8-(3-amino-piperidin-1-yl)-xanthines, their preparation, and their use as pharmaceuticals
AssigneeBoehringer Ingelheim International GmbH
InventorsWaldemar Pfrengle, Peter Sieger
Life of this patent
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Abstract
The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.
Claims21
A compound which is the monohydrochloride or dihydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine in crystalline anhydrous form.
A compound which is the monohydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine having a melting point of 260° C. to 270° C.
A compound which is the monohydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, and wherein an x-ray powder diagram of the monohydrochloride comprises the characteristic values 2θ=8.51°, 9.83°, 13.01°, 17.07°, 20.00°, 20.60°, 22.33°, 22.61°, 24.91°, and 25.43° with intensities of at least about 10%.
A compound which is the dihydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine having a melting point of 200° C. to 210° C.
A compound which is the dihydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, and wherein an x-ray powder diagram of the dihydrochloride comprises the characteristic values 2θ=7.86°, 10.04°, 11.53°, 12.20°, 15.77°, 18.50°, 21.64°, 26.79°, 29.48°, and 30.16° with intensities of at least about 18%.
A pharmaceutical composition comprising an excipient and a compound which is the monohydrochloride or dihydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine in crystalline anhydrous form.
A pharmaceutical composition comprising an excipient and a compound which is the monohydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine having a melting point of 260° C. to 270° C.
A pharmaceutical composition comprising an excipient and a compound which is the monohydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, and wherein an x-ray powder diagram of the monohydrochloride comprises the characteristic values 2θ=8.51°, 9.83°, 13.01°, 17.07°, 20.00°, 20.60°, 22.33°, 22.61°, 24.91°, and 25.43° with intensities of at least about 10%.
A pharmaceutical composition comprising an excipient and a compound which is the dihydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine having a melting point of 200° C. to 210° C.
A pharmaceutical composition comprising an excipient and a compound which is the dihydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, and wherein an x-ray powder diagram of the dihydrochloride comprises the characteristic values 2θ=7.86°, 10.04°, 11.53°, 12.20°, 15.77°, 18.50°, 21.64°, 26.79°, 29.48°, and 30.16° with intensities of at least about 18%.
A method for treating Type II diabetes mellitus or obesity in a mammal comprising administering to a mammal in need thereof a compound which is the monohydrochloride or dihydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine in crystalline anhydrous form.
A method for treating Type II diabetes mellitus or obesity in a mammal comprising administering to a mammal in need thereof a compound which is the monohydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine having a melting point of 260° C. to 270° C.
A method for treating Type II diabetes mellitus or obesity in a mammal comprising administering to a mammal in need thereof a compound which is the monohydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, and wherein an x-ray powder diagram of the monohydrochloride comprises the characteristic values 2θ=8.51°, 9.83°, 13.01°, 17.07°, 20.00°, 20.60°, 22.33°, 22.61°, 24.91°, and 25.43° with intensities of at least about 10%.
A method for treating Type II diabetes mellitus or obesity in a mammal comprising administering to a mammal in need thereof a compound which is the dihydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine having a melting point of 200° C. to 210° C.
A method for treating Type II diabetes mellitus or obesity in a mammal comprising administering to a mammal in need thereof a compound which is the dihydrochloride salt of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, and wherein an x-ray powder diagram of the dihydrochloride comprises the characteristic values 2θ=7.86°, 10.04°, 11.53°, 12.20°, 15.77°, 18.50°, 21.64°, 26.79°, 29.48°, and 30.16° with intensities of at least about 18%.
Dependencies are inferred from the claim text.