Granted Patent
B2
US 12,365,684 · App. 17/178,346 · Granted Jul 22, 2025
Short-acting benzodiazepine salts and their polymorphic forms
Assignee:
PAION UK LIMITED
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Abstract
The invention relates to besylate salts of the compound of formula (I): 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.
Claims (22)
1. A method of inducing anxiolysis or muscle relaxation or treating convulsion in a subject, comprising:
(a) reconstituting a lyophilized composition with an aqueous solution to afford an aqueous pharmaceutical composition; and
(b) administering to the subject an effective amount of the aqueous pharmaceutical composition;
wherein the lyophilized composition comprises a besylate salt of the compound of formula (I)
and at least one pharmaceutically acceptable carrier, excipient, or diluent, and wherein the lyophilized composition maintains at least 96.7% of the original amount of the compound of formula (I) following storage of the lyophilized composition at 40° C. and 75% relative humidity for a time period of from 1 week to 4 weeks, and wherein the amount of the compound of formula (I) in the lyophilized composition is measured by high-performance liquid chromatography.
2. The method of claim 1 , wherein the aqueous solution comprises dextrose or saline.
3. The method of claim 2 , wherein the aqueous solution comprises saline.
4. The method of claim 1 , wherein the aqueous pharmaceutical composition is administered to the subject by subcutaneous, intramuscular, intradermal, or intravenous administration.
5. The method of claim 4 , wherein the aqueous pharmaceutical composition is administered to the subject by intravenous administration.
6. The method of claim 5 , wherein the intravenous administration comprises a bolus injection or a continuous infusion.
7. The method of claim 6 , wherein the intravenous administration comprises a bolus injection.
8. The method of claim 6 , wherein the intravenous administration comprises a continuous infusion.
9. The method of claim 1 , wherein the aqueous pharmaceutical composition is administered to the subject during the time the subject is undergoing a diagnostic, operative or endoscopic procedure.
10. A method of inducing anxiolysis or muscle relaxation or treating convulsion in a subject, comprising administering to the subject an effective amount of a pharmaceutical composition comprising a besylate salt of the compound of formula (I)
and at least one pharmaceutically acceptable carrier, excipient or diluent, wherein the pharmaceutical composition is in the form of an aqueous solution comprising dextrose or saline.
11. The method of claim 10 , wherein the pharmaceutical composition is administered to the subject by subcutaneous, intramuscular, intradermal, or intravenous administration.
12. The method of claim 11 , wherein the pharmaceutical composition is administered to the subject by intravenous administration.
13. The method of claim 12 , wherein the intravenous administration comprises a bolus injection or a continuous infusion.
14. The method of claim 13 , wherein the intravenous administration comprises a bolus injection.
15. The method of claim 13 , wherein the intravenous administration comprises a continuous infusion.
16. The method of claim 10 , wherein the pharmaceutical composition is administered to the subject during the time the subject is undergoing a diagnostic, operative or endoscopic procedure.
17. The method of claim 2 , wherein the aqueous solution comprises dextrose.
Assignments (3)
CHANGE OF ADDRESS
Recorded Dec 6, 2022
From: PAION UK LIMITED
To: PAION UK LIMITED
Reel/Frame 062077/0856 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Feb 18, 2021
From: TILBROOK, GARY STUART; QUEGAN, LOUISA JANE
To: CENES LIMITED
Reel/Frame 055322/0271 →
CHANGE OF NAME
Recorded Feb 18, 2021
From: CENES LIMITED
To: PAION UK LIMITED
Reel/Frame 055322/0278 →
Priority Claims (2)
GB 0613692
· Jul 10, 2006
· national
GB 0613694
· Jul 10, 2006
· national
Continuity (6)
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