225 results about "Antifungal drugs" patented technology

The invention aims at providing chemical synthesis and preparation of an aromatic heterocyclic pyridine and the analogs thereof to obtain derivatives and analogs of a plurality of series of aromatic heterocyclic pyridine and medicinal salts or salts having the following formulas or prodrugs, and the preparation, a pharmacologically activity experimental method and pharmacologically activity thereof are provided. The definitions of dotted line, ring A, ring B, X1, X2, X3, X4, R1, R2 and R3 in formula I are shown in the description. The invention provides the aromatic heterocyclic pyridine derivatives and analogue with antibacterial and antifungal activities, also provides the application thereof as antibacterial and antifungal drugs and the application thereof in concomitant use with other known antibacterial and antifungal drugs and with drugs for curing bacteria infection coupled with various complicating diseases such as inflammation, virus, immune system diseases and the like, and also provides the preparation method of the aromatic heterocyclic pyridine analogs.

Since treatment effects of conventional external preparations were not satisfactory, it is aimed to provide a novel external preparation that is excellent in drug permeability to nail, capable of fully exhibiting effects of an antifungal drug, and effective for treatments of diseases such as nail mycosis and nail candidiasis, particularly, treatments for nail tinea. The external preparation of this invention is a pharmaceutical composition for nail characterized by containing an antifungal drug, alkylpyrrolidone or a derivative thereof, and a crosslinking hydrogel.

The invention belongs to the organic chemical field and relates to a method for preparing a medical compound chlorphenesin; wherein, the chlorphenesin belongs to an antifungal drug. For more than ten years, the product is internationally applied in necessities, such as medical soaps, soaps, ointments, nail polishes, etc. The product is also an intermediate product for preparing chlorphenesin carbamate. The invention has the advantages of easy preparation method and technique operation, easy industrialized production, high safety and stable product quality.

The invention discloses quinolone azole alcohol compounds which are shown in a general formula (I) and the structure of an intermediate (II) and has antimicrobial activity and a preparation method of pharmaceutically acceptable salts of the compounds. The invention also relates to application of the quinolone azole alcohol compounds and salts thereof as anti-infection medicines. According to the invention, the related preparation raw materials are high in commercialization degree, cheap and easily available, the preparation route is short, and the preparation method is simple and convenient. The quinolone azole alcohol compounds have certain inhibitory activity to gram-positive bacteria, gram-negative bacteria and fungi and can be used for preparing an antibacterial and / or antifungal drug. R1, R2, R3, R4, X and Im in the general molecular formula are defined in the claims.

The invention relates to a submicroemulsion antifungal drug spray preparation. The preparation mainly comprises the following components: an antifungal chemical synthetic drug, lecithin serving as an emulsifier, a transdermal absorption penetration enhancer and a skin protectant, soybean oil or other essential oils serving as an oil soluble diluent, glycerin serving as an isoosmotic adjusting agent, oleic acid serving as a co-emulsifier and a transdermal absorption penetration enhancer, azone serving as a transdermal absorption penetration enhancer, vitamin E serving as an antioxidant and a skin protectant, ethyl alcohol serving as a transdermal absorption penetration enhancer, natural essential oil serving as a transdermal absorption penetration enhancer, an antibacterial natural drug and essence. The submicroemulsion antifungal drug spray preparation has the advantages that the solubility and the uniformity of oil soluble antifungal drugs in water are increased, the transdermal absorption of the drugs is enhanced, the drugs are fed into dermis, and the absorption and utilization ratios of the drugs are increased, so that the effects of the antifungal drugs are increased; in the meantime, a cosolvent with side effects is avoided from being used, so that toxic and side effects caused by drugs entering whole body blood circulation systems and the stimulation to the skin are reduced, and the efficacies of protecting the skin and improving the looks are provided.

The invention relates to the medical technical field, in particular to a new triazole alcohols antifungal compound and salts thereof with the following chemical structure formula and a preparation method and the application thereof; R1 is selected from n-propyl, isopropyl or butyl; R2 is selected from alkyl or halogen; the salts include hydrochloride, hydrobromide and methane sulphonate. The compound has strong antifungal activity on various fungi in shallow parts and deep parts. Compared with the antifungal medicines used in the existing clinical applications, the compound has the advantages of high efficiency, low toxicity, broad antifungal spectrum, and the like, and can be used for preparing new antifungal medicines.

