Novel medical uses of 4,5-dihydro-1h-pyrazole derivatives having cb1- antagonistic activity

A pharmaceutical composition comprising an amount of at least one compound of formula (I), at least one prodrug thereof, at least one tautomer thereof, at least one salt thereof, or a mixture of two or more of the foregoing,

• wherein the at least one compound of formula (I) has the following structure:
• wherein
• - R and R1 independently of each other represent
• unsubstituted naphthyl, or
• phenyl, thienyl or pyridyl groups, which groups are unsubstituted or substituted with 1, 2 or 3 substituents Y, which can be the same or different, and are chosen from
• C1-3-alkyl, C1-3-alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, nitro, amino, mono (C1-2)-alkylamino, di (C1-2)-alkylamino, mono (C1-2)-alkylamido, di (C1-2)-alkylamido, (C1-3)-alkyl sulfonyl, dimethylsuIfamido, C1-3-alkoxycarbonyl, carboxyl, trifiuoromethylsulfonyl, cyano, carbamoyl, sulfamoyl and acetyl,
• - R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy,
• - Aa represents one of the groups (i), (ii), (iii), (iv) or (v)
• wherein
• - R4 and R5 independently of each other represent hydrogen or C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R4 represents acetamido, dimethylamino, 2,2,2-trifluoroethyl, phenyl, or pyridyl with the proviso that R5 represents hydrogen,
• - R6 represents hydrogen or C1-3 unbranched alkyl,
• - Bb represents sulfonyl or carbonyl,
• - R3 represents a benzyl, phenyl, thienyl or pyridyl group, which groups are unsubstituted or substituted with 1, 2 or 3 substituents Y, which can be the same or different and are independently chosen as set forth above, or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents unsubstituted naphthyl,
• wherein the amount is an amount effective for the prophylaxis or treatment of at least one condition chosen from:
• at least one CB1 receptor related disease in a juvenile patient in need of such treatment or prophylaxis,
• drug induced obesity in a juvenile or adolescent patient in need of such treatment or prophylaxis, and
• a combination of any of the foregoing, and at least one auxiliary excipient.

A method of treatment or prophylaxis of at least one condition chosen from:

• at least one CB1 receptor related disease in a juvenile patient in need of such treatment or prophylaxis, drug induced obesity in a juvenile or adolescent patient in need of such treatment or prophylaxis, and a combination of any of the foregoing,
• comprising:
• administering to the patient in need of said treatment or prophylaxis an amount of at least one compound of formula (I), at least one prodrug thereof, at least one tautomer thereof, at least one salt thereof, or a mixture of two or more of the foregoing,
• wherein the at least one compound of formula (I) has the following structure:
• wherein
• - R and R1 independently of each other represent
• unsubstituted naphthyl, or
• phenyl, thienyl or pyridyl groups, which groups are unsubstituted or substituted with 1, 2 or 3 substituents Y, which can be the same or different, and are chosen from
• C1-3-alkyl, C1-3-alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, nitro, amino, mono (C1-2)-alkylamino, di (C1-2)-alkylamino, mono (C1-2)-alkylamido, di (C1-2)-alkylamido, (C1-3)-alkyl sulfonyl, dimethylsuIfamido, C1-3-alkoxycarbonyl, carboxyl, trifiuoromethylsulfonyl, cyano, carbamoyl, sulfamoyl and acetyl,
• - R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy,
• - Aa represents one of the groups (i), (ii), (iii), (iv) or (v)
• wherein
• - R4 and R5 independently of each other represent hydrogen or C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R4 represents acetamido, dimethylamino, 2,2,2-trifluoroethyl, phenyl, or pyridyl with the proviso that R5 represents hydrogen,
• - R6 represents hydrogen or C1-3 unbranched alkyl,
• - Bb represents sulfonyl or carbonyl,
• - R3 represents a benzyl, phenyl, thienyl or pyridyl group, which groups are unsubstituted or substituted with 1, 2 or 3 substituents Y, which can be the same or different and are independently chosen as set forth above, or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents unsubstituted naphthyl,
• wherein the amount is an amount effective for said treatment or prophylaxis.

A method of treatment or prophylaxis of drug induced weight gain in a patient in need of such treatment or prophylaxis comprising:

• administering to the patient in need of said treatment or prophylaxis an amount of at least one compound of formula (I), at least one prodrug thereof, at least one tautomer thereof, at least one salt thereof, or a mixture of two or more of the foregoing,
• wherein the at least one compound of formula (I) has the following structure:
• wherein
• - R and R1 independently of each other represent
• unsubstituted naphthyl, or
• phenyl, thienyl or pyridyl groups, which groups are unsubstituted or substituted with 1, 2 or 3 substituents Y, which can be the same or different, and are chosen from
• C1-3-alkyl, C1-3-alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, nitro, amino, mono (C1-2)-alkylamino, di (C1-2)-alkylamino, mono (C1-2)-alkylamido, di (C1-2)-alkylamido, (C1-3)-alkyl sulfonyl, dimethylsuIfamido, C1-3-alkoxycarbonyl, carboxyl, trifiuoromethylsulfonyl, cyano, carbamoyl, sulfamoyl and acetyl,
• - R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy,
• - Aa represents one of the groups (i), (ii), (iii), (iv) or (v)
• wherein
• - R4 and R5 independently of each other represent hydrogen or C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R4 represents acetamido, dimethylamino, 2,2,2-trifluoroethyl, phenyl, or pyridyl with the proviso that R5 represents hydrogen,
• - R6 represents hydrogen or C1-3 unbranched alkyl,
• - Bb represents sulfonyl or carbonyl,
• - R3 represents a benzyl, phenyl, thienyl or pyridyl group, which groups are unsubstituted or substituted with 1, 2 or 3 substituents Y, which can be the same or different and are independently chosen as set forth above, or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents unsubstituted naphthyl,
• wherein the amount is an amount effective for said treatment or prophylaxis.