US4393052A
Expired / Lapsed
US
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Antitumor anthracycline glycosides, their preparation, intermediates therefor, and compositions and use thereof
Assignee: Pfizer Italia SRL
•
Filing: 1981-10-29
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Granted: 1983-07-12
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Expires: 2001-10-29
Abstract
Abstract Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-threo-hexopyra nosyl chloride; 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-arabino-hexopy ranosyl chloride or 2,3,6-trideoxy-4-C-trifluoroacetamidomethyl-3-trifluoroacetamido-3-O-t rifluoroacetyl-L-lyxo-hexopyranosyl chloride.
Inventors
- 👤 Alberto Bargiotti
- 👤 Giuseppe Cassinelli
- 👤 Sergio Penco
- 👤 Federico Arcamone
- 👤 Annamaria Casazza
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 21:35
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/02; C07H15/04; A; A61; A61P; A61P35/00; A61P35/02; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30; C07H13/00; C07H13/02; C07H13/04; C07H15/20; C07H15/24; C07H15/252
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
65 words
An anthracycline glycoside of the formula I: ##STR5## wherein R 1 is hydrogen or hydroxy; R 2 is hydrogen or trifluoroacetyl; R 3 is methyl, hydroxymethyl, aminomethyl or trifluoroacetylaminomethyl; and R 4 is hydrogen or hydroxy, with the proviso that when R 4 is hydroxy, R 3 is aminomethyl; or R 3 and R 4 together form methylene, and pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim
65 words
An anthracycline glycoside of the formula I: ##STR5## wherein R 1 is hydrogen or hydroxy; R 2 is hydrogen or trifluoroacetyl; R 3 is methyl, hydroxymethyl, aminomethyl or trifluoroacetylaminomethyl; and R 4 is hydrogen or hydroxy, with the proviso that when R 4 is hydroxy, R 3 is aminomethyl; or R 3 and R 4 together form methylene, and pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim
12 words
A compound according to claim 1 wherein the salt is the hydrochloride.
Claim 4
Dependent Claim
10 words
A compound according to claim 1 which is 4'-deoxy-4'-C-methylene-daunorubicin hydrochloride.
Claim 5
Dependent Claim
10 words
A compound according to claim 1 which is 4'-deoxy-4'-epi-C-methyl-daunorubicin hydrochloride.
Claim 6
Dependent Claim
10 words
A compound according to claim 1 which is 4'-deoxy-4'-epi-C-methyl-doxorubicin hydrochloride.
Claim 7
Dependent Claim
10 words
A compound according to claim 1 which is 4'-C-aminomethyl-daunorubicin hydrochloride.
Claim 8
Dependent Claim
10 words
A compound according to claim 1 which is 4'-C-aminomethyl-doxorubicin hydrochloride.
Claim 9
Dependent Claim
10 words
A sugar compound selected from the group consisting of ##STR6##
Claim 10
Dependent Claim
10 words
A sugar compound selected from the group consisting of ##STR6##
Claim 11
Dependent Claim
26 words
A pharmaceutical composition for treating P388 ascitic leukemia comprising a therapeutically effective amount of a compound according to claim 1 in combination with a carrier therefor.
Claim 12
Dependent Claim
28 words
A method of inhibiting the growth of P388 ascitic leukemia comprising administering to a mammal afflicted therewith, a therapeutically effective amount of a compound according to 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) | 1986-07-11 | 1987-01-10 | 1987-07-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-07-11 | 1991-01-10 | 1991-07-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-07-11 | 1995-01-10 | 1995-07-12 | $7700.00 | Window Closed / Lapsed |