Method for decrease of spontaneous rbc aggregation in patients with abdominal obesity

FIELD: medicine.

SUBSTANCE: invention is referred to the area of medicine, namely to hematology, endocrinology and cardiology and can be used for decease of spontaneous RBC aggregation in patients with abdominal obesity. To do that the metformin infusion are performed with the background of hypocaloric diet and dosed static and dynamic physical exercises. Physical exercises include morning hygiene gymnastics, therapeutic gymnastics, single physical exercises during the day, daily swimming for no less than 30 minutes a day in the middle of the day. Metformin is given in the dose 500 mg twice a day. The treatment shall be performed for 1 month.

EFFECT: method provides for normalization of spontaneous RBC aggregation within 1 month, bringing it down on the level close to that in healthy people and thus decreasing the risk of thrombotic complications in patients with abdominal obesity.

2 ex, 1 dwg

 

The invention relates to medicine, namely to Hematology, endocrinology and cardiology.

Analogues of the proposed method of reducing the spontaneous aggregation of erythrocytes (SAE) in patients with abdominal obesity (AO) does not exist.

In the correction pattern of patients JSC often includes a low-calorie diet, physical exercise, swimming and Metformin.

In preparing this proposal was tasked to develop an effective and affordable way to reduce aggregation of erythrocytes in patients with AO, which would solve the problem of AO correction with simultaneous normalization of SAE and thus prevention of the wider group of patients JSC development of myocardial infarction, cerebral stroke and thrombosis of different localization.

However, never before medical complex, consisting of a low-calorie diet, individually tailored physical training, swimming and drug Metformin has been used in patients with AO to normalize SAE.

The aim of the invention is to increase the efficiency of correction of violations SAE in patients with AO.

The essence of the proposed method lies in the fact that for the correction SAE ill AO long is assigned a complex of low-calorie diet, exercise workouts, daily swimming for at least 30 min a day in the middle of the day and the drug Metformin 500 mg 2 times the day.

The method allows to correct SAE patients JSC within 1 month, translating it to a level close to that of healthy people. Subject to the subsequent recommendations of the proposed method can be maintained SAE, and therefore, the rheology of blood in an optimal state, which will significantly reduce the risk of thrombotic complications, reduce the number of cases of temporary disability, to accelerate and improve the quality of patient treatment, reduce disability, and also to prolong the life and reduce mortality of patients with AO from a heart attack, stroke and thrombosis of different localization.

The inventive method is carried out as follows.

Taking 9 ml of blood is produced in the morning after a 14-hour fast from Vienna through the thick needle by gravity into a test tube with sodium citrate in the ratio of 9:1 to assess the aggregation of erythrocytes.

Erythrocyte aggregation is assessed by the degree of ability of erythrocytes to spontaneously aggregate (Pokrova O.A., Grineva MR, Ivanov K.S. Methodology and clinical significance of the study the rheological properties of blood // Bulletin of the Ivanovo medical Academy. - 2008. - T13, No. 1-2. - s.89-98).

To assess the aggregation of erythrocytes blood from a vein taken in sodium citrate in the ratio of 9:1 and centrifuged 10 min at 3000 rpm/min In 96-well pad fill 2 holes 0.2 ml plasma discuss ebimage. From the tube removed all the plasma and the layer of leukocytes. Erythrocytes resuspended standard phosphate buffer in the ratio 1:4, followed by centrifugation for 10 min at 3000 rpm, allowing you to wash them from the remnants of the plasma when removing the supernatant. After this is taken as 0.02 ml of erythrocytes and resuspended first filled with autologous plasma-well 96-well Ouija boards, allowing you to get 10% hematocrit. Then from this hole, take a clean, dry pipette 0,02 ml content and placed in the second filled the hole that allows you to get 1% hematocrit. After that 1 grid in the camera Goryaeva fill obtained a suspension of red blood cells, incubated 3 min for the occurrence of spontaneous aggregation and shall count free erythrocytes (including 2 of the erythrocyte together) and units, starting with 3 cells, connected in the form of "monetary columns") in 2 large squares of the camera (lens×40, eyepiece×10). Considered the number of "coin of columns and the number of red blood cells, involved in them.

Based on these results, calculate the following indicators that assess SAE:

1. The average unit size (CPA):

CPA=sea/KA

Sea - the sum of all cells in the units;

KA - the number of units.

2. The index of aggregation (PA):

PA=(PA·KA+CTU)/(KA+CTU)

CSE - number free the x erythrocytes.

3. The percentage of aggregated erythrocytes (PNA):

PNA=CSE·100/(PA·KA+CTU)

Normative values for CPA are 4-5, PA 1,05-1,30, for the PNA 80,0-92,0%. The increase in CPA above 5, and PA above 1.30 and lowering the PNA below 80,0% talks about increasing the SAE. In case of violation of at least one of these three indicators patients JSC must be treated according to the claimed method.

