公开(公告)号：US09499530B2

公开(公告)日：2016-11-22

申请号：US14234326

申请日：2012-07-21

申请人： Shulong Wang ,  Jian Cai ,  Qiufu Ge ,  Dianwu Guo ,  Lan Yang ,  Binnan Huang ,  Zhenhua Liu ,  Zhonghua Peng ,  Ximing Shen ,  Feiyu Feng

发明人： Shulong Wang ,  Jian Cai ,  Qiufu Ge ,  Dianwu Guo ,  Lan Yang ,  Binnan Huang ,  Zhenhua Liu ,  Zhonghua Peng ,  Ximing Shen ,  Feiyu Feng

IPC分类号： C07D417/04 ,  C07D405/14 ,  C07D405/04 ,  C07D403/14

CPC分类号： C07D417/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14

摘要： A class of quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof with novel structures is provided; meanwhile, a pharmaceutical composition comprising a pharmaceutically effective amount of said quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof, and pharmaceutically acceptable excipients or additives is also provided. By modifying and transforming the quinazoline and screening of the transformed compounds on the activity of tyrosine kinase inhibition, most of the compounds have been found to possess inhibitory activity against one or several of EGFR, VEGFR-2, c-erbB-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70 and fyn kinases. The present invention has the advantages of reasonable design, broad source of and easy access to the raw materials, simple and easy operation of the preparation methods, mild reaction conditions, high yield of the products and being beneficial for industrial-scale production.

摘要翻译： 提供了一类具有新颖结构的喹唑啉衍生物或其药学上可接受的盐或溶剂合物; 同时，还提供了包含药学上有效量的所述喹唑啉衍生物或其药学上可接受的盐或溶剂合物以及药学上可接受的赋形剂或添加剂的药物组合物。 通过修饰和转化喹唑啉和筛选转化的化合物对酪氨酸激酶抑制的活性，已经发现大多数化合物具有对EGFR，VEGFR-2，c-erbB-2，c- erbB-4，c-met，tie-2，PDGFR，c-src，lck，Zap70和fyn激酶。 本发明设计合理，原料来源广泛，易于获得原料，操作简便，制备方法简单，反应条件温和，产品收率高，有利于工业规模生产。

公开(公告)号：US20150080392A1

公开(公告)日：2015-03-19

申请号：US14234326

申请日：2012-07-21

申请人： Shulong Wang ,  Jian Cai ,  Qiufu Ge ,  Dianwu Guo ,  Lan Yang ,  Binnan Huang ,  Zhenhua Liu ,  Zhonghua Peng ,  Ximing Shen ,  Feiyu Feng

发明人： Shulong Wang ,  Jian Cai ,  Qiufu Ge ,  Dianwu Guo ,  Lan Yang ,  Binnan Huang ,  Zhenhua Liu ,  Zhonghua Peng ,  Ximing Shen ,  Feiyu Feng

IPC分类号： C07D417/04 ,  C07D403/14 ,  C07D405/04

CPC分类号： C07D417/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14

摘要： A class of quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof with novel structures is provided; meanwhile, a pharmaceutical composition comprising a pharmaceutically effective amount of said quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof, and pharmaceutically acceptable excipients or additives is also provided. By modifying and transforming the quinazoline and screening of the transformed compounds on the activity of tyrosine kinase inhibition, most of the compounds have been found to possess inhibitory activity against one or several of EGFR, VEGFR-2, c-erbB-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70 and fyn kinases. The present invention has the advantages of reasonable design, broad source of and easy access to the raw materials, simple and easy operation of the preparation methods, mild reaction conditions, high yield of the products and being beneficial for industrial-scale production.

摘要翻译： 提供了一类具有新颖结构的喹唑啉衍生物或其药学上可接受的盐或溶剂合物; 同时，还提供了包含药学上有效量的所述喹唑啉衍生物或其药学上可接受的盐或溶剂合物以及药学上可接受的赋形剂或添加剂的药物组合物。 通过修饰和转化喹唑啉和筛选转化的化合物对酪氨酸激酶抑制的活性，已经发现大多数化合物具有对EGFR，VEGFR-2，c-erbB-2，c- erbB-4，c-met，tie-2，PDGFR，c-src，lck，Zap70和fyn激酶。 本发明设计合理，原料来源广泛，易于获得原料，操作简便，制备方法简单，反应条件温和，产品收率高，有利于工业规模生产。