Halomacrolides and derivatives having immunosuppressive...

Details Halomacrolides and derivatives having immunosuppressive... Halomacrolides and derivatives having immunosuppressive...

C - Chemistry, Metallurgy

07

H

C07H 19/24 (2006.01) A61K 31/70 (2006.01) C07H 19/01 (2006.01)

Patent

CA 2052885

18/RJN6 31/RJN13 Case 18090 TITLE OF THE INVENTION NEW HALOMACROLIDES AND DERIVATIVES HAVING IMMUNOSUPPRESSIVE ACTIVITY ABSTRACT OF THE DISCLOSURE Novel C-3" and C-4" halogen-substituted macrolides of FK-506 type structural Formula I: Image I 18/RJN6 - i - Case 18090 31/RJN31 are described. These macrolide immunosuppressants are useful in a mammalian 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 rejec- tion 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 eosinophilias, Lupus erythematosus or Alopecia areata.

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