Treating-preventive mud composition

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

 

The invention relates to medicine, in particular to medicinal form applicators and candles, and can be used in the manufacture of mud treatment-and-prophylactic products 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 representing the FDS is th 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-prophylactic means, is to increase the effectiveness and impact of the funds made based on the body.

To achieve the technical result of the proposed use of the composition of the mud treatment-and-prophylactic agent containing a polyethylene glycol 4000, 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 (%):

Pre-prepared
silt-clay sediments of lake Tambukan15-25
Polyethylene glycol 150015-25
Cremophor RH3-5
Carbon dioxide plant extracts and/or
carbon dioxide extract of propolis0.5 to 1.5
Polyethylene glycol 4000rest

moreover, as carbon dioxide plant extracts used carbon dioxide extracts of plants selected from the group comprising, at least, eucalyptus, rose hip, hop, Laurel, chamomile, licorice and oak.

Used in the production of mud treatment-and-prophylactic means (applicators, candles) 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, amino acids, humic and vitamin like compound).

Before rst is the group of the composition of the mud preventive and curative medicines silt-clay sediments of lake Tambukan undergoing the phase of preparation, during which preliminary separate foreign mechanical inclusions included in the original silt-clay sediments with subsequent grinding of the particles silt-clay sediments to the size 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 mud treatment-and-prophylactic means, composed of silt-clay sediments of lake Tambukan, allow to obtain the specified technical result.

In the production of mud treatment-and-prophylactic means original mix components included in the composition, and form from them a cylindrical, preferably, with pointed ends or flat items.

In the future, the nature and advantages of the developed composition of the mud of health care resources will be discussed using examples of implementation.

1. Patient S., aged 54. Diagnosis: chronic Colitis, the stage of incomplete remission. At admission the patient is moderately expressed vocal is the mucous membrane of the rectum and sigmoid colon. To relieve inflammation in the distal bowel the patient underwent a course of medical microenemas in combination with the placement of the applicators in the stomach. The treatment applicator - the closest analogue for 30 days (routine 40 minutes) did not lead to a noticeable improvement of the patient. Was treated by the similar method (a combination of rectal applicator swab and overlay applicator on his stomach on the area of the rectum and sigmoid colon) using the applicator composition (%):

Pre-prepared
silt-clay sediments of lake Tambukan25
Polyethylene glycol 150015
Cremophor RH3
Carbon dioxide extracts of rosehip0,5
Carbon dioxide extract of propolis1,0
Polyethylene glycol 400055,5

Procedures were performed every other day. The course of treatment consisted of 8 treatments. As a result of treatment of the patient using applicat the RA developed composition has been used to achieve the disappearance of pathological subjective and objective symptoms and get lasting therapeutic effect with prolonged remission.

2. Patient U., 52 years old. Diagnosis: Chronic combined hemorrhoids. Remission stage. Outpatient patients received rectal treatment with use of the applicator closest analogue. The procedures were carried out 2 days in a row with a break on the 3rd day. Treatment consisted of 8 treatments. Improving the condition of the patient was not followed. They were followed by a similar treatment with the applicator designed composition (%):

Silt-clay sediments of lake Tambukan20
Polyethylene glycol 150020
Cremophor RH5
Carbon dioxide extract of oak0,5
Carbon dioxide extract of propolis1,0
Polyethylene glycol 400053,5

Improved therapeutic effect in a patient came after 4-5 treatments. Decreased discomfort, pain in the rectum.

3. Patient M., 42 years. Diagnosis: granulating fissures. Ambulatory patients received rectal treatment with use of the applicator closest analogue. P is ocedure was carried out 3 days in a row with a break on the 4th day. Treatment consisted of 9 treatments. Improving the condition of the patient was not followed. Then were treated with the use of candles designed composition (%):

Pre-prepared
silt-clay sediments of lake Tambukan22
Polyethylene glycol 150017
Cremophor RH4
Carbon dioxide extracts of chamomile1
Polyethylene glycol 400056

Patients received a course of rectal mud designed applicator. Procedures were performed every other day. Conducted 8 procedures. After 3 treatments stopped the pain in the area of the crack. After 7 treatments during the inspection, complete healing of the fissure.