To create a negative energy balance in the body, patients are advised individually selected low-calorie diet.

Calorie daily diet individually for each patient is calculated in kcal by the formula:

for women 18-30 years (0,0621×body weight (kg)+2,0357)×240,

31-60 years (0,0342×body weight (kg)+3,5377)×240,

over 60 years of age (0,0377×body weight (kg)+2,7545)×240,

for men 18-30 years (0,0630×body weight (kg)+2,8957)×240,

31-60 years (0,0484×body weight (kg)+3,6534)×240,

over 60 years of age (0,0491×body weight (kg)+2,4587)×240.

The resulting coefficient remains unchanged with minimal physical activity, multiplied by 1.3 in moderate and 1.5 - high physical activity (usually in patients with JSC physical activity level low).

It is recommended that 3 main meals and 2 intermediate. With regular skipping one meal significantly increases the incidence of obesity, have also put the other correlation between obesity and skipping Breakfast. It is recommended that the following distribution of daily calories: Breakfast - 25%, 2nd Breakfast - 10%, lunch - 35%, tea - 10%, dinner - 20%.

To compile menu the patient uses a special table with the instructions of the chemical composition and caloric content of products, given that the main sources of energy: protein (1 g contains 4 kcal), fat (9 kcal), carbohydrates (4 kcal) and alcohol (7 kcal).

The second component of the proposed method is feasible regular physical exercise.

In real life you can implement the three forms of physical activity: 1) morning hygienic gymnastics (charging); 2) health care gymnastics; 3) fractional exercise during the day.

1. Morning hygienic gymnastics (charging).

Morning gymnastics should do after waking up to Breakfast in a ventilated room. Under the influence of training the body is released from the state of inhibition of the physiological processes taking place during sleep.

The sequence of the exercises involves the alternation of load on different muscle groups (arms, legs, body). Exercises are performed with gradually increasing excursion breathing, stretching, limited use of power conditions. Breathing exercise should be free, rhythmic, without delay, mainly che is ez nose; the exhalation should be longer than the inhale (breath in 2-3 sec, exhale 3-5).

In good health the load, you can increase the number of repetitions faster, increase range of motion and shorter pauses between exercises.

When fatigue should reduce the load, increase the duration of pauses between exercises, to fill their quiet breathing.

After gymnastics, you must go to the rubbing or take a shower.

Morning exercises should evoke a sense of vitality, increase activity, improve well-being and health.

If you feel unwell, develop shortness of breath or pain in the heart and behind the sternum should be temporarily suspend classes and consult a doctor.

During the day, patients JSC recommended treatment and preventive exercises. Depending on the initial fitness may apply at the beginning of the lightweight option, physical activity, and subsequently enhanced option.

2. Complexes of preventive and curative gymnastics for people with AO.

2.1. The lightweight version of preventive and curative gymnastics.

Exercise 1. Standing. A quiet walk with a gradual acceleration and deceleration 1-2 minutes on the exercise of the gradual deepening of the breath.

Exercise 2. Circular motion in the shoulder joints. When breeding - breath, when the information is NII - exhale with a slight tilt of the torso and retraction of the abdominal wall 6-8 times. The fingers touch the shoulders, elbows close to the torso.

Exercise 3. Standing, hands on his belt. Alternately shifting the weight of the body from one foot to the other with a small bending the legs at the knee joint without lifting the feet from the floor. Exercise done 10-16 times with the muscles of the legs.

Exercise 4. Standing, feet apart at shoulder width, hands on his belt. Bending the trunk forward, touch right hand to left toe. 4-6 times alternately. When straightened position - breath, when the tilt - exhale. To look ahead.

Exercise 5. Standing with arms along the body. At the same time to take straight arm and one leg to the side with alternating lead leg. 4-6 times in each direction in turn. A wave of the hands and feet, breathe freely, do not delay.

Exercise 6. Standing, feet apart, hands in front of chest with palms down. With a turn of the body to dissolve hand in hand with turning the palms up - breath. To return to the original position with a small tilting forward, exhale. 3-5 times in each direction in turn. Breathing to harmonize with the movement of hands and body. By the end of exhalation to engage the wall of the abdomen.

Exercise 7. Standing, hands free. The walk free - 1 min, then with high flexion of the hips - 10-20 movements with subsequent transition to a peaceful walk 1-2 minutes Breathing rhythmic, the Central depth.

Exercise 8. Sitting on the edge of the chair, hands on the waist. The bowing of the back and bending forward of the body. Repeat 6-10 times. Breathing is not to delay.

Exercise 9. Sitting on the edge of the chair, the emphasis tassels on the edge of a chair, and your feet slightly in front of the chair. Squats with a focus hands on the edge of a chair - 4-6 times. When you squat exhale.

Exercise 10. Standing sideways to the back of the chair to hold it with one hand. Swing free straight arm with leg pulling back. To return to the original position. Repeat 4-6 times for each leg and arm. Breathing is not to delay.

