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Details for Patent: 8,232,281

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Details for Patent: 8,232,281

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)
Filing Date:May 04, 2007
Application Number:11/744,703
Claims:1. A method of reducing the risk of a macrovascular complication in the treatment of patients who have been diagnosed with manifest type 2 diabetes comprising the steps of preparing an oral medicament comprising 1-[(4-methyl -quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperid- in-1-yl) -xanthine or one of the salts thereof, and administering said oral medicament to said patient, wherein the oral medicament is a tablet and the amount of said 1-[(4-methyl -quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperid- in-1-yl) -xanthine administered to said patient is 0.5 mg, 1 mg, 2.5 mg, 5 mg, or 10 mg, and wherein the macrovascular complication is myocardial infarction, acute coronary syndrome, unstable angina pectoris, stable angina pectoris, haemorrhagic or ischaemic stroke, peripheral arterial occlusive disease, cardiomyopathy, left heart insufficiency, right heart insufficiency, global heart failure, heart rhythm disorders, or vascular restenosis.

2. The method of claim 1, wherein the medicament further comprises an active substance selected from: metformin, pioglitazone, miglitol, atorvastatin, valsartan and telmisartan.

3. The method of claim 1, wherein the medicament further comprises metformin.

4. The method of claim 1, wherein the medicament further comprises pioglitazone.

5. A method of treating a patient who has been diagnosed with manifest type 2 diabetes comprising administering to the patient an oral medicament in the form of a tablet comprising 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-a- mino-piperidin-1-yl)-xanthine or one of the salts thereof, wherein the amount of said 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-a- mino-piperidin-1-yl)-xanthine administered to said patient is 0.5 mg, 1 mg, 2.5 mg, 5 mg, or 10 mg, and wherein the risk of a macrovascular complication is reduced by using the medicament, and wherein the macrovascular complication is myocardial infarction, acute coronary syndrome, unstable angina pectoris, stable angina pectoris, haemorrhagic or ischaemic stroke, peripheral arterial occlusive disease, cardiomyopathy, left heart insufficiency, right heart insufficiency, global heart failure, heart rhythm disorders, or vascular restenosis.

6. The method of claim 1 wherein the oral medicament further comprises telmisartan.

7. The method of claim 5 further comprising administering an active substance selected from metformin, pioglitazone, miglitol, atorvastatin, valsartan and telmisartan.

8. The method of claim 5 further comprising administering metformin.

9. The method of claim 5 further comprising administering pioglitazone.

10. The method of claim 5 further comprising administering telmisartan.

11. The method of claim 1, wherein the amount of 1-[(4-methyl -quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperid- in-1-yl)-xanthine administered to said patient is a daily dose of 5 mg.

12. The method of claim 5, wherein the amount of 1-[(4-methyl -quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn- 1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine administered to said patient is a daily dose of 5 mg.

13. The method of claim 1, wherein the amount of 1-[(4-methyl -quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperid- in-1-yl)-xanthine administered to said patient is 2.5 mg or 5 mg.

14. The method of claim 5, wherein the amount of 1-[(4-methyl -quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperid- in-1-yl)-xanthine administered to said patient is 2.5 mg or 5 mg.

15. The method of claim 3 wherein metformin is comprised in an amount of about 500 mg, 850 mg, or 1000 mg.

16. The method of claim 3 wherein metformin is comprised in delayed-release form in an amount of about 500 mg, 1000 mg, 1500 mg, or 2000 mg.

17. The method of claim 4 wherein pioglitazone is comprised in an amount of about 15 mg, 30 mg, or 45 mg.

18. The method of claim 6 wherein telmisartan is comprised in an amount from about 20 mg to about 160 mg.

19. The method of claim 5 further comprising administering an active substance selected from: metformin; sulphonylureas selected from glibenclamide, tolbutamide, glimepiride, glipizide, gliquidon, glibornuride and gliclazide; nateglinide; repaglinide; thiazolidinediones selected from rosiglitazone and pioglitazone; alpha-glucosidase blockers selected from acarbose, voglibose and miglitol; insulin and insulin analogues selected from human insulin, insulin lispro, insulin glusilin, r-DNA-insulinaspart, NPH insulin, insulin detemir, insulin zinc suspension and insulin glargin; and GLP-1 and GLP-1 analogues selected from Exendin 4.

