CN105189517A - 含多环取代的吡唑类激酶活性抑制剂及其用途 - Google Patents

含多环取代的吡唑类激酶活性抑制剂及其用途 Download PDF

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CN105189517A
CN105189517A CN201480004085.9A CN201480004085A CN105189517A CN 105189517 A CN105189517 A CN 105189517A CN 201480004085 A CN201480004085 A CN 201480004085A CN 105189517 A CN105189517 A CN 105189517A
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methyl
phenyl
pyrazolecarboxamides
another
amino
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CN105189517B (zh
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陆涛
王越
陈亚东
陆旖
王占伟
金乔梅
杨涛涛
林国武
郭青龙
赵丽
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Shanghai Fosun Pharmaceutical Development Co Ltd
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Abstract

本发明涉及药物化学领域,具体涉及4-(五元杂环并嘧啶/吡啶取代)氨基-1H-3-吡唑甲酰胺类衍生物、它们的制备方法、含有这些化合物的药用组合物以及它们的医疗用途,特别是作为蛋白激酶抑制剂的抗肿瘤用途。

Description

PCT国内申请,说明书已公开。

Claims (1)

  1. PCT国内申请,权利要求书已公开。
CN201480004085.9A 2013-01-08 2014-01-07 含多环取代的吡唑类激酶活性抑制剂及其用途 Active CN105189517B (zh)

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CN201480004085.9A CN105189517B (zh) 2013-01-08 2014-01-07 含多环取代的吡唑类激酶活性抑制剂及其用途
CN201710450213.8A CN107098903B (zh) 2013-01-08 2014-01-07 含多环取代的吡唑类激酶活性抑制剂及其用途

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CN2013100052586 2013-01-08
CN2013100052586A CN103012428A (zh) 2013-01-08 2013-01-08 4-(五元杂环并嘧啶/吡啶取代)氨基-1H-3-吡唑甲酰胺类CDK/Aurora双重抑制剂及其用途
CN201480004085.9A CN105189517B (zh) 2013-01-08 2014-01-07 含多环取代的吡唑类激酶活性抑制剂及其用途
PCT/CN2014/070195 WO2014108053A1 (zh) 2013-01-08 2014-01-07 含多环取代的吡唑类激酶活性抑制剂及其用途

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EP (1) EP2955185B1 (zh)
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AU (1) AU2014204633B2 (zh)
BR (1) BR112015016327A8 (zh)
CA (1) CA2897366C (zh)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110835334A (zh) * 2018-08-16 2020-02-25 中国药科大学 吲哚取代唑类化合物及其用途

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103012428A (zh) * 2013-01-08 2013-04-03 中国药科大学 4-(五元杂环并嘧啶/吡啶取代)氨基-1H-3-吡唑甲酰胺类CDK/Aurora双重抑制剂及其用途
CN103435606A (zh) * 2013-08-22 2013-12-11 中国药科大学 CDK2与GSK3β双重抑制剂及用途
CN104592251B (zh) * 2015-01-23 2019-10-01 上海复星医药产业发展有限公司 4-(稠杂环取代氨基)-1h-吡唑-3-甲酰胺类化合物及其用途
CN107235906B (zh) * 2017-06-28 2020-05-01 郑州大学第一附属医院 一组吡唑酰胺类衍生物及其应用
CN107245073B (zh) * 2017-07-11 2020-04-17 中国药科大学 4-(芳杂环取代)氨基-1h-3-吡唑甲酰胺类flt3抑制剂及其用途
IL272838B2 (en) 2017-10-06 2023-09-01 Forma Therapeutics Inc Peptidase-specific ubiquitin inhibition 30
CN109970717B (zh) * 2017-12-28 2022-10-18 中国药科大学 4-(脂肪环并嘧啶/吡啶取代)氨基-1h-3-吡唑甲酰胺类flt3抑制剂及其用途
SG11202011299PA (en) 2018-05-17 2020-12-30 Forma Therapeutics Inc Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors
PE20211053A1 (es) 2018-10-05 2021-06-07 Forma Therapeutics Inc Inhibicion de la proteasa 30 especifica de la ubiquitina (usp30)
CN111171044B (zh) * 2018-11-13 2022-06-24 沈阳化工研究院有限公司 一种噻吩并嘧啶类化合物及其医药用途
WO2020132384A1 (en) 2018-12-21 2020-06-25 Celgene Corporation Thienopyridine inhibitors of ripk2
CN113677341B (zh) * 2019-02-01 2024-07-05 南卡罗莱纳大学 双环吡啶组合物及其用于癌症治疗的方法
KR20200100429A (ko) * 2019-02-18 2020-08-26 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 신규한 피리도[3,4-d]피리미딘-8-온 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물
CN110183464B (zh) * 2019-05-31 2021-08-31 淮阴工学院 一种抗癌化合物艾斯替尼及其合成方法和应用
CN112794855B (zh) * 2019-11-13 2023-07-28 中国药科大学 N-芳基嘧啶-4-胺类衍生物的制备方法与应用
CN112043710A (zh) * 2020-09-28 2020-12-08 广州智睿医药科技有限公司 一种治疗或预防与lrrk2激酶或异常lrrk2突变激酶活性相关疾病的药物
WO2023168246A2 (en) * 2022-03-01 2023-09-07 Purdue Research Foundation Selective g protein-coupled receptor kinase 5 inhibitors, compositions, and methods of use
CN114685371A (zh) * 2022-03-08 2022-07-01 四川大学 吡唑甲酰胺衍生物及其制备方法和用途
CN115746002B (zh) * 2022-11-13 2023-12-08 药康众拓(江苏)医药科技有限公司 一种氘代氮杂吲哚氨基-吡唑甲酰胺类化合物及其用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1826323A (zh) * 2003-07-22 2006-08-30 阿斯泰克斯治疗有限公司 3,4-二取代的1h-吡唑化合物及其作为细胞周期蛋白依赖性激酶(cdk)和糖原合成酶激酶-3(gsk-3)调节剂的用途
WO2009134658A2 (en) * 2008-04-30 2009-11-05 National Health Research Institutes Fused bicyclic pyrimidine compounds as aurora kinase inhibitors
CN103012428A (zh) * 2013-01-08 2013-04-03 中国药科大学 4-(五元杂环并嘧啶/吡啶取代)氨基-1H-3-吡唑甲酰胺类CDK/Aurora双重抑制剂及其用途

