CN109890820B - 用作神经营养因子酪氨酸激酶受体抑制剂的氨基吡唑并嘧啶化合物 - Google Patents

用作神经营养因子酪氨酸激酶受体抑制剂的氨基吡唑并嘧啶化合物 Download PDF

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Publication number
CN109890820B
CN109890820B CN201780064022.6A CN201780064022A CN109890820B CN 109890820 B CN109890820 B CN 109890820B CN 201780064022 A CN201780064022 A CN 201780064022A CN 109890820 B CN109890820 B CN 109890820B
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phenyl
ethyl
methyl
independently selected
hydroxy
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Chinese (zh)
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CN109890820A (zh
Inventor
祝力
胡远东
吴伟
戴丽光
段小伟
杨艳青
孙颖慧
韩永信
彭勇
孔凡胜
罗鸿
杨玲
徐宏江
郭猛
仲兆柏
王善春
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Centaurus Biopharma Co Ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
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Centaurus Biopharma Co Ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201780064022.6A 2016-10-28 2017-10-27 用作神经营养因子酪氨酸激酶受体抑制剂的氨基吡唑并嘧啶化合物 Active CN109890820B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2016109703143 2016-10-28
CN201610970314 2016-10-28
CN201710044000 2017-01-21
CN2017100440005 2017-01-21
PCT/CN2017/108100 WO2018077246A1 (zh) 2016-10-28 2017-10-27 用作神经营养因子酪氨酸激酶受体抑制剂的氨基吡唑并嘧啶化合物

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CN109890820A CN109890820A (zh) 2019-06-14
CN109890820B true CN109890820B (zh) 2020-11-03

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US (1) US10829492B2 (https=)
EP (1) EP3533796B1 (https=)
JP (1) JP7046940B2 (https=)
KR (1) KR102616249B1 (https=)
CN (1) CN109890820B (https=)
AU (1) AU2017348826B2 (https=)
CA (1) CA3041942C (https=)
DK (1) DK3533796T3 (https=)
ES (1) ES2896943T3 (https=)
HU (1) HUE057733T2 (https=)
MX (1) MX380283B (https=)
PL (1) PL3533796T3 (https=)
PT (1) PT3533796T (https=)
RU (1) RU2764523C2 (https=)
WO (1) WO2018077246A1 (https=)

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US11286264B2 (en) * 2017-07-28 2022-03-29 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof
DK3674307T3 (da) 2017-08-23 2023-09-11 Chia Tai Tianqing Pharmaceutical Group Co Ltd Makrocyklus indeholdende aminopyrazol og pyrimidin og farmaceutisk sammensætning og anvendelse deraf
CN108794370A (zh) * 2018-07-31 2018-11-13 上海弈柯莱生物医药科技有限公司 一种拉罗替尼中间体的制备方法
CA3122136A1 (en) * 2018-12-07 2021-06-11 Betta Pharmaceuticals Co., Ltd Tyrosine kinase inhibitors, compositions and methods there of
JP7209415B2 (ja) 2019-03-19 2023-01-20 セントラル チャイナ ノーマル ユニバーシティ ピラゾロピリミジン化合物、医薬組成物、及びその使用
CN112979654B (zh) * 2019-12-16 2024-03-19 赛诺哈勃药业（成都）有限公司 杂芳基稠环化合物、其制备方法及应用
TW202214635A (zh) * 2020-06-11 2022-04-16 大陸商貝達藥業股份有限公司 酪氨酸激酶抑制劑的鹽型、晶型、藥物組合物及其用途
CN111620881B (zh) * 2020-07-08 2023-03-31 浙江合聚生物医药有限公司 拉罗替尼衍生物及其制备方法和应用
CN113563343B (zh) * 2020-07-27 2022-05-24 杭州邦顺制药有限公司 取代的吡唑并[1,5-a]嘧啶化合物及其用途
CN112010860B (zh) * 2020-08-05 2023-03-10 南京纳丁菲医药科技有限公司 苄氧基吡唑并嘧啶化合物和药物组合物及其应用
CN114437075B (zh) * 2020-11-03 2026-01-30 上海瑶琪生物科技有限公司 用作ntrk激酶抑制剂的化合物及其应用
CN113200963A (zh) * 2021-03-31 2021-08-03 广东石油化工学院 N-(吡咯基)-3-吡唑基胺及其制备方法
JP7840066B2 (ja) * 2021-05-03 2026-04-03 ジェービーケーラボ カンパニー リミテッド ２，６－ジクロロ－４－（４－（４－ヒドロキシシクロヘキシルアミノ）－７ｈ－ピロロ［２，３－ｄ］ピリミジン－５－イル）フェノールを活性成分として含有する、がんを予防、緩和、または処置するための医薬組成物
CN117751121A (zh) * 2021-07-30 2024-03-22 正大天晴药业集团股份有限公司 氨基吡唑并嘧啶化合物的晶体
WO2023011616A1 (zh) * 2021-08-06 2023-02-09 正大天晴药业集团股份有限公司 氨基吡唑并嘧啶化合物在治疗trk激酶介导的肿瘤中的用途
CN117088800B (zh) * 2023-08-18 2024-05-28 龙曦宁（上海）医药科技有限公司 一种5-甲基吡咯烷-3-醇盐酸盐的制备方法

