Pyrazolopyrimidinone antianginal agents

Details Pyrazolopyrimidinone antianginal agents Pyrazolopyrimidinone antianginal agents

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01)

Patent

CA 2044748

Compounds of the formula: (see fig.I) wherein R1 is H, C1-C3 alkyl, C3-C5 cycloalkyl or C1-C3 perfluoroalkyl; R2 is H, C1-C6 alkyl optionally substituted by CH, C1-C3 alkoxy or C3-C6 cycloalkyl, or C1-C3 perfluoroalkyl; R3 is C1-C3 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 CONR7R8R6 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.

Composés de formule : (voir fig. I) où R1 est H, un alkyle en C1-C3, un cycloalkyle en C3-C5 ou un perfluoroalkyle en C1-C3; R2 est H, un alkyle en C1-C6 facultativement substitué par CH, un alcoxy en C1-C3 ou un cycloalkyle en C3-C6 ou un perfluoroalkyle en C1-C3; R3 est un alkyle en C1-C3, un alkényle en C3-C6, un alkynyle en C3-C6, un cycloalkyle en C3-C7, un perfluoroalkyle en C1-C6 ou un (cycloalkyle en C3-C6) alkyle en C1-C6; R4 combiné à l'atome d'azote auquel il est fixé complète un groupe pyrrolidinyle, pipéridino, morpholino ou 4-N-(R6)-pipérazinyle; R5 est H, un alkyle en C1-C4, un alcoxy en C1-C3, NR7R8 ou CONR7R8R6 est H, un alkyle en C1-C6, un (alcoxy en C1-C3)alkyle en C2-C6, un hydroxyalkyle en C2-C6 , (R7R8N)alkyle en C2-C6, (R7R8NCO)alkyle en C1-C6, CONR7R8, CSNR7R8 ou C(NH)NR7R8; R7 et R8 sont chacun indépendamment H, un alkyle en C1-C4, un (alcoxy en C1-C3)alkyle en C2-C4 ou un hydroxyalkyle en C2-C4; et sels pharmaceutiquement acceptables de ces derniers; ces composés sont des inhibiteurs sélectifs de la GMPc phosphodiestérase (PDE) utiles dans le traitement des affections cardio-vasculaires comme l'angine, l'hypertension, l'insuffisance cardiaque et l'athérosclérose.

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