Medicated mud composition

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, namely to a medicated mud composition. The medicated mud composition contains prepared sludge argillaceous deposits of Tambukan Lake, Witepsol W 35, Witepsol H 15, polyethylene glycol 1500, Cremophore RH, as well as carbon-dioxide herbal extracts specified in a group consisting of at least the common willow, sea buckthorn, oak, calendula, licorice, brier, sage and/or carbon-dioxide extract of propolis taken in certain relations.

EFFECT: composition enables extending the range of medicinal agents using therapeutic sludge argillaceous deposits.

10 ex

 

The invention relates to medicine, in particular to drugs - applicators and candles, and can be used in the production of mud treatment-and-prophylactic broad-spectrum (analgesic, anti-inflammatory, antispasmodic).

Known (patent RU 107943, publ. 2011) applicator for the treatment of fibrocystic mastopathy, containing the liner, made in the form of a circle with radius 5 cm or 7 cm, with a cutout in the center of the circle having the diameter of 3 cm, and with a remote sector, when folded having a form of a truncated cone, the liner is impregnated with a therapeutic composition of the juice of white cabbage and covered with plastic wrap.

A disadvantage of the known applicator admittedly limited scope.

Also known (patent RU 53902, publ. 2006) applicator in the form of a shell of material inside mud, representing homogenized silt-clay sediments, particle size of not more than 0.35 mm, and the sheath material inert to silt sulfide mud and provides movement of the useful components of mud in any direction to the skin or mucosa of the patient.

A disadvantage of the known applicator should recognize the lack of efficiency.

Known (patent RU 77159, publ. 2008) applicator, predstavlyalsya shell, inside mud, representing silt-clay sediments of lake Tambukan, mechanically cleaned from pollutants and pre-fragmented mineral inclusions, the sheath material is a nonwoven material, and the shell is additionally placed in a light - and gas-tight film.

A disadvantage of the known applicator should recognize the lack of efficiency.

The technical problem to be solved by the developed device is the extension of the range of pharmaceuticals, therapeutic uses of silt-clay sediments.

The technical result obtained by the implementation of the developed part of the mud treatment and prevention, is to increase the effectiveness and impact of the funds made based on the body.

To achieve the technical result of the proposed use mud treatment-and-prophylactic used to prepare applicators and candles mud containing Witepsol W 35, Witepsol N 15, polyethylene glycol 1500, pre-prepared silt-clay sediments of lake Tambukan, cremophor RH and carbon dioxide plant extracts and/or carbon dioxide extract of propolis in the following ratio of components (%):

p>
Witepsol N 1510-20
Pre-prepared
silt-clay sediments of lake Tambukan15-25
Polyethylene glycol 150015-25
Cremophor RH3-5
Carbon dioxide extracts and/or
carbon dioxide extract of propolis0.5 to 1.5
Witepsol W 35rest

moreover, the composition contains carbon dioxide extracts of plants selected from the group comprising, at least, willow, buckthorn, oak, calendula, licorice, rose hips, sage.

Used in the production of mud treatment-and-prophylactic silt-clay sediments of lake Tambukan contain crystallochemistry complex (20-50%), minerals (sulfides and chlorides of sodium, magnesium and potassium) and macroelements (calcium, iron, and others), hydrogen sulfide (0,2-0,4%), trace elements (zinc, copper, manganese, and others), biologically active substances (lipids, carotenoids, is minamikata, humic and vitamin-like compounds).

Before the introduction in the developed part of the medical-preventive silt-clay sediments of lake Tambukan undergoing the phase of preparation, during which the preliminary separating foreign mechanical inclusions included in the original silt-clay sediments with subsequent grinding of the particles silt-clay sediments up to a particle size of not more than 0.1 mm, determine the physico-chemical and sanitary-bacteriological indicators of crushed particles of sediment and lead to the correction of deviations of the parameters from the predefined parameters by chemical and/or mechanical impact.

It was experimentally found that only when using prepared this way, silt-clay sediments of lake Tambukan applicators and candles, composed of silt-clay sediments of lake Tambukan, achieved the specified technical result.

In the production of the composition of the mud treatment-and-prophylactic original mix components. In the following the obtained composition is formed cylindrical with pointed ends or flat items.

Further features and advantages of the developed composition will be disclosed in the examples.

