Details for Patent: 6,872,701

Title:	Glycopeptide phosphonate derivatives
Abstract:	Disclosed are glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Inventor(s):	Leadbetter; Michael R. (San Leandro, CA), Linsell; Martin S. (San Mateo, CA)
Assignee:	Theravance, Inc. (South San Francisco, CA)
Filing Date:	May 12, 2003
Application Number:	10/436,341
Claims:	1. A lyophilized composition comprising: (a) a compound of the formula: ##STR9## or a pharmaceutically acceptable salt thereof; and (b) a cyclodextrin. 2. The composition of claim 1, wherein the cyclodextrin is hydroxypropyl-.beta.-cyclodextrin. 3. The composition of claim 1, wherein the cyclodextrin is sulfobutyl ether .beta.-cyclodextrin. 4. The composition of claim 1, wherein the weight ratio of the cyclodextrin to the compound is from about 1:1 to about 10:1. 5. The composition of claim 1, wherein the pharmaceutically-acceptable salt is a hydrochloride salt. 6. The composition of claim 1, wherein the composition further comprises an excipient selected from the group consisting of mannitol, sucrose, lactose and combinations thereof. 7. The composition of claim 6, wherein the excipient is mannitol. 8. A lyophilized composition comprising: (a) a compound of the formula: ##STR10## or a hydrochloride salt thereof; (b) hydroxypropl-.beta.-cyclodextrin; and (c) mannitol. 9. A process for preparing a lyophilized composition, wherein the lyophilized composition comprises: (i) a compound of the formula: ##STR11## or a pharmaceutically-acceptable salt thereof; and (ii) a cyclodextrin; wherein the process comprising the steps of: (a) providing an aqueous solution comprising the compound or pharmaceutically-acceptable salt thereof and the cyclodextrin; and (b) lyophilizing the aqueous solution to provide the lyophilized composition. 10. The process of claim 9, wherein the cyclodextrin is hydroxypropyl-.beta.-cyclodextrin. 11. The process of claim 9, wherein the cyclodextrin is sulfobutyl ether .beta.-cyclodextrin. 12. The process of claim 9, wherein the weight ratio of the cyclodextrin to the compound is from about 1:1 to about 10:1. 13. The process of claim 9, wherein the pharmaceutically-acceptable salt is a hydrochloride salt. 14. The process of claim 9, wherein the composition further comprises an excipient selected from the group consisting of mannitol, sucrose, lactose and combinations thereof. 15. The process of claim 14, wherein the excipient is mannitol. 16. The product prepared by the process of claim 9. 17. A vial containing a lyophilized composition comprising: (a) 250 mg to 1000 mg of a compound of the formula: ##STR12## or a pharmaceutically-acceptable salt thereof; and (b) 250 mg to 10 g of hydroxypropyl-.beta.-cyclodextrin. 18. The vial of claim 17, wherein the pharmaceutically-acceptable salt is a hydrochloride salt. 19. The vial of claim 17, wherein the lyophilized composition further comprises from 0 to 50 g of an excipient selected from mannitol, sucrose, lactose and combinations thereof. 20. The vial of claim 19, wherein the excipient is mannitol.