4. Patient K., 36 years. Diagnosis: Oophoritis chronic stage of remission. Pelvic ganglioneuritis. At admission the patient was worried about prolonged cramping abdominal pain associated with hypothermia, excessive discharge. The patient on the background of antibiotic therapy and electrophoresis of magnesium on the pelvic organs, using the receiving applicator - the closest analogue is additionally treated mud vaginal tampons temperature of 40-42°C in combination with disposable mud applicators in combination with thermocompression temperature 39-41°C "trusilova" zone with a duration of 20-30 minutes. Procedures were performed at the same time 2 days in a row with next day interruption of treatment 12 procedures. therapeutic effect is weak. Additionally, we performed a similar course using the applicator designed composition (%):

Silt-clay sediments of lake Tambukan25
Polyethylene glycol 150020
Cremophor RH5
Carbon dioxide extracts of hops0,5
Carbon dioxide extract of propolis0,5
Polyethylene glycol 400049

At the end of treatment showed a decrease in the frequency of pain and restoration of normal menstrual cycle.

5. Patient I., 32 years. Diagnosis: Condition after surgery for uterine fibroids. Expressed infiltrative, extensive adhesions of the change in pelvic cavity. Patient treatment mud vaginal tampons - the closest analogue is the temperature of 38-42°C by the developed method and the imposition of disposable applicators temperature of 38-42°C in complex with thermocompression "trusilova zone", with a duration of 10-20 minutes. The temperature of the mud treatments increased gradually during the course of treatment. Mud tampons were appointed after taking 2-3x mud applications. In the first half of the treatment procedures were applied every other day, the second two days in a row with the subsequent day of rest. The treatment course of 12 treatments. Treatments were alternated with General admission baths, vaginal irrigation and physiotherapy. therapeutic effect is weak. The treatment was repeated using using applicator designed composition (%):

Silt-clay sediments of lake Tambukan25
Polyethylene glycol 150025
Cremophor RH3
Carbon dioxide extract of eucalyptus0,5
Carbon dioxide extract of oak0,5
Polyethylene glycol 4000 46

The patient in the mud marked decrease in pain in the lower abdomen and lumbosacral region on the 8th procedure, reducing palpation tenderness and discharge to the 10th procedure. When the extract showed a significant improvement in health.

6. Patient E., 56 years. Was admitted to the neurology ward of the hospital with a diagnosis of syndrome of the shoulder blade periarthritis, secondary muscle contracture of the shoulder joint on the left. At clinical examination on the background of cervicobrachialgia bothered by pain in the establishment of the hands to the shoulder blade, the inability to bend the shoulder forward and take him to the horizontal line of the shoulder girdle. It was noted the pain of all muscles involved in shoulder girdle. Disease duration of 13 months. For the treatment of upper periostraca used the procedure developed mud applicators Tambukan dirt. Originally applicator closest analogue is imposed on nadopasana area to the left. On top of the applicator was positioned thermocouples with a temperature of 38°C and held layered wrap. Procedure duration 15-30 minutes. The treatment was carried out daily within 10 days of the procedure, the patient endured well. therapeutic effect is weak, the mobility of the arm and shoulder has not changed. The course was repeated using Apple atore composition (%):

Pre-prepared

Silt-clay sediments of lake Tambukan20
Polyethylene glycol 150020
Cremophor RH5
Carbon dioxide extracts of licorice0,5
Carbon dioxide extract of propolis0,5
Polyethylene glycol 400054

After 3 treatments the patient has decreased shoulder pain, neck muscles, increased range of motion in the cervical spine and shoulder. Dynamic observation showed that after each procedure, the amount of movement in the frontal and sagittal planes was increased by 5-7°. By the end of the treatment of movement in the shoulder joint increased significantly. After 4 months the patient caused by visual inspection. Had no complaints.

