71 results about "Azole antifungal" patented technology

Water soluble prodrugs of azole antifungal agents are provided by quaternizing a nitrogen atom of the azole ring with a phosphonooxymethyl group.

The present invention relates to a method and composition of an oral preparation of itraconazole, an excellent azole antifungal drug. More particularly, it relates to an oral preparation of itraconazole having improved bioavailability, which is prepared by following steps of: i) dissolving itraconazole and bydrophilic polymer with solvent, ii) spray-drying said mixture, and iii) preparing the solid dispersions for oral preparation. The solid dispersions prepared in this invention may be useful in preparing tablets, granules and other oral dosage forms.

Formulations of azole antifungals such as itraconazole and particularly formulations, co-formulations and compositions of itraconazole with one or more oligomeric and/or polymeric excipients are disclosed. Methods for preparation of the formulations, co-formulations and compositions include co-precipitating the two materials from a common solvent or solvent mixture using a compressed (typically supercritical or near-critical) fluid anti-solvent as in the GAS (Gas Anti-Solvent) precipitation method. The formulations, co-formulations, compositions, methods of making and methods of delivering, are useful as pharmaceutical compositions and in medical treatment by virtue of their at least parity, preferably improved or enhanced solubility or dissolution characteristics, resulting in at least parity, preferably improved or enhanced bioavailability and/or pharmacokinetics.

The present invention provides a solid molecularly dispersed composition comprising a poorly water soluble and weakly basic azole antifungal compound and a pH sensitive polymer, pharmaceutical compositions, comprising the solid molecularly dispersed composition of the invention and methods of treating and/or preventing a fungal infection in a patient in need thereof comprising orally administering a pharmaceutical composition comprising a composition of the invention to a patient in need thereof. Preferably the antifungal, compound is posaconazole, and the pH sensitive polymer is HPMCAS.

The invention pertains to the technical field of medicaments, more particularly relates to a (sulfur) urea derivative with substituted semicarbazone thiochromanones and provides a novel and efficient antifungal agent. The structural formula of the derivative is shown as the Formula I. The invention also relates to a chemically acceptable compound of the derivative and a medicament combination taking the compound as an active ingredient. As a novel antifungal agent, the compound has relatively strong effect of killing pathomycete commonly seen clinically and is expected to overcome the defects that azoles antifungal medicaments widely used in clinical treatment has serious toxic side effect and is easy to generate medicament resistance, and the like. The compound is prepared by the condensation of substitutable thiochromanones and substitutable semicarbazone (sulfur) in an organic solvent.

The present invention relates to medicine technology and is especially new use of baicalein, which is one kind of effective components extracted from skullcap root and has been used in treating various kinds of inflammation, as antifungal medicine synergist. Baicalein is added into antifungal pyrrole medicine in the added amount of 4-16 mcg/ml. Experiments show that adding baicalein into antifungal medicine of fluconazole, ketocanazole, miconazole, etc can ensure the treating effect on fungal inflection and resist the drug tolerance of drug resisting fungi, so that baicalein may be used as the synergist of antifungal medicine.

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 present invention relates generally to the fields of bacteriology and mycology. More particularly, the present invention provides novel inhibitors of multidrug transport proteins that may be used in combination with existing antibacterial agent and/or antifungal agents to increase the toxic effects of the antimicrobial agents. More specifically the present invention provides methods and compositions for enhancing the antibacterial action of fluoroquinolones by administering fluoroquinolones in combination with an inhibitor of multidrug transporters and of enhancing the antifungal action of azole antifungal agents by administering an azole antifungal agent in combination with an inhibitor of multidrug transporters. Compositions comprising indole, urea, quinoline or aromatic amide based inhibitors also are disclosed.

