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Details for Patent: 8,664,232

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Details for Patent: 8,664,232

Title:8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
Abstract: The present invention relates to substituted xanthines of general formula ##STR00001## wherein R.sup.1 to R.sup.3 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).
Inventor(s): Himmelsbach; Frank (Mittelbiberach, DE), Langkopf; Elke (Biberach an der Riss, DE), Eckhardt; Matthias (Biberach an der Riss, DE), Mark; Michael (Biberach an der Riss, DE), Maier; Roland (Biberach an der Riss, DE), Lotz; Ralf R. H. (Schemmerhofen, DE), Tadayyon; Mohammad (Hertford, GB)
Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG (Ingelheim am Rhein, DE)
Filing Date:Apr 17, 2012
Application Number:13/448,495
Claims:1. A method of treating a diabetic complication comprising administering to a patient in need thereof a pharmaceutically effective amount of a compound of the formula ##STR00006## wherein R.sup.1 denotes a 4-methyl-2-quinazolinylmethyl group; R.sup.2 denotes a methyl group; and R.sup.3 denotes a 2-butyn-1-yl group; or an enantiomer, mixture thereof, or a salt thereof, optionally in conjunction with an other active substance selected from antidiabetics, lipid lowering agents, HDL-raising compounds, active substances for the treatment of obesity, and drugs for treating high blood pressure, and wherein the diabetic complication is selected from diabetic retinopathy, diabetic nephropathy, and diabetic neuropathy.

2. A method of treating a diabetic complication 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)-a- mino-piperidin-1-yl)-xanthine or a physiologically acceptable salt thereof with an inorganic or organic acid, optionally in conjunction with an other active substance selected from antidiabetics, lipid lowering agents, HDL-raising compounds, active substances for the treatment of obesity, and drugs for treating high blood pressure, and wherein the diabetic complication is selected from diabetic retinopathy, diabetic nephropathy, and diabetic neuropathy.

3. The method according to claim 1, wherein the compound of formula (I) is a physiologically acceptable salt formed with an inorganic or organic acid.

4. The method of claim 1, wherein said diabetic complication is diabetic retinopathy.

5. The method of claim 1, wherein said diabetic complication is diabetic nephropathy.

6. The method of claim 1, wherein said diabetic complication is diabetic neuropathy.

7. A method of treating a diabetic complication 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)-a- mino-piperidin-1-yl)-xanthine, wherein the diabetic complication is selected from diabetic retinopathy, diabetic nephropathy, and diabetic neuropathy.

8. The method of claim 7, wherein said diabetic complication is diabetic retinopathy.

9. The method of claim 7, wherein said diabetic complication is diabetic nephropathy.

10. The method of claim 7, wherein said diabetic complication is diabetic neuropathy.

11. A method of treating a diabetic complication comprising administering to a patient in need thereof a pharmaceutical composition 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 a physiologically acceptable salt thereof with an inorganic or organic acid, optionally together with one or more inert carriers and/or diluents, and wherein the diabetic complication is selected from diabetic retinopathy, diabetic nephropathy, and diabetic neuropathy.

12. A method of treating a diabetic complication comprising administering to a patient in need thereof a pharmaceutical composition comprising 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-a- mino-piperidin-1-yl)-xanthine, optionally together with one or more inert carriers and/or diluents, and wherein the diabetic complication is selected from diabetic retinopathy, diabetic nephropathy, and diabetic neuropathy.

13. The method of claim 12, wherein said diabetic complication is diabetic retinopathy.

14. The method of claim 12, wherein said diabetic complication is diabetic nephropathy.

15. The method of claim 12, wherein said diabetic complication is diabetic neuropathy.
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