IP Library › Granted Patent US 7,615,573
Granted Patent B2
US 7,615,573 · App. 11/702,425 · Granted Nov 10, 2009

Synthesis of UDP-glucose: N-acylsphingosine glucosyltransferase inhibitors

Assignees: The Regents of the University of Michigan; Genzyme Corporation
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Quick Facts
Patent No.
US 7,615,573
App. No.
11/702,425
Granted
Nov 10, 2009
Kind
B2
Abstract

Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Claims (36)

1. A method of inhibiting glucosylceramide synthase or lowering glycosphingolipid concentrations in a subject in need thereof, comprising administering to the subject an effective amount of a compound represented by the following structural formula:

or a physiologically acceptable salt thereof.

2. The method of claim 1 , wherein the compound has an enantiomeric excess of at least 25%.

3. The method of claim 1 , wherein the compound has an enantiomeric excess of at least 50%.

4. The method of claim 1 , wherein the compound has an enantiomeric excess of at least 90%.

5. The method of claim 1 , wherein the compound has an enantiomeric excess of at least 99%.

6. A method of treating a subject with Fabry disease, comprising administering to the subject an effective amount of a compound represented by the following structural formula:

or a physiologically acceptable salt thereof.

7. The method of claim 6 , wherein the compound has an enantiomeric excess of at least 25%.

8. The method of claim 6 , wherein the compound has an enantiomeric excess of at least 50%.

9. The method of claim 6 , wherein the compound has an enantiomeric excess of at least 90%.

10. The method of claim 6 , wherein the compound has an enantiomeric excess of at least 99%.

11. A method of inhibiting glucosylceramide synthase or lowering glycosphingolipid concentrations in a subject in need thereof, comprising administering to the subject an effective amount of a compound represented by the following structural formula:

or a physiologically acceptable salt thereof.

12. The method of claim 11 , wherein the compound has an enantiomeric excess of at least 25%.

13. The method of claim 11 , wherein the compound has an enantiomeric excess of at least 50%.

14. The method of claim 11 , wherein the compound has an enantiomeric excess of at least 90%.

15. The method of claim 11 , wherein the compound has an enantiomeric excess of at least 99%.

16. A method of treating a subject with Fabry disease, comprising administering to the subject an effective amount of a compound represented by the following structural formula:

or a physiologically acceptable salt thereof.

17. The method of claim 16 , wherein the compound has an enantiomeric excess of at least 25%.

18. The method of claim 16 , wherein the compound has an enantiomeric excess of at least 50%.

19. The method of claim 16 , wherein the compound has an enantiomeric excess of at least 90%.

20. The method of claim 16 , wherein the compound has an enantiomeric excess of at least 99%.

21. A method of treating a subject with Gaucher disease, comprising administering to the subject an effective amount of a compound represented by the following structural formula:

or a physiologically acceptable salt thereof.

22. The method of claim 21 , wherein the compound has an enantiomeric excess of at least 25%.

23. The method of claim 21 , wherein the compound has an enantiomeric excess of at least 50%.

24. The method of claim 21 , wherein the compound has an enantiomeric excess of at least 90%.

25. The method of claim 21 , wherein the compound has an enantiomeric excess of at least 99%.

26. A method of treating a subject with Gaucher disease, comprising administering to the subject an effective amount of a compound represented by the following structural formula:

or a physiologically acceptable salt thereof.

27. The method of claim 26 , wherein the compound has an enantiomeric excess of at least 25%.

28. The method of claim 26 , wherein the compound has an enantiomeric excess of at least 50%.

29. The method of claim 26 , wherein the compound has an enantiomeric excess of at least 90%.

30. The method of claim 26 , wherein the compound has an enantiomeric excess of at least 99%.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2018
From: SHAYMAN, JAMES A
To: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Reel/Frame 047500/0545 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 14, 2018
From: SIEGEL, CRAIG; NELSON, CAROL A; HARRIS, DAVID J; COPELAND, DIANE P
To: GENZYME CORPORATION
Reel/Frame 047500/0548 →
Continuity (5)
Division 1109183600 · Mar 28, 2005
Continuation 1091682400 · Aug 12, 2004
Division 1019722700 · Jul 16, 2002
Provisional Application 6030581400 · Jul 16, 2001
Related Publication 20070203223A1 · Aug 30, 2007