Patent · US Expired

Carbamates of rapamycin

US5118678A · kind A · utility

248Cited by
6References
23Claims
0Family size

Assignee

Inventors

Key dates

Filing dateApr 17, 1991
Grant dateJun 2, 1992
Priority date
Expiry dateApr 17, 2011

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D498/18
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONH(CR.sup.3 R.sup.4).sub.n --X; PA1 R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, aralkyl, cycloalkyl, halogen, or trifluoromethyl; PA1 X ix hydrogen, lower alkyl, cycloalkyl, trifluoromethyl, nitro, alkoxy, carboalkoxy, aralkyl, halo, dialkylamino, thioalkyl, or Y; PA1 Y is a phenyl group which may be optionally mono-, di-, or tri- substituted with a group selected from alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, dialkylamino, or alkylthio; PA1 n=0-5; PA1 with the proviso that R.sup.1 and R.sup.2 are not both hydrogen and when n=0, X is lower alkyl, cycloalkyl, aralkyl, or Y; or a pharmaceutically acceptable salt thereof when X is dialkylamino, 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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.