FIELD: pharmaceuticals.
SUBSTANCE: invention relates to a compound of formula (I)
,
in which R1 is: a hydrogen atom, C1-C6 alkyl group optionally substituted with a deuterium atom(s), halogen atom(s), a group(s) -OR13, -NR15R16, -COOR14, cyano, -CONR11R12 or -S(O)nR17, C3-C8 cycloalkyl group, optionally substituted with -OR13, C1-C6 alkoxy-C1-C6 alkyl group, optionally substituted with -OR13, -CONR11R12, 4–6 membered heterocyclyl group containing 1 to 2 nitrogen atoms or an oxygen atom in the ring, optionally substituted with C1-C6 alkyl group, C1-C6 alkoxy-C1-C6 alkyl group, halogen-C1-C6 alkyl group, a benzyl group, C1-C7 acyl group, -COOR14, R13O-C1-C6 alkyl group, -S(O)nR17, 4–6 membered heterocyclyl-C1-C6 alkyl group containing 1–2 heteroatoms in ring selected from nitrogen and oxygen atom, optionally substituted with a halogen atom, C1-C6 alkyl group, C1-C7 acyl group, an oxo group or a protective group selected from tetrahydropyranyl, a benzyl group optionally substituted with C1-C6 alkoxy group; and X is N or CR2, where R2 is: a hydrogen atom, a halogen atom, C1-C6 alkyl group optionally substituted with a halogen atom or C1-C6 alkoxy group, a C3-C8 cycloalkyl group, C1-C6 alkoxy group or a cyano group; p and q, independently of each other, represent a natural number from 1 to 3 with the proviso that the sum of p and q is a natural number from 2 to 4; R11 and R12 independently represent a hydrogen atom or C1-C6 alkyl group; R13 represents a hydrogen atom, C1-C7 acyl group or a protective group selected from tetrahydropyranyl; R14 represents a hydrogen atom or C1-C6 alkyl group; R15 and R16 independently represent a hydrogen atom, C1-C6 alkyl group, a benzyl group, C1-C7 acyl group or -S(O)nR17; R17 is C1-C6 alkyl group; and n is 2; or a pharmacologically acceptable salt thereof, which is a VAP-1 inhibitor.
EFFECT: substituted guanidine derivatives are disclosed.
34 cl, 75 tbl, 122 ex
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