EP0470804A1
Expired / Lapsed
EP
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Oxorapamycin
Assignee: Wyeth LLC
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Filing: 1991-08-06
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Granted: —
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Expires: 2011-08-06
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.
Inventors
- 👤 Gregory Francis Von Burg
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-01 16:45
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: 8
Claim 1
Independent Claim
7 words
42-Oxorapamycin or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
31 words
A process for making 42-oxorapamycin or a pharmaceutically acceptable salt thereof which comprises oxidising rapamycin using a ruthenium based oxidant and if desired isolating the product as a pharmaceutically acceptable salt.
Claim 3
Dependent Claim
16 words
A process as claimed in Claim 2 in which the oxidant is tris(triphenylphosphine)ruthenium dichloride/N-methyl morpholine N-oxide.
Claim 4
Dependent Claim
15 words
A process as claimed in Claim 2 in which the oxidant is ruthenium (IV) oxide.
Claim 5
Dependent Claim
16 words
A process as claimed in Claim 2 in which the oxidant is tetra-n-propylammonium perruthenate/N-methyl morpholine N-oxide.
Claim 6
Dependent Claim
16 words
A pharmaceutical composition comprising 42-oxorapamycin or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
Claim 7
Dependent Claim
13 words
A pharmaceutical composition as claimed in Claim 6 when in unit dosage form.
Claim 8
Dependent Claim
31 words
Use of 42-oxorapamycin or a pharmaceutically acceptable salt thereof in the preparation of a medicament for the treatment of transplantation rejection, host vs. graft disease, autoimmune diseases or diseases of inflammation.
References Cited (Backward Citations)
EP0323042A1
Cited
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