FIELD: chemistry.
SUBSTANCE: invention relates to piperidine derivatives of formula 1, where X is C6 aryl C1-4 alkyl; fused 9-membered bicyclic ring in which a C6 aryl ring is fused with a non-aromatic C5 cycloalkyl ring, fused 9-member bicyclic ring in which 6-member heteroaryl ring containing 1-3 N is fused with a non-aromatic C5 cycloalkyl ring; or fused 9-membered bicyclic ring in which the C6 aryl ring is fused with non-aromatic 5-membered heterocyclic ring containing 1-3 O, where X is substituted or not substituted with one or more R1; A is 5-6-membered heteroaryl containing 1-3 heteroatoms selected from the group consisting of N, O and S; L is -(CH2)3; -(CH2)aCO-; -(CH)aCO-; (CH2)bO(CH2)cCO-; or 5-membered aromatic or non-aromatic heterocycle containing 1-3 heteroatoms selected from the group consisting of N and O, where said a, b, c independently represent integer from 1 to 5; B is COOH; CH2COOH; CONHOH; SO2NH2; carboxamido; 4-5-membered non-aromatic heterocycle containing 1-3 heteroatoms selected from the group consisting of N and O; or 5-member heteroaryl containing 1-4 heteroatoms selected from the group consisting of N and O; R1 is halogen or C1-4 alkylsulfonyl; R2 is hydrogen, C1-4 alkyl, C1-4 haloalkyl, hydroxy, oxo (O) or C6 aryl C1-4 alkyl; R3 is hydrogen, C1-4 alkyl, C1-4 alkoxy or halogen; R4 is hydrogen, halogen or C1-4 alkyl; R5 is hydrogen or C1-4 alkyl. Invention also relates to the use of compounds of formula 1 for the manufacture of a medicinal agent for preventing or treating a disease associated with activity of autotaxin, use of compounds of formula 1 for producing a drug for preventing or treating radiation-induced fibrosis and a pharmaceutical composition containing a compound of formula 1. Invention also relates to a piperidine derivative, which is N-(5,6-difluoro-2,3-dihydro-1H-inden-2-yl)-5-(5-(4-morpholinopiperidin-1-yl)-1,3,4-oxadiazol-2-yl)pyrimidin-2-amine.
EFFECT: compounds of formula 1, having inhibitory activity on autotaxin.
18 cl, 71 ex, 1 tbl
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