- 8-(3-AMINO-PIPERIDIN-1-YL)-XANTHINES, THEIR PREPARATION, AND THEIR USE AS PHARMACEUTICALS
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The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.
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Page/Page column 4
(2008/06/13)
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- METHOD FOR PRODUCING CHIRAL 8-(3-AMINO-PIPERIDIN-1-YL)-XANTHINES
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The invention relates to an improved method for producing enantiomer-free 8-(3-amino-piperidin-1-yl)-xanthines.
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Page/Page column 13
(2008/06/13)
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- 8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINE, THE PRODUCTION THEREOF AND THE USE IN THE FORM OF A DPP INHIBITOR
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The invention relates to substituted xanthines of general formula (I), wherein R is such as defined in claim 1, and to the tautomers, stereoisomers, mixtures and the salts thereof, said products exhibiting precious pharmacological properties, in particular an inhibiting effect on a dipeptidylpeptidasa-IV (DPP-IV) enzyme activity.
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Page/Page column 41
(2008/06/13)
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- Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4- triazolo[3,4-a]phthalazines as GABAA receptor agonists at the α3 subunit
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We have previously identified the 7,8,9,10-tetrahydro-7,10-ethano-1,2,4- triazolo[3,4-a]phthalazine (1) as a potent partial agonist for the 0.3 receptor subtype with 5-fold selectivity in binding affinity over α1. This paper describes a detailed investigation of the substituents on this core structure at both the 3- and 6-positions. Despite evaluating a wide range of groups, the maximum selectivity that could be achieved in terms of affinity for the α3 subtype over the α1 subtype was 12-fold (for 57). Although most analogues showed no selectivity in terms of efficacy, some did show partial agonism at α1 and antagonism at α3 (e.g., 25 and 75). However, two analogues tested (93 and 96), both with triazole substituents in the 6-position, showed significantly higher efficacy for the α3 subtype over the α1 subtype. This was the first indication that selectivity in efficacy in the required direction could be achieved in this series.
- Russell, Michael G. N.,Carling, Robert W.,Atack, John R.,Bromidge, Frances A.,Cook, Susan M.,Hunt, Peter,Isted, Catherine,Lucas, Matt,McKernan, Ruth M.,Mitchinson, Andrew,Moore, Kevin W.,Narquizian, Robert,Macaulay, Alison J.,Thomas, David,Thompson, Sally-Anne,Wafford, Keith A.,Castro, José L.
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p. 1367 - 1383
(2007/10/03)
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