Fullerene pharmaceutical compositions for preventing or...

Details Fullerene pharmaceutical compositions for preventing or... Fullerene pharmaceutical compositions for preventing or...

2001-10-17

2004-08-17

Reamer, James H. (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Radical -xh acid, or anhydride, acid halide or salt thereof...

C514S553000, C514S075000, C514S080000

Reexamination Certificate

active

06777445

ABSTRACT:

RELATED APPLICATION DATA
This Application claims priority under 35 U.S.C. §119 to Taiwanese (ROC) Application No. 089105485, filed Mar. 24, 2000, now Taiwanese (ROC) Patent No. 09011012000.
1. Field of the Invention
The present invention relates to the use of fullerenes in preventing or treating disorders, particularly infections.
2. Background of the Invention
Fullerenes are formed when vaporized carbon condenses in an inert gas atmosphere. Fullerenes are a class of carbon molecule having an even number of carbon atoms arranged in the form of a cluster, such as a closed hollow cage, typically spheroid like a soccer ball, wherein the carbon-carbon bonds define a polyhedral structure. The carbon clusters contain an even amount of carbon atoms, generally ranging from 40-80 carbon atoms. Typically, fullerenes each have 12 pentagons, but differing numbers of hexagons. This is in accordance with Euler's law that states that for any polygon with n edges, where n is an even number greater than 22, at least one polyhedron can be constructed with 12 pentagons and (n−20)/2 hexagons. The pentagons are required in order to allow curvature and eventual closure of the surface upon itself. The majority of the fullerenes produced are C
60
and C
70
. The most abundant species to date is the C
60
molecule known as buckminsterfullerene, named after R. Buckminster Fuller, the architect of the geodesic dome. Its crystal and molecular structure have been resolved using single-crystal x-ray diffraction methods (S. Uu, et al.,
Science,
254:408-410, 1991). C
60
consists of 12 pentagons and 20 hexagons and is classified as an icosahedron, the highest symmetry structure possible.
Several functionalized fullerene derivatives have been reported. For example, fullerenes with relatively small functional groups or addends such as amido, alkoxy, and halides have been described. Macromolecules have also been reported to attach fullerenes.
Fullerenes containing multiple covalently attached substituents or multiple covalently attached amine-derived substituents (A. Hirsch, et al.,
Angew. Chem. Int. Ed. Engl.,
30:1309-1310, 1991; V. Mehrotra, et al.,
Chem. Mat.,
4:20-22, 1992) have been shown to have water solubility, but the lability of the former, and the configurational dynamism and complex isomerism of the latter compound would preclude a ready and unequivocal evaluation of structure-activity data in biological systems. Polyhydroxylated, water-soluble fullerenes have also been prepared, but no single, fully characterized isomer has been isolated to date (L. Y. Chiang, et al., J. Chem. Soc. Chem. Commun., 1992:1701-1793, 1992).
There are several studies on the biological activities of fullerene derivatives (Da Ros, T. et al.,
Chem. Commun.
1999:663). The size, hydrophobicity, and electronic effects of fullerenes make these molecules particularly attractive for biomedical investigations. Functionalized fullerenes can be used in photodynamic therapy (Tokuyama, H., et al.,
J. Am. Chem. Soc.,
115:7918); as inhibitors of HIV-1 protease (Friedman, S. H. et al.,
J. Am. Chem. Soc.,
115:6505; Sijbesma, R. et al.,
J. Am. Chem. Soc.,
115:6510); as neuroprotective agents (Dugan L. L. et al.,
Proc. Natl. Acad. Sci. USA
94:9434-9439); as antiapoptotic agents (Hsu S. C. et al.,
Blood
91:2658-2663; Huang, Y. L. et al.,
Eur. J. Biochem.
254:38-43); as a protective agent against iron-induced oxidative stress (Lin, A. M. et al.,
J. Neurochem.
72:1634-1640); or as an in vitro antibacterial agent (Da Ros, T. et al.,
J. Org. Chem.,
1996, 61:9070). However, none of these teach the administration to mammalian subjects of water soluble fullerene derivatives to treat certain bacterial infections, such as
E. coli., Staphylococcus aureus
, Group A Streptococcus, Group B Streptococcus, vancomycin-resistant Enterococcus infections or bacterial meningitis. Nor do these teach the use of such fullerene compounds to treat viral infections, such as infections caused by dengue 2 virus or Japanese encephalitis virus.
Additionally, current therapies for the above-mentioned infections have numerous disadvantages, such as toxicity and poor efficacy. Therefore, there is a definite need for additional pharmacotherapies to treat these diseases.
SUMMARY OF THE INVENTION
The foregoing problems are solved and a technical advance is achieved in the present invention. The present invention generally comprises the in vivo administration of fullerenes to treat a variety of diseases.
Other features or advantages of the present invention will be apparent from the following detailed description of several embodiments of the invention and from the claims.


REFERENCES:
patent: 5475172 (1995-12-01), Cahill et al.
patent: 5587476 (1996-12-01), Kampe et al.
patent: 5648523 (1997-07-01), Chiang
patent: 5994410 (1999-11-01), Chiang et al.
patent: 6162926 (2000-12-01), Murphy et al.
Jensen et al, Bioorganic & Medicinal Chemistry, vol. 4(6), pp. 767-779, 1996.*
Lin et al, Virology, vol. 275, pp. 258-262, 2000.*
Wang et al, J. Med. Chem., vol. 42, pp. 4614-4620, 1999.

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