7. Patient I., 56 years. Diagnosis: chronic nonspecific prostatitis. Complaints during examination: pain syndrome, manifested by pain in the lumbar-sacral area and perineum, impaired urination, fatigue, irritability, loss libidos history: first diagnosed 9 years ago. Often, especially in the last 4-5 years. Treatment medication. In 2008, a Spa treatment (radon baths and mud packs "Cowards" for 6 treatments). Noted short-term improvement. Objective: clinical studies of the blood - increased leukocytosis, ECG without obvious signs of disturbance. During transrectal ultrasound revealed an increase in anterior-posterior size to 3.3±0.5 cm in diameter to 4.9-0.6 cm, prostate volume average increased up to 58.1±2.1 cm3violations echogenicity of the parenchyma. Indicators rheovasography reliably indicate venous stasis, reducing the level of all indicators of well-being, activity, mood, increased level of reactive anxiety.

The patient was prescribed a course of treatment: rectal swabs (composition - the nearest equivalent) with silt sulfide mud entered disposable syringe with a volume of 200-250 g, the temperature of the mud in the first procedure 38-40°C, subsequent procedures were carried out at a temperature of dirt 40-42°C, the exposure time when the first procedure 35 min, the subsequent procedures for 40 min, the course of treatment consisted of 14 treatments. The improvement has not come. Was repeated treatment with the use of the applicator composition (%):

Pre-prepared
silt-clay sediments of lake Tambukan23
Polyethylene glycol 150018
Cremophor RH5
Carbon dioxide extract of hops0,5
Carbon dioxide chamomile0,5
Polyethylene glycol 400053

The positive therapeutic effect of treatment was observed after 4-6 treatments and was accompanied by positive clinical dynamics and improvement of psychological status on tests and SAN Spielberg. The tolerability of the procedure was assessed by the patient on a scale as "comfortable". Indicators of days after treatment testified to normalize blood circulation in the pelvic organs, improve blood circulation by improving blood flow and reducing hypertonicity vessels. Improvement of the structure of the prostate after treatment were also observed at rectal ultrasound: reducing the size of the prostate gland, the disappearance of the seal areas of the parenchyma of the prostate. The patient noted improvement in psychoan the national status test (SAN): long-term results (after 6-12 months) were preserved and confirmed positive clinical and physiological given

8. Sick,, 32, Diagnosis: Cholelithiasis. Ultrasound of the gallbladder lumen many concretions up to 8 mm in diameter. On his stomach on the area of the gallbladder was placed applicator closest analogue 25 - 45 minutes daily for 14 days. A positive trend for smaller concretions and their sizes are not marked. Applied the applicator composition (%):

Pre-prepared
silt-clay sediments of lake Tambukan25
Polyethylene glycol 150015
Cremophor RH3
Carbon dioxide extract of licorice1,5
Polyethylene glycol 400055,5

Repeated ultrasound showed in the lumen of the significant decrease in the number of concretions, as well as their size up to 4 mm in diameter.

9. Patient M., 43 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. The rst is about the complex treatment, including the sanitation of the oral cavity, removal of above - and subgingival dental plaque, granulation, conducted the election of presledovanie teeth. Parallel mud using applicator - the closest analogue. The course was 15 daily procedures. therapeutic effect is not achieved. The course was repeated using the applicator composition (%):

Pre-prepared
silt-clay sediments of lake Tambukan25
Polyethylene glycol 150025
Cremophor RH5
Carbon dioxide extract of Laurus0,5
Carbon dioxide extract of oak0,5
Polyethylene glycol 400044

Before and after treatment conducted 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 orthopantomogram is the Amma marked tendency to the termination of 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.