1. Patient I., 21 years. Diagnosis: sclerosis the religious changes of the ovaries. Infertility 1. Married 10 years, her husband is healthy. The last 7 years of age are not protected. It was suggested treatment applicators on the device closest to analogue. A noticeable effect in the treatment within 1 year is not marked. It is proposed to use the applicator containing the composition (%):

Witepsol N 1515
Pre-prepared
silt-clay sediments of lake Tambukan20
Polyethylene glycol 150020
Cremophor RH4
Carbon dioxide extract of sea buckthorn0,5
Carbon dioxide extract of propolis0,5
Witepsol W 3540

During the first procedure was performed by exposure of the applicator of the specified structure on the area of the inguinal folds at points located at a distance of 8-9 cm from the midline, for a period of 8-9 minutes Then the treatment was continued with daily application of 1 min with prolongation for 1 minute to 30 minutes Then 5 minutes prolonges the it applications to achieve a 3-hour period. Start of treatment November 2010 end of March 2011 completed Treatment in connection with pregnancy. Delivery on time. Research on hormone levels in the blood did not. The common analysis of a blood in norm throughout the treatment period, the treatment was carried out under the supervision of a gynecologist.

2. Patient S., aged 57. The diagnosis of adenoma of the prostate gland. Therapy within 2 months of using the applicator according to the decision - closest analogue to the area of the prostate. Procedures were performed daily. Noticeable relief was noted. It was proposed to use the applicator composition (%):

Witepsol N 1512
Pre-prepared
silt-clay sediments of lake Tambukan22
Polyethylene glycol 150017
Cremophor RH3
Carbon dioxide extract of oak1
Witepsol W 3545

The first procedure 5 min with daily renewal 5 minutes after reaching 3-hour prod is littelest the treatment was performed with preservation of the period of exposure for 7 months. Before treatment, the frequent urge to urinate, up to 6 times per night. After treatment retching stopped. According to the ultrasound volume adenomas decreased 1.5 times. Residual urine volume 15 ml (was 5 ml instead of 20 ml). Feeling good in the blood decrease previously elevated leukemia to normal values. Treatment discontinued at the patient in the absence of clinical symptoms. The decrease in adenoma confirmed by a urologist.

3. Patient M., aged 39. The diagnosis of fibrocystic disease of the breast. Confirmed by mammography and ultrasound. Worried about breast tenderness to palpation. Previously conducted within 6 months of the treatment applicator, known from the closest analogue. The effect is negligible. Was the use of the treatment applicator composition (%):

Witepsol W 35
Witepsol N 1510
Pre-prepared
silt-clay sediments of lake Tambukan25
Polyethylene glycol 150015
Cremophor RH3
Carbon dioxide extract of sage1,5
45,5

Application was carried out on breast liners on line at 3-5 cm above the nipple. The duration of the first treatment 5 min, daily renewal procedures for 5 minutes until a total exposure of 2 h were Treated for 3 months with the supervision of a specialist, after the treatment was carried out radiography and ultrasound. Pathological changes there (ultrasound monitoring was conducted twice during treatment at the place of residence and mammosite). Breast tenderness to palpation disappeared. General analysis of blood and urine for the entire period of treatment without significant deviations from the norm. Follow-up within 2 years of the signs of mastitis is not revealed. The patient was withdrawn from the account of the district oncologist.

4. Patient N., 38 years. The diagnosis of a cyst of the left ovary, 4×7 see Complaints about dragging pain in the left side. Was conducted therapy with the use of the applicator, known from the source - the closest analogue in 4 months. Noticeable improvement is not observed. It was proposed to use candles composition (%):

Witepsol N 1514
Pre-prepared
silt-clayey sediments of the lake There is given 22
Polyethylene glycol 150022
Cremophor RH3
Carbon dioxide extract of sea buckthorn1,5
Witepsol W 3537,5

Application was carried out on the pelvic area for 4 months according to the following scheme: 1 procedure applique for 1 min, daily extension for 1 min to achieve 30 minutes Then daily extension for 5 min to achieve a 3-hour threshold. Ultrasound monitoring on a monthly basis. Therapy was discontinued in connection with the disappearance of the cyst that was established by two independent experts ultrasound in the clinic and in research Institute of obstetrics and gynecology. General analysis of blood and urine without features the entire period of treatment, being fully normalized, the pain disappeared.

5. Patient M 17 years. Complaints of irregularity and extreme pain mensis. Data pelvic ultrasound without pathology. General analysis of blood without features. Research on hormones showed a decrease in total oestrogens in the blood of 50 PG/ml in all phases of the cycle. Was therapy applicator, known from the technical solutions - the closest analogue in 3 months. Tangible effect is not obtained. Proposed and the use applicator composition (%):

Witepsol N 1515
Pre-prepared
silt-clay sediments of lake Tambukan20
Polyethylene glycol 150015
Cremophor RH4
Carbon dioxide extract of sea buckthorn0,5
Carbon dioxide extract of propolis0,5
Witepsol W 3545

impact on the field of appendages for 2 months according to the following scheme: 1 procedure applique for 5 min, then daily extension for 5 min to achieve a 3-hour duration after treatment, normalization of menstrual cycle, a sharp reduction of morbidity mensis. The content of oestrogens in the blood (PG/ml): phase I 78, II 220, III 250, which corresponds to normal.

