New 1,5 - diazabicyclo 3,3,0 octane - 2,6 - of dihydroxydiones

摘要

Novel compounds of formula FORM:1124982/C2/1 wherein R, R1, R2 and R3 are H, C1- 8 alkyl or aryl, and X is O or H2 are prepared either by refluxing for 8-10 hours a compound of formula FORM:1124982/C2/2 wherein R and R1 are as defined, with an equimolar amount of a compound of formula FORM:1124982/C2/3 wherein R2 and R3 are as defined in the presence of two equimolar amounts of a tertiary organic base in an inert anhydrous organic solvent, or by reacting a compound of the Formula (I) above with an equimolar amount of hydrazine in an inert anhydrous organic solvent at a temp. below 10 DEG C., then raising the temp. to 50-70 DEG C. for 2-3 hrs. and subjecting the resultant compound of formula FORM:1124982/C2/4 either to distillation or to refluxing for 2-3 hours with two equimolar amounts of a tertiary organic base in an inert anhydrous organic solvent, and if desired, converting the keto groups of the resulting dione to CH2 by hydrogenation with LiAlH4 in an organic solvent. A therapeutic composition comprises a compound of the first formula given above, together with a pharmaceutically acceptable carrier. The compositions may be administered orally and have anti-inflammatory activity.