CN113966331A - 含脲结构的三芳环化合物及其应用 - Google Patents

含脲结构的三芳环化合物及其应用 Download PDF

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Publication number
CN113966331A
CN113966331A CN202180002962.9A CN202180002962A CN113966331A CN 113966331 A CN113966331 A CN 113966331A CN 202180002962 A CN202180002962 A CN 202180002962A CN 113966331 A CN113966331 A CN 113966331A
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CN113966331B (zh
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蔡倩
张章
吴开富
肖国荣
何蕊
黄晶
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Jinan University
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Jinan University
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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

本发明提供了一种具有式(I)所示结构的含脲结构的三芳环化合物或其药学上可接受的盐或其立体异构体或其前药分子或其代谢产物或其溶剂化物，该类化合物可以有效地抑制激酶，尤其是FLT3和RET激酶，进而调节下游的多条通路的激活，可以用于制备防治RET激酶、FLT3激酶和/或Kit激酶相关的多种疾病的药物，比如白血病、肿瘤。

Description

PCT国内申请，说明书已公开。

Claims (24)

  1. PCT国内申请，权利要求书已公开。
CN202180002962.9A 2020-03-11 2021-03-05 含脲结构的三芳环化合物及其应用 Active CN113966331B (zh)

Applications Claiming Priority (3)

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CN2020101661011 2020-03-11
CN202010166101 2020-03-11
PCT/CN2021/079354 WO2021180008A1 (zh) 2020-03-11 2021-03-05 含脲结构的三芳环化合物及其应用

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CN113966331A true CN113966331A (zh) 2022-01-21
CN113966331B CN113966331B (zh) 2024-04-12

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023129667A1 (en) 2021-12-30 2023-07-06 Biomea Fusion, Inc. Pyrazine compounds as inhibitors of flt3

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1544420A (zh) * 1997-12-22 2004-11-10 用取代杂环脲抑制raf激酶
CN101448843A (zh) * 2006-03-17 2009-06-03 埃姆比特生物科学公司 用于疾病治疗的咪唑并噻唑化合物
CN101835472A (zh) * 2007-11-08 2010-09-15 埃姆比特生物科学公司 N-(5-叔丁基-异噁唑-3-基)-N′-{4-[7-(2-吗啉-4-基-乙氧基)咪唑并[2,1-b][1,3]苯并噻唑-2-基]苯基}脲治疗增殖性疾病的给药方法
US20120225880A1 (en) * 2011-03-04 2012-09-06 National Health Research Institutes Pyrazole compounds and thiazole compounds as protein kinases inhibitors
CN107459521A (zh) * 2016-06-03 2017-12-12 合肥中科普瑞昇生物医药科技有限公司 Flt3激酶的新型抑制剂及其用途
CN110437220A (zh) * 2018-07-13 2019-11-12 暨南大学 三氮唑类化合物及其应用

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1544420A (zh) * 1997-12-22 2004-11-10 用取代杂环脲抑制raf激酶
CN101448843A (zh) * 2006-03-17 2009-06-03 埃姆比特生物科学公司 用于疾病治疗的咪唑并噻唑化合物
CN101835472A (zh) * 2007-11-08 2010-09-15 埃姆比特生物科学公司 N-(5-叔丁基-异噁唑-3-基)-N′-{4-[7-(2-吗啉-4-基-乙氧基)咪唑并[2,1-b][1,3]苯并噻唑-2-基]苯基}脲治疗增殖性疾病的给药方法
US20120225880A1 (en) * 2011-03-04 2012-09-06 National Health Research Institutes Pyrazole compounds and thiazole compounds as protein kinases inhibitors
CN107459521A (zh) * 2016-06-03 2017-12-12 合肥中科普瑞昇生物医药科技有限公司 Flt3激酶的新型抑制剂及其用途
CN110437220A (zh) * 2018-07-13 2019-11-12 暨南大学 三氮唑类化合物及其应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KAIFU WU ET AL.: "Discovery of 3,5-diaryl-1H-pyrazol-based ureas as potent RET inhibitors", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》, vol. 251, pages 115237 *

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WO2021180008A1 (zh) 2021-09-16

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