Substances of antimicrobial, antifungoid and antiprotozoan activities

FIELD: medicine, veterinary science.

SUBSTANCE: a new group of compounds, such as: 1) 1.3-benzodixole-5-β-nitroethylene

, 2) 1.3-benzodioxole-5-β-nitropropylene

, 3)benzimidazole-5-β-nitropropylene

, 4) 2-methylbenzimidazole-5-β-nitroethylene

, 5) benzoxazole-5-β-nitroethylene

, 6) 2-methylbenzoxazole-5-β-nitropropylene

has been suggested to protect against the agents of bacterial, protozoan and fungoid nature. Compounds are being the derivatives of heteronitroalkenes (dioxoles, oxazoles, imidazoles) with below-mentioned structural formulas being efficient to gram-positive bacteria and gram-negative aerobes, fungi of Candida, Trichophyton and other types, trichomonads. They could be applied at treating wound infections, fungoid lesions, septic states, pneumonia, trachoma, ornithosis, salmonellosis.

EFFECT: higher efficiency of protection.

5 cl, 5 tbl

 



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention proposes an agent for treatment of toxoplasmosis. Agent represents willow bark an aqueous extract prepared by method of thermal treatment in the ratio bark : water = 1:10, or willow bark powder. Invention expands assortment of agents of indicated prescription and provides treatment of patients with toxoplasmosis being among them with prevalent myocardium damage.

EFFECT: valuable medicinal properties of agent.

2 ex

The invention relates to medicine, namely to dermatology, and can be used for treatment of sexually transmitted infections
The invention relates to medicine, in particular to novel solid pharmaceutical compositions containing hexadecylphosphocholine (miltefosine) for oral administration in the treatment of leishmaniasis, to a method for the production of specified pharmaceutical compositions for the treatment of leishmaniasis specified pharmaceutical composition to a combination that includes the specified solid pharmaceutical composition, an antiemetic and/or antidiarrheal agent

The invention relates to medicine, in particular to venereology, and for the treatment of trichomoniasis

FIELD: medicine, dermatology, chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to an antifungal gel pharmaceutical composition based on ketoconazole and clotrimazole that are derivatives of imidazole. The composition comprises ketoconazole or clotrimazole as an active component, polyethylene glycol-400 (PEG-400) as a solvent, carboxyvinyl polymer as a gel-forming agent, polyethylene glycol as a gel stabilizing agent, organic amine or inorganic bas as a regulator of pH and water taken in the definite ratio of components. The composition is prepared by dissolving active component in PEG-400, dispersing carboxyvinyl polymer in water, successive addition to dispersion propylene glycol as a stabilizing agent and regulator of pH and combination of prepared solution and gel followed by stirring the mixture up to preparing the gel composition with pH 5-7. Invention provides preparing antifungal composition with reduced adverse effect.

EFFECT: improved preparing method, valuable medicinal properties of composition.

2 cl, 1 tbl, 11 ex

FIELD: medicine, veterinary science, mycology.

SUBSTANCE: the suggested preparation for external application includes the mixture of Microsporum canis, Microsporum gypseum and Trichophyton mentagrophytes homogenates at the ratio of 1:1:2 in solvent, for example, in physiological solution, and formalin. Concentration of mycotic elements corresponds to 50.0-500.0 mln./ml ready-to-use product. This preparation should be applied in the method to treat dermatomycosis due to rubbing it into affected skin sites till hyperemia at 0.2-2.0 ml preparation/1-4 sq.cm skin surface once daily for 4-6 d. Both the preparation and the method suggested provide healing during the terms mentioned being convenient, reliable and efficient.

EFFECT: higher efficiency of therapy.

4 cl, 5 ex

FIELD: chemico-pharmaceutical industry.

SUBSTANCE: the present innovation deals with new stabilized pharmaceutical composition in its lyophilized form including the compound of formula I

as an active ingredient and lactose disaccharide as a stabilizing agent. The present pharmaceutical compositions are of high stability at storage. As for active ingredient it is not destroyed in the course of time.

EFFECT: higher efficiency.

10 cl, 15 ex, 6 tbl

FIELD: medicine.

SUBSTANCE: preparation comprises echinocandine substance of formula I or its pharmaceutically permissible salt, pharmaceutically permissible micelle-forming surface-active agent and non-toxic aqueous solvent and stabilizing agent.

EFFECT: improved stability and bioaccessibility properties.

48 cl, 4 tbl

FIELD: medicine, dermatology, pharmacy.

SUBSTANCE: invention relates to an antifungal preparation for external applying. The preparation comprises 2-chloro-4-nitrophenol, polyethylene glycol (PEG-400) and 50% ethyl alcohol. The preparation is used for treatment of epidermophytosis, trichophytosis, fungal eczema, cutaneous candidiasis and other diseases. Invention provides preparing the more effective antifungal preparation based on the domestic raw.

