PYRIMIDINE COMPOUND (VARIANTS) AND PHARMACEUTICAL COMPOSITION SHOWING AFFINITY TO DOPAMINE D-RECEPTORS Russian patent published in 2001 - IPC

FIELD: organic chemistry, heterocyclic compounds, pharmacology. SUBSTANCE: invention relates to novel pyrimidine compounds or their salts with pharmaceutically acceptable acids and to pharmaceutical composition based on thereof. Proposed compounds are selective ligands of dopamine D₃- receptors that interfere selectively to limbic system because of their low affinity with D₂-receptors and show less adverse effects as compared with classic neuroleptics. Compounds can be used in pharmaceutical industry for treatment of patients with diseases associated with antagonists of dopamine D₃-receptors or as substances showing affinity to D₃-receptors, for example, central nervous system disorders, in part, schizophrenia, depression, neurosis and psychosis and for treatment of sleep disorders and as antihistaminic agents. Pyrimidine compounds correspond to the general structural formulas (I) and (I'), respectively where B means residues of the formula (a) , (b) and (d) ; A means alkylene that can include or be bound with pyrimidine ring through O, S, NR⁴,CONR⁴,NR⁴CO, COO, OCO and double or triple bond; R¹,R²,R³ are taken independently among the group: H, NR⁴R⁵,OR⁴,SR⁴,CF₃,CO₂R⁴ and C_1-4-alkyl; R⁴ is hydrogen atom, C_1-4-alkyl; R⁵ has values of R⁴; Ar means phenyl, pyridyl, pyrimidinyl, triazinyl that can be substituted and condensed with or 5-6- membered nonaromatic carbocyclic ring possibly substituted with C_1-4- -alkyl. Invention relates to also the pharmaceutical composition showing affinity to D₁-receptors and includes pyrimidine compound of the formula (I) as an active substance and physiologically acceptable vehicle and/or accessory substance. EFFECT: new compound indicated above, valuable medicinal and pharmacological properties. 21 cl, 10 tbl, 7 ex