PYRAZOLLOPYRIMIDINONE DERIVATIVE, METHOD FOR PREPARING THEREOF AND USE THEREOF

摘要

PURPOSE: A pyrazollopyrimidinone derivative showing an excellent inhibiting effect on 3', 5'-monophosphate specific phosphoesterase, a method for preparing thereof and a use thereof are provided. CONSTITUTION: A pyrazollopyrimidinone derivative is represented by the following formula 1, where R¬1 is one selected from the group consisting of hydrogen, alkyl having 1-3 carbon atoms which is either substituted or unsubstituted by more than one fluorine atoms and cycloalkyl having 3-6 carbon atoms; R¬2 is one selected from the group consisting of hydrogen, hydroxy, alkoxy having 1-3 carbon atoms, cycloalkyl having 3-6 carbon atoms, alkyl having 1-6 carbon atoms which is either substituted or unsubstituted by more than one fluorine atom, alkenyl having 2-6 carbon atoms and alkynyl having 2-6 carbon atoms; R¬3 is one selected from the group consisting of cycloalkyl having 3-6 carbon atoms, alkyl having 1-6 carbon atoms which is either substituted or unsubstituted by more than one fluorine atom, alkenyl having 2-6 carbon atoms and alkynyl having 2-6 carbon atoms; R¬4 is either a SO2NR¬5R¬6 or NHCOR¬7, where each R¬5 and R¬6 forms one selected from the group consisting of pyrollidinyl group, piperidino group, morpholino group and piperazinyl group with a nitrogen atom and each of them is substituted by a substituent of R¬8; and R¬7 is one selected from the group consisting of cycloalkyl having 3-6 carbon atoms, alkyl having 1-6 carbon atoms which is either substituted or unsubstituted by more than one fluorine atom and cycloalkyl having 3-7 carbon atoms, where R¬8 is one selected from the group consisting of CO2H, (alkyl having 1-4 carbon atoms)CO2H, PO(OR¬9)(OR¬10) and (alkyl having 1-4 carbon atoms)PO(OR¬9)(OR¬10), where R¬9 and R¬10 are same or different from each other and each of them is either hydrogen atom or alkyl having 1-4 carbon atoms. The pyrazollopyrimidinone derivative of the formula 1 and pharmaceutically acceptable salt thereof are prepared by a ring-formation reaction of the compound of the following formula 2, where the R¬1, R¬2, R¬3 and R¬4 are same as defined above; R¬11 is either the R¬4 or a precursor of the R¬4. The pharmaceutical composition contains the pyrazollopyrimidinone derivative of the formula 1 or pharmaceutically acceptable salt thereof as an effective ingredient and pharmaceutically acceptable diluent or carrier and the pharmaceutical composition is used for treating diseases caused by the 3', 5'-monophosphate specific phosphoesterase such as impotence, heart attack, heart failure, renal failure, vascular contraction, Raynaud's disease, inflammatory disease, apoplexy, chronic asthma, hyperpiesia, allergic coryza, glaucoma and the like.