PYRAZOLOPYRIMIDINONS INHIBITING CYCLIC GUANOSINE 3', 5'-MONOPHOSPHATE PHOSPHODIESTERASE TYPE 5 (cGMP PDE5), FOR THE TREATMENT OF SEXUAL DYSFUNCTION

摘要

The compounds are powerful and selective cGMP PDE5 inhibitors, useful in the threatment of male erection and female sexual dysfunction. They have the formulae where R1 is C1 to C3 alkyl substituted with C3 to C6 cycloalkyl, CONR5R6 or N-bound heterocyclic group; (CH2)nHet or (CH2)nAr; R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1-C4 alkoxy; R4 is SO2NR7R8; R5 and R6 are independently selected from H and C1 to C4 alkyl, optionally substituted with C1 to C4 alkoxy or together with the nitrogen atom to which they are adjuncted form 5- or 6-member heterocaclic group; R7 & R8 together with the nitrogen atom to which they are adjuncted for 4-R10-piperazinyl group; R10 is H, or C1 to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; Het is optionally substituted C-bound 5- or 6-member heterocyclic group, Ar is optionally substituted; and n has the value of 0 or 1. The invention also relates to veterinary acceptable salts and solvates of the above compounds. 18 claims