申请人:Kabushiki Kaisha Yakult Honsha
公开号:EP1044971A1
公开(公告)日:2000-10-18
Taxane derivatives represented by general formula (1) or salts thereof and drugs containing the same as the active ingredient wherein A1 represents (a) (wherein R1 represents H or optionally substituted alkyl) or (b) (wherein R2 represents amino, mono- or dialkylamino, piperidino, pyrrolidino or morpholino); X represents H, alkoxycarbonyl or benzoyl; Y represents H or trialkylsilyl; A2 represents furyl, alkylfuryl, alkyl or fluorophenyl; Ac represents acetyl; and Bz represents benzoyl. These compounds are excellent in solubility in water and antitumor activity.
由通式(1)代表的紫杉烷衍生物或其盐类以及含有通式(1)作为活性成分的药物 其中 A1 代表(a)(其中 R1 代表 H 或任选取代的烷基)或(b)(其中 R2 代表氨基、单烷基或二烷基氨基、哌啶基、吡咯烷基或吗啉基);X 代表 H、烷氧羰基或苯甲酰基;Y 代表 H 或三烷基硅基;A2 代表呋喃基、烷基呋喃基、烷基或氟苯基;Ac 代表乙酰基;Bz 代表苯甲酰基。这些化合物具有优异的水溶性和抗肿瘤活性。