Method for treating obesity
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.