公开(公告)号：US20100056517A1

公开(公告)日：2010-03-04

申请号：US12513835

申请日：2007-11-15

申请人： Jonathan Bayldon Baell ,  Guillaume Laurent Lessene ,  Brad Edmund Sleebs ,  Wayne J. Fairbrother ,  John A. Flygare ,  Michael F.T. Koeler

发明人： Jonathan Bayldon Baell ,  Guillaume Laurent Lessene ,  Brad Edmund Sleebs ,  Wayne J. Fairbrother ,  John A. Flygare ,  Michael F.T. Koeler

IPC分类号： A61K31/5377 ,  A61K31/496 ,  C07D413/14 ,  C07D239/86 ,  A61P35/00

CPC分类号： C07D239/94

摘要： The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins: wherein A1, A2, B1, B2, B3, X, Z, R1, R2, R3 and t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.

摘要翻译： 本发明一般涉及模拟某些肽和蛋白质的生物学活性的小分子，含有它们的组合物及其用途。 特别地，本发明涉及模拟仅含BH3蛋白的生物学活性的通式（I）的化合物，并能够结合并中和原生存Bcl-2蛋白：其中A1，A2，B1，B2， B3，X，Z，R1，R2，R3和t如本文所述。 本发明还涉及制备模仿肽和蛋白质的一部分的苯磺酰胺化合物的方法，以及这些化合物在调节细胞死亡中的用途以及治疗和/或预防与细胞死亡调节相关的疾病或病症 。