PRODRUG 1,3-DIAMINO-2-HYDROXYPROPANE DERIVATIVES Russian patent published in 2009 - IPC C07D263/32 C07D277/30 C07C321/14 C07C311/09 C07C317/50 C07C237/06 C07C233/65 C07C237/22 A61K31/421 A61K31/426 A61K31/166 A61K31/18 A61K31/24 

FIELD: chemistry.

SUBSTANCE: invention relates to the compounds of the formula and their pharmaceutically acceptable salts used as inhibiting agent in the relation of fermentative beta-secretase and it also relates to pharmaceutical compositions based on the formula. In general formula one of R_N and R_N' represents hydrogen, and another represents - C(=O)-(CRR')_0-6R₁₀₀, or where R₄ is chosen from the group including H; NH₂; -NR₅₀CO₂R₅₁; -(C₁-C₄)-alkyl-NR₅₀CO₂R₅₁; where n₇ is equal to 0, 1, 2 or 3; R₅₀ represents H or C₁-C₆alkyl; R₅₁ is chosen from the group including phenyl-(C₁-C₄)-alkyl and (C₁-C₆)-alkyl; X is chosen from the group including -(C₁-C₆)-alkylidenyl optionally substituted with 1, 2 or 3 metal groups; Z is chosen from the group including bond, SO₂, SO and S; Y stands for (C₁-C₁₀)-alkyl; R₁ represents -(C₁-C₆)-alkylphenyl where phenyl ring is optionally substituted by 1, 2, 3 or 4 halogen atoms; R and R' independently represent hydrogen or (C₁-C₆)-alkyl; R₂ represents hydrogen; R₃ represents hydrogen; R_c represents - (CR₂₄₅R₂₅₀)_0-4-aryl; where aryl is optionally substituted by 1, 2 or 3 R₂₀₀; R₂₀₀ is chosen from the group including (C₁-C₆)-alkyl optionally substituted with 1, 2 or 3 groups R₂₀₅; halogen; C=N; R₂₀₅ stands for halogen; R₂₄₅ and R₂₅₀ in each case stands for H; either R₂₄₅ or R₂₅₀ are taken together with carbon atom whereto attached to form carbocycle from 3, 4, 5, 6 or 7 carbon atoms; R₁₀₀ represents 5-6-merous heteroaryl with 1-2 heteroatoms chosen from nitrogen and sulphur, -phenyl-W-heteroaryl where heteroaryl is 5-6-merous ring containing 1-2 heteroatoms, chosen from nitrogen and oxygen and where cyclic parts of each group are optionally substituted by 1, 2 or 3 groups independently chosen among C₁-C₆alkyl, -(CH₂)_0-4-CO₂-NR₁₀₅R'₁₀₅, -(CH₂)_0-4-SO₂-NR₁₀₅R'₁₀₅, -(CH₂)_0-4-N(R₁₅₀)-CO-R₁₀₅, -(CH₂)_0-4-N(R₁₅₀)-SO₂-R₁₀₅; W represents -(CH₂)_0-4; R₁₀₅ and R'₁₀₅ independently represent (C₁-C₆)-alkyl optionally substituted with -NH₂ or halogen; R₁₅₀ represents hydrogen.

EFFECT: compounds can be applied to prevent and treat diseases mediated by excess activity of beta-secretase such as Alzheimer's disease.

11 cl, 12 tbl, 3 dwg, 1729 ex