Succinate of n-(2,4,6-trimethylphenyl)amide 2-(beta-n,n-diethylamino ethylamino)-4-oxo-4-(4-methyylphenyl)-2-butenoic acid

FIELD: chemistry.

SUBSTANCE: novel compound relates to amine derivatives of pyruvic acid amides and is biologically active - succinate of N-(2,4,6-trimethylphenyl) amide 2-(β-N,N-diethylamino ethylamino)-4-oxo-4-(4-methyl-phenyl)-2-butenoic acid of formula


EFFECT: compound has marked local anaesthetic and antimicrobial activity.

1 cl, 1 ex, 3 tbl


The claimed connection relates to the field of organic chemistry, amino amides arilpirolilor acids, namely to new biologically active compounds, succinate N-(2,4,6-trimetilfenil)amide 2-(β-N,N-diethylaminoethylamine)-4-oxo-4-(4-(were) 2-butenova acid of the formula (I):

which can find use as a local anesthetic, antiseptic drug.

Known structural analogues of the claimed compounds, obtained by the interaction of amides aroylpropionic acids with aromatic amines [Ahomelae5v, Antonimina, Rod, Woosley, Tradeshow. Amides and hydrazides arilpirolilor acids. Message 10. Synthesis, antimicrobial and analgesic activity of arylamido 4-aryl-arylamino-4-oxo-2-butenova acids // Chem.-Pharm. Journe. - 2004. - V.38. No. 7. - P.19-21].

As the standard of comparison taken local anesthetic drug - trimekain [Mashkovsky PPM Medicines. 2 so - 14th ed., Rev., Corr. and extra - M.: OOO "Publishing house New Wave", 2000].

The aim of the invention is the synthesis of new, not previously described succinate N-(2,4,6-trimetilfenil)amide 2-(β-N,N-diethylaminoethylamine)-4-oxo-4-(4-(were)2-butenova acid with local anesthetic and PR is tuomikoski properties. This goal is achieved dellisola 5-(4-were)-2,3-dihydro-2,3-furandione with 2,4,6-trimethylaniline under mild conditions with subsequent interaction with N,N-diethylaminoethylamine scheme:

Synthesis of N-(2,4,6-dimetilfenil)amide 2-hydroxy-4-oxo-4-(4-chlorophenyl) 2-butenova acid (III) is carried out by analogy with the previously described methodology [andrejchikov US, Milutin A.V., I. Krylov, Sarajevo Russia, having got, Dormidontova E.V., Kovacikova L.P., Nazmitdinov FA, Call VA Synthesis and biological activity of heterylamides aroylpropionic acid and 5-arylpyrazole-3-carboxylic acid // Chem.-Pharm. Journe. - 1990. - 24. No. 7. - Pp.33-35].

An example of obtaining the compound (II)

To a solution of 3.25 g (0,01 mol) of N-(2,4,6-trimetilfenil)amide 4-(4-were)-2-hydroxy-4-oxo-2-butenova acid (III), dissolved in 15-20 ml of absolute toluene, with stirring, was added a solution of 1.16 g (0,01 mol) of N,N-diethylaminoethylamine and boiled for 15 minutes. The mixture was left for 1 day at room temperature. The solution is evaporated, the resin overwrote hexane, the solid residue is recrystallized from cyclohexane. Received 2.53 g (60%) of crystalline substances (II) with TPL119-121°C. C26H35N3O2. Range of PMR, δ, ppm, 0,98 t (6N, 2CH2-CH3), 2,22 (N, SN3), 2,55 ° C, (4H, CH2-CH2), 3,43 kV (4H, 2CH 2-CH3), 5,90 s (1H, CH), 7,05-7,74 m (7H,6H4With6H3), 10,06 (1H, CONH), 10,56 t (1H, NH).

