NEW THERAPEUTIC USE OF BENZYLIDENEGUANIDINE DERIVATIVES FOR TREATING PROTEOPATHIES Russian patent published in 2020 - IPC C07C281/18 C07D213/61 C07D253/75 A61K31/155 A61K31/165 A61K31/216 A61K31/44 A61K31/53 A61P25/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention refers to using the compound of formula (I) or its pharmaceutically acceptable salt or tautomer as PPP1R15A inhibitor. In formula (I) R₁ means OC_1-12alkyl, Cl, F or Br; R₂H or F; R₃ is H; R₄ is H; R₅ means H; or R₄ and R₅ are combined to form 5–6-member saturated or unsaturated heterocyclic group, optionally containing 1 or 2 heteroatoms, such as N, in addition to those N atoms to which R₄ and R₅, wherein said heterocyclic group is optionally substituted with one or more groups R₁₀; each R₁₀ is independently selected from =O and C_1-12alkyl; X and Z each independently denotes CR₁₁, and Y is selected from CR₁₁ and N; R₁₁ means H or C_1-12alkyl. Invention also relates to use of compound of formula (I) or its pharmaceutically acceptable salt or tautomer, where R₁ means Cl, F or Br; R₂ H or F; R₃ is H; R₄ is H; R₅ means H; or R₄ and R₅ are combined to form 5–6-member saturated or unsaturated heterocyclic group, optionally containing 1 or 2 heteroatoms, such as N, in addition to those N atoms to which R₄ and R₅, wherein said heterocyclic group is optionally substituted with one or more groups R₁₀; each R₁₀ is independently selected from C_1-12alkyl; X and Z each independently denotes CR₁₁, and Y is selected from CR₁₁ and N; R₁₁ means H.

EFFECT: treating a disease associated with exposure to mis-stacking of proteins, particularly accumulation of misfolded proteins, and selected from a group of leukodystrophies.

13 cl, 14 dwg, 1 tbl, 16 ex