Pharmaceutical composition of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine and uses thereof
View Patent ↗Pharmaceutical compositions comprising 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine; or a pharmaceutically acceptable salt thereof. The compositions are used for treating, preventing or delaying the onset of disorders mediated by LTB 4 , TXA 2 or adenosine.
1. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or a pharmaceutically acceptable salt thereof.
2. The pharmaceutical composition according to claim 1 , comprising (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine substantially free of the corresponding (S)-enantiomer; or a pharmaceutically acceptable salt thereof.
3. The composition according to claim 2 wherein the amount of (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 85% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.
4. The composition according to claim 3 wherein the amount of (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 90% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl -7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.
5. The composition according to claim 4 wherein the amount of (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 95% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl -7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.
6. The composition according to claim 5 wherein the amount of (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 99% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.
7. The pharmaceutical composition according to claim 1 , comprising (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine substantially free of the corresponding (R)-enantiomer; or a pharmaceutically acceptable salt thereof.
8. The composition according to claim 7 wherein the amount of (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 85% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.
9. The composition according to claim 8 wherein the amount of (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 90% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl -7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.
10. The composition according to claim 9 wherein the amount of (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 95% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.
11. The composition according to claim 10 wherein the amount of (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 99% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl -7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.
12. The pharmaceutical composition according to claim 1 , comprising a racemic mixture of the (R)- and (S)-enantiomers of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or a pharmaceutically acceptable salt thereof.
13. A method of treating a disorder characterized by convulsive seizures in an individual in need of such treatment, comprising administering to said individual a therapeutically effective amount of the composition according to claim 1 sufficient to inhibit convulsive seizures in said individual.
14. A method of treating a disorder characterized by convulsive seizures in an individual in need of such treatment, comprising administering to said individual a therapeutically effective amount of the composition according to claim 2 sufficient to inhibit convulsive seizures in said individual.
15. A method of treating a disorder characterized by convulsive seizures in an individual in need of such treatment, comprising administering to said individual a therapeutically effective amount of the composition according to claim 7 sufficient to inhibit convulsive seizures in said individual.
16. A method of treating a disorder characterized by convulsive seizures in an individual in need of such treatment, comprising administering to said individual a therapeutically effective amount of the composition according to claim 12 sufficient to inhibit convulsive seizures in said individual.