Pfizer Corporation

Stephen Derek Albert Street

Mark Edward Bunnage

John Paul Mathias

Anthony Wood

Keith Michael DeVries

Philip Charles Levett

Albert Shaw Wood

Laurence James Harris

Joanna Teresa Negri

David James Rawson

Graham Nigel Maw

A process for the preparation of Compounds of the formula (1): wherein R, R, Rand Rare as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: are potent and selective inhibitors of type 5 cyclic guanosine 3',5&#x2032;-monophosphate phosphodiestbrase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

Process for preparing pharmaceutically active compounds

Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein Ris Cto Calkyl substituted with Cto Ccycloalkyl, CONRRor a N-linked heterocyclic group; (CH)Het or (CH)Ar, Ris Cto Calkyl; Ris Cto Calkyl optionally substituted with Cto Calkoxy; Ris SONRR; Rand Rare each independently selected from H and Cto Calkyl optionally substituted with Cto Calkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; Rand R, together with the nitrogen atom to which they are attached, form a 4-R-piperazinyl group; Ris H or Cto Calkyl optionally substituted with OH, Cto Calkoxy or CONH; Het is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction

Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3',5&#x2032;-monophosphate phosphodiesterase (cGMP-PDE5) for the treatment of sexual dysfunction

Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R is C to C alkyl substituted with C to C cycloalkyl, CONR R or a N-linked heterocyclic group; (CH ) Het or (CH ) Ar; R is C to C alkyl; R is C to C alkyl optionally substituted with C to C alkoxy; R is SO NR R ; R and R are each independently selected from H and C to C alkyl optionally substituted with C to C alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R and R , together with the nitrogen atom to which they are attached, form a 4-R -piperazinyl group; R is H or C to C alkyl optionally substituted with OH, C to C alkoxy or CONH ; H is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction.

Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3&prime;,5&prime;&mdash;monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction

Pharmaceutically active compounds

Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction

Pyrazolopyrimidinone CGMP PDE5 inhibitors for the treatment of sexual dysfunction

There is provided compounds of formula IA and of formula IB,

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Sandwich, United Kingdom

Stephen Derek Albert Street