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Details for Patent: 5,250,534

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Summary for Patent: 5,250,534

Title: Pyrazolopyrimidinone antianginal agents
Abstract:Compounds of the formula: ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.5 cycloalkyl or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.2 is H, C.sub.1 -C.sub.6 alkyl optionally substituted by OH, C.sub.1 -C.sub.3 alkoxy or C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 perfluoroalkyl or (C.sub.3 -C.sub.6 cycloalkyl)C.sub.1 -C.sub.6 alkyl; R.sup.4 taken together with the nitrogen atom to which it is attached completes a pyrrolidinyl, piperidino, morpholino, or 4-N-(R.sup.6)-piperazinyl group; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, NR.sup.7 R.sup.8, or CONR.sup.7 R.sup.8 ; R.sup.6 is H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.3 alkoxy) C.sub.2 - C.sub.6 alkyl, hydroxy C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 N)C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 NCO)C.sub.1 -C.sub.6 alkyl, CONR.sup.7 R.sup.8, CSNR.sup.7 R.sup.8 or C(NH)NR.sup.7 R.sup.8 ; R.sup.7 and R.sup.8 are each independently H, C.sub.1 -C.sub.4 alkyl, (C.sub.1 -C.sub.3 alkoxy)C.sub.2 -C.sub.4 alkyl or hydroxy C.sub.2 -C.sub.4 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.
Inventor(s): Bell; Andrew S. (Groton, CT), Brown; David (Groton, CT), Terrett; Nicholas K. (Groton, CT)
Assignee: Pfizer Inc. (New York, NY)
Application Number:07/882,988
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent PDF download available with subscription

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Foreign Priority and PCT Information for Patent: 5,250,534

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom9013750Jun 20, 1990

International Patent Family for Patent: 5,250,534

Country Document Number Publication Date Supplementary Protection Certificate SPC Country SPC Expiration
Portugal98011Mar 31, 1992
New Zealand238586Aug 26, 1993
Yugoslavia108791Jan 20, 1994
Ireland66040Dec 13, 1995
JapanH07121945Dec 25, 1995
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Preferred citation:

Friedman, Y. Location of pharmaceutical innovation: 2000–2009 Nature Reviews Drug Discovery 9, 835–836 (2010).

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