US4650803A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Prodrugs of rapamycin
Assignee: KANSAS LAWRENCE KANSAS A CORP OF KANSAS, University of
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Filing: 1985-12-06
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Granted: 1987-03-17
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Expires: 2005-12-06
Abstract
Abstract Water soluble prodrugs of rapamycin are disclosed which are useful as components in injectable pharmaceutical formulations for the treatment of tumors in mammals.
Inventors
- 👤 Valentino J. Stella
- 👤 Paul E. Kennedy
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 17:10
CPC Classifications
C; C07; C07H; C07H1/00; C07D; C07D498/00; C07D498/12; C07D498/18; A; A61; A61P; A61P31/00; A61P31/04; A61P43/00
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
94 words
Derivatives of rapamycin which are water soluble and which are mono-substituted derivatives at position 28 and disubstituted derivatives at positions 28 and 43 of rapamycin with the substituents having the configuration: ##STR2## wherein m is an integer from 1 to 3, wherein R 1 and R 2 is each hydrogen or an alkyl radical having from one to three carbon atoms or wherein R 1 and R 2 together with the nitrogen to which they are attached form a saturated heterocyclic ring having four carbon atoms and the pharmaceutically acceptable salts of such derivatives.
Claim 2
Dependent Claim
94 words
Derivatives of rapamycin which are water soluble and which are mono-substituted derivatives at position 28 and disubstituted derivatives at positions 28 and 43 of rapamycin with the substituents having the configuration: ##STR2## wherein m is an integer from 1 to 3, wherein R 1 and R 2 is each hydrogen or an alkyl radical having from one to three carbon atoms or wherein R 1 and R 2 together with the nitrogen to which they are attached form a saturated heterocyclic ring having four carbon atoms and the pharmaceutically acceptable salts of such derivatives.
Claim 3
Dependent Claim
11 words
The mono-substituted derivative of claim 1 wherein the substituent is ##STR3##
Claim 4
Dependent Claim
11 words
The mono-substituted prodrug derivative claim 1 wherein the substituent is ##STR4##
Claim 5
Dependent Claim
11 words
The mono-substituted derivative of claim 1 wherein the substituent is ##STR5##
Claim 6
Dependent Claim
31 words
An injectable pharmaceutical composition useful in the treatment of tumors comprising a pharmaceutically acceptable carrier and an effective amount of a water soluble derivative of rapamycin as defined in claim 1.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-03-16 | 1990-09-15 | 1991-03-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-03-16 | 1994-09-15 | 1995-03-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-03-16 | 1998-09-15 | 1999-03-17 | $7700.00 | Window Closed / Lapsed |