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US4605645A
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5-fluoro-2'-deoxyuridine derivatives and a process for the preparation thereof
Assignee: Teijin Ltd
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Filing: 1982-12-09
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Granted: 1986-08-12
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Expires: 2002-12-09
Abstract
Abstract 5-fluoro-2'-deoxyuridine derivatives expressed by general formula (1) and their pharmacologically permissible salts ##STR1## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; the letter n indicates 0 or 1, and when n is 0, it indicates that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, or substituted phenyl group; however, when Y is a hydrogen atom, n is 1; R indicates a hydrogen atom or alcohol-protecting group. These compounds have a very strong antitumor activity.
Inventors
- 👤 Kenzo Watanabe
- 👤 Yoshinori Kato
- 👤 Masahiko Saito
- 👤 Takeo Oba
- 👤 Hisashi Fukushima
- 👤 Takeshi Hara
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 23:15
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/10; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
138 words
5-fluoro-2'-deoxyuridine derivatives expressed by general formula (1) and their pharmacologically permissible salts ##STR23## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; n indicates 0 or 1, and when n is 0, it indicated that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, halogen-substituted phenyl group, alkyl-substituted phenyl group having 1 to 8 carbon atoms in the alkyl group, or an acyl substituted phenyl group having 1 to 8 carbon atoms in the acyl group; however, when Y is a hydrogen atom, n is 1; R indicates hydrogen atom or alcohol-protecting group, and wherein, when Y in general formula (1) is a hydrogen atom, A is a member selected from saturated or unsaturated divalent aliphatic hydrocarbon groups having 8 to 24 carbon atoms.
Claim 2
Dependent Claim
138 words
5-fluoro-2'-deoxyuridine derivatives expressed by general formula (1) and their pharmacologically permissible salts ##STR23## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; n indicates 0 or 1, and when n is 0, it indicated that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, halogen-substituted phenyl group, alkyl-substituted phenyl group having 1 to 8 carbon atoms in the alkyl group, or an acyl substituted phenyl group having 1 to 8 carbon atoms in the acyl group; however, when Y is a hydrogen atom, n is 1; R indicates hydrogen atom or alcohol-protecting group, and wherein, when Y in general formula (1) is a hydrogen atom, A is a member selected from saturated or unsaturated divalent aliphatic hydrocarbon groups having 8 to 24 carbon atoms.
Claim 3
Dependent Claim
67 words
5-Fluoro-2'-deoxyuridine derivatives according to claim 1, wherein, when Y in general formula (1) is a phenyl group, halogen-substituted phenyl group, alkyl-substituted phenyl group having 1 to 8 carbon atoms in the alkyl group, or an acyl-substituted phenyl group having 1 to 8 carbon atoms in the acyl group, A is a member selected from saturated or unsaturated divalent aliphatic hydrocarbon groups haveng 3 to 8 carbon atoms.
Claim 4
Dependent Claim
51 words
5-Fluoro-2'-deoxyuridine derivatives according to claim 1, wherein, when Y in general formula (1) is a phenyl group, halogen-substituted phenyl group, alkyl-substituted phenyl group having 1 to 8 carbon atoms in the alkyl group, or an acyl-substituted phenyl group having 1 to 8 carbon atoms in the acyl group, n is 0.
Claim 5
Dependent Claim
33 words
5-Fluoro-2'-deoxyuridine derivatives according to claim 1, wherein R in general formula (1) is a member selected from the group consisting of a hydrogen atom and acyl group having 1 to 10 carbon atoms.
Claim 6
Dependent Claim
168 words
An anti-tumor agent comprising a pharmaceutically acceptable carrier and a composition having anti-tumor activity on tumors transplanted into test animals comprising an anti-tumor effective amount of one or more 5-fluoro-2'-deoxyuridine derivatives expressed by the general formula (1) and their pharmacologically permissible salts ##STR24## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; n indicates 0 or 1, and when n is 0, it indicates that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, halogen-substituted phenyl group, alkyl-substituted phenyl group having 1 to 8 carbon atoms in the alkyl group, or an acyl substituted phenyl group having 1 to 8 carbon atoms in the acyl group; however when Y is a hydrogen atom, n is 1; R indicates hydrogen atom or alcohol-protecting group, and wherein, when Y in general formula (1) is a hydrogen atom, A is a member selected from saturated or unsaturated divalent aliphatic hydrocarbon groups having 8 to 24 carbon atoms.
