Patent US5221670A successfully refreshed from Google Patents.
US5221670A
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US
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Rapamycin esters
Assignee: Wyeth LLC
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Filing: 1991-10-17
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Granted: 1993-06-22
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Expires: 2011-10-17
Abstract
Abstract A compound of the structure ##STR1## where 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## 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 immunosuppresive 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
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 13:13
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/12; C07D498/18; C07H; C07H19/00; C07H19/01; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
168 words
A compound of the structure ##STR10## wherein R 1 , R 2 , and R 3 are each, independently, hydrogen or ##STR11## 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 ##STR12## R 5 and R 6 are each, independently, alkyl of 1-6 carbon atoms, phenylalkyl wherein the alkyl group contains 1-3 atoms, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, or a carboxylic acid; X is ##STR13## R 7 and R 8 are each, independently, hydrogen or alkyl of 1-6 carbon atoms; 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.
Claim 2
Dependent Claim
168 words
A compound of the structure ##STR10## wherein R 1 , R 2 , and R 3 are each, independently, hydrogen or ##STR11## 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 ##STR12## R 5 and R 6 are each, independently, alkyl of 1-6 carbon atoms, phenylalkyl wherein the alkyl group contains 1-3 atoms, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, or a carboxylic acid; X is ##STR13## R 7 and R 8 are each, independently, hydrogen or alkyl of 1-6 carbon atoms; 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.
Claim 3
Dependent Claim
27 words
A compound of claim 1 where R 4 is --(CH 2 ) m X(CH 2 ) n CO 2 R 5 or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim
16 words
A compound of claim 1 where R 4 is ##STR14## or a pharmapharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
14 words
A compound of claim 1 which is rapamycin-14,31,42-tris(monobenzylsuccinate) or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
14 words
A compound of claim 1 which is rapamycin-31,42-bis(monobenzylsuccinate) or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
14 words
A compound of claim 1 which is rapamycin-42-(monobenzylsuccinate) or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim
14 words
A compound of claim 1 which is rapamycin-31,42-bishemiglutarate or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
10 words
A compound of claim 1 which is rapamycin-31,42-hemiglutarate bissodium salt.
Claim 10
Dependent Claim
10 words
A compound of claim 1 which is rapamycin-31,42-bishemiglutarate bistromethamine salt.
Claim 11
Dependent Claim
14 words
A compound of claim 1 which is rapamycin-42-hemi-3'-oxoglutarate or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
14 words
A compound of claim 1 which is rapamycin-31,42-bishemi-3'-oxoglutarate or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
10 words
A compound of claim 1 which is rapamycin-31,42-bishemi-3'-oxoglutarate disodium salt.
Claim 14
Dependent Claim
10 words
A compound of claim 1 which is rapamycin-31,42-bishemi-3'-oxoglutarate bistromethamine salt.
Claim 15
Dependent Claim
14 words
A compound of claim 1 which is rapamycin-31,42-bishemisuccinate or a pharmaceutically acceptable salt thereof.
Claim 16
Dependent Claim
10 words
A compound of claim 1 which is rapamycin-31,42-bishemisuccinate bistromethane salt.
Claim 17
Dependent Claim
14 words
A compound of claim 1 which is rapamycin-42-monomethylsuccinate or a pharmaceutically acceptable salt thereof.
Claim 18
Dependent Claim
14 words
A compound of claim 1 which is rapamycin-42-(4-trifluoromethylbenzyl)succinate or a pharmaceutically acceptable salt thereof.
Claim 19
Dependent Claim
25 words
A pharmaceutical composition for use as an immunosuppressive agent comprising an immunosuppressive amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.
Claim 20
Dependent Claim
11 words
A composition as claimed in claim 18, in unit dosage form.
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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) | 1996-06-21 | 1996-12-21 | 1997-06-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-06-21 | 2000-12-21 | 2001-06-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-06-21 | 2004-12-21 | 2005-06-22 | $7700.00 | Window Closed / Lapsed |