FIELD: organic chemistry; pharmaceuticals.
SUBSTANCE: group of inventions relates to new compounds that inhibit apoptotic signal-regulating kinase 1 (ASK-1). The following is disclosed: the compounds of formula I or a pharmaceutically acceptable salt thereof, wherein
selected from the group consisting of
represents
or
;
represents
; R1 is selected from the group consisting of the following: 1) hydrogen; 2) -C1-C6 alkyl; 3) halogen -C1-C6 alkyl; and 4) -C3-C6 cycloalkyl; R2 represents
X represents either N or CR3; R3 is selected from the group consisting of the following: 1) hydrogen; 2) halogen; 3) -C1-C6 alkyl; and 4) -C1-C6 alkoxy; R4 is selected from the group consisting of the following: 1) hydrogen; 2) halogen; 3) -C1-C6 alkyl; 4) halogen-C1-C6 alkyl; and 5) -N(R5)(R6); where R5 and R6 are combined with the nitrogen atom to which they are attached to form a 3–8 membered heterocycloalkyl containing 1 nitrogen atom, 2 nitrogen atoms or a nitrogen atom and an oxygen atom, optionally substituted with a C1-C4-alkyl. In addition, a pharmaceutical composition for the treatment of an ASK-1-mediated disease or condition based on the above compounds is disclosed, as well as the use of the said compounds for the treatment of an ASK-1-mediated disease or condition.
EFFECT: group of inventions provides effective inhibition of apoptotic signal-regulating kinase 1 (ASK-1).
11 cl, 1 tbl, 84 ex
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