168464-61-7Relevant academic research and scientific papers
Pyrazolopyrimidine Derivatives
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, (2008/06/13)
Pyrazolo[3,4-d]pyrimidin-4-one derivatives of formula (I) and salts and solvates thereof are described, in which:, R1 represents arylmethyl or C1 6alkyl optionally substituted by one or more fluorine atoms;, R2 represents methyl;, R3 represents C2 4alkyl;, R4 represents nitro, cyano, C1 6alkoxy, C(=X)NR6R7, NR8R9, (CH2)mNR10C(=Y)R11 or a 5-membered heterocyclic ring selected from thienyl, thiazolyl and 1,2,4-triazolyl each ring optionally substituted by a C1 4alkyl or aryl group; or when R1 is arylmethyl or C1 6alkyl substituted by one or more fluorine atoms then R4 may also represent hydrogen;, R5 represents hydrogen or C1 6alkyl;, R6 represents hydrogen or C1 6alkyl;, R7 represents hydrogen, amino, hydroxyl, C1 6alkyl, aryl or arylC1 4alkyl;, R8 represents hydrogen or C1 6alkyl;, R9 represents hydrogen, C1 6alkyl, SO2R12, CO2R12, C(=NCN)SR12 or C(=NCN)NR13R14;, R10 represents hydrogen or C1 6alkyl;, R11 represents C1 6alkyl optionally substituted by one or more halogen atoms, or R11 represents aryl, arylC1 4alkyl, thienyl, NR15R16, CH2NR17R18 or R10 and R11 together represent -A(CH2)n-;, R12 represents C1 6alkyl, aryl or arylC1 4alkyl;, R13 represents hydrogen or C1 6alkyl;, R14 represents hydrogen, C1 6alkyl, aryl, arylC1 4alkyl or R13 and R14 together with the nitrogen atom to which they are attached form a morpholine, piperazine or N-C1 4alkylpiperazine ring;, R15 represents hydrogen or C1 6alkyl or R10 and R15 together represent -A(CH2)n-;, R16 represents hydrogen, C1 6alkyl, aryl, arylC1 4alkyl, CO2R12, CH2CO2R12 or R15 and R16 together with the nitrogen atom to which they are attached form a morpholine, piperazine or N-C1 4alkylpiperazine ring;, R17 represents hydrogen or C1 6alkyl;, R18 represents hydrogen, C1 6alkyl, aryl, arylC1 4alkyl, COR12 or R17 and R18 together with the nitrogen atom to which they are attached form a morpholine, piperazine or N-C1 4alkylpiperazine ring;, A represents CH2 or C=O;, m represents zero or 1;, n represents 1,2 or 3;, X represents S or NH, or when R7 represents amino then X may also represent O;, Y represents O or S; for use in therapy. These compounds are potent and selective inhibitors of cyclic guanosine 3',5'-monophosphate specific phosphodiesterase (cGMP specific PDE) and are useful in a variety of therapeutic areas, including the treatment of cardiovascular disorders.
