Compositions And Methods Relating To Novel Compounds And Targets Thereof

Abstract

The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like.

1 . A compound described by the following formula: 
       
         
           
           
               
               
           
         
         wherein X is selected from the group consisting of halogen, alkyl, and an alkyl group substituted with at least one halogen or a heteroaromatic or aromatic moiety; and 
         R 2  is selected from the group consisting of hydrogen and a linear or branched alkyl; 
         including both R and S enantiomeric forms and racemic mixtures thereof; 
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         2 . The compound of  claim 1 , wherein R 2  is hydrogen or methyl. 
     
     
         3 . The compound of  claim 1 , wherein X is bromo, iodo, methyl, ethyl, isopropyl, or an alkyl group substituted with at least one halogen or a heteroaromatic or aromatic moiety. 
     
     
         4 . The compound of  claim 1 , wherein X is bromo, iodo, trifluoromethyl, or an alkyl group substituted with phenyl. 
     
     
         5 . The compound of  claim 2 , wherein X is bromo, iodo, trifluoromethyl, or an alkyl group substituted with phenyl. 
     
     
         6 . The compound of  claim 1 , wherein said compound is described by: 
       
         
           
           
               
               
           
         
         including both R and S enantiomeric forms and racemic mixtures thereof, or a pharmaceutically acceptable salt thereof. 
       
     
     
         7 . The compound of  claim 1 , wherein the compound is selected from the group consisting of: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         including R and S enantiomeric forms and racemic mixtures thereof; 
         and pharmaceutically acceptable salts thereof. 
       
     
     
         8 . A pharmaceutical composition comprising a compound of  claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. 
     
     
         9 . A method of treating a disorder selected from the group consisting of an immune disorder, hyperproliferative disorder, and chronic inflammatory disease, comprising administering an effective amount of a compound of  claim 1  or a pharmaceutically acceptable salt thereof, to a subject in need thereof. 
     
     
         10 . The method of  claim 9 , wherein said immune disorder is graft versus host disease, rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, Crohn's disease, Celia Sprue, or idiopathic thrombocytopenic thrombotic purpura. 
     
     
         11 . The method of  claim 9 , wherein said disorder is cancer. 
     
     
         12 . The method of  claim 11 , wherein said cancer is a tumor, a neoplasm, a lymphoma, or a leukemia. 
     
     
         13 . The method of  claim 9 , wherein said disorder is a chronic inflammatory disease. 
     
     
         14 . The method of  claim 13 , wherein said chronic inflammatory disease is asthma or inflammatory bowel disease. 
     
     
         15 . The method of  claim 9 , wherein said disorder is psoriasis. 
     
     
         16 . The method of  claim 9 , wherein the subject is a human.