6. Patient A., 64 years. Diagnosis: deforming arthrosis of knee joints, sharp pain when moving. Was offered therapy with the use of the applicator closest analogue in 4 months. Tangible improvements not n is stepped. It was proposed to use the applicator composition (%):

Witepsol N 1520
Pre-prepared
silt-clay sediments of lake Tambukan20
Polyethylene glycol 150015
Cremophor RH5
Carbon dioxide extract of sea buckthorn0,5
Carbon dioxide extract of rose hips0,5
Witepsol W 3539

The most pronounced inflammatory process defined using palpation, the patient was held applique with elastic fixation bandage. The treatment was carried out according to the scheme: 1 procedure applique for 5 min, daily renewal application in 5 minutes each day to achieve a 6-hour duration. The duration of treatment is 6 months. Result of treatment: the disappearance of pain in the area of the joint space and the condyles of the tibia palpation and restore joint mobility.

7. Patient I., aged 35. EGNOS: postthrombotic disease of the right lower limb, complicated by trophic ulcers in the granulation phase. The patient is suffering from this disease for 12 years. The treatment was performed using a mud applicator - the closest analogue. The ulcer was cured, but during the autumn and spring came again. It was proposed to use for the treatment applicator composition (%):

Witepsol N 1517
Pre-prepared
silt-clay sediments of lake Tambukan25
Polyethylene glycol 150015
Cremophor RH3
Carbon dioxide extract of calendula0,5
Carbon dioxide extract of propolis1,0
Witepsol W 35a 38.5

The treatment was performed by applying the applicators on the right lower limb. Treatment consisted of ten procedures, one procedure per day. The duration of one procedure from 40 to 50 minutes. In the course of treatment was observed positive the th dynamics - decreased swelling of the legs, decreased inforce skin tibia, improved granulation of ulcers. Within two years, the ulcer appears. Subjectively noted improvement in health.

8. Patient U., 42 years. Diagnosis: generalized form of periodontitis of moderate severity. Complained of bleeding gums, hyperesthesia enamel, tooth mobility of 1-2 degrees in the frontal section, II-III degree in the group of molars. Received treatment within 2 months using applicators - closest analogues without a noticeable improvement in the condition of the oral cavity. Then underwent treatment with the use of applicators composition (%):

Witepsol N 1518
Pre-prepared
silt-clay sediments of lake Tambukan22
Polyethylene glycol 150015
Cremophor RH5
Carbon dioxide extract of oak0,5
Carbon dioxide extract of sage0,5
Witepsol W 35 39

The applicator was on the gums for 15-20 minutes. Procedures were performed continuously for 15 days. Before and after treatment was performed in vivo biomicroscopy, reproduktory, orthopantomogram. Identified improvement of microcirculation in the gums with a decrease in venous-lymphatic stasis and increase the active surface of the capillaries, reducing interstitial edema. On the orthopantomogram a tendency to stop the horizontal and vertical bone resorption. Clinically Desna has normal color, decreased mobility of the teeth to 0-1 extent, disappeared hyperesthesia of the teeth and bleeding gums.

9. Patient M., aged 47. Diagnosis: chronic generalized gingivitis, hypertrophic form of moderate severity. Was conducted the standard medical treatment, removal of dental plaque, scraping pathological pockets and additionally underwent a course of rehabilitation treatment using applicator - the closest analogue. Noticeable effect was not obtained. It was proposed to use the applicator composition (%):

Witepsol N 1510
Pre-prepared
silt-clay sediments of lake Tambukan25
Polyethylene glycol 150020
Cremophor RH5
Carbon dioxide extract of oak1,0
Carbon dioxide extract of calendula0,5
Witepsol W 35a 38.5

Procedures were performed daily for 12 days. After 7-8 sessions, there was significant improvement of the patient. After the 12th session gingival bleeding completely stopped.

10. Patient O., 37 years. Complaints of constant aching pain in the right hypochondrium, nausea after ingestion of fatty foods, bitter taste in the mouth, yellow sclera and skin. Cholelithiasis is suffering for 6 years. Objective examination revealed that the sclera and skin, jaundice, tongue moist, coated thick root yellow tinge, there are imprints of teeth. Palpation of the abdomen is painful, in right hypochondrium positive symptoms Kera-Hausman, Ortner. Cardiovascular, respiratory systems without features. Ultrasound examination showed the presence of stones in the gall about is the OK. Previously operated on for acute calculous cholecystitis, mechanical jaundice. Produced cholecystectomy, drainage choledochus by Halstead. Treated by the application of the projection liver applicators composition (%):

Witepsol N 1515
Pre-prepared
silt-clay sediments of lake Tambukan25
Polyethylene glycol 150015
Cremophor RH5
Carbon dioxide extract of licorice1,0
Carbon dioxide extract of oak0,5
Witepsol W 35a 38.5

The treatment was performed within 14 days of sessions for 30 minutes Upon completion of the course the stones in the bile ducts are absent.