Exercise 11. Standing, legs apart widely, hands on waist. Turns the body right and left - 6-10 times alternately. The head does not turn, to look forward.

Exercise 12. Standing, feet together, hands down. Move the hands to the sides, inhale, bend the leg at the knee and pressed his hands to his stomach exhale. 3-5 times each leg alternately. Strive to maintain balance; on the exhale, draw your abdomen.

Exercise 13. Standing, feet together, hands down. The side slopes of the case with flexion of the opposite hand ("pump"). Breathing is not to delay, to strive for greater excursion of movement.

Exercise 14. Standing. A quiet walk with a uniform average depth of breathing. 1-2 minutes

Exercise 15. Lying on the Mat to put under your head with a pillow. Go to a half-sitting position and bent to hug the hips exhale, rotisa to its original position - the breath. Breath hold. Strive in a semi-sitting position to maintain balance. Run 4-6 times.

Exercise 16. Lying down, arms at sides, legs apart. A semi-circular motion right straight leg to the left with the rotation of the pelvis - exhale - return to the starting position and inhale. 3-5 times in each direction. Alternately left and right, with the greatest possible excursion movement of the leg, keeping the emphasis brushes the floor.

Exercise 17. Sitting on the floor; a) to stand on all fours; b) to move into position on his knees; hands up - breath, torso, and hands to take back - exhale. When the tilt pull the stomach. Repeat 4-6 times; d) to go into a standing position, and then in the supine position; (e) self-massage of the abdomen small polukrugom movements clockwise - 1-2 minutes Rest 2 min; W) quiet breathing; C) exercise the protrusion (calm) and retraction (active) abdominal wall. The retraction of the abdomen combined with exhale through the mouth. Repeat 4-6 times.

Exercise 18. Standing with arms bent. Energetic walking on the spot or area of high flexion of the hips and waving of hands - 20-30 steps. Breathing is not to delay.

Exercise 19. Sitting on a chair, legs apart, hands on the waist or rest against the edge of a chair. The circular motion of the pelvis with the retraction of the abdomen when moving the pelvis back. 4-6 times in each direction.

Exercise 20. Standing. Calm is odba breathing an average depth of 2-3 minutes

When the source sufficient trained or arising in the course of the practice of tolerance to physical loads, you can use the following set of exercises.

2.2. Enhanced preventive and curative gymnastics.

Exercise 1. Standing. The quiet walk with rubbing the palms of the thorax, abdomen, lower back. Runs 1-2 minutes

Exercise 2. Standing, hands down. Simultaneous bending with tension and free "throwing" hand forward, sideways and upwards of 12-16 times. When you bend exhale, when the alignment of breath.

Exercise 3. Standing, hands on waist, legs shoulder-width apart. Lateral motion of the pelvis to the right and left, back and forth. Is 6-10 times alternately. Breathe freely.

Exercise 4. Standing, feet shoulder-width apart, hands down. Circular motion direct hand in the shoulder joints, 6-10 times with a maximum excursion, breathing, do not delay.

Exercise 5. Standing, hands in front of chest, bent at the elbows. Walking with high flexion of the hips, with a touch of the hand. 6 to 10 times for each leg alternately. Motion of energetic, hip flexion - exhale through the mouth.

Exercise 6. The quiet walk 1-2 minutes

Exercise 7. Sitting on the edge of the chair, hands on the waist. Bending and bowing of the body. The exercise is performed 8-10 times. The energetic movement. When straightening - breath, bending exhale.

Exercise 8. the toy sideways to the chair, to hold back, the other hand on the waist. Alternate sweeps straight leg forward, with the greatest possible tour. Swing legs to be combined with the exhalation. Runs 4-6 times.

Exercise 9. Standing, feet apart, hands at sides. Bending the body forward, touch right brush left toe of the feet, the other hand is allotted up. To return to the original position. Tilt combined with exhalation, by straightening the breath by 4-6 times.

Exercise 10. Walking the quiet breathing of medium depth. 1-2 minutes

Exercise 11. Standing, hands in a fist and lowered: (a) bending of the arms at the elbows with the power and extension of their diverting ago, with possibly large rectification and voltage and delay in the stress state within 2-3 C. Standing, hands on waist; b) proprietary with subsequent lifting in socks and tension legs. The exercise is performed 4-6 times with possibly large rectification and voltage and delay in the stress state within 2-3 C.

Exercise 12. Sitting on the edge of the chair. In the raised position and bent knee leg to make alternate shaking the hands of the calf muscles and thighs. To reduce muscle tension. 1-2 minutes

Exercise 13. Sitting on the edge of the chair, straight leg divorced. Pinch open and direct the hands and feet. When breeding breath, when the note - exhale. Is 4-8 times.

