公开(公告)号：EP2233467A1

公开(公告)日：2010-09-29

申请号：EP08858616.9

申请日：2008-12-11

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： NAN, Fajun ,  LI, Jia ,  DING, Jian ,  LIU, Gang ,  XIE, Chuanming ,  MIAO, Zehong ,  TAI, Wanyi

IPC分类号： C07C237/16 ,  C07C233/05 ,  C07C233/09 ,  C07C233/18 ,  C07C233/20 ,  A61K31/16 ,  A61P35/00

CPC分类号： C07C237/22 ,  C07C247/12 ,  C07C271/22 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/74 ,  C07D209/14 ,  C07D209/20 ,  C07D233/54 ,  C07D307/24 ,  C07D307/94

摘要： The present invention relates to filed of pharmaceutical chemistry. Disclosed are a series of α-amino-N-substituted amide compounds having a structure of the following formula, the pharmaceutically acceptable salts thereof, and the pharmaceutical composition comprising the same. The α-amino-N-substituted amide compounds or the pharmaceutically acceptable salts thereof according to the present invention have anti-tumor and/or anti-cancer activities in vivo and in vitro, can effectively depress the growth of various tumor cells and/or cancer cells, and thus can be used in preparing drugs for treating tumors and/or cancers.

公开(公告)号：EP1626050B1

公开(公告)日：2009-12-02

申请号：EP04730460.5

申请日：2004-04-30

申请人： East China University of Science and Technology ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Dalian University of Technology

发明人： QIAN, Xuhong ,  LI, Yonggang ,  XU, Yufang ,  DING, Jian ,  LIN, Liping ,  MIAO, Zehong ,  ZHU, Hong ,  QU, Baoyuan

IPC分类号： C07D495/06 ,  C07D513/06 ,  C07D221/14 ,  A61K31/473 ,  A61K31/4743 ,  A61K31/4745 ,  A61P35/00

CPC分类号： C07D495/06 ,  C07D221/14 ,  C07D405/12 ,  C07D513/06 ,  C09B57/08 ,  C09B69/102 ,  C09B69/109

摘要： The present invention relates to sulfur-containing naphthoylimide derivatives, the preparation and the use thereof. By expanding the conjugate plane of the naphthoylimide with condensed 5- or 6-member aromatic heterocyclic ring and / or introducing a sulfur atom, the antineoplastic activity of the compounds is improved. For inhibition of the proliferation of tumor-cells from different origins, such as lung cancer, carcinoma ventriculi, liver cancer and leucaemia in human beings, the compounds show remarkable effects with clear quantity-effect relationships.

摘要翻译： 含硫萘酰亚胺衍生物及其制备和用途本发明涉及含硫萘酰亚胺衍生物及其制备和用途。 通过用稠合的5-或6-元芳香杂环扩展萘甲酰亚胺的共轭面和/或引入硫原子，可以改善化合物的抗肿瘤活性。 为了抑制来自不同来源的肿瘤细胞的增殖，例如人类的肺癌，胃腔，肝癌和白血病，所述化合物显示出显着的效果，具有明确的量效关系。