Applicators and candles on the basis of the developed composition have analgesic, anti-inflammatory, antispasmodic action.

The mud treatment-and-prophylactic, characterized by the fact that it contains pre-training is blennie silt-clay sediments of lake Tambukan, Witepsol W 35, Witepsol N 15, polyethylene glycol 1500, cremophor RH and carbon dioxide extracts selected from the group comprising, at least, willow, buckthorn, oak, calendula, licorice, rose hips, sage and/or carbon dioxide extract of propolis in the following ratio of components (%):

Witepsol N 1510-20
Pre-prepared
silt-clay sediments of lake Tambukan15-25
Polyethylene glycol 150015-25
Cremophor RH3-5
Carbon dioxide extracts and/or
carbon dioxide extract of propolis0.5 to 1.5
Witepsol W 35rest



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry, namely to a treating-preventive mud composition. The treating-preventive mud composition contains preliminarily prepared silt-clayey deposits of lake Tambukan, polyethyleneglycol 4000, polyethyleneglycol 1500, cremophor RH, as well as a carbon dioxide extract of propolis and/or a carbon dioxide vegetable extract, selected from the group, which includes, at least, eucalyptus, dog-rose, hop, laurel, chamomile, licorice and oak, taken in a specified ratio of components.

EFFECT: composition has an increased treating-preventive activity with respect to a patient's organism.

9 ex

Novel application // 2530567

FIELD: medicine.

SUBSTANCE: group of inventions relates to medicine and deals with a preparation for the prevention of an inflammatory disease of the intestine, which represents galactooligosaccharide, which has a degree of polymerisation 3 or higher, selected from the group, consisting of trisaccharides Gal(β 1-6)-Gal(β 1-4)-Glc, Gal(β 1-3)-Gal(β 1-4)-Glc, tetrasaccharide Gal(β 1-6)-Gal(β 1-6)-Gal(β 1-4)-Glc and pentasaccharide Gal(β 1-6)-Gal(β 1-6)-Gal(β 1-6)-Gal(β 1-4)-Glc; application of the claimed galactooligosaccharide for the prevention of the inflammatory disease of the intestine; a method of preventing the inflammatory disease of the intestine, which includes peroral introduction to a mammal of an effective quantity of galactooligosaccharide.

EFFECT: group of inventions provide the powerful anti-inflammatory effect with respect to the inflammatory diseases of the intestine.

10 cl, 9 dwg, 4 ex

FIELD: medicine.

SUBSTANCE: invention refers to immunology and biotechnology. What is presented is a single-domain antibody (VHH) able to bind the cytokine human necrosis factor (TNF), a DNA fragment coding the antibody according to the invention, as well as a method for identifying the human TNF and measuring it in a biological sample.

EFFECT: invention provides the specific block of macrophague-monocytic TNF cells and can find further application in therapy of the diseases associated with an undesired TNF-dependent inflammatory response.

4 cl, 5 ex, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: in general formula A1 stands for CR10R11 or S; A2 stands for CR12R13, C(=O), O, S or S(=O)2; R1 stands for C1-10-alkyl, saturated or unsaturated, branched or non-branched, non-substituted, or monosubstituted, or polysubstituted; C3-10-cycloalkyl or 5- or 6-membered heterocyclyl with the O-atom, each time saturated or unsaturated, non-substituted, or monosubstituted, or polysubstituted; C6-10-aryl or C5-10-heteroaryl with 1-3 heteroatoms, selected from N, O or S, each time non-substituted, or monosubstituted, or polysubstituted; through C1-8-alkyl or C2-8-heteroalkyl bound by the bridge bond C3-10-cycloalkyl, each time saturated, non-substituted, and the alkyl or heteroalkyl chain each time can be branched or non-branched, saturated, non-substituted; or through C1-8-alkyl, bound by the bridge bond aryl or heteroaryl, each time non-substituted, or monosubstituted, or polysubstituted, and the alkyl chain each time can be branched or non-branched, saturated or unsaturated, non-substituted, or monosubstituted, or polysubstituted; R2, R3 and R4 each time independently on each other stand for H; F; Cl; Br; I; methyl; O-C1-6-alkyl or NRaRb, and Ra and Rb together with the nitrogen atom that binds them form heterocyclyl, saturated, non-branched, non-substituted; R5, R6, R7, R8, R10, R11, R12 and R13each time independently on each other stand for H; F; Cl; Br; I; OH or C1-10-alkul; or R5 and R6 or R7 and R11 together with carbon atom(s), that bind(s) them form C3-8-cycloalkyl, each time saturated or non-saturated, non-substituted, or monosubstituted, or polysubstituted; with respective remaining substituents R5, R6, R7, R8, R10, R11, R12 and R13 having the value given above; R9 stands for C3-10-cycloalkyl, saturated, non-substituted; C6-10-aryl or 5- or 6-membered heteroaryl with heteroatom, selected from N and S, each time non-substituted or monosubstituted.

