UREA DERIVATIVE Russian patent published in 2022 - IPC C07C275/28 C07C275/30 C07C275/34 C07C275/42 C07C323/44 C07D207/10 C07D211/06 C07D295/135 C07D333/36 A61K31/198 A61K31/381 A61K31/40 A61K31/4453 A61P13/12 A61P43/00 

FIELD: pharmaceutics.

SUBSTANCE: present invention relates to a pharmaceutical composition, comprising a compound of general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient and at least one pharmaceutically acceptable additive. In formula (I): R¹ and R² are identical or different and represent C₁-C₆ alkyl group, halo C₁-C₆ alkyl group or C₃-C₆ cycloalkyl group; Ar is an optionally substituted phenyl group, the substituents are identical or different and represent from one to two substituents selected from the group, including a fluorine atom, a chlorine atom, a cyano group, C₁-C₆ alkyl group, halo C₁-C₆ alkyl group, cyano C₁-C₆ alkyl group, cyano C₃-C₆ cycloalkyl group, C₁-C₆ alkoxy group , halogen C₁-C₆ alkoxy group, C₁-C₆ alkylthio group, halo C₁-C₆ alkylthio group, saturated cyclic amino group, saturated cyclic halogenoamino group, phenyl group and halogenophenyl group; or Ar is an optionally substituted thienyl group, the substitute is a halogen atom. Also disclosed is a compound of general formula (I) and use thereof, a crystalline form of the compounds, an agent for reducing blood indoxyl sulphate, agent for delaying the transition to renal replacement therapy in a patient during conservative treatment of chronic kidney disease, agent for suppressing deterioration of residual renal function in a patient after switching to renal replacement therapy, a method for reducing blood indoxyl sulphate and a method for preventing or treating a disease caused by an increase in blood indoxyl sulphate.

EFFECT: disclosed pharmaceutical agent is capable of excellent inhibiting tryptophanase and suppressing deterioration of renal function to preserve kidneys by reducing production of indoxyl sulphate in blood.

53 cl, 8 dwg, 12 tbl, 57 ex