NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME FOR TREATMENT OF INFLAMMATORY DISORDERS Russian patent published in 2018 - IPC C07D471/04 A61K31/426 A61K31/437 A61K31/496 A61K31/5377 A61K31/541 A61P35/00 A61P37/00 A61P29/00 A61P25/28 A61P11/00 A61P9/00 

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, specifically to a heterocyclic compound of formula I, where R^1a: H or halogen; R^1b: halogen, C_1-4-alkyl (optionally substituted with three halogens), C_1-4-alkoxy group (optionally substituted with three halogens); X: -S-, -O- or -N=CH-; W: N or CR³, when W is N, R² is H or -CN, when W is CR³, one of R² or R³ represents H, -CN, halogen, C_1-4-alkyl (optionally substituted with one substituent selected from OH or CN), -C(=O)CH₃, -C(=O)CF₃, -C(=O)OCH₃, -C(=O)NH₂, -NHC(=O)CH₃, and the other one is H or C_1-4-alkyl; R⁴: C_1-4-alkyl; R⁵: C_1-4-alkyl optionally substituted with one or three substituents selected from CN, halogen or -C(=O)NH₂; one of R^6a or R^6b is selected from H, -CH₃ and halogen, and the other is H; Cy: 4–6 membered monocyclic heterocycloalkyl containing 1-2 heteroatoms selected from O, N and S, or 5-6 membered heterocycloalkenyl containing 1 double bond containing 1-2 heteroatoms independently selected from O, N and S; R⁷: OH, oxo, halogen and C_1-4-alkyl; the subscript a is 0, 1, or 2; R⁸: -(L₁-W₁)_m-L₂-G₁, where L₁ is absent or represents -C(=O)-, -NRⁱ, -NR^hC(=O)- or -SO₂-; W₁: C_1-4alkylene; the subscript m is 0 or 1; L₂ is absent or represents -O-, -C(=O)-, -C(=O)O-, -OC(=O)-, -C(=O)-C(=O)-, -C(=O)-C(=O)NR^a-, -NR^b-, -C(=O)NR^c-, -SO₂- or -SO₂NR^e-; G₁: H, -CN, C_1-4-alkyl (optionally substituted with one or three substituents selected from -CN, OH, halogen or phenyl), C_3-6-cycloalkyl (optionally substituted with -NH₂), 5-membered heterocycloalkenyl containing 1 double bond, containing 2 heteroatoms independently selected from O and N (optionally substituted with one substituent selected from groups R⁹), 4–6 membered monocyclic heterocycloalkyl containing 1-2 heteroatoms independently selected from O and N (optionally substituted with one or two substituents independently selected from the groups R⁹), or a 5-membered heteroaryl containing 1–4 heteroatoms independently selected from O, N, and S (optionally substituted with one substituent independently selected from the groups R¹⁰), R⁹: oxo or R¹⁰; R¹⁰: -OH, halogen, -CN, C_1-4-alkyl (optionally substituted with one substituent selected from OH or phenyl), C₃-cycloalkyl, -SO₂CH₃, -C(=O)C_1-4-alkoxy, -C(=O)C_1-4-alkyl or -NR^gC(=O)C_1-4-alkyl; and each R^a, R^b, R^c, R^e, R^g, R^h and Rⁱ is independently selected from H and C_1-4-alkyl. Invention also relates to specific compounds, a pharmaceutical composition based on a compound of formula I and use thereof.

I.

EFFECT: obtaining novel heterocyclic compounds with autotaxin inhibitory activity.

15 cl, 9 tbl, 6 ex