WO2013058681A3 - Substituted phenoxyacetic acids and esters and amides thereof, comprising a 2,6-dioxo-2,3,6,7-tetrahydro-1н-purine-8-yl fragment and constituting а2a adenosine receptor antagonists, and the use thereof - Google Patents

Abstract

The invention relates to novel compounds of general formula 1, namely substituted phenoxyacetic acids and esters and amides thereof, which comprise a 2,6-dioxo-2,3,6,7-tetrahydro-1H-purine-8-yl fragment and exhibit antagonist activity against A_2A adenosine receptors, and to the use thereof as a therapeutic principle and agent (adjuvant) for pharmaceutical compositions and drugs, as well as to methods for treating diseases of the central nervous system, oncological diseases and viral and bacterial diseases, where R1, R2 and R3, not necessarily simultaneously, are hydrogen, C1-C5 alkyl, C3-C5 alkenyl or C3-C5 alkynyl; R4 is hydrogen, a halogen atom, a hydroxyl, C1-С3 alkyl, C1-С3 alkyloxy; R5 is hydrogen, C1-C3 alkyl, the group -C(O)R6; and R6 is a hydroxyl, C1-С5 alkyloxy, С3-С5 alkenyloxy, С3-С5 alkynyloxy, an optionally substituted amino group where the substitutes, not necessarily identical, are selected from hydrogen, C1-C5 alkyl optionally substituted with a mono- or dialkylamino group or an alkoxy group or a 5-6 membered saturated heterocyclyl comprising 1-2 heteroatoms selected from nitrogen and oxygen; pyridyl or phenyl optionally substituted with 1-3 methoxy groups; or an optionally substituted 6 membered saturated heterocyclyl optionally annulated with a 5 membered unsaturated heterocyclyl and comprising 2 nitrogen atoms, where the substitutes are selected from С1-С5 alkyl optionally substituted with a 5 membered heteroaryl comprising 1-3 heteroatoms selected from nitrogen and oxygen; or a 6 membered optionally saturated heterocyclyl comprising 1-2 nitrogen atoms optionally substituted with C1-C5 alkyl, oxo, optionally substituted with phenyl; and the broken line with an adjacent unbroken line represents a single, double or triple bond.