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100355750C (zh) 2000-09-15 2007-12-19 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡唑化合物
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
CL2004000797A1 (es) * 2003-04-16 2005-05-27 Astrazeneca Ab Compuestos derivados de quinazolina, inhibidores de aurora quinasa; procedimiento de preparacion; composicion farmaceutica; y su uso para preparar un medicamento para tratar cancer colorrectal, de mama, de pulmon, de prostata, de vejiga, renal o panc
JP4681548B2 (ja) * 2003-07-22 2011-05-11 アステックス・セラピューティクス・リミテッド 3,4−ジ置換1h−ピラゾール化合物および、そのサイクリン依存性キナーゼ(cdk)およびグリコーゲン・シンセターゼ・キナーゼ−3(gsk−3)調節剤としての使用
MY141220A (en) * 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
US7601725B2 (en) 2004-07-16 2009-10-13 Sunesis Pharmaceuticals, Inc. Thienopyrimidines useful as Aurora kinase inhibitors
WO2006032851A1 (en) 2004-09-20 2006-03-30 Biolipox Ab Pyrazole compounds useful in the treatment of inflammation
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
WO2008007113A2 (en) 2006-07-14 2008-01-17 Astex Therapeutics Limited Pharmaceutical combinations
MX2007008781A (es) 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
US20080161355A1 (en) * 2005-01-21 2008-07-03 Astex Therapeutics Limited Combinations of Pyrazole Kinase Inhibitors and Further Antitumor Agents
EP1847531A4 (en) 2005-02-09 2009-04-22 Takeda Pharmaceutical PYRAZOLE DERIVATIVE
WO2008007122A2 (en) 2006-07-14 2008-01-17 Astex Therapeutics Limited Combinations of pyrazole derivatives for the inhibition of cdks and gsk's
EP2049516A2 (en) * 2006-07-14 2009-04-22 Astex Therapeutics Limited Pharmaceutical compounds
WO2008009954A1 (en) 2006-07-21 2008-01-24 Astex Therapeutics Limited Medical use of cyclin dependent kinases inhibitors
WO2009078432A1 (ja) 2007-12-18 2009-06-25 Taisho Pharmaceutical Co., Ltd. 1-アルキル-4-アミノ-1h-ピラゾール-3-カルボキサミド化合物
CN102232071B (zh) * 2008-09-26 2016-03-23 财团法人卫生研究院 作为蛋白激酶抑制剂的稠合多环化合物
AU2009322270B2 (en) * 2008-12-05 2014-12-18 Abbvie Bahamas Ltd Thieno [3, 2-c] pyridine derivatives as kinase inhibitors for use in the treatment of cancer
BR112012002336A2 (pt) 2009-08-07 2016-05-31 Merck Patent Gmbh compostos aza-heterocíclicos
TW201132644A (en) 2009-12-23 2011-10-01 Biocryst Pharm Inc Heterocyclic compounds as Janus kinase inhibitors
CN102060772A (zh) * 2010-12-17 2011-05-18 中国药科大学 N-(4-取代苯基)-1h-3-吡唑甲酰胺类细胞周期蛋白依赖性激酶2抑制剂及其用途
EP2723747A1 (en) * 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1826323A (zh) * 2003-07-22 2006-08-30 阿斯泰克斯治疗有限公司 3,4-二取代的1h-吡唑化合物及其作为细胞周期蛋白依赖性激酶(cdk)和糖原合成酶激酶-3(gsk-3)调节剂的用途
WO2009134658A2 (en) * 2008-04-30 2009-11-05 National Health Research Institutes Fused bicyclic pyrimidine compounds as aurora kinase inhibitors
CN103012428A (zh) * 2013-01-08 2013-04-03 中国药科大学 4-(五元杂环并嘧啶/吡啶取代)氨基-1H-3-吡唑甲酰胺类CDK/Aurora双重抑制剂及其用途

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110835334A (zh) * 2018-08-16 2020-02-25 中国药科大学 吲哚取代唑类化合物及其用途
CN110835334B (zh) * 2018-08-16 2022-10-18 中国药科大学 吲哚取代唑类化合物及其用途

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