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US 8,785,418 B2Granted
Lyophilization cakes of proteasome inhibitors
AssigneeCephalon, Inc.
InventorsDenis Bricout, Helene Cambourieux, Michael L. Cappola, Nicole Frati, Piyush R. Patel
Life of this patent
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Abstract
Lyophilized cakes of proteasome inhibitors are described, as well as methods for their production and use.
Claims17
A lyophilized cake comprising:
- (a) a compound of Formula I or a pharmaceutically acceptable salt or ester thereof:
- wherein R1 is an optionally substituted 5-, 6-, or 10-membered heteroaryl having at least one N or R1 is an optionally substituted 6- or 10-membered aryl;
- (b) a cyclodextrin;
- and
- (c) a bulking agent comprising a monosaccharide.
2 more elements
A method for manufacturing a lyophilized cake comprising the steps of:
- (a) providing a first mixture comprising a cyclodextrin, a bulking agent comprising a monosaccharide, and water;
- (b) mixing a surfactant and a portion of the first mixture to form a second mixture;
- (c) combining a compound of Formula I, or a salt or ester thereof, and the second mixture to form a drug mixture;
- wherein R1 is an optionally substituted 5-, 6-, or 10-membered heteroaryl having at least one N or R1 is an optionally substituted 6- or 10-membered aryl;
- (d) mixing the remainder of the first mixture with the drug mixture to form a pre-lyophilization solution;
- and
- (e) lyophilizing the pre-lyophilization solution.
4 more elements
A method for manufacturing a lyophilized cake comprising:
- (a) providing a first mixture containing a cyclodextrin, a bulking agent comprising a monosaccharide, and water;
- (b) providing a drug mixture containing a compound of Formula I, or a salt or ester thereof, and tert-butanol;
- wherein R1 is an optionally substituted 5-, 6-, or 10-membered heteroaryl having at least one N or R1 is an optionally substituted 6- or 10-membered aryl;
- (c) combining the first mixture and the drug mixture to provide a pre-lyophilization solution;
- and
- (d) lyophilizing the pre-lyophilization solution.
3 more elements
Dependencies are inferred from the claim text.