NEW BENZyl SUBSTITUTED DERIVATIVES OF 1,4-BENZOTIEPIN-1,1-DIOXIDE, METHOD FOR PRODUCING THEM, MEDICINES CONTAINING SUCH COMPOUNDS, AND THEIR APPLICATION

摘要

1. The compounds of formula I! ! where X is O, NH, CH2 or a bond; ! R1 is (C1-C6) alkyl; ! R2, R2 ', R3, R3', R4, R4 ', R5 and R5' independently are H, Cl, Br, I, OH, - (CH2) -OH, CF3, NO2, N3, CN, S (O) p-R6, OS (O) p-R6, (C1-C6) -alkylene-S (O) p-R6, (C1-C6) -alkylene-OS (O) p-R6, COOH, COO (C1-C6) -alkyl, CONH2, CONH (C1-C6) -alkyl, CON [(C1-C6) -alkyl] 2, (C1-C6) -alkyl, (C2-C6) -alkenyl, (C2- C6) -alkynyl, O- (C1-C6) -alkyl, moreover, in the alkyls one, several or all of the hydrogen atoms may be substituted by fluorine; phenyl, - (CH2) -phenyl, - (CH2) n-phenyl, O-phenyl, O- (CH2) m-phenyl, - (CH2) -O- (CH2) m-phenyl, and phenyl may have from one up to 3 substituents, such as F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O- (C1-C6) -alkyl, (C1-C6) -alkyl, NH2, NH (C1-C6 ) -alkyl, N [(C1-C6) -alkyl] 2, SO2-CH3, COOH, COO- (C1-C6) -alkyl, CONH2; ! wherein at least one of the radicals R2, R2 ', R3, R3', R4, R4 ', R5 and R5' has the meaning -O- (CH2) m-phenyl or - (CH2) -O- (CH2) m- phenyl, while phenyl can have from one to 3 substituents, such as F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O- (C1-C6) -alkyl, (C1-C6) - alkyl, NH2, NH (C1-C6) -alkyl, N [(C1-C6) -alkyl] 2, SO2-CH3, COOH, COO- (C1-C6) -alkyl, CONH2; ! R6 is H, OH, (C1-C6) -alkyl, NH2, NH (C1-C6) -alkyl, N [(C1-C6) -alkyl] 2; ! n is 2, 3, 4, 5, 6; ! m is 1, 2, 3, 4, 5, 6; ! p is 0, 1, 2; ! and their pharmaceutically acceptable salts. ! 2. The compounds of formula I according to claim 1, characterized in that in them! X is O, NH, CH2 or a bond; ! R1 is (C1-C6) alkyl; ! R2, R2 ', R3, R3', R4, R4 ', R5 and R5' independently are H, Cl, Br, I, OH, - (CH2) -OH, CF3, NO2, N3, CN, S (O) p-R6, (C1-C6) -alkylene-S (O) p-R6, COOH, COO (C1-C6) -alkyl, CONH2, CONH (C1-C6) -alkyl, CON [(C1- C6) -alkyl] 2, (C1-C6) -alkyl, (C2-C6) -alkenyl, (C2-C6) -alkynyl, O- (C1-C6) -alkyl, moreover, in alkyls one, several or all atoms hydrogen may be substituted by fluorine; phenyl, - (CH2) -phenyl, - (CH2) n-phenyl, O-phenyl, O- (CH2) m-phenyl, - (CH2) -O- (CH2) m-phenyl, and phenyl may have from one up to 3 substituents, such as F, Cl, Br, I, OH, CF3, NO2, CN, OCF3, O- (C1-C6) -alkyl, (C1-C6) -alkyl, NH2, NH (C1-C6 ) -alkyl, N [(C1-C6) -alkyl] 2, SO2-CH3, COOH, COO- (C1-C6) -alkyl, CONH2; ! pr