8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
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First Claim
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1. A pharmaceutical composition comprising a first compound of the formula (I):
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Abstract
The present invention relates to substituted xanthines of general formula
wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
279 Citations
48 Claims
- 1. A pharmaceutical composition comprising a first compound of the formula (I):
- 15. A method of treating type II diabetes mellitus or obesity comprising administering to a patient in need thereof a pharmaceutically effective amount of a first compound
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35. A method of treating type II diabetes mellitus or obesity comprising administering to a patient in need thereof a pharmaceutically effective 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 an other therapeutic agent selected from metformin, sulphonylureas, nateglinide, repaglinide, thiazolidinediones, PPAR-gamma agonists and antagonists, PPAR-gamma/alpha modulators, alpha-glucosidase inhibitors, other DPPIV inhibitors, alpha2 antagonists, insulin, GLP-1, exendin-4, amylin, SGLT2 inhibitors, inhibitors of protein tyrosine phosphatase 1, inhibitors of glucose-6-phosphatase, inhibitors of fructose-1,6-bisphosphatase, inhibitors of glycogen phosphorylase, glucagon receptor antagonists, inhibitors of phosphoenolpyruvate carboxykinase, inhibitors of glycogen synthase kinase, inhibitors of pyruvate dehydrokinase, HMG-CoA-reductase inhibitors, bezafibrate, fenofibrate, nicotinic acid, PPAR-alpha agonists, PPAR-delta agonists, ACAT inhibitors, cholesterol resorption inhibitors, bile acid-binding substances, inhibitors of ileac bile acid transport, inhibitors of CETP, regulators of ABC1, sibutramin, tetrahydrolipostatin, antagonists of the cannabinoid 1 receptor, MCH-1 receptor antagonists, MC4 receptor agonists, NPY5 or NPY2 antagonists, β - 3-agonists, agonists of the 5HT2c receptor,AII antagonists, ACE inhibitors, diuretics, and β
-blockers.
- 3-agonists, agonists of the 5HT2c receptor,AII antagonists, ACE inhibitors, diuretics, and β
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36. A method of treating type II diabetes mellitus or obesity comprising administering to a patient in need thereof a pharmaceutically effective amount of 1-[(4-methyl-quinazolin-2-yl)]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, in combination with
a pharmaceutically effective amount of another therapeutic agent selected from metformin, sulphonylureas, nateglinide, repaglinide, thiazolidinediones, PPAR-gamma agonists, alpha-glucosidase inhibitors, alpha2 antagonists, insulin, GLP-1, exendin-4 and amylin.
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37. A method of treating type II diabetes mellitus or obesity comprising administering to a patient in need thereof a pharmaceutically effective amount 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 pharmaceutically effective amount of an other therapeutic agent selected from inhibitors of protein tyrosine phosphatase 1, inhibitors of glucose-6-phosphatase, inhibitors of fructose-1,6-bisphosphatase, inhibitors of glycogen phosphorylase, glucagon receptor antagonists, inhibitors of phosphoenolpyruvate carboxykinase, glycogen synthase kinase or pyruvate dehydrokinase, HMG-CoA-reductase inhibitors, bezafibrate, fenofibrate, nicotinic acid, cholesterol resorption inhibitors, bile acid-binding substances, inhibitors of CETP, regulators of ABC1, sibutramin, tetrahydrolipostatin, and β - 3-agonists.
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38. A method of treating type II diabetes mellitus or obesity comprising administering to a patient in need thereof a pharmaceutically effective amount 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 pharmaceutically effective amount of a drug for treating high blood pressure selected from AII antagonists, ACE inhibitors, diuretics, and β - -blockers.
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39. A method of treating type II diabetes mellitus comprising administering to a patient in need thereof a pharmaceutically effective 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 an antidiabetic selected from metformin, sulphonylureas, nateglinide, repaglinide, thiazolidinediones, PPAR-gamma agonists, alpha-glucosidase inhibitors, insulin, GLP-1 and exendin-4.
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40. A pharmaceutical composition comprising 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, and
an antidiabetic selected from metformin, sulphonylureas, nateglinide, repaglinide, thiazolidinediones, PPAR-gamma agonists, and alpha-glucosidase inhibitors.
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41. A method of treating type II diabetes mellitus comprising administering to a patient in need thereof a pharmaceutically effective 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 an antidiabetic selected from metformin, a sulphonylurea, and a thiazolidinedione.
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43. A method of treating type II diabetes mellitus comprising administering to a patient in need thereof a pharmaceutically effective 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 an antidiabetic selected from metformin, a sulphonylurea, nateglinide, repaglinide, a thiazolidinedione, a PPAR-gamma agonist, an alpha-glucosidase inhibitor and insulin.
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44. A pharmaceutical composition comprising 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine and metformin
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45. A method of treating type II diabetes mellitus comprising administering to a patient in need thereof a pharmaceutically effective 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 metformin
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46. A pharmaceutical composition comprising 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1 -yl)-8-(3-(R)-amino-piperidin-1 -yl)-xanthine and pioglitazone.
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47. A method of treating type II diabetes mellitus comprising administering to a patient in need thereof a pharmaceutically effective 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 pioglitazone.
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48. A method of treating type II diabetes mellitus comprising administering to a patient in need thereof a pharmaceutically effective 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 sulphonylurea.
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Litigation Data
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Current AssigneeBoehringer Ingelheim International GmbH (C.H. Boehringer Sohn AG & Co. KG)
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Original AssigneeBoehringer Ingelheim Pharma GmbH & Company Kg (C.H. Boehringer Sohn AG & Co. KG)
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InventorsHimmelsbach, Frank, Langkopf, Elke, Eckhardt, Matthias, Mark, Michael, Maier, Roland, Lotz, Ralf, Tadayyon, Mohammad
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Primary Examiner(s)BERCH, MARK L
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Application NumberUS12/143,128Publication NumberTime in Patent Office1,425 DaysField of Search514/234.2, 514/263.2, 514/263.21, 514/263.22, 514/263.23, 514/263.31, 514/263.32US Class Current514/263.21CPC Class CodesA61P 13/12 of the kidneysA61P 19/02 for joint disorders, e.g. a...A61P 25/02 for peripheral neuropathiesA61P 27/02 Ophthalmic agentsA61P 3/04 Anorexiants; Antiobesity ag...A61P 3/10 for hyperglycaemia, e.g. an...C07D 473/04 two oxygen atomsC07D 473/06 with radicals containing on...C07D 473/08 with methyl radicals in pos...C07D 519/00 Heterocyclic compounds cont...
