| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to new substituted phenoxyacetic acids of general formula 1 possessing the properties of a selective antagonist inhibiting Aadenosine receptor activity. The compounds may be used in preventing and treating central nervous system diseases, such as cognitive disorders, Parkinson's disease, or depression, tumour diseases, inflammatory processes. The invention also refers to an agent for intensification of immune response or action of drug preparations in the combination treatment of the diseases. In general formula, R1, R2 and R3, optionally simultaneously represent hydrogen. C-Calkyl, C-Calkenyl or C-C-alkynyl; R4 represents hydrogen, a halogen atom, hydroxyl, C-Calkyl, C-Calkyloxy; R5 represents hydrogen, C-Calkyl, the group -C(O)R6;R6 represents hydroxyl, C-Calkyloxy, C-Calkenyloxy, C-Calkynyloxy optionally substituted by an amino group wherein the substitutes optionally identical are specified in hydrogen, C-Calkyl optionally substituted by a mono- or dialkylaminogroup, an alkyloxygroup, 5-6-member saturated heterocyclyl containing 1-2 heteroatoms specified in nitrogen and oxygen: pyridyl, phenyl optionally substituted by 1-3 methoxygroups; or optionally substituted 6-member, optionally annulated with 5-member unsaturated heterocyclyl, saturated heterocyclyl containing 2 nitrogen atoms wherein the substitutes are specified in C-Calkyl optionally substituted by 5- member heteroaryl containing 1-3 heteroatoms specified in nitrogen and oxygen; or 6- member optionally saturated heterocyclyl containing 1-2 nitrogen atom optionally substituted by C-Calkyl, oxo, optionally substituted by phenyl; a dashed line with an accompanying continuous linerepresents a single, double or triple bond.EFFECT: preparing new substituted phenoxyacetic acids of general formula 1 possessing the properties of the selective agonist inhibiting Aadenosine receptor activity.15 cl, 3 tbl, 7 ex |
