JP2000026287A - Suppressant for molecular expression function - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject suppressant capable of suppressing or inhibiting functions expressed by a multidimensional structure of a reactional substrate by including a specific 6-membered ring compound containing carbonyl group as an active ingredient. SOLUTION: This suppressant is obtained by including a compound represented by formula I [R1 to R6 are each H, a halogen, a 1-6C alkyl, amidino, a 3-8C cycloalkyl, an aryl or the like; A is H or a group represented by formula II (R7 is a 1-6C alkyl, sulfide or the like; R8 and R9 are each H, allyl or the like)] (e.g. 4-isopropyl-2-cyclohexen-1-one) as an active ingredient. When using the compound as a medicine, the compound can be mixed with a pharmaceutically required ingredient such as a carrier, an excipient or a diluent, prepared as a pharmaceutical composition in a dosage form such as a powder, a granule, a tablet, a capsule or a parenteral injection and administered. The active ingredient is preferably included in an amount of 0.1-80 wt.% in the case of the powder, granule, tablet and capsule and usually preferably 0.01-20 wt.% in the case of the parenteral injection.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

[0001] The present invention relates to a substrate (lipid, carbohydrate, amino acid, etc.) having a molecular weight of 10,000 or less which basically constitutes the structure and function of an organism, and a peptide or a biologically synthesized peptide from the substrate. Shows inhibitory or inhibitory effects on functions expressed in macromolecules such as proteins, enzymes, nucleic acids, and genes (DNA, tRNA, mRNA, rRNA), and has antibacterial, antifungal, antiviral, and disinfectant (food Preservatives, germination or maturation inhibitors for fruits and vegetables, antibacterial agents associated with molding of plastics, antibacterial paints, interior resin waxes, antibacterial and antifungal agents for household appliances, daily necessities, household goods, paper, pulp, etc. Slime inhibitors, cleaning agents in the electronics field, antibacterial and antifungal agents against metalworking oils, antibacterial and antifungal agents against waste treatment, etc.), anticancer , Spermicides or topical contraceptives, blood coagulation / fibrinolysis inhibitors or inhibitors, inhibitors of the function of physiologically active substances (enzymes, peptides, genes, etc.) or function repairing agents or inhibitors, or antigen-antibody reaction inhibitors or Inhibitors, organ tissue preservatives, thrombolytics, sugar chain coordination agents,
Arteriosclerosis inhibitor, metabolic (lipid, sugar) improver, wound healing,
The present invention relates to an epithelialization promoter (including a hair-growth effect). Non-biological molecules (phospholipids, glyceryl groups, sulfhydryl groups, thiol ester groups, monosaccharides and disaccharides and polysaccharides,
Silicone, vinyl base, cellulose, etc.), free radical scavengers, desulfide agents or antioxidants (antioxidants). Further, a depolymerizing agent, a surfactant improving agent, and a phase transfer agent for non-biological low molecular weight and high molecular weight substances based on the organic chemical and molecular orbital properties of the molecular expression function inhibitor described in the present invention. Or a phase change improver, a plasticizer or a plasticity improver, a fiber softener or a fiber softness improver, a pressure-sensitive adhesive or a tackifier, an adhesive or an adhesion improver, a paint or a paint improver, Moldability improver, copolymerizer, polymerization regulator, stabilizer,
Antioxidant, filling improver, lubricity improver, UV absorber or UV absorbability improver, impact resistance improver, light stability improver, release improver, nucleating agent improver, abrasion improver Agent, anti-aging agent, physical property function improver, function or performance improver, flow property improver, water absorption / water resistance improver, rigidity / hardness softness improver, amorphous agent or amorphous improver, softener or softener Improver further physical property or function improver of polymer composite material,
Physical property or function improver of functional polymer composite material, dye,
The present invention relates to a modulator or improver for a fluorescence wavelength or an excitation wavelength of a paint, a pigment, or a colorant, a photodecomposer or a photodegradability improver.

[0002]

2. Description of the Related Art Conventionally, basic principles of organic structural chemistry, that is, bond angle and bond distance, group size and shape, hydrogen bond, resonance, acidity and basicity, optical activity, and configuration have been known in the reactor. It is well known that the preface is important (Morrison, Boyd, Organic Chemistry, Chapter 6).
Edition, Tokyo Chemical Doujin Publishing (Reference 1)). On the other hand, biological components such as substrates (lipids, carbohydrates, amino acids, etc.) that basically constitute the structure and function of an organism, and peptides, proteins, enzymes, nucleic acids, and genes (DNA, tRNA) that are biologically synthesized from the substrates , MRNA, rRNA), etc., as well as the multi-dimensional structure (conformation) of cell membranes, intracellular organelles, and extracellular and extracellular matrices, which are the basic components of biological components It is well known that multidimensional structure is important for the expression of physiological functions, recognition of substances, and reception of substances (Alberts, Bray, Lewis, Raff, Roberts and Watso
n, The Molecular Biology of the CELL, Garland P
ublishing Inc., 3rd edition <Reference 2>). It is also known that a methyl group contributes to the creation of fluidity and hydrophobicity of non-living substances containing lipids and proteins. Is also composed of a hydrophobic component outside the membrane and plays an important role in receiving signals from outside the cell to the inside.
The extremely thin film-like membrane composed of lipids and protein molecules binds cells and surrounds organelles inside the cell.The protein embedded in the membrane is the cell and its surroundings, or cells. It has high activity as a mediator between the interior of organelles and the cytoplasm. In addition, it is known that there are various types of intracellular substrates, such as various enzymes involved in intracellular signal transduction and various enzymes involved in intracellular respiration, depending on cell types. In addition, the existence of tubulin and the like involved in cell shape maintenance, division, and proliferation is also known. Plasma membrane proteins are also involved in intercellular recognition. In addition, hydroxyl group, sulfhydryl group (-SH), and disulfide bond form an ester to change a physiological function expressed by a multidimensional structure of a substance by a cross-linking reaction, and the amino nitrogen exhibits not only basicity but also nucleophilicity. When a peptide or protein is denatured, the coil state of the peptide or protein can be unraveled, and the multidimensional structure peculiar to each peptide or protein is broken. At the same time, the biological activity specific to the peptide or protein is lost. The same applies to complexes (for example, nucleic acids) of phospholipids and glycoproteins as well as peptides and proteins. Furthermore, in order to ensure the specificity of these membrane structures, the enzymes present in the cells, the cytoskeleton, the substrates synthesized in the cells, and the physiological functions of the substances secreted outside the cells, the organisms must be It is well known that two-dimensional and three-dimensional structures (helical structures) are important for the constituent materials. It is known that the charge distribution of a molecule and the state of molecular charge density of a substance which expresses a function by these multidimensional structures differ not only in a biological species difference and a normal state but also in a pathological state <Reference 2>
>. Viruses, which are organisms without cell membranes, are also composed of peptide chains, proteins, etc., formed by linking a large number of inanimate amino acids, and form two-dimensional and three-dimensional multidimensional structures. Among the multidimensional structures, the helix structure has 3.6 amino acid residues per helix rotation,
The 3.6-helix creates a space that can be occupied by side chains, and all possible hydrogen bonds can form. Also the α domain,
It is also an important known fact that the concept of the β domain, α / β domain, exon, and intron is expressed by a multidimensional structure. In the homologous protein, the core in the structure is conserved, but the helical loop region is changed. Also, what kind of conformation depends on the number of amino acids contained in the helix loop and the type of secondary structure to which the loop is connected, that is, α-α, β-β, α, rather than depending on the amino acid sequence It is also known that it often depends on which of -β and β-α is used. It is also known that the multidimensional structure of biological materials such as helical loops causes changes in the cytoskeleton and mitotic proliferation due to the three-dimensional structure associated with changes in intracellular energy such as tubulin and spectrin during cell division. ,
Attention has also been focused on the mechanism of cell spontaneous death (eg, apoptosis) of neurons and the like that emerges due to the mechanism of canceration and anti-cancer of cells as well as the mechanism of anti-proliferation and aging. The development of beneficial drugs has been awaited. Despite the effects of conventional antibacterial agents and anticancer agents, etc., result in cell death, the form of death causes necrosis due to degeneration, coagulation, etc., which must be solved including the emergence of mutants and resistant species. Yes, and that's why there is interest in apoptosis. In addition, organisms can move automatically, and flagella, pili and sperm are equipped with fine motors. It is also known that this biological motor also depends on a change in energy generated by hydrolysis of adenosine triphosphate, etc., in a multidimensional structure generally possessed by a biological substance such as a helix loop such as myosin. These multidimensional structures are important for the mechanism of expression of physiological functions based on recognition of the two-dimensional and three-dimensional structures of each substance, which applies to various genes and antibodies, based on recent molecular biology knowledge. <Reference 2> is also a known scientific fact. However, the substances constituting the living body are not always present at the same position, but are always in a dynamic state (for example, in the case of a membrane protein, about 10 times less than that of
(0 times slower). Furthermore, the more active the movement of lipid molecules, the greater the fluidity of the membrane.However, the ease of movement varies depending on the type of lipid, and in vivo, the ability to automatically regulate membrane fluidity is included. It is also known as a cause of disease development in humans due to impaired regulatory ability, and a countermeasure is awaited. Furthermore, the stability of the bilayer lipid bilayer, known as a fluidity model, is largely due to the hydrophobic interaction between hydrophobic groups, and most of the amino acid hydrophobic side chains are buried inside the protein. Thus, the higher-order structure of a protein that is not in contact with water is maintained by hydrogen bonding, hydrophobic interaction, and van der Waals forces, and it is well known that a flexible structure is formed. That is, it is considered that a solute having a higher hydrophobicity is more likely to bind to a protein, and the conformation of the protein is changed because the hydrophobic molecule penetrates into a hydrophobic region near the protein surface. In this way, capturing life activity in a dynamic and multidimensional manner is important for understanding life phenomena. Not to mention the scientific interest in controlling the quality of life activity, Historically, it has been eager to propose a method for preventing or preventing obstacles (disease, disease, etc.) in performing normal life activities of living organisms, especially humans, based on such a logical configuration.

[0003] Not to mention the history of human beings and diseases, the battle against pathogenic microorganisms such as bacteria and viruses
Despite being vigorously done even now,
Although it is a serious problem that needs to be solved medically, human death due to multiple organ failure with sepsis and generalized intravascular coagulation is a serious problem despite the development of advanced medicine. (Koyama, hypotension-pathophysiology for clinicians-Fujita Publishing Project <Reference 3>. Pathogenic microorganisms and viruses such as Staphylococcus aureus, streptococci, Escherichia coli, acid-fast bacteria, and fungi are always living spaces of humans. It is widely known as a causative organism of various infectious diseases.The prevention of pathogenic microorganisms and viral infections is not only controlled by the hygiene of the human living space, but also by human life. Many drugs have been developed and applied to prevent and treat infectious diseases with disinfectants and bactericides in space and around living activities, but many results have been achieved. In the development of substances, the application of drugs has been accompanied by the emergence of resistant bacteria, which has raised social as well as medical problems, such as methicillin-resistant Staphylococcus aureus (hereinafter abbreviated as <MRSA>). The emergence of a variety of drug-resistant bacteria, which is representative of MRSA, because S. aureus is resistant to many β-lactam drugs.
Treatment of infectious diseases is difficult, and opportunistic infections
It becomes a causative bacterium for postoperative infection and the like, and the infected patients become more serious and easily fall into sepsis or multiple organ failure, which is a very serious problem in many hospitals. This Pseudomonas aeruginosa countermeasure is a major problem because of its relationship with Pseudomonas aeruginosa infection and cystic pulmonary fibrosis, which are difficult to prevent secondary burn infection. Helicobacter pylori
Has recently received much attention as a causative or aggressive factor for peptic ulcers. In addition, acid-fast bacilli and fungi are currently becoming an international problem in human immunodeficiency syndrome (AID).
It is also a problem as a fatal complication of S).
Therefore, development of a drug that exhibits antibacterial action against MRSA and mycobacteria, an Escherichia coli infection that easily causes sepsis, a refractory mycosis, and a drug that is effective against a viral infection are extremely important international issues.

[0004] Recently, opportunistic infections not only in hospitals but also in human living spaces (for example, veterans' disease due to air-conditioning contamination) and living activities have become a problem. Disinfectants are being re-recognized. With the emergence of an aging society close at hand, urgent technological development is expected for measures such as medical care for the elderly. In general, Staphylococcus aureus, mycobacteria, fungi, and viruses are more likely to encounter infection via the respiratory and digestive tracts, such as through the nasal cavity and pharynx. Conventional disinfectants often rely on physical methods around the human living space and living behavior, and methods of administering antibiotics and other drugs to humans are oral, intravenous, and It may be limited to direct administration, and there is anxiety and inconvenience not only for patients but also for healthcare professionals, nursing assistants, and relatives who are the center of home care.
However, people continue to come into contact with the outside atmosphere through the skin and the respiratory tract (alveoli) during their lives, and there is a hope for a method of administration that uses the atmosphere, which is the living space of human beings.

In general, bacteria acquire resistance through various genetic phenomena such as mutation and selection, transduction, and plasmid self-transfer. Therefore, it is impossible to completely prevent them by using a single synthetic chemical agent. It is said that there is currently no chemotherapeutic agent that does not allow the emergence of resistant bacteria.However, conventionally, antibacterial effects have to be sought by inhibiting the primary structure of substances constituting bacteria such as bacterial membranes. Many drugs for the purpose have been used. Therefore, it is important to devise a method of administering an antibacterial agent and to develop an antibacterial agent and an antiviral agent based on a multidimensional structure of various structures constituting bacteria. In addition, on a global scale, the population is increasing remarkably, especially in underdeveloped countries, and its deterrence measures are important from the viewpoint of future food conservation and nature conservation. However,
Contraceptive surgery for both genders, ovulation control using hormones for women, and the spread of physical contraception methods such as condoms and pessaries have been proposed and promoted internationally. In order to reduce fertility without damaging the genetic information possessed, a contraceptive method capable of inhibiting sperm motility is also expected.
On the other hand, despite the scientific knowledge that it is important for the expression of various functions of organisms expressed by the multidimensional structure of substances in biology described above, the functions expressed by the multidimensional structure of substances are represented by simple chemical structural formulas There is no example of a substance that can suppress and inhibit physiological functions and is safe and has little harm to the survival of life as a unified body. Its effective effects are urgently expected not only in interdisciplinary aspects such as biology, chemistry, and medicine, but also in practical medicine that saves lives.

[0006] Analyzing and understanding the physical properties of low-molecular substances and high-molecular substances, making use of their physical properties and the functional properties they produce, and producing and improving each of them, a number of things necessary for the current human society are realized. Although daily necessities and industrial materials and environmental materials have been provided, the functionality, efficiency, comfort, safety, etc. are improved by further improving the physical properties of low-molecular substances and high-molecular substances. There is a long-awaited need for methods and specific examples that can be used. For example, an outline is given of surface activity, a polymer substance, and the like, which are one of the physical properties of a polymer substance.

That is, the degree of surface activity is related to the critical micelle formation concentration, solubilization, Krafft point, and the like. It is known that the value of the micelle formation concentration is also large. Due to the structural characteristics of the surfactant molecules, the effects such as foaming, wetting, lowering of surface tension, emulsification (formation of emulsion), solubilization, formation of micelles, and detergency can be made effective. Furthermore, from this characteristic, when a substance that is insoluble in water and has a strong hydrophilic group and the intermolecular force between molecules spreads widely on the water surface smaller than the intermolecular force between the molecule and the water molecule, it forms a one-molecule layer film. It is also known to form a so-called monomolecular film arranged on the water surface. If this monomolecular film can be transferred to a solid surface as it is, a hydrophobic surface can be obtained. Therefore, it is expected that a surface activity improving agent is proposed for producing a thin film such as an LB film. Furthermore, surfactants have bactericidal and hard water-resistant properties, and by utilizing this effect, they are added to cosmetics such as cleansing creams, shampoos, rinses, etc. Agents, aerosol foaming agents, dyeing assistants, etc. are widely used, and proposals for surface activity improvers are expected in a wide range. Polyethylene is also an example of a number of polymeric substances. Polyethylene is a crystalline thermoplastic, conceptual structures -CH ₂ CH ₂ -, but are repeated in, branching occurs depending process, this degree of crystallinity decreased with the rigidity decreases and transparent This leads to an increase in performance. Further, during polymerization, short-chain branching (ethyl branch or butyl branch) is generated by hydrogen abstraction reaction in the molecule due to backbiting, resulting in low density, or branching (long chain) comparable to the main chain due to hydrogen abstraction reaction between molecules. Branches), linear low density polyethylene (LLD polyethylene) has impact strength, medium density polyethylene (MD polyethylene) and ultra low density polyethylene (VLD polyethylene) are used as resin modifiers, Ultra high molecular weight polyethylene (UHMW polyethylene) has excellent impact resistance, abrasion resistance, and self-lubricating properties, and is widely applied. However, it is expected that a proposal for an improver of each material property will improve the quality. Have been. Polymers among the high molecular substances have characteristics of each substance, and for example, an ethylene / vinyl acetate copolymer is excellent in elasticity, transparency, toughness, and heat sealability. Among methacrylic resins and acrylonitrile-based resins, methacrylic acid ester-based polymers are collectively referred to as methacrylic resins. Widely used for household goods. Furthermore, the physical properties of the polymer include film forming performance, rubber properties, mechanical toughness, creep resistance, flexibility, thermoplasticity, heat resistance,
Utilizes features such as dimensional stability, phase change, impact resistance, fluidity, surface gloss, water resistance, chemical resistance, and the physical properties of polymers include processability, printing, painting, vapor deposition, and lamination. Secondary workability, covering properties, water repellency, release properties, defoaming properties, etc.
Antioxidant properties, thickening properties, high temperature curing properties, room temperature gelling properties, heat deformability, heat resistance, alkali resistance, bending strength, flexural modulus, tensile strength, electrical properties, adhesion, corrosion resistance, heat resistant sliding There are also dynamic characteristics, radiation resistance, polyvalent metal ion trapping ability (chelating ability), dispersibility, aggregating ability, etc. By using the combination of these properties, it is indispensable in our current social civilization life. There is a need to provide more effective materials by improving their physical properties. Polyethylene glycol is an example of a polymer commonly used on a daily basis. Polyethylene glycol is used in a wide variety of applications, such as cream lotions in the cosmetics industry, lubricants in the textile industry and metalworking industries, binders for tablets in the pharmaceutical industry, and raw materials for surfactants. It is also used as an agent, a resin modifier (hydrophilization), a thickener, a binder such as ceramics, an inorganic coagulant such as clay, etc., and further improves the properties of polyethylene glycol safely and efficiently. Is required. Highly polymerized sodium polyacrylate is also approved as a food additive and cosmetic material, and it is necessary to further improve and improve the physical properties derived from the multidimensional structure of each of these versatile polyacrylamide polymers. Proposals for methods and substances that can do this are expected.

[0008] Characteristic expression of fibers such as cellulose-based natural fibers, hydrocarbon-based synthetic fibers, polyvinyl alcohol-based synthetic fibers, acrylic-based synthetic fibers, polyamide-based synthetic fibers, aramid fibers, polyester-based synthetic fibers, polyurethane-based fibers and carbon fibers. In addition to the molecular structure, multi-dimensional structural characteristics based on the molecular structure bring out their respective characteristics.Natural and synthetic rubber latex that show rubber-like elasticity at the operating temperature also have multi-dimensional structural characteristics based on the molecular structure. Each rubber characteristic changes, collagen also forms a left-handed helix, and the right-handed three-helix structure has a different functional role depending on the multidimensional structure. By improving these multidimensional structures, it is expected that the expression of functions and the use thereof will be further improved according to the purpose.

[0009] Examples of the use of polymers include paints, powder paints, radiation-curable paints, and the like, which utilize film-forming properties, such as pigment dispersants for water-based paints, scale inhibitors, conductive treatment agents, and emulsion polymerization stabilizers. Paints other than solution-type paints such as dispersion paints are also used for home appliances, automobiles, building materials, furniture, electric wire insulation coatings, etc., and methods and substances that can improve the physical properties of these paints are used. Suggestions are expected.

[0010] Also, in order to expand the use of polymers, appropriate adhesives are also required. Improving the functions of these adhesives is required in various fields (eg, Medicine, transportation, communications, construction, etc.).

In addition, with recent technological development, various special functions (optical transmission, magnetism, recording medium for electronic equipment, separation film, electrical conductivity, transparent and electrical conductivity, electrical conductivity by light irradiation, vibration suppression, Polymer composite materials that exhibit sound insulation and thermal conductivity have been used. Polymer composite materials that exhibit this special function include modules for separation, metallized resins, vibration damping, shock absorbing materials, conductive materials, Optical fibers, magnetic recording media, optical recording media, write-once and rewritable optical disks, etc.
In order to improve the functional performance, not only the structure of the material but also a technique and a method capable of freely controlling the function are desired.

Further, a functional polymer, which is a polymer material that undergoes a chemical or physical change by itself due to a chemical or physical stimulus from the outside, or a polymer material whose state changes by interaction with a partner substance The function of a material is expressed by the action of a functional group with a specific function introduced into the main chain or side chain of a polymer or polymer precursor, the inherent properties of an additive, a specific shape, etc. is there. For example, electrical materials, semiconductor-related materials, photosensitive polymer materials,
Recording materials, liquid crystal display materials and elements Polymer liquid crystals, optoelectronic materials, thin film materials, photochromic materials, optical recording materials, optical elements, holographic recording, non-linear optical elements, photoresponsive functional materials, sensors or transducer related materials, etc. is there. Improvements and improvements in the functions of these functional polymer materials are expected to improve the expression efficiency, expression accuracy, and stabilization of each functional property. Furthermore, the transparency, mechanical strength, heat resistance, etc. required for the optical disk substrate material are improved, and the multi-dimensional structure of thin film materials, such as amorphous films, in which the structure of the polymer film is three-dimensionally cross-linked. It is also expected that the functional properties will be improved. In addition, as an example of the use of polymers, there is a method that incorporates a photochemical reaction to utilize structural changes such as cross-linking, polymerization, polarity change, collapse, and depolymerization caused by light. In addition to the improvement of the structure of the polymer material, a method and a technique for improving the physical properties exhibited by the three-dimensional structure are also expected.

Further, some polymers are used as polymers for foods, cosmetics, detergents, etc., and the properties and functions of the respective polymers are improved in order to improve the quality and properties of these polymers. There is a strong demand for improving the three-dimensional structure that expresses the compound and making it a substance having more useful physical properties in order to improve the quality of life and the environment. Also, the properties of polymers are used as medical auxiliaries, and the development of useful bioadaptive materials by further improving and improving the properties of bioadaptive materials using such polymers is expected. More light,
Stabilizers that maintain stability against heat, etc., antioxidants (or anti-aging agents) that prevent the progress of oxidation and ozonolysis, plasticizers and softeners that improve plasticity and processability, and difficulties in imparting flame retardancy Flame retardant, cross-linking agent, filler, fiber treatment agent, oil agent, antistatic agent, softening agent, polymer finishing agent, plastic additive, ultraviolet absorber, light stabilizer,
Lubricants, vulcanizing agents, antioxidants, softeners, tackifiers and reinforcing agents, fillers, adhesive additives, paint additives, pigments, solvents, curing agents and curing accelerators, deterioration inhibitors, dispersants Are used as additives for polymer materials according to their purposes. By improving the properties of additives used in these polymer materials, the inherent functions of low-molecular and high-molecular materials It is expected to produce more useful functional characteristics while controlling, suppressing, and inhibiting the effect.

There are many types of polymers such as polymers for foods, cosmetics, detergents, etc. Among them, polymers for foods include polysaccharides, food proteins, polymers for gums and the like. It is typical. In addition, the polymer for gum is a natural resin containing natural additives such as tickle, solver, gelton, etc. as polymer materials used in chewing gum, and vinyl acetate resin and polyisobutylene as food additives. , Polybutene, butyl rubber, styrene-butadiene rubber (SBR), polyethylene, terpene resin and the like. Animal products for detergents and cosmetics
Vegetable and even synthetic polymers are used. For the purpose of improving the quality and properties of these polymers, improving the three-dimensional structure that expresses the physical properties and functions of each and making it a substance with more useful physical properties will improve the quality of life and the environment. It is strongly required to measure. Furthermore, the properties of polymers are used as medical aids, and one example is a dialysis membrane. As the material of the dialysis membrane, natural polymers (cellulose, cellulose acetate) and synthetic polymers (polymethyl methacrylate, polyacrylonitrile, polysulfone, ethylene / vinyl alcohol copolymer, etc.) are widely used. The development of useful bioadaptive materials by further improving and improving the characteristics of bioadaptive materials using polymers is also expected. Stabilizers to maintain stability against light, heat, etc., antioxidants (or anti-aging agents) to prevent oxidation and ozonolysis, plasticizers and softeners to improve plasticity and processability, and flame retardancy Flame retardants, other cross-linking agents (or vulcanizing agents), fillers, fiber treatment agents, oil agents (oil agents include spinning oil agents and spinning oil agents), antistatic agents (compounds containing polyethylene glycol chains and surfactants) Agents, softeners, polymeric finishes, additives for plastics, UV absorbers / light stabilizers, lubricants, vulcanizing agents,
Anti-aging agents, softeners (softeners act as lubricants between rubber molecules, help dispersibility of other additives and also increase the volume of compounding agents), tackifiers and reinforcements Agents (such as carbon black: often added to rubber products to improve physical properties such as hardness, tensile strength, modulus, rebound resilience, friction resistance, and tear resistance), fillers, and adhesives Agents, paint additives, pigments, solvents, curing agents and curing accelerators, anti-deterioration agents, dispersants, etc. are used as additives for polymer materials according to their purposes. It is desired to improve the properties of the additives used.

[0015]

On the basis of the above-mentioned biological facts, substances forming organisms, macromolecules, extracellular matrices, cell membranes, cytoskeletons, intracellular matrices, intracellular organelles, etc. or synthetic molecules Anti-fungal, anti-fungal, anti-viral agents by suppressing or blocking the functions expressed by the multidimensional structure of complex macromolecules (including enzymes, genes, antibodies, etc.) such as proteins, saccharides, lipids, etc. Disinfectants, anticancer agents, blood coagulation / fibrinolytic inhibitors or inhibitors, antigen-antibody reaction inhibitors or inhibitors, preservatives for organ tissues and preservatives such as food, germination or maturation inhibitors for fruits and vegetables, plastics Antibacterial agents, antibacterial paints, antibacterial resin waxes, antibacterial and antifungal agents for household appliances, daily necessities, household goods, slime inhibitors for paper, pulp, etc. Cleaning agents, antibacterial and antifungal agents against metalworking oils, antibacterial and antifungal agents against waste treatment, inhibitors or inhibitors of the function of bioactive substances (enzymes, peptides, genes, etc.), spermicides Agent or external contraceptive agent, thrombolytic agent, sugar chain coordinating agent, anti-atherosclerotic agent, metabolic (lipid, sugar, protein) improving agent, wound healing, epithelialization promoting agent, and multidimensional structure for biological constituent substrates There has been a demand for the development of regulators, inhibitors and inhibitors of the functions to be expressed.

[0016] An object of the present invention is to solve the above-mentioned problems, have a simple chemical structural formula, and suppress or inhibit a function expressed by a multidimensional structure of a reaction substrate. Is to provide.

[0017]

Means for Solving the Problems The inventors of the present invention have conducted intensive studies to achieve the above object, and as a result, the following general formulas (1a) and (1b), general formulas (2) and The inventors have found that a compound represented by the formula (3a) or (3b) or an acid addition salt thereof as an active ingredient achieves the above object, and completed the present invention.

In order to achieve the above object, the invention according to claims 1 to 4 is a molecular expression function inhibitor having a basic molecular structure represented by the general formula (1a) or (1b). An antibacterial agent, an antifungal agent, an antiviral agent, a disinfectant, a disinfectant, an anticancer agent, a blood coagulation / fibrinolytic system inhibitor or inhibitor, an antigen-antibody reaction inhibitor or inhibitor, an organ containing a compound, a derivative thereof or an acid addition salt thereof as an active ingredient Tissue preservatives, preservatives for foods and the like, germination or maturation inhibitors for fruits and vegetables, antibacterial agents associated with molding of plastics, antibacterial paints, antibacterial resin waxes, antibacterial and antibacterial agents for household appliances, daily necessities and household goods Fungicides, slime inhibitors for paper, pulp, etc., cleaning agents in the electronics field, antibacterial and antifungal agents against metalworking oils, antibacterial and antifungal agents against waste treatment,
Spermicide or contraceptive, thrombolytic agent, sugar chain coordination agent, anti-atherosclerotic agent, metabolic (lipid, sugar) improver, wound healing, promotion of epithelial formation to prevent sperm fertility Agents (including hair-growth effects), inhibitors and inhibitors of the function expression of bioactive substances (enzymes, peptides, genes, etc.) and the multidimensional structure (conformation) of the substances that make up the form and function of the organism It can suppress and inhibit the expressed function, and can control, suppress and inhibit the function expressed by multidimensional structure (conformation) of not only living organisms but also high molecular substances and high molecular composite materials. Provide available chemicals. Further, a halogen compound such as an alkali metal halide, an alkaline earth metal halide, or a zinc halide can be added to induce a reaction, and a colloidal gold or the like can be added to create a labeling substance. It can be used as a bleeding (diffusion) inhibitor for dyeing and printing dyes, as an ink stabilizer or a dye fixing agent, and by adding a coloring agent such as a dye, the color development of the dye can be enhanced. Agents can be added to create fragrance. Further, a depolymerizing agent, a surfactant or a surfactant improving agent, a phase transfer agent or a phase change improving agent, a micro phase separation structure improving agent, a plasticizer or a plasticity improving agent, a copolymerizing agent or a copolymerizing improving agent, a polymerization controlling agent Or a polymerization control improver, stabilizer or stabilization improver, antioxidant or antioxidant,
Amorphous or amorphous modifiers, rheological properties improvers, softeners or softening improvers, dyes, paints, pigments or colorants fluorescent or excitation wavelength modifiers or modifiers, low molecular weight substances It can also be used as a physical property or function improving agent, a physical property or function improving agent for a polymer substance, or a physical property improving agent for a polymer composite material or a functional polymer composite material.