EFFECT: invention relates to substituted nicotinamides of general formula (1), to a medication based on them and their application for treating KCNQ2/3-mediated diseases.

13 cl, 3 tbl, 224 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound of formula (I) , where ring A is cycloalkane ring with number of members from 3 to 7, benzene ring or monocyclic 5-member or 6-member aromatic heterocyclic ring, containing 1 heteromember of ring, selected from the group, containing N and S, and benzene and heterocyclic rings can optionally have one or two similar or different substituents, selected from the group, containing halogen, HO-, R1-O-, H2N-C(O)- and NC-; Y is selected from the group, containing S, C(R12)=C(R13) and C(R15)=N; Z is selected from the group, containing C(R16); R1, R30, R33, R35, R54 and R55 independently on each other group R1, R30, R33, R35, R54 and R55 are selected from the group, containing (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C7)-cycloalkyl and (C3-C7)-cycloalkyl-(C1-C4)-alkyl-, and all of them can optionally have one or more similar or different substituents R70; R3 and R5 represent hydrogen; R4 and R6 are selected independently on each other, from the group, containing hydrogen and , (C1-C4)-alkyl; R12, R13, R15 and R16 are selected independently on each other, from the group, containing hydrogen, halogen and O2N-; R20 is selected from the group, containing hydrogen and (C1-C4)-alkyl; one of the groups R21 and R22 is group of formula II: R24-R23-, and the other of groups R21 and R22 is selected from the group, containing hydrogen, halogen, R30, HO-, R30-O-, R30-S(O)m-, H2N-, R30-NH-, R30-N(R30)-, R30-C(O)- and NC-; R23 is chain, containing from 1 to 5 chain members of which 0 or 1 chain member is heteromember of chain, selected from the group, containing N(R25), O, S, with other chain members being similar or different groups C(R26)(R26), where two adjacent groups can be bound to each other by double bond; R24 is selected from the group, containing hydrogen, R31, R31-O-, R31-NH-, R31-N(R31)-, R31-C(O)-NH-, HO-C(O)- and monocyclic, bicyclic or tricyclic ring with number of members from 5 to 10, which is saturated or non-saturated and contains 0, 1, 2 or 3 similar or different ring heteromembers, selected from the group, containing N, N(R32), O, S, and ring can optionally have on ring carbon atoms one or 2-3 similar or different substituents, selected from the group, containing halogen, R33, R33-O-, R33-S(O)m-, R33-C(O)-NH-, R33-S(O)2-NH-, R33-C(O)-, HO-C(O)-, H2N-C(O)-, R33-NH-C(O)-, R33-N(R33)-S(O)2-, NC-, oxo, phenyl and Het; on condition that total number of C, N, O and S atoms, present in two groups R23 and R24, constitutes not less than 5; R25 is selected from the group, containing hydrogen and (C1-C4)-alkyl; R26, independently on each other group R26, is selected from the group, containing hydrogen, fluorine, (C1-C4)-alkyl and HO-, or two groups R26, together with included into them chain members, form monocyclic ring with number of members 4, which is saturated and contains 1 ring heteromember, selected from the group, containing O; R31 is selected from the group, containing (C1-C6)-alkyl, which can optionally have one substituent R70; R32 is selected independently on each other, from the group, containing hydrogen, R35 and phenyl; R50 is selected from the group, containing R51-O- and R52-N(R53)-; R51 is selected from the group, containing hydrogen and R54; R52 is selected from the group, containing hydrogen; R53 is selected from the group, containing hydrogen; R70 is selected from the group, containing HO-, R71-O-, H2N-, R71-NH-, R71-N(R71)-, R71-C(O)-NH-, HO-C(O)-, H2N-C(O)- and phenyl; R71, independently on each other group R71, is selected from the group, containing (C1-C4)-alkyl; Het, independently on each other group Het, is monocyclic heterocyclic ring with number of members 5, which contains 1 or 2 similar or different ring heteromembers, selected from the group, containing N and S, and ring is saturated or non-saturated and optionally substituted with one or more similar or different substituents, selected from the group, containing (C1-C4)-alkyl; m, independently on each other number m, is integer number, selected from the group, containing 0, 1 and 2; phenyl, independently on each other phenyl group, can optionally have one or more similar or different substituents, selected from the group, containing halogen and (C1-C4)-alkyl.

