Biotin esters of rapamycin

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United States of America Patent

PATENT NO 5504091
SERIAL NO

08224206

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Abstract

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A compound of the structure ##STR1## R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR2## X is ##STR3## Y is ##STR4## Z is --CH.sub.2 --, --S--S--, or ##STR5## R.sup.3 is hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, --(CH.sub.2).sub.q CO.sub.2 R.sup.5, --(CH.sub.2).sub.r NR.sup.6 R.sup.7, carbamylalkyl, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenylmethyl, imidazoylmethyl, halo, trifluoromethyl, or phenyl which is optionally mono-, di-, or tri-substituted; R.sup.4, R.sup.6, and R.sup.7 are each, independently, hydrogen, alkyl, or arylalkyl; R.sup.5 is hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, or phenyl which is optionally mono-, di-, or tri-substituted; h=0-1; j=0-1; m=0-6; n=0-6; p=0-10; q=0-10; r=0-6; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen, or a pharmaceutically acceptable salt thereof which is useful for inducing immunosuppression; in the treatment of transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, solid tumors, fungal infections, adult T-cell leukemia/lymphoma, and hyperproliferative vascular disorders; for measuring levels of rapamycin; for isolating rapamycin-binding proteins; and detecting monoclonal antibodies specific for rapamycin or derivatives thereof.

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Patent Owner(s)

Patent OwnerAddress
WYETHFIVE GIRALDA FARMS MADISON NJ 07940 UNITED STATES OF AMERICA

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Huang, John J San Carlos, CA 5 210
Molnar-Kimber, Katherine L Glenside, PA 9 347
Ocain, Timothy D Waltham, MA 17 641
Vernon, Steven K Havertown, PA 1 121

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