The invention relates to the technical field of medicament, and provides a novel azole antifungal compound and salts thereof, a preparation method and application thereof. The compound has a chemical structure formula as the right, wherein, X is hydroxide radical; Ar is 2,4-difluorophenyl; R1 is hydrogen or a linear chain with 1 to 6 carbon atoms or low alkyl group with unsaturated or saturated branched chain; and R2 is selected from hydrogen, alkyl, halogen, cyano-group, nitryl and alkoxyl, can be positioned on ortho, meta, para positions of a benzene ring, and can be mono-substituted or multi-substituted. Salts of the compound can be hydrochloride, nitrate, hydrobromide or methane sulfonate. Pharmacological tests prove that the compound has strong antifungal activity, has the advantages of high efficiency, low toxicity, wide antifungal spectrum and the like compared with the prior antifungal medicines applied in clinic, and can be used for preparing antifungal medicines.

A pharmaceutical composition containing one or more antifungal agents selected from an arylamidine derivative represented by the general formula:

(wherein R¹ represents an amidino group that may be substituted with a hydroxyl group that may be protected with an acyl group, an amidino group that may be substituted with an alkoxy group that may be substituted, or an amidino group that may be substituted with an aralkyloxy group that may be substituted; R² and R³ identically or differently represent a hydrogen atom or a halogen atom) or a salt thereof, an azole antifungal agent, a polyene antifungal agent, a candin antifungal agent and a fluoropyrimidine antifungal agent has a strong antifungal activity and is useful for the treatment of fungal infection. A method for using them in combination is useful as an excellent therapeutic method for fungal infection. A pharmaceutical composition containing the arylamidine derivative represented by the above general formula or a salt thereof and an immunosuppressant has a strong antifungal activity and is useful for the treatment of fungal infection and a skin disease such as atopic dermatitis. A method for using them in combination is useful as an excellent therapeutic method for fungal infection and a skin disease such as atopic dermatitis.

The invention is a sulfur/nitrogen-containing azole antifungal compound as well as a preparation method and an application of the sulfur/nitrogen-containing azole antifungal compound, relates to the technical field of medicine. The sulfur/nitrogen-containing azole antifungal compound is a novel azole antifungal compound and has a chemical structural formula which is shown in the specification, wherein, R1 is hydrogen or a straight-chain or branched-chain saturated or unsaturated lower alkyl having 1-6 carbon atoms; R2 is selected from hydrogen, alkyl, halogen, cyano group, a nitro group, an amino and an alkoxy, can be located at the ortho, meta or para position of the benzene ring and can be monosubstituted or polysubstituted. The invention also provides a preparation method and an application of the compound. The compound disclosed by the invention has strong antifungal activity on the deep fungal, has the advantages of high efficiency, low toxicity, broad anti-fungal spectrum and the like compared with the current clinically applied antifungal drugs, and therefore, the compound can be used for the preparation of efficient antifungal agents.

The invention relates to the field of medicine technology, and a series of novel 2-aryl-2,3-dihydrogen-4(1H)-quinolinone semicarbazone derivatives (I) and pharmaceutically acceptable salts, solvates,optical isomers or polymorphs are designed and synthesized. The derivative (I) and its pharmaceutically acceptable salt, solvate, optical isomer or polymorph can be mixed as an active ingredient witha pharmaceutically acceptable carrier to prepare a pharmaceutical composition. A double dilution method is used for test of the antifungal activity of the derivative (I) and its pharmaceutically acceptable salt, solvate, optical isomer or polymorph, and the results show that the derivative has stronger killing effect on clinically common pathogenic fungi, and is expected to overcome the defects oflarge toxic and side effects, easy generation of drug resistance of azole antifungal medicines which are widely used clinically. The specific formula is shown in the description.

The invention provides a novel azole antifungal compound. According to the azole antifungal compound, a structural general formula is shown in the specification, wherein X is hydroxyl, Ar is 2,4-difluoro phenyl, and R is selected from hydrogen, alkyl, halogen, cyano-group, nitryl, amino or alkoxy and can be positioned at the ortho-position, meta-position or para-position of a benzene ring and can be mono-substituted or multi-substituted; the alkyl has 1 to 4 carbon atoms; the halogen is selected from F, Cl, Br and I; the amino is selected from -NH2, one or two aminos substituted by the alkyl and cyclic amino; and the alkoxy is selected from methoxyl, ethyoxyl and tert-butyl oxygroup. The invention also provides a method for preparing the compound and application of the compound to preparation of antifungal medicines. Compared with the conventional antifungal medicines which are applied clinically, the azole antifungal compound has the advantages of high antifungal activity on invasive fungi, high efficiency, low toxicity, broad spectrum and the like; and the method is simple and high in yield, and the prepared compound has a good antifungal effect.