EFFECT: invention also relates to method of obtaining compound of formula (I) and its application for manufacturing pharmaceutical for inhibiting receptor Edg-2.

17 cl, 14 tbl, 362 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) , where R1 and R2 have the following values: (i) R1 and R2 together form =O; (ii) R1 and R2 together with carbon atom, which they are bound with, form duoxacycloalkyl; R1 represents hydrogen or halogen; and R2 represents halogen; (iv) R1 represents C1-6alkyl, where alkyl is optionally substituted with cyano, -RxS(O)qRv or -RxNRyRz; and R2 represents hydrogen; (v) R1 represents -OR12 or -NR13R14; and R2 represents hydrogen, deutero or phenyl, which is optionally substituted with halogen; R3 represents hydrogen, halogen, C1-6alkyl, cyano, halogen C1-6alkyl, C3-10cycloalkyl or C1-6alkoxy; R4 and R5 represent hydrogen; R6 is independently selected from halogen, C1-6alkyl, halogenC1-6alkyl, -RxOR18 and -RxS(O)qRv; R7 independently represents halogen or -RxORw; R12 is selected from hydrogen and C1-6alkyl, R13 represents hydrogen; R14 is selected from hydrogen, C3-10cycloalkyl, -C(O)Rv and -C(O)ORw; R18 represents hydrogen, C1-6alkyl, or pyperidinyl, where R18 is optionally substituted with 1-3 Q1 groups, each Q1 is independenly selected from hydroxyl, C1-6alkoxy, C1-6alkoxycarbonyl, carboxyl and morpholinyl; Rx independently represents C1-6alkylene or simple bond; Rv and Rw represent hydrogen or C1-6alkyl; Ry and Rz represent hydrogen; n has value 0-4; p has value 0-5; and each q independently has value 0, 1 or 2. Invention also relates to compounds of formula (II) , where substituents have values, given in the invention formula, to pharmaceutical composition, possessing inhibiting activity with respect to JAK kinases, containing compounds of formula (I) or (II), methods of treating JAK-modulated disease, and application of compounds of formula (I) or (II).

EFFECT: compounds of formula (I) or (II) as inhibitors of JAK kinases.

32 cl, 6 dwg, 2 tbl, 84 ex

FIELD: medicine.

SUBSTANCE: method is implemented by correcting rat's prostatic structural homeostasis in adaptation to low seasonal temperature conditions with the use of dihydroquercetin administered daily in a dose of 5 mg/kg of body weight prior to cooling for four weeks.

EFFECT: developing the method for increasing the adaptive capability of laboratory animal's prostate to low seasonal temperatures.

2 dwg, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new benzene sulphonamide compounds, wherein the compounds are specified in a group of the following compounds, including additive salts with pharmaceutically acceptable acid, additive salts with pharmaceutically acceptable base and enantiomers of these compounds: 1) 3-[(4-but-2-inyloxybenzenesulphonyl)-methylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 2) (S)-3-(4-but-2-inyloxybenzenesulphonylamino)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 3) (S)-3-(4-benzyloxybenzenesulphonylamino)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 4) (S)-3-[(4-benzyloxybenzenesulphonyl)-methylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 5) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 6) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(naphthalen-1-ylmethoxy)-benzenesulphonylamino]-propionamide, 7) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-(4-propoxybenzenesulphonylamino)-propionamide, 8) (S)-3-[4-(3-cyanobenzyloxy)-benzenesulphonylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 9) (S)-3-[4-(4-cyanobenzyloxy)-benzenesulphonylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 10) benzyl-4-{(S)-1-hydroxycarbamoyl-2-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-entyl}-piperazine-1-carboxylate, 11) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-phenylpiperidin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 12) (R)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 13) (S)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-2-piperazin-1-ylpropionamide, 14) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide hydrochloride, 15) tert-butyl-3-{4-[(S)-2-hydroxycarbamoyl-2-(4-methanesulphonylpiperazin-1-yl)-ethylsulphamoyl]-phenoxymethyl}-2-methylindole-1-carboxylate difluoroacetate, 16) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(quinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 17) (S)-2-(4-benzylpiperazin-1-yl)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 18) (S)-2-[4-(4-fluorobenzyl)-piperazin-1-yl]-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino-propionamide, 19) (S)-2-(4-ethulpiperazin-1-yl)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 20) (S)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-2-[4-(4-trifluoromethylbenzyl)-piperazin-1-yl]-propionamide, 21) (S)-N-hydroxy-2-[4-(4-methylbenzyl)-piperazin-1-yl]-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 22) (S)-3-[4-(benzoisoxazol-3-ylmethoxy)-benzenesulphonylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 23) (S)-N-hydroxy-2-(4-isobutyrylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 24) (S)-N-hydroxy-2-[4-(2-methylpropane-1-sulphonyl)-piperazin-1-yl]-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 25) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-trifluoromethylpyrazolo[1,5-a]pyridin-3-ylmethoxy)-benzenesulphonylamino]-propionamide, 26) (S)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-2-[4-(propane-2-sulphonyl)-piperazin-1-yl]-propionamide, and 27) (S)-2-(4-benzylpiperazin-1-yl)-N-hydroxy-3-[4-(2-trifluoromethylpyrazolo[1,5-a]pyridin-3-ylmethoxy)-benzenesulphonylamino]-propionamide. The invention also refers to pharmaceutical and cosmetic compositions on the basis of the above compounds possessing TNFα-converting enzyme (TACE) activity.

