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US 5,091,431 AGranted
Phosphodiesterase inhibitors
AssigneeSchering Corporation
InventorsDeen Tulshian, Ronald J. Doll
Life of this patent
Estimating the term…
Abstract
Compounds having an optionally-substituted purine derivative portion and a carbobicyclic or heterobicyclic portion, which compounds are useful as phosphodiesterase inhibitors, are disclosed. Also disclosed are intermediates, methods for making the inhibitors, pharmaceutical compositions and methods for treating hypertension using the compounds.
Claims6
Compounds represented by the formula ##STR19## R.sub.1 is hydrogen or R.sub.1 and R.sub.2 together form a double bond;
- R.sub.2 is hydrogen or R.sub.2 may form a double bond with either R.sub.1 or X;
- R.sub.3 is hydrogen or OH;
- R.sub.4 is hydrogen or --(CH.sub.2).sub.n COOR.sub.6 ;
- R.sub.5 is R.sub.4 or --CH(COOR.sub.6)(CH.sub.2 COOR.sub.6), provided that R.sub.4 and R.sub.5 are not both hydrogen;
- R.sub.6 is hydrogen or lower alkyl;
- n is 0-4;
- X is --CH.sub.2 -- or when R.sub.1 is hydrogen, X may be --CH.dbd. and form a double bond with R.sub.2 ;
- Y is --CH.sub.2 -- or --O--;
- B is ##STR20## R.sub.8 --OH or --NH.sub.2 ;
- R.sub.9 is hydrogen, lower alkyl or aryl;
- R.sub.10 is hydrogen, amino, lower alkylamino, arylamino, or lower alkylcarbonylamino;
- R.sub.11 is hydrogen, halogeno, lower alkyl or aryl;
- and the pharmaceutically acceptable esters or salts thereof.
10 more elements
Dependencies are inferred from the claim text.