PYRAZOLOPYRIMIDINONE COMPOUNDS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT Russian patent published in 1998 - IPC

FIELD: organic chemistry, heterocyclic compounds, biochemistry. SUBSTANCE: products: new derivatives of pyrazolo-[4,3-d]-pyrimidine-7-one of the formula (I) where R¹ - H, CH₃,C₂H₅; R² - CH₃,CH₂OH,CH₂OCH₃ or n-C₃H₇; R³ - C₂H₅, CH₂=CH-CH₂; R⁴ together with nitrogen atom to which it is bound forms 4-R⁵-piperidino- or 4-N-(R⁶)-piperazyl group; R⁵ - H, N-(CH₃)₂,CONH₂; R⁶ - H, CH₃, i-C₃H₇,CH₂CH₂OH,CSNH₂,C(NH)NHCH₃ or C(NH)S-CH₃, and their pharmaceutically acceptable salts. Invention relates to also pharmaceutical composition showing inhibitory activity with respect to cyclic guanosine-3',5'-monophosphate phosphodiesterase that has 1-400 mg of compound of the formula (I) per a single dose in mixture with pharmaceutically acceptable vehicle or carrier. Invention relates to also a method of treatment or prophylaxis of states caused by phosphodiesterase activity by prescription to human an effective dose of compound of the formula (I) or its pharmaceutically acceptable salt of above indicated composition. Invention relates to also intermediate compounds of formulas (II) and (IV) where R¹,R²,R³ have values given above. In compounds of the formula (II) radical R³ can mean atom H and Y - atom Cl. EFFECT: improved method of synthesis of new compounds, enhanced effectiveness. 9 cl, 2 tbl