Exercise 14. Standing. Walking quiet what with moving to a rhythmic quiet running (Jogging) on the spot or moving. For fatigue to go on a peaceful walk with the breath of medium depth. 2-5 minutes

Exercise 15. Lying on the Mat. Simultaneous lifting of the body and legs on the exhale. 4-6 times. Arms and legs should be straight, to keep the balance.

Exercise 16. Lying on the Mat, the emphasis brushes the floor. Cross movement straight leg - scissors. 4-8 times. Breathing is not to delay.

Exercise 17. With a quick straightening of the legs to move into a sitting position, then to lie down. You can help stroke 4-6 times.

Exercise 18. Lying on your back, legs bent. Calm breathing 4-6 times.

Exercise 19. Lying on his back, hands diluted with emphasis brushes the floor. With the rotation of the pelvis to the left, bend the legs, rotate the pelvis with legs crossed to the right and stretch the legs. To repeat such a circular motion feet 3-6 times in each direction alternately. Hands not off the floor. Breathing is not to delay.

Exercise 20. Lying on your back, arms and legs separated. Alternate turns the body right and left laying one hand to the other. Feet are not slipping. When divorced hands - breath, turning exhale. Performed 3-6 times.

Exercise 21. Lying on your back, arms along the body: a) turn on your left side; b) to turn on the right side; C) switch to lying on his stomach; to kneel; d) to move in a standing position; (e) walking on the spot with high flexion of the hips and d is iraniam hands - 20-30 steps; g) to sit on the Mat; C) lie on your back, relaxing breath. The whole complex repeat 3-4 times.

Exercise 22. Standing. Walking the quiet breathing of the average depth of 1-2 minutes

Exercise 23. Standing, feet apart on the width of the foot, hands on waist. Circular motion of the pelvis, right and left 6-8 times. Breathing is not to delay.

Exercise 24. Standing with legs wide apart, hands in front of chest. Alternately bending the legs with the transfer to it of gravity of the body with stretching hand to toe of the bent leg. 4-6 times in each direction. The other leg is straight. When straightening - breath, when the tilt - exhale.

Exercise 25. Standing, feet apart at shoulder width, hands on waist. Circular head movements by 4-10 times in each direction.

Exercise 26. Standing, feet apart at shoulder width, hands on waist. Bend trunk to the right, pulling the left arm up - breath. Return to starting position - exhale. 4-6 times alternately.

Exercise 27. The same hands to the shoulders. Circular motion of the brushes with the maximum excursion in the shoulder joints, when breeding - breath during the mixing and retraction of the abdominal wall exhale. Breathing deep.

Exercise 28. Standing. A peaceful walk and breath the average depth. The reduction of the total load. 1-2 minutes

3. Fractional exercise during the day.

Depending on the conditions of real life ill the AO can recommend various exemplary embodiments of the fractional loads to increase physical (motor) activity during the day.

Option 1.

Exercise 1. Sitting - dilute the elbows to the sides, inhale, extend hands forward voltage exhale, 4-6 times.

Exercise 2. Sit - to stand with the deflection of the housing and land - 8-10 times.

Exercise 3. Sitting mimicking the movements of a boxer with possibly a large turn of the body is 10-12 times.

Option 2.

Exercise 1. Standing - walking with high flexion in the hip - 16-30 times.

Exercise 2. Standing - circular head movements to the right and left - 3-8 times in each direction.

Exercise 3. Standing legs apart widely imitated the movements of Costa - 10-12 times.

Exercise 4. Sitting - transition into the standing - 10-12 times.

Option 3.

Exercise 1. The quiet walk - 1 min

Exercise 2. Walking fast - 1 minute

Exercise 3. Walking with high flexion of the hips and alternate wave of the hands 20-30 times.

Exercise 4. Walking the quiet breathing of 1-2 min; quiet running on the spot or move around the room - 2-5 minutes

Option 4.

Walk the pedestrian varying length.

Option 5.

Physical work in different ways and with different duration depending on the conditions (cleaning, home services, cleaning, gardening work, and others).

The third component of the claimed method is a daily swim in the sea, the river or the pool for at least 30 minutes a day in the middle of the day.

The fourth component of way of leveling advanced SAE patients JSC is the purpose of Metformin 500 mg 2 times a day.

Example 1. Patient M 44 years, suffering the AO for 6 years, screened during a medical checkup. The patient was taken to the blood in a plastic tube with subsequent study of the aggregation activity of erythrocytes (CPA=5,4, PA=1,42, PNA=70,1%), indicating that the increase of the AOC.

The patient was recommended a low-calorie diet, measured static and dynamic exercise, daily swimming for at least 30 min a day in the middle of the day and Metformin 500 mg 2 times a day.

After 3 weeks. it is established that the patient SAE (CPA=4,6, PA=1,14, PNA=to 85.2%) is normalized.

