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 PDFInfo
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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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- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
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- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
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- MSWTVSDFEYSRMQ-UHFFFAOYSA-N tert-butyl n-methyl-n-(2-oxoethyl)carbamate Chemical compound O=CCN(C)C(=O)OC(C)(C)C MSWTVSDFEYSRMQ-UHFFFAOYSA-N 0.000 description 1
- MHYGQXWCZAYSLJ-UHFFFAOYSA-N tert-butyl-chloro-diphenylsilane Chemical compound C=1C=CC=CC=1[Si](Cl)(C(C)(C)C)C1=CC=CC=C1 MHYGQXWCZAYSLJ-UHFFFAOYSA-N 0.000 description 1
- BCNZYOJHNLTNEZ-UHFFFAOYSA-N tert-butyldimethylsilyl chloride Chemical compound CC(C)(C)[Si](C)(C)Cl BCNZYOJHNLTNEZ-UHFFFAOYSA-N 0.000 description 1
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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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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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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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- 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
- A61K31/435—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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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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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)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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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)
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)
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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