Carbamates of rapamycin

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

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C07D49816, A61K 31395

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active

054809886

ABSTRACT:
A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.4 R.sup.5).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## --R.sup.12, or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;
R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, p--OH, --CF.sub.3, or --F;
R.sup.6 is hydrogen or --OR.sup.13 ;
R.sup.7 is hydrogen or alkyl;
R.sup.10 is hydrogen, alkyl, or arylalkyl;
R.sup.11, R.sup.12, and R.sup.13 are each independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;
R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, Tri-(alkyl)silyethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;
R.sup.15 and R.sup.16 are each independently, hydrogen or alkyl; ##STR3## R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ring may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyll, arylalkyl, halogen, --CF.sub.3, ---OR.sup.14, or --CO.sub.2 R.sup.10 ;
R.sup.22 is hydrogen, alkyl, or arylalkyl;
m=0-6;
n=1-6;
p=0-6; and
r=1-6
with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, anti inflammatory, antifungal, antiproliferative, and antitumor agent.

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