一类用作激酶抑制剂的化合物及其应用 |
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CN116283914A (zh) * | 2021-12-01 | 2023-06-23 | 上海艾力斯医药科技股份有限公司 | 一类嘧啶类化合物、其制备方法及应用 |
KR20240110861A (ko) | 2022-04-01 | 2024-07-16 | 티와이케이 메디슨즈, 인코포레이티드 | 키나아제 억제제로 사용되는 화합물 및 이의 용도 |
CN115925618A (zh) * | 2023-01-06 | 2023-04-07 | 河南省科学院化学研究所有限公司 | 一种2-(2,2,2-三氟乙氧基)-6-氯-3-氨基吡啶的合成方法 |
Citations (6)
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CN104761544A (zh) * | 2014-01-03 | 2015-07-08 | 南京波尔泰药业科技有限公司 | Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂 |
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 |
CN106559991A (zh) * | 2014-06-19 | 2017-04-05 | 阿里亚德医药股份有限公司 | 用于激酶抑制的杂芳基化合物 |
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 |
CN112292378A (zh) * | 2019-05-22 | 2021-01-29 | 上海翰森生物医药科技有限公司 | 含吲哚类衍生物抑制剂、其制备方法和应用 |
CN114174269A (zh) * | 2019-07-26 | 2022-03-11 | 南京明德新药研发有限公司 | 作用于egfr和erbb2的嘧啶类化合物 |
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EP3205650B1 (en) * | 2014-10-11 | 2021-08-04 | Shanghai Hansoh Biomedical Co., Ltd. | Egfr inhibitor, and preparation and application thereof |
CN108069939B (zh) * | 2016-11-16 | 2020-03-10 | 中国科学院上海药物研究所 | 含有共轭联烯酰胺结构的化合物、其制备方法、药物组合物和用途 |
CN108191861B (zh) * | 2018-03-01 | 2020-10-02 | 天津大学 | N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-反式-2,4-戊二烯酰胺 |
CN110790749B (zh) * | 2018-08-03 | 2023-07-14 | 北京普祺医药科技股份有限公司 | 一种含氮杂环化合物、药物组合物以及其用途 |
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2021
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- 2021-03-15 EP EP21768468.7A patent/EP4119553A4/en active Pending
- 2021-03-15 CN CN202180013936.6A patent/CN115175902B/zh active Active
- 2021-03-15 US US17/911,138 patent/US20230150975A1/en active Pending
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
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CN104761544A (zh) * | 2014-01-03 | 2015-07-08 | 南京波尔泰药业科技有限公司 | Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂 |
CN106559991A (zh) * | 2014-06-19 | 2017-04-05 | 阿里亚德医药股份有限公司 | 用于激酶抑制的杂芳基化合物 |
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 |
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 |
CN112292378A (zh) * | 2019-05-22 | 2021-01-29 | 上海翰森生物医药科技有限公司 | 含吲哚类衍生物抑制剂、其制备方法和应用 |
CN114174269A (zh) * | 2019-07-26 | 2022-03-11 | 南京明德新药研发有限公司 | 作用于egfr和erbb2的嘧啶类化合物 |
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US20230150975A1 (en) | 2023-05-18 |
WO2021180238A1 (zh) | 2021-09-16 |
EP4119553A1 (en) | 2023-01-18 |
CN115175902B (zh) | 2024-07-26 |
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