Cytotoxic bicyclo (7.3.1)-tridec-4-ene-2,6-diyne compounds and process for the preparation thereof
申请人:Bristol-Myers Squibb Company
公开号:EP0538898A2
公开(公告)日:1993-04-28
The present invention relates to a novel and efficient process for the preparation of 8-hydroxy-bicycloÄ7.3.1Ütridec-4-ene-2,6-diyne ring system which is part of the aglycone of esperemicin and to novel cytotoxic antitumor agents having said bicyclic ring system. The present invention also provides a method for treating mammalian malignant tumors by administering to an animal in need of such treatment an antitumor effective amount of a compound of the present invention.
本发明涉及一种制备8-羟基-双环Ä7.3.1Ütridec-4-烯-2,6-二炔环系统的新颖而有效的工艺,该环系统是依斯瑞米星(esperemicin)苷元的一部分,本发明还涉及具有所述双环系统的新型细胞毒性抗肿瘤药物。本发明还提供了一种治疗哺乳动物恶性肿瘤的方法,即向需要治疗的动物施用抗肿瘤有效量的本发明化合物。