Example obtain the claimed compound (I)

To a solution 4,22 g (0,01 mol) of N-(2,4,6-trimetilfenil)amide 4-(4-were)-2-(β,β-N,N-diethylaminoethylamine)-4-oxo-2-butenova acid dissolved in 15-20 ml of ethanol, with stirring solution was added 1.18 g (0,01 mol) of succinic acid in 10-15 ml of ethanol was boiled for 5-7 minutes. The mixture was left for 1 day at room temperature. The solution is evaporated, the resin overwrote hexane, the solid residue is recrystallized from isopropyl alcohol and dried in air to constant weight. Received 4,70 g (87%) of crystalline substances (I) with Tpl.126-128°C. C30H41N3O6. The IR spectrum v cm-1(the crystals): 3232 (NH), 1720 (COOH), 1656 (CONH), 1608, 1596 (WITH the chelate, C=C). Range of PMR, δ, ppm, CDCl3: 1,13 t (6N, 2CH2-CH3), to 2.18 (3H, CH3), 2,22 (6N, 2CH3), to 2.35 (3H, CH3), 2,96 ° C (8H, CH2-CH2), 3,66 kV (4H, 2CH2-CH3), of 5.92 (1H, CH), 6,07 s (1H, CH), 6,83 with (2N, C6H2), 7,07 for 7.78 m (5H,6H4, NH+), with a total of 8.74 (1H, CONH), 10,53 t (1H, NH), 14,34 (1H, WITHHE).

The inventive compound (I) is a colorless crystalline substance, soluble in water, DMF, ethanol, soluble in isopropyl alcohol, nerator is my in hexane.

Study of biological activity

Acute toxicity intraperitoneal injection was determined by nonlinear white mice-males weighing 18-24 g test substance and the reference product was administered into the abdominal cavity in the form of a solution in 1%starch mucus at a rate of 0.1 ml / 10 g weight of the animal in increasing doses. The results were processed by Prozorovsky calculation of the median lethal dose (LD50) at P<0,05 [Prozorovsky CENTURIES, Prozorovsky BTW, Demchenko V.M. Pharmacol. toxicol., v.41, №4, s-502 (1978)].

The study of connections for local anesthetic activity. In the experience used generalizirovanny rabbits (males) weighing 2.0 to 2.5 kg were Determined sensitivity threshold of the cornea of the rabbit to tactile impact. The original sensitivity of the cornea of the rabbit (control) was measured twice with an interval of 5 minutes. A solution of the substance in a volume of 0.4 ml was injected into the conjunctival SAC of the eye of the rabbit for 2 times, with an interval of 30 seconds. Each concentration was tested 8 times, using the cornea different eyes. Determined index Rainier characterizing the depth of surface anesthesia and represent the sum of the mechanical stimulation of the cornea within the hour, and the duration of anesthesia in minutes. [Manual on experimental (dokli is practical) study of new pharmacological substances. M, the RF Ministry of health, 2005].

The results were processed statistically using student's criterion [Belenky, M. elements of a quantitative evaluation of the pharmacological effect. L., 1963]. The obtained results are considered significant at p≤0,05. The results of studies of acute toxicity and local anesthetic activity of the claimed compounds and drug comparisons are presented in tables 1 and 2.

Table 1
Acute toxicity of compounds with intraperitoneal injection
ConnectionToxicity intraperitoneal injection, mg/kg
I255,0 (290,0÷420,0)
Trimekain154,0 (132,0÷178,0)

Table 2
The activity of compounds at the surface anesthesia
ConnectionSurface anesthesia
Index RainierThe duration of anesthesia, min
Trimekain559,0±26,1of 31.8±4,4