EFFECT: enhanced effectiveness of preparation, valuable medicinal properties.

2 ex

FIELD: medicine, cosmetics.

SUBSTANCE: the present innovation deals with, a) at least, one fungicide substance and b) at least, one water-soluble film-forming substance, where b)-component is chitosan derivative chosen out of hydroxyalkyl chitosans and carboxyalkyl chitosans; nail vanish that includes the above-mentioned composition, and nail vanish that includes, at least, one water-soluble film-forming substance chosen out of hydroxyalkyl chitosans and carboxyalkyl chitosans. The suggested nail vanish is of high fungicide action and is free of multiple dermatological and esthetic disadvantages.

EFFECT: higher efficiency of application.

23 cl, 10 ex, 1 tbl

The invention relates to a pharmacy, namely the creation of herbal medicines, exhibiting antifungal activity

The invention relates to chemical-pharmaceutical industry, in particular to the creation and production of tools for the treatment of skin diseases

The drug cundiff" // 2237487
The invention relates to the pharmaceutical industry, and is intended for the prevention and treatment of viral, bacterial and fungal infections

The invention relates to medicine, specifically to antifungal medicinal preparation containing as active ingredient a therapeutically effective amount of clotrimazole and targeted supplements, which are used lactose, starch, MCC, citric acid, salt of stearic acid

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to new 5-aryl-1-phenyl-4-heteroyl-3-hydroxy-3-pyrroline-2-ones of the formula:

wherein (1) X means sulfur atom (S); R means (CH3)2CH; (2) X means sulfur atom (S); R means (CH3)3C; (3) X means oxygen atom (O); R means (CH3)3C. Compounds of the formula (I) are prepared by interaction of the corresponding heteroylpyruvic acid methyl ester with mixture of aniline and aromatic aldehyde in acetic acid medium at short-time heating. Compounds elicit an anti-bacterial activity with value MIC = 3.9-7.8 mcg/ml as compared with 62-1000 mcg/ml for analogue.

EFFECT: valuable properties of compounds.

1 tbl, 3 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention describes a method for preparing derivatives of benzoxazine and describes a method for preparing compound represented by the formula . Method involves of compound represented by the formula (I): with compound represented by the formula (II-1-a): in the presence of a base to form compound represented by the formula (III-1-a): followed by reduction of this compound to compound represented by the formula (IV-a): , interaction of this compound with compound represented by the following formula: to form compound represented by the formula (V-a): and the following treatment of this compound in the presence of a base to obtain compound represented by the formula (VI-a): , treatment of this compound with compound of boron trifluorine and its conversion by this manner to the boron chelate compound represented by the following formula: followed by reaction of this compound with 4-methylpiperazine to obtain compound represented by the following formula: followed by cleavage and elimination of boron chelate of this compound. In each of above given formulas X1, X2 and X3 represents independently halogen atom; R1 represents a leaving group; R3 represents hydrogen atom or carboxyl-protecting group; R4 represents hydroxyl-protecting group; each R5 and R6 represents independently alkyl group comprising 1-6 carbon atoms; R7 represents carboxyl-protecting group; Y represents alkoxy-group comprising 1-6 carbon atoms, halogen atom or dialkylamino-group (wherein alkyl groups can be similar or different and each represents alkyl group comprising 1-6 carbon atoms). Also, invention describes variants above described method, methods for preparing intermediate compounds and intermediate compound. Invention provides industrially favorable methods for preparing intermediate compounds that are useful for preparing compounds with antibacterial properties.

EFFECT: improved preparing methods, valuable properties of compounds.

96 cl, 102 ex

FIELD: applied immunology.

SUBSTANCE: composition contains, wt parts: borax decahydrate1-25, sodium thiosulfate pentahydrate 10-5-10-4, potassium carbonate 30-150, refined sugar 30-200, and water 100-200 per 100 wt parts of sodium metasilicate pentahydrate. In addition to its capability of improving resistance to diseases, body weight increase, productivity of agricultural plants, quality of crop, and ripening term (harvest time), composition according to invention possesses nonspecific immunostimulating activity, including production of antibodies and enhancement of immunity through activation of immunocytes thereby maximally strengthening vaccination effect regarding diseases caused by malignant neoplasm viruses.

EFFECT: increased assortment of immunostimulating agents.

10 cl, 11 dwg, 12 ex

FIELD: silicon-containing substances, medicine, pharmacy.