The present invention belongs to the field of medicine synthesis technology, and is especially 1- (3-indolyl)-1, 2, 3, 4-tetrahydro-beta-carboline compounds and analogs in the general expression as shown and with substituted hydroxyl radical or acyl radical in the 2nd position, and their preparation process and medical application. Initial pharmacodynamic research of extracorporeal rice blast mold resisting experiment and extracorporeal antitumor experiment shows that these compounds has excellent antifungal activity and antitumor activity, so that they may be developed into antifungal medicine and antitumor medicine.

In a pharmaceutical composition for external use containing a compound such as luliconazole and / or a salt thereof in an amount of 5% by mass or more, comprised is / are acetone, a polyoxyethylene alkyl (having 8 to 30 carbon atoms) ether, and / or a polyoxyethylene alkenyl (having 8 to 30 carbon atoms) ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrrolidone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and / or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and / or a salt thereof produced under a preservation condition of 60° C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and / or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5° C. for 2 weeks after manufacture.

The invention relates to a preparation method and an application of aloe emodin azole compounds, belonging to the technical field of chemical synthesis. The aloe emodin azole compounds are representedas the general formulas I-V and have high biological activity and have shown great development value and broad application prospect in the field of bio-organic pharmaceutical chemistry, antimicrobialactivity test in vitro shows that these compounds have certain inhibitory activity on one or more of gram-positive bacteria, gram-negative bacteria and fungi, these compounds can be used to prepare anti-bacterial and / or anti-fungal drugs, thus providing an opportunity to provide more safe, efficient and diversified candidate drugs for clinical antimicrobial therapy, and helping to solve the increasingly serious clinical treatment problems of drug resistance, persistent pathogenic microorganisms and emerging harmful microorganisms. Its preparation material is simple, cheap and easy to obtain,the synthesis route is short, and the application of anti-infection has important significance.

The invention discloses antifungal application of fraxetin, belonging to the technical field of medicines. In-vitro experiments show that fraxetin has relatively good inhibition effect to the fungi, is capable of restoring the effect of an antifungal drug, namely fluconazole to drug-resistant fungi and therefore can be taken as the antifungal drug and a synergist for the antifungal drug. Accordingto the antifungal application, the new use of fraxetin is opened up, fraxetin is used as the antifungal drug and the synergist for the antifungal drug, a new candidate drug is provided for the fungustreatment, and the antifungal effects of existing drugs are improved. Under the conditions that clinical fungus drug resistance becomes common increasingly and the drug resistance level becomes serious increasingly, the effect of an antifungal drug to the drug-resistant fungi is restored, and the use dosage of the antifungal drug is reduced, so that the medical expense of a patient is saved, andthe toxic and side effects of the drugs are reduced.

The invention relates to the technical field of medicine and discloses 2-substituted benzopyran-4-one compounds with a structure shown in general formula I and an application of the compounds in preparation of antifungal drugs and synergistic antifungal drugs. The compounds can be jointly used with azole antifungal drugs, can improve sensibility of drug-resistance bacteria to the azole drugs, reverses drug resistance and produces a synergistic antifungal function.

The invention provides a novel highly-efficient, low-toxic, broad-spectrum antifungal azole alcohole compound to substitute for phenoxyalkylamine triadimenol compounds, namely1-(1H-1,2,4- triazole-1-group)-2-(2,4-difluoro phenyl)-3-(N-substitute for phenoxyalkylamine)-2-propanol compounds (including racemic body and R or S type isomer of the compounds) and hydrochloride, nitrate, hydrobromide andmethane sulphonate of the compounds, and a preparation method thereof. The compound has strong antifungal effect on various funguses in shallow and deep parts. Compared with the prior antifungal medicines applied in clinical practice, the compound has the advantages of high efficiency, low toxin and broad antifungal spectrum, and can be used for preparing novel antifungal medicines.

The invention discloses ketene-bridged berberine azole derivatives with structures in general formulas I-VII and medicinal salts thereof. The compounds have certain inhibitory activity on gram positive bacteria, gram negative bacteria and fungi, can be used for preparing antibacterial / antifungal drugs, and can also be used for preparing DNA- cleavage agents and intercalators. The preparation raw materials are high in commercial degree and are cheap and available, the preparation route is short, and the method is simple and convenient. The general formulas are as shown in the specification.

The invention provides an antifungal drug composition for external use, and a preparation method of an external preparation, and application of the composition in treating superficial fungal infections, such as tinea manus and pedis, tinea corporis, tinea cruris, tinea unguium, tinea versicolor and oidiomycosis cutis. The drug composition contains terbinafine or pharmaceutical salt thereof, sertaconazole or pharmaceutical salt thereof, and any one or multiple pharmaceutically acceptable excipient. An experimental study shows that the terbinafine or pharmaceutical salt thereof and the sertaconazole or pharmaceutical salt thereof have obvious synergistic effect when the proportion thereof in the drug composition for treating the superficial fungal infections is (1: 10) to (5: 1)(w / w). The antifungal drug composition for treating the superficial fungal infections has the advantages of being good in security, excellent in curative effect, short in treatment course, high in curing rate, low in relapse rate and the like.

