New tri:cyclic hetero atom contg. cpds. for arthritis treatment - have immunosuppressive and antiinflammatory activity for treatment of skin disorders e.g. psoriasis and dermatitis and auto-immune disease

摘要

Tricyclic cpds. of formula (I) contg. heteroatoms are new. R1 = opt. protected OH, O or acyloxy; R2 = opt. protected OH or acyloxy; R3 = Me, Et, n-Pr or allyl; R4 = (alkyl)imino and R5 = OH; or R4 = O and R5 = (acyl)amino or R4+R5 together form -OCH2NH-. R6 not given. USE/ADVANTAGE - Used to treat and prevent resistance to organ and tissue transplants, e.g. of heart, liver, kidney bone marrow, skin etc. graft versus host disorders in bone marrow transplant, autoimmune diseases e.g. rheumatoid arthritis, systemic lupus erythernatodes, Hashomoto's thyroiditis, multiple sclerosis, myastheria gravis, Type I diabetes, Ureitis etc. and for the therapy of inflammatory and hyperproliferative skin diseases e.g. psoriasis, atopic- or seborrhoeic-dermatitis, lichen piarus, pernphigus bullosic pernphigoid, epidermolysis bullosa, urticeria, angiooedema, vasculitis, erytherna, cutaneous eosinophilia, lupus erythermatodes, acne and alopecia areata. Pref. daily doses for systemic use are 0.15-1.5 mg/kg. (I) can also be used topically.