Inhibitory or blocking agents of molecular generating and/or inducing functions

Abstract

A method for inhibiting or blocking molecular generating and / or inducing functions of molecules using an inhibitory or blocking agent of the formula: wherein R1-6 are as defined herein.

Description

[0001] This application is a continuation of application Ser. No. 10 / 718,854, filed Nov. 24, 2003, now abandoned, which is a division of application Ser. No. 10 / 029,259, filed Dec. 28, 2001, now U.S. Pat. No. 6,710,090, which is a division of application Ser. No. 08 / 813,842, filed Mar. 7, 1997, now U.S. Pat. No. 6,346,551, which is a continuation of international application PCT / JP95 / 01783, filed Jul. 9, 1995, now abandoned, which claims priority of Japanese patent application No. 6-252660, filed Sep. 9, 1994, all of which are incorporated herein by reference.TECHNICAL FIELD [0002] This invention relates to compounds which have inhibitory effect or blocking effects on substrates (for example, lipids, carbohydrates, amino acids) of less than 10000 of molecular weight which has constituted structure and function of organism fundamentally and, function which is generated by macromolecules such as peptides, proteins, enzymes, nucleic acids and genes (DNA, tRNA, mRNA, rRNA) which are syn...

AI Technical Summary

Benefits of technology

[0032] The invention mentioned on claims 25-46 provides depolymerization agents, improving agents for surface active substances, spermatocidal agents and / or contraceptive agents for external use, thrombolytic agents, conformation altering agents of saccharide-chains, agents for preventing arteriosclerosis, metabolism (lipids, sugar) improving agents, agents for wound healing, epithelialization promoting agents, phase transition agents, improving agents of phase transition, improving agents of microphase separation structure, plasticity and / or elasticity promoting agents, plasticity and / or elasticity improving agents (plasticizers), copolymerization agents, copolymerization improving agents, polymerization regulators, improving agents of polymerization adjustment, stabilizers, stabilization improving agents, antioxidants, oxidation preventing agents, improving agents of crystallized materials and / or amorphous materials, fluidability improving agents, flexibility promoters (softers), improving agents for changing flexibility (softener improving agents), improving agents of excitation wavelength and fluorescent wavelength of colorants, pigmentums, coating materials and cosmetic pigments, and alterable agents of excitation wavelength and fluorescent wavelength of pigmentums, coating materials and cosmetic pigments, agents which can improve physical property of low molecule substances, agents which can improve function of low molecule substances, agents which can improve physical property of macromolecules substance, agents which can improve function of macromolecules substances, agents which can improve physical property of macromolecules composite materials and functional macromolecules composite materials.

[0039] Moreover, protecting substituent of amino group, amino lower alkyl group, lower alkylamino group, and lower alkylamino lower alkyl group may be a pharmaceutically acceptable amino-protecting group which is easily detached in an organism.

[0040] In addition, protecting substituent of hydroxyl group and hydroxy lower alkyl group may be a pharmaceutically acceptable protecting group of hydroxyl group which is easily detached in an organism.

[0043] The compounds provided in this invention can be directly applied on the surface of infected wound such as burn and decubitus. And, those can be used by combining with the carrier substances which are allowable on pharmaceutic use. In addition, when it is applied to living space, environment and at industry, those can be used during and / or after manufacturing step of materials according to the objective. Though it is not restricted to representative applications, it is also possible to be added those compounds on any manufacturing steps of surface processing by attaching, painting or spraying as agents to prevent bacterial and fungal proliferation and / or infection for construction materials, furnitures, lavatory goods, bathtub supplies, washing supplies, house holding electric instruments and / or daily use goods. Moreover, when those compounds are utilized in a thread kneading and / or later processing concerning any step of manufacturing fibers and these materials, effect of preventing bacterial and fungal proliferation and / or infection and an anti-allergic effect can be gained. An effect of the objective which is shown by claims can be made by using seats and film materials.