A of the general formula 1

Embedded image

Formula (b)

Embedded image

Where (i) R1, R2, R3, R
4, R5, R6, R10 and R11 each independently represent a hydrogen atom; a halogen atom; a C1-C6 alkyl group; an amidino group; a C3-C8 cycloalkyl group; a C1-C6 alkoxy C1-C6 alkyl group; An aralkyl group in which one or more C1-C6 alkyl groups are bonded to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene rings; C1-C6 alkylene groups; benzoyl groups; cinnamyl groups; cinnamoyl groups; Group,

(Ii) A is a hydrogen atom or

Embedded image And

(Where R7 is a C1-C6 alkyl group;
A sulfide group; or a phosphate group, wherein R8 and R9 are each independently a hydrogen atom; a halogen atom; a linear or branched C1-C6 alkyl group; an aryl group; an allyl group; One or two or more C1s on the aromatic ring selected from
An aralkyl group having a C1 to C6 alkyl group bonded thereto;
An alkylene group, a benzoyl group, a cinnamyl group, a cinnamoyl group, or a furoyl group) (iii) R1, R
2, any of R3 and R4 and / or R5, R6R
Any of 10 and R11 may be a substituted or unsubstituted cyclopentyl group; a substituted or unsubstituted cyclohexyl group; or a substituted or unsubstituted naphthyl group;
R5, R6, R10 and R11 may combine with another condensed polycyclic hydrocarbon compound or a heterocyclic compound to form a ring, and (v) R3, R4, R5, R6, R10
And R11 represent a halogen atom, a cyano group, a carboxyl group which may be protected, a hydroxyl group which may be protected, an amino group which may be protected, C1-C6
Alkyl group, C1-C6 alkoxy group, C1-C7 alkoxycarbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl (Vi) may be substituted with one or more substituents selected from the group consisting of a C1-C6 alkylamino group and a di-C1-C6 alkylamino group;
R2 and R5 are a halogen atom, a C1-C6 alkyl group, an optionally protected carboxyl group, an optionally protected hydroxyl group, an optionally protected amino group, an optionally protected C1-C6 Alkylamino group, optionally protected C1-C6 aminoalkyl group, optionally protected C1-C6 alkylamino C
1-C6 alkyl group, optionally protected C1-C6
(Vii) R 3, R 4, R 5, R 6, which may be substituted with one or more substituents selected from the group consisting of hydroxyalkyl group and C 3 -C 6 cycloalkylamino group
When R10 and R11 are an alkyl group, the terminal of the alkyl group may be substituted by a C3-C8 cycloalkyl group.

The aryl group in (i), (ii) and (v) is
It may be a phenyl, tolyl, xylyl or naphthyl group, the substituted cyclopentyl group in (iii) may be a cyclopentylamino group or a cyclopentylcarbinol group, and the substituted cyclohexyl group may be a cyclohexylamino group, a cyclohexylaldehyde group or a cyclohexylacetic acid. May be a group, the substituted naphthyl group may be a naphthylamino group or a naphthylaminosulfonic acid group, and the condensed polycyclic hydrocarbon compound in (iv) is pentalene, indene, naphthalene, azulene, heptalene, biphenylene, Indacene, acenaphthylene, fluorene, phenalene, phenanthene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-
It may be cyclopentacyclooctene or benzocyclooctene, and the heterocyclic compound may be furan, thiophene, pyrrole, gamma-pyran, gamma-thiopyran, pyridine, thiazole, imidazolepyrimidine, indole or quinoline.

In order to achieve the above object, the invention according to claims 5 and 6 is a molecular expression function inhibitor having a basic molecular structure represented by the general formula (2), wherein the compound, its derivative or its derivative is Antibacterial agent, antifungal agent, antiviral agent, disinfectant, anticancer agent, blood coagulation / fibrinolytic system inhibitor or inhibitor, antigen-antibody reaction inhibitor or inhibitor, organ tissue preservative, food etc. Antiseptic preservatives, germination or maturation inhibitors for fruits and vegetables, antibacterial agents associated with molding of plastics, antibacterial paints, antibacterial resin waxes,
Bactericidal and antibacterial fungicides for household appliances, daily necessities and household goods, paper,
Anti-slime agent for pulp, cleaning agent in electronics field, antibacterial antibacterial and antifungal agent for metalworking oil,
Antibacterial and antifungal agents for waste treatment, spermicides or contraceptives for inhibiting fertility of sperm, thrombolytic agents, sugar chain coordination agents, arteriosclerosis inhibitors, metabolism (lipids, Sugars) improvers, wound healing, epithelialization promoters (including hair growth effects), inhibitors and inhibitors of the function expression of bioactive substances (enzymes, peptides, genes, etc.) and form and function of organisms The function expressed by the multidimensional structure (conformation) of the existing substance can be suppressed and inhibited, and it is expressed by the multidimensional structure (conformation) of not only living organisms but also high molecular substances and polymer composite materials. Provide a chemical substance capable of controlling, suppressing and inhibiting the function. Further, a halogen compound such as an alkali metal halide, an alkaline earth metal halide, or a zinc halide can be added to induce a reaction, and a colloidal gold or the like can be added to create a labeling substance. It can be used as a bleeding (diffusion) inhibitor for dyeing and printing dyes, as an ink stabilizer or a dye fixing agent, and by adding a coloring agent such as a dye, the color development of the dye can be enhanced. Agents can be added to create fragrance. Further, a depolymerizing agent, a surfactant or a surfactant improving agent, a phase transfer agent or a phase change improving agent, a micro phase separation structure improving agent, a plasticizer or a plasticity improving agent, a copolymerizing agent or a copolymerizing improving agent, a polymerization controlling agent Or a polymerization control improver, stabilizer or stabilization improver, antioxidant or antioxidant, amorphous or amorphous improver, flow property improver, softener or softener, pigment, paint, Modifier or improver of fluorescent or excitation wavelength of pigment or colorant, physical property or function improver of low molecular weight substance, physical property or function improver of high molecular weight substance, polymer composite material or functional polymer composite It can be used as a physical property improving agent for the material.

Formula 2

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Wherein (i) R1, R2, R3, R
4, R5 and R6 each independently represent a hydrogen atom; a halogen atom; a C1-C6 alkyl group; an amidino group;
Cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl having one or more C1-C6 alkyl groups bonded to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene rings. A benzoyl group; a cinnamyl group; a cinnamoyl group; or a furoyl group, and (ii) any of R1, R2, R3 and R4 and / or any of R5 and R6 is substituted or unsubstituted. A cyclopentyl group; a substituted or unsubstituted cyclohexyl group; or a substituted or unsubstituted naphthyl group, and (iii) R5 and R6 bind to another condensed polycyclic hydrocarbon compound or a heterocyclic compound to form a ring. (Iv) R3, R4, R5 and R6 may be a halogen atom, a cyano group, Carboxyl group, hydroxyl group which may be protected, amino group which may be protected, C1-C6 alkyl group, C1-C6
6 alkoxy groups, C1 to C7 alkoxycarbonyl groups,
Aryl group, C3-C6 cycloalkyl group, C1-C6
Acylamino group, C1-C6 acyloxy group, C2-C
6 alkenyl group, C1-C6 trihalogenoalkyl group,
It may be substituted by one or more substituents selected from the group consisting of a C1 to C6 alkylamino group and a diC1 to C6 alkylamino group, and (v) R2 and R5 are a halogen atom, a C1 to C6 alkyl group. An optionally protected carboxyl group, an optionally protected hydroxyl group, an optionally protected amino group, an optionally protected C1-C6 alkylamino group, an optionally protected C1-C6 One or more selected from the group consisting of an aminoalkyl group, an optionally protected C1-C6 alkylamino C1-C6 alkyl group, an optionally protected C1-C6 hydroxyalkyl group and a C3-C6 cycloalkylamino group May be substituted with (vi)
When R3, R4, R5 and R6 are an alkyl group, the terminal of the alkyl group may be substituted by a C3-C8 cycloalkyl group.

The aryl group in (i) and (iv) may be a phenyl, tolyl, xylyl or naphthyl group, and the substituted cyclopentyl group in (ii) may be a cyclopentylamino group or a cyclopentylcarbinol group. The substituted cyclohexyl group may be a cyclohexylamino group, a cyclohexylaldehyde group or a cyclohexylacetic acid group, the substituted naphthyl group may be a naphthylamino group or a naphthylaminosulfonic acid group,
The condensed polycyclic hydrocarbon compound in (iii) is pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-
It may be cyclopentacyclooctene or benzocyclooctene, and the heterocyclic compound may be furan, thiophene, pyrrole, gamma-pyran, gamma-thiopyran, pyridine, thiazole, imidazolepyrimidine, indole or quinoline.

[0029] In order to achieve the above object, claims 7 to 11 are provided.
The invention described in (1) is a molecular expression function inhibitor having a basic molecular structure represented by the general formula (3a) or (3b), wherein the compound, a derivative thereof or an acid addition salt thereof is used as an active ingredient. Antibacterial agent, antifungal agent, antiviral agent, disinfectant, anticancer agent, blood coagulation / fibrinolytic system inhibitor or inhibitor, antigen-antibody reaction inhibitor or inhibitor, organ tissue preservative, preservative preservative such as food, fruits and vegetables Germination inhibitor or maturation inhibitor,
Antibacterial agents, antibacterial paints, antibacterial resin waxes, antibacterial and antifungal agents for household appliances, daily necessities and household goods, slime inhibitors for paper and pulp, cleaning agents in the electronics field, metals Bactericidal antibacterial and fungicide for processing oil, antibacterial and fungicide for waste treatment, spermicide or contraceptive for inhibiting fertility of sperm, thrombolytic agent, sugar chain coordination modifier , Arteriosclerosis inhibitor, metabolic (lipid, sugar) improver, wound healing, epithelial formation promoter (including hair-growth effect), inhibitors and inhibitors of the function expression of bioactive substances (enzymes, peptides, genes, etc.) and It can suppress and inhibit the function expressed by the multidimensional structure (conformation) of the substance that constitutes the form and function of the organism. A function expressed by a multi-dimensional structure of postal such (conformation), control, providing a chemical capable of suppressing and inhibiting. Further, a halogen compound such as an alkali metal halide, an alkaline earth metal halide, or a zinc halide can be added to induce a reaction, and a colloidal gold or the like can be added to create a labeling substance. It can be used as a bleeding (diffusion) inhibitor for dyeing and printing dyes, as an ink stabilizer or a dye fixing agent, and by adding a coloring agent such as a dye, the color development of the dye can be enhanced. Agents can be added to create fragrance. Further, a depolymerizing agent, a surfactant or a surfactant improving agent, a phase transfer agent or a phase change improving agent, a micro phase separation structure improving agent, a plasticizer or a plasticity improving agent, a copolymerizing agent or a copolymerizing improving agent, a polymerization controlling agent Or a polymerization control improver, stabilizer or stabilization improver, antioxidant or antioxidant,
Amorphous or amorphous modifiers, rheological properties improvers, softeners or softening improvers, dyes, paints, pigments or colorants fluorescent or excitation wavelength modifiers or modifiers, low molecular weight substances It can also be used as a physical property or function improving agent, a physical property or function improving agent for a polymer substance, or a physical property improving agent for a polymer composite material or a functional polymer composite material.

In general formula 3, a

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B of the general formula 3

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Wherein (i) R3, R4, R5 and R6 each independently represent a hydrogen atom; a halogen atom;
C6 alkyl group; amidino group; C3-C8 cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; one or more aromatic rings selected from the group consisting of benzene, naphthalene and anthracene rings An aralkyl group to which a C1 to C6 alkyl group is bonded; a C1 to C6 alkylene group; a benzoyl group; a cinnamyl group; a cinnamoyl group;
Any of R3 and R4 and / or any of R5 and R6 may be a substituted or unsubstituted cyclopentyl group; a substituted or unsubstituted cyclohexyl group; or a substituted or unsubstituted naphthyl group; (iii) R5 and R6 are It may combine with other condensed polycyclic hydrocarbon compound or heterocyclic compound to form a ring, and (iv) R3, R4,
R5 and R6 each represent a halogen atom, a cyano group, an optionally protected carboxyl group, an optionally protected hydroxyl group, an optionally protected amino group,
6 alkyl groups, C1-C6 alkoxy groups, C1-C7 alkoxycarbonyl groups, aryl groups, C3-C6 cycloalkyl groups, C1-C6 acylamino groups, C1-C6 acyloxy groups, C2-C6 alkenyl groups, C1-C6 trihalogeno (V) may be substituted with one or more substituents selected from the group consisting of an alkyl group, a C1-C6 alkylamino group and a di-C1-C6 alkylamino group;
R5 is a halogen atom, a C1-C6 alkyl group, an optionally protected carboxyl group, an optionally protected hydroxyl group, an optionally protected amino group, an optionally protected C1-C6 alkylamino Groups, optionally protected C1-C6 aminoalkyl groups, optionally protected C1-C6 alkylamino C1-C6 alkyl groups, optionally protected C1-C6 hydroxyalkyl groups and C3-C6 cycloalkyl May be substituted with one or more substituents selected from the group consisting of amino groups, and (vi) when R3, R4, R5 and R6 are alkyl groups, the terminal of the alkyl group is C3-C8 cycloalkyl. It may be substituted by an alkyl group.

The aryl group in (i) and (iv) may be a phenyl, tolyl, xylyl or naphthyl group, and the substituted cyclopentyl group in (ii) may be a cyclopentylamino group or a cyclopentylcarbinol group. The substituted cyclohexyl group may be a cyclohexylamino group, a cyclohexylaldehyde group or a cyclohexylacetic acid group, the substituted naphthyl group may be a naphthylamino group or a naphthylaminosulfonic acid group,
The condensed polycyclic hydrocarbon compound in (iii) is pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-
It may be cyclopentacyclooctene or benzocyclooctene, and the heterocyclic compound may be furan, thiophene, pyrrole, gamma-pyran, gamma-thiopyran, pyridine, thiazole, imidazolepyrimidine, indole or quinoline.

[0034] The invention according to claims 12 to 20 provides a conformational change action, a thermodynamic action, a phase transition action, a softening action, a depolymerization action of the molecule expression function inhibitor according to claims 1 to 11, Antibacterial agents, anti-microbial agents, anti-microbial agents, utilizing polymer function improving effect, chemical reaction kinetic effect, reducing effect, free radical scavenging effect, desulfide effect, antioxidant effect, molecular orbital nucleophilic and electrophilic effects Fungicides, antiviral agents, disinfectants, anticancer agents, blood coagulation / fibrinolytic inhibitors or inhibitors, antigen-antibody reaction inhibitors, organ tissue preservatives, and preservatives.

According to the twenty-first aspect of the present invention,
A labeling reagent capable of detecting the site of expression of a molecular expression function by incorporating a substance serving as a label into at least one substituent, utilizing the action of the molecule expression function inhibitor described in 1 on a specific site; did. Claims 22, 23, 2
The invention according to Claim 4 utilizes a reducing action, a free radical scavenging action, and a desulfide action of the molecule expression function inhibitor according to any one of claims 1 to 11 to reduce and react with the free radical scavenging agent and the desulfide agent, respectively. did.

The inventions according to claims 25 to 46 provide a conformational change action, a thermodynamic action, a phase transition action, a softening action, a depolymerization action of the molecule expression function inhibitor according to claims 1 to 11, Depolymerizing agents utilizing polymer function improving effect, chemical reaction kinetic effect, reduction effect, free radical scavenging effect, desulfide effect, antioxidant effect, molecular orbital nucleophilic electrophilic effect and hydrophobic effect , Surface activity improver, spermicide or topical contraceptive, thrombolytic agent, sugar chain coordination change agent, arteriosclerosis inhibitor, metabolic (lipid, sugar, protein) improver, wound healing, epithelial formation promoter, phase Transfer agent or phase change improver, micro phase separation structure improver, plasticizer or plasticity improver, copolymerizer or copolymer improver, polymerization regulator or polymerization control improver, stabilizer or stabilization improver, oxidation Inhibitor or anti Agents, HiAkirazai or amorphous modifiers,
Flow property improver, softener or softener, dye,
Modulator or modifier of the fluorescence wavelength or excitation wavelength of paints, pigments, or colorants, physical property or function improver of low molecular substances, physical property or function improver of high molecular substances, polymer composite materials and high functional properties It was used as a physical property improver for molecular composite materials.

In the present specification, unless otherwise specified, a halogen atom means, for example, a fluorine atom, a chlorine atom, a bromine atom or an iodine atom;
For example, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tor
a C1-10 alkyl group such as t-butyl, benzyl, hexyl, or octyl; a lower alkyl group is, for example, a C1-5 alkyl group among the above-mentioned alkyl groups; an alkoxy group is, for example, A lower alkylamino group, for example, an -O-alkyl group (the alkyl group represents the above-mentioned C1-10 alkyl group);
A C1-5 alkylamino group such as methylamino, ethylamino or propylamino; a di-lower alkylamino group; for example, a di-C1-5 alkylamino group such as dimethylamino; a lower alkenyl group ,
For example, vinyl, allyl, 1-propenyl or 1-
A C2-5 alkenyl group such as butenyl and the like; a cycloalkyl group is a C3-6 such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl.
An aryl group is, for example, phenyl or naphthyl; an alkoxycarbonyl group is, for example, a -COO-alkyl group (an alkyl group is
It represents the above-mentioned C1-10 alkyl group. A hydroxy lower alkyl group is, for example, hydroxymethyl,
An amino-C1-5 alkyl group such as hydroxyethyl or hydroxypropyl; an amino-lower alkyl group is, for example, an amino-C1-5 alkyl group such as aminomethyl, aminoethyl or aminopropyl; An amino lower alkyl group is, for example, a C1-5 alkylamino-C1-5 alkyl group such as methylaminomethyl, ethylaminomethyl or ethylaminoethyl; a di-lower alkylamino lower alkyl group is, for example, A di-C1-5 alkylamino-C1-5 alkyl group such as dimethylaminomethyl or diethylaminomethyl; a cyclic amino group is
For example, piperazinyl, morpholinyl or 1,4-
4 such as diazabicyclo (3,2,1) octyl
A cyclic amino lower alkyl group is a 4- to 6-membered cyclic amino group such as 1-piperazinylmethyl, 1-pyridinylmethyl, 1-azetidinylmethyl or 1-morpholinylmethyl; Cyclic amino-C1-5
An alkyl group; an acylamino group includes, for example, a C1-4 acylamino group such as formylamino, acetylamino, propionylamino, or butyrylamino; an acyloxy group includes, for example, formyloxy;
A C 1-4 acyloxy group such as acetyloxy, propionyloxy or butyryloxy; a trihalogeno-lower alkyl group is, for example, a trihalogeno-C 1-5 alkyl group such as trichloromethyl or trifluoromethyl; The formula group is an oxygen atom,
A 5- or 6-membered ring containing one or more atoms selected from a nitrogen atom and a sulfur atom or a fused ring thereof, for example, furyl, pyrrolyl, thienyl, oxazolyl, imidazolyl, thiazolyl, 1-pyrrolidinyl, benzofuryl, benzothiazolyl, Groups such as pyridyl, quinolyl, pyrimidinyl or morpholinyl are meant respectively.

In each formula, R3, R4, R5, R
6, the alkyl represented by R10 and R11 is linear,
It may be branched, and may be, for example, lower alkyl (C1-
4) methyl, ethyl, propyl, isopropyl,
Examples thereof include butyl isobutyl, sec-butyl, 1-butyl, pentyl, isopentyl, neopentyl, and hexyl. These alkyls may further have a lower cycloalkyl (C3-4) at the terminal (for example, cyclopropylmethyl, cyclobutylethyl, cyclopentylmethyl, etc.).

In each formula, R3, R4, R5, R
6, lower cycloalkyl (C3-4) among cycloalkyls represented by R10 and R11 includes, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and the like. Examples of the alkoxyalkyl include, for example, ethyl, methyl, methoxyethyl, ethoxyethyl, propoxyethyl, isopropoxyethyl,
Putoxyethyl, methoxypropyl, 2-ethoxy-1
-Methylethyl and the like.

In each formula, R3, R4, R5, R
Examples of the linear or branched alkylene represented by 6, R10 and R11 include methylene, ethylene, trimethylene, tetramethylene, 1,2-dimethylethylene and the like.

In each formula, R3, R4, R5, R
6, each of the groups R10 and R11 or the methylene group represented by a in Formula 3 may be a halogen atom, a cyano group, an optionally protected carboxyl group, an optionally protected hydroxyl group, or an optionally protected group. Selected from an amino group, an alkyl group, an alkoxy group, an alkoxycarbonyl group, an aryl group, a cycloalkyl group, an acylamino group, an acyloxy group, a lower alkenyl group, a trihalogeno-lower alkyl group, a lower alkylamino group or a di-lower alkylamino group. And each of R2 and R5 may be a halogen atom, a lower alkyl group, an optionally protected carboxyl group, an optionally protected hydroxyl group, A good amino group, a lower alkylamino group which may be protected,
Optionally protected amino lower alkyl group, optionally protected lower alkylamino lower alkyl group, optionally protected hydroxy lower alkyl group, di-lower alkylamino group, di-lower alkylamino lower alkyl group Alternatively, it may be substituted with one or more substituents selected from a cyclic amino lower alkyl group and the like.

Examples of the carboxyl-protecting group include pharmaceutically acceptable carboxyl-protecting groups such as ester-forming groups which are easily eliminated in vivo. Examples of the protecting group for an amino group, an amino lower alkyl group, a lower alkylamino group, and a lower alkylamino lower alkyl group include, for example, pharmaceutically acceptable amino protecting groups which are easily eliminated in a living body.

Further, examples of the protecting groups for the hydroxyl group and the hydroxy lower alkyl group include pharmaceutically acceptable hydroxyl protecting groups which are easily eliminated in vivo.

Although a halogen compound can be added to the composition of the present invention, it is necessary to pay close attention to the toxicity of the composition. By adding a halogen compound, coloring by light can be prevented. Examples of the halogen compound used in the composition of the present invention include alkali metal halides such as potassium bromide, sodium bromide, potassium chloride, sodium chloride, potassium iodide and sodium iodide; calcium bromide, magnesium bromide ,
Alkaline earth metals such as calcium chloride and magnesium chloride; and zinc halides such as zinc bromide and zinc chloride.

In the present specification, unless otherwise specified or unless otherwise apparent from the context, an “alkyl group”
Include those having a straight chain and those having a branch. Similarly, in the group containing an alkyl group such as an “alkoxyl group”, an “aralkyl group”, and an “alkylamino group”, a straight-chain alkyl group and a branched alkyl group are also included. Further, the “cycloalkyl group” also includes a branched group such as an ethylcyclopentyl group and a methylcyclohexyl group.

The composition of the present invention can also be applied directly to the surface of wounds such as burns, pressure sores or infectious diseases,
It can also be used in combination with a pharmaceutically acceptable carrier. Further, when used in a living space, environment or industry, it can be used in the production processing stage of the target material and also in the post-processing. Although not limited to the examples, for example, as a countermeasure against antibacterial, antibacterial and mildew of building materials, furniture, furniture, bathtub toiletries, home appliances, household goods, household goods, etc., to be added at each production processing stage. It is also possible to carry out surface treatment by attached spraying after each production. Further, it can be used for kneading into the yarn at the stage of producing and processing the material such as fiber, and can also be used in post-processing. By using a sheet or a film material, the intended effects described in the claims can be achieved.

The pharmaceutically acceptable carrier includes, for example, polyoxyalkylene alkyl ether, polyoxyethylene sorbitan fatty acid ester, polyvinylpyrrolidone, hydrocarbon, paraffin, alcohol, polyhydric alcohol, alcohol ester, polyhydric alcohol ester, Examples include biologically acceptable carriers such as fatty acids or metal salts of fatty acids. In addition, chitosan, polyethylene glycol, polyglycerin fatty acid ester (caprylic acid, capric acid, lauric acid) and the like can be exemplified.

Further, when the composition of the present invention is used in combination with a pharmaceutically acceptable carrier, it is generally known in the form of a cream, ointment, plaster, poultice, emulsion, suspension, or the like. Agents, liniments, lotions, aerosols, solutions, tapes and the like can be used in various forms depending on the form of treatment. Further, a solubilizing agent, a tonicity agent, a pH adjuster, a deodorant, a preservative, a flavoring agent, and the like may be added. It can be added not only as a food preservative, but also as a germicidal, antibacterial and antifungal agent for building materials, furniture, bathroom tub toiletries, home appliances, daily necessities, household goods, etc. at each production and processing stage. Yes, after each production, the surface can be processed by attached spraying or the like. Further, it can be used for kneading into the yarn at the stage of producing and processing the material such as fiber, and can also be used in post-processing. By using a sheet, a film material or the like, a desired effect can be obtained as a wallpaper or a filter. When used as a spermicide or contraceptive, surface treatment of contraceptive devices such as ointments and creams, as well as condoms, can also be performed.

Hereinafter, the present invention will be described in detail. As the inhibitor or inhibitor of the function expressed by the multidimensional structure used in the present invention, the above-mentioned object can be achieved even when administered alone, as long as the molecular charge distribution and the molecular charge density are not significantly changed. It can also be used in the form of an acid addition salt, an emulsifier, an ester, or a polymerizer. For example, the chemical formulas (1a), (1b), (2), and (3a)
The acid addition salt of the substance represented by (3b) is a pharmaceutically acceptable non-toxic salt, for example, hydrochloric acid, hydrobromic acid,
Examples thereof include inorganic acids such as phosphoric acid and sulfuric acid, and organic acids such as acetic acid, citric acid, tartaric acid, lactic acid, succinic acid, fumaric acid, maleic acid, and metasulfonic acid.

In the present invention, among the compounds represented by the chemical formula (1a), specific examples of the compound represented by the chemical formula (1a) include the following compounds. However, the present invention is not limited by the specific examples illustrated. Specifically, for example, R1, R
Alkanes in which 2, R3, R4, R5, R6, R8, and R9 are all hydrogen atoms and hydrogen atoms and R7 is an acyclic hydrocarbon include (1) 4-isopropyl-2-cyclohexen-1-one. (2) 4-isobutyl-2-cyclohexen-1-one (3) 4-isopentyl-2-cyclohexen-1-one (4) 4-isohexyl-2-cyclohexen-1-one and the like, and R1, R2, R3, R4, R5, R6, R
Examples of amine hydrazines in which 8, R9 are all hydrogen atoms and R7 is nitrogen include (5) 4-dimethylamino-2-cyclohexene-1-
ON (6) 4-dimethylhydrazono-2-cyclohexene-
1-one (7) 4-Isopropylidenehydrazino-2-cyclohexen-1-one and the like, and also R1, R2, R3, R4, R
Examples of phosphines and analogs in which 5, R6, R8, and R9 are all hydrogen atoms and R7 is phosphorus, arsenic, or antimony include: (8) 4-dimethylphosphinetrile-2-cyclohexen-1-one (9) 4-Dimethylaridinetrile-2-cyclohexen-1-one (10) 4-dimethylstibinetril-2-cyclohexen-1-one (11) 4-dimethylbismutinetrile-2-cyclohexen-1-one and the like R1, R2, R3, R4, R
Sulfur compounds in which 5, R6, R8, and R9 are all hydrogen atoms and R7 is sulfur include (12) 4-isopropanesulfo-2-cyclohexen-1-one (13) 4-isopropanesulfino-2 -Cyclohexen-1-one (14) 4-Isopropanesulfeno-2-cyclohexen-1-one and the like, and their acid addition salts. In the present invention, among the compounds represented by the chemical formula (1b), for example, specific compounds of the chemical formula (1b) include:
For example, the following compounds can be mentioned. However, the present invention is not limited by the specific examples illustrated. Specifically, for example, R1, R2, R3, R4,
Alkanes in which R5, R6, R8, R9, R10 and R11 are all hydrogen atoms and R7 is an acyclic hydrocarbon include (1) 4-isopropyl-2-cyclohexane-1-one (2) 4- Isobutyl-2-cyclohexane-1-one (3) 4-isopentyl-2-cyclohexane-1-one (4) 4-isohexyl-2-cyclohexane-1-one and the like, and also R1, R2, R3, R4, R5, R6 , R
Amine and hydrazines in which 8, R9, R10 and R11 are all hydrogen atoms and R7 is nitrogen include (5) 4-dimethylamino-2-cyclohexane-1-
ON (6) 4-dimethylhydrazono-2-cyclohexane-
1-one (7) 4-Isopropylidenehydrazino-2-cyclohexane-1-one and the like and also R1, R2, R3, R4, R
Examples of phosphines and analogs in which 5, R6, R8, R9, R10, and R11 are all hydrogen atoms and R7 is phosphorus, arsenic, or antimony include: (8) 4-dimethylphosphinetrile-2-cyclohexane-1- On (9) 4-Dimethylaridinetrile-2-cyclohexane-1-one (10) 4-Dimethylstibinetril-2-cyclohexane-1-one (11) 4-Dimethylbismutinetrile-2-cyclohexane- 1-one and the like, R1, R2, R3, R4, R
5, R6, R8, R9, R10, and R11 are all hydrogen atoms and R7 is sulfur.
2) 4-Isopropanesulfo-2-cyclohexane-1
-One (13) 4-Isopropanesulfino-2-cyclohexane-1-one (14) 4-isopropanesulfeno-2-cyclohexane-1-one and the like, and acid addition salts thereof.

