CN109890820A - 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
CN109890820A
CN109890820A CN201780064022.6A CN201780064022A CN109890820A CN 109890820 A CN109890820 A CN 109890820A CN 201780064022 A CN201780064022 A CN 201780064022A CN 109890820 A CN109890820 A CN 109890820A
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hydroxyl
independently selected
group
alkyl
phenyl
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CN201780064022.6A
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CN109890820B (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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Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Shouyao Holdings Beijing Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Shouyao Holdings Beijing 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
    • 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
    • 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

Abstract

本申请提供了用作神经营养因子酪氨酸激酶受体抑制剂的由如下结构式表示的氨基吡唑并嘧啶化合物，其能够抑制Trk激酶的活性，并可以治疗哺乳动物的由Trk酪氨酸激酶受体介导的疾病。

Description

PCT国内申请，说明书已公开。

Claims (17)

  1. PCT国内申请，权利要求书已公开。
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
CN201610970314 2016-10-28
CN2016109703143 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 true CN109890820A (zh) 2019-06-14
CN109890820B CN109890820B (zh) 2020-11-03

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US (1) US10829492B2 (zh)
EP (1) EP3533796B1 (zh)
JP (1) JP7046940B2 (zh)
KR (1) KR102616249B1 (zh)
CN (1) CN109890820B (zh)
AU (1) AU2017348826B2 (zh)
BR (1) BR112019008656A8 (zh)
CA (1) CA3041942C (zh)
DK (1) DK3533796T3 (zh)
ES (1) ES2896943T3 (zh)
HU (1) HUE057733T2 (zh)
MX (1) MX2019004847A (zh)
PL (1) PL3533796T3 (zh)
PT (1) PT3533796T (zh)
RU (1) RU2764523C2 (zh)
WO (1) WO2018077246A1 (zh)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112010860A (zh) * 2020-08-05 2020-12-01 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
CN113563343A (zh) * 2020-07-27 2021-10-29 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
WO2022095909A1 (zh) * 2020-11-03 2022-05-12 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

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3071032A1 (en) * 2017-08-23 2019-02-28 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Macrocycle containing aminopyrazole and pyrimidine and pharmaceutical composition and use thereof
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
US20210395256A1 (en) * 2018-12-07 2021-12-23 Betta Pharmaceuticals Co., Ltd. Tyrosine kinase inhibitors, compositions and methods there of
WO2020187291A1 (zh) 2019-03-19 2020-09-24 华中师范大学 吡唑并嘧啶化合物和药物组合物及其应用
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
CN115551863A (zh) * 2020-06-11 2022-12-30 贝达药业股份有限公司 酪氨酸激酶抑制剂的盐型、晶型、药物组合物及其用途
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
WO2023006057A1 (zh) * 2021-07-30 2023-02-02 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
CN117088800A (zh) * 2023-08-18 2023-11-21 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 (9)

* Cited by examiner, † Cited by third party
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
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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10356579A1 (de) * 2003-12-04 2005-07-07 Merck Patent Gmbh Aminderivate
US8841462B2 (en) 2008-07-01 2014-09-23 Robert A. Heald Bicyclic heterocycles as MEK kinase inhibitors
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
BR112013021638A2 (pt) 2011-02-25 2016-08-02 Irm Llc "compostos inibidores de trk, seu uso e composições que os compreendem"
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

Patent Citations (9)

* Cited by examiner, † Cited by third party
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

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113563343A (zh) * 2020-07-27 2021-10-29 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
CN112010860A (zh) * 2020-08-05 2020-12-01 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
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
WO2022095909A1 (zh) * 2020-11-03 2022-05-12 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

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ES2896943T3 (es) 2022-02-28
EP3533796A1 (en) 2019-09-04
AU2017348826B2 (en) 2021-12-02
AU2017348826A1 (en) 2019-05-23
JP7046940B2 (ja) 2022-04-04
CA3041942C (en) 2023-03-14
US20190352306A1 (en) 2019-11-21
CN109890820B (zh) 2020-11-03
RU2019114600A (ru) 2020-11-30
JP2019537588A (ja) 2019-12-26
KR20190067913A (ko) 2019-06-17
PT3533796T (pt) 2021-11-18
DK3533796T3 (da) 2021-11-08
MX2019004847A (es) 2019-08-29
CA3041942A1 (en) 2018-05-03
WO2018077246A1 (zh) 2018-05-03
BR112019008656A2 (pt) 2019-07-09
EP3533796A4 (en) 2020-06-03
US10829492B2 (en) 2020-11-10
BR112019008656A8 (pt) 2022-06-07
RU2764523C2 (ru) 2022-01-18
KR102616249B1 (ko) 2023-12-21
PL3533796T3 (pl) 2022-01-17
RU2019114600A3 (zh) 2021-02-20
HUE057733T2 (hu) 2022-06-28
EP3533796B1 (en) 2021-09-29

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