42-oxorapamycin

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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540456, 546 90, A61K 31395, C07D49116

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active

050232630

ABSTRACT:
This invention provides an oxidized derivative of rapamycin in which the hydroxyl at the 42-position has been oxidized to the corresponding ketone or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive and antifungal activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, and fungal infections and a process for the preparation of this oxidized derivative of rapamycin. ##STR1##

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Immunology, C.V. Moseby Co., pp. 12.8-12.11 (1989).

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