Selective glycosidase inhibitors and uses thereof

Patent metadata

Field	Value
Publication number	US-9243020-B2
Application number	US-201113997484-A
Country	US
Kind code	B2
Filing date	Dec 21, 2011
Priority date	Dec 23, 2010
Publication date	Jan 26, 2016
Grant date	Jan 26, 2016

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.

First claim

What is claimed is:

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

Assignees

• Kaul Ramesh
• Mceachern Ernest J
• Selnick Harold G
• Vocadlo David J
• Zhou Yuanxi
• Zhu Yongbao
• Alectos Therapeutics Inc
• Merck Sharp & Dohme

Inventors

• Kaul Ramesh
• Mceachern Ernest J
• Selnick Harold G
• Vocadlo David J
• Zhou Yuanxi
• Zhu Yongbao

Classifications

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P5/14

  of the thyroid hormones, e.g. T3, T4 · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title