US2004053891A1PendingUtilityA1
5-(E)-bromovinyl uracil analogues and related pyrimidine nucleosides as anti-viral agents and methods of use
Priority: Jul 21, 1999Filed: Sep 2, 2003Published: Mar 18, 2004
Est. expiryJul 21, 2019(expired)· nominal 20-yr term from priority
C07H 19/06
54
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Claims
Abstract
The present invention relates to pyrimidine nucleoside compounds and their use to treat viral infections of Varicella Zoster Virus, Epstein Barr Virus and Kaposi's Sarcoma virus, also known as HV-8 and related complications of these viral infections. In another aspect of the present invention, the use of one or more nucleoside compound to increase the retention or half-life of 5-fluorouracil (FU) in patients is also described.
Claims
exact text as granted — not AI-modified1 . A method for treating a viral infection in a patient caused by Epstein-Barr virus, Varicella-Zoster virus or Kaposi's Sarcoma virus comprising administering to said patient a therapeutically effective amount of a compound according to the structure:
X is H, F, Br, Cl, I or CH 3 and
R 1 is H, a C 1 to C 20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group.
2 . The method according to claim 1 where R is
and X is H, Cl, Br or I.
3 . The method according to claim 1 where R is Br or I.
4 . The method according to claim 1 where R 1 is a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group
5 . The method according to claim 2 where R 1 is a C 1 to C 20 acyl group, a phosphate group, a triphosphate group or a phosphodiester group
6 . The method according to claim 1 wherein said viral infection is caused by Varicella Zoster virus, R is
and X is Cl, Br or I.
7 . The method according to claim 6 where R 1 is a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group
8 . The method according to claim 6 wherein X is Br or I.
9 . The method according to claim 6 where R 1 is a C 1 to C 20 acyl group, a phosphate group, a triphosphate group or a phosphodiester group
10 . The method according to claim 1 wherein said viral infection is a Varicella Zoster virus infection.
11 . The method according to claim 1 wherein said viral infection is an Epstein Barr virus infection.
12 . The method according to claim 1 wherein said viral infection is an HV-8 virus infection.
13 . The method according to claim 11 wherein R is
and X is Cl, Br or I.
14 . The method according to claim 13 where R 1 is a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group
15 . The method according to claim 1 wherein X is Br or I.
16 . The method according to claim 15 where R 1 is a C, to C 2-0 acyl group, a phosphate group, a triphosphate group or a phosphodiester group.
17 . The method according to claim 12 wherein R is
and X is Cl, Br or I.
18 . The method according to claim 16 where R 1 is a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group
19 . The method according to claim 12 wherein X is Br or I.
20 . The method according to claim 18 where R 1 is a C 1 to C 20 acyl group, a phosphate group, a triphosphate group or a phosphodiester group.
21 . A method for preventing or delaying the onset of an infection caused by the Epstein-Barr virus infection, a Varicella-Zoster virus infection or a HV-8 infection in a patient in need thereof comprising administering to said patient a compound according to the structure:
X is H, F, Br, Cl, I or CH 3 and
R 1 is H, a C 1 to C 20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group.
22 . The method according to claim 20 wherein wherein R is
and X is Cl, Br or I.
23 . The method according to claim 21 where R 1 is a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group
24 . The method according to claim 20 wherein X is Br or I.
25 . The method according to claim 20 where R 1 is a C 1 to C 20 acyl group, a phosphate group, a triphosphate group or a phosphodiester group
26 . The method according to claim 20 wherein said viral infection is caused by Epstein Barr Virus or HV-8, R is
and X is Cl, Br or I.
27 . The method according to claim 25 where R 1 is a C 1 to C 20 acyl group, a phosphate group or a phosphodiester group
28 . The method according to claim 26 wherein X is Br or I.
29 . The method according to claim 20 wherein said viral infection is caused by HV-8, wherein R 1 is a C 1 to C 20 acyl group, a phosphate group, a triphosphate group or a phosphodiester group
30 . A method for preventing or delaying the onset of EBV-related lymphoma or cancer or Kaposi's Sarcoma in patients comprising administering to a patient at risk for an EBV-related lymphoma or cancer or Kaposi's Sarcoma a therapeutically effective amount of a compound according to the formula:
X is H, F, Br, Cl, I or CH 3 and
R 1 is H, a C 1 to C 20 acyl or ether group, a phosphate, diphiosphate, triphosphate or phosphodiester group.
31 . The method according to claim 29 wherein said patient is immunodeficient.
32 . The method according to claim 29 wherein said patient is an organ transplant patient.
33 . The method according to claim 29 wherein said patient has had a blood transfusion.
34 . The method according to claim 29 wherein R is
and X is I or Br.
35 . A method of increasing the retention of 5-Fluorouracil or a prodrug of 5-Fluorouracil in a cancer patient comprising co-administering to said patient along with an anti-cancer effective amount of 5-Fluorouracil an effective amount of at least one compound according to the chemical structure:
X is H, F, Br, Cl, I or CH 3 and
R 1 is H, a C 1 to C 20 acyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group.
36 . The method according to claim 34 wherein R is
and X is Br.
37 . The method according to claim 34 wherein said prodrug of 5-Flurouracil is selected from the group consisting of 2-(1)tetrahydrofurano-5-Fluorouracil and 5-fluoropyrimidin-2-one.Join the waitlist — get patent alerts
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