Purine derivatives
AssigneeBurroughs Wellcome Co.
InventorHoward J. Schaeffer
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Abstract
9-Hydroxyethoxymethyl (and related) derivatives of certain 6-, and 2,6-substituted purines have been discovered to have potent anti-viral activities. Novel compounds and their pharmaceutically acceptable salts, pharmaceutical formulations containing the compounds of this invention, and the treatment of viral infections with these formulations are all disclosed. 9-(2-hydroxyethoxymethyl) guanine and 2-amino-9-(2-hydroxyethoxymethyl)adenine are examples of especially active compounds of this invention.
Claims16
A substituted purine of formula ##STR12## wherein X is sulphur or oxygen;
- R.sup.1 is halogen, hydrogen, thio,alkylthio, alkoxy or azide;
- R.sup.2 is hydrogen, halogen, amino or azide;
- R.sup.3 is nitrogen, straight or branched chain or cyclic alkyl, hydroxyalkyl, benzyloxyalkyl or phenyl;
- R.sup.4 is hydrogen, hydroxy, or lower alkyl;
- R.sup.5 is hydrogen, hydroxy, amino, alkyl, hydroxyalkyl, benzoyloxy, benzoyloxymethyl, benzyloxy, sulphamoyloxy, phosphate, carboxypropionyloxy, or acetoxy;
- and R.sup.6 is hydrogen alkyl, hydroxyalkyl or a pharmaceutically acceptable salt thereof.
A compound of formula (I) ##STR13## wherein R.sup.1 is chlorine, R.sup.2 is amino, R.sup.5 is benzoyloxy and R.sup.3, R.sup.4 and R.sup.6 are each hydrogen or a pharmaceutically acceptable salt thereof, wherein X is oxygen.
The compound of the formula I ##STR14## wherein X is sulphur or oxygen;
- R.sup.1 is hydrogen, halogen, hydroxy, alkoxy, azide, thio, or alkylthio;
- R.sup.2 is hydrogen, halogen, alkylthio, amino or azide, provided R.sup.2 is not amino when R.sup.1 is hydroxy;
- R.sup.3 is hydrogen, straight or branched chain or cyclic alkyl, hydroxyalkyl, benzyloxyalkyl or phenyl, R.sup.4 is hydrogen, hydroxy or alkyl;
- R.sup.5 is hydrogen hydroxy, amino, alkyl, hydroxyalkyl, benzyloxy, benzoyloxy, benzoyloxymethyl, sulphamoyloxy, phosphate, or straight or branched chain or cyclic acyloxy having from 1 to 8 carbon atoms;
- R.sup.6 is hydrogen or alkyl;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.