Determination of the bacteriostatic activity was performed by the method of twofold serial dilutions in liquid nutrient medium [Manual on experimental (preclinical) study of new pharmacological substances. - M., 2000, s-273]. For all the studied compounds were determined IPC in respect of pharmacopoeial strains: S. aureus ATCC 6538-P, E. coli ATCC 25922, .albicans ATCC 885-653. Crops produced in mesopotania broth, pH 7.0 with different concentrations of the tested compounds. The cultures were grown in test tubes on a beveled apparitional environment (mastopathy agar solid medium Saburo). To determine the antimicrobial activity was used 18-20-48-hour culture of microorganisms. For preparation of the working suspension of microbes produced washout grown culture isotonic sodium chloride solution, and set the density of the microbial suspension according to the turbidity standard 5 units. Next, from the obtained microbial suspension (500 million M.L./ml) were prepared working solution of bacteria with a concentration of 5 million M.L./ml of This suspension of microbes was made in the amount of 0.1 ml in tubes with serial dilutions of study drug. Thus, microbial load, the lubricant when determining the ACA was 250000 M.L./ml The target compound in the amount of 0.05 g was dissolved in 5 ml of DMSO, 1 ml of the prepared dilution of 1:100 was combined with 4 ml mycopathologia broth or liquid Saburo (1:500). Next was preparing a series of serial dilutions of the compounds twice with decreasing concentration.

Records of the results produced after 18-20 hours of exposure control and experimental tubes in the incubator at 37°C for bacteria and 48 hours at 22°C for fungi. Minimal inhibitory concentration (MIC) was determined by the absence of signs of growth on nutrient medium: the last tube of stunting (clear broth) corresponds to the IPC of the drug in relation to this strain. Bacteriostatic effect of the studied compounds was compared with the action dioksidina [Padalka E.N. Infection and antimicrobial therapy, 2001, Vol.3, No. 5, p.150-155], turisticheskiy - fluconazole [Rex J.Y., Walsh T.J., J. Sobel d/ et all, Clin. Infect. Dis., 2000, v.30, No.4, R-678]. The results are shown in table 3.

Table 3
Antimicrobial activity (μg/ml) of the compound (I)
ConnectionS. aureusE. coliS.
Dioxidineat 62.5-10003,9-62,5-

The compound (I) has antimicrobial activity against Staphylococcus Staphylococcus and Escherichia coli (IPC 31-62 mg/ml) and yeast fungi (IPC 125-250 µg/ml).

Thus, succinate N-(2,4,6-trimetilfenil)amide 2-(β-N,N-diethylaminoethylamine)-4-oxo-4-(4-were)-2-butenova acid exhibits a more pronounced local anesthetic effect with less toxicity than Comparators in terms of activity and duration of action. Therefore, the inventive compound can be used in medicine as a local anesthetic and antimicrobial drugs.

Succinate of N-(2,4,6-trimetilfenil)amide 2-(β-N,N-diethylamino-ethyl amino)-4-oxo-4-(4-were)-2-butenova acid formula


Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to amide of δ-amino-γ-hydroxy-ω-arylalcane acid of formula and its pharmaceutically acceptable salts. Also described are pharmaceutical compositions, which include said compounds, and application of said compounds for preparation of medication, intended for treatment of pathological states, associated with renin activity, in particular for treatment of hypertension.

EFFECT: obtaining pharmaceutically acceptable salts, which possess rennin-inhibiting ability.

21 cl, 161 ex

FIELD: chemistry.

SUBSTANCE: invention discloses N-(2,6-dimethylphenyl)amide of 2-(β-N,N-diethylaminoethylamino)-4-oxo-4-(4-ethoxy-phenyl) of 2-butenoic acid of formula (I)


EFFECT: local anaesthetic activity.

