Fluoromacrolides having immunosuppressive activity

C - Chemistry – Metallurgy – 07 – H

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

Patent

CA 2076419

TITLE OF THE INVENTION FLUOROMACROLIDES HAVING IMMUNOSUPPRESSIVE ACTIVITY ABSTRACT OF THE DISCLOSURE Fluoromacrolides and derivatives of the general structural Formula I: Image I - i - have been prepared from suitable precursors by oxidation and fluorination at C-20. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ 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. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma. Furthermore, these macrolides are useful as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis.

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