Method for treating obesity

Abstract

The present invention relates, in general, to obesity, and, in particular, to a method of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight-loss promoting anticonvulsant either alone or in combination with bupropion or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.

1 - 17 . (canceled)  
     
     
         18 . A method of treating obesity in a mammal comprising administering to a mammal in need of such treatment a metabolite of bupropion, and at least one weight-loss promoting anticonvulsant wherein said anticonvulsant is of the formula (I):  
       
         
           
           
               
               
           
         
       
       wherein X is CH 2  or oxygen, 
 R 1  is hydrogen or alkyl,  
 R 2 , R 3 , R 4  and R 5  are independently hydrogen or lower alkyl, and when X is CH 2 , R 4  and R 5  can be alkene groups joined to form a benzene ring and when X is oxygen, R 2  and R 3  and/or R 4  and R 5  together can be a methylenedioxy group of the following formula (II):  
                     
 wherein  
 R 6  and R 7  are the same or different and are hydrogen, lower alkyl or are alkyl and are joined to form a cyclopentyl or cyclohexyl ring.  
 
     
     
         19 . The method of  claim 18  wherein R 1  is hydrogen or a C 1 -C 4  alkyl, straight and branched chain, and R 2 , R 3 , R 4 , R 5 , R 6  and R 7  are a C 1 -C 3  alkyl, straight or branched chain.  
     
     
         20 . The method of  claim 18 , wherein said anticonvulsant is topiramate.  
     
     
         21 . A method of treating obesity in a mammal comprising administering to a mammal in need of such treatment a metabolite of bupropion, and at least one weight-loss promoting anticonvulsant wherein said anticonvulsant is of formula (III):  
       
         
           
           
               
               
           
         
       
       wherein R 1  is hydrogen or a halogen atom, R 2  and R 3  are the same or different and are each hydrogen or an alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atom, provided that the group —CH 2 SO 2 NR 2 R 3  is bonded to the carbon atom of either of X and Y, or an alkali metal salt thereof.  
     
     
         22 . The method of  claim 20  wherein said anticonvulsant is zonisamide.  
     
     
         23 . The method of any one of  claim 18  or  claim 21  wherein said anticonvulsant and said metabolite of bupropion are administered separately.  
     
     
         24 . The method of any one of  claim 18  or  claim 21  wherein said anticonvulsant and said metabolite of bupropion are administered concurrently.  
     
     
         25 . A method of reducing the risk of hypertension, diabetes or dyslipidaemia in a mammal comprising administering to a mammal in need of such reduction a metabolite of bupropion, and at least one weight-loss promoting anticonvulsant according to formula (I) or formula (III) in amounts such that said reduction is effected, where formula (I) is:  
       
         
           
           
               
               
           
         
       
       wherein X is CH 2  or oxygen, 
 R 1  is hydrogen or alkyl,  
 R 2 , R 3 , R 4  and R 5  are independently hydrogen or lower alkyl, and when X is CH 2 , R 4  and R 5  can be alkene groups joined to form a benzene ring and when X is oxygen, R 2  and R 3  and/or R 4  and R 5  together can be a methylenedioxy group of the following formula (II):  
                     
 wherein  
 R 6  and R 7  are the same or different and are hydrogen, lower alkyl or are alkyl and are joined to form a cyclopentyl or cyclohexyl ring, and wherein formula (III) is:  
                     
 wherein R 1  is hydrogen or a halogen atom, R 2  and R 3  are the same or different and are each hydrogen or an alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atom, provided that the group —CH 2 SO 2 NR 2 R 3  is bonded to the carbon atom of either of X and Y, or an alkali metal salt thereof.  
 
     
     
         26 . The method of  claim 25  wherein said at least one weight-loss promoting anticonvulsant of formula (III) is zonisamide.  
     
     
         27 . The method of  claim 25  wherein said at least one weight-loss promoting anticonvulsant of formula (I) is topiramate.  
     
     
         28 . A composition comprising a metabolite of bupropion, and at least one weight-loss promoting anticonvulsant of formula (I):  
       
         
           
           
               
               
           
         
       
       wherein X is CH 2  or oxygen, 
 R 1  is hydrogen or alkyl,  
 R 2 , R 3 , R 4  and R 5  are independently hydrogen or lower alkyl, and when X is CH 2 , R 4  and R 5  can be alkene groups joined to form a benzene ring and when X is oxygen, R 2  and R 3  and/or R 4  and R 5  together can be a methylenedioxy group of the following formula (II):  
                     
 wherein  
 R 6  and R 7  are the same or different and are hydrogen, lower alkyl or are alkyl and are joined to form a cyclopentyl or cyclohexyl ring.  
 
     
     
         29 . The composition of  claim 28  wherein said anticonvulsant is topiramate.  
     
     
         30 . A composition comprising a metabolite of bupropion, and at least one weight-loss promoting anticonvulsant of formula (III):  
       
         
           
           
               
               
           
         
         wherein R 1  is hydrogen or a halogen atom, R 2  and R 3  are the same or different and are each hydrogen or an alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atom, provided that the group —CH 2 SO 2 NR 2 R 3  is bonded to the carbon atom of either of X and Y, or an alkali metal salt thereof, in an amount sufficient to effect said treatment.  
       
     
     
         31 . The composition of  claim 30  wherein said anticonvulsant is zonisamide.  
     
     
         32 . The composition of any one  claim 28  or  claim 30  wherein said composition is in dosage unit form.  
     
     
         33 . The composition of any one  claim 28  or  claim 30  wherein said composition is in the form of a tablet or capsule.