1 cl, 1 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: present invention relates to methods for synthesis of compounds of formula (A), where R1 denotes halogen, C1-C6halogenalkyl, C1-C6alkoxy(C1-C6)alkyloxy or C1-C6alkoxy(C1-C6)alkyl; R2 denotes halogen, C1-C4alkyl or C1-C4alkoxy; R3 and R4 independently denote a branched C3-C6alkyl; and R5 denotes C3-C12cycloalkyl, C1-C6alkyl, C1-C6hydroxyalkyl, C1-C6alkoxy(C1-C6)alkyl, C1-C6alkanoyloxy(C1-C6)alkyl, C1-C6aminoalkyl, C1-C6alkylamino(C1-C6)alkyl, C1-C6dialkylamino(C1-C6)alkyl, C1-C6alkanoylamino(C1-C6)alkyl, HO(O)C-(C1-C6)alkyl, C1-C6alkyl-O-(O)C-(C1-C6)alkyl, H2N-C(O)-(C1-C6)alkyl, C1-C6alkyl-HNC(O)-(C1-C6)alkyl or (C1-C6alkyl)2N-C(O)-(C1-C6)alkyl, or their pharmaceutically acceptable salts which have renin inhibiting activity, as well as to basic intermediate compounds obtained during steps for synthesis of the desired compounds and to methods for synthesis of said intermediate compounds.

EFFECT: alternative synthesis method.

43 cl, 8 dwg, 11 ex

Anxiolytics // 2398761

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to new amino acid derivatives of 3,4-dimethoxyphenylethylamine 1-4 exhibiting anxiolytic activity and described by general formula (1-4). In the formula, R represents

NH represents (COOH)2 (1-4); Y = 1 (1, 2); Y = 3 (3); Y = 0 (4).

EFFECT: preparation of an anxiolytic compound.

2 cl, 6 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention is aimed at obtaining a new compound - hydrobromide 3-[N-(3-ethoxycarbonyl-methylene)benzylamino]-4-hydroxy-N-benzylbutaneamide, which widens the range of substances with growth regulating properties and with antimicrobial activity.

EFFECT: when the proposed compound is used in optimum dosage, growth-stimulating effect on wheat seedlings significantly surpasses counterparts on structure and effect; when using the proposed compound on staphylococcus aureus, significant increase in bacteriostatic and bactericidal effect compared to the counterpart is observed.

1 cl, 3 ex, 1 tbl

Dpp-iv inhibitors // 2345067

FIELD: chemistry, pharmaceutics.

