US5023263A
Expired / Lapsed
US
⏱️ 0.0 years remaining
42-oxorapamycin
Assignee: Wyeth LLC
•
Filing: 1990-08-09
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Granted: 1991-06-11
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Expires: 2010-08-09
Abstract
Abstract This invention provides an oxidized derivative of rapamycin in which the hydroxyl at the 42-position has been oxidized to the corresponding ketone or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive and antifungal activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, and fungal infections and a process for the preparation of this oxidized derivative of rapamycin. ##STR1##
Inventors
- 👤 Gregory F. Von Burg
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 22:35
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/02; C07D498/12; C07D498/18; A; A61; A61P; A61P29/00; A61P31/00; A61P31/04; A61P31/10; A61P37/00; A61P37/02; A61P37/06; C07H; C07H19/00; C07H19/01
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
7 words
42-Oxorapamycin or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
7 words
42-Oxorapamycin or a pharmaceutically acceptable salt thereof.
Claim 3
Independent Claim
32 words
A method of treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation in a mammal by administering an effective amount of 42-oxorapamycin or a pharmaceutically acceptable salt thereof.
Claim 4
Independent Claim
32 words
A method of treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation in a mammal by administering an effective amount of 42-oxorapamycin or a pharmaceutically acceptable salt thereof.
Claim 5
Independent Claim
19 words
A method of treating fungal infections by administering an effective amount of 42-oxorapamycin or a pharmaceutically acceptable salt thereof.
Claim 6
Independent Claim
19 words
A method of treating fungal infections by administering an effective amount of 42-oxorapamycin or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
14 words
A process for making 42-oxorapamycin from rapamycin using a ruthenium catalyst as an oxidant.
Claim 8
Dependent Claim
14 words
A process for making 42-oxorapamycin from rapamycin using a ruthenium catalyst as an oxidant.
Claim 9
Dependent Claim
11 words
A process according to claim 4 using tris(triphenylphosphine)ruthenium as the oxidant.
Claim 10
Dependent Claim
13 words
A process according to claim 4 using ruthenium (IV) oxide as the oxidant.
Claim 11
Dependent Claim
12 words
A process according to claim 4 using tetra-n-propylammonium perruthenate as the oxidant.
Claim 12
Dependent Claim
19 words
A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim
11 words
A composition as claimed in claim 8 in unit dosage form.
References Cited (Backward Citations)
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-06-10 | 1994-12-10 | 1995-06-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-06-10 | 1998-12-10 | 1999-06-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-06-10 | 2002-12-10 | 2003-06-11 | $7700.00 | Window Closed / Lapsed |