In the present invention, among the compounds represented by the chemical formula (2), for example, specific compounds of the chemical formula (2) include the following compounds. However, the present invention is not limited by the specific examples illustrated. Specifically, for example, R3, R4, R5,
When R6 is a hydrogen atom and R1 and R2 are acyclic saturated hydrocarbon alkyl groups, (15) 4,4,6-trimethyl-2-cyclohexen-1-one (16) 4,4 -Dimethyl-6-ethyl-2-cyclohexen-1-one (17) 4,4-dimethyl-6-propyl-2-cyclohexen-1-one (18) 4,4-dimethyl-6-isopropyl-2-cyclohexene -1-one (19) 6-butyl-4,4-dimethyl-2-cyclohexen-1-one (20) 4,4-dimethyl-6-isobutyl-2-cyclohexen-1-one (21) 6-bentyl -4,4-dimethyl-2-cyclohexen-1-one (22) 4,4-dimethyl-6-hexyl-2-cyclohexen-1-one (23) 4,4-dimethyl-6-octyl-2 Cyclohexen-1-one, etc., and the like their acid addition salts are exemplified. When R3, R4, R5, and R6 are hydrogen atoms and R1 and R2 are alkoxy groups of a heterocyclic compound, (24) 6-pentyloxy-4,4-dimethyl-2-cyclohexene-1- On (25) 4,4-dimethyl-6-hexyloxy-2-cyclohexen-1-one and the like, and acid addition salts thereof are exemplified. When R3, R4, R5, and R6 are hydrogen atoms and R1 and R2 are lower alkylamino groups of an amine, (26) 4,4-dimethyl-6-methylamino-2-cyclohexene-1- On (27) 4,4-dimethyl-6-ethylamino-2-cyclohexen-1-one (28) 4,4-dimethyl-6-propylamino-2-one
Cyclohexen-1-one (29) 4,4-dimethyl-6-dimethylamino-2-
Examples thereof include cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5, and R6 are hydrogen atoms and R1 and R2 are alkenyl groups of an acyclic unsaturated hydrocarbon, (30) 6-vinyl-4,4-dimethyl-2-cyclohexene -1-one (31) 6-allyl-4,4-dimethyl-2-cyclohexen-1-one (32) 4,4-dimethyl-6-isopropenyl-2-
Examples thereof include cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5 and R6 are hydrogen atoms and R1 and R2 are cycloalkyl groups of a monocyclic hydrocarbon, (32) 6-cyclopropyl-4,4-dimethyl-2-
Cyclohexen-1-one (32) 6-cyclobutyl-4,4-dimethyl-2-cyclohexen-1-one (32) 6-cyclopentyl-4,4-dimethyl-2-
Cyclohexen-1-one (32) 6-cyclohexyl-4,4-dimethyl-2-
Examples thereof include cyclohexen-1-one and the like, and acid addition salts thereof. R3, R4, R5, and R6 are hydrogen atoms, and R1 and R2 are alliable aromatic monovalent aromatic groups.
(32) 4,4-dimethyl-6-phenyl-2-cyclohexen-1-one (32) 4,4-dimethyl-6-naphthyl-2-cyclohexen-1-one and the like; Examples thereof include acid addition salts. R3, R4, R5 and R6 may be hydrogen atoms, and R1 and R2 may be alkoxycarbonyl groups as esters. R3, R4, R5, R6, R
When 8, R9 are hydrogen atoms and R1, R2 are hydroxy lower alkyl groups, (33) 4,4-dimethyl-6-hydroxymethyl-2
-Cyclohexen-1-one (34) 4,4-dimethyl-6-hydroxyethyl-2
-Cyclohexen-1-one (35) 4,4-dimethyl-6-hydroxypropyl-
Examples thereof include 2-cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5 and R6 are hydrogen atoms and R1 and R2 are amino lower alkyl groups, (36) 6-aminomethyl-4,4-dimethyl-2-cyclohexen-1-one (37 ) 6-Aminoethyl-4,4-dimethyl-2-cyclohexene-1-
On (38) 6-aminopropyl-4,4-dimethyl-
Examples thereof include 2-cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5 and R6 are hydrogen atoms and R1 and R2 are lower alkylamino lower alkyl groups, (39) 4,4-dimethyl-6-methylaminomethyl-
2-cyclohexen-1-one (40) 4,4-dimethyl-6-ethylaminomethyl-
2-cyclohexen-1-one (41) 4,4-dimethyl-6-ethylaminoethyl-
Examples thereof include 2-cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5, and R6 are hydrogen atoms and R1 and R2 are di-lower alkylamino lower alkyl groups, (42) 4,4-dimethyl-6-dimethylaminomethyl-2-cyclohexene- 1-one (43) 4,4-Dimethyl-6-diethylaminomethyl-2-cyclohexen-1-one and the like, and acid addition salts thereof are exemplified. When R3, R4, R5, and R6 are hydrogen atoms and R1 and R2 are cyclic amino groups, (44) 4,4-dimethyl-6-piperazinyl-2-cyclohexen-1-one (45) Examples thereof include 4,4-dimethyl-6-morpholinyl-2-cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5, and R6 are hydrogen atoms and R1 and R2 are cyclic amino lower alkyl groups, (46) 4,4-dimethyl-6-piperazinylethyl-
2-cyclohexen-1-one (47) 4,4-dimethyl-6-pyrrolidinylmethyl-
2-cyclohexen-1-one (48) 6-azetidinylmethyl-4,4-dimethyl-
2-cyclohexen-1-one (49) 4,4-dimethyl-6-morpholinylmethyl-
Examples thereof include 2-cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5, and R6 are hydrogen atoms and R1 and R2 are acylamino groups of a monoacylamine, (50) 4,4-dimethyl-6-formylamino-2-
Cyclohexen-1-one (51) 6-acetylamino-4,4-dimethyl-2-
Cyclohexen-1-one (52) 4,4-dimethyl-6-propionylamino-
2-cyclohexen-1-one (53) 6-butyrylamino-4,4-dimethyl-2-
Examples thereof include cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5, and R6 are hydrogen atoms and R1 and R2 are acyloxy groups that are esters, (54) 4,4-dimethyl-6-formyloxy-2-
Cyclohexen-1-one (55) 6-acetyloxy-4,4-dimethyl-2-
Cyclohexen-1-one (56) 4,4-dimethyl-6-propionyloxy-
2-cyclohexen-1-one (57) 6-butyryloxy-4,4-dimethyl-2-
Examples thereof include cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5 and R6 are hydrogen atoms and R1 and R2 are trihalogeno lower alkyl groups, (58) 4,4-dimethyl-6-trichloromethyl-2
-Cyclohexen-1-one (59) 4,4-dimethyl-6-trifluoromethyl-
Examples thereof include 2-cyclohexen-1-one and the like, and acid addition salts thereof. When R3, R4, R5, and R6 are hydrogen atoms and R1 and R2 are heterocyclic groups, (60) 4,4-dimethyl-6-furyl-2-cyclohexen-1-one (61) ) 4,4-Dimethyl-6-pyrrolyl-2-cyclohexen-1-one (62) 4,4-dimethyl-6-thienyl-2-cyclohexen-1-one (63) 4,4-dimethyl-6-isoxazolyl -2
-Cyclohexen-1-one (64) 4,4-dimethyl-6-imidazolyl-2-cyclohexen-1-one (65) 4,4-dimethyl-6-thiazolyl-2-cyclohexen-1-one (66) 4 , 4-Dimethyl-6-pyrrolidinyl-2-cyclohexen-1-one (67) 6-benzofuryl-4,4-dimethyl-2-cyclohexen-1-one (68) 6-benzothiazolyl-4,4-dimethyl-2
-Cyclohexen-1-one (69) 6-Viridyl-4,4-dimethyl-2-cyclohexen-1-one (70) 4,4-Dimethyl-6-quinolyl-2-cyclohexen-1-one (71) 4 , 4-dimethyl-6-pyrimidinyl-2-cyclohexen-1-one (72) 4,4-dimethyl-6-morpholinyl-2-cyclohexen-1-one and the like, and acid addition salts thereof.

In the present invention, the compound represented by the chemical formula (3a)
Of the substituents, for example, the substituent R of the chemical formula (3a)
3, R4, R5 and R6 are all hydrogen atoms
4,4-dimethyl-6-methylene-2-cyclohex
Sen-1-one can be mentioned. In addition,
Specific compounds include, for example, the following compounds
Can be However, depending on the specific examples illustrated,
The invention is not limited. Specifically, for example
If the substituents R3 and R4 are alkyl of an acyclic saturated hydrocarbon,
When it is a group, (73) 6-methylene-4,4,5-trimethyl-2-
Cyclohexen-1-one (74) 4,4-dimethyl-5-ethyl-6-methylene
-2-cyclohexen-1-one (75) 4,4-dimethyl-5-propyl-6-methyle
2-cyclohexen-1-one (76) 4,4-dimethyl-5-isopropyl-6-me
Tylene-2-cyclohexen-1-one (77) 5-butyl-4,4-dimethyl-6-methylene
-2-cyclohexen-1-one (78) 4,4-dimethyl-5-isobutyl-6-methyl
Ren-2-cyclohexen-1-one (79) 5-bentyl-4,4-dimethyl-6-methyle
2-cyclohexen-1-one (80) 4,4-dimethyl-5-hexyl-6-methyl
2-cyclohexen-1-one (81) 4,4-dimethyl-5-octyl-6-methyl
2-cyclohexen-1-one and the like and their
Examples thereof include acid addition salts. For example, when the substituents R3 and R4 are
When it is an alkoxy group of a heterocyclic compound, (82) 5-pentyloxy-4,4-dimethyl-6-methyl
Tylene-2-cyclohexen-1-one (83) 4,4-dimethyl-5-hexyloxy-6-me
Thilen-2-cyclohexen-1-one and the like and the like
These acid addition salts are exemplified. For example, the substituents R3, R
When 4 is a lower alkylamino group of an amine, (84) 4,4-dimethyl-5-methylamino-6-methyl
Tylene-2-cyclohexen-1-one (85) 4,4-dimethyl-5-ethylamino-6-me
Tylene-2-cyclohexen-1-one (86) 4,4-dimethyl-5-propylamino-6-
Methylene-2-cyclohexen-1-one (87) 4,4-dimethyl-5-dimethylamino-6-
Methylene-2-cyclohexen-1-one and the like
These acid addition salts are exemplified. For example, the substituent R3,
When R4 is an alkenyl group of an acyclic unsaturated hydrocarbon
(88) 5-vinyl-4,4-dimethyl-6-methylene
-2-cyclohexen-1-one (89) 5-allyl-4,4-dimethyl-6-methylene
-2-cyclohexen-1-one (90) 4,4-dimethyl-5-isopropenyl-6-
Methylene-2-cyclohexen-1-one and the like
These acid addition salts are exemplified. For example, the substituent R3,
When R4 is a cycloalkyl group of a monocyclic hydrocarbon,
Is (91) 5-cyclopropyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (92) 5-cyclobutyl-4,4-dimethyl-6-meth
Tylene-2-cyclohexen-1-one (93) 5-cyclopentyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (94) 5-cyclohexyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one and the like
These acid addition salts are exemplified. For example, the substituent R3,
When R4 is an aryl group of a monovalent aromatic hydrocarbon group,
Is (95) 4,4-dimethyl-5-phenyl-6-methylene
2-cyclohexen-1-one (96) 4,4-dimethyl-5-naphthyl-6-methyl
2-cyclohexen-1-one and the like and their
Examples thereof include acid addition salts. Substituents R3 and R4 are esters
Alkoxycarbonyl aromatic hydrocarbon monovalent ally
In some cases, it may be a radical. (98) 4,4-dimethyl-5-hydroxymethyl-6
-Methylene-2-cyclohexen-1-one (99) 4,4-dimethyl-5-hydroxyethyl-6
-Methylene-2-cyclohexen-1-one (100) 4,4-dimethyl-5-hydroxypropyl
-6-methylene-2-cyclohexen-1-one and the like
And their acid addition salts. For example, the substituent
When R3 and R4 are amino lower alkyl groups, (101) 5-aminomethyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (102) 5-aminoethyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (103) 5-aminopropyl-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and the like and
Examples thereof include acid addition salts. For example, the substituent R
3. When R4 is a lower alkylamino lower alkyl group,
In the case, (104) 4,4-dimethyl-5-methylaminomethyl
-6-methylene-2-cyclohexen-1-one (105) 4,4-dimethyl-5-ethylaminomethyl
-6-methylene-2-cyclohexen-1-one (106) 4,4-dimethyl-5-ethylaminoethyl
-6-methylene-2-cyclohexen-1-one and the like
And their acid addition salts. For example, the substituent
R3 and R4 are di-lower alkylamino lower alkyl groups
(107) 4,4-dimethyl-5-dimethyl
Aminomethyl-6-methylene-2-cyclohexene-1
-On (108) 4,4-dimethyl-5-diethylaminomethyl
Ru-6-methylene-2-cyclohexen-1-one and the like
And their acid addition salts. For example, replace
When the groups R3 and R4 are cyclic amino groups, (109) 4,4-dimethyl-5-piperazinyl-6
Methylene-2-cyclohexen-1-one (110) 4,4-dimethyl-5-morpholinyl-6
Methylene-2-cyclohexen-1-one and the like
These acid addition salts are exemplified. For example, the substituent R3,
When R4 is a cyclic amino lower alkyl group, (111) 4,4-dimethyl-5-piperazinylethyl
-6-methylene-2-cyclohexen-1-one (112) 4,4-dimethyl-5-pyrrolidinylmethyl
-6-methylene-2-cyclohexen-1-one (113) 5-azetidinylmethyl-4,4-dimethyl
-6-methylene-2-cyclohexen-1-one (114) 4,4-dimethyl-5-morpholinylmethyl
-6-methylene-2-cyclohexen-1-one and the like
And their acid addition salts. For example, the substituent
R3 and R4 are acylamino groups of monoacylamine
In the case, (115) 4,4-dimethyl-5-formyl
Amino-6-methylene-2-cyclohexen-1-one (116) 5-acetylamino-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (117) 4,4-dimethyl-5-propionylamino
-6-methylene-2-cyclohexen-1-one (118) 5-butyrylamino-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and the like and
Examples thereof include acid addition salts. For example, the substituent R
3, when R4 is an acyloxy group of an ester, (119) 4,4-dimethyl-5-formyloxy-6
-Methylene-2-cyclohexen-1-one (120) 5-acetyloxy-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (121) 4,4-dimethyl-5-propionyloxy
-6-methylene-2-cyclohexen-1-one (122) 5-butyryloxy-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and the like and
Examples thereof include acid addition salts. For example, the substituent R
3, when R4 is a trihalogeno lower alkyl group
Is (123) 4,4-dimethyl-5-trichloromethyl-
6-methylene-2-cyclohexen-1-one (124) 4,4-dimethyl-5-trifluoromethyl
-6-methylene-2-cyclohexen-1-one and the like
And their acid addition salts. For example, the substituent
When R3 and R4 are heterocyclic groups, (125) 4,4-dimethyl-5-furyl-6-methyl
2-cyclohexen-1-one (126) 4,4-dimethyl-5-pyrrolyl-6-methyl
Len-2-cyclohexen-1-one (127) 4,4-dimethyl-5-thienyl-6-methyl
Len-2-cyclohexen-1-one (128) 4,4-dimethyl-5-isoxazolyl-
6-methylene-2-cyclohexen-1-one (129) 4,4-dimethyl-5-imidazolyl-6
Methylene-2-cyclohexen-1-one (130) 4,4-dimethyl-5-thiazolyl-6-meth
Tylene-2-cyclohexen-1-one (131) 4,4-dimethyl-5-pyrrolidinyl-6
Methylene-2-cyclohexen-1-one (132) 5-benzofuryl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (133) 5-benzothiazolyl-4,4-dimethyl-
6-methylene-2-cyclohexen-1-one (134) 5-viridyl-4,4-dimethyl-6-methyl
Len-2-cyclohexen-1-one (135) 4,4-dimethyl-5-quinolyl-6-methyl
Ren-2-cyclohexen-1-one (136) 4,4-dimethyl-5-pyrimidinyl-6
Methylene-2-cyclohexen-1-one (137) 4,4-dimethyl-5-morpholinyl-6
Methylene-2-cyclohexen-1-ones and them
And the like. For example, when the substituent R5 is a non-ring
When it is an alkyl group of the formula saturated hydrocarbon, (138) 3,4,4-trimethyl-6-methylene-2
-Cyclohexen-1-one (139) 4,4-dimethyl-3-ethyl-6-methyle
2-cyclohexen-1-one (140) 4,4-dimethyl-6-methylene-3-pro
Pyr-2-cyclohexen-1-one (141) 4,4-dimethyl-3-isopropyl-6-
Methylene-2-cyclohexen-1-one (142) 3-butyl-4,4-dimethyl-6-methyle
2-cyclohexen-1-one (143) 4,4-dimethyl-3-isobutyl-6-me
Tylene-2-cyclohexen-1-one (144) 3-Ventyl-4,4-dimethyl-6-methyl
Len-2-cyclohexen-1-one (145) 4,4-dimethyl-3-hexyl-6-methyl
Ren-2-cyclohexen-1-one (146) 4,4-dimethyl-6-methylene-3-oct
Tyl-2-cyclohexen-1-one and their acids
Examples thereof include addition salts. For example, when the substituent R5 is a heterocyclic
When it is an alkoxy group of the compound, (147) 3-pentyloxy-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (148) 4,4-dimethyl-3-hexyloxy-6
Methylene-2-cyclohexen-1-ones and them
And the like. For example, when the substituent R5 is an amino group
(149) 4,4-dimethyl-3-methylamino-6-
Methylene-2-cyclohexen-1-one (150) 4,4-dimethyl-3-ethylamino-6
Methylene-2-cyclohexen-1-one (151) 4,4-dimethyl-6-methylene-3-pro
Pyramino-2-cyclohexen-1-one (152) 4,4-dimethyl-3-dimethylamino-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, when substituent R5 is non-
When it is an alkenyl group of a cyclic unsaturated hydrocarbon, (153) 3-vinyl-4,4-dimethyl-6-methylene
2-cyclohexen-1-one (154) 3-allyl-4,4-dimethyl-6-methyle
2-cyclohexen-1-one (155) 4,4-dimethyl-3-isopropenyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, when the substituent R5 is
When it is a cycloalkyl group of a cyclic hydrocarbon, (156) 3-cyclopropyl-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (157) 3-cyclobutyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (158) 3-cyclopentyl-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (159) 3-cyclohexyl-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, when the substituent R5 is
When it is an aryl group of a monovalent aromatic hydrocarbon group, (160) 4,4-dimethyl-3-phenyl-6-methyl
Len-2-cyclohexen-1-one (161) 4,4-dimethyl-6-methylene-3-naph
Tyl-2-cyclohexen-1-one and their acids
Examples thereof include addition salts. When the substituent R5 is an alkoxycarbo
It may be converted to a nyl group to form an ester. For example, replace
When the group R5 is a hydroxy lower alkyl group, (163) 4,4-dimethyl-3-hydroxymethyl-
6-methylene-2-cyclohexen-1-one (164) 4,4-dimethyl-3-hydroxyethyl-
6-methylene-2-cyclohexen-1-one (165) 4,4-dimethyl-3-hydroxypropyl
-6-methylene-2-cyclohexen-1-one and
Examples thereof include acid addition salts. For example, the substituent R5
Is a amino lower alkyl group, (166) 3-aminomethyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (167) 3-aminoethyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (168) 3-aminopropyl-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, when the substituent R5 is low
(169) 4,4-dimethyl-3-methylaminomethyl when it is a lower alkylamino lower alkyl group;
-6-methylene-2-cyclohexen-1-one (170) 4,4-dimethyl-3-ethylaminomethyl
-6-methylene-2-cyclohexen-1-one (171) 4,4-dimethyl-3-ethylaminoethyl
-6-methylene-2-cyclohexen-1-one and
Examples thereof include acid addition salts. For example, the substituent R5
Is a di-lower alkylamino lower alkyl group
Is (172) 3-dimethylaminomethyl-4,4-dimethyl
Le-6-methylene-2-cyclohexen-1-one (173) 3-diethylaminomethyl-4,4-dimethyl
6-methylene-2-cyclohexen-1-one and
And their acid addition salts. For example, the substituent R
When 5 is a cyclic amino group, (174) 4,4-dimethyl-6-methylene-3-pipe
Radinyl-2-cyclohexen-1-one (175) 4,4-dimethyl-6-methylene-3-mol
Holinyl-2-cyclohexen-1-ones and them
And the like. For example, when the substituent R5 is cyclic
(176) 4,4-dimethyl-6-methylene-3-pipe when it is an amino lower alkyl group;
Radinylethyl-2-cyclohexen-1-one (177) 4,4-dimethyl-6-methylene-3-pyro
Lysinylmethyl-2-cyclohexen-1-one (178) 3-azetidinylmethyl-4,4-dimethyl
-6-methylene-2-cyclohexen-1-one (179) 4,4-dimethyl-6-methylene-3-mol
Folinylmethyl-2-cyclohexen-1-one and
Examples thereof include acid addition salts. For example, the substituent R5
Is the acylamino group of a monoacylamine, (180) 4,4-dimethyl-3-formylamino-6
-Methylene-2-cyclohexen-1-one (181) 3-acetylamino-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (182) 4,4-dimethyl-6-methylene-3-pro
Pionylamino-2-cyclohexen-1-one (183) 3-butyrylamino-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, if the substituent R5 is
(184) 4,4-dimethyl-3-formyloxy-6 when it is an acyloxy group of a stele;
-Methylene-2-cyclohexen-1-one (185) 3-acetyloxy-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (186) 4,4-dimethyl-6-methylene-3-pro
Pionyloxy-2-cyclohexen-1-one (187) 3-butyryloxy-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, when the substituent R5 is
(188) 4,4-dimethyl-6-methylene-3-trialkyl
Chloromethyl-2-cyclohexen-1-one (189) 4,4-dimethyl-6-methylene-3-tri
Fluoromethyl-2-cyclohexen-1-one and
Examples thereof include acid addition salts. For example, the substituent R5
Is a heterocyclic group, (190) 4,4-dimethyl-3-furyl-6-methyl
2-cyclohexen-1-one (191) 4,4-dimethyl-6-methylene-3-pyro
Ryl-2-cyclohexen-1-one (192) 4,4-dimethyl-6-methylene-3-thier
Nyl-2-cyclohexen-1-one (193) 4,4-dimethyl-3-isoxazolyl-
6-methylene-2-cyclohexen-1-one (194) 4,4-dimethyl-3-imidazolyl-6
Methylene-2-cyclohexen-1-one (195) 4,4-dimethyl-6-methylene-3-thia
Zolyl-2-cyclohexen-1-one (196) 4,4-dimethyl-6-methylene-3-pyro
Lysinyl-2-cyclohexen-1-one (197) 3-benzofuryl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (198) 3-benzothiazolyl-4,4-dimethyl-
6-methylene-2-cyclohexen-1-one (199) 3-viridyl-4,4-dimethyl-6-methyl
Ren-2-cyclohexen-1-one (200) 4,4-dimethyl-6-methylene-3-quino
Ryl-2-cyclohexen-1-one (201) 4,4-dimethyl-6-methylene-3-pyri
Midinyl-2-cyclohexen-1-one (202) 4,4-dimethyl-6-methylene-3-mol
Holinyl-2-cyclohexen-1-ones and them
And the like. For example, when the substituent R6 is a non-ring
When it is an alkyl group of the formula saturated hydrocarbon, (203) 6-methylene-2,4,4-trimethyl-2
-Cyclohexen-1-one (204) 4,4-dimethyl-2-ethyl-6-methyle
2-cyclohexen-1-one (205) 4,4-dimethyl-6-methylene-2-pro
Pyr-2-cyclohexen-1-one (206) 4,4-dimethyl-2-isopropyl-6-
Methylene-2-cyclohexen-1-one (207) 2-butyl-4,4-dimethyl-6-methyl
2-cyclohexen-1-one (208) 4,4-dimethyl-2-isobutyl-6-me
Tylene-2-cyclohexen-1-one (209) 2-Ventyl-4,4-dimethyl-6-methyl
Len-2-cyclohexen-1-one (210) 4,4-dimethyl-2-hexyl-6-methyl
Len-2-cyclohexen-1-one (211) 4,4-dimethyl-6-methylene-2-oct
Tyl-2-cyclohexen-1-one and their acids
Examples thereof include addition salts. For example, when the substituent R6 is a heterocyclic
When the compound is an alkoxy group, (212) 2-pentyloxy-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (213) 4,4-dimethyl-2-hexyloxy-6
Methylene-2-cyclohexen-1-ones and them
And the like. For example, when the substituent R6 is an amino group
(214) 4,4-dimethyl-2-methylamino-6-
Methylene-2-cyclohexen-1-one (215) 4,4-dimethyl-2-ethylamino-6-
Methylene-2-cyclohexen-1-one (216) 4,4-dimethyl-6-methylene-2-pro
Pyramino-2-cyclohexen-1-one (217) 2-dimethylamino-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, when substituent R6 is non-
When it is an alkenyl group of a cyclic saturated hydrocarbon, (218) 2-vinyl-4,4-dimethyl-6-methylene
-2-cyclohexen-1-one (219) 2-allyl-4,4-dimethyl-6-methyl
2-cyclohexen-1-one (220) 4,4-dimethyl-2-isopropenyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, when the substituent R6 is
When it is a cycloalkyl group of a cyclic hydrocarbon, (221) 2-cyclopropyl-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (222) 2-cyclobutyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (223) 2-cyclopentyl-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (224) 2-cyclohexyl-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, when the substituent R6 is
When it is an aryl group of a monovalent aromatic hydrocarbon group, (225) 4,4-dimethyl-2-phenyl-6-methyl
Ren-2-cyclohexen-1-one (226) 4,4-dimethyl-6-methylene-2-naph
Tyl-2-cyclohexen-1-one and their acids
Examples thereof include addition salts. Substituent R6 is an alkoxycarbo
In some cases, it is substituted with a phenyl group to form an ester. For example,
When the substituent R6 is a hydroxy lower alkyl group,
Is (228) 4,4-dimethyl-2-hydroxymethyl-
6-methylene-2-cyclohexen-1-one (229) 4,4-dimethyl-2-hydroxyethyl-
6-methylene-2-cyclohexen-1-one (230) 4,4-dimethyl-2-hydroxypropyl
-6-methylene-2-cyclohexen-1-one and
Examples thereof include acid addition salts. For example, the substituent R6
Is an amino lower alkyl group, (231) 2-aminomethyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (232) 2-aminoethyl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (233) 2-aminopropyl-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, when the substituent R6 is low
When it is a lower alkylamino lower alkyl group, (234) 4,4-dimethyl-2-methylaminomethyl
-6-methylene-2-cyclohexen-1-one (235) 4,4-dimethyl-2-ethylaminomethyl
-6-methylene-2-cyclohexen-1-one (236) 4,4-dimethyl-2-ethylaminoethyl
-6-methylene-2-cyclohexen-1-one and
Examples thereof include acid addition salts. For example, the substituent R6
Is a di-lower alkylamino lower alkyl group
Is (237) 2-dimethylaminomethyl-4,4-dimethyl
6-methylene-2-cyclohexen-1-one (238) 2-diethylaminomethyl-4,4-dimethyl
6-methylene-2-cyclohexen-1-one and
And their acid addition salts. For example, the substituent R
When 6 is a cyclic amino group, (239) 4,4-dimethyl-6-methylene-2-pipe
Radinyl-2-cyclohexen-1-one (240) 4,4-dimethyl-6-methylene-2-mol
Holinyl-2-cyclohexen-1-ones and them
And the like. For example, when the substituent R6 is cyclic
When it is an amino lower alkyl group, (241) 4,4-dimethyl-6-methylene-2-pipe
Radinylethyl-2-cyclohexen-1-one (242) 4,4-dimethyl-6-methylene-2-pyro
Lysinylmethyl-2-cyclohexen-1-one (243) 2-azetidinylmethyl-4,4-dimethyl
-6-methylene-2-cyclohexen-1-one (244) 4,4-dimethyl-6-methylene-2-mol
Folinylmethyl-2-cyclohexen-1-one and
Examples thereof include acid addition salts. For example, the substituent R6
Is the acylamino group of a monoacylamine, (245) 4,4-dimethyl-2-formylamino-6
-Methylene-2-cyclohexen-1-one (246) 2-acetylamino-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (247) 4,4-dimethyl-6-methylene-2-pro
Pionylamino-2-cyclohexen-1-one (248) 2-butyrylamino-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, if the substituent R6 is
(249) 4,4-dimethyl-2-formyloxy-6 when it is an acyloxy group of a stele;
-Methylene-2-cyclohexen-1-one (250) 2-acetyloxy-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one (251) 4,4-dimethyl-6-methylene-2-pro
Pionyloxy-2-cyclohexen-1-one (252) 2-butyryloxy-4,4-dimethyl-6
-Methylene-2-cyclohexen-1-one and it
These acid addition salts are exemplified. For example, if the substituent R6 is
When it is a lihalogeno lower alkyl group, (253) 4,4-dimethyl-6-methylene-2-tri
Chloromethyl-2-cyclohexen-1-one (254) 4,4-dimethyl-6-methylene-2-tri
Fluoromethyl-2-cyclohexen-1-one and
Examples thereof include acid addition salts. For example, the substituent R6
Is a heterocyclic group, (255) 4,4-dimethyl-2-furyl-6-methylene
2-cyclohexen-1-one (256) 4,4-dimethyl-6-methylene-2-pyro
Ryl-2-cyclohexen-1-one (257) 4,4-dimethyl-6-methylene-2-thie
Nyl-2-cyclohexen-1-one (258) 4,4-dimethyl-2-isoxazolyl-
6-methylene-2-cyclohexen-1-one (259) 4,4-dimethyl-2-imidazolyl-6
Methylene-2-cyclohexen-1-one (260) 4,4-dimethyl-6-methylene-2-thia
Zolyl-2-cyclohexen-1-one (261) 4,4-dimethyl-6-methylene-2-pyro
Lysinyl-2-cyclohexen-1-one (262) 2-benzofuryl-4,4-dimethyl-6-
Methylene-2-cyclohexen-1-one (263) 2-benzothiazolyl-4,4-dimethyl-
6-methylene-2-cyclohexen-1-one (264) 2-viridyl-4,4-dimethyl-6-methyl
Len-2-cyclohexen-1-one (265) 4,4-dimethyl-6-methylene-2-quino
Ryl-2-cyclohexen-1-one (267) 4,4-dimethyl-6-methylene-2-pyri
Midinyl-2-cyclohexen-1-one (268) 4,4-dimethyl-6-methylene-2-mol
Holinyl-2-cyclohexen-1-ones and them
And the like. For example, the chemical formula (3a)
Wherein R5 and R6 are condensed polycyclic hydrocarbon compounds or condensed
When it is a bonding group of a heterocyclic compound, (269) 5H-4-dimethyl-6-methylene-7-o
Oxo-indene (270) 4-dimethyl-2-methylene-1-oxo-
Tetralin (271) 3H-4-dimethyl-2-methylene-1-o
Oxo-anthracene (272) 5H-4-dimethyl-6-methylene-7-o
Oxo-benzothiophene (273) 5H-4-dimethyl-6-methylene-7-o
Oxo-benzofuran (274) 5H-4-dimethyl-6-methylene-7-o
Oxo-indole (275) 6H-5-dimethyl-7-methylene-8-o
Oxo-quinoline (276) 6H-5-dimethyl-7-methylene-8-o
Oxo-quinoxaline (277) 6H-5-dimethyl-7-methylene-8-o
Oxo-sinoline (278) 5H-5-dimethyl-7-methylene-8-o
Oxo-1,4-dithianophthalene (279) 3H-4-dimethyl-2-methylene-1-o
Examples include xo-thianthrene and their acid addition salts.
It is.

