Patent · US Expired

Silyl ethers of rapamycin

US5120842A · kind A · utility

289Cited by
6References
9Claims
0Family size

Assignee

Inventors

Key dates

Filing dateApr 1, 1991
Grant dateJun 9, 1992
Priority date
Expiry dateApr 1, 2011

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61P37/06
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

A compound of the structure ##STR1## wherein R.sup.1 is --SiR.sup.3 R.sup.4 R.sup.5 ; PA1 R.sup.2 is hydrogen or --SiR.sup.3 R.sup.4 R.sup.5 ; and PA1 R.sup.3, R.sup.4, and R.sup.5 are each, independently, alkyl, alkenyl, aralkyl, triphenylmethyl, or phenyl 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. This invention also provides a method of using rapamycin 42-[O-[(1,1-dimethylethyl)-dimethylsilyl] ether for the preparation of 31-substituted rapamycin derivatives.

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