SUBSTITUTED CHROMANS Russian patent published in 2020 - IPC C07D491/52 C07D407/12 C07D417/14 A61K31/453 A61K31/353 A61K31/36 A61K31/436 A61K31/4433 A61K31/5377 A61P11/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, where X is CR² and Y is CR³; or X is N and Y is CR³; or X is CR² and Y is N; m is equal to 0; R¹ and R² each independently represent hydrogen, halogen, C₁-C₆ haloalkyl, C₁-C₆ alkyl, -OR^1A or -C(O)OR^1B; each R^1A in each case independently represents hydrogen, C₁-C₆ haloalkyl or C₁-C₆ alkyl; where C₁-C₆ alkyl is substituted with one or two substitutes independently selected from a group consisting of -OR^ZA, -C(O)OR^ZA and G^1A; R^ZA in each case independently represents hydrogen or C₁-C₆ alkyl; and R^1B is hydrogen or C₁-C₆ alkyl; R³ and R¹⁴ each independently represent hydrogen, halogen, C₁-C₆ alkyl or -O-(C₁-C₆ alkyl); R⁴ represents hydrogen, C₁-C₆ haloalkyl or C ₁ -C ₆ alkyl; R⁵ is hydrogen, -C(O)Rⁱ, -C(O)OH, -C(O)O(C₁-C₆ alkyl), -C(O)N(R^h)₂, C₁-C₆ haloalkyl, C₁-C₆ alkyl or G^2A; or R⁴ and R⁵ together with the carbon atom to which they are attached form C₃-C₆ cycloalkyl or 4–6 membered heterocycle, in which one heteroatom is selected from N; wherein each 4–6 membered heterocycle is optionally substituted with 1 group R^p; G^2A, in each case, independently represents cycloalkyl, 4–6 membered heterocycle, in which one or two heteroatoms are selected from N, O or S, phenyl or 5–6 membered heteroaryl containing 1, 2, 3 or 4 heteroatoms selected from N, O or S, each of which is independently unsubstituted or substituted with 1 or 2 independently selected groups R^q; R^p and R^q, in each case, each independently represent C₁-C₆ alkyl, halogen, C₁-C₆ haloalkyl, oxo, -OR^h, -S(O)₂R^h, -C(O)R^h, -C(O)OR^h, -C(O)N(R^h)₂ or -C(O)N(R^h)S(O)₂R^h, where each C₁-C₆ haloalkyl and C₁-C₆ alkyl are optionally substituted with one or two substitutes independently selected from a group consisting of -OR^h; R^h in each case independently represents hydrogen, C₁-C₆ haloalkyl, C₁-C₆ alkyl or G^A, where each C₁-C₆ haloalkyl and C₁-C₆ alkyl are optionally substituted with one or two substitutes independently selected from a group consisting of -OR^j and G^A; Rⁱ in each case independently represents G^A; R⁶ denotes hydrogen; R⁷ is hydrogen or -(C₁-C₆ alkylenyl)-G^3A; R⁸ is hydrogen; each R⁹, R¹⁰ and R¹³ independently represent hydrogen or halogen; each R¹¹ and R¹² independently represent halogen; G^1A, G^3A and G^A, in each case, each independently represent cycloalkyl, indenyl, 3–7-member heterocycle, containing one, two, three or four heteroatoms independently selected from a group consisting of O, N and S, or phenyl, each of which is independently unsubstituted or substituted with 1 or 2 independently selected groups R^s; where R^s in each case independently represents C₁-C₆ alkyl, C₁-C₆ haloalkyl, oxo, -OR^j, -C(O)OR^j, halogen or -(C₁-C₆ alkylenyl)-OR^j; R^j in each case independently represents hydrogen or C₁-C₆ alkyl. Invention also relates to a pharmaceutical composition having modulating activity on a cystic fibrous cell transconductivity regulator (CFTR) based on said compounds.

EFFECT: obtaining novel compounds and a pharmaceutical composition based thereon, which can be used in medicine as agents for treating cystic fibrosis.

66 cl, 3 tbl, 203 ex