In the present invention, the compound represented by the chemical formula (3b)
Of the substituents, for example, the substituent R of the chemical formula (3b)
3, R4, R5 and R6 are all hydrogen atoms,
4,4-dimethyl-2-cyclohexen-1-one
I can do it. In addition, specific compounds and
For example, the following compounds can be mentioned. I
However, the specific examples illustrated limit the invention.
Not something. Specifically, for example, substituents R3 and R4
Is a noncyclic saturated hydrocarbon alkyl group, (280) 4,4,5-trimethyl-2-cyclohexene
1-one (281) 4,4-dimethyl-5-ethyl-2-cyclo
Hexen-1-one (282) 4,4-dimethyl-5-propyl-2-cycl
Rohexen-1-one (283) 4,4-dimethyl-5-isopropyl-2-
Cyclohexen-1-one (284) 5-butyl-4,4-dimethyl-2-cyclo
Hexen-1-one (285) 4,4-dimethyl-5-isobutyl-2-cy
Clohexen-1-one (286) 5-Bentyl-4,4-dimethyl-2-cycl
Rohexen-1-one (287) 4,4-dimethyl-5-hexyl-2-cycl
Rohexen-1-one (288) 4,4-dimethyl-5-octyl-2-cycl
Rohexen-1-one and the like and their acid addition salts
Is exemplified. For example, when the substituents R3 and R4 are heterocyclic compounds
(289) 5-pentyloxy-4,4-dimethyl-2-
Cyclohexen-1-one (290) 4,4-dimethyl-5-hexyloxy-2-
Cyclohexen-1-one and the like and acid addition salts thereof
Etc. are exemplified. For example, when the substituents R3 and R4 are
When it is a lower alkylamino group, (291) 4,4-dimethyl-5-methylamino-2-
Cyclohexen-1-one (292) 4,4-dimethyl-5-ethylamino-2-
Cyclohexen-1-one (293) 4,4-dimethyl-5-propylamino-2
-Cyclohexen-1-one (294) 4,4-dimethyl-5-dimethylamino-2
-Cyclohexen-1-one and the like and acid addition thereof
Salts and the like are exemplified. For example, when the substituents R3 and R4 are acyclic
When it is an alkenyl group of an unsaturated hydrocarbon, (295) 5-vinyl-4,4-dimethyl-2-cyclo
Hexen-1-one (296) 5-allyl-4,4-dimethyl-2-cyclo
Hexen-1-one (297) 4,4-dimethyl-5-isopropenyl-2
-Cyclohexen-1-one and the like and acid addition thereof
Salts and the like are exemplified. For example, when the substituents R3 and R4 are monocyclic
When it is a hydrocarbon cycloalkyl group, (298) 5-cyclopropyl-4,4-dimethyl-2
-Cyclohexen-1-one (299) 5-cyclobutyl-4,4-dimethyl-2-
Cyclohexen-1-one (300) 5-cyclopentyl-4,4-dimethyl-2
-Cyclohexen-1-one (301) 5-cyclohexyl-4,4-dimethyl-2
-Cyclohexen-1-one and the like and acid addition thereof
Salts and the like are exemplified. For example, when the substituents R3 and R4 are aromatic
(302) 4,4-dimethyl-5-phenyl-2-cyclyl when the aryl group is a monovalent hydrocarbon group;
Rohexen-1-one (303) 4,4-dimethyl-5-naphthyl-2-cycl
Rohexen-1-one and the like and their acid addition salts
Is exemplified. Substituents R3 and R4 are ester alkoxy
When the carbonyl group is an aromatic hydrocarbon monovalent aryl group
In some cases. (305) 4,4-dimethyl-5-hydroxymethyl-
2-cyclohexen-1-one (306) 4,4-dimethyl-5-hydroxyethyl-
2-cyclohexen-1-one (307) 4,4-dimethyl-5-hydroxypropyl
-2-cyclohexen-1-one and the like and their acids
Examples thereof include addition salts. For example, when the substituents R3 and R4 are
In the case of a mino lower alkyl group, (308) 5-aminomethyl-4,4-dimethyl-2-
Cyclohexen-1-one (309) 5-aminoethyl-4,4-dimethyl-2-
Cyclohexen-1-one (310) 5-aminopropyl-4,4-dimethyl-2
-Cyclohexen-1-one and the like and acid addition thereof
Salts and the like are exemplified. For example, when the substituents R3 and R4 are lower
When it is a alkylamino lower alkyl group, (311) 4,4-dimethyl-5-methylaminomethyl
-2-cyclohexen-1-one (312) 4,4-dimethyl-5-ethylaminomethyl
-2-cyclohexen-1-one (313) 4,4-dimethyl-5-ethylaminoethyl
-2-cyclohexen-1-one and the like and their acids
Examples thereof include addition salts. For example, when the substituents R3 and R4 are di
When it is a lower alkylamino lower alkyl group, (314) 4,4-dimethyl-5-dimethylaminomethyl
Ru-2-cyclohexen-1-one (315) 4,4-dimethyl-5-diethylaminomethyl
2-cyclohexen-1-one and the like and their
Examples thereof include acid addition salts. For example, when the substituents R3 and R4 are
In the case of a cyclic amino group, (316) 4,4-dimethyl-5-piperazinyl-2-
Cyclohexen-1-one (317) 4,4-dimethyl-5-morpholinyl-2-
Cyclohexen-1-one and the like and acid addition salts thereof
Etc. are exemplified. For example, when the substituents R3 and R4
(318) 4,4-dimethyl-5-piperazinylethyl
-2-cyclohexen-1-one (319) 4,4-dimethyl-5-pyrrolidinylmethyl
-2-cyclohexen-1-one (320) 5-azetidinylmethyl-4,4-dimethyl
-2-cyclohexen-1-one (321) 4,4-dimethyl-5-morpholinylmethyl
-2-cyclohexen-1-one and the like and their acids
Examples thereof include addition salts. For example, when the substituents R3 and R4 are
When it is an acylamino group of noacylamine, (322) 4,4-dimethyl-5-formylamino-2
-Cyclohexen-1-one (323) 5-acetylamino-4,4-dimethyl-2
-Cyclohexen-1-one (324) 4,4-dimethyl-5-propionylamino
-2-cyclohexen-1-one (325) 5-butyrylamino-4,4-dimethyl-2
-Cyclohexen-1-one and the like and acid addition thereof
Salts and the like are exemplified. For example, when the substituents R3 and R4
(326) 4,4-dimethyl-5-formyloxy-2
-Cyclohexen-1-one (327) 5-acetyloxy-4,4-dimethyl-2
-Cyclohexen-1-one (328) 4,4-dimethyl-5-propionyloxy
-2-cyclohexen-1-one (329) 5-butyryloxy-4,4-dimethyl-2
-Cyclohexen-1-one and the like and acid addition thereof
Salts and the like are exemplified. For example, when the substituents R3 and R4 are
(330) 4,4-dimethyl-5-trichloromethyl-
2-cyclohexen-1-one (331) 4,4-dimethyl-5-trifluoromethyl
-2-cyclohexen-1-one and the like and their acids
Examples thereof include addition salts. For example, when the substituents R3 and R4 are
In the case of a cyclic group, (332) 4,4-dimethyl-5-furyl-2-cyclo
Hexen-1-one (333) 4,4-dimethyl-5-pyrrolyl-2-cycl
Rohexen-1-one (334) 4,4-dimethyl-5-thienyl-2-cycl
Rohexen-1-one (335) 4,4-dimethyl-5-isoxazolyl-
2-cyclohexen-1-one (336) 4,4-dimethyl-5-imidazolyl-2-
Cyclohexen-1-one (337) 4,4-dimethyl-5-thiazolyl-2-cy
Clohexen-1-one (338) 4,4-dimethyl-5-pyrrolidinyl-2-
Cyclohexen-1-one (339) 5-benzofuryl-4,4-dimethyl-2-
Cyclohexen-1-one (340) 5-benzothiazolyl-4,4-dimethyl-
2-cyclohexen-1-one (341) 5-biridyl-4,4-dimethyl-2-cycl
Rohexen-1-one (342) 4,4-dimethyl-5-quinolyl-2-cycl
Rohexen-1-one (343) 4,4-dimethyl-5-pyrimidinyl-2-
Cyclohexen-1-one (344) 4,4-dimethyl-5-morpholinyl-2-
Cyclohexen-1-one and their acid addition salts and the like
Is exemplified. For example, when the substituent R5 is an acyclic saturated hydrocarbon
(345) 3,4,4-trimethyl-2-cyclohexene
1-one (346) 4,4-dimethyl-3-ethyl-2-cyclo
Hexen-1-one (347) 4,4-dimethyl-3-propyl-2-cycl
Rohexen-1-one (348) 4,4-dimethyl-3-isopropyl-2-
Cyclohexen-1-one (349) 3-butyl-4,4-dimethyl-2-cyclo
Hexen-1-one (350) 4,4-dimethyl-3-isobutyl-2-cy
Clohexen-1-one (351) 3-Ventyl-4,4-dimethyl-2-cycl
Rohexen-1-one (352) 4,4-dimethyl-3-hexyl-2-cycl
Rohexen-1-one (353) 4,4-dimethyl-3-octyl-2-cycl
Examples include rohexen-1-one and their acid addition salts.
Is done. For example, when the substituent R5 is an alcohol of a heterocyclic compound
When it is a xy group, (354) 3-pentyloxy-4,4-dimethyl-2-
Cyclohexen-1-one (355) 4,4-dimethyl-3-hexyloxy-2-
Cyclohexen-1-one and their acid addition salts and the like
Is exemplified. For example, when the substituent R5 is a lower alkyl of an amine.
(356) 4,4-dimethyl-3-methylamino-2-
Cyclohexen-1-one (357) 4,4-dimethyl-3-ethylamino-2-
Cyclohexen-1-one (358) 4,4-dimethyl-3-propylamino-2
-Cyclohexen-1-one (359) 3-dimethylamino-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R5 is an acyclic unsaturated carbon
When it is an alkenyl group of hydrogen, (360) 3-vinyl-4,4-dimethyl-2-cyclo
Hexen-1-one (361) 3-allyl-4,4-dimethyl-2-cyclo
Hexen-1-one (362) 4,4-dimethyl-3-isopropenyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R5 is a monocyclic hydrocarbon
When it is a cycloalkyl group, (363) 3-cyclopropyl-4,4-dimethyl-2
-Cyclohexen-1-one (364) 3-cyclobutyl-4,4-dimethyl-2-
Cyclohexen-1-one (365) 3-cyclopentyl-4,4-dimethyl-2
-Cyclohexen-1-one (366) 3-cyclohexyl-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R5 is an aromatic hydrocarbon 1
(367) 4,4-dimethyl-3-phenyl-2-cycloalkyl when it is an aryl group of a valency group
Rohexen-1-one (368) 4,4-dimethyl-3-naphthyl-2-cycl
Examples include rohexen-1-one and their acid addition salts.
Is done. When the substituent R5 becomes an alkoxycarbonyl group,
It can be a steal. For example, if substituent R5 is hydro
(370) 4,4-dimethyl-3-hydroxymethyl-
2-cyclohexen-1-one (371) 4,4-dimethyl-3-hydroxyethyl-
2-cyclohexen-1-one (372) 4,4-dimethyl-3-hydroxypropyl
-2-Cyclohexen-1-one and their acid addition
Salts and the like are exemplified. For example, when the substituent R5 is an amino lower amine,
When it is a alkyl group, (373) 3-aminomethyl-4,4-dimethyl-2-
Cyclohexen-1-one (374) 3-aminoethyl-4,4-dimethyl-2-
Cyclohexen-1-one (375) 3-aminopropyl-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R5 is a lower alkyl
(376) 4,4-dimethyl-3-methylaminomethyl when it is a lower alkyl group
-2-cyclohexen-1-one (377) 4,4-dimethyl-3-ethylaminomethyl
-2-cyclohexen-1-one (378) 4,4-dimethyl-3-ethylaminoethyl
-2-Cyclohexen-1-one and their acid addition
Salts and the like are exemplified. For example, when the substituent R5 is a di-lower alkyl
And (379) 3-dimethylaminomethyl-4,4-dimethyl.
2-cyclohexen-1-one (380) 3-diethylaminomethyl-4,4-dimethyl
R-2-cyclohexen-1-one and their acids
Salting is exemplified. For example, when the substituent R5 is a cyclic amino
When it is a group, (381) 4,4-dimethyl-3-piperazinyl-2-
Cyclohexen-1-one (382) 4,4-dimethyl-3-morpholinyl-2-
Cyclohexen-1-one and their acid addition salts and the like
Is exemplified. For example, when the substituent R5 is a cyclic amino lower alkyl
When it is a kill group, (383) 4,4-dimethyl-3-piperazinylethyl
-2-cyclohexen-1-one (384) 4,4-dimethyl-3-pyrrolidinylmethyl
-2-cyclohexen-1-one (385) 3-azetidinylmethyl-4,4-dimethyl
-2-cyclohexen-1-one (386) 4,4-dimethyl-3-morpholinylmethyl
-2-Cyclohexen-1-one and their acid addition
Salts and the like are exemplified. For example, when the substituent R5 is a monoacyla
(387) 4,4-dimethyl-3-formylamino-2 when it is an acylamino group of a min.
-Cyclohexen-1-one (388) 3-acetylamino-4,4-dimethyl-2
-Cyclohexen-1-one (389) 4,4-dimethyl-3-propionylamino
-2-cyclohexen-1-one (390) 3-butyrylamino-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R5 is an acyl ester
When it is an oxy group, (391) 4,4-dimethyl-3-formyloxy-2
-Cyclohexen-1-one (392) 3-acetyloxy-4,4-dimethyl-2
-Cyclohexen-1-one (393) 4,4-dimethyl-3-propionyloxy
-2-cyclohexen-1-one (394) 3-butyryloxy-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R5 is a trihalogeno lower
When it is an alkyl group, (395) 4,4-dimethyl-3-trichloromethyl-
2-cyclohexen-1-one (396) 4,4-dimethyl-3-trifluoromethyl
-2-Cyclohexen-1-one and their acid addition
Salts and the like are exemplified. For example, when the substituent R5 is a heterocyclic group,
In some cases, (397) 4,4-dimethyl-3-furyl-2-cyclo
Hexen-1-one (398) 4,4-dimethyl-3-pyrrolyl-2-cycl
Rohexen-1-one (399) 4,4-dimethyl-3-thienyl-2-cycl
Rohexen-1-one (400) 4,4-dimethyl-3-isoxazolyl-
2-cyclohexen-1-one (401) 4,4-dimethyl-3-imidazolyl-2-
Cyclohexen-1-one (402) 4,4-dimethyl-3-thiazolyl-2-cy
Clohexen-1-one (403) 4,4-dimethyl-3-pyrrolidinyl-2-
Cyclohexen-1-one (404) 3-benzofuryl-4,4-dimethyl-2-
Cyclohexen-1-one (405) 3-benzothiazolyl-4,4-dimethyl-
2-cyclohexen-1-one (406) 3-viridyl-4,4-dimethyl-2-cycl
Rohexen-1-one (407) 4,4-dimethyl-3-quinolyl-2-cycl
Rohexen-1-one (408) 4,4-dimethyl-3-pyrimidinyl-2-
Cyclohexen-1-one (409) 4,4-dimethyl-3-morpholinyl-2-
Cyclohexen-1-one and their acid addition salts and the like
Is exemplified. For example, when the substituent R6 is an acyclic saturated hydrocarbon
(410) 2,4,4-trimethyl-2-cyclohexene
1-one (411) 4,4-dimethyl-2-ethyl-2-cyclo
Hexen-1-one (412) 4,4-dimethyl-2-propyl-2-cycl
Rohexen-1-one (413) 4,4-dimethyl-2-isopropyl-2-
Cyclohexen-1-one (414) 2-butyl-4,4-dimethyl-2-cyclo
Hexen-1-one (415) 4,4-dimethyl-2-isobutyl-2-cy
Clohexen-1-one (416) 2-Bentyl-4,4-dimethyl-2-cycl
Rohexen-1-one (417) 4,4-dimethyl-2-hexyl-2-cycl
Rohexen-1-one (418) 4,4-dimethyl-2-octyl-2-cycl
Examples include rohexen-1-one and their acid addition salts.
Is done. For example, when the substituent R6 is an alcohol of a heterocyclic compound
When it is a xy group, (419) 2-pentyloxy-4,4-dimethyl-2-
Cyclohexen-1-one (420) 4,4-dimethyl-2-hexyloxy-2-
Cyclohexen-1-one and their acid addition salts and the like
Is exemplified. For example, when the substituent R6 is a lower alkyl of an amine.
(421) 4,4-dimethyl-2-methylamino-2-
Cyclohexen-1-one (422) 4,4-dimethyl-2-ethylamino-2-
Cyclohexen-1-one (423) 4,4-dimethyl-2-propylamino-2
-Cyclohexen-1-one (424) 2-dimethylamino-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R6 is an acyclic saturated hydrocarbon
(425) 2-vinyl-4,4-dimethyl-2-cycloalkyl
Hexen-1-one (426) 2-allyl-4,4-dimethyl-2-cyclo
Hexen-1-one (427) 4,4-dimethyl-2-isopropenyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R6 is a monocyclic hydrocarbon
When it is a cycloalkyl group, (428) 2-cyclopropyl-4,4-dimethyl-2
-Cyclohexen-1-one (429) 2-cyclobutyl-4,4-dimethyl-2-
Cyclohexen-1-one (430) 2-cyclopentyl-4,4-dimethyl-2
-Cyclohexen-1-one (431) 2-cyclohexyl-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R6 is an aromatic hydrocarbon 1
(432) 4,4-dimethyl-2-phenyl-2-cyclyl when it is an aryl group of a valent group
Rohexen-1-one (433) 4,4-dimethyl-2-naphthyl-2-cycl
Examples include rohexen-1-one and their acid addition salts.
Is done. When the substituent R6 is an alkoxycarbonyl group,
It can be a steal. For example, if the substituent R6 is hydro
When it is a xy lower alkyl group, (435) 4,4-dimethyl-2-hydroxymethyl-
2-cyclohexen-1-one (436) 4,4-dimethyl-2-hydroxyethyl-
2-cyclohexen-1-one (437) 4,4-dimethyl-2-hydroxypropyl
-2-Cyclohexen-1-one and their acid addition
Salts and the like are exemplified. For example, when the substituent R6 is an amino lower amine
When it is a alkyl group, (438) 2-aminomethyl-4,4-dimethyl-2-
Cyclohexen-1-one (439) 2-aminoethyl-4,4-dimethyl-2-
Cyclohexen-1-one (440) 2-aminopropyl-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R6 is a lower alkylamino
(441) 4,4-dimethyl-2-methylaminomethyl when it is a lower alkyl group
-2-cyclohexen-1-one (442) 4,4-dimethyl-2-ethylaminomethyl
-2-cyclohexen-1-one (443) 4,4-dimethyl-2-ethylaminoethyl
-2-Cyclohexen-1-one and their acid addition
Salts and the like are exemplified. For example, when the substituent R6 is a di-lower alkyl
(444) 2-dimethylaminomethyl-4,4-dimethyl
Ru-2-cyclohexen-1-one (445) 2-diethylaminomethyl-4,4-dimethyl
R-2-cyclohexen-1-one and their acids
Salting is exemplified. For example, when the substituent R6 is a cyclic amino
When it is a group, (446) 4,4-dimethyl-2-piperazinyl-2-
Cyclohexen-1-one (447) 4,4-dimethyl-2-morpholinyl-2-
Cyclohexen-1-one and their acid addition salts and the like
Is exemplified. For example, when the substituent R6 is a cyclic amino lower alkyl
When it is a kill group, (448) 4,4-dimethyl-2-piperazinylethyl
-2-cyclohexen-1-one (449) 4,4-dimethyl-2-pyrrolidinylmethyl
-2-cyclohexen-1-one (450) 2-azetidinylmethyl-4,4-dimethyl
-2-cyclohexen-1-one (451) 4,4-dimethyl-2-morpholinylmethyl
-2-Cyclohexen-1-one and their acid addition
Salts and the like are exemplified. For example, when the substituent R6 is a monoacyla
(452) 4,4-dimethyl-2-formylamino-2 when it is an acylamino group of a min.
-Cyclohexen-1-one (453) 2-acetylamino-4,4-dimethyl-2
-Cyclohexen-1-one (454) 4,4-dimethyl-2-propionylamino
-2-cyclohexen-1-one (455) 2-butyrylamino-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R6 is an ester acyl
When it is an oxy group, (456) 4,4-dimethyl-2-formyloxy-2
-Cyclohexen-1-one (457) 2-acetyloxy-4,4-dimethyl-2
-Cyclohexen-1-one (458) 4,4-dimethyl-2-propionyloxy
-2-Cyclohexen-1-one (459) 2-butyryloxy-4,4-dimethyl-2
-Cyclohexen-1-one and acid addition salts thereof and the like
Is exemplified. For example, when the substituent R6 is a trihalogeno lower
When it is an alkyl group, (460) 4,4-dimethyl-2-trichloromethyl-
2-cyclohexen-1-one (461) 4,4-dimethyl-2-trifluoromethyl
-2-Cyclohexen-1-one and their acid addition
Salts and the like are exemplified. For example, when the substituent R6 is a heterocyclic group,
In some cases, (462) 4,4-dimethyl-2-furyl-2-cyclo
Hexen-1-one (463) 4,4-dimethyl-2-pyrrolyl-2-cycl
Rohexen-1-one (464) 4,4-dimethyl-2-thienyl-2-cycl
Rohexen-1-one (465) 4,4-dimethyl-2-isoxazolyl-
2-cyclohexen-1-one (466) 4,4-dimethyl-2-imidazolyl-2-
Cyclohexen-1-one (467) 4,4-dimethyl-2-thiazolyl-2-cy
Clohexen-1-one (468) 4,4-dimethyl-2-pyrrolidinyl-2-
Cyclohexen-1-one (469) 2-benzofuryl-4,4-dimethyl-2-
Cyclohexen-1-one (470) 2-benzothiazolyl-4,4-dimethyl-
2-cyclohexen-1-one (471) 2-Viridyl-4,4-dimethyl-2-cycl
Rohexen-1-one (472) 4,4-dimethyl-2-quinolyl-2-cycl
Rohexen-1-one (473) 4,4-dimethyl-2-pyrimidinyl-2-
Cyclohexen-1-one (474) 4,4-dimethyl-2-morpholinyl-2-
Cyclohexen-1-one and their acid addition salts and the like
Is exemplified. For example, R5 of formula (3b) and
R6 is a condensed polycyclic hydrocarbon compound or a condensed heterocyclic compound
(475) 5H-4-dimethyl-7-oxo-indene (476) 4-dimethyl-1-oxo-tetralin (477) 3H-4-dimethyl-1-oxo-anthra
Sene (478) 5H-4-dimethyl-7-oxo-benzothi
Offen (479) 5H-4-dimethyl-7-oxo-benzof
Orchid (480) 5H-4-dimethyl-7-oxo-indo-
(481) 6H-5-dimethyl-8-oxo-quinoline (482) 6H-5-dimethyl-8-oxo-quinoxa
Phosphorus (483) 6H-5-dimethyl-8-oxo-sinoline (484) 5H-5-dimethyl-8-oxo-1,4di
Thianophthalene (485) 3H-4-dimethyl-1-oxo-thiant
Examples include len and their acid addition salts.

The chemical formulas (1a) and (1b) of the present invention,
The compounds represented by (2), (3a) and (3b) can be synthesized from existing organic compounds by known organic synthesis methods, and can also be obtained from natural vegetable oils.
General formulas (1a), (1b), (2), (3a) (3
When the compound shown in b) or an acid addition salt thereof is used as an inhibitor or inhibitor of a function expressed by a multidimensional structure, it can be administered alone or in combination with a pharmaceutically acceptable carrier. However, it is not necessary to limit to the method shown in the present invention. The composition is determined by the administration route, administration schedule and the like.

The chemical formulas (1a) and (1b) of the present invention,
When the compounds represented by (2), (3a) and (3b) and the acid addition salts thereof are used as the above pharmaceuticals, pharmacologically acceptable additives (eg, carriers, excipients, diluents) And the like, and can be appropriately mixed with pharmaceutically necessary components to obtain a pharmaceutical composition in the form of powder, granules, tablets, capsules, injections and the like, and can be administered orally or parenterally. In addition, the effect can be expected in a gaseous state.

Chemical formulas (1a) and (1b) of the present invention:
The compounds of (2), (3a) and (3b) are administered orally in the form of tablets, capsules, powders, granules, liquids, and the like. Used in sterile form. When used in the form as described above, a solid or liquid non-toxic carrier may be included in the composition.

As an example of the solid carrier, a gelatin type capsule is usually used. The active ingredient is tableted, granulated, or powder-packed with or without an auxiliary agent. As the excipient used in these cases,
Water: Gelatin: Lactose, sugars such as glucose: Corn, wheat, rice, corn starch and other starches: Fatty acids such as stearic acid: Fatty bases such as calcium stearate and magnesium stearate: Talc: Vegetable oil: Stearyl alcohol, benzyl alcohol Alcohol such as: gum:
And polyalkylene glycols.

These capsules, tablets, granules and powders generally contain from 0.1 to 80% by weight, preferably from 0.1 to 60% by weight, of the active ingredient.
Water, physiological saline, dextrose or a similar saccharide solution, glycols such as ethylene glycol, propylene glycol, and polyethylene glycol, and polyoxyethylene sorbitan monooleate are preferred as the liquid carrier.

When administered parenterally by intramuscular injection, intravenous injection, or subcutaneous injection, the compounds represented by the general formulas (1a) and (1b):
The compounds (2), (3a) and (3b) are used as a sterile solution to which other solutes such as salt or glucose are added to make the solution isotonic. Suitable solvents for injection include sterile water, lidocaine hydrochloride solution (intramuscular injection), physiological saline, glucose, liquid for intravenous injection, electrolyte solution (for intravenous injection) and the like. In the case of these injections, the active ingredient is usually contained at 0.01 to 20% by weight, preferably 0.05 to 5% by weight.

In the case of liquids for oral administration, a suspension or syrup containing 0.01 to 20% by weight of the active ingredient is preferred. In this case, an aqueous excipient such as a flavor, syrup, or pharmaceutical micelle is used as the carrier.

When the composition of the present invention is formulated in combination with a pharmaceutically acceptable carrier, it may be formulated by a generally known method. Specifically, for example, an ointment, cream or emulsion may be prepared. In the case of production, the silver-carrying inorganic compound and the drug, and if necessary, at the time of melt mixing, emulsification or after emulsification, are added simultaneously, and an ointment
Creams or emulsions can be prepared. Also,
The drug and, if necessary, the halogen compound may be added first.

When the composition of the present invention is used as a sterilizing and disinfecting agent for living space, an effect can be obtained by using the composition alone or in combination with a necessary carrier. Specifically, it is made to directly or indirectly act on the solid surface by spraying, coating, and vaporizing. In addition, a sterilizing effect can be obtained by adding to the water of the humidifier or placing it on the circulation path of the air conditioner. Further, the composition of the present invention may be used as a depolymerizing agent, a surfactant improving agent, a reducing agent, a free radical scavenger, a desulfide agent, a phase change agent or a phase change improver, a micro phase separation structure improver, a plasticizer or a plasticity improver. , Copolymerizers or copolymer modifiers, polymerization regulators or polymerization regulators, stabilizers, antioxidants or antioxidants,
Amorphous or amorphous modifier, softener or softener, dye, paint, pigment or colorant modulator or modifier of fluorescence or excitation wavelength, physical property or function improvement of low molecular weight substance When used as an agent, a physical property or functional property improver of a polymer substance, or a physical property improver of a polymer composite material or a functional polymer composite material, the desired physical properties can be obtained by combining them alone or with a necessary carrier. Properties can be effectively controlled, suppressed, or expressed. Specifically, efficiency can be improved by adjusting the mixing ratio with the polymer substance, the stirring temperature, the amount of energy such as protons and electromagnetic waves, and the selection of transition metals.

[0063]

BEST MODE FOR CARRYING OUT THE INVENTION The chemical substance used in the present invention is not particularly limited, but is the simplest in organic chemistry, easy to synthesize, and is considered to be biologically relevant. Specifically, unless otherwise specified, one of the specific examples of the substituents R3, R4, R5, R
4,4-dimethyl-6-methylene-2-cyclohexen-1-one (hereinafter referred to as Yos) in which 6 is a hydrogen atom.
Hixol, referred to as Yoshixol) is synthesized to provide an example of its efficacy. The chemical formula of this composite is as follows:

[0064]

Embedded image

Yoshixol was synthesized by the following method. However, the present invention is not limited to the synthesis method exemplified here.