The invention relates to the technical field of medicines and discloses an indoletriazole alkaloid antifungal compound with a novel framework, i.e. fructus evodiae triazole alkali (3-[2-N-methyianiline]-triazolo[4,3-a]-3,4-dihydto-beta-carboline) which is a compound with a brand-new framework. The invention also relates to a preparation method and application of the indoletriazole alkaloid antifungal in the field of medicines. Particularly, the compound has strong antifungal activity, and compared with the antifungal medicaments clinically applied at present, the compound has the advantages of high efficiency, low toxicity, broad antifungal spectrum, and the like, opens a new approach for deeply researching and developing new antifungal medicaments and can be used for preparing new antifungal medicaments.

The present invention is directed to new nanosuspensions of antifungal azole derivatives, particularly itraconazole, with with improved impurity profile optimized for inhaled administration for the prevention, reversal and medical treatment of fungal infections of the respiratory tract including adjacent lymph nodes. The new formulation which is devoid of particulate inorganic contamination can be safely administered by inhalation. This administration route results in an improved therapeutic effect and reduced side effect profile as compared to the previously used clinical administration route, i.e. oral or parenteral (intravenous) administration.

The present invention provides one new gene MgKIN17 from Pyricularia gisea, and the gene features that it has the amino acid sequence from the site 1 to the site 3544 in the SEQ ID No. 1, the cDNA with the nucleotide sequence of SEQ ID No. 2, the promoter with the nucleotide sequence of SEQ ID No. 4, and coded protein with the amino acid sequence of SEQ ID No. 3. The insertion mutation and gene complementation of the present invention shows that the destruction of the gene leads the formation of Pyricularia gisea infecting organ and reduced lesion capacity of rice. Wheat bakanae fungus, corn stalk rot and other pathogenic fungus have homogenous protein with homogeneity over 40 % to MgKIN17 and maybe similar biological function. The gene of the present invention and its protein expression and modification may be used as the target site for designing and screening antifungal medicines.

The invention relates to the technical field of medicine, and provides substituted tricyclo-quinone compounds and pharmaceutically acceptable salts thereof. The structural general formula of the substituted aromatic tetracyclic compounds is disclosed in the specification. The invention also provides a preparation method of the compounds and application of the compounds in preparation of antifungal drugs.

The invention discloses a terbinafine nanometer antifungal which is prepared by terbinafine, oil, surfactant, water according to the following method: First, the said raw materials are unloaded and weighed and reserved, then surfactants and oil is blended and mixed; terbinafine is added into cosurfactant and completely dissolved; the solution with terbinafine dissolved in it is added to the homogeneous mixed surfactant and oil, stirring uniform, finally, distilled water is slowly added dropwise, dropwising and stirring until the stable, homogeneous, transparent terbinafine nanometer antifungal is obtained. The drug with small particles, small viscosity, good fluidity and good nature stability, can reach through the skin and get into the blood circulation, inhibit squalene cycloxygenase, so as to treat the dermatophyte infection and many deep mycotic infection with a drastic therapeutic effect, and what is more the preparation of the invented products is simple, low energy consumption and without special equipment the drug can be mass produced.

The invention relates to the technical field of medicine and particularly discloses a 3-substituted propyl-2-alkene-1-ketone compound and application thereof to preparation of antifungal drugs and synergistic antifungal drugs. The compound can be used together with azole type antifungal drugs and improve sensibility of drug-resistance bacteria to the azole type antifungal drugs, so that the reversing drug-resistance effect is achieved, and the synergistic antifungal effect is generated.

The invention relates to a substituted triazolone benzyl amine triazole antifungal compound, i.e. 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[N-methyl-N-(2-substituted-2H-1,2,4-triazol-3-one-4-yl) benzylaminoformyl]-2-propanols compounds, their salts and their preparation process. The compounds has very strong antimycotic effect.

The invention relates to a Polyrhachis vicina extractive and antifungal medical purpose thereof. Specifically, the invention relates to a traditional Chinese medicine Polyrhachis vicina extractive with function of controlling fungal infection diseases, and a preparation method and medical purpose thereof in preparation of antifungal drugs. The Polyrhachis vicina extractive provided by the invention is prepared by organic solvent immersion and extraction on dried bodies of Polyrhachis vicina. The extractive has significant activity on inhibiting the growth of Candida albicans, and can be prepared into tablets, granules, capsules, pills, an oral liquid, dripping pills, a coating agent, an external liniment, a film agent, an ointment, a spraying agent, an injection, a transdermal patch and an aerosol, and used in the preparation of medicines, daily chemical products or medical devices for prevention and treatment of fungal infections.

