Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2001-07-11
2003-05-27
Padmanabhan, Sreeni (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S354000
Reexamination Certificate
active
06569864
ABSTRACT:
CROSS-REFERENCES TO RELATED APPLICATIONS
Not applicable.
STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT
Not applicable.
REFERENCE TO MICROFICHE APPENDIX
Not applicable.
FIELD OF THE INVENTION
This invention relates to pharmaceutical agents for the treatment of viral diseases, and more specifically, to pharmaceutical agents containing acyclovir and fusaric acid or derivatives thereof.
BACKGROUND OF THE INVENTION
Acyclovir, 2-amino-1,9-dihydro-9-[(2-hydroxyethoxy)metyl]-6H-purin-6-one, has been used for the inhibition of herpes simplex virus types 1 (HSV-1), 2 (HSV-2), and varicella-zoster virus (VZV). Acyclovir is a synthetic purine nucleoside analogue with in vitro and in vivo inhibitory activity against HSV-1, HSV-2 and VZV, which can be found in capsule, tablet, topical and suspension formulations. The following structural formula represents acyclovir:
The inhibitory activity of acyclovir is highly selective due to its affinity for the enzyme thymidine kinase encoded by HSV-1, HSV-2 and VZV. This viral enzyme converts acyclovir into acyclovir monophosphate, a nucleotide analogue. The monophosphate is further converted into diphosphate by cellular guanylate kinase and into triphosphate by a number of cellular enzymes. In vitro, acyclovir triphosphate stops replication of herpes viral DNA. This is accomplished by: 1) competitive inhibition of viral DNA polymerase, 2) incorporation into and termination of the growing viral DNA chain and 3) inactivation of the viral DNA polymerase.
While the use of acyclovir is useful in the treatment of some herpes viruses, it has limitations related to tissue permeability and viral resistance that make its use less desirable. For example, acyclovir is not effective in topical formulation against herpes labialis and herpes genitalis. As such, acyclovir may not be used topically to effectively treat herpes labialis, herpes genitalis or other viral diseases, disorders, or conditions. Moreover, prodrugs of acyclovir have only minimal effects in herpes labialis. For example, the use of denavir to treat herpes labialis reduces the median duration of the illness by 6 hours. However, herpes labialis typically lasts in the range of about 6 to 7 days. Also, viral strains resistant to acyclovir and its prodrugs have emerged, which further limit its clinical usefulness.
Accordingly, there is a need to provide compositions that may be used topically to successfully treat a wide range of viral diseases.
SUMMARY OF THE INVENTION
In overcoming the above disadvantage, it is an object of the invention to produce compositions, which may be used topically to successfully treat a wide range of viral diseases.
Accordingly, and in one aspect of the invention, a composition including at least one nucleoside analogue inhibitor, a pharmaceutically acceptable salt, solvate, or prodrug thereof and fusaric acid, a derivative, or pharmaceutically acceptable salt of fusaric acid is provided.
In a second aspect, a pharmaceutical composition comprising the above-described composition of the invention and a pharmaceutically acceptable carrier is provided.
In a third aspect, a method of treating a viral disease, disorder, or condition comprising the administration of a pharmaceutically effective dose of the above-described pharmaceutical composition to a patient is provided.
In a fourth aspect, a topical preparation is provided that includes at least one above-described composition of the invention and a liquid vehicle.
In a fifth aspect, a systemic preparation is provided that includes at least one above-described pharmaceutical composition.
Other objects and features will be in part apparent and in part pointed out hereinafter.
REFERENCES:
patent: 5767135 (1998-06-01), Fernandez-Pol
patent: 6127393 (2000-10-01), Fernandez-Pol
Zouiran Cream Summary of Product Characteristics, Feb. 2000, pp. 1-5.*
Transfusion Science, vol. 23, No. 3, Dec. 2000 (249-250); “Combining iron chelators with the nucleoside analog didanosine in anti-HIV Therapy”; by Georgiou, Niki A. et al.
Journal of Chemotherapy, vol. 5, No. 1 (3-9) 1993: Mode of Action of Zn-Complexes on Herpes Simplex Virus Type 1 Infection In Vitro; by T.L. Varadinova, P.R. Bontchev; C.K. Nachev; S.A. Shishkov; D. Strachilov; Z. Paskalev; A. Toutekova and M. Panteva.
Journal of Pharmaceutical Sciences, vol. 77, No. 4, Apr. 1988 (285-298): Glycolamide Esters as Biolabile Prodrugs of Carboxylic Acid Agents: Synthesis, Stability, Bioconversion, and Physicochemical Properties; by Neils Mork Nielsen and Hans Bungaard.
Handbook of Animal Models of Infection 1988, Aug.; 9 (5) 911-918; Animal Models of Herpes Skin Infection: Guinea-pig by Spruance SL, McKeough MB.
Journal of Pharmaceutical Sciences, an.1977; vol. 66 (1): 1-19. Pharmaceutical Salts; Berge SM, Bighley LD et al.
Anticancer Research 21:931-958 (2001) Essential Viral and Cellular Zinc and Iron Containing Metalloproteins as Targets for Novel Antiviral and Anticancer Agents: Implications for Prevention and Therapy of Viral Diseases and Cancer; J. Alberto Fernandez-Pol, Paul D. Hamilton and Dennis J. Klos.
Amin Avinash N.
Douglas Michael G.
Amos Ahaji K.
Bahar Mojdeh
Novactyl, Inc.
Thompson & Coburn LLP
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