公开(公告)号：US06495522B1

公开(公告)日：2002-12-17

申请号：US09649810

申请日：2000-08-28

申请人： Yan Wang ,  Sui Xiong Cai ,  Eckard Weber ,  Gordon B. Mills ,  Douglas R. Green ,  Lufeng Guan

发明人： Yan Wang ,  Sui Xiong Cai ,  Eckard Weber ,  Gordon B. Mills ,  Douglas R. Green ,  Lufeng Guan

IPC分类号： A61K31195

CPC分类号： C07C271/28 ,  C07C271/12 ,  C07C271/22

摘要： The present invention is directed to novel substituted &agr;-hydroxy acid thereof, represented by the general Formula I: where R1-R5, X and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

摘要翻译： 本发明涉及由通式I表示的新型取代的α-羟基酸：其中R1-R5，X和Z如本文所定义。 本发明还涉及发现具有式I的化合物是胱天蛋白酶的有效抑制剂和凋亡性细胞死亡。 因此，本发明的抑制剂可以在发生细胞，组织或整个器官的损失的各种临床病症中阻滞或阻断细胞死亡。