Hydroxymacrolide derivatives having immunosuppressive activity

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514 63, 514411, 540452, 540456, A61K 31395, A61K 31695, C07D49816, C07F 701

Patent

active

050648357

ABSTRACT:
Novel hydroxymacrolide derivatives of the general structural Formula I: ##STR1## have been prepared from (a) suitable precursor(s) by selective reduction of the ketone at C-2. These macrolide immunosuppressants are useful in a human host for the treatment of autoimmune diseases (such as juvenile-onset diabetes melitus, multiple sclerosis and rheumatoid arthritis), infectious diseases and/or the prevention of rejection of foreign organ transplants, e.g. bone marrow and heart transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses such as: psoriasis, atopical dermatitiis, contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasculitides, erythemas, cutaneous eospinphilias, Lupus erythematosus or Alopecia areata.

REFERENCES:
patent: 4894366 (1990-01-01), Okuhara et al.
"Organic Chemistry", 3rd Ed. (1973) by Morrison and Boyd, pp. 590-591, 665-666 and 668-689.

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