Applicators and candles designed composition have analgesic, anti-inflammatory, antispasmodic action.

The mud treatment-and-prophylactic, characterized by the fact that it contains pre-prepared silt-clay sediments of lake Tambukan, polyethylene glycol 4000, polyethylene glycol 1500, cremophor RH and carbon dioxide plant extracts and/or carbon dioxide extract of propolis in the following ratio of components (%):

Pre-prepared
silt-clay sediments of lake Tambukan15-25
Polyethylene glycol 150015-25
Cremophor RH3-5
Carbon dioxide plant extracts and/or
Carbon dioxide extract of propolis0.5 to 1.5
Polyethylene glycol 4000rest

and ka is este carbon dioxide plant extracts used carbon dioxide extracts of plants, selected from the group which includes, at least, eucalyptus, rose hip, hop, Laurel, chamomile, licorice and oak.



 

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Novel application // 2530567

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

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FIELD: medicine.

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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: group of inventions refers to medicine and peptide chemistry, and concerns using tripeptide of general formula Tyr-Pro-D-Ser-X, wherein X - OH, OCH3, OC2H5 as an anti-inflammatory and analgesic agent, as well as a dosage form containing the above tripeptide for treating pains and inflammatory processes.

EFFECT: group of inventions provides higher efficacy of the agent and the dosage form.

3 cl, 22 ex, 5 tbl

FIELD: medicine.

SUBSTANCE: invention represents a drug preparation for treating diseases caused by type 1 herpes simplex and cytomegalovirus, containing recombinant human interferon 2α, lisocyme, Licopid, carnitine 20%, vitamin E and a fatty base.

EFFECT: higher clinical effectiveness and reduced length of treatment, prolonged intercurrent periods, lower recurrent rate by prophylactic administration, reduced manifestation of neurotoxic effects of herpes viruses, lower administration of antibiotics for preventing bacterial complications in infectious-inflammatory diseases caused by herpes simplex virus and cytomegalovirus in children.

2 cl, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a solid pharmaceutical product for oral administration which contains a photosensitiser representing a compound of general formula I:

wherein R1 represents a substituted or unsubstituted unbranched, branched or cyclic alkyl group, and each R2 independently represents a hydrogen atom or optionally a substituted alkyl group or its pharmaceutically acceptable salt, and at least one pharmaceutically acceptable carrier or excipient. The above pharmaceutical product is presented in the form of a tablet, a pill or a capsule having an enteric and gastroresistant coating, or in the form of the tablet or the capsule containing a number of balls, drops, granules or mini-pills with an enteric and gastroresistant coating. The above coating disintegrates in the lower gastrointestinal tract. The invention also refers to using the above photosensitiser in preparing the solid pharmaceutical product applicable in photodynamic treatment or diagnostics of a cancer condition in the lower gastrointestinal tract. What is also described is a photodynamic method of treating or diagnosing the cancer condition in the lower gastrointestinal tract by administering the solid pharmaceutical product containing the photosensitiser.

EFFECT: invention provides photosensitiser delivery to the lower gastrointestinal tract, and homogenous distribution of the photosensitiser in the target region, thereby improving the response to photodynamic treatment or diagnostics.

20 cl, 2 dwg, 2 tbl, 54 ex

FIELD: veterinary medicine.

SUBSTANCE: suppositories comprise active substance triphenyl-(3,5-di-tret-butyl-4-hydroxybenzyl) phosphonium bromide in an amount of 1%. As the pharmaceutically acceptable carriers the suppositories comprise "polyethylene glycol-6000" (30%), higher fatty alcohols C16-C21 (0.6%), calcium stearate (0.8%) and sucrose (42.8%), foaming agents contain citric acid (10%), sodium bicarbonate (14.8%).

EFFECT: agent has high bactericidal, antimycotic, antioxidant activity, provides high curative and preventive effect for treatment and prevention of puerperal purulent-catarrhal endometritis in farm animals.

