DERIVATIVES OF 5- OR 6-SUBSTITUTED BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION Russian patent published in 2009 - IPC C07D401/14 C07D401/06 C07D405/14 C07D401/12 A61K31/4184 A61P11/00 A61P31/12 

FIELD: medicine.

SUBSTANCE: invention relates to derivatives of 5- or 6-substituted benzimidazoles, being inhibitory active as regards replication of respiratory syncytial viruses and having formula (I), wherein Q is R^6a, piperidinyl, substituted with R⁶; G is methylene; R¹ is piridyl, substituted with 2 substitutes, chosen from hydroxy, C_1-6alkyl; one of R^2a and R^2b is cyano-C_2-6alkenyl, Ar³C_1-6alkyl, Het-C_1-6alkyl, N(R^8aR^8b)C_1-6alkyl, Ar³C_2-6alkenyl, Ar³-amino-C_1-6alkyl, Het-amino-C_1-6alkyl, Het-C_1-6alkyl-amino-C_1-6alkyl, Ar³tioC_1-6alkyl, Ar³amino-carbonyl, Het-amino-carbonyl, Ar³(CH₂)_ncarbonyl-amino, Het-(CH₂)_ncarbonyl-amino; and the other of R^2a and R^2b represents hydrogen; R³ represents hydrogen or C_1-6alkyl; in the case when R^2a represents hydrogen, R³ represents hydrogen; in the case when R^2b represents hydrogen, R³ represents hydrogen or C_1-6alkyl; R⁵ represents hydrogen; R⁶ represents C_1-6alkyl, optionally substituted with one or two substitutes, each of which is independently chosen from group consisting of NR^7aR^7b, Ar², hydroxy, amino-carbonyl, amino-sulphonyl; R^6a is C_1-6alkyl, substituted with one or two substitutes, each of which is independently chosen from group consisting of Ar², hydroxy or heterocyclic, chosen from a group consisting of piperidinyl, piperazinyl; R^7a represents hydrogen; R^7b represents hydrogen; R^8a represents Ar³, C_1-6alkyl, hydroxyC_1-6alkyl, C_1-6alkoxy C_1-6alkyl, cyanoC_1-6alkyl, di(C_1-6alkyl)aminoC_1-6alkyl, Ar³C_1-6alkyl, HetC_1-6alkyl, amino-carbonyl C_1-6alkyl, carboxylC_1-6alkyl; R^8b represents Ar³, C_1-6alkyl, hydroxyC_1-6alkyl, Ar³C_1-6alkyl, HetC_1-6alkyl; each independently represents 1; Ar¹ represents phenyl; Ar² represents phenyl or phenyl substituted with one C_1-6alkyl-oxy; Ar³ represents phenyl, naphtalenyl, 1,2,3,4-tetra-hydro- naphtalenyl or indanyl, wherein said phenyl, naphtyl, 1,2,3,4- tetra-hydro- naphtalenyl or indanyl can be optionally and each individually substituted with one or more, for example, 2 or 3 substitutes chosen from group consisting of halogen, hydroxy-, mercapto- cyano-, C_1-6alkyl, C_2-6alkinyl, Ar³ , hydroxy-C_1-6alkyl, CF₃, cyano-C_1-6alkyl, amino-carbonyl, C_1-6alkyl-oxy, C_1-6alkyltio, Ar¹-oxy, Ar¹-amino, amino-sulphonyl, amino-carbonylC_1-6alkyl, C_1-4alkyl-carbonyl, C_1-4alkyl-carbonyl-amino and C_1-4alko-oxy-carbonyl; Het represents heterocycle chosen from phuranyl, imidazolyl, morpholinyl, piridyl, quinolene, iso-quinolene, each of said heterocycles can be optionally substituted with hydroxyl-Sibalkyl, as well as to acid additional salt thereof and stereo-chemical isomeric forms. In addition, the invention relates to pharmaceutical composition on the basis of compound of formula I and to application of compound of formula I and for production of medicinal preparation.

EFFECT: new derivatives of benzimidazole having useful biological properties.

22 cl, 6 tbl, 18 ex