Benzofuran compounds, compositions, kits and/or methods thereof

Abstract

Benzofuran compound, composition thereof, kit thereof, and/or method thereof. A benzofuran-2-carboxamide moiety may be N-arylated and/or N-alkylated, and the resulting benzofuran compound may be a sigma receptor ligand that binds to, e.g., a σ1 receptor and/or a σ2 receptor with relatively high affinity and/or selectivity. For example, the benzofuran compound may be 5,6-dimethoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, 3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamide, or 6-methoxy-3-methyl-N-phenyl-N-(3-(piperidin-1-yl) propyl)benzofuran-2-carboxamide. The composition may include the benzofuran compound and a pharmaceutically acceptable carrier.

1 . A composition comprising:
 a pharmaceutically acceptable carrier; and   a compound of Formula I:   
       
         
           
           
               
               
           
         
         wherein R 1  and R 2  are independently selected from C 1-20 -alkyl, C 1-20 -alkoxy, and hydrogen, R 3  is independently selected from (piperidin-1yl)C 3-20 -alkyl, and R 4  is independently selected from C 1-20 -alkyl, an organic functional group, and hydrogen. 
       
     
     
         2 . The composition of  claim 1 , further including a salt of the compound of Formula I. 
     
     
         3 . The composition of  claim 1 , wherein R 1  and R 2  are in one of ortho substitution, meta substitution, and para substitution. 
     
     
         2 . The composition of  claim 1 , wherein R 1  and R 2  are independently selected from C 1-2 -alkyl, C 1-2 -alkoxy, and hydrogen, R 3  is independently selected from (piperidin-1yl)C 3-5 -alkyl, and R 4  is independently selected from C 1-2 -alkyl, a formyl group, a carboxyl group, and hydrogen. 
     
     
         4 . The composition of  claim 1 , wherein the pharmaceutically acceptable carrier is in the form of an emulsion, a paste, a cream, a lotion, a gel, jelly, ointment, oil, aerosol, powder, and/or solvent. 
     
     
         5 . The composition of  claim 1 , wherein the pharmaceutically acceptable carrier is in the form of a liposome, a micelle, a peptide, a synthetic polymer, and/or a natural polymer. 
     
     
         10 . The composition of  claim 1 , wherein the pharmaceutically acceptable carrier is in the form of a nanomaterial. 
     
     
         11 . The composition of  claim 1 , wherein the compound of Formula I is one or more of linked with the pharmaceutically acceptable carrier and physically sequestered by the pharmaceutically acceptable carrier. 
     
     
         12 . The composition of  claim 1 , wherein one or more of the compound of Formula I and the pharmaceutically acceptable carrier are functionalized with a ligand for a specific target. 
     
     
         13 . The composition of  claim 1 , further including at least one other therapeutic compound including one or more of a neurological disease drug and a cancer drug. 
     
     
         14 . A kit comprising:
 a container; and   a composition including a pharmaceutically acceptable carrier and a compound of Formula I:   
       
         
           
           
               
               
           
         
         wherein R 1  and R 2  are independently selected from C 1-20 -alkyl, C 1-20 -alkoxy, and hydrogen, R 3  is independently selected from (piperidin-1yl)C 3-20 -alkyl, and R 4  is independently selected from C 1-20 -alkyl, an organic functional group, and hydrogen.