公开(公告)号：US09409845B2

公开(公告)日：2016-08-09

申请号：US14723785

申请日：2015-05-28

申请人： PHARMAXYN LABORATORIES LTD.

发明人： Guizhen Ao ,  Jihua Nie ,  Huanqiu Li ,  Lingxuan Mo ,  Lei Chen ,  Heng Song ,  Shaohua Chen

IPC分类号： C07C45/00 ,  A61K31/00 ,  C07C49/753 ,  C07C317/24 ,  C07C225/22 ,  C07C45/45

CPC分类号： C07C49/753 ,  C07C45/45 ,  C07C225/22 ,  C07C317/24 ,  C07C2601/14

摘要： The present invention discloses a α-(3,5-dimethoxybenzylidene)-α′-hydrocarbyl methylene cyclic ketone with the following formula: wherein R is aryl or alkyl, its preparation method is: the cyclic ketone blended with morpholine are subjected to azeotropic dehydration to give enamine, the enamine is condensed with 3,5-dimethoxybenzaldehyde and then condensed with alkyl or aryl formaldehyde under acidic or basic conditions to give the product, the present invention further discloses an antitumor agent comprising α-(3,5-dimethoxybenzylidene)-α′-hydrocarbyl methylene cyclic ketone or medically acceptable salts and pharmaceutically acceptable carriers thereof. Through the above, the present invention providesα-(3,5-dimethoxybenzylidene)-α′-hydrocarbyl methylene cyclic ketone and preparation method thereof, the said compound is a high activity antitumor agent obtained by piecing and modifying the formulas of natural anti-tumor active ingredient resveratrol and curcumin, which has a good inhibitory effect on epidermal growth factor receptor.

摘要翻译： 本发明公开了具有下式的α-（3,5-二甲氧基亚苄基）-α'-烃基亚甲基环酮，其中R是芳基或烷基，其制备方法是：与吗啉共混的环酮进行共沸脱水 给予烯胺，烯胺与3,5-二甲氧基苯甲醛缩合，然后在酸性或碱性条件下与烷基或芳基甲醛缩合得到产物，本发明还公开了一种抗肿瘤剂，其包含α-（3,5-二甲氧基亚苄基） -α'-烃基亚甲基环酮或其医药上可接受的盐和药学上可接受的载体。 通过上述，本发明提供α-（3,5-二甲氧基亚苄基）-α'-烃基亚甲基环酮及其制备方法，所述化合物是通过接头和改性天然抗肿瘤剂的方法得到的高活性抗肿瘤剂 活性成分白藜芦醇和姜黄素，对表皮生长因子受体具有良好的抑制作用。