Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-05-14
1998-07-07
Peselev, Elli
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546 90, A61K 3144, C07D49100
Patent
active
057769435
ABSTRACT:
This invention provides metabolites of rapamycin, the first of which is 41-O-desmethyl rapamycin, having a deprotonated molecular ion detected at a mass to charge ratio of 899, and a characteristic desorption chemical ionization mass spectroscopic fragmentation pattern comprising ions detected at a mass to charge ratio of 591, 569, 559, 543, 529, 421, and 308. A second compound of this invention is a hydroxylated metabolite of rapamycin having a deprotonated molecular ion detected at a mass to charge ratio of 928, and a characteristic direct chemical ionization mass spectroscopic fragmentation pattern comprising ions detected at a mass to charge ratio of 607, 571, 545, 513, 322, 290, and 241 amu. The compounds of this invention, by virtue of their immunosuppressive activity are useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of their antitumor activity are useful in treating solid tumors; and by virtue of their antifungal activity are useful in treating fungal infections.
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Christians Uwe
Sattler Martin
Sewing Karl F.
American Home Products Corporation
Milowsky Arnold S.
Peselev Elli
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