公示专栏

关于浙江大学6项专利转让的公示

发布者:郭晓洁发布时间:2020-08-25浏览次数:122

浙江大学6项专利拟转让,现将相关信息予以公示。

[1]专利名称:多氟取代芳联杂环类衍生物、含其的药物组合物及其应用

专利号:ZL201710053576.8

专利简介:本发明公开了一种多氟取代芳联杂环类衍生物,具有通式I或通式I’所示的结构,其中R1R2中至少有一个氟原子;RcRdReRf中至少两个取代基为氟原子;以及其光学异构体;或其药学上可接受的盐或溶剂合物;或其光学异构体药学上可接受的盐或溶剂合物。本发明同时公开了含有上述多氟取代芳联杂环类衍生物的组合物以及其在制备抗肿瘤药物中的应用。本发明发明人通过多次实验证实,本发明化合物对Akt1有显著的抑制作用,对人卵巢癌细胞株、结肠癌细胞株、前列脲癌细胞株等肿瘤细胞株显示出强效的增殖抑制活性。因此,本发明化合物可作为Akt抑制剂应用于治疗人或动物细胞增殖性相关的实体瘤或血癌的药物中。

 

[2]专利名称:一种多氟取代芳联杂环类化合物的晶型、制备方法和应用

专利号:ZL201810756914.9

专利简介: 本发明公开了一种结构式I所示的多氟取代芳联杂环类化合物的晶型A,其X射线粉末衍射谱图具有衍射角2θ为4.3°±0.2°,8.6°±0.2°,11.4°±0.2°,13.1°±0.2°,15.0°±0.2°,17.2°±0.2°,19.8°±0.2°,21.9°±0.2°的特征峰。本发明同时公开了上述晶型A的制备方法和应用。本发明得到的晶型A的热力学稳定性、对光照的稳定性、对高湿度的稳定性以及长期稳定性均较好。且制备方法简单。

 

[3]专利名称:一种Akt抑制剂中间体SM1及其制备方法

专利号:201811375174.0

专利简介:本发明公开了一种Akt抑制剂中间体SM1及其制备方法,其采用化合物IM1与对甲苯磺酸反应得到。所述化合物IM1由下述方法制备得到:(1)化合物4和化合物9在吡咯烷催化剂和苯甲酸作用下反应,反应结束后加入三氟醋酸,反应结束后,加入碱,萃取得到化合物10的溶液;(2)将化合物10的溶液与三氟醋酸、三乙基硅烷反应,反应结束后,加入碱,萃取得到中间体的溶液,该中间体在碱作用下与Boc酸酐反应,得到化合物11(3)化合物11在还原剂作用下,得到化合物IM1;本发明提供的中间体SM1为固体,便于称量、便于保存,容易精制,克服了现有技术中的IM1是液体、难以精制的缺点,在生产上易于建立SM1的质量控制标准。

 

[4]专利名称:一种多氟取代芳联杂环类化合物的制备工艺

专利号:201811375437.8

专利简介:本发明公开了一种多氟取代芳联杂环类化合物的制备工艺,包括:采用叔丁基(3S,4S)3氨基4(3,4二氟苯基)哌啶1羧酸酯对甲苯磺酸盐为原料,经游离,再与24(1甲基1H吡唑5)苯甲酸进行缩合反应,再脱保护基,最终与L苹果酸成盐,得到4(1甲基1H吡唑)N((3S,4S)4(3,4二氟苯基)哌啶3)2氟苯甲酰胺L苹果酸盐。本发明采用的原料SM1为固体,稳定性更高,便于称量、便于保存,克服了现有技术中的IM1易成液体、难以精制的缺点,在生产上易于建立SM1的质量控制标准,原料商可以提供纯品的SM1;同时,采用原料SM1其本身手性纯度较高,从源头上保证了最终产品的纯度和整体收率。

 

[5]专利名称:POLYFLUORO-SUBSTITUTED AROMATIC HETEROCYCLIC COMPOUND DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND APPLICATIONS THEREOF                      

专利号:EP3575291A4

专利简介:A polyfluoro-substituted aromatic heterocyclic compound derivative having the structure as represented by formula I or formula I', where at least one of R1 and R2 is a fluorine atom, and at least two substituents of Rc, Rd, Re, and Rf are fluorine atoms; and an optical isomer of the derivative, or a pharmaceutically acceptable salt or solvate of same, or a pharmaceutically acceptable salt or solvate of the optical isomer of same. A composition containing the polyfluoro-substituted aromatic heterocyclic compound derivative and applications of the composition in preparing an anti-tumor medicament. The compound provides significant inhibitory effects with respect to Akt1 and demonstrates strong proliferation inhibitory activity with respect to tumor cell lines such as an ovarian cancer cell line, a colon cancer cell line, and a prostate cancer cell line. Therefore, the compound is applicable as an Akt inhibitor in the medicament for treating a cell proliferation-related solid tumor or blood cancer in the human or animal body.

 

[6]专利名称:POLYFLUORO-SUBSTITUTED AROMATIC HETEROCYCLIC COMPOUND DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND APPLICATIONS THEREOF                      

专利号:US16480599

专利简介:A polyfluoro-substituted aromatic heterocyclic compound derivative having the structure as represented by formula I or formula I', where at least one of R1 and R2 is a fluorine atom, and at least two substituents of Rc, Rd, Re, and Rf are fluorine atoms; and an optical isomer of the derivative, or a pharmaceutically acceptable salt or solvate of same, or a pharmaceutically acceptable salt or solvate of the optical isomer of same. A composition containing the polyfluoro-substituted aromatic heterocyclic compound derivative and applications of the composition in preparing an anti-tumor medicament. The compound provides significant inhibitory effects with respect to Akt1 and demonstrates strong proliferation inhibitory activity with respect to tumor cell lines such as an ovarian cancer cell line, a colon cancer cell line, and a prostate cancer cell line. Therefore, the compound is applicable as an Akt inhibitor in the medicament for treating a cell proliferation-related solid tumor or blood cancer in the human or animal body.

 

转化方式:转让

定价方式:协议定价

转化价格:1亿元

 

公示期自2020825日至202098日。如有异议,请在公示期内向科学技术研究院提交异议书及有关证据。

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