Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
1998-01-12
2001-09-25
Raymond, Richard L. (Department: 1613)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C549S315000
Reexamination Certificate
active
06294678
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to cancer treatment. More particularly, it relates to a method for treating and curing cancer, and to compounds for use in the treatment. The present invention provides a totally new and unique approach to the identification of the primary carcinogenic lesion and site in DNA and to removal of the lesion and restoration of the site to achieve normal function.
BACKGROUND OF THE INVENTION
A cancer is a malignant tumor of potentially unlimited growth. It is primarily the pathogenic replication (a loss of normal regulatory control) of various given types of cells found in the human body. By select mutation resulting from a primary lesion, the DNA of a cancer cell evolves and converts the cell into an autonomous system. Conventional cancer treatments have focused mainly on killing cancerous cells. Such treatments threaten noncancerous cells, inherently are stressful to the human body, produce many side effects, and are of uncertain efficacy. More important, such treatment regimens are not ordinarily directed toward the actual chemical bond root of the cancer problem.
Cancer cells possess uncontrolled replication. Such uncontrolled replication readily can be caused by a chemical bond lesion in the cell's deoxyribonucleic acid (DNA). Specifically, certain chemical and radiation energy sources can cause chemical bond alterations in DNA. These alterations can and do result in production of photoproducts and chemical energy products in various parts of the genome. One such product, called an ozonide, has the catalytic properties to continuously activate cell replication, to produce mutations within the genome, and to replicate itself by autoxidation. References 1-4. This catalytic lesion in the nucleotide sequence responsible for activating the oncogene is identified herein as the primary carcinogenic lesion, and has served as the basis of the design of the compounds of the present invention. As yet, no compounds, other than those presented herein, have been designed or used specifically to dissociate the chemical bonds of an ozonide in DNA, nor are any treatment methods available that are directed toward correcting this chemical bond aberration to DNA replication, i.e., for eliminating the primary carcinogenic lesion in DNA.
There is an unmet need for a therapeutic regimen for cancer, one that is based on removing a critical lesion in one of DNA's regulatory structures and thus normalizing DNA replication and returning the regulatory system to its normal state whereby it can activate apoptosis (cell suicide). There further is an unmet need for compounds designed to be effective in such a treatment regimen. There also is an unmet need for a treatment regimen and associated compounds that are not toxic to the patient, but that instead simply eliminate the primary carcinogenic lesion and correct the regulatory aberration.
SUMMARY OF THE INVENTION
The present invention relates to a method for cancer treatment and to compounds for use in that treatment. The present invention focuses on the uncontrolled replication of DNA, the primary lesion initiating carcinogenesis, and the TATA box in DNA. The TATA box (so named for its base pair sequence of Thymine-adenine, Adenine-thymine, Thymine-adenine, Adenine-thymine) is located at the beginning of a DNA promoter (a promoter is a section of DNA that directs the binding of ribonucleic acid (RNA) polymerase to initiate transcription). Reference no. 5. The TATA box protein (TBP) activates the box and thus the promoter by bending the box and providing the appropriate cofactors to initiate transcription. References no. 3 and 4. The TATA box functions as a regulatory unit —an on-off switch—for DNA transcription and (via transcription) replication. The on-off switch in the TATA box is a function of the movement of the hydrogen ion between a thymine oxygen and an adenine nitrogen in the TATA box.
DNA transcription is activated when the TATA box is contacted and straddled by the TBP to form a TBP/TATA box complex. Reference no. 6. When the TBP straddles the TATA box, it bends the TATA box at an angle of 100° along the DNA axis. Reference no. 7. The TBP-induced bend initially breaks the oxygen-based hydrogen bond between the first of the complimentary adenine-thymine pairs in the TATA box, and in so doing creates within that thymine nucleoside a second oxygen double bond (prior to the bending, only one oxygen double bond existed in the thymine nucleoside). When the TATA box is bent by the TBP, these two oxygen double bonds are moved into close proximity to one another. If energy impacts these two momentarily associated oxygen double bonds, an energy process which attacks a nearby carbon-carbon double bond, a covalent-bonded ozonide is produced. Reference no. 2.
The ozonide thus consists of the nucleoside's three oxygens and the two carbons from the thymine nucleoside's 5-6 double bond. The ozonide eliminates the possibility of hydrogen bond formation with the thymine oxygen atom (which is now bound within the ozonide) to turn the system “off.” The ozonide in the regulatory replication-initiation TATA sequence of the DNA oncogene thus locks the TATA system in the “on” (transcription/replication) state, forming the basis for the malignancy. It is to be noted that the Law of Bergonie and Tribondeau, published in 1906, states that a tissue is more radiation-sensitive (and can become cancerous) the more undifferentiated its cells are morphologically and physiologically, the more active they are mitotically, and the longer they remain in an active state of proliferation (the more divisions they undergo between the youngest precursor cell and the mature functional cell). The bending of the TATA box during such active proliferation momentarily provides open windows for energy absorption and lesion production in the momentarily associated oxygen double bonds within the TATA box. Reference no. 4. This is the primary mechanism responsible for the genesis of cancer, and the ozonide is thus the primary lesion responsible for carcinogenesis. All mutations in the genome resulting from this lesion and from other sources are considered secondary effects in the cancer process. However, many of these mutations are essential to the evolution of an operational and autonomous cancer cell.
The ozonide is highly diamagnetic due to the coupling and pairing of all of its electrons (diamagnetism is exhibited by elements possessing an even number of electrons and no incomplete inner shells). All effective ozonide orbitals are filled continuously by paired pi and lone electrons from structures surrounding the lesion and correspond to the electron configuration of krypton (this is the Sidgwick effective atomic number process). Reference no. 8.
The ozonide has known physicochemical autoxidation properties, which enable the ozonide to self-replicate. When the ozonide is produced in one thymine nucleoside during the DNA replication process, it immediately can replicate itself, by autoxidation, in an associated thymine nucleoside. Thus, the structure of the TATA box permits replication of the ozonide from the thymine in the DNA mother strand to the thymine in the adjacent daughter strand, thereby permitting, during normal strand separation, during replication, the transfer of the ozonide lesion from one cell to another.
The present invention is based on compounds that are designed to address and dissociate the covalent bonds of the ozonide lesion in the TATA box of the oncogene. Each of the compounds contains a constituent that orients the compound toward, and transports it to, the TATA lesion in the DNA. Each compound also has constituents that dissociate the ozonide's bonds, and hydrogenate the nucleotide-linking oxygen in the thymine nucleoside. The constituents of the compounds have been highly selected, and the compounds designed specifically, to reconvert the carcinogenic chemical structure of the thymine nucleoside to that found in normal DNA. The preferred compounds applicable for this purpose include the p
Dorsey & Whitney LLP
Raymond Richard L.
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