公开(公告)号：US5747502A

公开(公告)日：1998-05-05

申请号：US851853

申请日：1992-03-16

申请人： Miyoji Hanaoka ,  Hisao Ekimoto ,  Fumiko Kobayashi ,  Yukio Irie ,  Katsutoshi Takahashi ,  Masanobu Suzuki ,  Takeshi Nakanishi ,  Osamu Kogawa ,  Keizou Ishikawa

发明人： Miyoji Hanaoka ,  Hisao Ekimoto ,  Fumiko Kobayashi ,  Yukio Irie ,  Katsutoshi Takahashi ,  Masanobu Suzuki ,  Takeshi Nakanishi ,  Osamu Kogawa ,  Keizou Ishikawa

IPC分类号： A61K31/473 ,  A61K31/44 ,  C07D471/00

CPC分类号： A61K31/473 ,  Y10S514/883 ,  Y10S514/908

摘要： The present invention relates to benzo�c!phenanthridinium derivative of the general formula A: ##STR1## wherein M and N individually represent a hydroxyl or lower alkoxy group, or M and N simultaneously represent a hydrogen atom or together form a methylenedioxy group, X.sup.- represents an acid residue or a hydrogen acid residue, and R represents a lower alkyl group, and a process for preparing such derivatives. The compounds exhibit both potent antitumor activity and platelet aggregation inhibition activity, and are expected to be useful for the treatment of tumors. The process has good reproducibility and may be effected under moderate conditions, and therefore the process is practically useful. In addition, hydrogen salts of the present compounds have an enhanced stability, which is an advantage in formulating the same into pharmaceutical preparations.

摘要翻译： 本发明涉及通式A的苯并[c]菲啶鎓衍生物：其中M和N各自表示羟基或低级烷氧基，或M和N同时代表氢原子或一起形成亚甲二氧基 基团，X-表示酸残基或氢酸残基，R表示低级烷基，以及制备该衍生物的方法。 该化合物表现出有效的抗肿瘤活性和血小板聚集抑制活性，并且预期可用于治疗肿瘤。 该方法具有良好的再现性并且可以在中等条件下进行，因此该方法实际上是有用的。 此外，本发明化合物的氢盐具有增强的稳定性，这将其配制成药物制剂是有利的。