The invention provides an azole antifungal compound and its pharmaceutically acceptable salt. The structural general formula of the azole antifungal compound is shown in the specification, wherein R is selected from various aliphatic primary amine or secondary amine, aromatic primary amine or secondary amine and various substituted phenylpiperazine; the substituent group on phenyl of the substituted phenylpiperazine is hydrogen, alkyl group, halogen, cyanogroup, nitro-group, amino group or alkoxy group, is arranged at ortho, meta or para position of phenyl ring, and is monosubstituted or polysubstituted; the alkyl group is the alkyl group with 1-4 carbon atoms; the halogen is selected from F, Cl, Br or I; and the alkoxy group is selected from methoxy, ethoxy and t-butyl oxygroup. The compound provided by the invention has strong antifungal activity to deep fungi. In comparison with present antifungal drugs applied in clinic, the compound provided by the invention has advantages of high efficiency, low toxicity, wide antifungal spectrum and the like. Thus, the compound can be applied to prepare antifungal drugs. A preparation method of the compound is simple and has high yield. The prepared compound has a good antifungal effect.

The invention provides a novel (i) N (/i)-(2,3-dihydro benzo [(i) b (/i)] thiapyran-4-imino)-(i) N'-(/i)-(4-methyl phenyl) guanidine derivative, a preparation method thereof, and pharmaceutically acceptable salts thereof, and also relates to a pharmaceutical composition with the compound as an active component, and the pharmaceutical composition as an antifungal agent has a strong killing effect on clinical common pathogenic fungi, and is expected to overcome the defects of strong toxic and side effects, low tendency to produce drug resistance, and the like of azole antifungals clinically widely used in the prior art. The structural formula is as a formula I compound and the pharmaceutically acceptable salts thereof.

The invention relates to 2,3,4,5-tetrahydro-4H-benzo[b]thiopyrano[4,3,c]pyrazole-2-formamide derivatives and a preparation method thereof. The structural formula of the compounds is shown in the specifications. The invention also relates to pharmaceutically acceptable salts of the derivatives and medicines taking the derivatives and the salts thereof as active ingredients. The structure of the derivates is obtained according to an association principle in pharmaceutical chemistry; and the inventor has systematically and comprehensively studied the compounds, modified and transformed a plurality of sites in the structure, and tested the in-vitro antifungal activity of the compounds by a double dilution method. Serving as novel antifungal agents, the compounds have higher killing effect on clinically common pathogenic fungi, and can overcome the defects of large toxic and side effect, high possibility of generating tolerance and the like of the clinically widely used azole antifungal medicines at present.

The invention relates to technical field of medicine, in particular to novel azole antifungal compound and salt thereof and the application, wherein, X presents hydroxyl or straight-chain ester group or branch-chain ester group with 1-6 carbon atoms and the ester group with easily-leaving group; Y presents substituent group on aromatic ring; M presents propargyl group or cyanomethyl; P presents various substituent groups on benzene ring, the substituent positions can be different positions on aromatic ring, mono substitution, or polysubstitution combined by the substituent groups; Z presents C or N atom; if Z presents Z atom, the position can be different positions on ring, and can be mono substitution, or polysubstitution; n is equal to 0-5; the salt comprises hydrochloride, nitrate, hydrobromide or methane sulfonate. The advantages of the invention are as follows: the compound provided by the invention has strong antifungal activity, low toxicity, and wide antifungal spectrum, and can be used for preparing novel antifungal drugs.

A pharmaceutical composition comprising a phenylamidine derivative or a salt thereof, represented by a general formula,

wherein R¹ and R² may be same or different, and represent an optionally substituted C_3-4alkyl group; and one or more agents selected from azole antifungal agents, polyene antifungal agents, candin antifungal agents and fluoropyrimidine antifungal agents, and a method for combination use of the phenylamidine derivative or a salt thereof and the agents are useful for treating fungal infections caused by a fungal pathogen.

