JP6667014B2 - ピリミジン誘導体、その調製方法および医療での使用 - Google Patents

ピリミジン誘導体、その調製方法および医療での使用 Download PDF

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JP6667014B2
JP6667014B2 JP2018560780A JP2018560780A JP6667014B2 JP 6667014 B2 JP6667014 B2 JP 6667014B2 JP 2018560780 A JP2018560780 A JP 2018560780A JP 2018560780 A JP2018560780 A JP 2018560780A JP 6667014 B2 JP6667014 B2 JP 6667014B2
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tert
heterocyclyl
alkyl
cycloalkyl
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JP2019519512A5 (enExample
JP2019519512A (ja
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陳磊
関東亮
白▲か▼
苟俊
趙偉峰
王中利
凌龍
馬玉涛
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Zhejiang Hisun Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/14—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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/12—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
    • 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/10—Spiro-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2018560780A 2016-05-20 2017-05-19 ピリミジン誘導体、その調製方法および医療での使用 Active JP6667014B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610341444.0 2016-05-20
CN201610341444 2016-05-20
PCT/CN2017/085135 WO2017198221A1 (zh) 2016-05-20 2017-05-19 嘧啶类衍生物、其制备方法和其在医药上的用途

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JP2019519512A JP2019519512A (ja) 2019-07-11
JP2019519512A5 JP2019519512A5 (enExample) 2020-01-16
JP6667014B2 true JP6667014B2 (ja) 2020-03-18

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US (4) US10654836B2 (enExample)
EP (1) EP3459952B1 (enExample)
JP (1) JP6667014B2 (enExample)
CN (1) CN108884097B (enExample)
CA (1) CA3024532C (enExample)
TW (1) TWI669300B (enExample)
WO (1) WO2017198221A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201602069WA (en) 2013-10-18 2016-04-28 Eisai R&D Man Co Ltd Pyrimidine fgfr4 inhibitors
SG10201810057UA (en) 2015-04-14 2018-12-28 Eisai R&D Man Co Ltd Crystalline fgfr4 inhibitor compound and uses thereof
US11357769B2 (en) 2016-05-10 2022-06-14 Eisai R&D Management Co., Ltd. Drug combinations for reducing cell viability and/or cell proliferation
CN108822048A (zh) * 2018-07-23 2018-11-16 上海昌肽生物科技有限公司 4-(4-乙基-4,7二氮杂螺环[3,3]辛基)-2-硝基苯胺的合成工艺
TWI723480B (zh) 2018-07-27 2021-04-01 大陸商北京加科思新藥研發有限公司 用作fgfr4抑制劑的稠環衍生物
CN115490670A (zh) * 2021-06-17 2022-12-20 浙江海正药业股份有限公司 Fgfr4选择性抑制剂的盐及其制备方法和用途
CN115504965A (zh) * 2021-06-23 2022-12-23 浙江海正药业股份有限公司 嘧啶类衍生物的晶型及其制备方法
CN116947825B (zh) * 2022-04-14 2025-11-28 浙江海正药业股份有限公司 Fgfr4选择性抑制剂化合物的晶型及其制备方法和用途

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0512324D0 (en) * 2005-06-16 2005-07-27 Novartis Ag Organic compounds
AR079257A1 (es) * 2009-12-07 2012-01-04 Novartis Ag Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas
CN102250065B (zh) * 2011-05-20 2015-05-13 浙江海正药业股份有限公司 取代的三嗪苯脲衍生物及其用途
AU2013227139B2 (en) * 2012-02-28 2017-02-16 Astellas Pharma Inc. Nitrogen-containing aromatic heterocyclic compound
KR20150037207A (ko) * 2013-09-30 2015-04-08 한미약품 주식회사 Fms 키나아제 저해 활성을 갖는 피리미딘 화합물
SG11201602069WA (en) * 2013-10-18 2016-04-28 Eisai R&D Man Co Ltd Pyrimidine fgfr4 inhibitors
AU2014338549B2 (en) 2013-10-25 2017-05-25 Novartis Ag Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
CN104860891B (zh) * 2014-02-25 2017-06-30 上海海雁医药科技有限公司 芳氨基嘧啶类化合物及其应用以及由其制备的药物组合物和药用组合物

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US11827625B2 (en) 2023-11-28
US20190161476A1 (en) 2019-05-30
EP3459952A4 (en) 2020-01-15
US20210221797A1 (en) 2021-07-22
TWI669300B (zh) 2019-08-21
CN108884097A (zh) 2018-11-23
WO2017198221A1 (zh) 2017-11-23
EP3459952B1 (en) 2022-01-05
US10654836B2 (en) 2020-05-19
CN108884097B (zh) 2021-05-28
TW201741303A (zh) 2017-12-01
US12358898B2 (en) 2025-07-15
CA3024532C (en) 2021-02-09
US11001572B2 (en) 2021-05-11
JP2019519512A (ja) 2019-07-11
US20240018130A1 (en) 2024-01-18
US20200207745A1 (en) 2020-07-02
EP3459952A1 (en) 2019-03-27
CA3024532A1 (en) 2017-11-23

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