DIAMINOPYRROLOQUINAZOLINES DERIVATIVES AS PROTEINTYROSINE PHOSPHATASE INHIBITORS Russian patent published in 2009 - IPC C07D487/04 A61K31/519 A61P3/10 

FIELD: medicine.

SUBSTANCE: new derivative of diaminopyrroloquinazolines of formula (I) and their pharmaceutically acceptable salts possess properties of proteintyrosine posphatase PTP1 inhibitors which can be used for treating the diseases mediated by action of the latter, particularly for decreasing glucose content in blood. In formula (I) , A stands for 6-membered aromatic ring, or 5- or 6-membered aromatic ring which contains 1 or 2 heteroatoms chosen from S, N and O; R₁ is specified from the group including the following radicals: C_1-6alkyl, hydroxyC_1-6alkyl, mono- or dihydroxy-substituted C_1-6alkyl, phenyl-(C_1-6alkyl), benzyloxyC_1-6alkyl and phenyl-(C_1-6alkoxy)C_1-6alkyl; R₂ is specified from the group including the following radicals: hydrogen, C_1-6alkyl, hydroxyC_1-6alkyl, mono- or dihydroxy-substituted C_1-6alkyl, phenyl-(C_1-6alkyl) and phenyl-(C_1-6alkoxy)C_1-6alkyl; R₃ represents hydrogen or methyl; Ra is specified from the group including the following radicals: hydrogen, C_1-6alkyl, C_1-6alkoxy, hydroxyC_1-6alkyl, mono- or dihydroxy-substituted C_1-6alkyl, phenyl(C_1-6alkyl), benzyloxyC_1-6alkyl or ; R₁₀ represents hydrogen or ; x and y separately stand for integers 0 to 4; Rb and Rc are separately specified from the group including the following radicals: hydrogen, C_1-6alkyl, perfluorochemical C_1-6alkyl, substituted C_1-6alkyl, C_1-6alkoxy, phenoxy, halogen, (unsubstituted C_1-6alkyl)-(substituted phenyl)-(C_1-6alkyl), phenyl-(C_1-6alkoxy) or ; R₁₁ represents hydrogen, phenyl or unsubstituted C_1-6alkyl; p stands for integer 0 to 1; Rd represents hydrogen, substituted C_1-6alkyl or perfluorochemical C_1-6alkyl; Re represents hydrogen, halogen, substituted C_1-6alkyl and perfluorochemical C_1-6alkyl; Rf represents hydrogen or C_1-6alkyl; the substitutes found in alkyl groups are independently specified from the following groups: hydroxy, C_1-6alkoxy, C_1-6alkanoyl; and the substitutes found in substituted phenyl as Rb and Rc, are independently specified from the following groups: C_1-6alkyl, C_1-6alkoxy, hydroxyC_1-6alkyl, hydroxyl, hydroxylC_1-6alkoxy, halogen, perfluorC_1-6alkyl and C_1-6alkanoyl.

EFFECT: improved properties of the derivatives.

29 cl, 2 dwg, 48 ex