| abstract |
FIELD: chemistry. n SUBSTANCE: invention relates to the field of organic chemistry, namely to benzoimidazole derivatives of formula (I), as well as to their enantiomers, diastereoisomers, racemates and pharmaceutically acceptable salts, where n equals from 2 to 4, each of R 1 substituents is independently selected from H, halogen, -C 1-4 alkyl, -C 1-4 pergaloalkyl, trifluoro-C 1-4 alkoxy, -NO 2 , -CN, CO 2 H, -OC 1-4 alkyl, -SC 1-4 alkyl, -S(C 1-4 alkyl)-R c , -S(O) 2 (C 1-4 alkyl)-R c , -S(O)-C 1-4 alkyl, -SO 2 -C 1-4 alkyl, -S-R c , -S(O)-R c , -SO 2 -R c , -SO 2 -NH-R c , -O-R c , -CH 2 -O-R c , -C(O)NH-R c , -NR a R b , benzyloxy, phenyl, optionally substituted with one-two R d , cyanobiphenyl-4-ylmethylsulpfanyl, cyanobiphenyl-4-ylmethanesulphonyl, or -S-(CH 2 ) 2 -morpholine and two adjacent groups R 1 can bind with formation of an aromatic 5-6-membered ring, optionally substituted with one methyl group or two atoms of halogen, optionally containing one or two S or N; R a and R b each independently represents C 1-4 alkyl, -C(O)C 1-4 alkyl, -C(O)-R c , -C(O)CH 2 -R e , C 1-4 alkyl-R e , -SO 2 -R c , -SO 2 -C 1-4 alkyl, phenyl, benzyl; or R a and R b together with a nitrogen atom, which they are bound with, form a monocyclic 5-6- membered heterocycloalkyl ring, optionally containing one heteroatom, selected from O; R c represents -C 3-8 cycloalkyl, phenyl, optionally substituted with one-two R d , benzyl, optionally substituted with one-three R d ; morpholine; R d independently represents halogen, -OH, -C 1-4 alkyl or -C 1-4 perhalogenalkyl, trifluorine C 1-4 alcoxy, -OC 1-4 alkyl, or -O-benzyl optionally substituted with halogen, R e represents -C 6 heterocycloalkyl, optionally containing one or two of O or N atoms, optionally substituted with a methyl group; R 2 and R 3 both represent H, -CF 3 or C 1-3 alkyl; each of Z represents a C or N atom, on condition that simultaneously not more than two Z represent N. The invention also relates to particular compounds, a pharmaceutical composition, based on formula (I) compound or a particular said compound, a method of treating diseases, mediated by propyl hydroxylase activity. n EFFECT: novel derivatives of benzimidazole, possessing an inhibiting activity with respect to PHD are obtained. n 11 cl, 1 tbl, 186 ex |