Claims for Patent: 10,195,210

Summary for Patent: 10,195,210

Title:	Dosing regimen for sedation with CNS 7056 (Remimazolam)
Abstract:	The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 20 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.
Inventor(s):	Karin Wilhelm-Ogunbiyi, Keith Borkett, Gary Stuart Tilbrook, Hugh Wiltshire
Assignee:	Paion UK Ltd
Application Number:	US16/039,198
Patent Claims:	1. A method for conducting a procedure involving sedation in a subject comprising: (a) administering intravenously to the subject one or more fixed doses of a pharmaceutical composition in an amount sufficient to sedate the subject, wherein the pharmaceutical composition comprises 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]-propionic methyl ester of formula (I) or a pharmaceutically acceptable salt thereof; and (b) passing an endoscope into the subject. 2. The method of claim 1, wherein the subject is 18 years or older. 3. The method of claim 1, wherein one or more doses of an opioid is administered to the subject prior to the administration of the pharmaceutical composition to the subject. 4. The method of claim 3, wherein the opioid is fentanyl. 5. The method of claim 1, wherein the procedure is an upper GI endoscopy. 6. The method of claim 1, wherein the procedure is a colonoscopy. 7. The method of claim 1, wherein the one or more fixed doses of the pharmaceutical composition is administered to the subject over a time period of one minute or less. 8. The method of claim 1, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 2 mg to about 10 mg of the compound of formula (I), or a pharmaceutically acceptable salt thereof. 9. The method of claim 8, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 10 mg of the compound of formula (I), or a pharmaceutically acceptable salt thereof. 10. The method of claim 9, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 9 mg of the compound of formula (I), or a pharmaceutically acceptable salt thereof. 11. The method of claim 10, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 5 mg to about 9 mg of the compound of formula (I), or a pharmaceutically acceptable salt thereof. 12. The method of claim 8, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 2 mg to about 10 mg of the compound of formula (I). 13. The method of claim 12, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 10 mg of the compound of formula (I). 14. The method of claim 13, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 9 mg of the compound of formula (I). 15. The method of claim 13, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 5 mg to about 8 mg of the compound of formula (I). 16. The method of claim 15, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises about 5 mg of the compound of formula (I). 17. The method of claim 1, wherein the one or more doses of the pharmaceutical composition comprise an amount of the compound of formula (I), or a pharmaceutically acceptable salt thereof, to achieve an MOAA/S score of less than or equal to 4 in the subject. 18. The method of claim 1, wherein the pharmaceutical composition comprises the besylate salt of the compound of formula (I). 19. A method for conducting a procedure involving sedation in a subject comprising: (a) administering intravenously to the subject one or more fixed doses of a pharmaceutical composition in an amount sufficient to sedate the subject, wherein the pharmaceutical composition comprises the besylate salt of 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]-propionic methyl ester of formula (I) and wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 2 mg to about 10 mg of the besylate salt of the compound formula (I); and (b) passing an endoscope into the subject. 20. The method of claim 19, wherein the subject is 18 years or older. 21. The method of claim 19, wherein one or more doses of an opioid is administered to the subject prior to the administration of the pharmaceutical composition to the subject. 22. The method of claim 21, wherein the opioid is fentanyl. 23. The method of claim 19, wherein the procedure is an upper GI endoscopy. 24. The method of claim 19, wherein the procedure is a colonoscopy. 25. The method of claim 19, wherein the one or more fixed doses of the pharmaceutical composition is administered to the subject over a time period of one minute or less. 26. The method of claim 19, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 10 mg of the besylate salt of the compound of formula (I). 27. The method of claim 26, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 3 mg to about 9 mg of the besylate salt of the compound of formula (I). 28. The method of claim 27, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 5 mg to about 9 mg of the besylate salt of the compound of formula (I). 29. The method of claim 19, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises from about 5 mg to about 8 mg of the compound of formula (I). 30. The method of claim 29, wherein each fixed dose of the pharmaceutical composition administered to the subject comprises about 5 mg of the compound of formula (I). 31. The method of claim 19, wherein the one or more doses of the pharmaceutical composition comprise an amount of the besylate salt of the compound of formula (I) sufficient to achieve an MOAA/S score of less than or equal to 4 in the subject. 32. A method for conducting a procedure involving sedation in a subject comprising: (a) administering to the subject one or more doses of a pharmaceutical composition, wherein each dose of the pharmaceutical composition comprises 5 mg of 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]-propionic methyl ester of formula (I) or a pharmaceutically acceptable salt thereof; and (b) passing a colonoscope into the subject. 33. The method of claim 1, wherein the procedure is a diagnostic procedure. 34. The method of claim 19, wherein the procedure is a diagnostic procedure. 35. The method of claim 32, wherein the procedure is a diagnostic procedure.