AMINOBENZIMIDAZOLES AND BENZIMIDAZOLES AS INHIBITORS OF REPLICATION OF RESPIRATORY SYNCYTIAL VIRUS Russian patent published in 2010 - IPC C07D401/06 C07D401/14 C07D405/14 C07D401/12 A61K31/4184 A61P11/00 A61P31/12 

FIELD: chemistry.

SUBSTANCE: present invention relates to novel derivatives of aminobenzimidazole and benzimidazole of general formula (I-b-1), additive salt or stereochemically isomeric form thereof, where G is a single bond or C_1-10alkanediyl; R¹ is halogenphenyl, pyridyl, pyrazinyl, quinolinyl, benzimidazoly or a radical of formula (c-4), where each of the said monocyclic or bicyclic heterorings can be optionally substituted with 1, 2 or 3 substitutes, independently selected from a group consisting of halogen, hydroxy, C_1-6alkyl, C_1-6alkyloxy, Ar¹C_1-6alkyloxy, C_1-6alkyloxy-CH₂-CH₂-O-; m equals 2; Q is hydrogen, amino or mono(C_1-4alkyl)amino; R^3b is hydrogen or C_1-6alkyl; R^4a is selected from a group of substitutes consisting of hydrogen, Ar²C_1-6alkyl, Het- C_1-6alkyl, hydroxy C_1-6alkyl, (hydroxyC_1-6alkyl)oxy C_1-6alkyl, C_1-6alkyl, (Ar¹C_1-6alkyloxy)(hydroxy)C_1-6alkyl, aminoC_1-6alkyl, mono- and di(C_1-6alkyl)amino-C_1-6alkyl, carboxyl-C_1-6alkyl, C_1-6alkyloxycarbonyl C_1-6alkyl, aminocarbonylC_1-6alkyl, (C_1-4alkyloxy)₂-P(=O)-C_1-6alkyl, aminosulphonylC_1-6alkyl; R^6a is hydrogen or C_1-6alkyl; R^6b is hydrogen, C_1-6alkyl, Ar¹ or Ar¹C_1-6alkyl; R^6c is C_1-6alkyl; Alk is C_1-6alkanediyl; R⁹, R¹⁰, R¹¹ are each independently selected from halogen, cyano, C_1-6alkyl, Het-C_1-6alkyl, Ar¹C_1-6alkyl, cyano C_1-6alkyl, C_2-6alkenyl, R^6b-O-C_3-6alkenyl, C_2-6alkynyl, Ar¹, R^6b-O-, R^6b-S-, R^6b-O- C_1-6alkyl-SO₂-, polyhalo-C_1-6alkyl, polyhaloC_1-6alkyloxy, polyhaloC_1-6alkylthio, R^6c-C(=O)-, R^6b-O-C(=O)-, N(R^6aR^6b)-C(=O)-, R^6b-O-C_1-6alkyl, R^6b-O-C(=O)-C_1-6alkyl, N(R^6aR^6b)-C(=O)-C_1-6alkyl, R^6c-C(=O)-NR^6b-, N(R^6aR^6b)-S(=O)₂-, H₂N-C(=NH)-, and R¹⁰ and/or R¹¹ can also be hydrogen; Ar¹ is phenyl; Ar² is phenyl; Het is a heteroring selected from imidazolyl or morpholinyl. The invention also relates to a pharmaceutical composition based on formula (I-b-1) compound, use of formula (I-b-1) compound to prepare a medicinal agent and a method of producing formula (I-b-1) compound.

EFFECT: novel aminobenzimidazole and benzimidazole derivatives with antiviral activity are obtained.

15 cl, 8 tbl, 31 ex