Example 2. Patient P. 58 years old, suffering from JSC for 9 years, were examined during a medical checkup. The patient was taken to the blood in a plastic tube with subsequent study of the aggregation activity of erythrocytes (CPA=5,5, PA=1,62, PNA=64,7%), indicating that the increase of the AOC and the risk of thrombosis.

The patient was recommended a low-calorie diet, measured static and dynamic exercise, daily swimming for at least 30 min a day in the middle of the day and Metformin 500 mg 2 times a day.

After 1 month of treatment indicators aggregation of erythrocytes (CPA=4,7, PA=1,22, PNA=83,0%) normalized, indicating a normalization of SA is the patient.

The use of the proposed correction method SAE in Hematology, endocrinology and cardiology will help to avoid many of vascular complications in patients with AO, to reduce their number of cases of temporary disability, to reduce the duration of hospitalization, reduce morbidity and mortality.

The way to reduce the spontaneous aggregation of red blood cells in abdominal obesity, comprising applying a low-calorie diet, measured static and dynamic physical loads, which includes morning hygienic gymnastics, therapeutic gymnastics, fractional exercise during the day, a daily swim at least 30 minutes a day in the middle of the day, Metformin 500 mg 2 times a day for 1 month.



 

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15 cl, 4 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to indole and indazole compounds of formula in which n equals a whole number from 1 to 3, m equals 0 or 1, A denotes phenyl, X denotes C or N, R1 denotes hydrogen, alkyl, -(CH2)rNR7R8, where r equals a whole number from 1 to 5, and R7 and R8 independently denote hydrogen, alkyl or alkylcarbonyl, or can together form an optionally alkyl-substituted alkylene chain, where optionally one methylene is substituted with a N atom, R2 denotes hydrogen, halogen, cyano, nitro, hydroxy, alkyl, alkoxy or trialkylsilyl, denotes -(CH2)pCO2R7, -(CH2)pOR7, -(CH2)pNR7R8, -NHR10, -N(H)S(O)2R7, -NHC(O)R10, -(CH2)pS(O)2R7 or (CH2)p-heterocycle-R10, where p equals a whole number from 0 to 3, R7 and R8 are as defined above, R10 denotes hydrogen, oxo, alkylsulphonyl, alkylcarbonyl, alkyloxycarbonyl, alkoxy, alkyl or heterocycle, R3 denotes hydrogen, cyano, halogen, alkyl or phenyl, or denoes -(CH2)n-heterocycle or -(CH2)n-aryl, where n equals a whole number from 0 to 3, provided that R3 denotes phenyl when X denotes C and m=0, R4 denotes -YR11, where Y denotes a direct bond or -(CR7R8)pY′-, where p equals a whole number from 0 to 3, R7 and R8 are as defined above, Y′ is selected from a group consisting of -O-, -S-, -NR12-, -NR12C(O)-, -C(O)-, -C(O)O-, -C(O)NR12-, -S(O)q- and -S(O)qNR12-, where R12 denotes hydrogen, alkyl, aryl or heteroaryl, q equals a whole number from 0 to 2, R11 is selected from a group consisting of hydrogen, cyano, halogen, hydroxy, thiol, carboxy, alkyl and -(CH2)tB-R13, where t equals a whole number from 0 to 3, B denotes heterocycle, heteroaryl or aryl, R13 denotes hydrogen, cyano, halogen, hydroxy, oxo, thiol, carboxy, carboxyalkyl, alkylcarbonyloxy, alkyl, alkoxy, alkylthio, alkylcarbonyl or alkylsulphonyl, R5 denotes hydrogen, alkyl, cycloalkyl, heterocycle or heterocyclylalkyl, R6 denotes (CR7R8)p-Z-D-W-R14, where Z denotes a direct bond, or is selected from a group consisting of -C(O)-, -C(O)O, -C(O)NR12- and -S(O)y-, y equals a whole number from 1 or 2, D denotes a direct bond, or denotes cycloalkyl, heteroaryl or heterocycle, W denotes a direct bond, or denotes -NR -, -C(O)-, -C(O)O-, -C(O)NR12-, -S(O)y-, -S(O)yNR12- or -NR12S(O)y, wherein R14 denotes hydrogen, hydroxy, alkyl, alkoxy, heterocycle, heteroaryl, aryl or aralkyl, R5 and R6 together denote an alkylene chain, provided that R6 denotes cycloalkyl or heterocyclyl when X denotes N, where the heteroaryl is a 5-6-member aromatic ring containing 1-2 heteroatoms selected from N, O and S, the heterocycle is a 3-8-member ring containing 1-3 heteroatoms selected from N, O and S, where the alkyl, alkoxy, aryl, cycloalky, heterocycle and heteroaryl can be optionally substituted, and the substitutes, one or more, are selected from a group consisting of hydroxy, halogen, nitrile, amino, alkylamino, dialkylamino, carboxy, alkyl, alkoxy, carboxyalkyl, alkylcarbonyloxy, alkylthio, alkyloxycarbonyl, alkylaminocarbonyl, arylalkoxy and oxo, and pharmaceutically acceptable salts or stereoisomers thereof. The invention also relates to a composition, as well as a method of preparing said composition.

