IP Library › Granted Patent US 8,673,927
Granted Patent B2
US 8,673,927 · App. 12/946,193 · Granted Mar 18, 2014

Uses of DPP-IV inhibitors

Inventors: Klaus Dugi (Dresden, DE); Frank Himmelsbach (Mittelbiberach, DE); Michael Mark (Biberach, DE)
Assignee: Boehringer Ingelheim International GmbH
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,673,927
App. No.
12/946,193
Granted
Mar 18, 2014
Kind
B2
Abstract

The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.

Claims (26)

1. A method of treating type II diabetes mellitus comprising administering to a patient in need thereof a pharmaceutically effective oral amount of 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, and a pharmaceutically effective amount of metformin, which is from 300 mg to 1000 mg once or twice a day, or delayed-release metformin in a dose of 500 mg to 1000 mg once or twice a day or 500 mg to 2000 mg once a day.

2. The method according to claim 1 , wherein the pharmaceutically effective oral amount of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is an oral daily dose of from 2.5 mg to 10 mg.

3. The method according to claim 1 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of from 0.5 mg to 50 mg.

4. The method according to claim 1 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of from 2.5 mg to 10 mg.

5. The method according to claim 1 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of 0.5 mg, 1 mg, 2.5 mg, 5 mg or 10 mg.

6. The method according to claim 1 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of 1 mg, 2.5 mg or 5 mg.

7. The method according to claim 1 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of 2.5 mg or 5 mg.

8. The method according to claim 1 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of from 2.5 mg to 50 mg.

9. The method according to claim 1 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral daily dose of 5 mg.

10. A method of treating type 2 diabetes or pre-diabetes comprising administering to a patient in need thereof a therapeutically effective oral dose of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine in combination with a therapeutically effective dose of metformin, which is 500 mg, 850 mg or 1000 mg metformin as a single dose with a total daily dose of metformin of 500-2850 mg, or which is 500 mg, 1000 mg, 1500 mg or 2000 mg metformin in delayed release form.

11. The method according to claim 10 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of from 0.5 mg to 50 mg.

12. The method according to claim 10 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of from 2.5 mg to 10 mg.

13. The method according to claim 10 , wherein the 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of 0.5 mg, 1 mg, 2.5 mg, 5 mg or 10 mg.

14. The method according to claim 10 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of 1 mg, 2.5 mg or 5 mg.

15. The method according to claim 10 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of 2.5 mg or 5 mg.

16. The method according to claim 10 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of from 2.5 mg to 50 mg.

17. The method according to claim 10 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral daily dose of 5 mg.

18. A method of treating type II diabetes mellitus comprising administering to a patient in need thereof a pharmaceutically effective oral amount of 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine which is an oral daily dose of from 2.5 mg to 10 mg, and a pharmaceutically effective amount of metformin.

19. A method of treating type II diabetes mellitus comprising administering to a patient in need thereof a pharmaceutically effective oral amount of 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine which is an oral daily dose of 5 mg, and a pharmaceutically effective amount of metformin.

20. A method of treating type 2 diabetes or pre-diabetes comprising administering to a patient in need thereof a therapeutically effective oral dose of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine in combination with a therapeutically effective dose of metformin, wherein the 1-[(R4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of from 0.5 mg to 50 mg.

21. The method according to claim 20 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of from 2.5 mg to 50 mg.

22. The method according to claim 20 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of from 2.5 mg to 10 mg.

23. The method according to claim 20 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of 0.5 mg, 1 mg, 2.5 mg, 5 mg or 10 mg.

24. The method according to claim 20 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of 1 mg, 2.5 mg or 5 mg.

25. The method according to claim 20 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral dosage of 2.5 mg or 5 mg.

26. The method according to claim 20 , wherein the 1-[(4-methyl-quinazolin-2-yl)-methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine is administered in an oral daily dose of 5 mg.

Priority Claims (1)
EP 06009203 · May 4, 2006 · regional
Continuity (2)
Continuation 11744703 · May 4, 2007
Related Publication 20110065731A1 · Mar 17, 2011