SUBSTANCE: invention describes silicon glycerates eliciting transcutaneous conductivity of medicinal agents with the composition of the formula: Si(C3H7O3)4 x xC3H8O3 wherein 3 ≤ x ≤ 10 with dynamic viscosity 4.6-28.5 Pa x s (20 ± 0.5°C). Compounds are prepared by interaction of tetraethoxysilane with glycerol in the mole ratio = 1:(7-14) in the presence of tetrabutoxy-titanium (0.06 mole/mole of tetraethoxysilane) and removal of formed ethyl alcohol in heating of reaction mass to 120-130°C and keeping at this temperature for 3 h, not less. Also, invention describes glycerohydrogels based on element-organic glycerates containing water and gel-forming additive that contain as element-organic glycerates silicon glycerates with the composition of the formula Si(C3H7O3)4 x xC3H8O3 wherein 3 ≤ x ≤ 10 as they contain electrolyte as a gel-forming additive in the following ratio of components, wt.-%: silicon glycerates, 8.2-65.1; electrolyte, 0.1-0.6, and water, the balance. Proposed compounds - silicon glycerates and glycerohydrogels based on thereof are physiologically active substances eliciting transcutaneous conductivity of medicinal agents with possible broad spectrum of their applying in medicine.

EFFECT: valuable medicinal properties of compounds.

2 cl, 2 tbl, 2 dwg, 7 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of aminomethylpyrrolidine of the formula (I) , their salts or hydrates wherein R1 represents aryl with from 6 to 10 carbon atoms or heteroaryl wherein heteroaryl is a five-membered ring or a six-membered ring and comprises from 1 to 2 heteroatoms taken among nitrogen, oxygen and sulfur atom; aryl and heteroaryl can comprise one or more substitutes taken among the group consisting of halogen atom or (C1-C6)-alkoxyl; each radical among R2, R3, R4, R5, R6, R7 and R8 represents hydrogen atom (H) independently; Q represents incomplete structure representing by the following formula: wherein R9 means (C3-C6)-cyclic alkyl that can be substituted with halogen atom; R10 means hydrogen atom (H); R11 means hydrogen atom (H), NH2; X1 means halogen atom; A1 represents incomplete structure representing by the formula (II): wherein X2 means hydrogen atom (H), halogen atom, halogenmethoxyl group, (C1-C6)-alkyl or (C1-C6)-alkoxyl group; X2 and above indicated R9 can be combined to form the ring structure and inclusion part of the main skeleton and such formed ring comprises oxygen, nitrogen or sulfur atom as a component atom of the ring and the ring can comprise (C1-C6)-alkyl as a substitute; Y means hydrogen atom (H). Compounds of the formula (I) elicit an antibacterial effect and can be used for preparing a therapeutic agent.

EFFECT: valuable medicinal properties of compounds.

2 tbl, 61 ex

FIELD: medicine, pharmaceutical industry.

SUBSTANCE: invention relates to an antibacterial, anti-inflammatory, antiviral, antiherpetic agent used for treatment of vulvovaginitis, palanitis, ballanopostitis induced by microorganisms, candidas, viruses, chlamydia, trichomones and infections of herpes simplex virus and for treatment of acne also. Invention relates to an antibacterial, anti-inflammatory, antiviral, antiherpetic medicinal agent used for treatment of diseases transferred by sexual way, in particular, to vulvovaginitis, palanitis, ballanopostitis induced by microorganisms, candidas, viruses, chlamydia, trichomones and infections of herpes simplex virus and for treatment of acne. The medicinal agent comprises a mixture of cream-like base (vehicle) and an alcoholic extract from leaves, fruits and stems of plant Tribulus terrestris (active component). This active component comprises active substance from Tribulus terrestris with the high content of steroid saponins. Also, invention relates to a method for preparing an antibacterial, anti-inflammatory, antiviral, antiherpetic medicinal agent that involves analysis of parts of plant Tribulus terrestris for gathering and further extraction, namely to a sample of leaves, fruits and stems of plant Tribulus terrestris gathered in the definite time period. Method involves addition of deionized water, stirring and evaluation of the level of water and foam in a mixer. After proving readiness of plant Tribulus terrestris for gathering samples of leaves, fruits and stems of plant Tribulus terrestris are taken. Samples are dried, milled and deionized water is added. The prepared aqueous mixture is treated in mixer, the level of water and foam is evaluated in an aqueous mixture. The prepared mixture is remained for precipitation, filtered, ethyl alcohol is distilled off and the concentrated aqueous extract is prepared. The prepared active component is added to the cream base (vehicle) or to a base (suppository). Agent promotes to effective treatment of vulvovaginitis, palanitis, ballanopostitis induced by microorganisms, candidas, viruses, chlamydia, trichomones and infections of herpes simplex virus and to treatment of acne also.

EFFECT: valuable medicinal properties of agent.

5 cl, 5 dwg

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