EFFECT: there are prepared new compounds and compositions on the basis thereof which can be used in medicine and veterinary science for treating rheumatoid arthritis, non-insulin dependent diabetes mellitus, Crohn's disease or inflammatory skin disease.

35 cl, 28 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I), wherein A means morpholinyl, 1,4-oxazepamyl, piperidinyl, pyrrolidinyl or azetidinyl which is bound to N; R1 means C1-C6-alkyl group; R2 means bicyclic aryl group specified in 1H-indolyl, 1H-pyrrolo[3,2-b]pyridyl, quinolyl, naphthyl, 1H-pyrrolo[2,3-b]pyridyl, 5H-pyrrolo[3,2-d]pyrimidinyl, 7H-pyrrolo[2,3-d]pyrimidinyl, benzo[b]thiophenyl, imidazo[1,2-a]pyridyl, benzo[b]thiazolyl, 5H-pyrrolol[2,3-b]pyrazinyl and quinoxalinyl which can be substituted by R4; R3 means hydrogen or halogen atom; R4 means C1-C6-alkyl group, C1-C6-halogenalkyl group, OR1A, halogen, -(CH2)aOH, CN, NHCOR1A, SO2R1A or NHSO2R1A; R5 means C1-C6-alkyl group, -(CH2)aOH, -(CH2)aOR1B, halogen or CONH2; provided p is a plural number, R5 can be identical or different, or R5 can be combined with another R5; each of R1A and R1B independently means C1-C6-alkyl group; a is equal to 0, 1 or 2; n is equal to 1 or 2; p is equal to 0, 1, 2, 3, 4 or 5. Besides, the invention refers to intermediate compounds of formulas (IA) and (IB) for preparing the compounds of formula (I), to a preventive or therapeutic agent containing the compounds of formula (I), pharmaceutical compositions, using the compounds of formula (I) and to a method for preventing or treating diseases.

EFFECT: compounds of formula (I) as selective 5-HT2B receptor antagonists.

11 cl, 1 dwg, 18 tbl, 88 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula

,

wherein: each of R1, R2, R4, R5, R6, R7, R8 R9, R10, R11, R12, R13, R14, R15 R16 and R17 is independently specified in a group consisting of deuterium or hydrogen; and R3 is independently specified in a group consisting of CD3 and CH3; provided R3 represents CH3, at least one of the groups R1, R2, R4, R5, R6, R7, R8 R9, R10, R11, R12, R13, R14, R15 R16 and R17 represents deuterium; and R18 represents hydrogen. The invention also refers to a drug on the basis of the above compound for treating a condition causing pain.

EFFECT: there are prepared new compounds inhibiting MMPs (metalloproteinases) which show the high activity, metabolic stability and/or lower toxicity in relation to the currently known MMP inhibitors for treating pain and other diseases, such as cancer.

16 cl, 2 dwg, 14 tbl, 136 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry, namely to a treating-preventive mud composition. The treating-preventive mud composition contains preliminarily prepared silt-clayey deposits of lake Tambukan, polyethyleneglycol 4000, polyethyleneglycol 1500, cremophor RH, as well as a carbon dioxide extract of propolis and/or a carbon dioxide vegetable extract, selected from the group, which includes, at least, eucalyptus, dog-rose, hop, laurel, chamomile, licorice and oak, taken in a specified ratio of components.

EFFECT: composition has an increased treating-preventive activity with respect to a patient's organism.

9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions concerns an oral care composition and using this composition for halitosis prevention. The presented oral composition for relieving indole-induced halitosis contains the amino acid L-serine in the amount of 0.3 to 10 wt %/wt. What is presented is a method of treating or preventing indole-induced halitosis with using the above composition and using the above composition in the method of treating or preventing indole-induced halitosis, wherein the above composition is administered into the oral cavity.

EFFECT: using L-serine in the above amounts as an ingredient of the oral care agents is effective for relieving indole-induced halitosis.

