Semi-synthetic immunosuppressive macrolides

C - Chemistry – Metallurgy – 07 – H

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C07H 19/01 (2006.01) A61K 31/70 (2006.01) C07D 498/18 (2006.01)

Patent

CA 2066138

103/JET53 18298 TITLE OF THE INVENTION SEMI-SYNTHETIC IMMUNOSUPPRESSIVE MACROLIDES ABSTRACT OF THE DISCLOSURE Macrolides of the general structural Formula I: Image I 103/JET53 -i- 13298 have been prepared. These macrolides are antagonists of FK-506-type immunosuppressants and 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. Furthermore, the compounds of the present invention may have utility as antidotes for overdoses of FK-506-type immunosuppressants. In addition, 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.

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