Chemical apparatus and process disinfecting – deodorizing – preser – Chemical reactor – With means applying electromagnetic wave energy or...
Reexamination Certificate
1999-06-23
2001-04-24
Mayekar, Kishor (Department: 1741)
Chemical apparatus and process disinfecting, deodorizing, preser
Chemical reactor
With means applying electromagnetic wave energy or...
C422S186040, C422S907000
Reexamination Certificate
active
06221319
ABSTRACT:
BACKGROUND OF THE INVENTION
Modern drug discovery has been revolutionized by the development of high-throughput screening techniques. The ability to clone receptors, combined with modern automation techniques, means that now thousands of compounds can be screened for receptor binding and, by extension, pharmaceutical activity, in the time previously required to screen only a few. Hodgson, 10
Biotech
. 973 (1992). Because of this screening capacity, new compound generation is now often the rate-limiting step in drug discovery. Dewitt, 1
Pharm. News
11 (1994). In addition, the statistics of this screening approach to drug discovery requires the testing of many thousands of compounds in order to discover one highly active new compound. The traditional sources of compounds for screening, such as natural products or the products of rational drug design, cannot furnish the numbers of compounds needed to meet this demand, while combinatorial synthesis produces large numbers of compounds but they have insufficient diversity of structures. The present invention is directed at the development of a new method to synthesize and screen large numbers of structurally diverse compounds.
There are two principal ways in which candidate compounds are currently provided for drug screening: isolation from natural products, and chemical synthesis. Natural products, such as plant extracts, provide a great amount of structural diversity. However, this approach typically requires laborious sample collection and preparation, followed by difficulties in identification, isolation, and production of compounds determined to be active via screening. Consequently, this approach is typically too slow to meet the capacity offered by high-throughput screening. Traditional chemical synthesis is also slow, and new technologies—primarily combinatorial approaches to stepwise synthesis—are being developed to rapidly generate collections of molecules for drug discovery. Dewitt, Ibid. Such combinatorial approaches can provide sufficient quantities of compounds quickly enough for high-throughput screening, but the structural diversity is restricted due to the limited number of starting materials and synthetic reactions for combining starting materials.
Plasma glow discharges have been used to prepare specific compounds from vaporized organic reactants. See, for example, Cvetanovic, 1
Adv. Photochem
. 115 (1963) wherein the production of an aldhyde, two epoxides and two ketones from a mixture of 2-pentene and oxygen was reported. See also, Suhr, 11
Angew. Chem. Int. Ed. Engl
. 781 (1972), which discloses the limited production of several cyclic compounds from acetylene; however, unless the reaction is rapidly quenched, the primary products are polymers. Ibid. The primary focus of prior attempts to synthesize new products by exposure of one or more reactants to a glow discharge has been to maximize conversion and yield of a single desired product which, due to the inherent difficulty in controlling plasma discharge reactions, has been largely unsuccessful. The present invention is based upon the recognition that such inherent uncontrollability can be used to advantage in preparing a multitude of organic compounds containing diverse chemical structures and functional groups, and that the resultant product mix, when coupled with bioactivity screening, can ultimately lead to the production of significant numbers of useful compounds.
SUMMARY OF THE INVENTION
The present invention comprises a novel process for synthesizing and identifying compounds with desirable bioactivity. Such compounds are useful in many areas of science and industry, such as the areas of drug discovery, toxicity testing, development of animal and plant growth hormones, and pesticide and herbicide development. The present invention utilizes a new, fast, low-cost method for the generation of mixtures of large numbers of unique compounds in the laboratory: plasma synthesis. As with natural sources of extracts, plasma synthesis promises to provide compounds with an extremely wide variety of structures for testing, but does not require laborious biological-sample collection and preparation. Sample generation may be conducted in the laboratory using small scale apparatus and a wide range of commonly available starting materials. Production of larger samples of promising bioactive materials will therefore be greatly simplified. Because of the high-energy synthesis procedures used, highly diverse structures can be generated from simple starting materials, yet reaction conditions can be adjusted such that the number of products, their molecular weights, and their chemical properties can be controlled. In addition, the number of unique compounds that can be generated using low-cost apparatus rivals that of the best combinatorial techniques.
The process envisioned for synthesis of compound mixtures is not strictly limited to plasma synthesis, but encompasses the interaction of a starting material with any high-energy source that can induce reaction of the starting material to produce a diverse set of products.
For example, a plasma itself is a complex environment. Starting materials exposed to a plasma can interact with ionizing radiation (e.g., radiation of sufficient energy to induce ionization of molecules such as ultraviolet (UV) or higher energy light), non-ionizing radiation (e.g., lower energy radiation that generally does not induce ionization such as near UV or visible light) and electric fields (e.g., those from radio frequency, audio frequency, alternating current or direct current), all of which may be present in the plasma. Any and all of these can impart sufficient energy to the starting materials to induce reactions to form new compounds that are different from the starting material.
The process comprises two main steps: (1) the production of organic compound mixtures of unlimited number and diversity by plasma chemical synthesis; and (2) subjecting these compound mixtures to screening tests for a desired biological activity. Once a particular mixture tests positive for desirable activity, the mixture is separated into its individual components by common chemical separation techniques, such as chromatography or extraction, and each component is then retested to determine which ones have activity.
REFERENCES:
patent: 1754186 (1930-04-01), Becker
patent: 2728723 (1955-12-01), Akerlof
patent: 3305466 (1967-02-01), McCoy
patent: 4097384 (1978-06-01), Coleman et al.
patent: 5433832 (1995-07-01), Rich et al.
Babcock Walter C.
Friesen Dwayne T.
Johnson Bruce M.
West James B.
Bend Research Inc.
Chernoff Vilhauer McClung & Stenzel LLP
Mayekar Kishor
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