5-Substituted pyrazolo[4,3-d]pyrimidine-7-ones and methods of use
First Claim
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1. A compound of the formula ##STR8## wherein R1 is lower alkyl of from one to six carbons, inclusive, lower alkenyl of from two to six carbons, inclusive, lower hydroxyalkyl of from one to six carbons, inclusive, lower hydroxyalkenyl of from two to six carbons, inclusive, dimethylaminoethyl or lower amino alkenyl of from two to six carbons, inclusive;
- n is 0-4; and
Ar is ##STR9## or 2, 3, or 4-pyridyl, wherein X, Y, and Z are independently (1) hydrogen;
(2) lower alkyl of from one to six carbons, inclusive;
(3) halogen;
(4) hydroxyl;
(5) lower alkoxy of from one to six carbons, inclusive;
(6) nitro;
(7) amino;
(8) NR'"'"'R" wherein R'"'"' and R" are each independently (a) hydrogen or (b) lower alkyl of from one to six carbons, inclusive, optionally substituted by (i) amino, (ii) morpholino or (iii) cycloalkyl of from five to seven carbons, inclusive;
(9) sulfo;
or (10) --SO2 NR'"'"'R" wherein R'"'"' and R" are as defined above with the proviso that not all of X, Y, and Z can be nitro, amino, or NR'"'"'R" at once; and
pharmaceutically acceptable salts thereof.
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Abstract
The present invention relates to novel 5-substituted pyrazolo[4,3-d]pyrimidine-7-one compounds, and compositions, methods of use and processes to make therefor. The novel compounds are useful in the treatment of cardiovascular disorders, such as heart failure or cardiac insufficiency. The novel compounds bind adenosine receptors and selectively inhibit phosphodiesterase.
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31 Claims
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1. A compound of the formula ##STR8## wherein R1 is lower alkyl of from one to six carbons, inclusive, lower alkenyl of from two to six carbons, inclusive, lower hydroxyalkyl of from one to six carbons, inclusive, lower hydroxyalkenyl of from two to six carbons, inclusive, dimethylaminoethyl or lower amino alkenyl of from two to six carbons, inclusive;
- n is 0-4; and
Ar is ##STR9## or 2, 3, or 4-pyridyl, wherein X, Y, and Z are independently (1) hydrogen;
(2) lower alkyl of from one to six carbons, inclusive;
(3) halogen;
(4) hydroxyl;
(5) lower alkoxy of from one to six carbons, inclusive;
(6) nitro;
(7) amino;
(8) NR'"'"'R" wherein R'"'"' and R" are each independently (a) hydrogen or (b) lower alkyl of from one to six carbons, inclusive, optionally substituted by (i) amino, (ii) morpholino or (iii) cycloalkyl of from five to seven carbons, inclusive;
(9) sulfo;
or (10) --SO2 NR'"'"'R" wherein R'"'"' and R" are as defined above with the proviso that not all of X, Y, and Z can be nitro, amino, or NR'"'"'R" at once; and
pharmaceutically acceptable salts thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31)
- n is 0-4; and
Specification