Silyl ethers of rapamycin
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United States of America Patent
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Jun 9, 1992
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N/A
app pub date -
Apr 1, 1991
filing date -
Apr 1, 1991
priority date (Note) -
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Abstract
A compound of the structure ##STR1## wherein R.sup.1 is --SiR.sup.3 R.sup.4 R.sup.5 ; R.sup.2 is hydrogen or --SiR.sup.3 R.sup.4 R.sup.5 ; and R.sup.3, R.sup.4, and R.sup.5 are each, independently, alkyl, alkenyl, aralkyl, triphenylmethyl, or phenyl which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections. This invention also provides a method of using rapamycin 42-[O-[(1,1-dimethylethyl)-dimethylsilyl] ether for the preparation of 31-substituted rapamycin derivatives.
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