EFFECT: obtaining novel biologically active compounds for preventing or treating necrosis and necrosis-associated diseases.

40 cl, 162 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a novel C-phenyl glycitol compound which serves as a preventive or therapeutic agent for sugar diabetes by inhibiting SGLT1 activity, as well as SGLT2 activity; demonstrating inhibiting effect on glucose absorption, and also acts on release of glucose with urine. The C-phenyl glycitol compound has formula (I) given below, or pharmaceutically acceptable salt or hydrate thereof, where R1 and R2 are identical or different and denote a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group, Y is a C1-6 alkylene group, -O-(CH2)n- (n is a whole number which assumes values from 1 to 4), provided that when Z denotes -NHC(= NH)NH2 or -NHCON(RB)Rc, n not equal to 1, Z is -CONHRA, -NHC(=NH)NH2 or -NHCON(RB)Rc, or The invention also relates to a pharmaceutical composition based on compounds of formula I.

EFFECT: high efficiency of the compounds.

19 cl, 8 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula in which Q together with carbon and nitrogen atoms whereto attached forms a 9-10-member bicyclic heterocycle, and R1 and R2, R3, R4, R5 and R6 are as specified in cl.1 of the patent claim, or to its enantiomers, or a mixture of its enantiomers, or to its pharmaceutically acceptable salt. Also, an invention refers to a method for activation of glucokinase activity in mammals, by introduction of the compound described above, to a method of treating the pathological conditions associated with glucokinase activity and impaired glucose tolerance by means of introduction of the compound of formula I, to a pharmaceutical composition on the basis of the presented compounds, and also to application of the compounds of formula I for preparing the pharmaceutical composition.

EFFECT: there are produced and described new compounds which are activators of glucokinase activity and can be used as therapeutic agents for preventing and treating impaired glucose tolerance, insulin-independent diabetes and obesity.

14 cl, 4 ex

FIELD: chemistry.

SUBSTANCE: present invention is related to new quinolone derivatives of general formula (I) where R1: C3-6cycloalkyl or lower alkylene C3-6cycloalkyl, R2: -H or halogen, R3: -H, halogen, -OR0 or -O-(lower alkylene)-phenyl, R0: are the same or different from each other, and each represents -H or lower alkyl, R4: lower alkyl, halogen(lower alkyl), lower alkyleneC3-6cycloalkyl, C3-7cycloalkyl or a heterocyclic group, where cycloalkyl and the heterocyclic group specified in R4 can be respectively substituted, R5: -NO2, -CN, -L-Ra, -C(O)R0, -O-Rb, -N(R6)2, lower alkylene-N(R6)(Rc), -N(R6)C(O)-Rd, lower alkylene-N(R6)C(O)-Rd, lower alkylene-N(R0)C(O)O-(lower alkyl), -N(R0)C(O)N(R0)-Re, lower alkylene-N(R0)C(O)N(R0)-Re, -N(R0)S(O)2N(R0)C(O)-Rd, -CH=NOH, C3-6cycloalkyl, (2,4-dioxo-1,3-thiazolidin-5-yliden)methyl or (4-oxo-2-tioxo-1,3-thiazolidin-5-yliden)methyl where cycloalkyl specified in R5 can be respectively substituted, R6: H, lower alkyl, lower alkylene-CO2R0 or lower alkylene-P(O)((OPp)2, where lower alkylene specified in R6 can be substituted, L: lower alkylene or lower alkenylene which can be respectively substituted, Ra: -OR0, -O-(lower alkylene)-phenyl, -O-(lower alkylene)-CO2R0, -CO2R0, -C(O)NHOH, -C(O)N(R6)2, -C(O)N(R0)-S(O)2-(lower alkyl), -C(O)N(R0)-S(O)2-phenyl, -C(O)N(R0)-S(O)2-(heterocyclic group), -NH2OH, -OC(O)R0, -OC(O)-(halogen(lower alkyl)), -P(O)(ORp)2, phenyl or the heterocyclic group where phenyl or the heterocyclic group specified in Ra can be substituted, Rp: R0, lower alkylene-OC(O)-(lower alkyl), lower alkylene-OC(O)-C3-6cycloalkyl, lower alkylene-OC(O)O-(lower alkyl), Rb: H, lower alkylene-Rba or lower alkenylene-Rba where lower alkylene or lower alkenylene specified in Rb can be substituted, Rba: -OR0, -CO2R0, -C(O)N(R0)2, -C(O)N(R0)-S(O)2-(lower alkyl), -C(O)N(R0)-S(O)2-[phenyl, -C(NH2)-NOH, -C(NH2)=NO-C(O)-(lower alkylene)-C(O)R0, -CO2-(lower alkylene)-phenyl, -P(O)(ORp)2, -C(O)R0, -C(O)-phenyl, C3-6cycloalkyl, phenyl or the heterocyclic group where phenyl and the heterocyclic group specified in Rba can be substituted, Rc: H, lower alkylene-OR0, lower alkylene-CO2R0, lower alkylene-P(O)((OPp)2, phenyl where lower alkylene and phenyl are specified in Rd can be substituted, Rd: C1-7-alkyl, lower alkenyl, halogen(lower alkyl), lower alkylene-Rda, lower alkylenylene-Rda, C3-6cycloalkyl, phenyl, naphthyl or the heterocyclic group, where lower alkylene, cycloalkyl, phenyl, naphthyl and the heterocyclic group specified in Rd can be substituted, Rda: -CN, -OR0, -O-(lower alkylene)-CO2R0, -O-naphthyl, -CO2R0, -CO2-(lower alkylene)-N(R0)2, -P(O)(ORp)2, -N(R6)2, -C(O)N(R0)-phenyl, -C(O)N(R0)-(lower alkylene which can be used by -CO2R0)-phenyl, -N(R0)C(O)-phenyl, -N(R0)C(O)-OR0, -N(R0)C(O)-O-(lower alkylene)-phenyl, -N(R0)S(O)2-phenyl, C3-6cycloalkyl, phenyl, naphthyl or the heterocyclic group, where phenyl, naphthyl and heterocyclic group specified in Ra can be substituted, Re: lower alkylene-CO2R0, phenyl, -S(O)2-phenyl or -S(O)2-(heterocyclic group), where phenyl and the heterocyclic group specified in Re can be substituted, X: CH, A: C(R7), R7: -H, or R4 and R7 together can form lower alkylene, where the substituted groups have the substituted specified in cl.1, and provided 7-(cyclohexylamino)-1-ethyl-6-fluor-4-oxo-1,4-dohydroquinoline-3-carbonitryl is excluded. Also, the invention refers to a pharmaceutical composition based on a compound of formula (I) and application of formula (I) for preparing a thrombocyte aggregation inhibitor or a P2Y12 inhibitor.

