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一种选择性FGFR4激酶抑制剂

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摘要

本发明涉及一种选择性FGFR4激酶抑制剂，提供式(I)化合物，其立体异构体、互变异构体或药学上可接受的盐，其作为FGFR4激酶选择性抑制剂及其在制备治疗由FGFR4或FGF19所致疾病的药物或药物组合物中的应用，本发明公开的化合物对FGFR4具有选择性的显著抑制活性，在肿瘤治疗领域具有广泛的应用前景。

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公开/公告号CN107304210A

专利类型发明专利
公开/公告日2017-10-31

原文格式PDF
申请/专利权人成都融科博海科技有限公司;
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申请/专利号CN201610395775.2
发明设计人李秀萍;
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申请日2016-06-07
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代理机构
代理人
地址 610041 四川省成都市高新区天府大道北段1480号1号楼A座E6号
入库时间 2023-06-19 03:35:50

法律信息

法律状态公告日

法律状态信息

法律状态
2019-11-12

发明专利申请公布后的视为撤回 IPC(主分类):C07D471/04 申请公布日:20171031 申请日:20160607

发明专利申请公布后的视为撤回
2017-10-31

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1. 一种选择性FGFR4激酶抑制剂 [P] . 中国专利： CN107304210A . 2017-10-31
2. 一种FGFR4激酶抑制剂及其制备方法和用途 [P] . 中国专利： CN110950867A . 2020-04-03
3. Ultrasensitive methodology for quantifying the kinase catalytic activity of any protein kinase in biological/clinical samples or recombinant/purified proteins using near-infrared-fluorescence (NIRF)-labeled, kinase-selective peptide substrates and a combination of kinase-selective inhibitors to define individual kinase activity [P] . 美国专利： US2014287447A1 . 2014-09-25

机译：使用近红外荧光（NIRF）标记的激酶选择性肽底物和激酶选择性抑制剂组合定义个体的超灵敏方法，用于定量生物学/临床样品或重组/纯化蛋白中任何蛋白激酶的激酶催化活性激酶活性
4. Polinucleotu00eddeo insulated tape of expression, host cell, isolated transgenic non-human animal polypeptide, which has been modified to express a polypeptide mutant with resistance to ALK, antibody that binds specifically to a polypeptide mutant with resistance to ALK, kit p For detection of a mutation with resistance to ALK inhibitor in a biological sample, and,Methods for evaluating a biological sample as a mutation with resistance to ALK inhibitor, for diagnosing a cancer that is resistant to or is likely to develop resistance to at least one inhibitor of kinase small molecule ALK, to evaluate a biological sample that Anto a mutation with resistance to ALK inhibitor.For diagnosing a cancer that is resistant to or is likely to develop resistance to at least one inhibitor of kinase small molecule ALK, to assess the biological sample as a mutation with resistance to ALK inhibitor, a cancer that is resistant to dianosticar Or is likely to develop resistance to PF - 02341066 in a pati [P] . BR112012026239A2 . 2016-11-29

机译：修饰的多聚核苷酸绝缘带，宿主细胞，分离的转基因非人类动物多肽，经过修饰以表达对ALK具有抗性的多肽突变体，与对ALK具有抗性的多肽突变体特异性结合的抗体，试剂盒p用于检测生物样品中对ALK抑制剂具有抗性的突变，以及用于评估生物样品为对ALK抑制剂具有抗性的突变的方法，用于诊断对至少一种对ALK抑制剂具有抗性或可能发展出抗性的癌症激酶小分子ALK，以评估Anto对ALK抑制剂具有抗性的突变的生物样品。用于诊断对至少一种激酶小分子ALK抑制剂具有抗药性或可能产生抗性的癌症，以评估该生物样品作为对ALK抑制剂有抗性的突变，即对狄诺司他抗性或可能对PF产生抗药性的癌症-02341066
5. isolated polynucleotide, expression cassette, host cell, isolated polypeptide, non-human transgenic animal that has been altered to express an alkali resistant mutant polypeptide, an antibody that specifically binds to an alkali resistant mutant polypeptide, a mutation detection kit alk inhibitor resistance in a biological sample, and methods for evaluating a biological sample for an alk inhibitor resistance mutation to diagnose cancer that is resistant to or likely to develop resistance to at least one alkaline inhibitor. small alk molecule kinase, to evaluate a biological sample for an alk inhibitor resistance mutation, to diagnose cancer that is resistant to or likely to develop resistance to pf-02341066 in a patient, to specifically reduce expression of an alk-resistant mutant to treat cancer associated with activating aberrant loop capacity that is resistant to at least one small molecule alk kinase inhibitor treating an aberrant cancer that is resistant to pf-02341066, identifyin [P] . BR112012026239A2 . 2018-06-26

机译：分离的多核苷酸，表达盒，宿主细胞，分离的多肽，已被改变以表达耐碱突变体多肽的非人类转基因动物，与耐碱突变体多肽特异性结合的抗体，突变检测试剂盒生物样品，以及用于评估生物样品中是否存在对烷基抑制剂的抗性突变以诊断对至少一种碱性抑制剂有抗药性或可能发展出抗药性的癌症的方法。小分子激酶，用于评估生物学样品中是否具有抑制碱性磷酸酶抑制剂的突变，以诊断对患者具有抗药性或可能对pf-02341066产生抗药性的癌症，从而特异性降低抗癌突变体的表达以治疗癌症与激活抗至少一种小分子烷基激酶抑制剂的异常环路能力有关，该抑制剂治疗对pf-02341066有抵抗力的异常癌症