US5100883A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Fluorinated esters of rapamycin
Assignee: Wyeth LLC
•
Filing: 1991-04-08
•
Granted: 1992-03-31
•
Expires: 2011-04-08
Abstract
Abstract A compound of the structure ##STR1## wherein R 1 and R 2 are each, independently, hydrogen or ##STR2## R 3 is a mono-, di-, poly-, or per-fluorinated alkyl group with the proviso that R 1 and R 2 are both not hydrogen, 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.
Inventors
- 👤 Guy A. Schiehser
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 05:37
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/12; C07D498/18
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
46 words
A compound of the formula ##STR6## wherein R 1 and R 2 are each, independently, hydrogen or ##STR7## R 3 is a mono-, di-, poly-, or per-fluorinated alkyl group of 1-10 carbon atoms; with the proviso that R 1 and R 2 are both not hydrogen.
Claim 2
Dependent Claim
46 words
A compound of the formula ##STR6## wherein R 1 and R 2 are each, independently, hydrogen or ##STR7## R 3 is a mono-, di-, poly-, or per-fluorinated alkyl group of 1-10 carbon atoms; with the proviso that R 1 and R 2 are both not hydrogen.
Claim 3
Dependent Claim
10 words
A compound of claim 1 where R 2 is hydrogen.
Claim 4
Dependent Claim
21 words
A compound of claim 1 where R 3 is a mono-, di-, poly-, or per-fluorinated alkyl group of 1-6 carbon atoms.
Claim 5
Dependent Claim
26 words
A compound of claim 1 where R 2 is hydrogen and R 3 is a mono-, di-, poly-, or per-fluorinated alkyl group of 1-6 carbon atoms.
Claim 6
Dependent Claim
12 words
A compound of claim 1 which is rapamycin, 42-ester with trifluoroacetic acid.
Claim 7
Dependent Claim
12 words
A compound of claim 1 which is rapamycin, 42-ester with 2,3,3,3-tetrafluoropropanoic acid.
Claim 8
Dependent Claim
12 words
A compound of claim 1 which is rapamycin, 42-ester with difluoroacetic acid.
Claim 9
Dependent Claim
12 words
A compound of claim 1 which is rapamycin, 42-ester with pentafluoropropionic acid.
Claim 10
Independent Claim
71 words
A method of treating transplantation rejection, host vs. draft disease, autoimmune diseases, and diseases of inflammation in a mammal by administering an effective amount of a compound having the formula ##STR8## wherein R 1 and R 2 are each, independently, hydrogen or ##STR9## R 3 is a mono-, di-, poly-, or per-fluorinated alkyl group of 1-10 carbon atoms; with the proviso that R 1 and R 2 are both not hydrogen.
Claim 11
Independent Claim
71 words
A method of treating transplantation rejection, host vs. draft disease, autoimmune diseases, and diseases of inflammation in a mammal by administering an effective amount of a compound having the formula ##STR8## wherein R 1 and R 2 are each, independently, hydrogen or ##STR9## R 3 is a mono-, di-, poly-, or per-fluorinated alkyl group of 1-10 carbon atoms; with the proviso that R 1 and R 2 are both not hydrogen.
Claim 12
Dependent Claim
19 words
A pharmaceutical composition for use as an immunosuppressive agent comprising an immunosuppressive amount of a compound of claim 1.
Claim 13
Dependent Claim
11 words
A composition as claimed in claim 10 in unit dosage form.
References Cited (Backward Citations)
US3929992A
Cited
US3993749A
Cited
US4885171A
Cited
US4316885A
Cited
US4401653A
Cited
US4650803A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-03-31 | 1995-09-30 | 1996-03-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-03-31 | 1999-09-30 | 2000-03-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-03-31 | 2003-09-30 | 2004-03-31 | $7700.00 | Window Closed / Lapsed |