公开(公告)号：US20070179143A1

公开(公告)日：2007-08-02

申请号：US10562615

申请日：2004-06-23

申请人： Myung-Hwa Kim ,  Kwnagwoo Chun ,  Jae-Won Chol ,  Bo-Young Joe ,  Sang-Woo Park ,  Kwang Kim ,  Byung-Kyu Oh ,  Jong-Hee Chol

发明人： Myung-Hwa Kim ,  Kwnagwoo Chun ,  Jae-Won Chol ,  Bo-Young Joe ,  Sang-Woo Park ,  Kwang Kim ,  Byung-Kyu Oh ,  Jong-Hee Chol

IPC分类号： A61K31/50 ,  A61K31/4965

CPC分类号： C07C323/41 ,  C07C381/00 ,  C07C2601/08 ,  C07C2603/34 ,  C07D213/81 ,  C07D213/82 ,  C07D307/68 ,  C07D333/38

摘要： The present invention relates to tricyclic derivatives or pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. More precisely, the present invention relates to tricyclic derivatives as colchicine derivatives, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. Tricyclic derivatives of the present invention show very powerful cytotoxicity to cancer cell lines but were much less toxic than colchicine or taxol, confirmed through animal toxicity test. Tricyclic derivatives of the invention also decrease the volume and weight of a tumor and have a strong angiogenesis inhibiting activity in HUVEC cells. Thus, tricyclic derivatives of the present invention can effectively be used as an anticancer agent, anti-proliferation agent and an angiogenesis inhibitor.

摘要翻译： 本发明涉及三环衍生物或其药学上可接受的盐，它们的制剂和含有它们的药物组合物。 更准确地说，本发明涉及作为秋水仙素衍生物的三环衍生物，其药学上可接受的盐，其制备物和含有它们的药物组合物。 本发明的三环衍生物对癌细胞系显示出非常强大的细胞毒性，但是通过动物毒性试验证实，它比秋水仙素或紫杉醇毒性低得多。 本发明的三环衍生物还降低了肿瘤的体积和重量，并且在HUVEC细胞中具有强的血管生成抑制活性。 因此，本发明的三环衍生物可以有效地用作抗癌剂，抗增生剂和血管发生抑制剂。