Claim 7
Dependent Claim
168 words
An anti-tumor agent comprising a pharmaceutically acceptable carrier and a composition having anti-tumor activity on tumors transplanted into test animals comprising an anti-tumor effective amount of one or more 5-fluoro-2'-deoxyuridine derivatives expressed by the general formula (1) and their pharmacologically permissible salts ##STR24## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; n indicates 0 or 1, and when n is 0, it indicates that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, halogen-substituted phenyl group, alkyl-substituted phenyl group having 1 to 8 carbon atoms in the alkyl group, or an acyl substituted phenyl group having 1 to 8 carbon atoms in the acyl group; however when Y is a hydrogen atom, n is 1; R indicates hydrogen atom or alcohol-protecting group, and wherein, when Y in general formula (1) is a hydrogen atom, A is a member selected from saturated or unsaturated divalent aliphatic hydrocarbon groups having 8 to 24 carbon atoms.
Claim 8
Dependent Claim
68 words
An anti-tumor agent according to claim 5, wherein, when Y in general formula (1) is a phenyl group halogen-substituted phenyl group, alkyl-substituted phenyl group having 1 to 8 carbon atoms in the alkyl group, or an acyl-substituted phenyl group having 1 to 8 carbon atoms in the acyl group, A is a member selected from saturated or unsaturated divalent aliphatic hydrocarbon groups having 3 to 8 carbon atoms.
Claim 9
Dependent Claim
52 words
An anti-tumor agent according to claim 5, wherein, when Y in general formula (1) is a phenyl group, halogen-substituted phenyl group, alkyl-substituted phenyl group having 1 to 8 carbon atoms in the alkyl group, or an acyl-substituted phenyl group having 1 to 8 carbon atoms in the acyl group, n is 0.
Claim 10
Independent Claim
137 words
A method of anti-tumor therapy comprising the use of a composition having anti-tumor activity on tumors transplanted into test animals comprising an anti-tumor effective amount of 5-fluoro-2'-deoxyuridine derivatives expressed by the general formula (1) and their pharmacologically permissible salts ##STR25## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; n indicates 0 or 1, and when n is 0, it indicates that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, or substituted phenyl group; however, when Y is a hydrogen atom, n is 1; R indicates hydrogen atom or alcohol-protecting group, and wherein, when Y in general formula (1) is a hydrogen atom, A is a member selected from saturated or unsaturated divalent aliphatic hydrocarbon groups having 8 to 24 carbon atoms.
Claim 11
Independent Claim
137 words
A method of anti-tumor therapy comprising the use of a composition having anti-tumor activity on tumors transplanted into test animals comprising an anti-tumor effective amount of 5-fluoro-2'-deoxyuridine derivatives expressed by the general formula (1) and their pharmacologically permissible salts ##STR25## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; n indicates 0 or 1, and when n is 0, it indicates that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, or substituted phenyl group; however, when Y is a hydrogen atom, n is 1; R indicates hydrogen atom or alcohol-protecting group, and wherein, when Y in general formula (1) is a hydrogen atom, A is a member selected from saturated or unsaturated divalent aliphatic hydrocarbon groups having 8 to 24 carbon atoms.
Claim 12
Dependent Claim
43 words
A method of antitumor therapy according to claim 8, wherein, when Y in general formula (1) is a phenyl group or substituted phenyl group, A is a member selected from saturated or unsaturated divalent aliphatic hydrocarbon groups having 3 to 8 carbon atoms.
Claim 13
Dependent Claim
27 words
A method of antitumor therapy according to claim 8, wherein, when Y in general formula (1) is a phenyl group or substituted phenyl group, n is 0.
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