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US 6,642,244 B2Granted
Pyrazolopyridopyrimidine inhibitors of cGMP phosphodiesterase
AssigneeBristol-Myers Squibb Company
InventorsJohn E. Macor, Yingzhi Bi
Life of this patent
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Abstract
Compounds of the formula (I) are useful as inhibitors of cGMP PDE especially Type 5.
Claims20
A compound of the formula (I) or a pharmaceutically-acceptable salt thereof:
- wherein:
- R1 is hydrogen, alkyl or substituted alkyl;
- R2 is hydrogen, halogen, —OR5 or —NR5R6;
- R3 at each occurrence is selected from hydrogen, halogen, alkyl, substituted alkyl and —OR7;
- R4 is hydrogen, alkyl, substituted alkyl, aryl, heteroaryl or heterocyclo, provided, however, that R4 is not hydrogen when Y is —SO2—;
- R5, R6 and R7 are independently selected from hydrogen, alkyl and substituted alkyl;
- Y is —SO2— or —(C═O)— provided, however, that Y is not —SO2— when R4 is hydrogen;
- and
- n is 4.
6 more elements
A compound having the formula,
- or a pharmaceutically-acceptable salt thereof:
- wherein:
- R1 is hydrogen, alkyl, or alkylaryl, the aryl of said alkylaryl being optionally-substituted with OR8;
- R2 is hydrogen, halogen, —OR5 or —NHR6;
- R3a is —O-alkyl or —O-substituted alkyl;
- R4 is five or six-membered heterocyclo, said heterocycle being optionally-substituted with alkyl, NH2, NH(alkyl), or N(alkyl)2;
- R6 is hydrogen, alkyl or alkylaryl, the aryl of said alkylaryl being optionally-substituted with halogen, hydrogen, or alkoxy;
- R8 is hydrogen or alkyl;
- and
- Y is —SO2— or —(C═O)—.
7 more elements
Dependencies are inferred from the claim text.