| abstract |
This invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of the invention are useful in the treatment and / or prevention of DPP IV-associated diseases (e.g., diabetes, particularly non-insulin dependent diabetes mellitus and impaired glucose tolerance). The present invention also relates to the preparation of the compounds and to pharmaceutical compositions containing them. In the formula, R 1 is H or CN; R 2 is -C (R 3, R 4) - (CH 2) n -R 5, -C (R 3, R 4) -CH 2 -NH-R 6, -C (R 3, R 4) -CH 2 -O-R 7, or tetralinyl, tetrahydroquinolinyl. - or a tetrahydroisoquinolinyl group, optionally substituted with one or three lower or lower alkyl, lower alkoxy, halogen, cyano and / or trifluoromethyl substituents selected from the group consisting of atetralinyl, tetrahydroquinolinyl or tetrahydroisoquinolinyl; R3 is hydrogen, lower alkyl, benzyl, hydroxybenzyl or indolylmethylene; R4 is hydrogen or lower alkyl; or R3 and R4 together with the carbon atom to which they are attached form a - (CH2) 2-5- group; R5 is 5-membered heteroaryl, bicyclic or heterocyclic, or aminophenyl; which may optionally be substituted by one to three groups which may be identical or different; R6 is a) pyridinyl or pyrimidinyl substituted with one or three identical or different aryl and / or heteroaryl groups; wherein the aryl or heteroaryl may be optionally substituted with one to three identical or different substituents; or b) a 5-membered heteroaryl or tricyclic heterocyclic group; which 5-membered heteroaryl or bi- or tricyclic heterocyclic group may be optionally substituted with one to three identical or different groups; R7 is optionally substituted by one to three aminophenyl, naphthyl or quinolinyl substituted with the same or different lower alkyl, lower alkoxy, halogen, cyano and / or trifluoromethyl; X is C (R8, R9) or S; R8 and R9 are independently hydrogen or lower alkyl and n is 0, 1 or 2. O |