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5-(E)-bromovinyl uracil analogues and related pyrimidine nucleosides as anti-viral agents and methods of use

a technology of bromovinyl uracil and pyrimidine nucleosides, which is applied in the field of 5(e)bromovinyl uracil analogues and related pyrimidine nucleosides as antiviral agents, can solve the problems of limiting their use, vzv infections can be life-threatening, and the host cell toxicity remains a more difficult and less treatable target, so as to prevent or delay the onset of viral

Inactive Publication Date: 2004-03-18
CHENG YUNG CHI +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0015] It is an additional object of the present invention to provide, in certain embodiments a method of increasing the retention or metabolic / catabolic half-life of 5-Fluorouracil in cancer patients.

Problems solved by technology

As human bacterial infections have become more manageable and treatable through the use of increasingly available antibiotic agents, viral infections have remained a more difficult and less treatable target.
The course of varicella is generally benign in immunocompetent patients, however, in immunocompromised patients, particularly patients suffering from the acquired immune deficiency syndrome (AIDS), transplant recipients, and cancer patients, VZV infections can be life-threatening.
ever, the efficacy and low oral bioavailability of ACV (De Miranda and Blum, "Pharmacokinetics of acyclovir after intravenous and oral administration." J.
However, metabolic stability of BVDU by pyrimidine nucleoside phosphorylase and, recently, drug interaction of BVaraU with anticancer agent 5-FU, which resulted in death of several patients with cancer and herpes zoster, have been potential drawbacks and limit their use.
ever, the carba derivatives perform very poorly in vivo although they are resistant to degradation and in cell cultures have antiviral activities comparable to those of the parent compounds. Spa
Certain patients, in particular, those with suppressed immune systems such as AIDS patients and organ transplant patients who are being treated with immunosuppressive agents, are particularly susceptible to EBV manifestations, especially the development of EBV-associated lymphomas.

Method used

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  • 5-(E)-bromovinyl uracil analogues and related pyrimidine nucleosides as anti-viral agents and methods of use
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  • 5-(E)-bromovinyl uracil analogues and related pyrimidine nucleosides as anti-viral agents and methods of use

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Embodiment Construction

[0094] General Methods. Melting points were determined on a Mel-temp II and are uncorrected. .sup.1H NMR spectra were recorded on a Bruker 400 AMX spectrometer for 400 MHz, with Me.sub.4Si as internal standard. Chemical shifts (b) are reported in parts per million (ppm) and signals are reported as s (singglet), d (doublet), t (triplet), q (quartet), m (multiplet), or br s (broad singlet). IR spectra were measured on a Nicolet 510P FT IR spectrometer. Optical rotations were perfomed on a Jasco DIP-370 Digital Polarimeter. TLC were performed on Uniplates (silica gel) purchased from Analtech Co. Column chromatography was performed using either Silica Gel-60 (220-440 mesh) for flash chromatography or Silica Gel G (TLC grade>440 mesh) for vacuum flash column chromatography. LV spectra were obtained on a Beckman DU 650 spectrophotometer. Elemental analysis was performed by Atlantic Microlab, Inc., Norcross, Ga.

[0095] 3',5'-Di-O-benzoyl-2'-bromo-2'-deoxy-L-uridine (2). To a suspension of 1...

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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.

Description

[0001] 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 rentention or the metabolic / catabolic half-life of 5-fluorouracil (FU) in cancer patients is also described.[0002] As human bacterial infections have become more manageable and treatable through the use of increasingly available antibiotic agents, viral infections have remained a more difficult and less treatable target. Emphasis in finding agents to treat viral infections has remained a high priority. Problematic virus is Varicella zoster virus, Epstein Barr virus and Kaposi's Sarcoma virus.[0003] Varicella zoster virus (VZV), a member of the herpes virus family, is a main causative agent for a primary infection (varicella and ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07H19/06
CPCC07H19/06
Inventor CHENG, YUNG-CHICHU, CHUNG K.LI, LINGCHAI, YONGSCOK
Owner CHENG YUNG CHI
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