JP7063899B2 - Ｆｇｆｒ４阻害剤、その製造方法及び使用 - Google Patents

Ｆｇｆｒ４阻害剤、その製造方法及び使用 Download PDF

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JP7063899B2
JP7063899B2 JP2019526465A JP2019526465A JP7063899B2 JP 7063899 B2 JP7063899 B2 JP 7063899B2 JP 2019526465 A JP2019526465 A JP 2019526465A JP 2019526465 A JP2019526465 A JP 2019526465A JP 7063899 B2 JP7063899 B2 JP 7063899B2
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tautomer
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JP2019537613A (ja
JP2019537613A5 (cg-RX-API-DMAC7.html
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ヂェンシャ チェン
チャオフェン ロン
ヤン ヂャン
シャオシン チェン
イーカイ ワン
メイビ ダイ
ヂュオウェイ リュウ
ハイシャ ヂャオ
シン リュウ
グオピン フー
ジアン リ
シューフイ チェン
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グアンドン ジョンシェン ファーマシューティカル カンパニー リミテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • 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
    • A61K31/435—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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/24—Heterocyclic 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
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/53—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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)
JP2019526465A 2016-11-17 2017-11-17 Ｆｇｆｒ４阻害剤、その製造方法及び使用 Active JP7063899B2 (ja)

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 (3)

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JP2019537613A JP2019537613A (ja) 2019-12-26
JP2019537613A5 JP2019537613A5 (cg-RX-API-DMAC7.html) 2020-10-15
JP7063899B2 true JP7063899B2 (ja) 2022-05-09

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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 (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009525956A (ja) 2006-01-20 2009-07-16 上▲海▼艾力斯医▲藥▼科技有限公司 キナゾリン誘導体、その調製法および使用法
WO2012136099A1 (zh) 2011-04-02 2012-10-11 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
JP2015523383A (ja) 2012-07-11 2015-08-13 ブループリント メディシンズ コーポレイション 線維芽細胞成長因子受容体の阻害剤
WO2016115412A1 (en) 2015-01-18 2016-07-21 Newave Pharmaceutical Llc Dual-warhead covalent inhibitors of fgfr-4
WO2016164703A1 (en) 2015-04-09 2016-10-13 Eisai R & D Management Co., Ltd. Fgfr4 inhibitors
WO2016168331A1 (en) 2015-04-14 2016-10-20 Eisai R&D Management Co., Ltd. Crystalline fgfr4 inhibitor compound and uses thereof
JP2016535000A (ja) 2013-10-18 2016-11-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピリミジンｆｇｆｒ４阻害剤

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014139145A1 (en) * 2013-03-15 2014-09-18 Hutchison Medipharma Limited Novel pyrimidine and pyridine compounds and usage 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 (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009525956A (ja) 2006-01-20 2009-07-16 上▲海▼艾力斯医▲藥▼科技有限公司 キナゾリン誘導体、その調製法および使用法
WO2012136099A1 (zh) 2011-04-02 2012-10-11 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
JP2015523383A (ja) 2012-07-11 2015-08-13 ブループリント メディシンズ コーポレイション 線維芽細胞成長因子受容体の阻害剤
JP2016535000A (ja) 2013-10-18 2016-11-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピリミジンｆｇｆｒ４阻害剤
WO2016115412A1 (en) 2015-01-18 2016-07-21 Newave Pharmaceutical Llc Dual-warhead covalent inhibitors of fgfr-4
WO2016164703A1 (en) 2015-04-09 2016-10-13 Eisai R & D Management Co., Ltd. Fgfr4 inhibitors
WO2016168331A1 (en) 2015-04-14 2016-10-20 Eisai R&D Management Co., Ltd. Crystalline fgfr4 inhibitor compound and uses thereof

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Publication number Publication date
US20200062716A1 (en) 2020-02-27
WO2018090973A1 (zh) 2018-05-24
IL266659B (en) 2022-01-01
JP2019537613A (ja) 2019-12-26
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
AU2017359819B2 (en) 2020-05-28
MX2019005723A (es) 2019-10-21
KR102249632B1 (ko) 2021-05-10
CN109952290B (zh) 2022-05-03
ZA201903845B (en) 2020-12-23

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