Patent · US Expired

Rapamycin hydrazones

US5120726A · kind A · utility

59Cited by
6References
18Claims
0Family size

Assignee

Inventors

Key dates

Filing dateMar 8, 1991
Grant dateJun 9, 1992
Priority date
Expiry dateMar 8, 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 is hydrogen, alkyl or aralkyl; R.sup.2 is hydrogen, alkyl, cycloalkyl, aralkyl, --COR.sup.3, --CO.sub.2 R.sup.3, --SO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, --CSNR.sup.4 R.sup.5, --COCONR.sup.4 R.sup.5, or Ar; R.sup.3 is alkyl, aralkyl, or Ar; R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, cycloalkyl, allyl, aralkyl, or Ar; PA0 Ar is ##STR2## R.sup.6, R.sup.7, R.sup.8 are each, independently, hydrogen, alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, trifluoromethoxy, amino, or a carboxylic acid; X is CH or N; Y is NH, O, or S; or a pharmaceutically acceptable salt thereof, 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.