公开(公告)号：US06548536B2

公开(公告)日：2003-04-15

申请号：US09793654

申请日：2001-02-27

申请人： Mitsunobu Hara ,  Takayuki Nakashima ,  Yutaka Kanda ,  Masami Hamano ,  Shun-ichi Ikeda ,  Yuko Uosaki ,  Yoko Takata ,  Junji Kanazawa

发明人： Mitsunobu Hara ,  Takayuki Nakashima ,  Yutaka Kanda ,  Masami Hamano ,  Shun-ichi Ikeda ,  Yuko Uosaki ,  Yoko Takata ,  Junji Kanazawa

IPC分类号： A61K3134

CPC分类号： C07D407/14 ,  A61K31/00 ,  A61K31/365 ,  C07H17/08

摘要： Agents for inducing apoptosis comprising a tetrocarcin derivative represented by the following formula (I) or a salt thereof as an active ingredient (---- represents a single bond or a double bond; j and k represent 0 or 1; R1 to R3, R7 to R10 and R14 represent a hydrogen atom, a lower alkyl group and the like; R4, R11, R12, R13 and R15 to R18 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like; R5 and R6 represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a group represented by the following formula (B) (R32 represents a formyl group and the like, R33 to R35 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like); R19 represents a hydroxyl group, a lower alkoxyl group, a lower alkanoyloxy group and the like). The agents are useful as medicaments for preventive and/or therapeutic treatment of diseases resulting from increased expression of Bcl-2 family proteins, for example, cancers, AIDS and the like.

摘要翻译： 用于诱导凋亡的药剂，其包含由下式（I）表示的四环卟啉衍生物或其盐作为活性成分（----表示单键或双键; j和k表示0或1; R 1至R 3， R 7〜R 10和R 14表示氢原子，低级烷基等; R 4，R 11，R 12，R 13，R 15〜R 18表示氢原子，羟基，低级烷基等; R 5，R 6表示 氢原子，羟基，低级烷基，下式（B）表示的基团（R32表示甲酰基等，R33〜R35表示氢原子，羟基，低级烷基， 类似）; R 19表示羟基，低级烷氧基，低级烷酰氧基等）。 这些药剂可用作预防和/或治疗由Bcl-2家族蛋白（例如癌症，AIDS等）表达增加而引起的疾病的药物。