Under a stream of nitrogen, anhydrous tetrahydrofuran (1
Diisopropylamine (7.27 grams, 7 mmol, 99% pure, Aldrich, Milwaukee, Wis.) Is dissolved in 50 milliliters, 97% purity, Aldrich, Milwaukee, Wis., And cooled to -78 ° C. . This was mixed with n-butyl lithium (44.4 milliliters, 1.62 mol / liter, 7
0 mmol, Aldrich, Milwaukee, Wis.) Was added dropwise and the temperature was raised to 0 ° C. and stirred for about 1 hour. The solution of lithium diisopropylamide thus prepared was cooled again to −78 ° C., and 4,4-dimethyl-2-cyclohexen-1-one (7.5 g, 60 g
Mmol, 97% purity, Aldrich, Milwaukee, Wis.) Was added dropwise and stirred at this temperature for 1 hour before paraformaldehyde (5 grams, purity 97%).
%, Manufactured by Aldrich Co., Milwaukee, Wis.) On an oil bath while blowing in formaldehyde gas diluted with nitrogen gas. Thereafter, the mixture is stirred at −78 ° C. for 2 hours, left overnight at room temperature, and then made weakly acidic by adding 1N hydrochloric acid. The solvent is distilled off, extracted with ether, and dried over anhydrous sodium sulfate. Distill off ether
4-dimethyl-6-methylene-2-cyclohexene-1
-One and 4,4-dimethyl-6-hydroxymethyl-2
A mixture of -cyclohexen-1-one (7.03 grams) is obtained. This mixture (3 grams) was dissolved in benzene (80 milliliters) and a catalytic amount of paratoluenesulfonic anhydride (97% purity, manufactured by Aldrich, Milwaukee, WI) and Molecular Sieve 3A (about 4 grams, Milwaukee, WI). Of Aldrich Co., Ltd.), and the mixture is heated under reflux for 2 hours. The reaction solution is washed with a 1N aqueous sodium hydrogen carbonate solution and saturated saline, and then dried over anhydrous sodium sulfate. The benzene is distilled off to give crude 4,4-dimethyl-6-methylene-2-cyclohexen-1-one (2.35 grams) (68% overall yield). Pure is obtained by column chromatography or Kugelrohr distillation, but the yield is considerably reduced. In addition, about H1-NMR measurement, CDCl3 was used unless otherwise stated. Janssen, J., Luttke, W. has already published Chem. Ber., 115:
This is consistent with the spectrum data shown in 1234-1243 (1982). IR (neat): 1670 (C = O), 1620 (C = C) / cm.
(60MHz, CCL4), dl.15 (s.6H, C (CH3) 2), 2.57
(bs, 2H, CH2), 5.20, 5.93 (2m, 2H, CH2 =), 5.87
(d, J = 10, 1H, 2-H), 6.63 (d, J = 10Hz, 3-H).

<Stability Under Light Scattering> A stock solution of Yoshixol was placed under room light scattering with the glass tube sealed, and the coloration, viscosity and aroma degree after 6 months were observed. As a result, coloring, viscosity, and aromaticity were the same as those at the time of preparation.

Yoshixol and its derivatives and acid addition salts thereof are mixed in effective amounts. The dose varies depending on the route of administration, symptoms, body weight or age of the patient.
1-5 mg / kg body weight / day, especially 0.1-
It is desirable to administer 2 milligrams / kilogram body weight / day in one to several portions a day.

In the case of intravenous administration, 0.01-50
0 microgram / kilogram body weight / day, especially 5-10
It is desirable to administer 0 microgram / kilogram body weight / day in 1 to several times a day. In addition, when the purpose is disinfection and sterilization, the range is preferably 0.5 to 100 picomoles.

The effectiveness of the present invention as a suppressor and inhibitor of the function expressed by the multidimensional structure will be described sequentially using Yoshixol. The action effect and the underlying mechanism of action of the present invention will be described in the simplest manner. To illustrate this, Yoshixol was taken as a specific example, and the method that could explain the mechanism of action most simply or the method that was closest to the starting point in scientific methodologies that promoted specialized division in the history of medical science was selected. Therefore, the molecular expression function inhibitor described in claims 1 to 6 of the present invention is not restricted at all by the exemplified experimental methods and experimental reagents. Further, the present invention is configured so that the above biological effects can be explained and proposed in terms of physical properties. Play. However, the effectiveness of low-molecular substances and high-molecular substances expressed by the multi-dimensional structure of the present invention as regulators, inhibitors and inhibitors, as in the case of biological effects, was sequentially determined using Yoshixol. In order to explain the effects of the present invention and the underlying mechanism of action in the simplest way, Yoshixol was taken as a specific example, and the method which can confirm the effects simply was selected. Therefore, the molecular expression function inhibitor described in claims 1 to 11 of the present invention is not limited at all by the exemplified experimental method, experimental reagent, analysis method, and the like.

<Reaction with Ribose, Glycerin, Cellulose, Polyvinyl, etc.>
A microliter and 1 milliliter of each of a 1 molar concentration of ribose, glycerin, cellulose, and polyvinyl solution were stirred and mixed in a test tube, and the reaction was carried out at room temperature (28 ° C), heating (80 ° C), The fluidity and translucency in a cold temperature (4 ° C.) state were examined. The fluidity and translucency of each product were softer at normal temperature and increased in translucency, increased in hardness and clouded when cooled, and improved in fluidity and translucency in a heated condition. This result indicates that Yoshixol has polymerization and depolymerization effects.

<Effects on NADPH, Heme and Cytochrome C> Cytochrome C (415, 520 and 550 nm) before and after adding 4 microliters of Yoshixol to 1 milliliter of human defibrin serum, NA
Changes in DPH (340 nm), heme (415 nm), and aromatic amino acids (280 nm) were measured and evaluated using an infrared spectrophotometer. as a result,
No addition of yoshixol caused any quantitative or qualitative change in cytochrome C, heme, or NADPH, but the peak in the characteristic wavelength range of amino acids disappeared, and the lower wavelength range (aromatic amines) Moved to). This result indicates that yoshixol not only causes a dehydrogenation reaction but also has an action of forming a new aromatic amine by a reduction reaction or hydrogen bond. FIG. 1 shows that there is no bimodal peak rising at 280 nanometers, and that the peak before and after the peak is extremely high and monomodal.

<Effects of Human Serum, Fibrinogen, and Thrombin on Amino Acid Composition> Yoshixol (4 microliters) for each amino acid composition of 1 milliliter of human serum, 1 milliliter of fibrinogen and 1 milliliter of thrombin at a concentration of 160 milligrams / desiliter. Amino analysis was performed for the effect of.
The total amino acids in human serum treated with Yoshixol are reduced by 41% compared to before treatment, and the amino acid content ratios of each are different, and phosphoserine is about 20-fold from 7.2 pmol to 164.8 pmol. It was increasing near. In addition, although the total amino acid amount of fibrinogen was not changed by the treatment with yoshixol, glutamic acid and hydroxylserine which existed before the treatment disappeared, and histathionine increased more than 5-fold. Further, in thrombin, glutamic acid, taurine, methionine, aminoisobutyric acid, etc. which were not present before the treatment were newly formed. These results indicate that Yoshixol has a cross-linking action such as a disulfone reaction, and has an action of changing a protein or amino acid molecule to another amino acid molecular structure. FIG. 2 shows the embodiment.

<Effects on human blood coagulation and fibrin formation> Effect of Yoshixol (4 microliters) on human blood coagulation and fibrin formation when thrombin was added to fibrinogen Thromboelastogram (THROMBELASTOGRAPH, manufactured by Helige, Germany)
D). The degree of fibrin web formed in human blood agglutination was observed with a scanning electron microscope. Human blood started coagulation in 1-2 minutes, showed maximum coagulation in about 15 minutes, and then gradually decreased due to the action of the coagulation and fibrinolysis system. Upon addition of thrombin to fibrinogen, coagulation began immediately, reaching maximal aggregation in 5-6 minutes and maintaining this maximum over the following 6 hours observed (see FIG. 3a). However, yoshixol (4 microliters) for 0.4 milliliters of whole blood or fibrinogen (160 milligrams / desiliter)
When coagulation was added, the start time of coagulation of whole blood was extended to 4-5 minutes, the maximum coagulation time was 6-8 minutes, and the coagulation degree was 90%.
It remained the same level over the 6 hours observed, while still being suppressed (see FIG. 3b). When thrombin to which yoshixol was added was treated with fibrinogen, no agglutination was observed. Morphological observations on whole blood agglutination showed that religion formation of red blood cells and development of a fibrin network were remarkable in the untreated group, while religion formation and fibrin network were observed in the group treated with Yoshixol. Did not. These results indicate that Yoshixol has an extremely strong anticoagulant effect (antithrombin effect) and also has an anticoagulant fibrinolytic effect.

<Effects of trypsin and thrombin on protein three-dimensional structure and its function> Physiological action of trypsin (produced by Wako Pure Chemical Industries) as a proteolytic enzyme and thrombin (produced by Boehringer Mannheim Yamanouchi, which forms fibrin as a monomer from fibrinogen) )
When bovine albumin (Sigma, St. Louis, Mo.) and myoglobin (Sigma, St. Louis, Mo.) are treated with trypsin, the primary structure of each constituent protein is changed by the action of trypsin proteolytic enzyme, and human fibrinogen ( When thrombin was acted upon by Boehringer Mannheim Yamanouchi, the primary structure of the fibrinogen constituent protein was lost. Immediately after adding yoshixol (4 microliters) to trypsin and thrombin, even if each reaction product is electrophoresed, any change appears in the primary structure of the constituent proteins of the substances produced by each reaction. Did not. However, when trypsin and thrombin treated with Yoshixol (4 microliters) were allowed to act on bovine albumin, myoglobin and fibrinogen, the physiological effects of trypsin and thrombin were not observed (see FIG. 4). These results indicate that Yoshixol blocks the functional specificity of each substance not by altering the primary structure of trypsin and thrombin but by altering the multidimensional structure.

<Effects on ABO Blood Group Serum Antibody Function> Generally, an antibody consists of two light chains and two heavy chains.
It is also well known that it has a Y-shaped structure with a chain and maintains the basic construction of the structure by an SS bond. The ABO blood group serum antibody reaction is historically important in understanding the antigen-antibody reaction. In the present invention, human blood of type A, type B, and type O (4
(00 microliters), and using each blood group antiserum treated with Yoshixol (4 microliters), it was examined whether or not the ABO blood type could be determined by an ordinary method. In the untreated blood group antiserum, blood coagulation occurs when anti-A serum is added to human blood of type A, and blood coagulation occurs when anti-B serum is added to human blood of type B. Blood coagulation did not occur even with the antiserum, and normal ABO blood type determination was possible (see FIG. 5a). However, in the determination of ABO blood group using each blood group antiserum treated with Yoshixol (4 microliters), blood aggregation did not occur in any of the combinations, and the determination of ABO blood group was not possible. It was possible (see FIG. 5b). In addition, when the primary structure of the blood group antiserum was examined by electrophoresis as shown below, no change was observed in the protein primary structure of the antiserum due to the treatment with Yoshixol. These results indicate that Yoshixol suppresses or inhibits the function of an antibody expressed by a multidimensional structure that is higher than the primary structure of the antibody.

<Effects of Peptide Vazopressin and Insulin on Physiological Function> Vazopressin and insulin have physiological actions such as an increase in blood pressure and a decrease in blood glucose level. The effect of Yoshixol on the physiological function of these peptides was compared between a group in which each hormone was administered to rabbits in vivo without treatment with Yoshixol and a group in which each hormone was treated with Yoshixol. Intravenous administration of vasopressin (100 nanograms / kilogram, Sigma, St. Louis, Mo.) in the untreated group increased the maximal blood pressure by 15-2.
5 millimeters of mercury and lasted about 25 minutes. However, the increase in systolic blood pressure in the group in which yoshixol (4 microliters) was previously treated with vasopressin (100 nanograms / kilogram) was about 5 millimeters of mercury (see FIG. 6). When insulin (5 units / kilogram, manufactured by Novo, Denmark) was administered, the maximum decrease in blood glucose level was 45 mg / desiliter. (5 units / kilogram), the maximum blood glucose reduction was 12 milligrams / desiliter. The results show that yoshixol has the ability to inhibit or block the physiological functions of low-molecular-weight hormones and bioactive peptides that are composed of amino acid sequences and have functional specificity. Is shown.

<Effect on Primary Structure of Protein> The molecular weight composition of each protein when it was reacted with Yoshixol (4 microliters) with the following high molecular weight proteins (1 milliliter each in a 1 molar solution) and denatured by heating. Non-SDS Wide Page (Tefco)
Was evaluated by electrophoresis. The high molecular proteins used were human defibrin serum, bovine albumin, human fibrinogen, myoglobin (described above), blood group anti-A serum, and anti-B serum (Midori Cross). Even after treatment with Yoshixol, the molecular weight range of each polymer protein determined by electrophoresis was the same as the untreated polymer protein (see FIG. 7). These results indicate that Yoshixol does not directly change the primary structure of the biopolymer protein, because Yoshixol shows a migration pattern similar to that of a biopolymer protein.

<Antibacterial Effect> (Effect on Methicillin-Resistant Staphylococcus aureus (MRSA)) Collected and cultured from human sepsis patients and used for mammals (mouse, rat,
(A rabbit, a dog) and a strain causing a strong circulatory shock (proprietary strain SCK18). The medium used was a brain heart infusion agar medium. Using a concentration of Yoshixol (0.25 microliters to 10 microliters per milliliter of culture), the number of bacteria was 1
0 ⁸ 24 hours after culture in the conditions of 37 ° C., were growth and the number of colonies (CFU) was measured. The CFU in the untreated group was 2
The cells grew to 10 ¹⁰ for 4 hours, but the number of cells decreased to 10 ⁴ by treatment with 0.25 microliter of Yoshixol per milliliter of culture. Furthermore, the number of bacteria was reduced to 10 ² in the treatment with 2 microliters, and the number of bacteria was zero in the treatment with 10 microliters per milliliter of the culture solution (see FIG. 8a). This result indicates that Yoshixol is a gram-positive bacterium that has acquired resistance to other antibiotics, MRSA.
It also has a strong bactericidal action against. (Effect on Escherichia coli) The effect of Yoshixol was examined using Escherichia coli (E. coli strain W3110).
The medium used was a brain heart infusion agar medium. Using a concentration of Yoshixol (2 microliters per milliliter of culture solution), the number of colonies (CFU) that grew after culturing for 24 hours at 37 ° C. with 10 ⁸ cells was measured. CFU in the untreated group was 10
^The number of bacteria grew to ¹⁰ , but in the treatment with 2 microliters of Yoshixol, the number of bacteria became zero one hour after the treatment, and was zero even after 24 hours (see FIG. 8b). This result indicates that Yoshixol has an extremely strong bactericidal action against Gram-negative bacteria Escherichia coli.

(Effect on Mycobacterium) The effect of Yoshixol was examined using an atypical mycobacterium (Mycobacterium Rapid Grower). The medium used was a heart infusion agar medium, and the effect was determined by the degree of the growth inhibition circle. An inhibition circle was formed at 0.2 microliter of Yoshixol per milliliter of the culture solution, and an inhibition circle of 22 millimeter was formed at 2 microliter. This grade is
This shows that Yoshixol has an extremely strong bactericidal action against atypical mycobacteria.

(About antifungal effect) In order to examine the effect of 2 microliters of Yoshixol per 1 milliliter of culture solution on fungi, a study was carried out using Trichophyton (Candida Albicans). The medium used was 5 milliliters of Sabouraud's medium and the number of Trichophyton was (10 ⁶ CFU / milliliter). CFU in the untreated group showed no change even after 3 hours, and showed an increasing trend. On the other hand, in the yoshixol-treated group, the CFU became zero after 1 hour and was also zero after 3 hours (see FIG. 8c). This result indicates that Yoshixol has strong antifungal activity.

The effect of Yoshixol on such bacteria showed an interesting finding in its dead form. M
In the RSA, each bacterial colony is separated from each other, and the surface structure of each bacterium is a scanning electron microscope image showing the appearance of small granules of about 10-50 nanometers exploding from inside the cell (Fig. 9). , And finally, small particles such as fireworks show concentrically discrete states. Such a finding was also observed in a transmission electron microscope image. Observation of Escherichia coli with a scanning electron microscope revealed that the surface was composed of a large number of particles of about 10 to 50 nanometers, the surface was not smooth, and bulges appeared (see FIG. 10). Of course, in this case as well, the adherent aggregates of the cells had disappeared, and the final structure had been made into fine particles. The same change was observed in acid-fast bacteria (see FIG. 11) and white bacteria (see FIG. 12). In Pseudomonas aeruginosa, no conjugation between the bacteria was observed, and it was observed that the cells swelled like a balloon and burst, and the bacterial structure became fine particles (see FIG. 13). This shows that Yoshixol has antibacterial and bactericidal effects,
Unlike the mechanism of action such as denaturation, necrosis, and coagulation with conventional antimicrobial bactericides, the killing mechanism prevents bacterial conjugation and, depending on the molecular composition involved in the morphogenesis of each bacterial species, It is characterized in that microbial components are formed into fine particles while showing the eruptive structure, explosive structure, and balloon structure. Such morphological findings are consistent with the morphological features of zeoosis and apoptosis that have been pointed out so far. This indicates that it can be applied as an effective antibacterial fungicide without the appearance of mutation and drug resistance.

<About the disinfecting and disinfecting effects> In order to examine the antibacterial effect of the vaporizable component of Yoshixol, the antibacterial effect of mesitillin-resistant Staphylococcus aureus, Escherichia coli,
Using the same strains as Trichophyton and Mycobacterium, respectively, the antibacterial action of Yoshixol of the present invention at a concentration of 50 microliters was examined on ordinary agar, BHI medium, HI medium, and Sabouraud medium. The filter paper disk soaked with the sample was placed on the bottom of a Petri dish, and the medium in which each bacterium was inoculated was used as a ceiling so that the sample did not come into contact with the medium. After 24 hours, the growth state of each bacterium was observed. As a result, at the constant temperature of 37 ° C., the growth of each of the above-mentioned bacteria was not recognized at all even by direct contact diffusion but indirect action of the vaporizable component of Yoshixol from the bottom of the petri dish at 37 ° C. From these results, it was confirmed that the volatile component of Yoshixol of the present invention acts as a strong sterilizing and disinfecting agent even in any place of the living space through the atmosphere.

<Regarding the production effect of nitric oxide> Recently, it is of interest that nitric oxide (NO) generated in the living body has an anticancer effect, a bactericidal effect, a suppression of antigen-antibody reaction, a circulatory system effect, and the like. Is held. NG-Methyl-L-Argi, a NO generation inhibitor, was used to determine the extent to which NO was involved in the effects of yoshixol on the blood coagulation test, fibrin formation test, and antimicrobial test against MRSA.
We examined using nine (NMLA). As a result, when 1 mol (NMLA, 4 microliters) was additionally added, the blood coagulation action, fibrin formation action, and antibacterial action against MRSA were all reduced by 10-20% compared to the single effect of Yoshixol. . These results indicate that Yoshixol is also a NO producing agent, and NO generated by Yoshixol also inhibits the antibacterial, anticancer, bactericidal, antiviral, and antigen-antibody reactions described in the present invention. It can be said that the action of Yoshixol shown in the present invention has a synergistic effect of about 10 to 20% with respect to the action and the like.

[0085] Phage solution was adjusted to <effect on bacteriophage> 1 milliliter per about 10 ⁷ (E7
9 double-stranded DNA phage) To 1 milliliter, add 4 microliters of Yoshixol and mix well. 5, 1
After 0, 20, and 30 minutes, take 10 microliters of this and quickly add to 10 milliliters of broth for dilution. Take 100 microliters from the phage dilution and place into a small tube of warm upper agar. To this is added 100 microliters of the indicator bacterial solution (Pseudomonas aeruginosa) cultured overnight, and mixed well. Pour the contents of the small test tube onto the agar plate and spread the upper agar evenly while turning the plate quickly. Leave it for about 10 minutes, and put it in a 37 ° C spatula when the layered agar has hardened sufficiently. After overnight culture, the number of plaques was counted. As a result, the number of plaques decreased to 33% in the 5-minute treatment group and to 15.6% in the 10- and 15-minute treatment groups, respectively, compared to the untreated group to which Yoshixol was not added. 20 more
No plaque formation was observed after more than one minute treatment (FIG. 1).
4).

<Antiviral Effect> In order to examine the effect on the virus, Escherichia coli bacteriophage double-stranded DNA, single-stranded DNA, and mRNA were treated with 4 milliliters of 1 milliliter each of 1 molar molar concentration of yoshixol. What is not treated, scanning type,
Each structural change was observed with a transmission electron microscope. In addition, in a usual bacteriological method, bacteriophage double-stranded DNA, single-stranded DNA, and 1 milliliter of mRNA at a molar concentration of 1 milliliter were treated with 4 microliters of Yoshixol and those not treated with Escherichia coli, respectively.
The degree of growth of each inoculated E. coli and the morphological changes (scanning and transmission electron microscope) of each inoculated E. coli were observed. As a result, the characteristic helical structure and complex multidimensional structural form of E. coli bacteriophage double-stranded DNA, single-stranded DNA, and mRNA have become simple structural forms when treated with Yoshixol. The distance between the chain structures forming each was remarkable. When the amino acid sequence (sequencing) of this single-stranded DNA was examined, the original amino acid sequence was changed when Yoshixol was treated. In addition, double-stranded DNA, single-stranded DNA and mRNA of bacteriophage were inoculated with Escherichia coli, and the degree of growth of each inoculated Escherichia coli was similar to that of the mother bacterium before removing the bacteriophage. Yoshixol-treated double-stranded DNA, single-stranded DNA and m
No growth in E. coli inoculated with RNA was observed. Furthermore, when these Escherichia coli were observed morphologically (scanning and transmission electron microscopy), in the untreated group, adhesion on the bacterial surface and presence in the bacteria were observed, whereas Yoshixol was treated. Was not recognized. Furthermore, chicken myeloblastosis virus (AMV) reverse transcriptase (manufactured by Gibco, Inc., Getelberg, MD)
The effect of Yoshixol on was investigated. Using 25 units of BRL AMV reverse transcriptase for 5 micrograms of RNA, the amount of cDNA synthesized with and without 0.01 microliter treatment of Yoshixol was amplified by PCR and measured. As a result, when Yoshixol was not treated, the expected amount of cDNA was produced. However, when Yoshixol was treated, cDNA synthesis was suppressed to about 10% of the expected amount (see FIG. 15). The results show that Yoshixol has the ability to destroy the virus, prevent the virus from adhering to the parasitic cells, change the multidimensional structure of the virus's own gene, and suppress the ability of the virus to proliferate in the parasitic cells. Indicates that you have.

<Regarding Anticancer Effect> Cell adhesion factor plays an important role in cancer metastasis and cancer cell proliferation. The intercellular structure of cultured kerato cells has been used to study intercellular adhesion factors. In the present invention, the intercellular structure and cell morphology of kerato cells after 5 days of secondary culture using kerato cells separated and cultured from human skin are measured with a phase-contrast microscope (Olympus, IMT-2), transmission type (JEOL Ltd.). Made by JEM 12
00, EXII) and scanning type (JSM-6000, manufactured by JEOL Ltd.)
F) Examination by electron microscope. In the untreated group, the cultured cells were systematically proliferating over the entire surface like an Ishigaki, some cells showed a bifission image, and intracellular organelles were also found normally. The cells were filled with extracellular matrix without any intercellular connections or blanks (see FIGS. 16a and 17a). In contrast, Yoshixol 4
In the treatment group in which microliters were added to the culture solution, the cultured cells exhibited various irregular morphologies, and are said to form cell membranes and organelles (Golgi apparatus, rough endoplasmic reticulum, and cytoskeleton) Tubulin, etc.) were destroyed to various extents, the intercellular connections were irregularly detached, and the extracellular matrix was irregularly dispersed from the cells as punctates of various sizes. (See FIGS. 16b, 17b). Cultured HeLa cells, a type of cancer cells (American
Similar effects were observed in Type Culture Collection, ATCC No. CCL2, Maryland, USA, see FIG. 18) and mouse cultured hepatocellular carcinoma cells. These results indicate that Yoshixol of the present invention has an effect of inhibiting cell division and proliferation, inhibiting cell-cell adhesion, and inhibiting division and proliferation of cancer cells and further metastasis. Furthermore, from the morphological findings, the cell destruction image caused by Yoshixol is a morphological image far from the necrotic form among the cell deaths conventionally pointed out (see FIG. 19), and is a morphological image called spontaneous death or apoptosis. (Such morphological images were also observed in the various bacteria described above). The particulate matter of this fragmented cell composition (10-100 nanometers) easily undergoes phagocytosis of macrophages, lymphocytes, etc., and is a biological phenomenon that is performed physiologically and naturally in living organisms. Shows that these particulates are incorporated into recycling.

<About organ tissue preservation effect> 4 microliters of Yoshixol was placed in a vacuum blood collection test tube having a volume of 10 milliliters, and blood 5 collected from a human elbow vein was further added.
The milliliter was immediately placed in the vacuum test tube containing Yoshixol, mixed gently, and stored at room temperature for 30 minutes, 1 hour, and 1 month, and the morphological change of blood red blood cells at each time point was measured. The morphological changes of blood erythrocytes without Yoshixol treatment were examined by transmission and scanning electron microscopy. When Yoshixol was not treated, blood clots were observed 30 minutes later, and after 1 month, the normal form of blood red blood cells was not observed and remained as a solid destructive object. However, the erythrocytes of the blood treated with Yoshixol were not clotted by fibrin,
As a whole, there are many lipocytes (stomatocytes), and some echinocytes are said to appear when pyruvate kinase deficiency or phosphoglycerate deficiency occurs.
However, cell membranes and intracellular organelles were preserved for one month (see FIG. 20). This indicates that blood treated with Yoshixol can be preserved even when stored at room temperature, and that it is also effective as an organ tissue preservative as a functional unit of other living organisms. ing.

<Regarding the Inhibitory Effect of Xenograft Skin Transplantation on the Rejection Effect> The whole skin layer (3 cm in diameter) on the back of a rabbit was transplanted to the back of a mongrel dog as a transplant, When the whole skin layer (3 cm in diameter) on the back of a dog was transplanted as a graft into the skin on the back of a rabbit, the engraftment state of the graft was observed visually and histologically for 3 months each. Observed. First, each graft was prepared by adding 10 microliters of Yoshixol to 5 milliliters of physiological saline (polyoxyethylene (20)
Sorbitan monooleate 1, manufactured by Wako Pure Chemical Industries, Ltd. <I
CI company, equivalent to Tween 80>, 2 ml of physiological saline was added to 2 ml, and a solution obtained by adding 10 ml of yoshixol to this solution was used. It was sutured and transplanted to the recipient. Then, for 3 days after the transplantation, 10 microliters of Yoshixol was sprayed on the wound. The graft treated as a control treated only with physiological saline began exfoliation 3-5 days after the transplantation, and the wound area was finally dirty due to inflammatory reaction and tissue necrosis of the graft. One week later, it was completely mummified, and after 10 days, it completely fell off. After three months, the implant healed with the self-renewed skin of each recipient. On the other hand, when the graft is immersed in the yoshixol solution, the treated graft becomes soft and thick, and it is very easy to insert a suture needle.The graft does not peel off and fall off even after 2 weeks of transplantation, and the inflammatory reaction is suppressed. I was After one month, the wound did not show any inflammatory tissue reaction and appeared to be covered with a glossy collagen film or chitin-like substance, and healed so that the boundary with the recipient's skin could not be discerned (The upper part of FIG. 21). This means that during transplantation of tissue and organs, including xenogeneic skin, the donor tissue or organ is pre-treated with Yoshixol,
In addition to suppressing rejection associated with transplantation, it also suppresses secondary complications due to infection of transplanted tissues and organs,
It shows that the transplantation effect is enhanced. The whole skin layer (3 cm in diameter) of a rabbit was used as a graft, and the graft was sewn to the skin of the back of a recipient dog without any treatment. Then, Yoshixol (10 microliters per body weight) was added to the skin. By implanting intravenously for a week (once a day), the engraftment status of the graft was observed for 3 months or more. Of course, conventional drugs such as antibiotics and immunosuppressants are not used in combination. The graft adhered to the dog's back for more than one month without causing rejection or bacterial infection. After three months, the surface of the graft was peeled off to remove the thin film. No epithelium was observed, but good epithelial formation was grossly and histologically observed (FIG. 21, lower panel). By such treatment with intravenous administration of Yoshixol, all adult mongrel dogs became more energized and their appetite, behavior, etc. became younger than those before treatment. This means that, in addition to the improvement of the general condition of the animal treated with intravenous administration of yoshixol, the rejection associated with transplantation can be suppressed, and at the same time, infection can be suppressed and the transplantation effect can be enhanced. Is shown.

