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Last Updated: March 28, 2024

Claims for Patent: 8,673,927


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Summary for Patent: 8,673,927
Title:Uses of DPP-IV inhibitors
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.
Inventor(s): Dugi; Klaus (Dresden, DE), Himmelsbach; Frank (Mittelbiberach, DE), Mark; Michael (Biberach, DE)
Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:12/946,193
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,673,927
Patent Claims: 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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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)-a- mino-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.

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