FIELD: medicine; pharmaceutics.
SUBSTANCE: invention relates to a compound of formula (I) or pharmaceutically acceptable salts thereof, which have inhibitory activity on IL-17. In formula (I), R1 is selected from a group consisting of 5-membered heteroaryl, which contains from 2 to 3 heteroatoms selected from N, O and S, 9- or 10-membered bicyclic heteroaryl, which contains from 2 to 3 heteroatoms , selected from N, O and S, phenyl, (C1-C6) alkoxy, (C3-C7) cycloalkoxy, (C1-C6) alkyl, phenyl-(C1-C4) alkyl, (C3-C7) cycloalkyl and -NRcRd, where said 5-membered heteroaryl, 9- or 10-membered bicyclic heteroaryl, phenyl, (C1-C6) alkoxy, (C3-C7) cycloalkoxy, (C1-C6) alkyl, phenyl-(C1-C4) alkyl and (C3-C7) cycloalkyl is optionally substituted with one or more substitutes independently selected from Ra; Ra is halogen, hydroxy, -NRcRd, (C1-C6) alkyl, (C3-C7) cycloalkyl, phenyl, 5- or 6-member heteroaryl, which contains from 1 to 3 heteroatoms, selected from N, O and S, or 4-6 membered heterocycloalkyl, which contains 1 heteroatom selected from O, where said (C1-C6) alkyl, (C3-C7) cycloalkyl, phenyl, 5- or 6-membered heteroaryl and 4-6-membered heterocycloalkyl are optionally substituted with one or more substitutes independently selected from halogen, hydroxy, cyano, (C1-C4) alkyl, (C3-C7) cycloalkyl, -SO2-(C1-C4) alkyl and -NRcRd; R2 is selected from a group consisting of 5- or 6-member heteroaryl, which contains from 1 to 3 heteroatoms selected from N, O and S, where said 5- or 6-member heteroaryl is optionally substituted with one or more substitutes independently selected from Rb, wherein said 5- or 6-membered heteroaryl optionally may contain -CO- as a ring member, and wherein when said 5-member heteroaryl contains nitrogen as a ring atom, said nitrogen can optionally be substituted with a substituent selected from R8; Rb is hydroxy, -NRcRd, (C1-C6) alkyl, (C1-C6) alkoxy or (C3-C7) cycloalkyl, where said (C1-C6) alkyl, (C1-C6) alkoxy or (C3-C7) cycloalkyl is optionally substituted with one or more substitutes, independently selected from deuterium, halogen, cyano and hydroxy; Rc and Rd are each independently selected from a group consisting of hydrogen and (C1-C6) alkyl, or Rc and Rd together form pyrrolidinyl or piperidinyl, where said (C1-C6) alkyl, pyrrolidinyl or piperidinyl is optionally substituted with one or more substitutes independently selected from hydroxy; R8 is selected from a group consisting of -L-PO(OH)2 and -CHRgO-(CO-A-NRh)m-CO-A-NRhRi, L is selected from a group consisting of -CHRgO-, m is 0 or 1; where each -CO-A-NRh- is an amino acid residue selected from -CO-CH(CH(CH3)2)-NRh-; Rg, Rh and Ri are independently selected from hydrogen and (C1-C6) alkyl; R3 is selected from hydrogen, hydroxy and halogen; R4 is hydrogen; R5 is -CHR6R7, where each R6 and R7 is independently (C3-C7) cycloalkyl, optionally substituted with one or more substitutes independently selected from halogen, cyano and (C1-C4) alkyl. Invention also relates to a pharmaceutical composition containing a compound of formula (I).
EFFECT: compound of formula (I) has inhibitory activity on IL-17.
19 cl, 1 tbl, 2 dwg, 485 ex
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