[0045] In addition, when the compounds mentioned in this invention are used as combined substances with the carrier substances which are allowable on pharmaceutic use, these can be applied in many kinds of the generally known agent types such as cream agents, ointments, pastes, poultices, milky lotions, suspensions, liniments, lotions, aerosol agents, solutions and tapes corresponding to prospected treatments. Also, it is allowed to add solvent supporting agents, isotonic changing agents, pH adjusters, deodorants, antiseptics or odorants in the compounds mentioned in this invention. It is also possible to be added those compounds on any manufacturing steps of surface processing by attaching, painting or spraying as agents to prevent bacterial and fungal proliferation and / or infection for construction materials, furnitures, lavatory goods, bathtub supplies, washing supplies, house holding electric instruments and / or daily use goods. Moreover, when those compounds are utilized in the thread kneading and / or later processing concerning any step of manufacturing fibers and these materials, effect of preventing bacterial and fungal proliferation and / or infection and an anti-allergic effect can be gained. An effect of the objective can be made as wall papers and filters by using seat and film material. When it is used as spermatocidal agents and contraceptive agents for external use, it is also possible to process surface of contraceptive possession such as condoms as well as ointments and creams.

[0559] Also, a sterilizing effect can be obtained by adding the compounds into water of humidifier and on any part of circulation circuits of air-conditioning device. In addition, when the compounds in this invention composition are used as depolymerization agents, improving agents for surface active substances, reductants, free radical scavengers, desulfurization agents, phase transition agents, improving agents of phase transition, improving agents of microphase separation structure, promoting agents for plasticity and / or elasticity, improving agent for plasticity and / or elasticity, copolymerization agents, copolymerization improving agents, polymerization regulators, improving agents for polymerization adjustment, stabilizers, antioxidants, improving agents for crystallized materials and / or amorphous materials, flexibility promoters and / or improving agents for changing in flexibility, those compounds can effectively control, inhibit and / or generate an objective property of substances by using as a single substance and / or a combination with adequate carriers. When the compounds in this invention are used as modulators or improving agents for fluorescent wavelength and excitation wavelength of pigmentums, coating materials, cosmetic pigments or colorants, improving agents of physical property with low molecule substance, improving agents of function with low molecule substance, improving agents of physical property of macromolecules substance, improving agents of function with macromolecules substance and / or improving agents of physical property with macromolecules composite materials and functional macromolecules composite materials, those compounds can effectively control, inhibit and / or generate an objective property with substances by using as a single substance and / or a combination with adequate carriers. Concretely, an improvement of efficiencies can be planned by selecting a mixing ratio with macromolecules substances, a churning temperature, an adjusting energy quantity such as protons and radio waves and / or transition metals.

Problems solved by technology

On the other hand, it is also known that a hindrance of those adjustment capability causes onset of diseases in human being.

Though it is not necessary to do more than to read history of relationship between a man and diseases, a fighting to pathogenic microbacterial infection such as bacteria and virus, it is serious problems which needs a medical resolution.

And, even though development of advanced medical technology, it is a serious problem that multiple organ failure accompanied with sepsis and disseminated intravascular coagulation causes to result in the death of human being (Hypotension—for clinician to understanding pathophysiology—Fujita Publ. by Koyama) <ref.

However, while development of antibacterial agents is noticeable, application of drugs concurs at an appearance of a resistant strain and, a social administrative problem as well as difficulties of medical care has been raised.

In order to show resistance to lots of beta-lactam group drugs in staphylococcus aureus, a treatment for infectious disease due to MRSA is difficult and, it becomes pathogenic organism such as opportunistic infection and postoperative infection in clinical practices and, an infected patient to this MRSA changes a serious illness and, he is easy to fall into sepsis and multiple organ failure.

Thus, onset of untreatable infection due to MRSA is a serious social issue.

From a point of related view with cystic pulmonary fibrosis, recently, an approach to preventing this infection of pseudomonas aeruginosa is a great problem.

In addition, infection of acid-fast bacteria and mycete is international problems as for an infectious complication whose acquired immune deficient syndrome (AIDS) is fatal.

However, though it is expected that a substance with simple chemical structure can inhibit and / or block the function generated or induced by the multi-dimensional structure of biological substances, there is not proposal of such representative substance, which is little harm and safety, concerning life continuation as integrated whole body at the present.

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