Pyrazolopyrimidinone antianginal agents
First Claim
1. A compound of the formula:
- ##STR22## 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 4-N-(R6)-piperazinyl group;
R5 is H, C1 -C4 alkyl, C1 -C3 alkoxy, NR7 R8, or CONR7 R8 ;
R6 is H, C1 -C6 alkyl, (C1 -C3 alkoxy) C2 -C6 alkyl hydroxy C2 -C6 alkyl, (R7 R8 N)C2 -C6 alkyl, (R7 R8 NCO)C1 -C6 alkyl, CONR7 R8, CSNR7 R8 or C(NH)NR7 R8 ;
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.
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Abstract
Compounds of the formula: ##STR1## 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, NR7 R8, or CONR7 R8 ; R6 is H, C1 -C6 alkyl, (C1 -C3 alkoxy) C2 - C6 alkyl, hydroxy C2 -C6 alkyl, (R7 R8 N)C2 -C6 alkyl, (R7 R8 NCO)C1 -C6 alkyl, CONR7 R8, CSNR7 R8 or C(NH)NR7 R8 ; 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.
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8 Claims
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1. A compound of the formula:
- ##STR22## 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 4-N-(R6)-piperazinyl group; R5 is H, C1 -C4 alkyl, C1 -C3 alkoxy, NR7 R8, or CONR7 R8 ; R6 is H, C1 -C6 alkyl, (C1 -C3 alkoxy) C2 -C6 alkyl hydroxy C2 -C6 alkyl, (R7 R8 N)C2 -C6 alkyl, (R7 R8 NCO)C1 -C6 alkyl, CONR7 R8, CSNR7 R8 or C(NH)NR7 R8 ; 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. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
- ##STR22## wherein R1 is H, C1 -C3 alkyl, C3 -C5 cycloalkyl or C1 -C3 perfluoroalkyl;
Specification