<Thrombolytic Effect> To examine the dissolving effect of Yoshixol on thrombus, about 1 milliliter of human and dog blood was immediately collected on a glass syringe and transferred to a petri dish (Greiner). ,
A phase contrast microscope (IMT-2, manufactured by Olympus Corporation) was used to confirm that thrombus formation and coin formation occurred, and 1 microliter of Yoshixol was sampled when thrombus was formed so that the entire visual field could not be identified as individual red blood cells. , The dissolution process of the formed thrombus is observed under a microscope, and recorded and recorded through a color video camera (CCD-IRIS, manufactured by Sony Corporation). The fluidization phenomenon was analyzed and studied. Immediately after the addition of Yoshixol, the thrombus that had formed a single mass became individualized into individual blood cells through a process completely opposite to the process of its formation,
Surprisingly, the red blood cells disperse from the thrombus while regaining their original morphology, no individual red blood cells are lysed by ruptured rupture, and individual positions disturb the position of other blood cells. But constantly moving on a certain order (see FIG. 22). When this process was analyzed by observation under a microscope or by dynamic image processing, it showed a behavior as a dissipative structure, similar to a liquefaction phenomenon or a gelation phenomenon of a solid. This indicates that thrombus formation can be thermodynamically interpreted in blood or serum, which is a typical example of non-Newtonian physical properties, and that the solidified physiological role of blood as the original blood In addition to showing the potential for yoshixol to improve circulatory disorders, a condition in which (flow characteristics) are impaired, it also shows that yoshixol can be applied not only as an inhibitor or inhibitor of thrombus formation but also as a thrombolytic agent. Results.

<Regarding Metabolic Improving Effect> Changes in Blood Chemical Components and Blood Cell Components of Yoshixol In order to examine the metabolic improving effect of oral administration of yoshixol, beagle dogs were given 100 g of 10 microliters of yoshixol per body weight in beagle dogs. (Dog Food <Beef>, New Zealand, imported from Daiei), which is a nutritional food that meets the standards of the Pet Food Fair Trade Council. Oral administration was continued for one week, and red blood cell count, white blood cell count, platelet count, total protein in serum (Burelet method), albumin (BCG) before administration, 1 day after administration, 3 days after administration, 1 day after administration, and 7 days after administration.
Method), urea nitrogen (GLDH-UV method), creatinine (enzymatic method), glucose (GDH method), total bilirubin (enzymatic method), GOT and GPT (JSCC-compliant method), TT
T and ZTT (standard procedure for liver function research group), cholinesterase (DMBT method), total cholesterol (PDO enzyme method), triglyceride (PDO enzyme method), uric acid (uricase PDO method), serum iron (nitroso PSAP method), creatine Phosphokines (SCC-compliant method), sodium, potassium and chlor (ISE dilution method), inorganic phosphorus (enzyme-UV method), and calcium (OCPC method) were measured. As a result, no change was observed in the red blood cell count, white blood cell count, and platelet count. No changes were observed in total bilirubin, GOT, GPT, TTT, ZTT, cholinesterase, serum iron, sodium, potassium and chlor, inorganic phosphorus, and calcium. Total protein increased 3 days after administration of Yoshixol, and at 1 week after administration, was at the same level as the untreated group.
Although albumin did not change (see FIG. 23), the albumin / globulin ratio increased 3 days after administration (FIG. 2).
4 See upper column), production of globulin was estimated. Also, the blood glucose level in the control group increased by 15% 3 days after ingestion of the feed, but no increase in blood glucose was observed in the yoshixol-administered group, and no rebound appeared 1 week after discontinuation of the administration (FIG. 24). See the bottom). There was no difference in total cholesterol and triglyceride between the control group and the yoshixol-administered group (see FIG. 25). However, residual nitrogen and creatinine showed lower values (70-80% of control) than one day after administration (see FIG. 26), and uric acid also maintained lower values during the administration period. Furthermore, creatinine phosphokines decreased (see FIG. 27), and enzymes such as γ-GPT, GOT, and GPT also decreased. Also, no abnormal values were shown in TTT, ZTT, and the like. No abnormal behavior, diarrhea, vomiting, bloody stool, etc. were observed during the course of Yoshixol administration and for one week after the administration, and neither weight loss nor appetite loss was observed. In addition, beagle dogs received 3 microliters of body weight per body weight of yoshixol for 1 month, and when observed for 3 months, similar effects can be obtained despite time delays and differences. did it. The results showed that oral administration of Yoshixol showed that carbohydrates, lipids,
The effect of improving nutrition and metabolism of proteins and the like can be expected even orally, and it can be applied not only as a therapeutic agent for diabetes, kidney disease, liver disease, hypoproteinemia, etc., but also as a cell function protectant It is the result which showed.

<Effect of Softening of Skin> The whole skin of rabbits and dogs was treated with 5 ml of physiological saline and Yoshixol 1
0 microliter (polyoxyethylene (20) sorbitan monooleate 1, manufactured by Wako Pure Chemical Industries, Ltd. <ICI
(Equivalent to Tween 80), add 88 ml of physiological saline to 2 ml, and use a solution obtained by adding 10 ml of yoshixol to this solution). The skin pieces are moist and soft and thick, can easily insert and penetrate the needle, and histologically, no structural destruction is observed,
Hematoxylin and eosin staining of the treated skin compared to that of the control saline showed the tissue as if it were a specimen made from fresher material. In addition, similar findings were found in refrigerated storage at 4 ° C and frozen storage and thawing at 20 ° C for one month. These results indicate that Yoshixol can be applied as a softening agent for tissues and substances having many fibrous structures such as skin, and that it can also be used as an organ preservative.

<Suppressive Effect on Sperm Flagellar Movement> Sperm of Wagyu beef cattle preserved in liquid nitrogen for the purpose of examining the effect of yoshixol on sperm flagellar movement (breed bull name: Shinmori Hide <Registration number, Zenwa Kurodai No. 1114, Lot No. 84Y28>) was thawed at a low temperature of 35 degrees Celsius, and after thawing, about 1 milliliter thereof was transferred onto a Petri dish (manufactured by Greiner), and was then subjected to a phase-contrast microscope (IMT-2, manufactured by Olympus). Observe the changes in flagellar movements, and record and record them via a color video camera (CCD-IRIS, manufactured by Sony Corporation), and use your own dynamic image analyzer to determine the wave cycle of the flagellar movements and the direction and speed of sperm movement. The analysis was considered.
In normal sperm, regular flagellar movements cause the head to move in the desired direction at a rate of 0.3-1.5 micrometers per second, while addition of 1 microliter of Yoshixol immediately stops flagellar movements and sperm movement. The movement speed has become zero. At this time, although the flagellar movement was stopped, the rotational movement of the head with the fulcrum as the fulcrum was observed for several tens of seconds. This result indicates that Yoshixol is strongly related to physical and functional properties related to sperm flagellar movement (hydrolysis reaction of contractile proteins such as actin and ATP as an energy source).
It shows that it is greatly related to the movement and information transmission of prokaryotes and eukaryotes, and also to the dynamic behavior that is the essence of living organisms. In addition, regarding the cell motility, proteins that cause motility are aggregated to form fine fibers and microtubules. Manufactured by JEM1200, E
XII) and a scanning type (JSM-6, manufactured by JEOL Ltd.)
000F) studied by electron microscope. 9+ for normal flagella
The outer surface, consisting of the two basic structures, is surrounded by a cell membrane, and the axle, which is a structure related to movement, is found inside. Nine double tubes (peripheral small tubes) were more ordered, and it was observed that the surface involved in the movement formed a smooth, orderly donut-shaped ring formation at the part involved in the movement. However, in spermatozoa treated with Yoshixol, there is no special change in the whole morphology of sperm, but when magnifying the magnification and observing the surface structure of the flagella, the sperm adheres so that particles of 10-30 nanometers are ejected. No donut-shaped ring formation was observed in a portion considered to be involved in the movement, and the adhesion of the fine particles was remarkable (see FIG. 28). In addition, transmission electron microscopy of the flagella maintains a basic image of the fiber-building unit, while the lack of continuity of the membrane surrounding the surface fibers and the fiber unit (muscle) No regular arrangement structure of fibrils and the like was observed, and the appearance of a high-density aggregate structure was observed (see FIG. 29). No significant morphological changes were observed in the surface structure and internal structure of the sperm head as compared with the flagella. These results indicate that the role of cytoskeleton in the dimerization of actin and tubulin (cancer, metastasis, cell death, etc.) is concerned with the control of sperm motility. The results are of course not only applicable to contraceptives that can be used, but also to applications to, for example, inhibitors of bacterial growth of prokaryotes, antibacterial agents, anticancer agents against eukaryotes, and the like. It also shows that it can be applied as a suppressor or regulator of the functional expression effect based on the polymerization reaction system related to cell adhesion, morphogenesis of living organisms, and each life phenomenon (including immune response). .

<Regarding Conversion Effect of Physical Properties of Polymer> The physical properties of the polymer (changes in gloss and gloss, accuracy of boundaries in mold formation, surface smoothness and uniformity, transparency, fineness, and amount of Change), etc., how 100% per 100 grams of each of the following substances
Add the microliter of Yoshixol, heat it until it is dissolved in the water tank, pour each solution into the caries filling tooth model by dental treatment, cool it down, take it out from the mold in a solid state, Observation was performed with a magnifying loupe of 5 times. All of the following substances added with Yoshixol,
A decrease in the melting point was observed as compared with the case where no additive was added. Octadecanol (Wako Pure Chemical Industries, Osaka) had better gloss and luster and sharper boundaries. Stearic acid (Wako Pure Chemical Industries, Osaka) is characterized by the appearance of smoothness and fineness and transparency, and lauric acid (Wako Pure Chemical Industries, Osaka) is characterized by appearance of smoothness and transparency, dodecanol (lauryl alcohol) (Wako Pure Chemical Industries, Osaka) was extremely soluble and could not maintain the casting form at room temperature. For palmitic acid (Wako Pure Chemical Industries, Osaka), a soft feeling appears, and for myristic acid (Wako Pure Chemical Industries, Osaka), the sharpness and uniformity of the boundaries are improved. For tetradecanol (myristyl alcohol) (Wako Pure Chemical Industries, Osaka) ) Was similar. Hexadecanol (Wako Pure Chemical Industries, Osaka) is characterized by reduced fineness and transparency. In decanoic acid (Wako Pure Chemical Industries, Osaka), glossiness and sharpness of the boundary appeared, but the surface was found to be rough with small bumps.
Polyethylene glycol 1000 (Wako Pure Chemical Industries, Osaka) has poor boundary sharpness and smoothness, and polyethylene glycol 1540 (Wako Pure Chemical Industries, Osaka) has good smoothness, uniformity, and transparency. With Wako Pure Chemical Industries, Osaka), polyethylene glycol 4000 (Wako Pure Chemical Industries, Osaka), and polyethylene glycol 6000 (Wako Pure Chemical Industries, Osaka), an effect of enhancing fineness, transparency and expandability was observed. Furthermore, N-isopropylacrylamide (manufactured by Aldrich of Milwaukee, Wis.) Showed gloss, sharpness of boundary, uniformity of surface, transparency and fineness. In addition, in order to examine the effect of Yoshixol on a high-molecular polymer, as one specific example, acrylate-based polymers, ie, lauryl methacrylate 471, methyl methacrylate 48, ethyl methacrylate 12
6. Using a standard product of isobutyl methacrylate 140 and butyl methacrylate 320 (polymer kit, acrylate standard product 18336-9, manufactured by Aldrich of Milwaukee, Wis.) At room temperature. When 150 microliters of yoshixol was added to 1 gram of each acrylate-based polymer, all the substances became liquid and transparent like glass, the powdery and crystalline structures disappeared, and changed to a uniform substance. Further addition of 100 microliters of yoshixol immediately increased the flowability of lauryl methacrylate 471, two weeks later developed flow stickiness, and one month later the amount was reduced when yoshixol was not added. In contrast, in the group to which yoshixol was added, it was observed that the liquid component and the translucent solid were separated. With methyl methacrylate 48, the powdery state of Sarasara disappears immediately after the addition, the fluidity increases in a uniform rice cake-like form, and after 2 weeks, it becomes a transparent paste and adheres to the tube wall. That amount was increasing. Even with ethyl methacrylate 126, the powdery form of Sarasara disappears immediately after the addition of Yoshixol, and stickiness appears in a lump, and after 2 weeks it becomes a paste and adheres to the tube wall, and after one month the transparency further increases Was. Even with isobutyl methacrylate 140, the powdery state disappears, and the appearance of stickiness appears as a lump of transparency. After 2 weeks, the viscosity increases further, and the paste becomes a paste and adheres to the tube wall. The unreacted portion had a color tone in a powdery state before the treatment. In the case of butyl methacrylate 320, the powdery state disappears, and the adhesiveness increases due to bulk transparency, and the paste adheres to the tube wall in a paste form. After two weeks, there is a difference in transparency depending on the adhered state. The part had a glassy transparency, and after one month, it had changed to a transparent and uniform lump of glass-like substance with less tackiness, and the amount thereof had increased.

Standard products of other acrylate polymers such as poly-2-ethylhexyl acrylate, polymethyl acrylate, polyoctadecyl acrylate, polyethyl acrylate, and polybutyl acrylate (polymer kit, polyacrylate standard product 18338-5,
Aldrich, Milwaukee, Wisconsin)
Was used to observe changes in physical properties when 200 microliters of Yoshixol was added at room temperature. With poly-2-ethylhexyl acrylate, the flowability increased immediately after the addition of yoshixol, but the color did not change. Two weeks later, the fluidity increased further, the volume increased, and the light refraction changed. One month later, the fluidity increased further, and the volume almost doubled. . Even with polymethyl acrylate, an increase in fluidity and an increase in volume were observed, the light transmittance was improved, and after one month, the fluidity was further enhanced, and the capacity was increased by about 2-3 times. In the case of polyoctadecyl acrylate, the powdery state of the smoothness disappeared and it became a uniform mass. In the case of polyethyl acrylate, the flowability was remarkably increased, the liquid state was increased, and the volume was significantly increased. After one month, the flowability was further increased, and the volume was further increased nearly three times. Even with polybutyl acrylate, the fluidity increased with the addition of Yoshixol. After 2 weeks, the fluidity further increased to become liquid, and after 1 month, the fluidity increased and the capacity further increased nearly 2-3 times. I was Another polymer, namely polydimethylsiloxane,
Polyvinyl acetate, polymethyl methacrylate,
50 each of standard products of polyvinyl chloride and polycarbonate resin (Polymer Kit 18337-7, manufactured by Aldrich of Milwaukee, WI)
Using 0 milligrams, changes in physical properties were observed when 200 microliters of Yoshixol was added at room temperature. Immediately after the addition of Yoshixol to the polydimethylsiloxane, it was difficult to mix it as a liquid supernatant, but two weeks later, the fluidity and volume increased, and one month later, the viscosity increased further. And the amount was increasing, but the light transmission was decreasing. Even in polyvinyl acetate, the viscosity increased and it became attached to the tube wall, and a liquid component was observed below. However, after 2 weeks, the liquid component disappeared and became a transparent viscous solution to enhance transparency. After one month, the transparency finally became constant. In the case of polymethyl methacrylate, immediately after the addition of yoshixol, a uniform and transparent state was obtained, but after one month, it was crystalline and cloudy glass. In the case of polyvinyl chloride, the powdery state of the smoothness disappeared and it became a fine non-uniform mass, but no remarkable change was observed when left at room temperature. With polycarbonate resin, immediately after the addition of yoshixol, the granularity of the silky particles disappeared, stickiness appeared, transparency decreased after 2 weeks, and no reflected light was observed in the form of cloudy glass. Was observed to increase. Also, 200 microliters of Yoshixol was added to 200 milligrams of N-isopropyl acrylamide (Aldrich, Milwaukee, Wis.), And immediately afterwards, Yoshixol penetrated into the crystal as if the sugar was immersed in water.
After -3 minutes, the formation of a transparent substance started from the lower layer without heat generation or gas generation. After 4 hours from the addition, the substance became a sherbet-like form. Was.

Other polyethylene polymers include polyethylene glycol phenyl ether acrylate (manufactured by Aldrich, Milwaukee, Wis.), Polyethylene 125,000 (manufactured by Aldrich, Milwaukee, Wis.), And polyethylene low density (manufactured by Milwaukee, Wis.). Aldrich (manufactured by Aldrich Co.) was added to 100 mg of Yoshixol and observed at room temperature.
In the case of polyethylene glycol phenyl ether acrylate, an increase in fluidity was observed immediately after the addition, and it was observed that the amount increased and the light transmittance increased with time. In the case of polyethylene 125,000, adhesion between the particles started, and two weeks later, although the shape of the particles remained, it was observed that each of the particles adhered. Further, in the case of low density polyethylene, the particle units became larger from the smooth state. For the purpose of studying the effect of Yoshixol on polystyrene-based polymers, polystyrene 45,000 (manufactured by Aldrich, Milwaukee, Wis.), Polystyrene 280,000 (manufactured by Aldrich, Milwaukee, Wis.), And polystyrene standard (milwaukee, Wis.) (Aldrich Co., Ltd.) of 200 milligrams. Polystyrene 45,000
Add 100 microliters of Yoshixol to
45,000 polystyrene loose particles disappeared and became sticky and became a glassy transparent substance. No crystal structure was observed, and the state was the same even after one month. Even with polystyrene 280,000, the smoothness of the particles disappeared and the particle structure disappeared with the appearance of tackiness, and the glass became glassy and the light transmittance was extremely improved, and it became transparent glass-like. Similar changes in physical properties were also observed in polystyrene standards. 200 mg of hydroxylated polyvinyl alcohol (Aldrich, Milwaukee, Wis.) Was added to Yoshixol 100
The addition of the microliter changed the powdery form of the rust from a rough powder to a fine and uneven fragile lump, and after a lapse of time, the powder disappeared and became powdery again, but easily adhered to the tube wall. These results indicate that Yoshixol can improve the physical properties of the polymer and modify and improve the function expressed by the structure of the polymer.

Further, in the above-mentioned examinations, since the description is mainly based on subjective macroscopic observations, the validity of the macroscopic observations was examined by further examining the microscopic observation results of the change in the physical properties of each polymer. The change in physical properties of the polymer was examined with a differential scanning calorimeter (DSC-50, manufactured by Shimadzu Corporation). In the differential scanning calorimeter, the signal of the temperature deviation ΔT from the reference material (this measurement used alumina) is displayed as a curve with respect to time or sample temperature, and the area of the portion surrounded by the baseline and the peak is shown. Is proportional to the heat energy required for melting. That is, under constant pressure conditions, the thermal energy supplied to the sample coincides with the increase in the enthalpy of the sample, so that there is a discontinuous change in the enthalpy with respect to the temperature as in the case of melting of the sample or the first-order phase transition of the crystal. In the physical property change phenomenon, the effect of decreasing the enthalpy of the sample (in other words, the decrease in the heat capacity of the sample, the decrease in the compressibility, etc.) is displayed as a downward peak, and the peak area is considered to be the amount of jump of the enthalpy. No change was observed in the change in the heat capacity of the differential scanning calorimeter with stearic acid and lauric acid, and a slight decrease in the melting point was observed with myristic acid and palmitic acid (100 microliters of yoshixol per 100 grams, see FIG. 30). However, there was no significant change in heat capacity. On the other hand, polyethylene glycol 1000 (100 g of Yoshixol 100
In microliters, the reaction of decreasing the enthalpy at 20-60 ° C in the control disappeared by the addition of yoshixol, and a phase in which the change in calorific value became a reaction of decreasing the enthalpy between 120-160 ° C was observed (see FIG. 31). ). With polyethylene glycol 4000, a decrease in the melting point was observed. In polystyrene 280,000 (200 micrograms of Yoshixol 100 microliters), the addition of Yoshixol produced a reaction phase of decreasing enthalpy from about 30 ° C. to about 280 ° C. (see FIG. 32). Methyl methacrylate (Yoshixol 20 in 500 mg)
0 microliter) the melting point does not change, but 230 ° C
When yoshixol is treated at about 340 ° C., a decrease in enthalpy appears when ethyl methacrylate (200 microliters of yoshixol in 500 milligrams) is treated as a whole by yoshixol treatment in ethyl methacrylate (see FIG. 33). In addition, isobutyl methacrylate (200 microliters of Yoshixol in 500 milligrams) also shows two new peaks in the enthalpy increasing reaction at about 60 ° C.-250 ° C., and shows suppression of the maximum enthalpy increasing reaction at about 320 ° C., and other lauryl methacrylates In addition, a phase transition phenomenon appeared in acrylate-based polymers such as polymethyl acrylate by treatment with Yoshixol. In addition, polyvinyl chloride (200 microliters of Yoshixol to 500 milligrams) is 300 ° C.
The enthalpy decrease response around -380 ° C. was approximately doubled by the treatment with Yoshixol as compared to the control (FIG. 34).
reference). In addition, polyethylene glycol 4000 (100
A new peak showing an enthalpy increasing reaction is generated from about 44 ° C. to about 50 ° C. in the case of 100 microliters of Yoshixol per gram, and a region of about 60 ° C. to 360 ° C. in the case of polymethyl acrylate (200 microliters of Yoshixol in 500 milligrams). The enthalpy increasing reaction was suppressed by the addition of Yoshixol (see FIG. 35).

When the expandability of polyvinyl chloride was examined using a thermomechanical analyzer (TMA-50, Shimadzu Corporation), an increase in volume was observed at about 315 ° C. in the case of no treatment. With vinyl chloride (200 microliters of Yoshixol in 500 milligrams), the increase reaction disappeared, and a decrease in the compressibility was observed (see FIG. 36). Based on these results, Yoshixol can improve the physical properties of molecules and polymers, especially thermodynamic properties (for example, structural changes due to changes in energy storage capacity, internal energy state, entropy, etc.). It can be said that it has the ability to modify and improve the functional properties expressed by the structure of the molecule or polymer.

<Effect of Base Pair on Molecular Weight Change of Newly Synthesized Dimer> DNA or RNA synthesizer (392-2)
5 bases (Perkin Elmer) using a 7 base sequence (C
Novel synthetic dimers of (TTCGGA) and (CTTCGGGG) (5 '> CTTCGGACTTCGAGA <3')
And (5 ′> CTTCGGGGCTTCGGGG <
3 ′) was synthesized, and the effect of Yoshixol on the change in the molecular weight of the dimer was examined. The pellet was dissolved in 50 microliters of Tris EDTA, and the OD260 was measured at 100-fold dilution, and the concentration was further made uniform with Tris EDTA and distilled water (5 nanograms / microliter). Then, the prepared synthetic dimer (4 microliters) was labeled at the 5 'end with 4 microliters of ATP labeled with P32, and 1 microliter of polynucleokinase (TaKaRa, Tokyo) was added. 3
After heating at 7 ° C. for 30 minutes and 70 ° C. for 5 minutes, 45 microliters of Tris EDTA, 20 microliters of Tris EDTA, 1 microliter of glycogen and 190 microliters of cold ethanol were added and mixed. The mixture was spun down at 000 rpm for 10 minutes, the supernatant was discarded, and the pellet was dried. It was again dissolved in 50 microliters of Tris EDTA, and 1 microliter of the radioactive solution was treated with 15 grams of urea, 5.7 grams of acrylamide, 0.3 grams of bisacrylamide, 3 milliliters of trisborate EDTA, 10%
0.1 milliliter of ammonium persulfate,
15 microliters of N, N, N, N-tetramethylethylenediamine was mixed with distilled water to make a total of 30 milliliters to prepare a 20% gel, electrophoresed at a constant voltage of 10 watts, and exposed on a film. . Final Tris E mentioned above
A comparison was made by adding 6 microliters of a stop solution to each of 2 microliters dissolved in DTA and 2 microliters of yoshixol as a control, and 2 microliters of distilled water as a control. The change in the molecular weight of the synthetic dimer to which yoshixol was added did not differ from that of the untreated one (see FIG. 37). This indicates that the newly synthesized dimer (5 ′>
CTTCGGACTTCGAGA <3 ′) or (5 ′> CT
It does not change the molecular weight of TCGGGCTTCGGG <3 ′), ie, does not change the primary structure.

<PCR effect of newly synthesized dimer of base pairs on DNA template> The above seven base sequence (CTTCGG)
G), a newly synthesized dimer (5 ′> CTTCGGGGCTTC)
GGG <3 ′) as a primer, snake (Blue General, b
lue-green snake, captured by Matsumoto City, Nagano Prefecture)
Was extracted, and the effect of Yoshixol on PCR using the DNA as a template was examined. The equipment used for the PCR reaction was DNK manufactured by PERKIN ELMER CETUS.
A thermal cycler (PJ-2000)
Was used. 5 microliter primer (100 picomoles / microliter) with 5 microliters of Yoshixol (P +) and without (P +)
-), 5 microliters of snake DNA (50
0 nanograms / microliter) plus 5 microliters of Yoshixol (D +) and no addition (D-), 1 microliter of polymerase enzyme (Recombinant Taq DNA Po)
lymphase, No. R001A, Takara Shuzo Co., Ltd., Otsu City: 5 units / microliter) plus 1 microliter of yoshixol (Pm +) and no addition (Pm-), and left at room temperature for 10 minutes. Diluted with distilled water to make the primer solution 1
The following combinations were prepared by adjusting 0 pmol / microliter, the DNA solution to 50 nanogram / microliter, and the polymerase enzyme solution to 0.5 unit / microliter. For PCR, use the diluted 5
Milliliter of primer solution, 5 milliliter of DN
Solution A, 0.25 microliter of polymerase enzyme solution, 5 microliter of PCR buffer solution and 4 microliter of dNTP mixture, and further adding distilled water to adjust the total volume to 50 microliter. Using. The combinations were those without Yoshixol added as controls (P-, D-, Pm
−), Only primer treated with yoshixol (P +, D−, Pm−), only DNA treated with yoshixol (P−, D +, Pm−), only polymerase enzyme treated with yoshixol (P−, D−, Pm +) and the P−, D−, Pm +
The amount of cDNA synthesis was amplified by PCR in five sets of P-, D-, and Pm + A in which the ratio of yoshixol to the polymerase enzyme solution was increased 100-fold in the series, and measured. In all untreated P-, D-, and Pm-, four bands were confirmed to be expressed in the range of a molecular weight of about 0.5 to 1.2 kb, and P +, D-, Pm-, P-, D + , Pm-, P-, D-, and Pm- did not show any change, while P-, D-, and Pm + suppressed the expression of the band.
Only one band in the lowest molecular weight range among the three bands was slightly expressed, and no expression was observed in P-, D-, and Pm + A (see FIG. 38). This result indicates that yoshixol inhibits the functional expression of a polymerase enzyme involved in transcription amplification of a nucleotide sequence expressed corresponding to a DNA template consisting of many nucleotide sequences. The newly synthesized dimer (5 ′> CTT exemplified here)
It goes without saying that the effect of suppressing the molecular function expression according to claims 1 to 11 of the present invention is not restricted by the primer, CGGGCTTCGGGG <3 ′), snake DNA or polymerase enzyme.

<Effect of Yoshixol on Change or Modulation of Absorbance Wavelength of Dye Molecule> In order to examine the effect of Yoshixol on change or modulation of the wavelength of the dye molecule Evans Blue, Evans Blue (Wako Pure Chemical Industries, Osaka) was used. , Ethidium bromide (MOLECULA
R PROBES INC. , USA) and eosin-
5-Iodoacetamide (MOLECULAR PRO
BES INC. , USA). 1 milliliter of a 1 molar solution of Evans blue, 1 milliliter of an ethidium bromide solution (10 milligrams / milliliter), and an eosin-5-iodoacetamide solution (10 milliliters)
1 milliliter of 10 microliters of yoshixol was added to each milligram / milliliter, and the absorbance was measured with a spectrophotometer (BIO SPECTRO, manufactured by Beckman). Regarding the basic wavelength range of each dye, there was no change in qualitative quantity as well as its basic peak wavelength regardless of the addition or non-addition of Yoshixol. The area has changed significantly. Particularly with ethidium bromide, it was visually observed that the addition of yoshixol reduced the transparency from a transparent dark red color to a reddish color like a ripe peach peel without addition. In the spectrophotometric measurement in this case, a large difference in quality and quantity was recognized in the wavelength range of 270 to 200 nanometers (see FIG. 39). This means
It shows that Yoshixol can modulate the wavelength range of the dye.

<Effects on Surfactants> Also, commercially available kitchen detergents (for example, trade name: Charming, Co., Ltd.) comprising a surfactant such as sodium alkyl ether sulfate, fatty acid alkanolamide, polyoxyethylene alkyl ether and the like. Company Lion: trade name Natera, Lion Corporation: trade name Moa, Kao Corporation) and lauryl sulfate, paraben, cetanol, edetate,
20 each of shampoos for hair washing composed of propylene glycol, polyoxyethylene lauryl ether sulfate and the like (for example, Pantene, Max Factor Co., Ltd .: Lux Styling Co., Ltd., Japan Reaver Co., Ltd .: Essential Styling, Kao Co., Ltd.) The effect was examined by adding 50 microliters of Yoshixol to milliliters. Each detergent and shampoo to which Yoshixol was added improved foaming, appeared smooth, and bubbles were fine,
The color tone was vivid, and oily stains could be easily washed with water. In addition, the amount of water required for washing with water was extremely small and washing was sufficiently possible. Furthermore, although there was no significant difference in the appearance of each detergent or shampoo to which Yoshixol was added, the viscosity of each detergent or shampoo was measured at 30 ° C. using a viscometer (Bismetrone VEA-L,
When measured using Shibaura System Co., Ltd., the results were lower than when no test sample was added (Table 1).
reference). Also, the shear rate-shear stress relationship was reduced by the addition. This indicates that the addition of Yoshixol to a commercially available detergent or shampoo can also improve the surfactant effect and properties of the detergent or shampoo.

[0103]

[Table 1]

<Effects on fatty acids, etc.> 5 g of lauric acid (Wako Pure Chemical Industries, Osaka), 5 g of mytistinic acid (Wako Pure Chemical Industries, Osaka), palmitic acid (Wako Pure Chemical Industries, Osaka) 5 grams of stearic acid (Wako Pure Chemicals, Osaka), 1 gram of oleic acid (Wako Pure Chemicals, Osaka) and 1 gram of linoleic acid (Wako Pure Chemicals, Osaka) A soap-like substance was prepared by adding 50 milliliters of a prescribed sodium hydroxide solution (neutralization method), and the effect of adding yoshixol was examined. The soap-like substance prepared by adding 50 microliters of Yoshixol has better foaming property, better cleaning property and less sticky feeling than the non-added substance, and does not show brown color even when left indoor for more than 6 months. Was. This indicates that Yoshixol can serve as an antioxidant for soaps made from vegetable oils, animal oils, and fatty acids, etc., as well as improve or improve the properties of soaps and the like that are arbitrarily planned. ing.

