Claims for Patent: 10,034,877

Summary for Patent: 10,034,877

Title:	Treatment for diabetes in patients inappropriate for metformin therapy
Abstract:	The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients for whom metformin therapy is inappropriate due to intolerability or contraindication against metformin.
Inventor(s):	Dugi; Klaus (London, GB), Graefe-Mody; Eva Ulrike (Ingelheim am Rhein, DE), Harper; Ruth (Reading, GB), Woerle; Hans-Juergen (Munich, DE)
Assignee:	Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:	15/287,228
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,034,877
Patent Claims:	1. A method of treating metabolic diseases in a patient for whom metformin therapy is inappropriate due to at least one contraindication against metformin comprising orally administering to the patient 5 mg of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-a- mino-piperidin-1-yl)-xanthine per day wherein the contraindication is selected from the group consisting of: renal disease, renal impairment or renal dysfunction, unstable or acute congestive heart failure, acute or chronic metabolic acidosis, and hereditary galactose intolerance, wherein no adjustment of the daily dose is required for 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-a- mino-piperidin-1-yl)-xanthine in a patient with mild, moderate or severe renal impairment or end-stage renal disease. 2. The method according to claim 1 wherein the patient is ineligible for metformin therapy due to contraindication against metformin. 3. The method according to claim 1 wherein the patient is in need of reduced dose metformin therapy due to contraindication against metformin. 4. The method according to claim 1 wherein the metabolic disease is type 2 diabetes mellitus. 5. The method according to claim 1 wherein the contraindication is renal disease, renal impairment or renal dysfunction. 6. The method according to claim 1 wherein the metabolic disorder is type 2 diabetes mellitus and wherein the contraindication is renal disease, renal impairment or renal dysfunction, and wherein said 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-a- mino-piperidin-1-yl)-xanthine is used for said patient in the same dose as for a patient with normal renal function. 7. The method according to claim 1 wherein the contraindication is mild, moderate or severe renal impairment or end-stage renal disease. 8. The method according to claim 1 further comprising administering the 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 one or more further active substances selected from antidiabetics, active substances that lower the blood sugar level, active substances that lower the lipid level in the blood, active substances that raise the HDL level in the blood, active substances that lower the blood pressure, active substances that are indicated in the treatment of atherosclerosis, and active substances that are indicated in the treatment of obesity. 9. The method according to claim 1 further comprising administering the 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 one or more further active substances selected from sulphonylureas, thiazolidinediones, glinides, alpha-glucosidase blockers, GLP-1 and GLP-1 analogues, and insulin and insulin analogues. 10. The method according to claim 1 further comprising administering the 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 one or more further active substances selected from repaglinide, pioglitazone, and insulin and insulin analogues. 11. The method according to claim 1 further comprising administering the 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 pioglitazone. 12. A method of treating 2 diabetes mellitus in a patient for whom metformin therapy is inappropriate due to at least one contraindication against metformin comprising orally administering to the patient 5 mg of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-a- mino-piperidin-1-yl)-xanthine per day, wherein the contraindication is selected from the group consisting of: renal disease, renal impairment or renal dysfunction, and acute or chronic metabolic acidosis, wherein no adjustment of the daily dose is required in patients with mild, moderate, or severe renal impairment or end-stage renal disease. 13. A method of treating 2 diabetes mellitus in a patient for whom metformin therapy is inappropriate due to at least one contraindication against metformin comprising orally administering to the patient 5 mg of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-a- mino-piperidin-1-yl)-xanthine per day, wherein the contraindication is selected from the group consisting of severe renal impairment or end-stage renal disease, wherein no adjustment of the daily dose is required in patients with severe renal impairment or end-stage renal disease. 14. The method according to claim 12, wherein the contraindication is severe renal impairment, acute metabolic acidosis, or chronic metabolic acidosis. 15. A method of treating 2 diabetes mellitus in a patient having renal impairment and for whom metformin therapy is contraindicated for renal impairment, comprising orally administering to the patient 5 mg of 1-[(4-methyl-quinazolin-2-yl)-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-pi- peridin-1-yl)-xanthine per day, wherein the daily dose of 1-[(4-methyl-quinazolin-2-yl)-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-pi- peridin-1-yl)-xanthine administered to the renally-impaired patient is the same as the daily dose of 1-[(4-methyl-quinazolin-2-yl)-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-pi- peridin-1-yl)-xanthine administered to a patient with normal renal function. 16. The method according to claim 15, wherein the renal impairment is severe renal impairment. 17. The method according to claim 15 or 16, wherein the patient is ineligible for metformin therapy.