Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.本發明揭示抑制抗細胞凋亡Bcl-xL蛋白之活性的化合物、含有該等化合物之組合物及治療其中表現抗細胞凋亡Bcl-xL蛋白之疾病的方法。