Compositions and therapeutic methods involving isoflavones and analogues thereof

Abstract

Isoflavone compounds are described and recommended as therapeutic agents. Exemplified and preferred compounds are (a). Indications show compounds have good competitive binding to estrogen receptors. This is exemplified.

1 - 34 . (canceled)  
   
   
       35 . A method for the treatment of at least one inflammatory disease, which comprises administering to a subject a therapeutically effective amount of one of more compounds having the formula:  
     
       
         
         
             
             
         
       
     
     in which 
 R 1  and R 2  are independently hydrogen, hydroxy, OR 9 , OC(O)R 10 , alkyl, or halo,  
 T is chosen from hydrogen, alkyl and halo,  
 W is chosen from hydrogen, halo and alkyl,  
 R 6  is hydrogen,  
 R 9  is chosen from alkyl, haloalkyl, aryl, arylalkyl, C(O)R 11  where R 11  is hydrogen, alkyl, aryl, arylalkyl or an amino acid, or Si(R 13 ) 3  where each R 13  is independently hydrogen, alkyl or aryl,  
 R 10  is hydrogen, alkyl, haloalkyl, amino, aryl, arylalkyl, an amino acid, alkylamino or dialkylamino,  
 X is O,  
 R 14 , R 15  and R 16  are independently chosen from hydrogen, hydroxy, OR 9 , OC(O)R 10 , OS(O)R 10 , CHO, C(O)R 10 , COOH, CO 2 R 10 , CONR 3 R 4 , alkyl, haloalkyl, aryl, arylalkyl, thio, alkylthio, amino, alkylamino, dialkylamino, nitro or halo,  
 wherein  
 R 3  is chosen from hydrogen, alkyl, aryl, arylalkyl, an amino acid, C(O)R 1  where R 11  is as previously defined, or CO 2 R 12  where R 12  is hydrogen, alkyl, haloalkyl, aryl or arylalkyl,  
 R 4  is chosen from hydrogen, alkyl or aryl,  
 or R 3  and R 4  taken together with the nitrogen to which they are attached comprise pyrrolidinyl or piperidinyl,  
 with the proviso that  
 when  
 R 1  is hydroxy, or OC(O)R A  where R A  is alkyl or an amino acid, and  
 R 2  is hydrogen, hydroxy, OR B  where R B  is an amino acid or C(O)R A  where R A  is as previously defined, and  
 W is hydrogen, and  
 R 15  is hydrogen, and  
 R 16  is hydrogen, then  
 R 14  is not hydrogen, hydroxy, acetoxy, alkoxy, or alkyl.  
 
   
   
       36 . The method of  claim 35 , wherein halo is selected from chloro and bromo.  
   
   
       37 . The method of  claim 35 , wherein alkyl is methyl.  
   
   
       38 . The method of  claim 35 , wherein R 15  and R 16  are hydrogen.  
   
   
       39 . The method of  claim 38 , wherein R 14  is hydroxy.  
   
   
       40 . The method of  claim 35 , wherein at least one of said one or more compounds is selected from:  
     
       
         
         
             
             
         
       
     
   
   
       41 . The method of  claim 35 , wherein said inflammatory disease is chosen from inflammatory bowel disease, ulcerative colitis, and Crohn's disease.  
   
   
       42 . The method of  claim 35 , wherein said one or more compounds are formulated for administration by a route selected from oral, rectal, optical, buccal, parenteral and transdermal administration.  
   
   
       43 . The method of  claim 42 , wherein said formulation for oral administration comprises a drink or food-stuff comprising said one or more compounds.  
   
   
       44 . The method of  claim 42 , wherein said formulation further comprises one or more substances selected from pharmaceutical carriers and excipients.  
   
   
       45 . The method of  claim 35 , further comprising administering a therapeutically effective amount of vitamin E to said subject.