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

摘要

Delta 18 FR-520 derivs. of formula (I) are new: R3 = OH or OMe; R2 = Me, Et, n-propyl or allyl. USE/ADVANTAGE - (I) have immunosuppressive, antiinflammatory and antiproliferative activities; they are useful for e.g. preventing transplant rejection; or treating 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/cytostatic agents.