CN114650991A - 桥环并醛基吡啶衍生物及其应用 - Google Patents

桥环并醛基吡啶衍生物及其应用 Download PDF

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CN114650991A
CN114650991A CN202080075456.8A CN202080075456A CN114650991A CN 114650991 A CN114650991 A CN 114650991A CN 202080075456 A CN202080075456 A CN 202080075456A CN 114650991 A CN114650991 A CN 114650991A
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CN114650991B (zh
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王�琦
段公平
华威
张兴民
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Broadenbio Co Ltd
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    • C07D471/00—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
    • 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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    • A—HUMAN NECESSITIES
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • C07D471/12—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 three hetero rings
    • C07D471/18—Bridged systems
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • C07D471/00—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
    • 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
    • C07D471/08—Bridged systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

提供一种式(I)化合物或其药学上可接受的盐、溶剂化物、活性代谢物、多晶型物、同位素标记物、异构体或前药,及其应用。上述化合物，对FGFR4激酶活性以及FGFR4高表达的Hep 3B细胞增殖活性均具有很强的抑制作用。

Description

PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN202080075456.8A 2019-11-01 2020-10-21 桥环并醛基吡啶衍生物及其应用 Active CN114650991B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019110618018 2019-11-01
CN201911061801.8A CN112759593A (zh) 2019-11-01 2019-11-01 桥环并醛基吡啶衍生物及其应用
PCT/CN2020/122569 WO2021083011A1 (zh) 2019-11-01 2020-10-21 桥环并醛基吡啶衍生物及其应用

Publications (2)

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CN114650991A true CN114650991A (zh) 2022-06-21
CN114650991B CN114650991B (zh) 2024-10-18

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105392788A (zh) * 2013-05-13 2016-03-09 葛兰素史密斯克莱有限责任公司 用作沉默调节蛋白调节剂的取代的桥连脲类似物
CN107304210A (zh) * 2016-04-25 2017-10-31 成都融科博海科技有限公司 一种选择性fgfr4激酶抑制剂
CN109745321A (zh) * 2017-11-08 2019-05-14 上海翰森生物医药科技有限公司 包含fgfr4抑制剂的药物组合物
CN109922804A (zh) * 2016-11-02 2019-06-21 诺华股份有限公司 Fgfr4抑制剂和胆汁酸螯合剂的组合

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105392788A (zh) * 2013-05-13 2016-03-09 葛兰素史密斯克莱有限责任公司 用作沉默调节蛋白调节剂的取代的桥连脲类似物
CN107207496A (zh) * 2013-05-13 2017-09-26 葛兰素史密斯克莱有限责任公司 作为沉默调节蛋白调节剂的取代的桥环脲类似物
CN107304210A (zh) * 2016-04-25 2017-10-31 成都融科博海科技有限公司 一种选择性fgfr4激酶抑制剂
CN109922804A (zh) * 2016-11-02 2019-06-21 诺华股份有限公司 Fgfr4抑制剂和胆汁酸螯合剂的组合
CN109745321A (zh) * 2017-11-08 2019-05-14 上海翰森生物医药科技有限公司 包含fgfr4抑制剂的药物组合物

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AU2020375960B2 (en) 2023-07-20
EP4053126A4 (en) 2022-12-14
CA3156615A1 (en) 2021-05-06
EP4053126A1 (en) 2022-09-07
WO2021083011A1 (zh) 2021-05-06
JP7349572B2 (ja) 2023-09-22
US20230012600A1 (en) 2023-01-19
JP2023501288A (ja) 2023-01-18
AU2020375960A1 (en) 2022-06-09
KR20220088909A (ko) 2022-06-28
CN112759593A (zh) 2021-05-07

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