8-(piperazin-1yl)- and 8-([1,4]diazepan-1yl)-xanthines, the preparation thereof and their use as pharmaceutical composition
AssigneeBoehringer Ingelheim International GmbH
InventorsFrank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
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Abstract
The present invention relates to substituted xanthines of the general formula in which R1 to R3 and n are as defined in claims 1 to 8, their tautomers, their enantiomers, their diastereomers, their mixtures, their prodrugs and their salts, which have valuable pharmacological properties, in particular an inhibitory action on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Claims16
A compound of formula
- wherein
- R1 is
- (a) a heteroaryl-C1-3-alkyl group,
- wherein heteroaryl is selected from the group consisting of phenylpyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, quinoxalinyl, naphthyridinyl and phenanthridinyl which may be optionally substituted by R10, R11 and R12,
- where R10 is selected from hydrogen, fluorine, chlorine, bromine, methyl, difluoromethyl, trifluoromethyl, phenyl, cyano, methoxy, difluoromethoxy, trifluoromethoxy, amino, methylamino, dimethylamino, pyrrolidin-1-yl, piperidin-1-yl or morpholin-4-yl group;
- R11 is selected from hydrogen, methyl, methoxy or cyano;
- and
- R12 is hydrogen or methyl,
- or
- (b) a naphthyl-C1-3-alkyl group, which may be substituted by R13 and R14,
- where R13 is selected from hydrogen, fluorine, chlorine, bromine methyl, difluoromethyl,
- trifluoromethyl, cyano, methoxy, difluoromethoxy or trifluoromethoxy;
- and
- R14 is selected from hydrogen, methyl, methoxy or cyano;
- R2 is selected from methyl, ethyl, propyl, isopropyl, cyclopropyl or phenyl;
- R3 is selected from 2-butyn-1-yl, 1-buten-1-yl, 2-buten-1-yl or 3-methyl-2-buten-1-yl and
- n is 1 or 2;
- or a tautomer, enantiomer, diastereomer, mixture, prodrug or salt thereof.
A physiologically tolerable salt of a compound according to one of claims l-5 or 8 with at least one inorganic or organic acid.
Dependencies are inferred from the claim text.