20. The method of claim 8 wherein the amount of metformin is about 500 mg, 850 mg, or 1000 mg.

21. The method of claim 8 wherein the amount of metformin is about 500 mg, 1000 mg, 1500 mg, or 2000 mg, each in delayed-release form.

22. The method of claim 9 wherein the amount of pioglitazone is about 15 mg, 30 mg, or 45 mg.

23. The method of claim 10 wherein the amount of telmisartan is from about 20 mg to about 160 mg.

24. A method of reducing the risk of a macrovascular complication in the treatment of patients who have been diagnosed with manifest type 2 diabetes comprising administering to a patient in need thereof an oral medicament in the form of a tablet comprising 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl -7-(2-butyn-1-yl) 8-(3-(R)-amino-piperidin-1-yl)-xanthine in an amount of 2.5 mg or 5 mg, wherein the macrovascular complication is myocardial infarction, acute coronary syndrome, unstable angina pectoris, stable angina pectoris, haemorrhagic or ischaemic stroke, peripheral arterial occlusive disease, cardiomyopathy, left heart insufficiency, right heart insufficiency, global heart failure, heart rhythm disorders, or vascular restenosis.

25. The method of claim 24, wherein the medicament further comprises metformin.

26. The method of claim 24, wherein the medicament further comprises pioglitazone.

27. The method of claim 24, wherein the medicament further comprises telmisartan.

28. The method of claim 25 wherein metformin is comprised in an amount of about 500 mg, 850 mg, or 1000 mg.

29. The method of claim 26 wherein pioglitazone is comprised in an amount of about 15 mg, 30 mg, or 45 mg.

30. The method of claim 27 wherein telmisartan is comprised in an amount of about 20 mg to about 160 mg.

31. The method of claim 25 wherein metformin is comprised in delayed-release form in an amount of about 500 mg, 1000 mg, 1500 mg, or 2000 mg.

32. A method of reducing the risk of a macrovascular complication in the treatment of patients who have been diagnosed with manifest type 2 diabetes comprising administering to a patient in need thereof an oral medicament in the form of a tablet comprising 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl) -8-(3-(R)-amino-piperidin-1-yl)-xanthine in an amount of 5 mg, wherein the macrovascular complication is myocardial infarction, acute coronary syndrome, unstable angina pectoris, stable angina pectoris, haemorrhagic or ischaemic stroke, peripheral arterial occlusive disease, cardiomyopathy, left heart insufficiency, right heart insufficiency, global heart failure, heart rhythm disorders, or vascular restenosis.

33. The method of claim 32 further comprising administering an active substance selected from, metformin; sulphonylureas selected from glibenclamide, tolbutamide, glimepiride, glipizide, gliquidon, glibornuride and gliclazide; nateglinide; repaglinide; thiazolidinediones selected from rosiglitazone and pioglitazone; alpha-glucosidase blockers selected from acarbose, voglibose and miglitol; insulin and insulin analogues selected from human insulin, insulin lispro, insulin glusilin, r-DNA-insulinaspart, NPH insulin, insulin detemir, insulin zinc suspension and insulin glargin; and GLP-1 and GLP-1 analogues selected from Exendin 4.

