NOVEL CONDENSED DERIVATIVES OF IMIDAZOLE, INHIBITORS OF DIPEPTIDYL PEPTIDASE IV, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT AND USING BASED ON THEREOF Russian patent published in 2007 - IPC C07D487/04 A61K31/522 A61P3/00 A61P37/02 

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

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 T¹ 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 (C₂-C₆)-alkenyl group that can comprise one or more substitutes, (C₂-C₆)-alkynyl group, phenyl group that can comprise one or some substitutes chosen from alkyl group or halogen atom or phenyl-(C₁-C₆)-alkyl group; each Z¹ and Z² represents independently nitrogen atom or group of the formula -CR²=; each R¹ and R² represents independently group of the formula -A⁰-A¹-A² wherein A⁰ represents a single bond or (C₁-C₆)-alkylene group that can comprise 1-3 substitutes chosen from group B consisting of given below substitutes; A¹ 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 -SO₂-NR^A-, or group represented by formula -NR^A-SO₂-; each A² and R^A represents independently hydrogen atom, halogen atom, cyano-group, (C₁-C₆)-alkyl group, (C₃-C₈)-cycloalkyl group, (C₂-C₆)-alkenyl group, (C₂-C₆)-alkynyl group, (C₆-C₁₀)-aryl group, 5-10-membered heteroaryl group, 4-8-membered heterocyclic group, 5-10-membered heteroaryl-(C₁-C₆)-alkyl group, (C₆-C₁₀)-aryl-(C₁-C₆)-alkyl group or (C₂-C₇)-alkylcarbonyl group wherein each A² and R^A can comprise independently 1-3 substitutes chosen from the given below group of substitutes D: when Z² represents group of the formula -CR²= then R¹ and R² can form in common 5-7-membered ring with exception cases when: [1] R¹ represents hydrogen atom; Z¹ represents nitrogen atom, and Z² represents group -CH=; and [2] Z¹ represents nitrogen atom and Z² 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, (C₁-C₆)-alkyl group that can comprise one or some substitutes, (C₃-C₈)-cycloalkyl group, (C₂-C₆)-alkenyl group, (C₂-C₆)-alkynyl group, (C₆-C₁₀)-aryl group, 5-10-membered heteroaryl group, 4-8-membered heterocyclic group, (C₁-C)-alkoxy-group, (C₁-C₆)-alkylthio-group, group represented by formula -SO₂-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 (C₁-C₆)-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 -CH₂-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, (C₁-C₆)-alkyl group, (C₃-C₈)-cycloalkyl group, (C₂-C₆)-alkenyl group, (C₂-C₆)-alkynyl group, (C₆-C₁₀)-aryl group, 5-10-membered heteroaryl group, 4-8-membered heterocycle-(C₁-C₆)-alkyl group, (C₆-C₁₀)-aryl-(C₁-C₆)-alkyl group or 5-10-membered heteroaryl-(C₁-C₆)-alkyl group. Also, invention describes inhibitor, pharmaceutical composition, method of treatment and using based on thereof. Invention describes novel compounds possessing useful biological properties.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved method of treatment.

33 cl, 3 tbl, 352 ex