US4684631A
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Novel 5-fluoro-2-deoxyuridine derivatives and salts thereof, process for producing the same, and antitumor agents containing the same
Assignee: Toyama Chemical Co Ltd
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Filing: 1985-09-30
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Granted: 1987-08-04
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Expires: 2005-09-30
Abstract
Abstract This invention relates to a novel 5-fluoro-2'-deoxyuridine derivative and a salt thereof which have an antitumor effect on mammals, a process for producing the same, and an antitumor agent containing the same.
Inventors
- 👤 Takako Hori
- 👤 Isao Myokan
- 👤 Shinji Miyabara
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 10:26
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/10
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
110 words
A 5-fluoro-2'-deoxyuridine derivative represented by the general formula [I] or a salt thereof: ##STR41## wherein R 1 and R 2 are different from each other, one of which represents a C 1-30 aliphatic carboxylic acid residue and the other represents a group represented by the formula, ##STR42## in which R 3 represents an oxido group, A represents a C 1-5 -alkylene group and R 4 represents a tri-C 1-4 alkylammonio, pyridinio, pyridazinio, pyrimidinio, pyrazinio, 2H-imidazolio, 3H-imidazolio, 2H-pyrazolio, 1-methyl-piperidinio, 4-methylmorpholinio or 2H-1,2,4-triazol-1-io, which may be substituted by at least one substituent selected from the group consisting of hydroxyl, C 1-4 alkoxy, acetyloxy, propionyloxy, C 1-4 alkyl and di-C 1-4 alkyl-amino groups.
Claim 2
Dependent Claim
110 words
A 5-fluoro-2'-deoxyuridine derivative represented by the general formula [I] or a salt thereof: ##STR41## wherein R 1 and R 2 are different from each other, one of which represents a C 1-30 aliphatic carboxylic acid residue and the other represents a group represented by the formula, ##STR42## in which R 3 represents an oxido group, A represents a C 1-5 -alkylene group and R 4 represents a tri-C 1-4 alkylammonio, pyridinio, pyridazinio, pyrimidinio, pyrazinio, 2H-imidazolio, 3H-imidazolio, 2H-pyrazolio, 1-methyl-piperidinio, 4-methylmorpholinio or 2H-1,2,4-triazol-1-io, which may be substituted by at least one substituent selected from the group consisting of hydroxyl, C 1-4 alkoxy, acetyloxy, propionyloxy, C 1-4 alkyl and di-C 1-4 alkyl-amino groups.
Claim 3
Dependent Claim
66 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 1, wherein R 1 is a group represented by the formula, ##STR43## wherein R 3 and A have the same meanings as defined in claim 1, R 4 is a tric-C 1-4 alkylammonio, pyridinio, pyridazinio, pyrimidinio, pyrazinio, 2H-imidazolio, 3H-imidazolio, 2H-pyrazolio, 1-methylpiperidinio, 4-methylmorpholinio or 2H-1,2,4-triazol-1-io group; and R 2 is a C 1-30 -aliphatic carboxylic acid residue.
Claim 4
Dependent Claim
17 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 2, wherein A is an ethylene group.
Claim 5
Dependent Claim
20 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 3, wherein R 4 is a tri-C 1-4 -alkylammonio group.
Claim 6
Dependent Claim
18 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 4, wherein R 4 is a trimethylammonio group.
Claim 7
Dependent Claim
28 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to one of claims 2, 3, 4 and 5, wherein R 2 is a C 6-18 aliphatic carboxylic acid residue.
Claim 8
Dependent Claim
50 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 1, wherein R 1 is a C 1-30 aliphatic carboxylic acid residue and R 2 is a group represented by the formula, ##STR44## wherein R 3 , R 4 and A have the same meanings as defined in claim 1.
Claim 9
Dependent Claim
17 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 7, wherein A is an ethylene group.
Claim 10
Dependent Claim
20 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 8, wherein R 4 is a tri-C 1-4 -alkylammonio group.
Claim 11
Dependent Claim
18 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 9, wherein R 4 is a trimethylammonio group.
Claim 12
Dependent Claim
28 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to one of claims 7, 8, 9 and 10, wherein R 1 is a C 6-18 aliphatic carboxylic acid residue.
Claim 13
Dependent Claim
16 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 1, wherein the derivative is 5-fluoro-2'-deoxy-3'-O-stearoyl-β-uridine-5'-(2-trimethylammonioethyl)phosphate.
Claim 14
Dependent Claim
16 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 1, wherein the derivative is 5-fluoro-2'-deoxy-3'-O-oleoyl-β-uridine-5'-(2-trimethylammonioethyl)phosphate.
Claim 15
Dependent Claim
16 words
A 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 1, wherein the derivative is 5-fluoro-2'-deoxy-5'-O-oleoyl-β-uridine-3'-(2-trimethylammonioethyl)phosphate.
Claim 16
Dependent Claim
15 words
A 5-fluoro-2'-deoxyuridine derivative or salt thereof according to claim 1, wherein the derivative is 5-fluoro-2'-deoxy-5'-O-hexanoyl-β-uridine-3'-(2-trimethylammonioethyl)phosphate.
Claim 17
Dependent Claim
33 words
A pharmaceutical composition useful for treating tumors in a host mammal which comprises an effective amount of the compound in claim 1, in combination with a pharmaceutically acceptable inert excipient, diluent or carrier.
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) | 1990-08-03 | 1991-02-02 | 1991-08-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-08-03 | 1995-02-02 | 1995-08-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-08-03 | 1999-02-02 | 1999-08-04 | $7700.00 | Window Closed / Lapsed |