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US4195022A Expired / Lapsed US ⏱️ 0.0 years remaining

4-Desacetoxy-4α-hydroxyvinblastine and related compounds

Assignee: Eli Lilly and Co
•
Filing: 1978-03-27
•
Granted: 1980-03-25
•
Expires: 1998-03-27
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Abstract

Abstract 4-Desacetoxy-4 alpha -hydroxyvinblastine, prepared by reduction of 4-desacetoxy-4-oxovinblastine, and derivatives thereof, useful as antimitotic agents.

Inventors

  • 👤 Gerald L. Thompson

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-31 16:08
CPC Classifications
C; C07; C07D; C07D519/00; C07D519/04

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 101 words
An indole-dihydroindole of the formula ##STR4## wherein R is OCH 3 or NH--NH 2 , R 1 is H or acetyl, R 2 is CH 3 or CHO, and, when taken singly, R 5 is H and one of R 3 and R 4 is OH or H and the other is C 2 H 5 and when R 4 and R 5 are taken together, they form an α-epoxide ring and R 3 is C 2 H 5 , with the proviso that, when R is NH--NH 2 , R 1 is H, and pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim 101 words
An indole-dihydroindole of the formula ##STR4## wherein R is OCH 3 or NH--NH 2 , R 1 is H or acetyl, R 2 is CH 3 or CHO, and, when taken singly, R 5 is H and one of R 3 and R 4 is OH or H and the other is C 2 H 5 and when R 4 and R 5 are taken together, they form an α-epoxide ring and R 3 is C 2 H 5 , with the proviso that, when R is NH--NH 2 , R 1 is H, and pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim 43 words
A compound according to claim 1 in which R is OCH 3 , R 1 is H, R 2 is CH 3 , R 3 is OH, R 4 is C 2 H 5 and R 5 is H, said compound being 4-desacetoxy-4α-hydroxyvinblastine.
Claim 4
Dependent Claim 41 words
A compound according to claim 1 in which R is OCH 3 , R 1 is H, R 2 is CHO, R 3 is OH, R 4 is C 2 H 5 and R 5 is H, said compound being 4-desacetoxy-4α-hydroxyvincristine.
Claim 5
Dependent Claim 9 words
The sulfate salt of the compound of claim 3.
Claim 6
Dependent Claim 45 words
A compound according to claim 1 in which R is NH-NH 2 , R 1 is H, R 2 is CH 3 , R 3 is OH, R 4 is C 2 H 5 and R 5 is H, said compound being 4-desacetoxy-4α-hydroxyvinblastine C-3 carboxhydrazide.
Claim 7
Dependent Claim 10 words
A sulfate salt of a compound according to claim 1.

References Cited (Backward Citations)

US3392173A Cited
DE2558124A1 Cited
DE2558027A1 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1983-03-25 1983-09-24 1984-03-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1987-03-25 1987-09-24 1988-03-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1991-03-25 1991-09-24 1992-03-25 $7700.00 Window Closed / Lapsed

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