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Last Updated: April 24, 2024

Claims for Patent: 7,615,573


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Summary for Patent: 7,615,573
Title:Synthesis of UDP-glucose: N-acylsphingosine glucosyltransferase inhibitors
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.
Inventor(s): Siegel; Craig (Woburn, MA), Shayman; James A. (Ann Arbor, MI), Nelson; Carol A. (Westford, MA), Harris; David J. (Lexington, MA), Copeland; Diane P. (North Billerica, MA)
Assignee: The Regents of the University of Michigan (Ann Arbor, MI) Genzyme Corporation (Cambridge, MA)
Application Number:11/702,425
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 7,615,573
Patent Claims: 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: ##STR00032## 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: ##STR00033## 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: ##STR00034## 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: ##STR00035## 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: ##STR00036## 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: ##STR00037## 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%.

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