Antagonists of immunosuppressive macrolides

C - Chemistry – Metallurgy – 07 – H

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C07H 17/00 (2006.01) A61K 31/70 (2006.01) C07H 19/01 (2006.01)

Patent

CA 2044846

28/JET7 18054 TITLE OF THE INVENTION ANTAGONISTS OF IMMUNOSUPPRESSIVE MACROLIDES ABSTRACT OF THE DISCLOSURE Hydroxymacrolides and derivatives of the general structural Formula I: Image I 28/JET7 - i - 18054 have been prepared from suitable precursors by oxidation at C-20. These macrolides are useful as antagonists of FK-506-type immunosuppressants. The compounds of the present invention are useful for modifying dosages of FK-506-type immunosuppressants in the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, the compounds of the present invention have utility as antidotes for overdoses of FK-506-type immunosuppressants.

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