COMPOUNDS, COMPOSITIONS AND METHODS FOR INCREASING CFTR ACTIVITY Russian patent published in 2022 - IPC C07D413/14 C07D407/12 C07D307/54 C07D409/14 C07D413/12 C07D417/12 C07D405/12 C07D261/14 A61K31/341 A61K31/42 A61K31/422 A61P11/00 

FIELD: medicine.

SUBSTANCE: invention relates to a compound represented by the formula III or IV and to its pharmaceutically acceptable salt, where X₁ is N; X₃ is S; pp is 1; R₁₁, independently for each case when it is present, is selected from a group consisting of hydrogen and halogen; R₃₁ is selected from a group consisting of hydrogen and halogen; L₁ is C_3-6 cycloalkylene or C_3-6cycloalkylene-C_1-4alkylene; R₄₄ is 5-element heteroaryl containing one, two or three heteroatoms, each of which is selected from O, N and S; wherein heteroaryl can be optionally substituted with one or two substituents, each of which is independently selected from R_gg; R_gg, for each case when it is present, is selected from a group consisting of halogen, cyano, heterocycle selected from azetidinyl, oxetanyl and dioxidothietanyl, C_1-6 alkyl, wherein C_1-6 alkyl can be optionally substituted with one substituent selected from R_jj; and heterocycle is optionally substituted with one substituent selected from R_ll; R_jj, for each case when it is present, is selected from a group consisting of hydroxyl, C_1-6 alkoxy (optionally substituted with one substituent selected from R_kk), C_3-6 cycloalkoxy and -S(O)_w-C_1-3 alkyl, where w is equal to 2; R_kk, for each case when it is present, is selected from a group consisting of halogen, C_3-6 cycloalkyl, oxetanyl and azetidinyl (optionally substituted with C_1-6 alkyl); R_ll, for each case when it is present, is selected from a group consisting of C_1-6 alkyl (optionally substituted with one, two or three substituents, each of which is independently selected from halogen and C_3-6 cycloalkyl) and piperidinyl (optionally substituted with one substituent selected from C_1-6 alkyl). The invention also relates to a pharmaceutical composition for increasing activity of cystic fibrosis transmembrane conductance regulator (CFTR) based on the specified compounds.

EFFECT: new compounds and a pharmaceutical composition based on them are obtained, which can be used in medicine for the treatment of cystic fibrosis.

16 cl, 2 tbl, 79 ex