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一种IKKβ/NEMO小分子抑制剂及其在药物制备中的应用

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摘要

本发明公开了一种IKKβ/NEMO小分子抑制剂及其在药物制备中的应用，属于生物医药技术领域，所述IKKβ/NEMO小分子抑制剂为紫草素，还包括其药学上可接受的盐、水合物、溶剂化物或立体异构体，或具有前述一种或者多种的药物组合物，其用作抑制或破坏IKKβ/NEMO复合物的药物，可以有效地治疗IKKβ/NEMO相关疾病。

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公开/公告号CN113332265A

专利类型发明专利
公开/公告日2021-09-03

原文格式PDF
申请/专利权人大连医科大学;
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申请/专利号CN202110599250.1
发明设计人马骁驰;于振龙;王超;
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申请日2021-05-31
分类号A61K31/122(20060101);A61P35/00(20060101);A61P29/00(20060101);A61P37/06(20060101);C07C50/32(20060101);
代理机构11562 北京东方盛凡知识产权代理事务所(普通合伙);
代理人张换君
地址 116044 辽宁省大连市旅顺口区旅顺南路西段9号
入库时间 2023-06-19 12:29:04

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1. 一种IKKβ/NEMO小分子抑制剂及其在药物制备中的应用 [P] . 中国专利： CN113332265A . 2021-09-03
2. 化合物在制备小分子抑制剂或治疗癌症的药物中的应用及小分子抑制剂和治疗癌症的药物 [P] . 中国专利： CN112043705B . 2021.10.22
3. 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
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. Method for detecting and, if necessary, quantifying the activity of at least one protease inhibitor in a mixture to be analysed, and also application of the method for determining the (residual) activity of one (or more) separate (iso)type(s) of protease inhibitor(s) and application of the method for determining the total (residual) activity of a mixture, possibly after a processing process such as a process for the removal or inactivation of protease inhibitor(s). [P] . NL9301134A . 1995-01-16

机译：检测并在必要时定量待分析混合物中至少一种蛋白酶抑制剂活性的方法，以及该方法在确定一种（或多种）单独（同）型（残余）活性（残留）活性中的应用（一种或多种）蛋白酶抑制剂和确定混合物的总（残余）活性的方法的应用，可能在诸如蛋白酶抑制剂的去除或失活过程等加工过程之后。