SUBSTANCE: claimed invention relates to novel compounds of general formula (I) Z-C(R1R2)-C(R3NH2)-C(R4R5)-X-N(R6R7) (I), or its pharmaceutically acceptable salt which is different because Z represents phenyl; where Z can be substituted with one or more R8, where R8 represents halogen; R1, R4 represent H; R2, R5 represent H; R3 represents H; X is selected from group consisting of S(O)2 and C(O); R6, R7 are independently selected from group consisting of H, (C(R29R30))m-X1-Z1 and (C(R31R32))n-X2-X3-Z2 and C1-4alkyl, which carries substitution with one or more R29a, where R29a is independently selected from group consisting of R29b and Z1, on condition that R6 and R7 are selected in such way that R6 and R7 were not simultaneously independently selected from group consisting of H, CH3, CH2CH3, CH2CH2CH3 and CH(CH3)2; R29 R29b, R30, R31, R32 are independently selected from group consisting of H, C1-6alkyl and N(R32a)-C1-6alkyl; R32a represents C1-6alkyl; m is 0, 1 or 2; n is 2; X1 is independently selected from group consisting of covalent bond, -C1-6alkyl and -C1-6alkyl-N(R33)-; X2 represents -N(R35)-; X3 represents -C(O)-; R33 represents C1-6alkyl; R35 represents H; Z1, Z2 are independently selected from group consisting of Z3 and -C(R37a)Z3aZ3b; R37a represents H; Z3, Z3a, Z3b are independently selected from group consisting of T1, T2, C1-6alkyl, C1-6alkyl-T1 and C1-6alkyl-T2; T1 represents phenyl; where T1 is optionally substituted with one or more R38; R38 being independently selected from group consisting of halogen, CN, R39, C(O)NH2, S(O)2NH2, OT3, C(O)N(R40)T3 and T3, T2 is selected from group consisting of C3-7cycloalkyl, indanyl, tetralinyl, heterocycle and heterobicycle, T2 optionally carries substitution with one or more R41, where R41 is independently selected from group consisting of halogen, R42, OH and T3; R39 is selected from group consisting of C1-6alkyl, O-C1-6alkyl, S-C1-6alkyl, C(O)N(R44)-C1-6alkyl, S(O)-C1-6alkyl and S(O)2-C1-6alkyl, where each C1-6alkyl optionally carries substitution with one or more R45, where R45 is independently selected from group consisting of F, N(R46R47) and T3; R42 represents C1-6alkyl, each C1-6alkyl optionally carries substitution with one or more R45, where R45 is independently selected from group consisting of F; R40, R46, R47 are independently selected from group consisting of H and C1-6alkyl; R44 represents H; T3 is selected from group consisting of T4 and T5; T4 represents phenyl, where T4 optionally carries substitution with one or more R51, where R51 is independently selected from group consisting of halogen, OR52, S(O)2N(R52R53), C1-6alkyl; R52, R53 are independently selected from group consisting of H and C1-6alkyl; T5 is selected from group consisting of heretocycle C3-7cycloalkyl, where T5 optionally carries substitution with one or more R54, where R54 represents C1-6alkyl; where heterocycle represents ring of cyclobutane, cyclopentane, cyclohexane, which can contain double bonds in number up to maximal, or aromatic or non-aromatic ring which is fully or partially saturated or unsaturated, and in which at least one carbon atom, maximally up to four carbon atoms, are substituted with heteroatom, selected from group including oxygen and nitrogen, and where ring is bound with remaining part of molecule through carbon or nitrogen atom; where heterobicycle represents heterocycle as stated above, which is condensed with phenyl or other heterocycle with formation of bicyclic ring system, on condition that the following compound is excluded from claim:3-amino-N-cyclohexyl-4-phenylbutyramide. Invention also relates to pharmaceutical composition based on compound of general formula (I) and to their application for manufacturing medication for treatment and/or prevention of conditions during which it is desirable to inhibit DPP-IV.

EFFECT: obtaining novel group of compounds possessing useful biological properties.

26 cl, 8 tbl, 193 ex

FIELD: organic chemistry, insecticides.

SUBSTANCE: invention describes compounds of the formula (1) wherein A and B mean oxygen atom (O); J means pyrazole ring; K in common with two adjacent binding carbon atoms represents phenyl ring substituted with from 1 to 2 substitutes chosen independently from R4; L means a binding chain comprising from 1 to 2 members chosen from carbon atom and optionally substituted with one R13; or L means C(=E) wherein E means O; R3 means hydrogen atom (H) or (C1-C6)-alkyl; each R4 means independently (C1-C6)-alkyl, halogen atom or -CN; each R5 means independently (C1-C6)-halogenalkyl, halogen atom or (C1-C4)-halogenalkoxy-group; or each R5 means independently phenyl or pyridyl ring wherein each ring is substituted with R6; each R6 means halogen atom; each R13 means independently -COOH, (C2-C6)-alkoxycarbonyl or (C2-C6)-alkoxycarbonylalkyl; or each R13 means phenyl substituted with (C2-C6)-alkoxycarbonyl; pyridinyl or imidazole ring; n = 1 or 2. Proposed compounds show insecticide activity. Also, invention describes a composition used for control of insect-pests and a method for control of insect-pests, and compounds of the formula (6) wherein R3 means H or (C1-C4)-alkyl, one R4 is added to phenyl ring at position 2 and means CH3 or halogen atom, and the second R4 means optionally F, Cl, Br, J or -CN.

EFFECT: valuable properties of compounds and composition.

