NEW 5,6-DIHYDROPYRIDINE-2-ON COMPOUNDS APPLICABLE AS THROMBIN INHIBITORS Russian patent published in 2008 - IPC C07D211/98 C07D213/75 C07D401/12 C07D401/14 C07D409/12 A61K31/4412 A61K31/444 A61K31/4436 A61P7/02 

FIELD: chemistry.

SUBSTANCE: invention concerns new compounds of the formula I , where A is S(O)₂ or C_1-6alkylene possibly substituted by one or more fluorine atoms; R¹ is (a) C_1-10alkyl possibly substituted by one or more substitutes of aryl and Het¹, (b) aryl possibly substituted by one or two substitutes selected out of halogeno, C_1-4alkyl, CF₃ and C_1-4alkoxy, or (c) Het³; R^2a, R^2b, R^3a and R^3b are independently H or C_1-3alkyl; R⁴ is (a) H, (b) C_1-6alkyl; R⁵ and R⁶ are independently H, F or methyl; G is (a) -C(O)N(R^8a)-[CH(C(O)R⁹)]_0-1-C_0-3alkylene-(Q¹)_a-, (b) -C(O)N(R^8b)-C_2-3alkenylene-(Q¹)_a-, R⁹ is H; Q¹ is O; a is 0 or 1; L is (a) C_0-6alkylene-R^a, (b) or , (c) ; Ar is phenyl or naphthyl; Het is 5-10-member heterocyclic group including one or two rings and one sulfur or oxygen and/or nitrogen atom as heteroatom; R^11a is H or one or more substitute selected out of halogeno, OH, CN, C_1-6alkyl and C_1-6alkoxy (the last two groups are possibly substituted by one or more substitutes selected out of halogeno, OH, C_1-4alkoxy); R^11c is independently H or one or more substitute selected out of halogeno, OH, CN, C_1-6alkyl, C_1-6alkoxy; R^a, R^b and R^d are independently (a) , (b) , (c) , or (d) or R^b and R^d also can be H; Q³ is O; Q⁴ is O or CH₂; a is 0 or 1; R^13a-R^13b are independently (a) H, (b) C(O)OR¹⁶; R¹⁶ is C_1-10alkyl; R^8a-R^8b and R^14a-R^14d are independently (a) H or (b) C_1-4alkyl (the last group is possibly substituted by one or more substitutes selected out of halogeno and OH), or R^14a and R^14b are independently C(O)O-C_1-6alkyl, or R^14c is (a) C_3-7cycloalkyl, (b) C(O)O-C_1-6alkyl, or R^14c and R^14d together are C_3-6n-alkylene possibly interrupted by O, S, N(H) or N(C_1-4alkyl) and/or substituted by one or more C_1-4alkyl groups; each aryl is independently C_6-10carbocyclic aromatic group which can contain one or two rings and be possibly substituted by one or more substitutes selected out of (a) halogeno, (b) C_1-10alkyl, (c) OR^17a, R^17a is (a) H, (b) C_1-10alkyl; Het¹ and Het³ are independently 4-9-member heterocyclic groups including one or more heteroatom selected out of oxygen, nitrogen and/or sulfur, so that heterocyclic groups can contain one, two or three rings and be possibly substituted by one or more substitutes selected out of (a) halogeno, (b) C_1-10alkyl, (c) =O, (d) OR^19a, R^19a is (a) H, (b) C_1-10alkyl; n, p and q are independently 0, 1 or 2; or its pharmaceutically acceptable salts. Invention also concerns pharmaceutical composition; application; treatment method; method of obtaining compounds of the formula I; and compounds of the formula II, IV, V, VI.

EFFECT: new biologically active compounds with thrombin inhibition effect.

12 cl, 11 ex