| abstract |
FIELD: organic chemistry, medicine, biochemistry, pharmacy. n SUBSTANCE: invention relates to novel condensed derivatives of imidazole that are inhibitors of dipeptidyl peptidase IV. Invention describes compound represented by the following formula (I): or its salt or hydrate wherein T 1 represents monocyclic 5-6-membered heterocyclic group comprising one or two nitrogen atoms in ring that can comprise one or more amino-groups as substitutes; X represents (C 2 -C 6 )-alkenyl group that can comprise one or more substitutes, (C 2 -C 6 )-alkynyl group, phenyl group that can comprise one or some substitutes chosen from alkyl group or halogen atom or phenyl-(C 1 -C 6 )-alkyl group; each Z 1 and Z 2 represents independently nitrogen atom or group of the formula -CR 2 =; each R 1 and R 2 represents independently group of the formula -A 0 -A 1 -A 2 wherein A 0 represents a single bond or (C 1 -C 6 )-alkylene group that can comprise 1-3 substitutes chosen from group B consisting of given below substitutes; A 1 represents a single bond, oxygen atom, sulfur atom, sulfinyl group, sulfonyl group, carbonyl group, group represented by formula -O-CO-, group represented by formula -CO-O-, group represented by formula -NR A -, group represented by formula -CO-NR A -, group represented by formula -NR A -CO-, group represented by formula -SO 2 -NR A -, or group represented by formula -NR A -SO 2 -; each A 2 and R A represents independently hydrogen atom, halogen atom, cyano-group, (C 1 -C 6 )-alkyl group, (C 3 -C 8 )-cycloalkyl group, (C 2 -C 6 )-alkenyl group, (C 2 -C 6 )-alkynyl group, (C 6 -C 10 )-aryl group, 5-10-membered heteroaryl group, 4-8-membered heterocyclic group, 5-10-membered heteroaryl-(C 1 -C 6 )-alkyl group, (C 6 -C 10 )-aryl-(C 1 -C 6 )-alkyl group or (C 2 -C 7 )-alkylcarbonyl group wherein each A 2 and R A can comprise independently 1-3 substitutes chosen from the given below group of substitutes D: when Z 2 represents group of the formula -CR 2 = then R 1 and R 2 can form in common 5-7-membered ring with exception cases when: [1] R 1 represents hydrogen atom; Z 1 represents nitrogen atom, and Z 2 represents group -CH=; and [2] Z 1 represents nitrogen atom and Z 2 represents group -C(OH)=; <group of substitutes B>. Group of substitutes B represents group comprising: hydroxyl group, mercapto-group, cyano-group, nitro-group, halogen atom, trifluoromethyl group, (C 1 -C 6 )-alkyl group that can comprise one or some substitutes, (C 3 -C 8 )-cycloalkyl group, (C 2 -C 6 )-alkenyl group, (C 2 -C 6 )-alkynyl group, (C 6 -C 10 )-aryl group, 5-10-membered heteroaryl group, 4-8-membered heterocyclic group, (C 1 -C)-alkoxy-group, (C 1 -C 6 )-alkylthio-group, group represented by formula -SO 2 -NR B1 -R B2 , group represented by formula -NR B1 -CO-R B2 , group represented by formula -NR B1 -R B2 (wherein each R B1 and R B2 represents independently hydrogen atom or (C 1 -C 6 )-alkyl group), group represented by formula -CO-R B3 (wherein R B3 represents 4-8-membered heterocyclic group), group represented by formula -CO-R B4 -R B5 , and group represented by formula -CH 2 -CO-R B4 -R B5 wherein R B4 represents a single bond, oxygen atom or group represented by formula -NR B6 - wherein each R B5 and R B6 represents independently hydrogen atom, (C 1 -C 6 )-alkyl group, (C 3 -C 8 )-cycloalkyl group, (C 2 -C 6 )-alkenyl group, (C 2 -C 6 )-alkynyl group, (C 6 -C 10 )-aryl group, 5-10-membered heteroaryl group, 4-8-membered heterocycle-(C 1 -C 6 )-alkyl group, (C 6 -C 10 )-aryl-(C 1 -C 6 )-alkyl group or 5-10-membered heteroaryl-(C 1 -C 6 )-alkyl group. Also, invention describes inhibitor, pharmaceutical composition, method of treatment and using based on thereof. Invention describes novel compounds possessing useful biological properties. n EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved method of treatment. n 33 cl, 3 tbl, 352 ex |