The invention relates to the technical field of antimycotic medicaments, specifically to a liranaftate and mometasone furoate containing locally applied compound pharmaceutical composition, which contains one or more acceptable auxiliary materials for local application. The invention is characterized in that the weight ratio of liranaftate to mometasone furoate is 1:80-80:1; the balance contains matrix auxiliary materials; The pharmaceutical composition can be emulsifiable paste or ointment, gelata, a solution or an emulsion or a suspension, a coating agent, aerosol or a spraying agent or spray-film, a foaming agent and patch. With the application of the liranaftate and mometasone furoate compound pharmaceutical composition, as mometasone furoate has a vasoconstriction effect, the transdermal absorption rate of liranaftate slows down, local skin tissue concentration of liranaftate is increased, the medicament is minimized to penetrate through the skin into blood, and local skin concentration of the antimycotic medicament is maintained for a longer time.

The invention relates to a new preparation method for chitin deacetylase (chitin deacetylase, E.C.3.5.1.41, CDA), which comprises the following steps: shrimp-shell cultivated soil is taken as screened raw material; antifungal drug is used for restraining the growth of fungus; methods such as spread-plate, plate streaking and the like are used for purification; simultaneously N-paranitroacetanilide (PN)-casein plate is used for CDA activity verification; and finally bacillus cereous which can secrete CDA is obtained by separation. CDA is prepared by liquid fermentation; the CDA vitality of fermentation liquor supernatant is 0.598 to 0.912U / ml; the CDA has enzyme properties which are different from that reported in literatures. Bacillus cereous is used for secreting CDA to ectoenzyme; products are more easily obtained; and bacterium is suitable for large-scale industrial fermentation and can be applied without needing processing and transformation.

The invention relates to a compound ear drop for treating otitis externa mycotica, in particular to an ear drop for treating otitis externa mycotica. The drop is prepared by the the following ingredients: 3-30g of fluconazol, 5-50g of tinidazole, 3-30g of menthol, 100-800g of glycerine, 30-200ml of alcohol, 5-100ml of 1mol / L sodium hydroxide solution, and 1000ml of distilled water. The drop contains both antifungal drug and antianaerobic drug which enable the ear drop to have both antifungal activity and antianaerobic activity. In the process of preparation allocation, the tinidazole being slightly soluble into water need be heated by aqueous bath to be dissolved, the fluconazol and the menthol are easily dissolved into the alcohol. The alcohol is used for not only dissovling both the fluconazol and the menthol, but also being taken a transdermal accelerant of the ear drop, as well as drying the external acoustic meatus. The menthol can dispel wind to make the skin and the membrana mucosa cool and relieve the complaint and pain. A fixed amount of glycerine can protect the ear mucosa and keep the preparation tensile and adhesive.

The invention belongs to the technical field of antifungal action medicine and provides pyrazole derivatives of the structure in the general formula I and pharmaceutically acceptable salts thereof. The definition of R is stated as in a specification. The invention also relates to a preparation method of the compounds and discloses a pharmaceutical composition which takes the compounds and the pharmaceutically acceptable salts as effective active components and the application in antifungal medicine.

The invention relates to a preparation method of butoconazole. The method comprises the following specific steps: converting a raw material p-chlorobenzyl chloride into a Grignard reagent, reacting with chloro epoxypropane to obtain 1-4-chloro-p-chlorophenyl butanol-2, introducing imidazole, converting the hydroxyl into chlorine, introducing 2,6-dichloro thiophenol to obtain butoconazole, and acidifying with nitric acid to obtain butoconazole nitrate. The preparation method of butoconazole is simple in manufacture and low in production cost, and the butoconazole is an antifungal drug highly effective in the infection of Candida albicans and Candida albicans.

The invention relates to the technical field of medicines and is a new utilization of 10-bit substituting camplotheca acumiate fruit alkaline compound and the usage as a medicine. The compound structure of the invention is as indicated by a general formulation (I), which comprises the racemic mixture of the compound and an enantiomer of every compound. The compound of the invention has the function of inhibiting topoisomerase, has antitumor activity, antifungal activity and antibacterial activity, can be used as a topoisomerase inhibiter and can be used for preparing antitumor medicine, antifungal medicine and antibacterial medicine.