US3971784A
Expired / Lapsed
US
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5-Fluorouracil derivatives
Assignee: Mitsui Pharmaceuticals Inc
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Filing: 1974-11-25
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Granted: 1976-07-27
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Expires: 1994-11-25
Abstract
Abstract 5-Fluorouracil derivatives represented by the formula ##SPC1## Wherein R is arylcarbonyl, substituted arylcarbonyl, heterocyclic carbonyl, alkylsulfonyl, arylsulfonyl, substituted arylsulfonyl, heterocyclic sulfonyl or alicyclic sulfonyl are effective antimetabolites useful in mammary gland or gastrointestinal cancer therapy.
Inventors
- 👤 Masao Tada
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 13:14
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/52; C07D239/54; C07D239/545; C07D239/553; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61P; A61P35/00; A61P37/00; A61P37/02; A61P37/06
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
23 words
A 5-fluorouracil derivative represented by the formula ##SPC5## wherein R 1 represents phenyl, halogen substituted phenyl, nitro substituted phenyl, methylphenyl, methoxyphenyl or 2-furyl.
Claim 2
Dependent Claim
23 words
A 5-fluorouracil derivative represented by the formula ##SPC5## wherein R 1 represents phenyl, halogen substituted phenyl, nitro substituted phenyl, methylphenyl, methoxyphenyl or 2-furyl.
Claim 3
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 1 wherein R 1 is p-chlorophenyl and the compound is 1-(p-chlorobenzoyl)-5-fluorouracil.
Claim 4
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 1 wherein R 1 is p-methoxyphenyl and the compound is 5-fluoro-1-(p-methoxybenzoyl)uracil.
Claim 5
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 1 wherein R 1 is p-nitrophenyl and the compound is 5-fluoro-1-(p-nitrobenzoyl)uracil.
Claim 6
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 1 wherein R 1 is phenyl and the compound is 1-benzoyl-5-fluorouracil.
Claim 7
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 1 wherein R 1 is p-methylphenyl and the compound is 5-fluoro-1-(p-methylbenzoyl)uracil.
Claim 8
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 1 wherein R 1 is o-methoxyphenyl and the compound is 5-fluoro-1-(o-methoxybenzoyl)uracil.
Claim 9
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 1 wherein R 1 is 2,4-dichlorophenyl and the compound is 1-(2,4-dichlorobenzoyl)-5-fluorouracil.
Claim 10
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 1 wherein R 1 is o-methylphenyl and the compound is 5-fluoro-1-(o-methylbenzoyl)uracil.
Claim 11
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 1 wherein R 1 is 2-furyl and the compound is 5-fluoro-1-(2-furoyl)uracil.
Claim 12
Dependent Claim
34 words
A 5-fluorouracil derivative represented by the formula ##SPC6## wherein R 2 represents methyl, ethyl, phenyl, methyl or ethyl substituted phenyl, halogen substituted phenyl, nitro substituted phenyl, acetamido substituted phenyl, naphthyl, thiofuryl, quinolyl or camphoryl.
Claim 13
Dependent Claim
34 words
A 5-fluorouracil derivative represented by the formula ##SPC6## wherein R 2 represents methyl, ethyl, phenyl, methyl or ethyl substituted phenyl, halogen substituted phenyl, nitro substituted phenyl, acetamido substituted phenyl, naphthyl, thiofuryl, quinolyl or camphoryl.
Claim 14
Dependent Claim
18 words
The 5-l -fluorouracil derivative according to claim 11 wherein R 2 is methyl and the compound is 5-fluoro-1-methanesulfonyluracil.
Claim 15
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is phenyl and the compound is 1-benzenesulfonyl-5-fluorouracil.
Claim 16
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is p-tolyl and the compound is 5-fluoro-1-(p-toluenesulfonyl)uracil.
Claim 17
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is o-methylphenyl and the compound is 5-fluoro-1-(o-methylbenzenesulfonyl)uracil.
Claim 18
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 1 is ethyl and the compound is 1-ethylsulfonyl-5-fluorouracil.
Claim 19
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is p-chlorophenyl and the compound is 1-(p-chlorobenzenesulfonyl)-5-fluorouracil.
Claim 20
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is p-iodophenyl and the compound is 5-fluoro-1-(p-iodobenzenesulfonyl)uracil.
Claim 21
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is p-ethylphenyl and the compound is 1-(p-ethylbenzenesulfonyl)-5-fluorouracil.
Claim 22
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is p-acetamidophenyl and the compound is 1-(p-acetamidobenzenesulfonyl)-5-fluorouracil.
Claim 23
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is 2,4,6-trimethylphenyl and the compound is 5-fluoro-1-(2,4,6-trimethylbenzenesulfonyl)uracil.
Claim 24
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is o-nitrophenyl and the compound is 5-fluoro-1-(o-nitrobenzenesulfonyl)uracil.
Claim 25
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is β-naphthyl and the compound is 5-fluoro-1-(naphthalene-β-sulfonyl)uracil.
Claim 26
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is p-bromophenyl and the compound is 1-(p-bromobenzenesulfonyl)-5-fluorouracil.
Claim 27
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is 2-thiofuryl and the compound is 5-fluoro-1-(2-thiophenesulfonyl)uracil.
Claim 28
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is 8-quinolyl and the compound is 5-fluoro-1-(8-quinolinesulfonyl)uracil.
Claim 29
Dependent Claim
17 words
The 5-fluorouracil derivative according to claim 11 wherein R 2 is camphoryl and the compound is 1-(d-camphorsulfonyl)-5-fluorouracil.
References Cited (Backward Citations)
US3360520A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-07-27 | 1980-01-26 | 1980-07-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-07-27 | 1984-01-26 | 1984-07-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-07-27 | 1988-01-26 | 1988-07-27 | $7700.00 | Window Closed / Lapsed |