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 Russian patent published in 2011 - IPC C07D405/14 A61K31/506 A61K31/5377 A61P25/16 A61P25/28 A61P3/10 

Abstract RU 2433128 C2

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, C1-3alogenoalkinyl, SO2NRbRc, C0-2alkyl(O)NRbRc, C1-4alkylNBbRc, SO2Ri, C(O)ORa, CH(OH)Rj and C(O)Rj; R2 and R4 are independently selected from hydrogen, halogeno, cyano, NO2, C1-4alkyl, C1-3ahalogenoalkyl, ORa, C(O)NRbRc, SO2Ri, and C(O)ORa; 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, C1-3alkyl, cyano and C1-3halogenoalkyl; R8 represents hydrogen; Ra is selected from C1-3alkyl and C1-3halogenoakryl. 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

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RU 2 433 128 C2

Authors

Andersson Lars

Arzel' Ehrvan

Berg Stefan

Barrouz Dzheremi

Khell'Berg Sven

Khuehrta Fernando

Pedersen Torben

Rejn Tobias

Rottichchi Did'E

Staaf Karin

Turek Dominika

Dates

2011-11-10Published

2006-10-02Filed