16 cl, 15 tbl, 11 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to geranyl compounds represented by the following formulas (I-1) , (I-2) or (I-3) wherein R1 means compounds of the following formulas: or R2 means a group remaining after removing all carboxyl groups presenting in carboxylic acid chosen from group consisting of malic acid, citric acid, succinic acid, fumaric acid and others; m = 1, 2 or 3; n = 0, 1 or 2, and m + n represent a number of carboxylic groups presenting in indicated carboxylic acid; R3 means p-hydroxyphenyl or mercapto-group. Also, invention relates to derivatives of mevalonic acid represented by the following formula (I-4): wherein R means -CH2OH or CH3. Also, invention to an antitumor agent comprising as an active component geranyl compound of formulas (I-1), (I-2) or (I-3) or derivative of mevalonic acid of the formula (I-4), and optionally a pharmaceutically acceptable carrier or solvent. Also, invention relates to a method for treatment of liver cancer based on using geranyl compound of formulas (I-1), (I-2) or (I-3), or derivative of mevalonic acid of the formula (I-4) and using proposed compounds in manufacturing an antitumor agent. Invention provides using geranyl compounds or derivatives of mevalonic acid as antitumor agents.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

7 cl, 3 tbl, 17 ex

FIELD: organic chemistry, agriculture.

SUBSTANCE: invention relates to ortho-substituted arylamides of formula I , wherein J represents phenyl ring or pyrazole ring each substituted with one or two substitutes independently selected from R5; K represents -NR1C(=A)- or -NR1SO2-; L represents -C(=B)NR2-, -SO2NR2- or -C(=B)-; A and B represent O; R1 and R2 represent H; R3 represents C1-C6-alkyl optionally substituted with one or more substitutes, independently selected from group containing CN, NO2, C1-C4-alkylsulfonyl and C2-C6-alkoxycarbonyl; each R4 independently represents C1-C6-alkyl, halogen or CN; each R5 independently represents C1-C6-alkyl, halogen or C1-C4-haloalkoxy or pyridinyl optionally substituted with one substitute independently selected from R9; wherein R9 represents halogen; n = 1-2; with the proviso, that when K represents -NR1C(=A)- L is not -C(=B)NR2-, and salts thereof, method for insect controlling by using abovementioned compounds. Intermediate for synthesis of target compounds having formula 2 also is disclosed.

EFFECT: compounds with insecticide activity, useful in insect controlling.

15 cl, 21 tbl, 9 ex

FIELD: organic chemistry, biochemistry.

SUBSTANCE: invention relates to compounds used as intermediates substances for inhibitors of transfer of cholesteryl ester protein (CETP) and methods for their preparing. Indicated compounds are represented by the following formulae:

, ,

wherein R is taken among methyl and benzyl and by the formula

wherein R represents methyl.

EFFECT: improved preparing method, valuable biochemical properties of inhibitors.

15 cl, 9 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely, to anaesthesia in dentistry, and can be used if maxillary anaesthesia is needed. For this purpose, in a region of an alveolar process of an upper jaw between juga alveolaria 12 and 13 or teeth 22 and 23 respectively depending on a side of the jaw, at level of a projection of root ends, intraosseous injection of an anaesthetic solution is performed.

EFFECT: method provides safe adequate maxillary anaesthesia ensured by blocking the conduction of peripheral branches of an infraorbital nerve due to spongy bone impregnation with the anaesthetic solution to penetrate into an infraorbital canal.

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to traumatology and orthopedics and can be used in operations on Achilles tendon, ankle joint and foot. For this purpose block of tibial nerve is performed by introduction of anesthetic through point, located on the middle of the distance between internal ankle and internal edge of Achilles tendon. Additionally performed is block of common paroneal nerve by introduction of anesthetic through point, located behind fibular bone head.

EFFECT: method makes it possible to provide adequate anesthesia of foot for long term due to more accurate determination of reference points for additional block of paroneal nerve.