21 cl, 8 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of cosmetology and represents external preparation for skin, including (a) from 0.01 to 5 wt % of 4-isobutylresorcinol or its salt and (b) from 0.01 to 5 wt % of one or more compound, selected from L-ascorbic acid or its salt and 3-O-ethyl-L-ascorbic acid or its salt, and ingredients, which are usually applied in external preparations for skin - the remaining part.

EFFECT: invention provides excellent temperature stability, especially under high temperatures and photostability.

2 cl, 23 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to method of conserving water preparation of calcium compounds, which includes the following stages: (a) obtaining water preparation of at least one calcium compound; (b) addition to water preparation of stage a) of one or more sources of lithium ions in such quantity that the total quantity of lithium ions in water preparation constitutes from 750 to less than 3000 per mille , calculated relative to water in preparation; (c) addition to water preparation of stage a) of one or more sources of sodium ions and/or potassium ions in such quantity that the total quantity of sodium and/or potassium ions in water preparation constitutes from 3000 to less than 7500 per mille, calculated relative to water in preparation, where stages (b) and (c) can be performed simultaneously or separately in any order.

EFFECT: method improvement.

23 cl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to biologically active composition for treatment of genitourinary system in men and women, superficial skin injuries, as well as for intimate hygiene. Claimed composition includes essential oil of Melaleuca in amount 27-33 vol. %, essential oil of thyme in amount 18-22 vol. % and camphor.

EFFECT: invention provides increased efficiency of impact on human organism in case of said diseases.

2 cl, 12 ex

Baby shampoo // 2529811

FIELD: medicine.

SUBSTANCE: invention represents baby shampoo containing lauryl glucoside, cocamidoprophyl betaine, sodium cocoyl isethionate, coco-glycoside, glyceryl oleate, citric acid, hypoallergenic aromatic composition, methylisothiasolinone, iodopropyl butylcarbomate, propylene glycol extract of wheat grains, propylene glycol extract of chamomile and purified water.

EFFECT: extended range of baby shampoos that can be used for daily care.

2 ex

FIELD: medicine.

SUBSTANCE: invention represents baby cream for daily care containing D-panthenol, purified water, olive oil, vitamin E, cedar nut oil, polyglycerol 3-methylglucose distearate, saccharose stearate, sorbitan stearate, cetearyl alcohol, coco-caprylate/caprate, dicaprylyl ester, methylisothiazolinone and iodopropyl butylcarbomate, citric acid, hypoallergenic aromatic composition with the ingredients in cream taken in certain proportions, wt %.

EFFECT: extended range of products for daily baby skin care.

5 ex

Two-phase developer // 2529807

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to cosmetology and represents cosmetic preparation for treatment of keratin fibres, characterised by the fact that it includes, at least, two distant from each other phases and non-ionic, anionic, zwitterionic and/or amphoteric tensides and/or emulsifiers in the total amount less than 1 wt % calculated per the total weight of preparation, and first phase (I) represents water phase, which contains, at least, one chemical oxidiser, selected from hydrogen peroxide and second phase (II) represents hydrophobic phase, which contains, at least, one silicone oil, selected from cyclomethicone, and both phases are in two layers, one above the other.

EFFECT: invention ensures stabilisation of active agents in oxidising composition.

5 cl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to biologically active agent for preventing and treating urogenital diseases in men and women, skin surface damages, as well as to intime hygiene preparation for preventing sexually-transmitted diseases. The biologically active agent contains a biologically active composition and an excipient. The biologically active composition contains camphor, tea tree oil and thyme oil in certain amount.

EFFECT: biologically active agent is effective for preventing and treating urogenital diseases in men and women, skin surface damages, as well as the intime hygiene preparation for preventing sexually-transmitted diseases.

11 cl, 13 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to cosmetology and describes solid preparation in form of powder, which contains powder-like component, oil component as binding substance and mixture of amides, obtained by amidation of mixture of hexamethylenediamine and bisaminomethylcyclohexane with fatty acids of hydrogenated castor oil.

EFFECT: preparation prevents greasy luster, flowing of makeup and possessing long-lasting makeup effect.

25 cl, 4 dwg, 10 tbl, 10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry, namely to a treating-preventive mud composition. The treating-preventive mud composition contains preliminarily prepared silt-clayey deposits of lake Tambukan, polyethyleneglycol 4000, polyethyleneglycol 1500, cremophor RH, as well as a carbon dioxide extract of propolis and/or a carbon dioxide vegetable extract, selected from the group, which includes, at least, eucalyptus, dog-rose, hop, laurel, chamomile, licorice and oak, taken in a specified ratio of components.

EFFECT: composition has an increased treating-preventive activity with respect to a patient's organism.

9 ex

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