NOVEL PYRIMIDINE DERIVATIVES AND THEIR APPLICATION IN THERAPY, AS WELL AS APPLICATION OF PYRIMIDINE DERIVATIVES IN MANUFACTURING MEDICATION FOR PREVENTION AND/OR TREATMENT OF ALZHEIMER'S DISEASE

摘要

FIELD: medicine, pharmaceutics.;SUBSTANCE: claimed invention relates to novel pyrimidine derivatives or their pharmaceutically acceptable salts, possessing inhibiting activity with respect to glycogensintase kinase-3 (GSK3). In compound of formula I: R¹ is selected from hydrogen, cyano, C_1-3alogenoalkinyl, SO₂NR^bR^c, C_0-2alkyl(O)NR^bR^c, C_1-4alkylNB^bR^c, SO₂Rⁱ, C(O)OR^a, CH(OH)R^j and C(O)R^j; R² and R⁴ are independently selected from hydrogen, halogeno, cyano, NO₂, C_1-4alkyl, C_1-3ahalogenoalkyl, OR^a, C(O)NR^bR^c, SO₂Rⁱ, and C(O)OR^a; or R¹ and R² together with atoms, to which they are bound, are bound with formation of 5- or 6-member heterocyclic ring, which contains one S, any of the hydrogen atoms of group CH₂ in said heterocyclic ring can be substituted by oxo, hydroxy, and sulphur atom in said heterocyclic ring is probably oxydised to -SO₂-; R³ and R⁵ represent hydrogen; R⁶ represents tetrahydropyran; R⁷ is selected from hydrogen, C_1-3alkyl, cyano and C_1-3halogenoalkyl; R⁸ represents hydrogen; R^a is selected from C_1-3alkyl and C_1-3halogenoakryl. Other radicals are given in formula of invention.;EFFECT: compounds can be applied in manufacturing medication for prevention and/or treatment of predemential states, moderate cognitive failure and type II diabetes, Alzheimer's disease and Parkinson disease, as well as bone-associated malfunctions.;40 cl, 3 dwg, 1 tbl, 122 ex