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CN102056927A (zh) * 2008-05-13 2011-05-11 Irm责任有限公司 作为激酶抑制剂的稠合含氮杂环及其组合物
CN102264736A (zh) * 2008-10-22 2011-11-30 阵列生物制药公司 作为TRK激酶抑制剂的取代的吡唑并[1，5-a]嘧啶化合物
CN102596957A (zh) * 2009-07-09 2012-07-18 阵列生物制药公司 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物
WO2013028263A1 (en) * 2011-08-24 2013-02-28 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as pi3 kinase inhibitors
WO2014143242A1 (en) * 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN104114553A (zh) * 2011-12-12 2014-10-22 雷迪博士实验室有限公司 作为原肌球蛋白受体激酶(Trk)抑制剂的取代的吡唑并[1,5-a]吡啶
CN104650092A (zh) * 2013-11-16 2015-05-27 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
CN104995172A (zh) * 2013-02-19 2015-10-21 小野药品工业株式会社 Trk抑制化合物
WO2016097869A1 (en) * 2014-12-15 2016-06-23 Cmg Pharmaceutical Co., Ltd. Fused ring heteroaryl compounds and their use as trk inhibitors

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PT2350075E (pt) 2008-09-22 2014-06-09 Array Biopharma Inc Compostos imidazo[1,2b]piridazina substituídos como inibidores da trk cinase
WO2012034095A1 (en) * 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
WO2012116217A1 (en) 2011-02-25 2012-08-30 Irm Llc Compounds and compositions as trk inhibitors
DK3077397T3 (da) * 2013-12-06 2019-12-16 Vertex Pharma 2-amino-6-fluor-n-[5-fluor-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamidforbindelse anvendelig som atr-kinase-inhibitor, dens fremstilling, forskellige faste former og radiomarkerede derivater deraf

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Publication number Priority date Publication date Assignee Title
CN102056927A (zh) * 2008-05-13 2011-05-11 Irm责任有限公司 作为激酶抑制剂的稠合含氮杂环及其组合物
CN102264736A (zh) * 2008-10-22 2011-11-30 阵列生物制药公司 作为TRK激酶抑制剂的取代的吡唑并[1，5-a]嘧啶化合物
CN102596957A (zh) * 2009-07-09 2012-07-18 阵列生物制药公司 作为TRK激酶抑制剂的被取代的吡唑并[1,5-a]嘧啶化合物
WO2013028263A1 (en) * 2011-08-24 2013-02-28 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as pi3 kinase inhibitors
CN104114553A (zh) * 2011-12-12 2014-10-22 雷迪博士实验室有限公司 作为原肌球蛋白受体激酶(Trk)抑制剂的取代的吡唑并[1,5-a]吡啶
CN104995172A (zh) * 2013-02-19 2015-10-21 小野药品工业株式会社 Trk抑制化合物
WO2014143242A1 (en) * 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN104650092A (zh) * 2013-11-16 2015-05-27 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
WO2016097869A1 (en) * 2014-12-15 2016-06-23 Cmg Pharmaceutical Co., Ltd. Fused ring heteroaryl compounds and their use as trk inhibitors

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PL3533796T3 (pl) 2022-01-17
US10829492B2 (en) 2020-11-10
MX380283B (es) 2025-03-12
KR102616249B1 (ko) 2023-12-21
EP3533796B1 (en) 2021-09-29
RU2019114600A3 (https=) 2021-02-20
US20190352306A1 (en) 2019-11-21
CA3041942C (en) 2023-03-14
MX2019004847A (es) 2019-08-29
KR20190067913A (ko) 2019-06-17
BR112019008656A8 (pt) 2022-06-07
ES2896943T3 (es) 2022-02-28
WO2018077246A1 (zh) 2018-05-03
AU2017348826B2 (en) 2021-12-02
DK3533796T3 (da) 2021-11-08
EP3533796A4 (en) 2020-06-03
BR112019008656A2 (pt) 2019-07-09
PT3533796T (pt) 2021-11-18
EP3533796A1 (en) 2019-09-04
RU2019114600A (ru) 2020-11-30
JP7046940B2 (ja) 2022-04-04
JP2019537588A (ja) 2019-12-26
CA3041942A1 (en) 2018-05-03
CN109890820A (zh) 2019-06-14
AU2017348826A1 (en) 2019-05-23
HUE057733T2 (hu) 2022-06-28
RU2764523C2 (ru) 2022-01-18

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