AU2017327954B2 - Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof - Google Patents

Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof Download PDF

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AU2017327954B2
AU2017327954B2 AU2017327954A AU2017327954A AU2017327954B2 AU 2017327954 B2 AU2017327954 B2 AU 2017327954B2 AU 2017327954 A AU2017327954 A AU 2017327954A AU 2017327954 A AU2017327954 A AU 2017327954A AU 2017327954 B2 AU2017327954 B2 AU 2017327954B2
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alkyl
cancer
ethynyl
mmol
pyrazole
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AU2017327954A1 (en
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Xiangyang Chen
Yingxiang GAO
Norman Xianglong Kong
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Beijing Innocare Pharma Tech Co Ltd
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Beijing Innocare Pharma Tech Co Ltd
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    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic 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
    • A61K31/435—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D405/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2017327954A 2016-09-19 2017-01-25 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof Active AU2017327954B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201610833890.3A CN107840842A (zh) 2016-09-19 2016-09-19 炔代杂环化合物、其制备方法及其在医药学上的应用
CN201610833890.3 2016-09-19
PCT/CN2017/072570 WO2018049781A1 (zh) 2016-09-19 2017-01-25 炔代杂环化合物、其制备方法及其在医药学上的应用

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AU2017327954A1 AU2017327954A1 (en) 2019-05-02
AU2017327954B2 true AU2017327954B2 (en) 2022-02-03

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US (3) US10710981B2 (enExample)
EP (1) EP3517535B1 (enExample)
JP (1) JP6906811B2 (enExample)
KR (1) KR102783517B1 (enExample)
CN (2) CN107840842A (enExample)
AU (1) AU2017327954B2 (enExample)
CA (1) CA3036594C (enExample)
ES (1) ES2925212T3 (enExample)
MX (1) MX390747B (enExample)
RU (1) RU2729069C1 (enExample)
SG (1) SG10202102822RA (enExample)
WO (1) WO2018049781A1 (enExample)

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EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
AU2020412067A1 (en) * 2019-12-26 2022-08-11 Beijing Innocare Pharma Tech Co., Ltd. Crystalline forms of (S) -1- (1-acryloylpyrrolidin-3-yl) -3- ( (3, 5-dimethoxyphenyl) ethynyl) -5- (methylamino) -1H-pyrazole-4-carboxamide
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN116057045A (zh) * 2020-06-05 2023-05-02 金耐特生物制药公司 成纤维细胞生长因子受体激酶抑制剂
CN116096707A (zh) * 2020-06-05 2023-05-09 金耐特生物制药公司 成纤维细胞生长因子受体激酶的抑制剂
WO2022042613A1 (zh) * 2020-08-27 2022-03-03 上海和誉生物医药科技有限公司 一种1h-吡唑-4-酰胺衍生物，其制备方法和应用
CA3204407A1 (en) * 2021-01-12 2022-07-21 Yucheng PANG Process for preparing (s)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl) ethynyl)-5-(methylamino)-1h-pyrazole-4-carboxamide
CN115433190B (zh) * 2021-06-02 2024-09-20 药雅科技(上海)有限公司 不可逆杂环化合物fgfr抑制剂的制备方法和用途
CN114853739B (zh) * 2021-02-03 2023-09-22 药雅科技(上海)有限公司 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途
CN115043832B (zh) * 2021-03-08 2023-08-22 药雅科技(上海)有限公司 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途
JP2024539723A (ja) * 2021-11-03 2024-10-29 ベイジン・イノケア・ファーマ・テク・カンパニー・リミテッド （ｓ）－１－（１－アクリロイルピロリジン－３－イル）－３－（（３，５－ジメトキシフェニル）エチニル）－５－（メチルアミノ）－１ｈ－ピラゾール－４－カルボキサミドを含む非晶質固体分散体
CA3238193A1 (en) * 2021-11-16 2023-05-25 Jisong Cui Method for treating head and neck cancer
KR20240119095A (ko) * 2021-12-08 2024-08-06 킨네이트 바이오파마 인크. Fgfr 저해제의 고체 상태 형태
WO2023107870A1 (en) * 2021-12-08 2023-06-15 Kinnate Biopharma Inc. Inhibitors of fibroblast growth factor receptor kinases
EP4444713A4 (en) * 2021-12-08 2025-08-06 Kinnate Biopharma Inc CANCER TREATMENT WITH AN FGFR KINASE INHIBITOR

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WO2013014039A1 (en) * 2011-07-28 2013-01-31 Nerviano Medical Sciences S.R.L. Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors
EP3023100A1 (en) * 2013-07-18 2016-05-25 Taiho Pharmaceutical Co., Ltd. Antitumor drug for intermittent administration of fgfr inhibitor

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CN109843873B (zh) 2022-06-17
MX2019003143A (es) 2019-06-17
WO2018049781A1 (zh) 2018-03-22
EP3517535A1 (en) 2019-07-31
JP2019529444A (ja) 2019-10-17
ES2925212T3 (es) 2022-10-14
US20190210997A1 (en) 2019-07-11
EP3517535B1 (en) 2022-06-29
CN109843873A (zh) 2019-06-04
US20200339541A1 (en) 2020-10-29
JP6906811B2 (ja) 2021-07-21
CA3036594C (en) 2024-02-13
AU2017327954A1 (en) 2019-05-02
EP3517535A4 (en) 2020-02-26
US11059805B2 (en) 2021-07-13
US10710981B2 (en) 2020-07-14
RU2729069C1 (ru) 2020-08-04
MX390747B (es) 2025-03-21
KR20190052113A (ko) 2019-05-15
US11572353B2 (en) 2023-02-07
US20210332027A1 (en) 2021-10-28
CN107840842A (zh) 2018-03-27
SG10202102822RA (en) 2021-05-28
CA3036594A1 (en) 2018-03-22
KR102783517B1 (ko) 2025-03-19

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