Rapamycin esters for treating transplantation rejection
Abstract
Abstract A compound of the structure ##STR1## wherein R 1 , R 2 , and R 3 are each, independently, hydrogen or ##STR2## with the proviso that R 1 , R 2 , and R 3 are not all hydrogen; R 4 is --(CH 2 ) m X(CH 2 ) n CO 2 R 5 or ##STR3## R 5 and R 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; X is ##STR4## O, or S; R 7 and R 8 are each, independently, hydrogen or alkyl; Y is CH or N; m is 0-4; n is 0-4; with the proviso that m and n are not both 0 when X is O or S; or a pharmaceutically acceptable salt thereof, which is 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 useful in treating tumors, and by virtue of its antifungal activity is useful in treating fungal infections.
Inventors
- 👤 Craig E. Caufield
Bibliographic Details
Claims Analysis
Total Claims: 2References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-10-24 | 1998-04-25 | 1998-10-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-10-24 | 2002-04-25 | 2002-10-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-10-24 | 2006-04-25 | 2006-10-25 | $7700.00 | Window Closed / Lapsed |