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公开(公告)号：EP3954682A1
公开(公告)日：2022-02-16
申请号：EP19924592.9
申请日：2019-04-09
发明人： CHANG, Junbiao , DU, Jinfa , ZHU, Kaikai , WANG, Kai , LI, Jianyong , ZHANG, Chunxia , YI, Dongxu
IPC分类号： C07D403/04 , A61P35/00
摘要： The present invention discloses a new anti-lung cancer medicine, and specifically relates to a 2-(2,4,5-substituted phenylamino)pyrimidine derivative I and a crystal form B thereof, belonging to the field of medicinal chemistry. The derivative has the following structure: (1). According to the results of pharmacokinetic and pharmacodynamic research, doxitinib significantly reduces the production of a metabolic product N-Me with a greater toxicity, and maintains or improves the efficacy in comparison to osimertinib. Doxitinib is expected to be developed as a safer and more effective novel medicine for the treatment of non-small cell lung cancer with EGFR mutation in comparison to osimertinib.
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2.发明公开
公开(公告)号：EP3939984A1
公开(公告)日：2022-01-19
申请号：EP19920547.7
申请日：2019-04-18
发明人： CHANG, Junbiao , DU, Jinfa , YI, Dongxu
IPC分类号： C07H19/06 , A61K31/7068 , A61K31/7076 , A61P31/18
摘要： Disclosed is a crystal form A of a 2'-fluoro-4'-substituted nucleoside analog I, wherein same falls within the field of pharmaceutical chemistry. The crystal form A has the following structure: (I). The CuKα-XRPD pattern of the crystal form A of the compound I is as shown in figure 2 , wherein the crystal form A has a good stability and can easily be uniformly mixed with auxiliary materials. The crystal form A of the compound I is mixed with the auxiliary materials, so that the uniformity thereof in tablets is increased, and same is conducive to controlling the drug quality and ensuring the drug efficacy. The crystal form A is used for preparing anti-HBV or anti-HCV or anti-HIV drugs or anti-tumor drugs.
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