Dipeptidyl peptidase inhibitors
The present invention provides a compound of the formula: or stereoisomers or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, articles of manufacture comprising the same, and methods of using the same.
1. A compound of the formula
or stereoisomers or pharmaceutically acceptable salts thereof.
2. The compound according to claim 1 , wherein the compound is present as a mixture of stereoisomers.
3. The compound according to claim 1 , wherein the compound comprises a single stereoisomer.
4. A compound of the formula
or pharmaceutically acceptable salts thereof.
5. A compound of the formula
wherein the compound is present in a free base form, or stereoisomers thereof.
6. The compound according to claim 5 , wherein the compound is present as a mixture of stereoisomers.
7. The compound according to claim 5 , wherein the compound is present as a single stereoisomer.
8. A compound of the formula
wherein the compound is present in a free base form.
9. A compound of the formula
wherein the compound is present as a benzoate salt, or stereoisomers thereof.
10. The compound according to claim 9 , wherein the compound is present as a mixture of stereoisomers.
11. The compound according to claim 10 , wherein the compound is present as a single stereoisomer.
12. A compound of the formula
wherein the compound is present as a benzoate salt.
13. A pharmaceutical composition comprising, as an active ingredient, a compound of the formula
or stereoisomers or pharmaceutically acceptable salts thereof, and one or more compounds selected from the group consisting of excipients, diluents, lubricants, binders, adjuvants, carriers, wetting agents, emulsifying agents, solubilizing agents and pH buffering agents.
14. The pharmaceutical composition according to claim 13 , wherein the composition is a solid formulation adapted for oral administration.
15. The pharmaceutical composition according to claim 13 , wherein the composition is a tablet.
16. The pharmaceutical composition according to claim 13 , wherein the composition is a liquid formulation adapted for oral administration.
17. The pharmaceutical composition according to claim 13 , wherein the composition is a liquid formulation adapted for parenteral administration.
18. The pharmaceutical composition according to claim 13 , wherein the composition is adapted for administration by a route selected from the group consisting of orally, parenterally, intraperitoneally, intravenously, intraarterially, transdermally, sublingually, intramuscularly, rectally, transbuccally, intranasally, liposomally, via inhalation, vaginally, intraoccularly, via local delivery, subcutaneously, intraadiposally, intraarticularly, and intrathecally.
19. A pharmaceutical composition comprising, as an active ingredient, a compound of the formula
wherein the compound is present in a free base form, and one or more compounds selected from the group consisting of excipients, diluents, lubricants, binders, adjuvants, carriers, wetting agents, emulsifying agents, solubilizing agents and pH buffering agents.
20. The pharmaceutical composition according to claim 19 , wherein the composition is a solid formulation adapted for oral administration.
21. The pharmaceutical composition according to claim 19 , wherein the composition is a tablet.
22. The pharmaceutical composition according to claim 19 , wherein the composition is a liquid formulation adapted for oral administration.
23. The pharmaceutical composition according to claim 19 , wherein the composition is a liquid formulation adapted for parenteral administration.
24. The pharmaceutical composition according to claim 19 , wherein the composition is adapted for administration by a route selected from the group consisting of orally, parenterally, intraperitoneally, intravenously, intraarterially, transdermally, sublingually, intramuscularly, rectally, transbuccally, intranasally, liposomally, via inhalation, vaginally, intraoccularly, via local delivery, subcutaneously, intraadiposally, intraarticularly, and intrathecally.
25. A pharmaceutical composition comprising, as an active ingredient, a compound of the formula
wherein the compound is present as a benzoate salt, and one or more compounds selected from the group consisting of excipients, diluents, lubricants, binders, adjuvants, carriers, wetting agents, emulsifying agents, solubilizing agents and pH buffering agents.
26. The pharmaceutical composition according to claim 25 , wherein the composition is a solid formulation adapted for oral administration.
27. The pharmaceutical composition according to claim 25 , wherein the composition is a tablet.
28. The pharmaceutical composition according to claim 25 , wherein the composition is a liquid formulation adapted for oral administration.
29. The pharmaceutical composition according to claim 25 , wherein the composition is a liquid formulation adapted for parenteral administration.
30. The pharmaceutical composition according to claim 25 , wherein the composition is adapted for administration by a route selected from the group consisting of orally, parenterally, intraperitoneally, intravenously, intraarterially, transdermally, sublingually, intramuscularly, rectally, transbuccally, intranasally, liposomally, via inhalation, vaginally, intraoccularly, via local delivery, subcutaneously, intraadiposally, intraarticularly, and intrathecally.
31. An article of manufacture comprising:
a compound of the formula
or stereoisomers or pharmaceutically acceptable salts thereof; and
packaging materials.
32. The article of manufacture of claim 31 , wherein the packaging material comprises a container for housing the compound.
33. The article of manufacture of claim 32 , wherein the container comprises a label indicating one or more members of the group consisting of a disease state for which the compound is to be administered wherein the disease state is diabetes, storage information, dosing information and/or instructions regarding how to administer the composition.
34. The article of manufacture of claim 31 , wherein the article of manufacture comprises the compound in a multiple dose form.
35. An article of manufacture comprising:
a compound of the formula
wherein the compound is present as a free base form; and
packaging materials.
36. The article of manufacture of claim 35 , wherein the packaging material comprises a container for housing the compound.
37. The article of manufacture of claim 36 , wherein the container comprises a label indicating one or more members of the group consisting of a disease state for which the compound is to be administered wherein the disease state is diabetes, storage information, dosing information and/or instructions regarding how to administer the composition.
38. The article of manufacture of claim 35 , wherein the article of manufacture comprises the compound in a multiple dose form.
39. An article of manufacture comprising:
a compound of the formula
wherein the compound is present as a benzoate salt; and
packaging materials.
40. The article of manufacture of claim 39 , wherein the packaging material comprises a container for housing the compound.
41. The article of manufacture of claim 40 , wherein the container comprises a label indicating one or more members of the group consisting of a disease state for which the compound is to be administered wherein the disease state is diabetes, storage information, dosing information and/or instructions regarding how to administer the composition.
42. The article of manufacture of claim 39 , wherein the article of manufacture comprises the compound in a multiple dose form.
43. A method of treating type II diabetes in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound of the formula
or stereoisomers or pharmaceutically acceptable salts thereof.
44. A method of treating type I diabetes in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound of the formula
or stereoisomers or pharmaceutically acceptable salts thereof.
45. A method of treating breast cancer in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound according to claim 1 .
46. A method of treating type II diabetes in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound according to claim 8 .
47. A method of treating type I diabetes in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound according to claim 8 .
48. A method of treating breast cancer in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound according to claim 8 .
49. A method of treating type II diabetes in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound according to claim 12 .
50. A method of treating type I diabetes in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound according to claim 12 .
51. A method of treating breast cancer in a patient in need thereof, comprising administering to said patient a therapeutically effective amount of a compound according to claim 12 .