The invention discloses a preparation method of a copper-cerium bimetallic Fenton-like catalytic material, the prepared catalytic material and application of the catalytic material. The preparation method comprises the following steps: S1, preparing a precursor: adding a precipitant into a solution containing copper ions and cerium ions, adjusting the pH value of the system to be higher than 7, adding a glucose solution, and continuously stirring to obtain a blue precursor; and S2, carrying out hydrothermal reaction: putting the blue precursor prepared in the step S1 into a hydrothermal reaction kettle, carrying out solid-liquid separation on a product after the reaction is finished, and collecting a solid-phase part to obtain the catalytic material. According to the scheme, the catalyticmaterial is high in catalytic activity and can rapidly catalyze Fenton reaction to degrade organic pollutants in water, especially azole antifungal drugs.

The invention provides a pharmaceutical composition for treating dermatomycosis infection. The pharmaceutical composition is prepared from the components: azole antifungal drugs, radix sophorae flavescentis, fructus cnidii, spikes of Chinese mustard, radix angelicae dahuricae, fructus forsythiae, rhizoma atractylodis, radix clematidis, rhizoma smilacis glabrae, chaulmoogra, gallnut, cortex dictamni, cortex phellodendri, rheum officinale and auxiliary materials. The invention provides the pharmaceutical composition for treating dermatomycosis infection and a preparation process thereof. By adopting the theory of combination of traditional Chinese medicine and western medicine, the selected western medicine has an antifungal effect, and the selected traditional Chinese medicines have the effects of clearing heat and drying dampness. The pharmaceutical composition can treat both symptoms and root causes, has the advantages of wide treatment range, remarkable clinical effect, small toxic and side effects, convenient and safe use, simple and feasible preparation process, low cost and remarkable clinical application effect, and is suitable for wide popularization.

Macrolide derivatives having enhancing effect for activities of azole antifungal agents, acting at low concentration and within a short time against fungal infection and reducing the frequency of appearance of resistant microorganisms. One such substance is a compound represented by the formula [I]:

wherein R1 is Ac, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is H, when R1 Bzl, R2 and R3 are Bzl, and R4 is Me; when R1 is Ac, R2 and R3 are Pr, and R4 is Me; when R1 is Ac, R2 and R3 are Hex, and R4 is Me; when R1 is Ac, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 and R3 are Pr, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is Me; when R1 is H, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 is H, R3 is Bzl, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is H, or when R1 is H, R2 and R3 are Hex, and R4 is Et.

The invention relates to the technical field of medicines, discloses a novel 4H-pyridino-[3,2-e][1,3]thiazine-4-ketone derivate and an application thereof, and designs and synthesizes a series of novel-structure 4H-pyridino-[3,2-e][1,3]thiazine-4-ketone compounds and a medicine by taking the compounds or pharmaceutically acceptable solvates, optical isomers or polymorphic substances thereof as active ingredients. According to the novel 4H-pyridino-[3,2-e][1,3]thiazine-4-ketone derivate and the application thereof, the external antifungal activity of the derivate is tested by utilizing a double concentration dilution method, so that an initial structure-activity relationship is construction, and novel high-activity low-toxicity antifungal compounds capable of being applied to preclinical research are found; the compounds have a strong killing effect to clinically common disease-causing fungi, and are hopeful of overcoming defects of large toxic and side effects and easiness in generation of drug resistance of the existing clinically widely applied azole antifungal agent.

The invention relates to a soapberry in-situ gel preparation for treating candida albicans vaginitis and a preparing method thereof, and belongs to the technical field of gynecological medication. Thepreparing method comprises the steps: preparing a water extraction fermentation concentrate of soapberry, preparing a water extract fermentation liquid with a proper concentration according to the saponin content, and preparing a temperature-sensitive gel from the water extract fermentation liquid, wherein the effective residence time in vagina is ensured. The soapberry in-situ gel preparation has the advantages of simple production, little toxic and side effects, and significant effect against candida albicans, and can avoid the potential drug resistance threat of azole antifungal agents, has wide soapberry sources and convenient material taking.