34. The method of claim 32 further comprising administering an active substance selected from: ACE inhibitors selected from ramipril, lisinopril, cilazapril, quinapril, captopril, enalapril, benazepril, perindopril, fosinopril and trandolapril; angiotensin II receptor blockers (ARBs) selected from telmisartan, candesartan, valsartan, losartan, irbesartan, olmesartan and eprosartan; beta blockers selected from atenolol, bisoprolol, celiprolol, carvedilol, and metoprolol; and diuretics selected from hydrochlorothiazide, chlortalidone, xipamide, furosemide, piretanide, torasemide, spironolactone, eplerenone, amiloride and triamterene.

35. The method of claim 32 further comprising administering an active substance selected from: statins selected from simvastatin, atorvastatin, lovastatin, fluvastatin, pravastatin and rosuvastatin; fibrates selected from bezafibrate, fenofibrate, clofibrate, gemfibrozil, etofibrate and etofyllinclofibrate; cholesterol absorption inhibitors selected from ezetimib; and HDL-raising substances selected from torcetrapib, dalcetrapib and anacetrapib.

36. The method of claim 32 further comprising administering an active substance selected from metformin, pioglitazone, miglitol, atorvastatin, valsartan and telmisartan.

37. The method of claim 32 further comprising administering metformin.

38. The method of claim 32 further comprising administering pioglitazone.

39. The method of claim 32 further comprising administering telmisartan.

40. A method of reducing the risk of a macrovascular complication in the treatment of patients who have been diagnosed with manifest type 2 diabetes comprising administering to a patient in need thereof an oral medicament in the form of a tablet comprising 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl) -8-(3-(R)-amino-piperidin-1-yl)-xanthine, wherein the macrovascular complication is myocardial infarction, acute coronary syndrome, unstable angina pectoris, stable angina pectoris, haemorrhagic or ischaemic stroke, peripheral arterial occlusive disease, cardiomyopathy, left heart insufficiency, right heart insufficiency, global heart failure, heart rhythm disorders, or vascular restenosis, and wherein the total daily dose of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-- (3-(R)-amino-piperidin-1-yl)-xanthine administered is 5 mg.

41. The method of claim 40 further comprising administering an active substance selected from: metformin; sulphonylureas selected from glibenclamide, tolbutamide, glimepiride, glipizide, gliquidon, glibornuride and gliclazide; nateglinide; repaglinid; thiazolidinediones selected from rosiglitazone and pioglitazone; alpha-glucosidase blockers selected from acarbose, voglibose and miglitol; insulin and insulin analogues selected from human insulin, insulin lispro, insulin glusilin, r-DNA-insulinaspart, NPH insulin, insulin detemir, insulin zinc suspension and insulin glargin; and GLP-1 and GLP-1 analogues selected from Exendin 4.

42. The method of claim 40 further comprising administering an active substance selected from: ACE inhibitors selected from ramipril, lisinopril, cilazapril, quinapril, captopril, enalapril, benazepril, perindopril, fosinopril and trandolapril; angiotensin II receptor blockers (ARBs) selected from telmisartan, candesartan, valsartan, losartan, irbesartan, olmesartan and eprosartan; beta blockers selected from atenolol, bisoprolol, celiprolol, carvedilol, and metoprolol; and diuretics selected from hydrochlorothiazide, chlortalidone, xipamide, furosemide, piretanide, torasemide, spironolactone, eplerenone, amiloride and triamterene.

43. The method of claim 40 further comprising administering an active substance selected from: statins selected from simvastatin, atorvastatin, lovastatin, fluvastatin, pravastatin and rosuvastatin; fibrates selected from bezafibrate, fenofibrate, clofibrate, gemfibrozil, etofibrate and etofyllinclofibrate; cholesterol absorption inhibitors selected from ezetimib; and HDL-raising substances selected from torcetrapib, dalcetrapib and anacetrapib.

44. The method of claim 40 further comprising administering an active substance selected from metformin, pioglitazone, miglitol, atorvastatin, valsartan and telmisartan.

45. The method of claim 40 further comprising administering metformin.

46. The method of claim 40 further comprising administering pioglitazone.

47. The method of claim 40 further comprising administering telmisartan.
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