<Acute and Chronic Toxicity> A mixture of 50 microliters / kg of yoshixol in 1 milliliter of a 20% glucose solution was intravenously administered to unanesthetized mammals (rabbits and dogs). Immediately after the administration, a transient increase in respiratory rate, an increase in blood pressure, an increase in heart rate, and active movement of limbs (not convulsions) were observed for 1-2 minutes. However, although the increase in respiratory rate and blood pressure continued for 2 hours thereafter, no abnormal behavior was observed. In blood tests, hyperpigmentary anemia peaked 3 days after administration and then recovered 1 week later. No change was observed in the platelet count, and the white blood cell count increased 3 days after administration, but recovered to normal one week later. These animals were observed for one month and did not show any abnormal behavior. After anesthesia one month later, the mice were sacrificed with potassium chloride, and pathological examination of important organs was performed. No abnormalities were found visually or under a light microscope. This result shows that the action of Yoshixol is extremely low toxicity in vivo and has few side effects in the living body.
Its safety was confirmed.

For all of the above-mentioned examination items of the action of Yoshixol, the substituents R1, R2, R3, R4, R5, R6 represented by the general formula (1b) or the general formula (3b) Substituents R3, R4, R5, R6 represented by
The effect of a chemical substance (4,4-dimethyl-2-cyclohexen-1-one) in which all are hydrogen was examined for each, and this substance also exhibited a function expressed by the same multidimensional structure as Yoshixol shown above. , But high concentrations were required to obtain qualitatively the same effect as Yoshixol.
That is, the concentration of 4,4-dimethyl-2-cyclohexen-1-one is about 30 to 100 times that of a biological sample and about 10 to 50 times that of an inanimate low molecular weight or high molecular weight sample compared to the concentration of yoshixol. Twice the amount was required.

<Summary of Action, Unique Mechanism of Action, and Its Significance> The effects and actions of the present invention have been described with reference to Yoshixol, which is a specific example. However, the present invention is not limited. In the present invention, a wide range of specific effects from the molecular level to the whole organism have been described. Explaining the respective documents on the scientific basis is far from the description range of the present application, so the following two are shown as references for scientifically known matters. <Reference 1> Bern and Levy, Physiology, Sander
s Publishing Inc .: <Reference 2> Alberts, Ray, Lewis,
Raff, Roberts and Watson, The Molecular Biology o
f the CELL, Garland Publishing Inc .:

The significance of the present invention is that the mode of reaction at the molecular level, the modification of the function expressed by the multidimensional structure created by the macromolecular substance constructed from the molecule, and the modification of the macromolecular substance constructed from the molecule. It is the first time that it has been shown for a specific example that a biological function expressed by a certain multidimensional structure can be inhibited or changed. For living organisms, the inhibitory and inhibitory effects of the functions expressed by the species-specific multidimensional structure of cell membranes, which are evolutionarily determined by each species and built for coexistence with the outside world, are established. In the present invention, what can be done is significant, and it is significant in the history of science that the mechanism can be understood by molecular orbital theory. In addition, its practical significance is as set forth herein.
Furthermore, the social significance of the present invention is not only its effect, but also the molecular orbital method known in advance whether or not the substance shown in the present invention is an extremely simple substance in structural chemistry and useful for human beings. (Such as a method of approximating an isolated reactant), the effect of which can be predicted. For example, regarding the efficacy against viruses, which are transient pathogenic microorganisms composed of macromolecular structures, especially HIV infections, which are currently a global problem, the known scientific facts of molecular biology and the book It can be fully predicted from the embodiments of the invention. In addition to predicting drug interactions, the occurrence of side effects with concomitant drugs, the early prediction of the emergence of resistant bacteria in consideration of the ecosystem and its preventive measures, it is possible to predict not only the global environment but also Since the present invention includes the way of coexistence of human and nature, the significance of the present invention is described for the eternal happiness and peaceful coexistence of human society.

(1) to (46) described in the present invention.
As described in this specification, the outline of the logical explanation considered necessary for understanding the above items is divided into effects on living organisms and actions as substances as inanimate objects, and as shown in this specification, The mechanism is described. However, it goes without saying that the present invention is not limited by this description.

That is, by interpreting the action mechanism of the present invention thermodynamically and further in terms of molecular orbital theory, it is possible to uniquely explain the effects and actions of the present invention. Each molecule has a configuration, a conformation and a molecular orbital, and there is a space region according to the electron distribution, and the energy state based on it has the structure of the molecule itself, physicochemical properties, bonding with another molecule, etc. It is well known that interactions and reaction velocities can be explained by wave equations and frontier orbital theory (Reference: Explanation of Organic Electronics, 4th Edition, Minoru Imoto, Tokyo Kagaku Dojin, 1990; Frontier Orbital Method) Introduction to Fleming, supervised by Kenichi Fukui,
Translated by Tomoda Takeuchi, Kodansha, 1992; How to Understand Molecular Orbitals, 2nd Edition, Masayuki Yoshida, Tokyo Kagaku Doujin, 199
2 years). Many theoretical explanations of chemical reactions have been made based on organic electron theory, molecular orbital theory and quantum theory in the organic chemistry of each molecule. For example, the Woodward-Hoffman rule is one example.

In general, the density of electrons changes as the distance from the nucleus increases, and the distance corresponding to the highest point of the mountain is the location where the largest number of electrons exist (equilibrium distance). In general, the probability of existence in an electron cloud, that is, a place where electrons can spread, is determined according to energy, and this is a logical construction that has been systematized as quantum theory. In a bond (covalent bond) between C and H as an example of a hybrid orbit, if C and H can overlap, two electrons are shared by C and H, and the spin is reversed to 2
When one electron forms one bond, a large amount of energy such as overlapping energy is released,
The internal energy that it has is reduced and stabilized. That is, so-called binding energy is generated.
Conversely, in order to split the C—H bond to separate the original atoms from each other, the bond energy must be newly added in some way. In addition, molecules have quantized orbitals from stable orbitals to unstable orbitals (which means that they are discontinuous and have a constant orbital energy). It is known that electrons reverse spin and enter orbit.
Regarding the overlap of molecular orbitals, there are (+) and (-) phases (Phase), and only those having the same phase can overlap, that is, stabilize. Conversely, it is well known that if the phases are different between (+) and (-), they cannot overlap and repel each other and become unstable.
This is the basis of the so-called molecular orbital theory. The hydrogen ion is is denoted as H ^+, H ⁺ is a proton i.e. protons itself, without should be able to exist in a container such as a beaker particles by itself, is very unstable ones Although this is basic knowledge, it is also an important thing that you often forget when you understand life phenomena. That is, in the presence of water, H ₂ O is always kept in equilibrium with the state of “H ₃ O” ⁺ , and it is important to keep in mind when considering the function. Is a point. In consideration of such electron transfer theory and molecular orbital theory, it is natural to explore the possibility of constructing morphology and controlling, suppressing and blocking functional properties of living organisms and functional polymers. The present invention also constitutes a part of the logical construction of the effect of suppressing the expression of molecular functions described in claims 1 to 11 of the present invention.

In addition, the generation of σ bond in the bond molecular orbital
Is that the circular s orbitals overlap each other and become
And the sp orbits also overlap on the same direction axis and
And overlap when the p orbits also face each other in the same direction axis
Together, it becomes a σ coupling. Furthermore, the generated p orbitals of the π bond
When they are arranged in parallel, they overlap to form a π bond.
If not, the circular s orbit will be
Even if they overlap with different p-orbitals, they cannot be combined (that is,
This is a phenomenon called intercourse). As a further matter of phase
Is a σ bond when the p orbitals are on the same x axis, and py
If it is on orbit or px orbit, it becomes parallel and becomes π bond
However, the directions of the py and px orbits are different at right angles.
Therefore, they do not overlap, and if the phases are different, anti-bonding molecular orbitals
And does not become a bond. Furthermore, the electron isomer effect (E effect
Result) is double compared to the case where the
It becomes a π bond of the bond and greatly differs. Group O is sixth
Being a family, if you have six electrons belonging to it,
Electrically neutral without the ability to release tons
If you have an individual, it is natural that
You. This is a molecular expression function according to claims 1 to 11.
It is also a fundamental feature of the carbonyl group possessed by the inhibitor.
You. Also important is the delocalization and delocalization energy of π electrons
It is. When the π electrons are dispersed, the molecule becomes stable,
The amount of energy equivalent to the amount of stabilization is
Become energy. The carboxyl group -C (= O) -OH is
H in itself⁺ With a property or structure that provides
And H ⁺H as the second cause of easy release⁺ Out
-CO-O- after the anion
Since the electrons are dispersed, the delocalized energy
That is, resonance energy is generated and H⁺ By releasing
Can be further stabilized, and this state
⁺ The first factor that emits again is decisive. But life
For all aqueous solutions, including the body, [H_Three O⁺ ] X [OH
^- ] = Constant formula holds, such released professional
Tons are the interior of disorder in thermodynamically non-equilibrium open organisms
Although it is used as energy,
The energy of stabilization and ordering in materials that allow rotons
Changes the primary structure of the molecules that make up the body.
First, various functions expressed by the multidimensional structure (molecular recognition)
In order to prevent
Is a nucleophilic substance and has no proton releasing ability
Neutral molecules are considered ideal.

The frontier molecular orbital theory, in which the σ-π interaction or reaction in a π electron system is determined by the interaction between the HOMO molecular orbital and the LUMO molecular orbital, is an important concept. For example, a double bond is made up of a σ bond and a π bond, and the reaction occurs in a portion where the electron density is high. Taking the "rise" of the carbonyl group as an example, the π-covalent electron pair that connects C and O with a double bond is based on the E effect, and may be pulled toward O. . This is because the addition of a carbonyl group is referred to as a nucleophilic addition reaction, and since C 立 ち 上 が り O has the property of rising, oxygen takes an electron to make it easier to further increase the −charge. C = O has a π bond, but the molecular orbital method has an excess of electrons, so the binding molecular orbital with the electrons interacts with the anti-bonding molecular orbital of the C = O group. I do. That is, the HOMO molecular orbital of the anionic substance and C =
The LUMO orbitals of O become perturbed. From such a point, the part where the compound easily reacts is determined by the magnitude of the coefficient C of the HOMO molecular orbital or LUMO molecular orbital and the phase symmetry of the constituent atomic orbital. further,
According to the theory of organic electrons, an important factor that governs the activation energy of a chemical reaction is electric power. In the reaction with neutral molecules,
Polarization or electron transfer must occur, and the fact that the electron density in the reaction center is high or low has an important meaning, and substances related to morphogenesis and functions of organisms, etc. By changing the localization, it is responsible for the function expression and functional differentiation by reaction center sites and molecular recognition. The magnitude of the activation energy that determines the difficulty of such a reaction is determined by the energy required for the localization of π electrons in the transition state. The position where the target, nucleophilic, or radical reaction occurs is determined as follows. That is,
In the case of an electrophilic reaction, the position where the density of the two electrons belonging to the highest occupied orbit in the ground state is the highest (HOMO)
In the case of a nucleophilic reaction, the position where the electron density is highest when two electrons are arranged in the lowest unoccupied orbit in the ground state (LUMO). In the case of a radical reaction, HOMO and LUMO are two. One electron in each orbit
When they are arranged individually, this is the position where the sum of the two electron densities is the largest. As described above, the largest factor that determines the chemical reactivity is that the condition for obtaining a large stabilization in the reaction from the standpoint of stabilization by delocalization of electrons is the highest occupied orbital (HOMO molecular orbital) of the electron donating substance. ) And the symmetry of the lowest unoccupied orbital (LUMO molecular orbital) of the electron-accepting substance are shown to be consistent. When the HOMO molecular orbital and the LUMO molecular orbital have different symmetries while the energy can be obtained and the chemical reaction easily occurs, the stabilization energy of the system by the HOMO orbital-LUMO molecular orbital interaction becomes zero. Therefore, it is considered that the chemical reaction hardly occurs. Again, the π-electron energy level will be described in terms of typical substances related to biological reactions. For example, in the order of HOMO, the order is porphyrin>guanine>adenine>riboflavin>thymine>tryptophan> histidine, and the LUMO is low. Histidine>Guanine>
It is known that adenine>tryptophan>riboflavin> porphyrin in this order, and that in general, S2 compound (-SH) and then NH2 have a high HOMO and have a property of easily giving an electron.

Further, as described above, the intermolecular compound is composed of an electron donor (D) for giving an electron to a partner and an electron acceptor (A) for receiving an electron from the partner. Assuming that they are close to each other, a van der Waals force (attractive force acting between molecules) acts to cause a weak bond between D and A. This state is termed "non-bonded structure". . It is denoted by D. When the distance between A and D is further reduced, the electron clouds begin to overlap with each other, possibly causing the electrons to move. If one electron moves from D to A, each will have one unpaired electron, and these electrons will form a new pair of electrons, thus the A-D bond will be formed. Occur. This state is referred to as A. . D
Since this can be expressed as-, this is a state called "charge transfer structure" and is energy dependent.
The change and modulation of the multidimensional structure of a substance and its functional properties by such an energy state can be attributed not only to inanimate macromolecules but also to the conformation, configuration, and chiral of molecules, as well as morphogenesis, organization, and information. Multi-dimensional structures and their functional characteristics, which are assembled in order to construct living organisms from molecules such as transduction via macromolecules and express their functions smoothly, are important.

Further, in order to easily understand the thermodynamics of a chemical biological system, when a living body or a polymer is considered as the thermodynamics of an elastic body, the following equation holds: dE = TdS + fdL + μdN. f is the stretching force, L is the length, N is the number of chains or the number of structural units or monomers. In the case of a closed system, N is constant, and from the ideal rubber model formula of the wale, a shorter constituent unit is advantageous when the component 2 is combined, and becomes more dramatic if there is an interaction between the substances. Further, f
Is small, almost all of the constituent units tend to be in the α-form, and when f is somewhat large (critical temperature), almost all of the constituent units are suddenly changed to the β-type all at once. Such a phenomenon is caused by a phase transition (Phase Transitio).
This phenomenon is referred to as n), which is important for understanding sol formation, gelation, liquid crystal formation, and the like. Furthermore, when there is a bond of the second component, even if f (force) is constant, a change in P2 (pressure, volume) changes to a change in f, triggering a phase transition. Such an effect is called an allosteric effect, and is important not only for a macromolecule but also for a biological function. Also, life phenomena are not a matter of equilibrium,
It is born out of its dynamic behavior, and has attracted interest in the relationship between its structural form and function. The equilibrium condition of the reaction is that there is no change in free energy due to the reaction, that is, dH-TdS = 0, and dS is an entropy change accompanying the reaction. The chemical reaction rate quantitatively expresses how fast the chemical composition of a substance system changes.The reaction rate is a function of the concentration of the molecular species contained in the system, and the temperature, pressure, The most general function is represented by a reaction rate constant k, which is represented by k = Ae-Ea / R.
A is a frequency factor, and the index-related part indicates the probability that the reaction molecule has energy equal to or higher than the activation energy (Ea). In the case of a single-molecule (single-molecule) reaction, the reaction molecule itself reacts spontaneously, and activation is performed by light irradiation or heat, but a molecule having sufficient energy for the reaction is the same as vibration. Activating molecules are 100
Reacts in -10 Fent seconds.

Further, chemical reactions can be broadly classified into those in which the activation energy controls the speed and those in which the energy transfer is the main factor. In other words, ignition is the process of generating radicals having atoms and unpaired electrons that basically govern the reaction.Atoms and radicals are rich in reaction activity due to the small activation energy of the reaction, and the Can be promoted. That is, the chain reaction is an important reaction that occurs in various cases such as combustion, thermal decomposition of a hydrocarbon, and a polymerization reaction, and is also important for understanding biological phenomena. Also,
Living organisms are also composed of carbon compounds, and in general, the bonds between each atom of the carbon compound are mostly made up of covalent bonds, and in order to break the bonds, external energy must be applied. It is also known that as the number of carbon atoms increases, the number of isomers increases dramatically. What governs this life phenomenon on earth is the reason that it is said to be this optical isomer phenomenon.

Since the polymer structure has a single bond and can rotate internally, it has a spatial configuration (conformation) of polymer chains, and it has a short-range interaction and a long-range interaction (excluded volume). effective. For example, it is known that a linear polymer has a helical structure if entropy due to a change in the shape of the molecular chain is ignored, assuming that only the interaction energy in the molecular chain is used in the linear polymer. Furthermore, the energy due to the change of the bond angle between bond atoms,
Van der Waals attractive force between non-bonded atoms and repulsive force due to overlapping electron clouds between atoms, interaction between dipoles when polar groups are included, electrostatic interaction and molecules between ions when ionized atoms are included It is also known that internal hydrogen bonds are related to the conformation, and when it takes a helical structure, it is the most stable in terms of energy. ing. As the interaction between molecules, van der Waals attraction and repulsion due to overlapping of electron clouds between atoms, intermolecular hydrogen bonding, dipole interaction, and the like play a major role. In the copolymer, the blocks agglomerate with each other to cause fine phase separation. The magnitude of this phase separation is several tens of nanometers, which is on the order of molecular chains, and when a suitable heat treatment is performed, a spherical phase or a rod-like phase forms a macroscopic lattice. If the molecular chain is rotatable inside like polyethylene or polystyrene, the shape of the molecular chain changes from moment to moment due to the movement of the molecule, resulting in a random coil shape. In the case of a molecule such as a polyamino acid or DNA, the molecule has a rod-like structure when a helical structure is formed for hydrogen bonding, and a random coil shape when the hydrogen bond is broken. In addition, when the thermodynamic equilibrium state of the polymer is broken, a so-called volume phase transition in which the polymer swells and contracts appears.

Further, according to the second law of thermodynamics, it is known that natural phenomena proceed in a disordered direction. In a non-equilibrium system such as a living organism, the order formation is in a thermodynamically appropriate direction. According to the second law of thermodynamics, which is believed to be, the spontaneous change increases the entropy.
In other words, in natural phenomena, order breaks down to a more disordered state, but as is typically seen in life phenomena, it is theorized that nature creates order by itself. At first glance, it seems that life is contrary to the laws of physical chemistry, but under non-equilibrium conditions such as life, such order formation is a natural physicochemical process, and this is justified by the dissipative structure theory. This is an extension of the theory of self-organization (formation of an ordered structure) in a physicochemical system in a non-equilibrium state far from equilibrium. That is, simply, the entropy change dS of the system at a short time interval of dt can be expressed as the sum of the internally generated entropy diS and the entropy deS contributed by the flow (dS = deS + diS). Now
If the system is in a steady state such that dS / dt = 0, then deS = diS <0, ie, if a sufficiently large amount of negative entropy is given to the system, the spontaneous entropy in the system will increase. Is deleted, and an ordered structure can be maintained in the system.

[0119] Such a situation is applicable to life phenomena. Organisms, whether they are cells or organized tissues, organs, organs and individuals, are open to the body in a non-equilibrium system at any level. System. If the entropy generation due to the unplasticized process is considered as a variable of the rate of entropy generation by heat flow, the rate of entropy generation by material flow, and the rate of entropy generation by chemical reaction, the affinity between the product system and the reactant system Is a difference between the free energy and the larger the deviation from the equilibrium, the larger the value. When the chemical reaction has reached the equilibrium, it is zero. Therefore, entropy generation is (reaction rate) ×
(Deviation from the equilibrium of the chemical reaction). Generally, entropy generation in the non-equilibrium state is (flux)
X (thermodynamic force) is understood as the sum. Here, the term “flux” means a flow such as a heat flow, a diffusion flow, a chemical reaction rate, and the like. The thermodynamic force is a driving force that causes a flow, such as a temperature difference, a concentration difference (difference in chemical potential), and a chemical difference. The affinity of the reaction. For example, suppose that a new phase that is slightly different from the original system appears under the condition that the volume V and the internal energy E are constant. If it grows, the original system will disappear. In other words, the original system is unstable, and if such a state change is considered thermodynamically, even if the system is in a non-equilibrium state, local equilibrium is assumed here. According to two laws, a new phase will form if this perturbation increases entropy. Therefore, the condition under which the original system is stable requires that the entropy change due to perturbation be negative. In other words, the system in which the temperature drops when heat is applied and absorbs heat (negative constant heat capacity) or expands rapidly when pressure is applied (negative compressibility) is intuitively unstable. But it actually means the opposite. In addition, the generation of excess entropy per unit time is a value obtained by integrating (fluctuation of flux × change of thermodynamic force) over the entire system, and is shown to be always negative. Is a universal development criterion for Prigogine as common as the assumption holds. That is, when this relationship is disturbed for any reason, the reference state becomes unstable and develops into a new state, a vibration state occurs from a steady state, or a new pattern (eg, high functional Molecular material).

From the above-mentioned logical description and examples of the thermodynamically and molecularly orbitally inanimate molecules and macromolecules described in the present invention, the morphogenesis, which is the basic of life phenomena, The logic of the biological effects exemplified by the molecular expression function-suppressing agents according to claims 1 to 11 of the present invention from the viewpoint of non-equilibrium open systems based on thermodynamic or molecular orbital theory in terms of function expression and molecular recognition. Explain the appropriateness and validity. As an example, as an ideal anticancer agent property,
Despite the fact that it is theoretically required that there is no Bay region while having a large negative enthalpy and a small entropy or a high binding enthalpy and a low binding entropy, the realization is impossible. Has been treated as something special. In the following, we outline the cells, which are the basic structure of general living organisms, and outline the thermodynamic and organic electron importance of water, which is an important element in living organisms. This paper describes the approximate calculation results of the electron localization of yoshixol and its characteristics, and emphasizes the thermodynamic and molecular orbital validity of the effect and its significance in the history of science.

The biological membrane is a fluid mosaic composed of lipids, proteins and carbohydrates, and has both hydrophilic and hydrophobic properties. In general, in order to maintain normal membrane function in a new temperature environment, the composition of fatty acids of membrane phospholipids is changed to adjust membrane fluidity. The biological effect of Yoshixol exemplified in the present invention is, by analogy with the appearance of the thermodynamic effect of Yoshixol, for the thermodynamic state of each biological component, as exemplified in Examples of the present invention. It can be said that it is more reasonable than a series of grades. The stability of a biological membrane is largely affected by hydrophobic interactions between hydrophobic groups. Most amino acid hydrophobic side chains are buried inside the protein so that they do not come into contact with water. It is well known that a protein's higher-order structure forms a flexible structure while being maintained by hydrogen bonding, hydrophobic interaction, and van der Waals force. Such a flexible structure easily changes depending on the environmental conditions surrounding the polymer,
There is a variable characteristic that the original higher-order structure is restored again when the condition returns. Underlying this structure are hydrogen bonds and hydrophobic interactions. A solvent other than water cannot form such a structure. Entropy is large in such a flexible structure and in a state of a random coil.
Also, a hydrophobic interaction acts between the side chains, and water of hydration around the side chains is pushed out of the protein molecule. Therefore, many amino acid hydrophilic groups gather on the surface of the globular protein, and the protein can be dissolved in water while maintaining the higher-order structure. Globular proteins have a certain higher-order structure, but are similar to surfactant micelles because hydrophilic groups are concentrated on the outside and hydrophobic groups are concentrated on the inside. That is, it is considered that a solute having a higher hydrophobicity is more likely to bind to a protein, and the conformation of the protein is changed because the hydrophobic molecule penetrates into a hydrophobic region near the protein surface.

Thus, when the structure and function of the cell membrane are considered again, glycolipids are also important, and these sugar chains are responsible for discrimination and adhesion between cells, and various extracellular active factors and antigens. While acting as a receptor for molecules, it plays an active role in a wide variety of cell functions such as cell proliferation, differentiation, development, and tissue formation. As a simple example, blood types A, B, and O are phenomena that occur due to differences in the structure of the sugar chains of glycolipids on the surface of erythrocytes. It is also known that the growth of human cancer cells is suppressed by providing glycolipids. The inhibition of the molecular expression function of the compound described in claims 1 to 11 of the present invention can inhibit the biological function expressed by the multidimensional structure of the sugar chain-binding substance by changing its conformation or the like.

Also, it is well known that cells do not always exist at a steady position, but make various movements depending on the type of cells. Flagella are involved in the movement of sperm, while cilia are an effective mode of movement for moving liquid along the cell surface. The energy of such motion is derived from the flow of hydrogen ions.
Prokaryotic cells use hydrogen ions themselves,
The source of energy for eukaryotes is the flow of hydrogen ions due to the hydrolysis of adenosine triphosphate. In any case, these cell movements depend on the transfer of hydrogen ions, that is, electrons, and when considered as a change in thermodynamic entropy, the cell movement of the compounds according to claims 1 to 11 of the present invention is considered. The thermodynamic effect can explain the biological effects such as the antibacterial effect, anticancer effect, and inhibitory effect on sperm motility, based on the thermodynamic effect.

Further, the enzymatic action relating to the chemical reaction in the living body can be explained from the viewpoint of the function of expressing the molecular structure. For example, a hydrogen atom bonded to the nitrogen atom of the pyrimidine ring in the side chain of histidine dissociates at around pH 7, so that it often plays an important role in living organisms at almost exactly pH 7, The periphery has a shape complementary to the substrate, so that an appropriate binding force can be generated by van der Waals interaction. Since van der Waals interactions are inversely proportional to the seventh power of distance, the presence of tightly contacting surfaces creates a strong attractive force between them. In addition, the active site of an enzyme having a serine residue in the active site such as a serine enzyme (eg, trypsin, chymotrypsin, elastase, etc.) has a space surrounded by hydrophobic residues. Larger side chains fit into it, which makes it easier for some residues with aromatic or large hydrocarbon side chains to be hydrolyzed, and pepsin between amino acid residues with aromatic or large hydrocarbon side chains. Although the peptide bond can be hydrolyzed, the hydrolysis rate is affected not only by the residue next to the bond to be cleaved but also by the next residue, and the SH group of cysteine such as cysteine enzyme is It is also known that it works together with the imidazole ring of histidine, and the compounds described in claims 1 to 11 of the present invention have a molecular function expression suppressing effect such as thermodynamic effects and chemical reaction kinetics. Et al. Also, it is possible to explain the biological effect.

Further, based on the above description of the mechanism, the intracellular structure is supported by the cytoskeleton, and its main components are actin, microtubules, intermediate fibers and the like. It plays an important role in mitogenesis and morphogenesis, as well as in mitotic growth and death. The components constituting these cytoskeletons exert their biological functions by polymerization and depolymerization. For example, in actin fiber, about half of the intracellular actin remains a monomer having a molecular weight of 42,000, but the remaining polymerizes to form a fiber having a diameter of about 8 nanometers. In addition to the equilibrium between the actin filaments, the actin fibers are in a dynamic equilibrium state in which the actin fibers are elongated by polymerization at one end and shortened by dissociation on the other. In any case, by adopting a multidimensional structure, it can be said that various biological functions are expressed and morphogenesis is brought about. Furthermore, the microtubules and microfibers that make up the cytoskeleton
There are significant differences from the organelles such as nuclei, plastids and mitochondria. The latter is stable, while the former is newly generated or disappears depending on conditions. In other words, microtubules and microfibers are “moving structures”, which are not always stable in a fixed form but dynamic. Also, the shrinkage does not mean that the tentacles contract, but rather that the microtubules break down into tubulin at the base of the tentacles (depolymerization), so that the microtubules are rapidly broken down into their constituent protein units. The length of the microtubules shortens. When the polymerization and the depolymerization are in an appropriate equilibrium (dynamic equilibrium in which they fluctuate and balance each other), it is considered that normal cell survival. There are proposals for substances that attempt to suppress cell division and proliferation by promoting polymerization by utilizing such a thing (for example, taxol), but conversely, this depolymerization is regarded as a thermodynamic non-equilibrium system. By promotion, it is theoretically possible to suppress the growth of cancer cells and the like. The molecular function expression inhibitor according to any one of claims 1 to 11 of the present invention has a thermodynamic dynamic equilibrium state of a living body due to its thermodynamic effect and properties such as hydrophobicity, nucleophilicity, and electrophilicity. Biological effects can be explained by thermodynamically ordering the disorder of conformation such as conformational change and phase transition.

Furthermore, although it is well known that most of the living body is composed of water, it is an important factor that is often forgotten. In other words, it may be considered that both the inside and outside of the cell are in a concentrated solution state. This is a major cause of the above-described phase transition. When considering a biological substance as such an aqueous solution, the thermal motion of the hydration water around the hydrophobic group is slowed down, and the rotational motion of water molecules around the hydrophobic group is similarly slowed down. The method of hydration is completely different from the hydration of ions, sugars, and OH groups, and is called hydrophobic hydration. In a solution, the roles of the solute and the solvent are reversed depending on the concentration. Thus, the nature of the thermal motion of the molecule in the hydrated state is disordered. The negative change in entropy indicates that the hydration water of the hydrophobic substance has a smaller entropy than the bulk water. Also, a state with low entropy is not thermodynamically favorable, and when molecules having a sufficiently large hydrophobic group dissolve in water, these hydrophobic groups aggregate to push out water molecules that have been in contact with the hydrophobic group. In this case, the entropy of the entire solution becomes larger. The reason why surfactants and the like assemble to form micelles can be considered to be due to this hydrophobic interaction. This hydrophobic interaction is extremely important for living organisms.

The dynamic study of water in a living body is important not only for understanding biological biological phenomena but also for medical purposes. For example, the longer relaxation time in cancer tissue is thought to be due to the conformational change of the biopolymer, and the thermal motion of water in cancer cells is faster than in normal tissue. Therefore, if there is an appropriate neutralizing substance that enhances the structuring of water, it is possible to suppress the growth of cancer. In addition to cancer, even in pathological conditions such as virus infection, bacterial infection, inflammatory edema such as gastroenteritis and gastric ulcer, allergic (atopic) reaction, edema due to circulatory disorders, etc. The relaxation time has been found to be different from that of normal tissue. The water molecule in the cell is 10
It is in motion from picoseconds to 10 nanoseconds, which is significantly slower than the motional state of water molecules in extracellular and bulk waters, which is 10 Fent seconds. Since the entropy is greater when the thermal motion is more intense, it can be said that the structured water has a lower entropy.

