| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: novel derivatives of 4-phenyltetrahydroisoquinolines have total formula I: , in which R1, R2, R3 and R4 independently on each other represent H, F, CI, Br, I, alkyl with 1, 2, 3 or 4 C-atoms; R5 represents H, alkyl with 1, 2, 3 or 4 C-atoms; R6 represents H, alkyl with 1, 2, 3 or 4 C-atoms; R7, R8 and R9 independently on each other represent H, COOR60, -L-G; R60 represents H, alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms; L represents -NR30CO-, -CONR30-, -NR30CONR31-, -NR30COO-; and R30 and R31 independently on each other represent H; G represents groups Ca(OR32)xH2a+1-x, and one or more CH2-groups can be substituted with O; Cb(OR32)yH2b-1-y,and one or more CH2-groups can be substituted with O; CcH2c+1 and two or more CH2- groups can be substituted with O; -(CH2)z-COOR34, where atom of H group -(CH2)z - can be substituted with group OR32; -CR38R39-COOR40, -(CH2)Z-SO3R34; -(CH2)z-N+R35R36R37; -CR38R39NR41R42; a is equal 2, 3, 4, 5 or 6; x is equal 2, 3, 4, or 5 R32 represents H; b is equal 6; y is equal 4; c is equal 5; z is equal 1 or 2; R34, R35, R36 and R37 independently on each other represent H or alkyl with 1, 2, 3, 4, 5 or 6 C-atoms; R38 represents -(CH2)n-Y; n is equal 1 or 3; Y represents H, -COOR44, -CONR45R46, -NHC(NH)NH2, imidazole -4-yl; R44, R45 and R46 independently on each other represent H; R39 represents H; R40 represents H, alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms; R41 and R42 independently on each other represent H; and, at least, one of residues of R7, R8 or R9 must represent group -L-G, as well as their pharmaceutically acceptable salts and salts of trifluoroacetic acid. Invention also relates to medication and its application for treatment and prevention of number of diseases. ^ EFFECT: novel derivatives of 4-phenyltetrahydroisoquinalines, which have inhibiting effect on NHE3. ^ 14 cl, 2 tbl, 47 ex |
