IP Library Granted Patent US 9,243,020
Granted Patent B2
US 9,243,020 · App. 13/997,484 · Granted Jan 26, 2016

Selective glycosidase inhibitors and uses thereof

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Quick Facts
Patent No.
US 9,243,020
App. No.
13/997,484
Granted
Jan 26, 2016
Kind
B2
Abstract

The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.

Claims (57)

1. A compound which is

or a pharmaceutically acceptable salt thereof.

2. A compound which is

3. A compound which is

in the form of a pharmaceutically acceptable salt thereof.

4. A compound which is

or a pharmaceutically acceptable salt thereof.

5. A compound which is

6. A compound which is

in the form of a pharmaceutically acceptable salt thereof.

7. A compound which is

or a pharmaceutically acceptable salt thereof.

8. A compound which is

9. A compound which is

in the form of a pharmaceutically acceptable salt thereof.

10. A pharmaceutical composition comprising a compound which is

or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

11. The pharmaceutical composition of claim 10 wherein the compound is

12. The pharmaceutical composition of claim 10 wherein the compound is

in the form of a pharmaceutically acceptable salt thereof.

13. A pharmaceutical composition comprising a compound which is

or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

14. The pharmaceutical composition of claim 13 wherein the compound is

15. The pharmaceutical composition of claim 13 wherein the compound is

in the form of a pharmaceutically acceptable salt thereof.

16. A pharmaceutical composition comprising a compound which is

or a pharamaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

17. The pharmaceutical composition of claim 16 wherein the compound is

18. The pharmaceutical composition of claim 16 wherein the compound is

in the form of a pharmaceutically acceptable salt thereof.

19. A method of treating Alzheimer's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 1 or a pharmaceutically acceptable salt thereof.

20. A method of treating Alzheimer's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 2 .

21. A method of treating Alzheimer's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 3 in the form of a pharmaceutically acceptable salt thereof.

22. A method of treating Alzheimer's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 4 or a pharmaceutically acceptable salt thereof.

23. A method of treating Alzheimer's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 5 .

24. A method of treating Alzheimer's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 6 in the form of a pharmaceutically acceptable salt thereof.

25. A method of treating Alzheimer's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 7 or a pharmaceutically acceptable salt thereof.

26. A method of treating Alzheimer's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 8 .

27. A method of treating Alzheimer's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 8 in the form of pharmaceutically acceptable salt thereof.

28. A method of treating Parkinson's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 1 or a pharmaceutically acceptable salt thereof.

29. A method of treating Parkinson's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 2 .

30. A method of treating Parkinson's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 3 in the form of a pharmaceutically acceptable salt thereof.

31. A method of treating Parkinson's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 4 or a pharmaceutically acceptable salt thereof.

32. A method of treating Parkinson's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 5 .

33. A method of treating Parkinson's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 6 in the form of a pharmaceutically acceptable salt thereof.

34. A method of treating Parkinson's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 7 or a pharmaceutically acceptable salt thereof.

35. A method of treating Parkinson's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 8 .

36. A method of treating Parkinson's disease in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 9 in the form of pharmaceutically acceptable salt thereof.

37. A method of treating Progressive supranuclear palsy in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 1 or a pharmaceutically acceptable salt thereof.

38. A method of treating Progressive supranuclear palsy in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 2 .

39. A method of treating Progressive supranuclear palsy in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 3 in the form of a pharmaceutically acceptable salt thereof.

40. A method of treating Progressive supranuclear palsy in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 4 or a pharmaceutically acceptable salt thereof.

41. A method of treating Progressive supranuclear palsy in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 5 .

42. A method of treating Progressive supranuclear palsy in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 6 in the form of a pharmaceutically acceptable salt thereof.

43. A method of treating Progressive supranuclear palsy in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 7 or a pharmaceutically acceptable salt thereof.

44. A method of treating Progressive supranuclear palsy in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 8 .

45. A method of treating Progressive supranuclear palsy in a human patient in need thereof which comprises administering to the patient a therapeutically effective amount of the compound of claim 9 in the form of pharmaceutically acceptable salt thereof.

Assignments (7)
MERGER Recorded Mar 14, 2023
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 062981/0033 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 14, 2023
From: MERCK SHARP & DOHME LLC
To: ALECTOS THERAPEUTICS INC.
Reel/Frame 062981/0221 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2013
From: WEI, ZHONGYONG; MU, CHANGWEI; WANG, YAODE
To: PHARMARON BEIJING, CO. LTD.
Reel/Frame 031346/0091 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2013
From: KAUL, RAMESH; MCEACHERN, ERNEST J.; VOCADLO, DAVID J.; ZHOU, YUANXI; ZHU, YONGBAO
To: ALECTOS THERAPEUTICS INC.
Reel/Frame 031346/0195 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2013
From: PHARMARON, INC.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 031346/0266 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2013
From: PHARMARON BEIJING, CO. LTD.
To: PHARMARON, INC.
Reel/Frame 031346/0306 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 4, 2013
From: SELNICK, HAROLD G.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 031346/0396 →