Claims for Patent: 9,914,738

Summary for Patent: 9,914,738

Title:	Short-acting benzodiazepine salts and their polymorphic forms
Abstract:	The invention relates to besylate salts of the compound of formula (I): ##STR00001## Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
Inventor(s):	Tilbrook; Gary Stuart (Huntington, GB), Quegan; Louisa Jane (Cambridge, GB)
Assignee:	PAION UK LIMITED (Cambridge Cambridgeshire, GB)
Application Number:	15/703,945
Patent Claims:	1. A lyophilized composition comprising a besylate salt of the compound of formula (I) ##STR00005## and at least one pharmaceutically acceptable carrier, excipient or diluent, wherein said lyophilized composition maintains at least 96.7% of the original amount of the compound of formula (I) comprising said lyophilized composition following storage of said lyophilized composition at 40.degree. C. and 75% relative humidity for 4 weeks, and wherein said amount of the compound of formula (I) in said lyophilized composition is measured by high-performance liquid chromatography. 2. The lyophilized composition according to claim 1, wherein said lyophilized composition maintains at least 97.3% of the original amount of the compound of formula (I) comprising said lyophilized composition following storage of said lyophilized composition at 40.degree. C. and 75% relative humidity for 1 week, and wherein said amount of the compound of formula (I) in said lyophilized composition is measured by high-performance liquid chromatography. 3. The lyophilized composition according to claim 1, wherein said lyophilized composition maintains at least 97.3% of the original amount of the compound of formula (I) comprising said lyophilized composition following storage of said lyophilized composition at 40.degree. C. and 75% relative humidity for 2 weeks, and wherein said amount of the compound of formula (I) in said lyophilized composition is measured by high-performance liquid chromatography. 4. An aqueous pharmaceutical composition prepared by reconstitution of a lyophilized composition, said lyophilized composition comprising a besylate salt of the compound of formula (I) ##STR00006## and at least one pharmaceutically acceptable carrier, excipient or diluent, wherein said lyophilized composition maintains at least 96.7% of the original amount of the compound of formula (I) comprising said lyophilized composition following storage of said lyophilized composition at 40.degree. C. and 75% relative humidity for 4 weeks, and wherein said amount of the compound of formula (I) in said lyophilized composition is measured by high-performance liquid chromatography. 5. The aqueous pharmaceutical composition according to claim 4, wherein said lyophilized composition maintains at least 97.3% of the original amount of the compound of formula (I) comprising said lyophilized composition following storage of said lyophilized composition at 40.degree. C. and 75% relative humidity for 1 week, and wherein said amount of the compound of formula (I) in said lyophilized composition is measured by high-performance liquid chromatography. 6. The aqueous pharmaceutical composition according to claim 4, said lyophilized composition maintains at least 97.3% of the original amount of the compound of formula (I) comprising said lyophilized composition following storage of said lyophilized composition at 40.degree. C. and 75% relative humidity for 2 weeks, and wherein said amount of the compound of formula (I) in said lyophilized composition is measured by high-performance liquid chromatography. 7. The aqueous pharmaceutical composition according to claim 4, wherein said lyophilized composition is reconstituted with water, a dextrose solution or a saline solution. 8. The aqueous pharmaceutical composition according to claim 7, wherein said aqueous composition is presented in a unit dosage form selected from a bottle, an ampoule, a disposable injection device, and a vial. 9. The aqueous pharmaceutical composition according to claim 8, wherein said unit dosage form is an ampoule or a vial. 10. The aqueous pharmaceutical composition according to claim 9, wherein said unit dosage form contains from about 0.1 mg/mL to about 20 mg/mL of a besylate salt of the compound of formula (I). 11. The lyophilized composition according to claim 1, wherein said composition is presented in a unit dosage form selected from a bottle, an ampoule, a disposable injection device, and a vial. 12. The lyophilized composition according to claim 11, wherein said unit dosage form is an ampoule or a vial.