EP0463756A1 — Pyrazolopyrimidinone antianginal agents

USPTO Abstract

Compounds of the formula: wherein R¹ is H, C₁-C₃ alkyl, C₃-C₅ cycloalkyl or C₁-C₃ perfluoroalkyl; R² is H, C₁-C₆ alkyl optionally substituted by OH, C₁-C₃ alkoxy or C₃-C₆ cycloalkyl, or C₁-C₃ perfluoroalkyl; R³ is C₁-C₆ alkyl, C₃-C₆ alkenyl, C₃-C₆ alkynyl, C₃-C₇ cycloalkyl, C₁-C₆ perfluoroalkyl or (C₃-C₆ cycloalkyl)C₁-C₆ alkyl; R⁴ taken together with the nitrogen atom to which it is attached completes a pyrrolidinyl, piperidino, morpholino, or 4-N-(R⁶)-piperazinyl group; R⁵ is H, C₁-C₄ alkyl, C₁-C₃ alkoxy, NR⁷R⁸, or CONR⁷R⁸; R⁶ is H, C₁-C₆ alkyl, (C₁-C₃ alkoxy) C₂-C₆ alkyl, hydroxy C₂-C₆ alkyl, (R⁷R⁸N)C₂-C₆ alkyl, (R⁷R⁸NCO)C₁-C₆ alkyl, CONR⁷R⁸, CSNR⁷R⁸ or C(NH)NR⁷R⁸; R⁷ and R⁸ are each independently H, C₁-C₄ alkyl, (C₁-C₃ alkoxy)C₂-C₄ alkyl or hydroxy C₂-C₄ alkyl; and pharmaceutically acceptable salts thereof, are selective cGMP PDE inhibitors useful in the treatment of cardiovascular disorders such as angina, hypertension, heart failure and atherosclerosis.