Patent · US Expired

Rapamycin esters

US5221670A · kind A · utility

169Cited by
11References
19Claims
0Family size

Assignee

Inventor

Key dates

Filing dateOct 17, 1991
Grant dateJun 22, 1993
Priority date
Expiry dateOct 17, 2011

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61K38/00
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

A compound of the structure ##STR1## where R.sup.1, R.sup.2, and R.sup.3 are each, independently, hydrogen or ##STR2## with the proviso that R.sup.1, R.sup.2, and R.sup.3 are not all hydrogen; R.sup.4 is --(CH.sub.2).sub.m X(CH.sub.2).sub.n CO.sub.2 R.sup.5 or ##STR3## R.sup.5 and R.sup.6 are each, independently, alkyl, aralkyl, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid; PA1 X is ##STR4## R.sup.7 and R.sup.8 are each, independently, hydrogen or alkyl; Y is CH or N; PA1 m is 0-4; n is 0-4; PA1 with the proviso that m and n are not both 0 when X is O or S; PA1 or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppresive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, by virtue of its antitumor activity useful in treating 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.