Disclosed are substituted-benzodiazepine-2,5-dione derivatives represented by structural formula depicted herein, wherein the variables are as defined in the specification. These compounds are suitable for treating a disease or disorder selected from hyperproliferative disorder, autoimmune disorder, chronic inflammatory condition, or atherosclerosis, including conditions such as graft-versus-host disease, psoriasis, rheumatoid arthritis, cancer, Sjogren&rsquos syndrome, myasthenia gravis, asthma, systemic lupus erythematosus, multiple sclerosis, celiac sprue, idiopathic thrombocytopenia purpura, scleroderma, Crohn&rsquos Disease, inflammatory bowel disease, and ulcerative colitis.