US4765972A
Expired / Lapsed
US
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Vinca alkaloid photoactive analogs and their uses
Assignee: United States Department of Health and Human Services
•
Filing: 1986-04-03
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Granted: 1988-08-23
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Expires: 2006-04-03
Abstract
Abstract Pharmacologically active, radioactive, and photoactive vinblastine analogs are provided which can be used to bind covalently to cellular polypeptides which have high affinity for Vinca alkaloids. The compounds are N-(p-azido[3,4- 3 H]benzoyl)-N'beta-aminoethylvindesine and N-p-azido-[3- 125 I]-salicyl-N'-beta-aminoethylvindesine. The compounds can be used to identify cellular Vinca alkaloid receptors which may be involved in antineoplastic, cytotoxic and drug resistant mechanisms of actions. In addition to specific interaction with tubulin, these compounds specifically bind to a 150-180 kDa surface membrane glycoprotein which is overexpressed in multidrug resistant cells.
Inventors
- 👤 Ahmad R. Safa
- 👤 Ronald L. Felsted
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 01:30
CPC Classifications
C; C07; C07D; C07D519/00; C07D519/04
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
3 words
N-(p-azido-[3,4- 3 H]benzoyl)-N'-beta-aminoethylvindesine.
Claim 2
Dependent Claim
3 words
N-(p-azido-[3,4- 3 H]benzoyl)-N'-beta-aminoethylvindesine.
Claim 3
Dependent Claim
1 words
N-(p-azidosalicyl)-N'-beta-aminoethylvindesine.
Claim 4
Dependent Claim
1 words
N-(p-azidosalicyl)-N'-beta-aminoethylvindesine.
Claim 5
Dependent Claim
1 words
N-(p-azidobenzoyl)-N'-beta-aminoethylvindesine.
Claim 6
Dependent Claim
1 words
N-(p-azidobenzoyl)-N'-beta-aminoethylvindesine.
Claim 7
Dependent Claim
23 words
A reagent composition for photolabelling cells for determining the affinity of the cells for vinblastine comprising N-(p-azido-[3,4, 3 H]-benzoyl)-N'beta-aminoethylvindesine and a suitable carrier.
Claim 8
Dependent Claim
23 words
A reagent composition for photolabelling cells for determining the affinity of the cells for vinblastine comprising N-(p-azido-[3,4, 3 H]-benzoyl)-N'beta-aminoethylvindesine and a suitable carrier.
Claim 9
Dependent Claim
23 words
A reagent composition for radiolabelling cells to determine the affinity of the cells for vinblastine comprising N-(p-azido-3-[ 125 I]-salicyl-N'-beta-aminoethylvindesine and a suitable carrier.
Claim 10
Dependent Claim
23 words
A reagent composition for radiolabelling cells to determine the affinity of the cells for vinblastine comprising N-(p-azido-3-[ 125 I]-salicyl-N'-beta-aminoethylvindesine and a suitable carrier.
References Cited (Backward Citations)
US4203898A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-08-23 | 1992-02-22 | 1992-08-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-08-23 | 1996-02-22 | 1996-08-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-08-23 | 2000-02-22 | 2000-08-23 | $7700.00 | Window Closed / Lapsed |