Rapamycin amidino carbamates

Details Rapamycin amidino carbamates Rapamycin amidino carbamates

1995-05-24

1996-07-30

Goldberg, Jerome D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514241, 514242, 514256, A61K 3144, A61K 3153, A61K 31505

Patent

active

055411924

ABSTRACT:
A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5,
--COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3R.sup.5, --OR.sup.5, --SR.sup.5, or Ar; R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6,
--NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;
R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

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