Abstract: New griseolic acid derivatives have various groups attached to the sugar part in place of the adenine group of griseolic acid itself. These groups are all purine derivatives or ring-opened purine analogs. The compounds are useful as inhibitors of phosphodiesterases.

Abstract: A compound of the formula (I) is provided ##STR1## wherein A represents a group of the formula: ##STR2## R.sup.1 and R.sup.2 are independently hydrogen, halogen or a group of the formula --OR.sup.9 ; R.sup.9 is hydrogen, alkyl, alkylsulfonyl, haloalkylsulfonyl, arylsulfonyl or a hydroxy-protecting group; R.sup.3 and R.sup.4 are independently carbamoyl or carboxy; R.sup.5 and R.sup.6 both represent hydrogen or together represent an extra carbon-carbon bond between the carbon atoms to which they are attached; and Z represents hydrogen or unsubstituted or substituted hydroxy; or a pharmaceutically acceptable salt or ester thereof. The compounds are useful as inhibitors of phosphodiesterases.

Abstract: A compound of the formula (I) is provided ##STR1## wherein A represents a group of the formula: ##STR2## R.sup.1 and R.sup.2 are independently hydrogen, halogen or a group of the formula --OR.sup.9 ; R.sup.3 and R.sup.4 are independently carbamoyl or carboxy; R.sup.5 and R.sup.a both represent hydrogen or together represent an extra carbon-carbon bond between the carbon atoms to which they are attached; and R.sup.9 is hydrogen, alkyl, alkysulfonyl, haloalkylsulfonyl, arylsulfonyl or a hydroxy-protecting group; or a pharmaceutically acceptable salt or ester thereof. The compounds are useful as inhibitors of phosphodiesterases.

Abstract: A compound of the formula (I) is provided ##STR1## wherein A represents a group of the formula: ##STR2## R.sup.1 and R.sup.2 are independently hydrogen, halogen or a group of the formula --OR.sup.9 ; R.sup.9 is hydrogen, alkyl, alkylsulfonyl, haloalkylsulfonyl, arylsulfonyl or a hydroxy-protecting group; R.sup.3 and R.sup.4 are independently carbamoyl or carboxy; R.sup.5 and R.sup.6 both represent hydrogen or together represent an extra carbon-carbon bond between the carbon atoms to which they are attached; and W represents an alkoxy or aralkoxy; or a pharmaceutically acceptable salt or ester thereof. The compounds are useful as inhibitors of phosphodiesterases.

Abstract: New griseolic acid derivatives have various groups attached to the sugar part in place of the adenine group of griseolic acid itself. These groups are all purine derivatives or ring-opened purine analogs. The compounds are useful as inhibitors of phosphodiesterases.

Abstract: Griseolic acid and dihydrodesoxygriseolic acid derivatives having an alkyl or aralkyl group as a substituent on the amino group at the 6-position are prepared by reacting the unsubstituted compound with a compound R.sup.7 -X (where R.sup.7 is alkyl or aralkyl and X is halogen or sulfonyloxy). The group first substitutes and quaternizes the 1-nitrogen atom. The compound is then subjected to an appropriate combination of temperature and pH to cause ring cleavage, rearrangement and ring closure involving the 6-amino group and this quaternized 1-nitrogen to give a 6-alkylamino or 6-aralkylamino derivative.

Abstract: Griseolic acid derivatives of formula (I): ##STR1## wherein A represents: ##STR2## have enzyme-inhibitory activity, especially against cAMP PDE and cGMP PDE. When formulated as compositions with appropriate carriers or diluents, they may be used for the treatment of a variety of organic disorders and show toxicities less than griseolic acid itself.