New immunosuppressive and antiinflammatory FR520 derivs. - for treating e.g. transplant resistance, rheumatoid arthritis, multiple sclerosis, diabetes, etc.

摘要

24-oxo-FR520 derivs. of formula (I) are new: where R2 = Me, Et, n-propyl or allyl; R3 = MeO or OH. USE/ADVANTAGE - (I) have immunosuppressive, antiinflammatory or antiproliferative activities, useful for treating e.g. transplant rejection; rheumatoid arthritis, multiple sclerosis, psoriasis, dermatitis, urticaria, acne, etc.. (I) are admin. topically (1-3% concn.) or systemically (at 0.15-1.5 mg/kg/day). (I) can also be used to increase the activity, effect and/or sensitivity of other chemotherapeutic agents, e.g. they can be used to reduce the dose of toxic antineoplastic or cytostatic agents.