Method and composition

Details Method and composition Method and composition

2000-06-30

2002-06-11

Weddington, Kevin E. (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

C-o-group doai

C514S731000, C514S734000, C514S736000

Reexamination Certificate

active

06403652

ABSTRACT:

FIELD OF THE INVENTION
The indication and inhibition of disease causing bacteria has been one of the most significant events of the twentieth century. Diseases such as tuberculosis, pneumonia, and typhoid which were primary killers of people in the early twentieth century are presently far less significant diseases than they once were. One of the chief reasons for this phenomenon is the successful treatment of bacteria induced illness through the use of antimicrobial drugs such as antibiotics, semi synthetic antibiotics, and chemically synthesized compounds. However, bacteria have developed varying degrees of resistance to some or virtually all of these drugs. These “superbugs” can bring about a disease in a human which can result in death. Although such drug resistant bacteria can be found almost anywhere, they are a particular problem in hospitals, a locus where antibacterial drugs are used in high frequency. It has been recently reported that about 2 million hospital patients per year become infected, resulting in about 60,000 to 80,000 deaths. Staphylococcus bacteria, particularly staphaureus are the leading cause of hospital borne infection. Health care professionals are increasingly concerned about this issue. Greater focus is on the discovery of new chemical entities which will be successful in combating such bacteria.
It has now been discovered that certain types of compounds known to be effective antibacterial materials for many years are also effective against drug resistant bacteria. These compounds, particularly alkyl phenols, are effective against antibiotic resistant
staphylococcus aureas
(
S. aureas
). Specifically, these alkyl phenols are highly effective against methicillin resistant
S. aureas.
SUMMARY OF THE INVENTION
In accordance with the invention, there is a method for inhibiting drug resistant bacteria which comprises administering to a host or surface in need of said treatment a composition comprising an antibacterially effective amount against drug resistant bacteria of a compound or a mixture of compounds of the formula:
wherein
R
1
is selected from the group consisting of branched alkyl of four to about twenty carbon atoms, cycloalkyl of from four to about eight carbon atoms, mono cycloalkyl substituted alkyl of from four to about twelve carbon atoms where cycloalkyl is about four to about eight carbon atoms, and mono to tetra alkyl substituted cycloalkyl of from four to about eight carbon atoms wherein alkyl is one to about four carbon atoms;
R
2
is at the 4 or 5 position and is selected from the group consisting of branched alkyl of four to about twenty carbon atoms, cycloalkyl of from four to about eight carbon atoms, mono cycloalkyl substituted alkyl of from four to about twelve carbon atoms where cycloalkyl is about four to about eight carbon atoms, and mono to tetra alkyl substituted cycloalkyl of from four to about eight carbon atoms wherein alkyl is one to about four carbon atoms;
wherein n is 0 or 1 and R
4
is selected from the group consisting of hydrogen, alkyl of one to about twenty carbon atoms, cycloalkyl of from four to about eight carbon atoms, mono cycloalkyl substituted alkyl of from four to about twelve carbon atoms where cycloalkyl is about four to about eight carbon atoms, and mono to tetra alkyl substituted cycloalkyl of from four to about eight carbon atoms wherein alkyl is one to about four carbon atoms.
R
3
is selected from the group consisting of hydrogen and alkyl of three to eight carbon atoms with the provisio that when R
2
is at the 4 position then R
3
is at the 5 position and when R
2
is at the 5 position then R
3
is at the 4 position; and pharmaceutically acceptable salts thereof.


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Biological Activity of Essential Oils and Their Constituents by Tetsuo Nakatsu, Andrew T.. Lupo Jr., John W. Chinn Jr., and Raphael K.L. Kang, Takasago Institute for Interdisciplinary Science, 4 Volvo Dr., Rockleigh, NJ 07647 U.S.A.

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