2 dwg, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely, to anaesthesiology and dentistry, and can be used as an anaesthesia care of dental interventions. That is ensured by infiltration anaesthesia as follows. In the middle of each gingival papilla adjoining a tooth to be anaesthetised, a short-needle syringe is pricked in from a vestibular side at an angle 90 degrees to a surface of a mucous membrane of the medial and distal gingival papilla. The needle is moved forward firmly to a bone. Then an anaesthetic drug 0.2 ml of 4 % articaine and adrenaline of various concentrations is introduced from each side.

EFFECT: method provides the adequate and prolonged anaesthesia ensured by the most exact delivery of the anaesthetic drug and vasoconstrictive agent to nerve fibres.

1 ex

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine, namely, surgical dentistry and maxillofacial surgery and can be used for treatment and prevention of alveolitis. Ointment for treatment and prevention of alveolitis contains lanolin-vaseline base, crystalline iodine, water solution of potassium iodide, solcoseryl dental adhesive paste, anesthesin, polysorb MP, distilled water, with the following component ratio: lanolin-vaseline ointment 40.5-42.5; crystalline iodine 0.1-0.3; water solution of potassium iodide 0.4-0.5; solcoseryl dental adhesive paste 40.5-42.5; anesthesin 3.8-5.8; polysorb MP 0.3-0.5; distilled water - the remaining part.

EFFECT: invention makes it possible to accelerate healing of bone wounds, prevent development of inflammatory complications and reduce period of recovery of patients with alveolitis.

2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to neurology, and can be used in complex rehabilitation of the patients with central spastic paresis of upper extremities. For this purpose, first under block anaesthesia of branches of a brachial plexus, hand bracing is performed from an axillary approach. In bracing, a rigid bandage is applied to a level of the lower one-third of forearm 2 cm higher than a wrist joint. It is followed with physioprocedures every 15-30 minutes in the following order: paraffin-ozokerite applications or cryotherapy during 20 min, electrical myostimulation of extensor muscles of hand and fingers, massage of the affected extremities, physiotherapy exercises, mirror therapy. Thereafter, the hand is placed in the brace and fixed with an elastic bandage. The bracing time is 3-4 hours 1-2 times a day. A number of the physioprocedures of each type makes 15-20 procedures in the course. The bracing period is 3 weeks to 3 months, and the brace is used till muscle tone recovery, and also active finger extension. For one year after the suffered stroke, the rehabilitation courses are repeated for 3-4 times a year, further the therapeutic courses are performed 2 times a year.

EFFECT: method allows ensuring considerable recovery of motor functions disordered by a local brain damage and activation of neuroplasticity mechanisms of the central nervous system for a shorter period of time in the given category of patients due to optimal selection of a therapeutic regimen and more effective bracing.

2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine, namely to urology, andrology and anesthesiology, and can be used in necessity of performing blockade of spermatic cord. For this purpose in place of supposed puncture in visible, ultrasonic and infrared spectra of radiation state of tissues is determined and nearest to epididymis section of spermatic cord is selected. Spermatic cord is lifted, forming deflection of posterior wall above selected section, and fixed. After that into spermatic cord under US control with cut downward needle is introduced on anterior-external surface of scrotum and moved through subcutaneous fatty cellular tissue and anterior wall of spermatic cord on descending radius towards scrotum on minimal distance. After that angle of needle inclination with respect to anterior surface of cord in place of its puncture is reduced to 5-0°, and needle is moved inside cord at the distance equal to length of its cut with further introduction of 1-1.5 ml of solution of 2% lidocain hydrochloride and 1% cefazolin sodium salt at temperature +37°C. After that, correctness of needle introduction is estimated by ultrasonic visualisation of place and form of obtained drug infiltrate and entire procedure is repeated, after which solution is introduced until drug infiltrate of desired shape and size is not formed in cord canal. Needle is removed, skin in point of injection is processed with antiseptic and sterile bandage is applied.

