AU2017359819B2 - FGFR4 inhibitor and preparation method and use thereof - Google Patents

FGFR4 inhibitor and preparation method and use thereof Download PDF

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Publication number
AU2017359819B2
AU2017359819B2 AU2017359819A AU2017359819A AU2017359819B2 AU 2017359819 B2 AU2017359819 B2 AU 2017359819B2 AU 2017359819 A AU2017359819 A AU 2017359819A AU 2017359819 A AU2017359819 A AU 2017359819A AU 2017359819 B2 AU2017359819 B2 AU 2017359819B2
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group
mmol
compound
pharmaceutically acceptable
acceptable salt
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AU2017359819A1 (en
Inventor
Shuhui Chen
Xiaoxin Chen
Zhengxia CHEN
Meibi DAI
Guoping Hu
Jian Li
Xing Liu
Zhuowei LIU
Chaofeng LONG
Yikai WANG
Yang Zhang
Haixia Zhao
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Guangdong Zhongsheng Pharmaceutical Co Ltd
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Guangdong Zhongsheng Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/53Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2017359819A 2016-11-17 2017-11-17 FGFR4 inhibitor and preparation method and use thereof Active AU2017359819B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201611012431.5 2016-11-17
CN201611012431 2016-11-17
PCT/CN2017/111634 WO2018090973A1 (zh) 2016-11-17 2017-11-17 Fgfr4抑制剂及其制备方法和应用

Publications (2)

Publication Number Publication Date
AU2017359819A1 AU2017359819A1 (en) 2019-06-20
AU2017359819B2 true AU2017359819B2 (en) 2020-05-28

Family

ID=62145242

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AU2017359819A Active AU2017359819B2 (en) 2016-11-17 2017-11-17 FGFR4 inhibitor and preparation method and use thereof

Country Status (12)

Country Link
US (1) US11008292B2 (cg-RX-API-DMAC7.html)
EP (1) EP3543227B1 (cg-RX-API-DMAC7.html)
JP (1) JP7063899B2 (cg-RX-API-DMAC7.html)
KR (1) KR102249632B1 (cg-RX-API-DMAC7.html)
CN (1) CN109952290B (cg-RX-API-DMAC7.html)
AU (1) AU2017359819B2 (cg-RX-API-DMAC7.html)
CA (1) CA3043948C (cg-RX-API-DMAC7.html)
IL (1) IL266659B (cg-RX-API-DMAC7.html)
MX (1) MX389403B (cg-RX-API-DMAC7.html)
NZ (1) NZ754218A (cg-RX-API-DMAC7.html)
WO (1) WO2018090973A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201903845B (cg-RX-API-DMAC7.html)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL274274B2 (en) * 2017-11-01 2023-11-01 Guangdong Zhongsheng Pharmaceutical Co Ltd Salt form and crystal form of compound as fgfr4 inhibitor and preparation method thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016164703A1 (en) * 2015-04-09 2016-10-13 Eisai R & D Management Co., Ltd. Fgfr4 inhibitors

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101003514A (zh) 2006-01-20 2007-07-25 上海艾力斯医药科技有限公司 喹唑啉衍生物、其制备方法及用途
CN102731485B (zh) 2011-04-02 2016-06-15 齐鲁制药有限公司 4-(取代苯氨基)喹唑啉衍生物及其制备方法、药物组合物和用途
CN109627239B (zh) 2012-07-11 2021-10-12 缆图药品公司 成纤维细胞生长因子受体的抑制剂
WO2014139145A1 (en) * 2013-03-15 2014-09-18 Hutchison Medipharma Limited Novel pyrimidine and pyridine compounds and usage thereof
PH12016500676B1 (en) * 2013-10-18 2022-07-20 Eisai R&D Man Co Ltd Pyrimidine fgfr4 inhibitors
WO2016115412A1 (en) 2015-01-18 2016-07-21 Newave Pharmaceutical Llc Dual-warhead covalent inhibitors of fgfr-4
AU2016248056B2 (en) 2015-04-14 2020-07-23 Eisai R&D Management Co., Ltd. Crystalline FGFR4 inhibitor compound and uses thereof
IL274274B2 (en) * 2017-11-01 2023-11-01 Guangdong Zhongsheng Pharmaceutical Co Ltd Salt form and crystal form of compound as fgfr4 inhibitor and preparation method thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016164703A1 (en) * 2015-04-09 2016-10-13 Eisai R & D Management Co., Ltd. Fgfr4 inhibitors

Also Published As

Publication number Publication date
US20200062716A1 (en) 2020-02-27
WO2018090973A1 (zh) 2018-05-24
IL266659B (en) 2022-01-01
JP2019537613A (ja) 2019-12-26
JP7063899B2 (ja) 2022-05-09
CN109952290A (zh) 2019-06-28
CA3043948C (en) 2021-08-31
MX389403B (es) 2025-03-20
EP3543227B1 (en) 2020-12-30
NZ754218A (en) 2021-07-30
EP3543227A1 (en) 2019-09-25
CA3043948A1 (en) 2018-05-24
AU2017359819A1 (en) 2019-06-20
IL266659A (en) 2019-07-31
US11008292B2 (en) 2021-05-18
EP3543227A4 (en) 2019-10-30
KR20190077085A (ko) 2019-07-02
MX2019005723A (es) 2019-10-21
KR102249632B1 (ko) 2021-05-10
CN109952290B (zh) 2022-05-03
ZA201903845B (en) 2020-12-23

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