CN107840842A - 炔代杂环化合物、其制备方法及其在医药学上的应用 - Google Patents

炔代杂环化合物、其制备方法及其在医药学上的应用 Download PDF

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Publication number
CN107840842A
CN107840842A CN201610833890.3A CN201610833890A CN107840842A CN 107840842 A CN107840842 A CN 107840842A CN 201610833890 A CN201610833890 A CN 201610833890A CN 107840842 A CN107840842 A CN 107840842A
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alkyl
cycloalkyl
compound
independently selected
cyano group
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Chinese (zh)
Inventor
陈向阳
高英祥
孔祥龙
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Beijing Medical Technology Co., Ltd.
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Beijing Tiancheng Pharmaceutical Technology Co Ltd
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Priority to CN201610833890.3A priority Critical patent/CN107840842A/zh
Priority to PCT/CN2017/072570 priority patent/WO2018049781A1/zh
Priority to EP17849992.7A priority patent/EP3517535B1/en
Priority to AU2017327954A priority patent/AU2017327954B2/en
Priority to RU2019112046A priority patent/RU2729069C1/ru
Priority to MX2019003143A priority patent/MX390747B/es
Priority to SG10202102822RA priority patent/SG10202102822RA/en
Priority to CN201780057036.5A priority patent/CN109843873B/zh
Priority to KR1020197011454A priority patent/KR102783517B1/ko
Priority to JP2019515464A priority patent/JP6906811B2/ja
Priority to CA3036594A priority patent/CA3036594C/en
Priority to ES17849992T priority patent/ES2925212T3/es
Publication of CN107840842A publication Critical patent/CN107840842A/zh
Priority to US16/353,806 priority patent/US10710981B2/en
Priority to US16/925,738 priority patent/US11059805B2/en
Priority to US17/369,850 priority patent/US11572353B2/en
Withdrawn legal-status Critical Current

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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)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Plural Heterocyclic Compounds (AREA)
CN201610833890.3A 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 Withdrawn CN107840842A (zh)

Priority Applications (15)

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
CN201780057036.5A CN109843873B (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
KR1020197011454A KR102783517B1 (ko) 2016-09-19 2017-01-25 알키닐-치환된 헤테로시클릭 화합물, 이의 제조 방법 및 이의 의약 용도
AU2017327954A AU2017327954B2 (en) 2016-09-19 2017-01-25 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof
RU2019112046A RU2729069C1 (ru) 2016-09-19 2017-01-25 Алкинил-замещенное гетероциклическое соединение, способ его получения и его применение в медицине
MX2019003143A MX390747B (es) 2016-09-19 2017-01-25 Compuesto heterociclico sustituido con alquinilo, su metodo de preparacion y su uso medico.
SG10202102822RA SG10202102822RA (en) 2016-09-19 2017-01-25 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof
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
EP17849992.7A EP3517535B1 (en) 2016-09-19 2017-01-25 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof
JP2019515464A JP6906811B2 (ja) 2016-09-19 2017-01-25 アルキル置換複素環化合物、そのための調製方法およびその医学的用途
CA3036594A CA3036594C (en) 2016-09-19 2017-01-25 Alkynyl-substituted heterocyclic compound, preparation method thereof and medical use thereof
ES17849992T ES2925212T3 (es) 2016-09-19 2017-01-25 Compuesto heterocíclico sustituido con alquinilo, método de preparación y uso médico del mismo
US16/353,806 US10710981B2 (en) 2016-09-19 2019-03-14 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof
US16/925,738 US11059805B2 (en) 2016-09-19 2020-07-10 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof
US17/369,850 US11572353B2 (en) 2016-09-19 2021-07-07 Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use thereof

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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

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CN107840842A true CN107840842A (zh) 2018-03-27

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CN201610833890.3A Withdrawn 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
CN201780057036.5A Active CN109843873B (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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US (3) US10710981B2 (https=)
EP (1) EP3517535B1 (https=)
JP (1) JP6906811B2 (https=)
KR (1) KR102783517B1 (https=)
CN (2) CN107840842A (https=)
AU (1) AU2017327954B2 (https=)
CA (1) CA3036594C (https=)
ES (1) ES2925212T3 (https=)
MX (1) MX390747B (https=)
RU (1) RU2729069C1 (https=)
SG (1) SG10202102822RA (https=)
WO (1) WO2018049781A1 (https=)

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CN114853739A (zh) * 2021-02-03 2022-08-05 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
CN115043832A (zh) * 2021-03-08 2022-09-13 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
CN115433190A (zh) * 2021-06-02 2022-12-06 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
CN115867547A (zh) * 2020-08-27 2023-03-28 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
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

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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
MX2024005341A (es) * 2021-11-03 2024-05-20 Beijing Innocare Pharma Tech Co Ltd Dispersion solida amorfa que comprende (s)-1-(1-acriloilpirrolidin -3-il)-3-((3,5-dimetoxifenil)etinil)-5-(metilamino)-1h-pirazol-4- carboxamida.
MX2024005882A (es) * 2021-11-16 2024-05-29 Beijing Innocare Pharma Tech Co Ltd Metodo para el tratamiento del cancer de cabeza y cuello.
WO2023107870A1 (en) * 2021-12-08 2023-06-15 Kinnate Biopharma Inc. Inhibitors of fibroblast growth factor receptor kinases
AU2022407440A1 (en) * 2021-12-08 2024-06-20 Kinnate Biopharma Inc. Solid state forms of an fgfr inhibitor
TW202333686A (zh) * 2021-12-08 2023-09-01 美商奇奈特生物製藥公司 以fgfr激酶抑制劑治療癌症

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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN115867547A (zh) * 2020-08-27 2023-03-28 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
CN114853739A (zh) * 2021-02-03 2022-08-05 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
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
CN115043832A (zh) * 2021-03-08 2022-09-13 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
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
CN115433190A (zh) * 2021-06-02 2022-12-06 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

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