EFFECT: method makes it possible to increase efficiency and safety of performing blockade of spermatic cord due to increase of accuracy of medications solution introduction.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of medicine, namely to chemical-pharmaceutical industry, in particular to production of medications intended for external application for treatment of wounds of various etiology including those which occur after burns. Pharmaceutical composition contains active substances - lidocaine, acemine, ofloxacine, auxiliary substances: preservative - nipagine, solvent - propyleneglycole and shape-former - purified water.

EFFECT: activation of skin granulation tissue growth, regeneration stimulation, acceleration of affected tissue healing and reduction of edema.

3 ex

FIELD: chemistry.

SUBSTANCE: invention discloses N-(2,6-dimethylphenyl)amide of 2-(β-N,N-diethylaminoethylamino)-4-oxo-4-(4-ethoxy-phenyl) of 2-butenoic acid of formula (I)


EFFECT: local anaesthetic activity.

1 cl, 1 ex, 2 tbl

FIELD: medicine.

SUBSTANCE: in claimed methods pharmaceutical substance, which contains active ingredients, is introduced in form of microemulsion. Microemulsion is introduced by means of application system, which makes it possible to disperse microemulsion by gaseous medium, containing at least 25 vol. %, preferably, at least, 50 vol. % of oxygen.

EFFECT: efficient local delivery into skin of medications, including little and poorly-soluble, due to synergic action of active element of medication and oxygen, supplied under pressure and considerably increasing microcirculation.

20 cl, 3 tbl, 4 dwg, 7 ex

FIELD: medicine.

SUBSTANCE: in conditions requiring block of a superior gluteal nerve, a patient is horizontally pronated with his feet adducted. A line marked in the middle is drawn from behind through a lower edge of an ischial bone and an upper edge of a wing of ilium. A line transversal to a longitudinal axis of a body is drawn through the mark and extended on a gluteal skin. Thereafter, from one side through a projection of a centre of the lower edge of the ischial bone and the upper edge of the wing of ilium, a second line is drawn, and its intersection with the line drawn transversally to the longitudinal axis of the body on skin is dotted to trace a needle therethrough into tissues in a frontal plane perpendicularly to a sagittal plane. Thereafter, a medicinal solution containing 60 ml of 0.25 % novocaine and 10 mg of vitamin B12 is injected with 0.2 mg of dexamethasone added per each 1 ml of the administered solution.

EFFECT: higher efficacy of the block of the superior gluteal nerve due to more precise drug delivery thereto.

2 cl, 2 dwg, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, and can be used if extremity vein catheterisation is required for multiple intravenous introduction of drug solutions. That is ensured by vein catheterisation followed by change of an extremity position with respect to a patient's trunk so that an open pavilion of the catheter is arranged below a level of a patient's right atrium. An infrared imager is used to monitor an extremity surface condition within a projection of the catheter. If observing a region of local hyperthermia along the vein, its content is examined by ultrasound. A thrombus if any is sized up; tourniquets are applied below and above the region of local hyperthermia to complete sanguimotion cessation in the vein. Then, blood is taken from the vein to its devastation, and the volume of taken blood portion is measured that is followed by introduction of 2% lidocaine hydrochloride 0.5 ml and a thrombolytic solution at temperature +42°C in the volume necessary for complete vein filling. 3 minutes later, the whole liquid vein content is removed through the catheter, and the tourniquets are released, the vein content is examined by ultrasound. The presence of a thrombus requires another 3-minute tourniquet application with venous blood replacement by a local anaesthetic solution with a thrombolytic agent to stabilise thrombus size, then the catheter is removed, and the drugs are introduced by means of another catheter which is inserted in another extremity vein.

EFFECT: method allows higher safety and effectiveness of vein catheterisation due to early phlebitis detection and exact delivery of fibrinolytic agents to the thrombus to dissolve a "fresh" portion of the thrombus that allows reducing a risk of thromboembolism.

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