US4133877A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Anthracycline ethers and use therefor
Assignee: Pfizer Italia SRL
•
Filing: 1977-07-22
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Granted: 1979-01-09
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Expires: 1997-07-22
Abstract
Abstract Novel antitumor antibiotics, which are daunomycin analogues of the formula: <IMAGE> I wherein R1 is hydrogen or a C1-C4 lower alkyl, R2 is a C1-C4 lower alkyl, a C3-C6 cycloalkyl, phenyl, lower alkyl phenyl, lower alkoxy phenyl or halophenyl, and R3 is hydrogen or trifluoroacetyl are prepared by condensing 2,3,6-trideoxy-3-trifluoroacetamido-4-0-trifluoroacetyl- alpha -L-lyxopyranosyl chloride with novel aglycones of the formula: <IMAGE> II, which are in turn prepared by a novel method from 14-bromodaunomycinone through a series of novel intermediates.
Inventors
- 👤 Paolo Masi
- 👤 Antonino Suarato
- 👤 Pietro Giardino
- 👤 Luigi Bernardi
- 👤 Federico Arcamone
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 19:12
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/20; C07H15/24; C07H15/252; A; A61; A61P; A61P35/00
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
65 words
A compound of the formula: ##STR11## wherein R 1 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms, R 2 is a lower alkyl having from 1 to 4 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl, lower alkyl phenyl, lower alkoxy phenyl or halophenyl, and R 3 is hydrogen or trifluoroacetyl and pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim
65 words
A compound of the formula: ##STR11## wherein R 1 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms, R 2 is a lower alkyl having from 1 to 4 carbon atoms, cycloalkyl having 3 to 6 carbon atoms, phenyl, lower alkyl phenyl, lower alkoxy phenyl or halophenyl, and R 3 is hydrogen or trifluoroacetyl and pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim
9 words
A compound according to claim 1 which is N-trifluoroacetyl-14-ethoxydaunomycin.
Claim 4
Dependent Claim
9 words
A compound according to claim 1 which is N-trifluoroacetyl-14-methoxydaunomycin.
Claim 5
Dependent Claim
9 words
A compound according to claim 1 which is N-trifluoroacetyl-14-isopropyloxydaunomycin.
Claim 6
Dependent Claim
9 words
A compound according to claim 1 which is N-trifluoroacetyl-14-phenoxydaunomycin.
Claim 7
Dependent Claim
9 words
A compound according to claim 1, which is N-trifluoroacetyl-14-p-chlorophenoxydaunomycin.
Claim 8
Dependent Claim
9 words
A compound according to claim 1, which is N-trifluoroacetyl-14-p-methoxyphenoxydaunomycin.
Claim 9
Dependent Claim
9 words
A compound according to claim 1, which is N-trifluoroacetyl-14-o-methylphenoxydaunomycin.
Claim 10
Dependent Claim
9 words
A compound according to claim 1, which is N-trifluoroacetyl-14-m-methoxyphenoxydaunomycin.
Claim 11
Dependent Claim
9 words
A compound according to claim 1, which is 14-ethoxydaunomycin.HCl.
Claim 12
Dependent Claim
9 words
A compound according to claim 1, which is 14-methoxydaunomycin.HCl.
Claim 13
Dependent Claim
9 words
A compound according to claim 1, which is 14-isopropyloxydaunomycin.HCl.
Claim 14
Dependent Claim
9 words
A compound according to claim 1, which is 14-p-chlorophenoxydaunomycin.HCl.
Claim 15
Dependent Claim
9 words
A compound according to claim 1, which is 14-p-methoxyphenoxydaunomycin.HCl.
Claim 16
Dependent Claim
9 words
A compound according to claim 1, which is 14-o-methylphenoxydaunomycin.HCl.
Claim 17
Dependent Claim
9 words
A compound according to claim 1, which is 14-m-methoxyphenoxydaunomycin.HCl.
Claim 18
Dependent Claim
52 words
A compound of formula: ##STR12## wherein R 1 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms and R 2 is a lower alkyl having from 1 to 4 carbon atoms, cycloalkyl having from 3 to 6 carbon atoms, phenyl, lower alkyl phenyl, lower alkoxy phenyl or halophenyl.
Claim 19
Dependent Claim
52 words
A compound of formula: ##STR12## wherein R 1 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms and R 2 is a lower alkyl having from 1 to 4 carbon atoms, cycloalkyl having from 3 to 6 carbon atoms, phenyl, lower alkyl phenyl, lower alkoxy phenyl or halophenyl.
Claim 20
Dependent Claim
35 words
A method of inhibiting the growth of transplanted lymphocytic leukemia P 388 which comprises administering to a host afflicted therewith, a compound according to claim 1, in an amount sufficient to inhibit the growth thereof.
Claim 21
Dependent Claim
12 words
A method according to claim 18, wherein said compound is administered intraperitoneally.
Claim 22
Dependent Claim
21 words
A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 in combination with a carrier therefor.
References Cited (Backward Citations)
US4058519A
Cited
US4039663A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-01-08 | 1982-07-10 | 1983-01-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-01-08 | 1986-07-10 | 1987-01-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-01-08 | 1990-07-10 | 1991-01-09 | $7700.00 | Window Closed / Lapsed |