1. A method of selecting optimum gear of an automobile comprising the steps of:
(1) storing a universal characteristic curve of an engine of the automobile, gear ratios of a gearbox of the automobile, speed reduction ratios, and a tire radius of the automobile;
(2) collecting revolutions of the engine, an output torque of the engine, and a speed of the automobile in running;
(3) obtaining a current gear ratio by calculating the revolutions of the engine, the tire radius, the speed of the running automobile, and the speed reduction ratios; and determining a current gear based on the gear ratios of the gearbox;
(4) simulating gear shift; and obtaining the revolutions of the engine and the output torque of the engine by calculating gears other than the current gear;
(5) calculating fuel consumption rates of different gears based on a fuel consumption curve of the universal characteristic curve of the engine; comparing the fuel consumption rates of the different gears; and selecting an optimum gear from one of the gears having a lowest fuel consumption rate;
(6) deleting the calculation of fuel consumption rates of the different gears based on the fuel consumption curve of the universal characteristic curve of the engine of step (5) if the revolutions of the engine and the output torque of the engine do not fall on data points of the universal characteristic curve of the engine; and
(7) determining whether the optimum gear is the current gear; and outputting the optimum gear if the determination is negative.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
1. A method of making a medicament for the 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,
the method comprising:
combining 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, with at least one auxiliary excipient,
wherein the amount is an amount effective for said treatment or prophylaxis, and 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.
2. The method of making a medicament according to claim 1, wherein the at least one compound of formula (I) comprises at least one compound in which R is 4-chlorophenyl, R1 is phenyl, R2 is hydrogen, Aa is the group (i) wherein R4 is hydrogen and R5 is methyl, Bb is sulfonyl, and R3 represents 4-chlorophenyl, at least one salt thereof, or a mixture thereof.
3. The method of making a medicament according to claim 1, wherein the at least one compound of formula (I) comprises at least one levorotatory enantiomer.
4. 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.
5. The pharmaceutical composition according to claim 4, wherein the amount is an amount effective for the treatment or prophylaxis of at least one CB1 receptor related disease in a juvenile patient in need of such treatment or prophylaxis, wherein the disease is chosen from at least one psychiatric disorder, at least one gastrointestinal disorder, at least one cardiovascular disorder, and a combination of two or more of the foregoing.
6. The pharmaceutical composition according to claim 4, wherein the amount is an amount effective for the treatment or prophylaxis of drug induced obesity in a juvenile or adolescent patient in need of such treatment or prophylaxis.
7. 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.
8. The method of treatment or prophylaxis according to claim 7, wherein the at least one CB1 receptor related disease comprises at least one of: a psychiatric disorder, psychosis, anxiety, depression, attention deficit disorder, a memory disorder, an appetite disorder, obesity, a neurological disorder, Parkinson\u2019s disease, dementia, distonia, Alzheimer\u2019s disease, epilepsy, Huntington\u2019s disease, Tourette\u2019s syndrome, ischaemia, and pain.
9. The method of treatment or prophylaxis according to claim 7, wherein the method treats or prevents obesity in a juvenile patient.
10. The method of treatment or prophylaxis according to claim 7, wherein the method treats or prevents drug induced obesity in a juvenile patient or an adolescent patient.
11. The method of treatment or prophylaxis according to claim 7, wherein the method treats or prevents at least one CNS disorder involving cannabinoid neurotransmission.
12. 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.
13. The method of treatment or prophylaxis according to claim 12, wherein the patient is a juvenile patient.
14. The method of treatment or prophylaxis according to claim 12, wherein the patient is an adolescent patient.
15. The method of treatment or prophylaxis according to claim 12, wherein the at least one compound of formula (I) comprises at least one compound in which R is 4-chlorophenyl, R1 is phenyl, R2 is hydrogen, Aa is the group (i) wherein R4 is hydrogen and R5 is methyl, Bb is sulfonyl, and R3 represents 4-chlorophenyl, at least one salt thereof, or a mixture of the foregoing.
16. The method of treatment or prophylaxis according to claim 12, wherein the at least one compound of formula (I) comprises at least one levorotatory enantiomer.