As described above, Yoshixol exemplified in the examples of the present invention has the following molecular structural characteristics (see Table 2).
That is, 1) that the π electron density is localized up to the double bond centering on the carbonyl group and has no cyclic electron cloud; 2) there is a HOMO-LUMO gap (difference);
High reactivity to electrophilic species (amino group, hydroxyl group, etc.) and reactivity to nucleophilic species (proton, carbon cation, etc.). 3) Carbon (1st position) of carbonyl group in charge distribution.
Is a positively polarized oxygen but has no proton releasing ability and is a neutral molecule. 4) A methyl group which is an alkyl group on the opposite side of the carbonyl group (hydrophobic structure).
5) In addition to being three-dimensionally mirror-symmetrical, 6) not having a Bay region, etc. In addition, it is considered that the unstructured water molecule involved in structuring also suppresses the conformational expression function of the molecule.

[0129]

[Table 2]

That is, the effects of the compounds described in claims 1 to 11 of the present invention to suppress the expression of molecular functions are determined by factors such as thermodynamic entropy, force and length (or pressure and volume), and the number of combinations (probability). Altering the thermodynamic state of the receiving reacting substance or state by the interaction of any or each of the factors appears to be its basic mechanism of action. The manifestation of the thermodynamic state change such as the entropy increasing action is thermodynamically established regardless of the equilibrium system or closed system material or the non-equilibrium system such as living things or open system. Is multidimensionally modulated,
It indicates that change and further improvement are possible regardless of the living or inanimate substance, and the purpose is to elaborate the scientific logic and validity of this mechanism of action, Not only the above significance, but also the significance of the history of science was emphasized without regard to repeated duplication, and its significance was clarified.

The substituents R3 and R3 in the general formula (3b)
The effect of a derivative intermediate (4,4-dimethyl-2-cyclohexen-1-one) in which 4, R5 and R6 are hydrogen atoms as an antifungal agent or an antiandrogen, and as an aromatic agent; The action as a reagent necessary for optical activity is known (Japanese Patent Application Laid-Open Nos.
-105038, JP-A-4-316531, U.S. Pat. Nos. 4,081,458 and 5,169,993, and Swiss patent 603071). However, in the present invention, the chemical formula (1a)
(1b), (2), (3a) (3b) have the multidimensional structure (conformation) or configuration of the substance that constitutes the form and function of the organism Chemicals and compositions capable of suppressing and inhibiting the functions expressed by (configuration) are necessary for antifungal agents, anticancer agents, fragrances, optical activities based on the logical mechanism of action disclosed herein. Reagents and antibacterial agents, antiviral agents, germicidal disinfectants, blood coagulation / fibrinolytic inhibitors and inhibitors, spermicides or external contraceptives, thrombolytic agents, sugar chain coordination agents, arteriosclerosis inhibitors, metabolism ( Lipid, sugar, protein) improver, wound healing, epithelial formation promoter,
Bioactive substance (enzyme, peptide, gene, etc.) function inhibitor and inhibitor, or antigen-antibody reaction inhibitor or inhibitor, organ tissue preservative, and non-biological molecules (phospholipid, glyceryl group, sulfhydryl group) , Thiol ester groups, bonds between monosaccharides or disaccharides and polysaccharides, silicon, vinyl groups, cellulose, etc. (chain reaction polymerization, sequential reaction polymerization, radical vinyl polymerization, polymerization inhibition, copolymerization,
Configuration polymerization, sequential polymerization, spatial network polymerization, cross-linking reaction, etc.) methylation of carbohydrates, peptide bond of amide group, synthesis of soluble globular protein, control of stereochemistry and spatial recognition of other substances, and micellization of lipids, Organic composition containing an active ingredient as an emulsifying action of other substances, furthermore, a depolymerizing agent, a surfactant improving agent, a phase change agent or a phase change improving agent, a micro phase separation structure improving agent, a plasticizer or a plasticity improving agent , Copolymerizer or copolymer modifier, polymerization regulator or polymerization modifier, stabilizer or stabilization modifier, amorphous agent or amorphous modifier, rheological property modifier, softener or softening modifier , Antioxidants or antioxidants, dyes, paints, pigments, or colorants, modulators or modifiers of the fluorescence or excitation wavelengths, physical or functional modifiers of low molecular weight substances, and physical properties of high molecular weight substances. The function modifier is that it is needless to say that does not undergo limitations on the physical properties improving agent of macromolecular composite materials and functional macromolecular composite materials.

For example, flavonoid dyes such as chalcone, flavone, anthocyanidin, auron, etc., xanthone dyes such as gentisin, rickexanthone, etc. For example, benzoquinone, cyperaquinone, embelin, mesaquinone, purbic acid, copurinine, loson, juglone, romathiol, anthraquinone, anthrone, alizarin, rubiadin, etc. Phycobilin dyes, petalein dyes,
It can be clearly expected that the dyeability of each of the melanin-based dye and the synthetic organic compound-based dye can be sensitized, decolorized, and further changed in color.

[0133]

The present invention will be described below with reference to specific examples of preparations.

Formulation Example 1 [Cream (burnishing type)]
Yoshixol (0.3), citric acid. Monohydrate (0.
5), polypropylene glycol (4.5), distilled water (6)
7.7), cetanol (4.0), stearic acid (1
0.0), solid paraffin (2.0), octyldodecyl myristate (5.0), isopropyl myristate (5.0), and glyceryl monooleate (0.5). The mixture is heated and emulsified to obtain a burnishing cream (O / W emulsion).

Formulation Example 2 [Ointment formulation] Yoshixol is added to liquid paraffin and dispersed. This is added to Plastibase and mixed well to obtain an ointment (lipophilic ointment) containing 0.3% by weight of Yoshixol.

Formulation Example 3 [Tablet type] The tablets and capsules may be coated, if necessary, with a gastric film-coating agent (eg, polyvinyl acetal diethylaminoacetate) or an edible coloring agent which is usually used.

Formulation Example 4 [Injection] This injection is dissolved with a small amount of ethanol as necessary, and mixed with a commonly used injection liquid (eg, 20% glucose solution) to obtain an injection.

The embodiments of the present invention have been described above.
It is needless to say that the present invention is not limited to the above-described embodiment, and can be appropriately modified and implemented within the scope of the present invention.

[Brief description of the drawings]

FIG. 1 shows one of the molecular expression function inhibitors according to the present invention.
NADP of Yoshixol which is an embodiment of the invention
It is the graph which measured and evaluated the effect with respect to H, NADP, heme, and cytochrome C with an infrared spectrophotometer.

FIG. 2 is a graph showing the effect of Yoshixol on the amino acid composition of human serum, fibrinogen, and thrombin.

FIGS. 3 (a) and 3 (b) are graphs showing the effect of Yoshixol on human blood coagulation in a thromboelastogram.

[FIG. 4] FIG. 4 is a graph showing electrophoresis of the effect of yoshixol on trypsin and albumin in terms of the three-dimensional structure of protein and its function by electrophoresis. FIG.

FIGS. 5 (a) and 5 (b) are diagrams showing the effects of blood group determination by ABO blood group serum antibodies of Yoshixol, each of which is obtained by digitizing the degree of agglutination with a digitizer and converted into a graph. It is.

FIG. 6 is a graph showing the effect of yoshixol on increasing blood pressure of vasopressin.

FIGS. 7 (a), (b) and (c) are electropherograms obtained by examining the effects of Yoshixol on the primary structure of bovine albumin, blood group anti-A serum and anti-B serum proteins, respectively. FIG. 3 is a diagram showing a result obtained by digitizing a staining concentration by a digitizer and converting it into a graph display.

FIGS. 8 (a), (b) and (c) show yoshixol methicillin-resistant Staphylococcus aureus (MRSA),
It is a figure which shows the antibacterial effect with respect to Escherichia coli and Trichophyton.

FIG. 9 shows MRS immediately after Yoshixol treatment.
3 is a scanning electron microscope image of a dead form of A.

FIG. 10 is a scanning electron microscope image of a dead form of Escherichia coli immediately after treatment with Yoshixol.

FIG. 11 is a scanning electron microscope image of a killed form of acid-fast bacterium immediately after treatment with Yoshixol.

FIG. 12 is a scanning electron micrograph of a killed form of Trichophyton just after treatment with Yoshixol.

FIG. 13 is a scanning electron micrograph of a killed form of Pseudomonas aeruginosa immediately after treatment with Yoshixol.

FIG. 14 shows the effect of Yoshixol on plaque count of E. coli bacteriophage.

FIG. 15 shows the effect of Yoshixol on chicken myeloblastosis virus (AMV) reverse transcriptase.

FIGS. 16 (a) and (b) are cell specimen images obtained by observing the effect of Yoshixol on cultured kerato cells using a phase contrast microscope.

FIGS. 17 (a) and 17 (b) are cell specimen images obtained by observing the effect of Yoshixol on cultured kerato cells using a transmission electron microscope.

FIG. 18 shows Hela treated with Yoshixol.
It is a figure which shows the survival rate of a cell.

FIG. 19 is a scanning electron microscope image showing a killed image of Hela cells by Yoshixol.

FIGS. 20 (a) and (b) are cell specimen images obtained by observing the state of morphological change of blood erythrocytes caused by Yoshixol with a scanning electron microscope.

FIG. 21 is a histological image obtained by transplanting yoshixol-treated dog skin into rabbit skin and a histological image showing the engraftment effect of intravenously administering yoshixol to a dog transplanted with rabbit skin. It is.

FIG. 22 is a view showing the dissolving effect of Yoshixol after human blood clot formation.

FIG. 23 is a graph showing the effect of oral administration of yoshixol on changes in serum total protein and albumin levels in dogs.

FIG. 24 is a graph showing the effects of oral administration of yoshixol on changes in the ratio of serum albumin to globulin and blood glucose level when administered orally to dogs.

FIG. 25 is a graph showing the effects of oral administration of yoshixol on changes in serum cholesterol and triglyceride.

FIG. 26 is a graph showing the effects of oral administration of yoshixol on changes in serum residual nitrogen and creatinine when administered to dogs.

FIG. 27 is a serum creatinine image when yoshixol was orally administered to dogs.

FIG. 28 is a scanning electron microscope image showing the effect of Yoshixol on bovine sperm flagella.

FIG. 29 is a transmission electron microscope image showing the effect of Yoshixol on bovine sperm flagella.

FIG. 30 is a calorimetric diagram of a differential scanning calorimeter showing the effect of Yoshixol on palmitic acid.

FIG. 31 is a calorimetric diagram of a differential scanning calorimeter showing the effect of Yoshixol on polyethylene glycol 1000.

FIG. 32 shows polystyrene 28 of Yoshixol.
FIG. 4 is a calorimetric diagram with a differential scanning calorimeter showing the effect on 000.

FIG. 33 is a calorimetry diagram of a differential scanning calorimeter showing the effect of Yoshixol on methyl methacrylate and ethyl methacrylate.

FIG. 34 is a calorimetric diagram of a differential scanning calorimeter showing the effect of Yoshixol on isobutyl methacrylate and polyvinyl chloride.

FIG. 35 is a calorimetry diagram of a differential scanning calorimeter showing the effect of Yoshixol on polyethylene glycol 4000 and polymethyl acrylate.

FIG. 36 is a measurement diagram of a change in volume or swelling property with a thermomechanical analyzer showing the effect of Yoshixol on polyvinyl chloride.

FIG. 37 is an electrophoretogram showing the effect on molecular weight of a newly synthesized 7 base pair dimer of Yoshixol.

FIG. 38 is an electrophoretogram showing the effect of snake DNA on PCR using a newly synthesized 7 base pair dimer of Yoshixol as a primer.

FIG. 39 is a diagram showing a change in absorbance measured by a spectrophotometer showing the effect of Yoshixol on ethylene bromide.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 31/00 631 A61K 31/00 631H 635 635 637 637D 643 643D 31/34 31/34 31/40 31 / 40 31/42 31/42 31/425 31/425 31/435 31/435 31/47 31/47 31/495 31/495 31/505 31/505 31/535 31/535 C07C 49/403 C07C 49 / 403 E 49/463 49/463 49/603 49/603 49/687 49/687 49/713 49/713 C07F 9/117 C07F 9/117 // C07D 207/333 C07D 207/333 209/08 209/08 215/14 215/14 233/60 101 233/60 101 239/26 239/26 261/08 261/08 277/24 277/24 295/10 295/10 AZ 307/46 307/46 307/80 307 / 80 307/86 307/86

Claims (46)

[Claims] (1) a of the general formula (1) (Wherein (i) R1, R2, R3, R4, R5 and R6 are each independently a hydrogen atom; a halogen atom; C1
An amidino group; a C3-C8 cycloalkyl group; a C1-C6 alkoxy C1-C6 alkyl group;
Aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bonded to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene rings; C1-C6 alkylene group; benzoyl group; cinnamyl group; A cinnamoyl group; or a furoyl group; (ii)
A is a hydrogen atom or Wherein R7 is a C1-C6 alkyl group; a sulfide group; or a phosphate group; R8 and R9 are each independently a hydrogen atom; a halogen atom; a linear or branched C1-C6 alkyl group; An allyl group; one or two aromatic rings selected from the group consisting of benzene, naphthalene and anthracene rings.
An aralkyl group to which the above C1-C6 alkyl group is bonded;
A benzoyl group; a cinnamyl group; a cinnamoyl group; or a furoyl group) (iii)
Any of R1, R2, R3 and R4 and / or R5
And R6 may be a substituted or unsubstituted cyclopentyl group; a substituted or unsubstituted cyclohexyl group; or a substituted or unsubstituted naphthyl group;
And R6 may be combined with another condensed polycyclic hydrocarbon compound or a heterocyclic compound to form a ring, and (v) R
3, R4, R5 and R6 are a halogen atom, a cyano group,
A carboxyl group which may be protected, a hydroxyl group which may be protected, an amino group which may be protected, a C1-C6 alkyl group, a C1-C6 alkoxy group,
C1-C7 alkoxycarbonyl group, aryl group, C3
-C6 cycloalkyl group, C1-C6 acylamino group,
A C1-C6 acyloxy group, a C2-C6 alkenyl group,
C1 to C6 trihalogenoalkyl group, C1 to C6 alkylamino group and diC1 to C6 alkylamino group may be substituted by one or more substituents selected from the group consisting of: (vi) R2 and R5 are Halogen atom, C1
C6 alkyl group, carboxyl group which may be protected, hydroxyl group which may be protected, amino group which may be protected, C1-C6 which may be protected
Alkylamino group, optionally protected C1-C6 aminoalkyl group, optionally protected C1-C6 alkylamino C1-C6 alkyl group, optionally protected C1-C6 hydroxyalkyl group and C3-C6 And (vii) R3, R4,
When R5 and R6 are alkyl groups, the terminal represented by the alkyl group may be substituted by a C3-C8 cycloalkyl group) as the active ingredient. 2. The aryl group in (i), (ii) and (v) is a phenyl, tolyl, xylyl or naphthyl group, and the substituted cyclopentyl group in (iii) is a cyclopentylamino group or a cyclopentylcarbinol group. Wherein the substituted cyclohexyl group is a cyclohexylamino group, a cyclohexylaldehyde group or a cyclohexylacetic acid group, the substituted naphthyl group is a naphthylamino group or a naphthylaminosulfonic acid group, and the condensed polycyclic hydrocarbon in (iv). Compounds include pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-
Cyclopentacyclooctene or benzocyclooctene, wherein the heterocyclic compound is furan, thiophene,
The molecular function expression inhibitor according to claim 1, which is pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline. 3. The compound of the general formula 1 (Where (i) R1, R2, R3, R4, R5,
R6, R10 and R11 each independently represent a hydrogen atom; a halogen atom; a C1-C6 alkyl group; an amidino group;
-C8 cycloalkyl group; C1-C6 alkoxy C1-
C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bonded to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene rings; C1-C6 alkylene group; benzoyl group A cinnamyl group; a cinnamoyl group; or a furoyl group, and (ii) A is a hydrogen atom or Wherein R7 is a C1-C6 alkyl group; a sulfide group; or a phosphate group; R8 and R9 are each independently a hydrogen atom; a halogen atom; a linear or branched C1-C6 alkyl group; An allyl group; one or two aromatic rings selected from the group consisting of benzene, naphthalene and anthracene rings.
An aralkyl group to which the above C1-C6 alkyl group is bonded;
A benzoyl group; a cinnamyl group; a cinnamoyl group; or a furoyl group) (iii)
Any of R1, R2, R3 and R4 and / or R
5, R6, R10 and R11 may be a substituted or unsubstituted cyclopentyl group; a substituted or unsubstituted cyclohexyl group; or a substituted or unsubstituted naphthyl group; (iv) R5, R6, R10 and R11 are (V) R3, R4, R5, or a condensed polycyclic hydrocarbon compound or
R6, R10 and R11 represent a halogen atom, a cyano group,
A carboxyl group which may be protected, a hydroxyl group which may be protected, an amino group which may be protected, a C1-C6 alkyl group, a C1-C6 alkoxy group,
C1-C7 alkoxycarbonyl group, aryl group, C3
-C6 cycloalkyl group, C1-C6 acylamino group,
A C1-C6 acyloxy group, a C2-C6 alkenyl group,
C1 to C6 trihalogenoalkyl group, C1 to C6 alkylamino group and diC1 to C6 alkylamino group may be substituted by one or more substituents selected from the group consisting of: (vi) R2 and R5 are Halogen atom, C1
C6 alkyl group, carboxyl group which may be protected, hydroxyl group which may be protected, amino group which may be protected, C1-C6 which may be protected
Alkylamino group, optionally protected C1-C6 aminoalkyl group, optionally protected C1-C6 alkylamino C1-C6 alkyl group, optionally protected C1-C6 hydroxyalkyl group and C3-C6 And (vii) R3, R4,
When R5, R6, R10, and R11 are alkyl groups, the terminal of the alkyl group may be substituted with a C3-C8 cycloalkyl group), as an active ingredient. 4. The aryl group in (i), (ii) and (v) is a phenyl, tolyl, xylyl or naphthyl group, and the substituted cyclopentyl group in (iii) is a cyclopentylamino group or a cyclopentylcarbinol group. Wherein the substituted cyclohexyl group is a cyclohexylamino group, a cyclohexylaldehyde group or a cyclohexylacetic acid group, the substituted naphthyl group is a naphthylamino group or a naphthylaminosulfonic acid group, and the condensed polycyclic hydrocarbon in (iv). Compounds include pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-
Cyclopentacyclooctene or benzocyclooctene, wherein the heterocyclic compound is furan, thiophene,
The molecular function expression inhibitor according to claim 3, which is pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline. 5. General formula 2 (Wherein (i) R1, R2, R3, R4, R5 and R6 are each independently a hydrogen atom; a halogen atom; C1
An amidino group; a C3-C8 cycloalkyl group; a C1-C6 alkoxy C1-C6 alkyl group;
Aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bonded to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene rings; C1-C6 alkylene group; benzoyl group; cinnamyl group; A cinnamoyl group; or a furoyl group; (ii)
Any of R1, R2, R3 and R4 and / or R5
And R6 may be a substituted or unsubstituted cyclopentyl group; a substituted or unsubstituted cyclohexyl group; or a substituted or unsubstituted naphthyl group;
5 and R6 may combine with another condensed polycyclic hydrocarbon compound or a heterocyclic compound to form a ring, and (iv)
R3, R4, R5 and R6 each represent a halogen atom, a cyano group, an optionally protected carboxyl group, an optionally protected hydroxyl group, an optionally protected amino group, a C1-C6 alkyl group, C6 alkoxy group, C1-C7 alkoxycarbonyl group, aryl group,
A group consisting of a C3-C6 cycloalkyl group, a C1-C6 acylamino group, a C1-C6 acyloxy group, a C2-C6 alkenyl group, a C1-C6 trihalogenoalkyl group, a C1-C6 alkylamino group, and a di-C1-C6 alkylamino group May be substituted with one or more substituents selected from the group consisting of:
1-C6 alkyl group, optionally protected carboxyl group, optionally protected hydroxyl group, optionally protected amino group, optionally protected C1-C
6 alkylamino groups, optionally protected C1 to C6
One or more selected from the group consisting of an aminoalkyl group, an optionally protected C1-C6 alkylamino C1-C6 alkyl group, an optionally protected C1-C6 hydroxyalkyl group and a C3-C6 cycloalkylamino group (Vi) R3, R4,
When R5 and R6 are alkyl groups, the terminal represented by the alkyl group may be substituted by a C3-C8 cycloalkyl group) as the active ingredient. 6. The aryl group in (i) and (iv) is a phenyl, tolyl, xylyl or naphthyl group, and the substituted cyclopentyl group in (ii) is a cyclopentylamino group or a cyclopentylcarbinol group; The substituted cyclohexyl group is a cyclohexylamino group, a cyclohexylaldehyde group or a cyclohexylacetic acid group, the substituted naphthyl group is a naphthylamino group or a naphthylaminosulfonic acid group, and the condensed polycyclic hydrocarbon compound in (iii) is pentalene. , Indene, naphthalene, azulene, heptalene,
Biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-
Cyclopentacyclooctene or benzocyclooctene, wherein the heterocyclic compound is furan, thiophene,
The molecular function expression inhibitor according to claim 5, which is pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline. 7. A of the general formula 3 (Wherein (i) R3, R4, R5 and R6 each independently represent a hydrogen atom; a halogen atom; a C1-C6 alkyl group; an amidino group; a C3-C8 cycloalkyl group;
-C6 alkoxy C1-C6 alkyl group; aryl group;
An allyl group; an aromatic ring selected from the group consisting of benzene, naphthalene, and anthracene rings;
An aralkyl group having a 1-C6 alkyl group bonded thereto;
A benzoyl group; a cinnamyl group; a cinnamoyl group; or a furoyl group, and (ii) R3 and R4.
And / or any of R5 and R6 may be a substituted or unsubstituted cyclopentyl group; a substituted or unsubstituted cyclohexyl group; or a substituted or unsubstituted naphthyl group; (iii) R5 and R6 are other fused It may combine with a polycyclic hydrocarbon compound or a heterocyclic compound to form a ring, and (iv) R3, R4, R5 and R6
Is a halogen atom, a cyano group, an optionally protected carboxyl group, an optionally protected hydroxyl group,
An optionally protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxycarbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group and di-C1
(V) R5 may be substituted with one or more substituents selected from the group consisting of
Is a halogen atom, a C1-C6 alkyl group, an optionally protected carboxyl group, an optionally protected hydroxyl group, an optionally protected amino group, an optionally protected C1-C6 alkylamino group An optionally protected C1-C6 aminoalkyl group, an optionally protected C1-C6 alkylamino C1-C6 alkyl group, an optionally protected C1-C6 hydroxyalkyl group and a C3-C6 cycloalkylamino And (vi) when R3, R4, R5 and R6 are alkyl groups, the terminal of the alkyl group is a C3-C8 cycloalkyl. A compound represented by the formula (1) which may be substituted by a group): 8. The aryl group in (i) and (iv) is a phenyl, tolyl, xylyl or naphthyl group; the substituted cyclopentyl group in (ii) is a cyclopentylamino group or a cyclopentylcarbinol group; The substituted cyclohexyl group is a cyclohexylamino group, a cyclohexylaldehyde group or a cyclohexylacetic acid group, the substituted naphthyl group is a naphthylamino group or a naphthylaminosulfonic acid group, and the condensed polycyclic hydrocarbon compound in (iii) is pentalene. , Indene, naphthalene, azulene, heptalene,
Biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-
Cyclopentacyclooctene or benzocyclooctene, wherein the heterocyclic compound is furan, thiophene,
The molecular function expression inhibitor according to claim 7, which is pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline. 9. The method according to claim 7, wherein R3, R4, R5, and R6 are hydrogen atoms. 10. The b of the general formula 3 (Wherein (i) R3, R4, R5 and R6 each independently represent a hydrogen atom; a halogen atom; a C1-C6 alkyl group; an amidino group; a C3-C8 cycloalkyl group;
-C6 alkoxy C1-C6 alkyl group; aryl group;
An allyl group; an aromatic ring selected from the group consisting of benzene, naphthalene, and anthracene rings;
An aralkyl group having a 1-C6 alkyl group bonded thereto;
A benzoyl group; a cinnamyl group; a cinnamoyl group; or a furoyl group, and (ii) R3 and R4.
And / or any of R5 and R6 may be a substituted or unsubstituted cyclopentyl group; a substituted or unsubstituted cyclohexyl group; or a substituted or unsubstituted naphthyl group; (iii) R5 and R6 are other fused It may combine with a polycyclic hydrocarbon compound or a heterocyclic compound to form a ring, and (iv) R3, R4, R5 and R6
Is a halogen atom, a cyano group, an optionally protected carboxyl group, an optionally protected hydroxyl group,
An optionally protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxycarbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group and di-C1
(V) R5 may be substituted with one or more substituents selected from the group consisting of
Is a halogen atom, a C1-C6 alkyl group, an optionally protected carboxyl group, an optionally protected hydroxyl group, an optionally protected amino group, an optionally protected C1-C6 alkylamino group An optionally protected C1-C6 aminoalkyl group, an optionally protected C1-C6 alkylamino C1-C6 alkyl group, an optionally protected C1-C6 hydroxyalkyl group and a C3-C6 cycloalkylamino And (vi) when R3, R4, R5 and R6 are alkyl groups, the terminal of the alkyl group is a C3-C8 cycloalkyl. A compound represented by the formula (1) which may be substituted by a group): 11. The aryl group in (i) and (iv) is a phenyl, tolyl, xylyl or naphthyl group, and the substituted cyclopentyl group in (ii) is a cyclopentylamino group or a cyclopentylcarbinol group, The substituted cyclohexyl group is a cyclohexylamino group, a cyclohexylaldehyde group or a cyclohexylacetic acid group, the substituted naphthyl group is a naphthylamino group or a naphthylaminosulfonic acid group, and the condensed polycyclic hydrocarbon compound in (iii) is pentalene. , Indene, naphthalene, azulene, heptalene,
Biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-
Cyclopentacyclooctene or benzocyclooctene, wherein the heterocyclic compound is furan, thiophene,
The molecular function expression inhibitor according to claim 10, which is pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline. 12. The molecular expression-suppressing agent according to claim 1, which is an antibacterial agent. 13. The molecular expression function inhibitor according to claim 1, which is an antifungal agent. 14. The method according to claim 1, which is an antiviral agent.
3. The molecule expression function-suppressing agent according to 1.). 15. The molecular expression function inhibitor according to claim 1, which is a germicidal disinfectant. 16. The inhibitor according to claim 1, which is an anticancer agent. 17. The agent according to claim 1, which is a blood coagulation / fibrinolysis inhibitor or inhibitor. 18. The agent according to claim 1, which is an antigen-antibody reaction inhibitor or an inhibitor. 19. The composition according to claim 1, which is an organ tissue preservative.
2. The molecule expression function inhibitor according to 1. 20. The agent for suppressing a function of expressing a molecule according to claim 1, which is a preservative. 21. The molecular expression function-suppressing agent according to claim 1, which is a labeling reagent in which at least one substituent has a substance serving as a label indicating an action site as a substituent. 22. The molecule expression function inhibitor according to claim 1, which is a reducing agent. 23. The molecule expression function inhibitor according to claim 1, which is a free radical scavenger. 24. The method according to claim 1, which is a desulfidizing agent.
2. The molecule expression function inhibitor according to 1. 25. The molecular expression function inhibitor according to claim 1, which is a depolymerizing agent. 26. The method according to claim 1, which is a surfactant.
2. The molecule expression function inhibitor according to 1. 27. The agent according to claim 1, which is a spermicide or an external contraceptive. 28. The molecule expression function inhibitor according to claim 1, which is a thrombolytic agent. 29. The method according to claim 1, which is a sugar chain coordination changing agent.
2. The molecule expression function inhibitor according to 1. 30. The method according to claim 1, which is an arteriosclerosis inhibitor.
2. The molecule expression function inhibitor according to 1. 31. The molecular expression function inhibitor according to claim 1, which is a metabolism (lipid, sugar, protein) improver. 32. The inhibitor of molecular expression function according to claim 1, which is an agent for promoting wound healing and epithelial formation (including a hair-growth effect). 33. The inhibitor for inhibiting the function of expressing a molecule according to claim 1, which is a phase transition agent or a phase transition property improving agent. 34. The molecular expression function inhibitor according to claim 1, which is a microphase separation structure improving agent. 35. The molecular expression-suppressing agent according to claim 1, which is a plasticizer or a plasticity improving agent. 36. The molecular expression function inhibitor according to claim 1, which is a copolymerizing agent or a copolymerizing improver. 37. The molecular expression function inhibitor according to claim 1, which is a polymerization control agent or a polymerization control improvement agent. 38. The molecular expression function inhibitor according to claim 1, which is a stabilizer or a stabilization improving agent. 39. The molecular expression function inhibitor according to claim 1, which is an antioxidant or an antioxidant. 40. The molecular expression-suppressing agent according to claim 1, which is an amorphous agent or an amorphous modifier. 41. The method according to claim 1, which is a flow property improving agent.
2. The molecule expression function inhibitor according to 1. 42. The molecular expression function inhibitor according to claim 1, which is a softening agent or a softening improving agent. 43. The molecular expression-suppressing agent according to claim 1, which is a modulator or an improver of a fluorescent wavelength of a dye, a paint, a pigment, or a colorant. 44. The agent for suppressing a function of expressing a molecule according to claim 1, which is an agent for improving physical properties or a function of a low-molecular substance. 45. The molecular expression-suppressing agent according to claim 1, which is a physical property or function improving agent for a polymer substance. 46. The molecular expression-suppressing agent according to claim 1, which is a physical property improving agent for a polymer composite material or a functional polymer composite material.