2 cl, 3 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to an agent for preventing chronic fatigue syndrome in males. The agent for preventing chronic fatigue syndrome in males is presented in the form of suppositories containing male red deer's blood plasma, dry sweetvetch extract, L-arginine and additives in certain proportions.

EFFECT: agent is effective to prevent chronic fatigue syndrome in males; it corrects the psychoemotional status, and also promotes the activation of testosterone synthesis.

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are presented: using nalbuphine salt in the form of a hydrophilic emulsion suppository for treating moderate to severe pain syndrome, a pharmaceutical composition for the same application in the form of suppositories comprising nalbuphine hydrochloride as an active substance and a hydrophilic emulsion base in the following ratio, g/100 g of the composition: nalbuphine hydrochloride 0.0125-5.00, hydrophilic emulsion base up to 100 g, and a method for preparing the same.

EFFECT: effective and prolonged analgesic action with no laxative action has been shown.

7 cl, 3 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: declared products are presented in the form of suppositories and contain a mechanically active amorphous or amorphocrystalline calcium gluconate as an active substance and additives as a base. One of the declared agents contains hard fat, paraffin, cacao butter and Lutrol F68 as a base in specific proportions. The other agent contains Witepsol W35, Witepsol H15, kollidon CL and Cremophore RH-40 as a base in specific proportions.

EFFECT: invention provides the agents with uniformly released active substances, prolonged action and applicability for unassisted use by the patients; the declared agents provide a wide spectrum of therapeutic activity, particularly the regulation of Ca2+ and phosphate exchange, reduced resorption and higher bone tissue density, Ca2+ replacement, improved Ca2+ intestinal absorption, phosphate renal re-absorption, bone mineralisation, improved blood coagulation, maintained stable cardiac function, and enabled neurotransmission.

2 cl, 5 ex

FIELD: biotechnologies.

SUBSTANCE: conjugate represents benzoate-hydrocodone that has the following structure: benzoate-hydrocodone (Bz-HC). Invention also pertains to the application of pharmaceutical compound for obtaining the drug for curing the patient with illness, disease or condition mediated by opioid binding to the opioid receptors of the patient.

EFFECT: improvement of medical treatment efficiency or prevention of drug abuse, drug withdrawal symptoms or pain relief.

10 cl, 11 ex, 4 tbl, 20 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to combined antipyretic drug in form of rectal suppositories. Drug contains paracetamol, dimedrol and papaverine hydrochloride as active components, and lipophilic suppository base Suppocire (Suppocire NA-15) as auxiliary substance, with the following component ratio in g per 1 suppository with 2.0 g weight: paracetamol 0.3-0.5; dimedrol 0.03-0.05; papaverine hydrochloride 0.03-0.05; Suppocire (Suppocire NA-15) - the remaining part (to 2.0 g).

EFFECT: increased efficiency of paracetamol suppositories as antipyretic drugs, with absence of narcotic and psychostimulating substances in their composition.

4 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine, particularly to pharmacology in cardiology, particularly to a herbal tea for treating adolescents with labile arterial hypertension. The herbal tea for treating the adolescents suffering stable arterial hypertension containing dried grinded herbal raw material: quinquelobate motherwort herb, origanum herb, Baikal skullcap roots, thin-leaved milkwort roots taken in certain proportions.

EFFECT: herbal tea is effective in treating the adolescents with labile arterial hypertension.

2 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmacology in cardiology, particularly to a herbal tea for treating the adolescents suffering stable arterial hypertension. The herbal tea for treating the adolescents suffering stable arterial hypertension containing dried grinded herbal raw material: creeping thyme herb, Baical woundwort herb, rose hips, Siberian patrinia roots in certain proportions.

EFFECT: herbal tea is effective for treating the adolescents suffering stable arterial hypertension.

2 cl

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

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