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DrugPatentWatch concentrates deep knowledge on more than 6,400 small-molecule drugs and 2,300 generic ingredients from 1,700 branded and generic pharmaceutical companies and 700 suppliers, and more than 4,400 active and expired US patents and 74,000 international patents spanning 93 countries and regional patent offices. |
| 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; |
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | Type | RLD | Patent No. | Product | Substance | Delist_Flag | Patent Expiration | Patented / Exclusive Use | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Pfizer | REVATIO | sildenafil citrate | SOLUTION; INTRAVENOUS | 022473 | Nov 18, 2009 | RX | Yes | 5,250,534*PED | <disabled> | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Pfizer | REVATIO | sildenafil citrate | TABLET; ORAL | 021845 | Jun 3, 2005 | RX | Yes | 5,250,534*PED | <disabled> | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Pfizer Ireland | VIAGRA | sildenafil citrate | TABLET; ORAL | 020895 | Mar 27, 1998 | RX | Yes | 5,250,534*PED | <disabled> | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Pfizer Ireland | VIAGRA | sildenafil citrate | TABLET; ORAL | 020895 | Mar 27, 1998 | RX | No | 5,250,534*PED | <disabled> | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Foriegn Application Priority Data | ||
| Foreign Country | Foreign Patent Number | Foreign Patent Date |
| United Kingdom | 9013750 | Jun 20, 1990 |
| Country | Document Number | Publication Date | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Austria | 121403 | May 15, 1995 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Australia | 626757 | Aug 06, 1992 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Australia | 7915591 | Mar 19, 1992 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Brazil | 9102560 | Jan 21, 1992 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| The preview shows a limited data set. Complete access is available with a Subscription | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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