IP Library › Granted Patent US 7,538,093
Granted Patent B2
US 7,538,093 · App. 11/359,997 · Granted May 26, 2009

Compositions and methods for therapeutic use

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Quick Facts
Patent No.
US 7,538,093
App. No.
11/359,997
Granted
May 26, 2009
Kind
B2
Abstract

A method and pharmaceutical composition for the enhancement of transfer of a therapeutic agent to a cell wherein the therapeutic agent is formulated in a buffer comprising a compound of Formula I: wherein: n is an integer from 2-8; X 1 is a cholic acid group or deoxycholic acid group; and X 2 and X 3 are each independently selected from the group consisting of a cholic acid group, a deoxycholic acid group, and a saccharide group, wherein the saccharide group is selected from the group consisting of pentose monosaccharide groups, hexose monosaccharide groups, pentose-pentose disaccharide groups, hexose-hexose disaccharide groups, pentose-hexose disaccharide groups, and hexose-pentose disaccharide groups; and wherein at least one of X 2 and X 3 is a saccharide group.

Claims (34)

1. A compound of Formula I:

wherein:

n is an integer from 2-8;

X 1 is a cholic acid group or deoxycholic acid group; and X 2 and X 3 are each independently selected from the group consisting of a cholic acid group, a deoxycholic acid group, and a saccharide group, wherein the saccharide group is selected from the group consisting of hexose monosaccharide groups, pentose-pentose disaccharide groups, hexose-hexose disaccharide groups, pentose-hexose disaccharide groups, and hexose-pentose disaccharide groups; and wherein at least one of X 2 and X 3 is a saccharide group, and

wherein each cholic acid group is of the formula:

and each deoxycholic group is of the formula:

2. The compound according to claim 1 , wherein n is 3.

3. The compound according to claim 1 , wherein both X 1 and X 2 are both cholic acid groups.

4. The compound according to claim 1 , wherein X 1 and X 2 are both deoxycholic acid groups.

5. The compound according to claim 1 , wherein the saccharide group is a hexose monosaccharide group.

6. The compound according to claim 1 , wherein the saccharide group is a hexose-hexose disaccharide group.

7. The compound according to claim 1 , wherein n is 3, X 1 and X 2 are both cholic acid groups, and X 3 is a hexose monosaccharide group.

8. The compound according to claim 1 , wherein n is 3, X 1 and X 3 are both cholic acid groups, and X 2 is a hexose monosaccharide group.

9. The compound according to claim 1 , wherein n is 3, X 1 and X 2 are both cholic acid groups, and X 3 is a hexose-hexose disaccharide group.

10. The compound according to claim 1 , wherein n is 3, X 1 and X 3 are both cholic acid groups, and X 2 is a hexose-hexose disaccharide group.

11. The compound according to claim 1 , wherein n is 3, X 1 and X 2 are both cholic acid groups, and X 3 is a hexose-pentose disaccharide group.

12. The compound according to claim 1 , wherein n is 3, X 1 and X 3 are both cholic acid groups, and X 2 is a hexose-pentose disaccharide group.

13. A compound of claim 1 , where n is 3, and X 2 is a cholic acid group or a deoxycholic acid group.

14. The compound according to claim 13 , wherein both X 1 and X 2 are cholic acid groups and X 3 is a glucose group.

15. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

16. The composition of claim 15 , further comprising a pharmaceutically acceptable buffer.

17. The composition of claim 15 , wherein n is 3.

18. The composition of claim 15 , wherein both X 1 and X 2 are both cholic acid groups.

19. The composition of claim 15 , wherein X 1 and X 2 are both deoxycholic acid groups.

20. The composition of claim 15 , wherein saccharide group is a hexose monosaccharide group.

21. The composition of claim 15 , wherein the saccharide group is a hexose-hexose disaccharide group.

22. The composition of claim 15 , wherein n is 3, X 1 and X 2 are both cholic acid groups, and X 3 is a hexose monosaccharide group.

23. The composition of claim 15 , wherein n is 3, X 1 and X 3 are both cholic acid groups, and X 2 is a hexose monosaccharide group.

24. The composition of claim 15 , wherein n is 3, X 1 and X 2 are both cholic acid groups, and X 3 is a hexose-hexose disaccharide group.

25. The composition of claim 15 , wherein n is 3, X 1 and X 3 are both cholic acid groups, and X 2 is a hexose-hexose disaccharide group.

26. The composition according to claim 15 , wherein n is 3, X 1 and X 2 are both cholic acid groups, and X 3 is a hexose-pentose disaccharide group.

27. The composition according to claim 15 , wherein n is 3, X 1 and X 3 are both cholic acid groups, and X 2 is a hexose-pentose disaccharide group.

28. The composition of claim 15 , where n is 3, X 2 is a cholic acid group or a deoxycholic acid group; and X 3 is a saccharide group.

29. The composition of claim 15 , wherein both X 1 and X 2 are cholic acid groups and X 3 is a glucose group.

Assignments (1)
CHANGE OF NAME Recorded Aug 30, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028884/0151 →