JP7046940B2 - 神経栄養因子チロシンキナーゼ受容体阻害剤として用いられるアミノピラゾロピリミジン化合物 - Google Patents

神経栄養因子チロシンキナーゼ受容体阻害剤として用いられるアミノピラゾロピリミジン化合物 Download PDF

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JP7046940B2
JP7046940B2 JP2019522962A JP2019522962A JP7046940B2 JP 7046940 B2 JP7046940 B2 JP 7046940B2 JP 2019522962 A JP2019522962 A JP 2019522962A JP 2019522962 A JP2019522962 A JP 2019522962A JP 7046940 B2 JP7046940 B2 JP 7046940B2
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JP2019537588A5 (https=
JP2019537588A (ja
JPWO2018077246A5 (https=
Inventor
祝力
胡遠東
呉偉
戴麗光
段小偉
楊艷青
孫穎慧
韓永信
彭勇
孔凡勝
羅鴻
楊玲
徐宏江
郭猛
仲兆柏
王善春
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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    • 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
    • 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

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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)
JP2019522962A 2016-10-28 2017-10-27 神経栄養因子チロシンキナーゼ受容体阻害剤として用いられるアミノピラゾロピリミジン化合物 Active JP7046940B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201610970314 2016-10-28
CN201610970314.3 2016-10-28
CN201710044000 2017-01-21
CN201710044000.5 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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JP2019537588A JP2019537588A (ja) 2019-12-26
JP2019537588A5 JP2019537588A5 (https=) 2022-01-21
JPWO2018077246A5 JPWO2018077246A5 (https=) 2022-01-21
JP7046940B2 true JP7046940B2 (ja) 2022-04-04

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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

Citations (3)

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Publication number Priority date Publication date Assignee Title
JP2007513099A (ja) 2003-12-04 2007-05-24 メルク　パテント　ゲゼルシャフト　ミット　ベシュレンクテル　ハフトング アミン誘導体
JP2012532888A (ja) 2009-07-09 2012-12-20 アレイ バイオファーマ、インコーポレイテッド ＴＲＫキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピリミジン化合物
WO2013028263A1 (en) 2011-08-24 2013-02-28 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as pi3 kinase inhibitors

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WO2009140128A2 (en) 2008-05-13 2009-11-19 Irm Llc Compounds and compositions as kinase inhibitors
RU2509078C2 (ru) 2008-07-01 2014-03-10 Дженентек, Инк. Бициклические гетероциклы в качестве ингибиторов киназы мек
PT2350075E (pt) 2008-09-22 2014-06-09 Array Biopharma Inc Compostos imidazo[1,2b]piridazina substituídos como inibidores da trk cinase
AR074052A1 (es) * 2008-10-22 2010-12-22 Array Biopharma Inc Compuestos pirazolo{1,5-a}pirimidina sustituida como inhibidores de trk cinasa
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
KR20140105508A (ko) * 2011-12-12 2014-09-01 닥터 레디스 레보러터리즈 리미티드 트로포미오신 수용체 키나제(Trk) 억제제인 치환된 피라졸로[1,5-a]피리딘
MX362181B (es) 2013-02-19 2019-01-08 Ono Pharmaceutical Co Compuesto inhibidor de cinasa del receptor de tropomiosina (trk).
WO2014143242A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN104650092B (zh) * 2013-11-16 2017-11-10 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
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
CA2971024C (en) 2014-12-15 2023-09-26 Handok Inc. Fused ring heteroaryl compounds and their use as trk inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007513099A (ja) 2003-12-04 2007-05-24 メルク　パテント　ゲゼルシャフト　ミット　ベシュレンクテル　ハフトング アミン誘導体
JP2012532888A (ja) 2009-07-09 2012-12-20 アレイ バイオファーマ、インコーポレイテッド ＴＲＫキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピリミジン化合物
WO2013028263A1 (en) 2011-08-24 2013-02-28 Glaxosmithkline Llc Pyrazolopyrimidine derivatives as pi3 kinase inhibitors

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PL3533796T3 (pl) 2022-01-17
CN109890820B (zh) 2020-11-03
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
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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