EFFECT: there are produced new quinol-4-one derivatives showing effective biological properties.

11 cl, 83 tbl, 71 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to neuropathology, physiotherapy. Method includes carrying out general magnetic therapy at the background of basic rehabilitation treatment in two stages. For this purpose device "УМТИ-3Ф" Colibri-expert is used. At the first stage impact by "running" pulses of magnetic fields in configuration "cylinder" is performed on lower extremities. Impact is carried out in first mode, with value of magnetic induction 3.5 mT and pulse frequency 100 Hz, during 10 minutes. Procedures are carried out daily, three procedures per a course. At the second stage impact on upper part of body by "rotating" pulses of magnetic fields in configuration "prism" is performed. Impact is carried out in first mode, with value of magnetic induction 3.5 mT and pulse frequency 100 Hz, during 15 minutes. Procedures are carried out daily, 7-10 procedures per a course.

EFFECT: method extends indications for magnetic therapy and possibility of its application in early rehabilitation period.

2 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine, namely to therapy and can be used in pulmonology in selection of starting antibacterial therapy of community-acquired pneumonia (ABT CP) in patients addicted to persistent tobacco-smoking. Method includes anamnesis analysis and determination of persistent tobacco-smoking as risk factor. Additionally estimated is individual sensitivity of patient's organism to medication cefotaxime. For this purpose after introduction of cefotaxime dose to patient chromatographically determined is said medication concentration in blood serum. If concentration value is lower than 2.24 mcg/ml inhibitor-protected penicillins and other antibacterial cefotaxime-free medications are used. In tobacco-smoking patient smoking index is determined and if its value is more than 25 packets/years, in therapy inhibitor-protected penicillins and other cefotaxime-free medications are used in therapy.

EFFECT: method makes it possible to carry out adequate starting antibacterial therapy, taking into account such risk factor as tobacco-smoking, and basing on prediction of drug resistance and reduction of cefotaxime concentration in blood, which ensures increase of pneumonia treatment efficiency in said contingent of patients, reducing drug load on organism and treatment terms.

2 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: method of intensifying antiaggregant activity in an experiment involves use of a chemical compound which is a conjugate of beta-cyclodextrin with acetylsalicylic acid.

EFFECT: wider range of agents for increasing antiaggregant activity.

1 tbl

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to endocrinology and can be used for reduction of hypoglycemia acute exacerbation or severe hypoglycemia exacerbation in patients with type II diabetes after treatment with insulin. For this purpose vildagliptin or its salt is introduces to patient in combination with insulin.

EFFECT: invention ensures reduction of risk of hypoglycemia development, as well as necessity to apply several antihyperglycemic medications.

