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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
•
Filing: 1987-05-18
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Granted: 1988-04-26
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Expires: 2007-05-18
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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 22:28
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/10

Claims Analysis

Total Claims: 17
Claim 1
Independent Claim 114 words
A hydrate of 5-fluoro-2-deoxyuridine derivative represented by the formula [I] or a salt thereof: ##STR42## 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, ##STR43## 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-methylpiperidinio, 4-methylmorpholinio or 2H-1,2,4-triazol-1-io group which are substituted or not 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 alkylamino groups.
Claim 2
Dependent Claim 114 words
A hydrate of 5-fluoro-2-deoxyuridine derivative represented by the formula [I] or a salt thereof: ##STR42## 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, ##STR43## 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-methylpiperidinio, 4-methylmorpholinio or 2H-1,2,4-triazol-1-io group which are substituted or not 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 alkylamino groups.
Claim 3
Dependent Claim 52 words
A hydrate of 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 1, wherein R 1 is a group represented by the formula, ##STR44## wherein R 3 , R 4 and A have the same meaning as defined in claim 1; and R 2 is a C 1-30 aliphatic carboxylic acid residue.
Claim 4
Dependent Claim 19 words
A hydrate of 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 2, wherein A is an ethylene group.
Claim 5
Dependent Claim 22 words
A hydrate of 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 20 words
A hydrate of 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 4, wherein R 4 is a trimethylammonio group.
Claim 7
Dependent Claim 31 words
A hydrate of 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to any one of claims 2, 3, 4 or 5, wherein R 2 is a C 6-18 aliphatic carboxylic acid residue.
Claim 8
Dependent Claim 52 words
A hydrate of 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, ##STR45## wherein R 3 , R 4 and A have the same meanings as defined in claim 1.
Claim 9
Dependent Claim 19 words
A hydrate of 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 7, wherein A is an ethylene group.
Claim 10
Dependent Claim 22 words
A hydrate of 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 20 words
A hydrate of 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 hydrate of 5-fluoro-2'-deoxyuridine derivative or a salt thereof according to claim 7, 8, 9 or 10, wherein R 1 is a C 6-18 aliphatic carboxylic acid residue.
Claim 13
Dependent Claim 18 words
A hydrate of 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 18 words
A hydrate of 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 18 words
A hydrate of 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 18 words
A hydrate of 5-fluoro-2'-deoxyuridine derivative or a 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)

JPS457056Y1 Cited
BE767195A Cited
DE2308801A1 Cited
US3872083A Cited
JPS57128699A Cited
EP0081386A1 Cited
JPS5993096A Cited
US4684631A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-04-26 1991-10-26 1992-04-26 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-04-26 1995-10-26 1996-04-26 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-04-26 1999-10-26 2000-04-26 $7700.00 Window Closed / Lapsed

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