| abstract |
FIELD: medicine, pharmaceutics. n SUBSTANCE: invention refers to new phenylamide or pyridylamide derivatives of formula n or their acceptable salts, wherein A 1 is CR 12 or N; A 2 is CR 13 or N; R 1 and R 2 are independently specified in hydrogen, C 1-7 -alkyl, halogen and C 1-7 -alkoxygroup; R 12 and R 13 are independently specified in hydrogen, C 1-7 -alkyl, halogen, C 1-7 -alkoxygroup, amino group and C 1-7 -alkylsulphanyl; R 3 is specified in hydrogen, C 1-7 -alkyl, halogen, C 1-7 -alkoxygroup, cyano group, C 3-7 -cycloalkyl, five-merous heteroaryl and phenyl; R 4 is specified in methyl and ethyl; or R 3 and R 4 together represent -X-(CR 14 R 15 ) n - and form a part of the ring, wherein X is specified in -CR 16 R 17 -, O, S, C=O; R 14 and R 15 are independently specified in hydrogen or C 1-7 -alkyl; R 16 and R 17 are independently specified in hydrogen, C 1-7 -alkoxycarbonyl, heterocyclyl substituted by two groups specified in a halogen, or R 16 and R 17 together with an atom C, which they are attached to, form =CH 2 group; or X is specified in a group NR 18 ; R 14 and R 15 are hydrogen; R 18 is specified in hydrogen, C 1-7 -alkyl, halogen-C 1-7 -alkyl, C 3-7 -cycloalkyl, C 3-7 -cycloalkyl-C 1-7 -alkyl, heterocyclyl, heteroaryl-C 1-7 -alkyl, carboxyl-C 1-7 -alkyl, C 1-7 -alkoxycarbonyl-C 1-7 -alkyl, C 1-7 -alkylcarbonyloxy-C 1-7 -alkyl, phenyl, wherein phenyl is unsubstituted, phenylcarbonyl, wherein phenyl is substituted by C 1-7 -alkoxycarbonyl, and phenylsulphonyl, wherein phenyl is substituted by carboxyl-C 1-7 -alkyl, or R 18 and R 14 together represent -(CH 2 ) 3 - and form a part of the ring, or R 18 together with R 14 and R 15 represent -CH=CH-CH= and form a part of the ring; and n has the value of 1, 2 or 3; B 1 represents N or CR 19 and B 2 represents N or CR 20 , provided no more than one of B 1 and B 2 represents N; and R 19 and R 20 are independently specified in a group consisting of hydrogen and halogen-C 1-7 -alkyl; R 5 and R 6 are independently specified in a group consisting of hydrogen, halogen and cyano group; and one-three, provided R 4 represents methyl or ethyl, two of the residues R 7 , R 8 , R 9 , R 10 and R 11 are specified in C 1-7 -alkyl, halogen, halogen-C 1-7 -alkyl, halogen-C 1-7 -alkoxygroup, cyano group, C 1-7 -alkoxycarbonyl, hydroxy-C 3-7 -alkynyl, carboxyl-C 1-7 -alkyl, carboxyl-C 2-7 -alkenyl, C 1-7 -alkoxycarbonyl-C 2-7 -alkenyl, C 1-7 -alkoxycarbonyl-C 2-7 -alkynyl, C 1-7 -alkoxycarbonyl-C 1-7 -alkylaminocarbonyl, carboxyl-C 1-7 -alkylaminocarbonyl-C 1-7 -alkyl, carboxyl-C 1-7 -alkyl-(C 1-7 -alkylamino)-carbonyl-C 1-7 -alkyl, phenyl-carbonyl, wherein phenyl is unsubstituted, phenyl-C 1-7 -alkyl, wherein phenyl is substituted by 1-2 groups specified in a halogen, C 1-7 -alkoxygroup, carboxyl, phenyl-C 2-7 -alkynyl, wherein phenyl is substituted by 2 groups specified in halogen, carboxyl or C 1-7 -alkoxycarbonyl, and pyrrolidine carbonyl-C 1-7 -alkyl, wherein pyrrolidinyl is substituted by carboxyl, and the other R 7 , R 8 , R 9 , R 10 and R 11 represent hydrogen; the term 'heteroaryl' means an aromatic 5-merous ring containing one or two atoms specified in nitrogen or oxygen; the term 'heterocyclyl' means a saturated 4-merous ring, which can contain one atom specified in nitrogen or oxygen. Besides, the invention refers to a pharmaceutical composition based on the compound of formula I. n EFFECT: there are prepared new compounds possessing the GPBAR1 agonist activity. n 21 cl, 1 tbl, 190 ex |