12 cl, 1 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: invention relates to veterinary science. The combination preparation Praziotrem at praziquantel 75 mg and polytrem 100 mg per 1 kg of animal's weight is once prescribed for oral use that is followed by introduction of the hepatoprotector Tykveol 100 mg/kg of weight for 5 days running.

EFFECT: method is effective in treating opisthorchiasis with no adverse action of animal's body, normalised hepatic function, accelerated regeneration of parasite damaged areas.

4 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and pharmaceutical industry. A pharmaceutical composition for outward application for treating allergic and inflammatory skin diseases contains a glucocorticosteroid specified in a group: mometasone or its derivatives, betametasone or its derivatives, beclometasone or its derivatives, dexametasone or its derivatives, flumetasone or its derivatives; as an antibacterial quinolone compound, it contains a compound specified in a group: ofloxacin, lomefloxacin, norfloxacin, pefloxacin, ciprofloxacin, levofloxacin, sparfloxacin, moxifloxacin; as an antifungal azol compound, it contains a compound specified in a group: clotrimazole, ketoconazole, myconazole, fluconazole, itraconazole, voriconazole and additionally contains a synthetic polymeric high-molecular compound, particularly polyvinyl pyrrolidone, or polymers or copolymers of acrylic and metacrylic acid, or polyvinyl alcohol, or siloxane or silane polymers in certain proportions.

EFFECT: invention provides higher effectiveness in inflammatory and allergic skin diseases with no side reactions and systemic exposure.

2 tbl, 80 ex, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a drug coating composition for colonic delivery which contains water and water dispersed starch containing at least 40% of amylose, as well as a film-forming agent that is a water-insoluble polymer which controls pregelatinisation of starch under the specified aqueous medium. The invention also refers to a dosage form for colonic delivery which contains an active agent and said coating. There is also disclosed a method for preparing the coating composition involving mixing the ingredients, as well as a method of treating or a diagnostic technique for colonic diseases and pathological conditions.

EFFECT: invention provides easy and fast preparation of the composition with the colonic release active substance.

25 cl, 2 ex, 12 dwg

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to oncology, and can be used for treatment of patients with non0resectable signet ring cell adenocarcinoma. For this purpose laparotomy is performed. Into left gastric artery installed and fixed is catheter, through which 50-70 ml of ozonised physiological solution are introduced. After 30 minutes, 1000 mg of 5-fluoracyl and 50 mg leukovorin are introduced in the same way. After that, catheter is connected with port, installed in recess, specially created in subcutaneous adipose cellular tissue and brought under skin of anterior abdominal wall, wound is sewn layer-by layer. 7 days after operation into port, installed in anterior abdominal wall, connected with catheter, 50-70 ml of ozonised physiological solution are introduced. After 30 minutes, 1000 mg of 5-fluoracyl and 50 mg leukovorin are introduced in the same way. Procedure is repeated 5 more times with 1 week interval.

EFFECT: method ensures increase of anti-tumour activity of chemical preparations at the background of non-specific stimulation of patients' immunity, achieved by introduction of ozonised physiological solution.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, particularly immunology, namely immunocorrection drugs, and can be used as an inducer of a granulocyte-macrophage colony-forming factor in cells of a mononuclear phagocyte system in vitro and for efferent therapy in pathological conditions accompanied by decrease in cell-mediated immunity. The drug represents oxidised dextrane of average molecular weight 35 - 65 kDa. The drug can be presented in the form of a solution or a nanoliposomal emulsion of the concentration of oxidised dextrane 1-5 wt %. The drug is applied by introduction in a cell culture of the mononuclear phagocyte system in an amount containing oxidised dextrane 125-250 mcg per culture medium 1 ml.

EFFECT: drug under the invention exhibits high biocompatibility.

8 cl, 1 tbl, 4 ex

FIELD: medicine.

SUBSTANCE: invention is referred to the area of exercise therapy, rehabilitation after endovascular laser coagulation of lower extremities veins. Dynamic exercises are performed in the water. Lying on the back with cervical spine section pressed against swimming-pool nosing - alternating leg spread; its crossed joining and laterals; leg swings with pelvis turns to the left and to the right; knee flexion with leg spread, straightening, joining, knee flexion and spread; pulling of flexed legs to abdomen and its straightening; turn of knees, flexed legs, to the left and to the right; “bicycle” exercise; swings of straight leg forward. Standing sideways to the swimming-pool nosing, holding the nosing with the hand bent at the elbow - back swings with respective straight leg; swings with the other leg forward and 30° to the side; lateral raise of opposite flexed leg and its adduction. Lying on the chest, hanging on bent hands - flexion and spread of each leg in turn; half hanging on hands - flexion of legs in turns, flexing and spreading hands; pushing the legs off the hosing, straightening them back into lying position, then pressing the feet against the hosing; up-down swings with straight legs in turn.

EFFECT: method provides for restoring the functions of lower extremities, improvement of patient functional state, decrease of pathologic manifestations.

1 dwg, 3 ex, 1 tbl, 10 dwg

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