Spontaneous erythricite aggregation reduction method in patients with arterial hypertension and dislipidemy

FIELD: medicine.

SUBSTANCE: invention belongs to medicine, notably to haematology and cardiology and refers to reduction of spontaneous erythrocytes aggregation in patients with arterial hypertension and dislipidemy. To achieve this, combination of hypolipidemic diet with dosed different physical exercises, daily swimming during at lest 40 minutes in the middle of the day is used. Additionally is administered 10 mg of lisinopril in the morning once daily and simvastatin 20 mg after supper once daily. Course of treatment is 2 months.

EFFECT: method ensures correction of spontaneous erythrocyte aggregation in this group of patents and results risk decrement of such thrombotic complications as myocardial infarction, insult and thromboses of different localisation.

1 tbl, 2 ex

 

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

Analogues of the proposed method of reducing the spontaneous aggregation of erythrocytes (SAE) in patients with arterial hypertension (AH) with dyslipidemia (D) does not exist.

For the correction of arterial hypertension is often prescribed ACE inhibitors, including lisinopril for the treatment of D are used lipid-lowering diet and statins, including simvastatin, in the correction pattern of patients with arterial hypertension with D often includes physical exercise and swimming.

In preparing this proposal was tasked to develop an effective and affordable way to reduce aggregation of erythrocytes in patients with D, which would solve the problem of correction of AH D with simultaneous normalization of SAE and thereby prevention in a wide range of patients with hypertension with D. development of myocardial infarction, cerebral stroke and thrombosis of different localization.

When ever medical complex consisting of lipid-lowering diet, individually tailored physical training, swimming and drugs lisinopril and simvastatin, were not used in patients with AH D to normalize SAE.

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

The essence of the proposed method lies in the fact that for the correction SAE patients who G D long-term is assigned a complex of lipid-lowering diet, dosed physical exercise, daily swimming at least 40 minutes a day in the middle of the day and drugs lisinopril at a dose of 10 mg 1 time a day, morning and simvastatin 20 mg 1 time in the evening after a meal.

The method allows to correct SAE in patients with AH D for 2 months, 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 arterial hypertension with D 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. // The Bulletin of the Ivanovo medical Academy. - 2008. - V.13, who is 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 of the subject. 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) redni the unit size (CPA):

CPA=sea/KA

Sea - the sum of all cells in the units;

KA is the number of units;

2) the Index of aggregation (PA):

PA=(CPA·KA+CTU)/(KA+CTU)

CTU - free erythrocytes;

3) the Percentage of non-aggregated RBCs (PNA):

PNA=CSE·100/(CPA·KA+CSP).

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% indicates increase in SAE. In case of violation of at least one of these three indicators of sick AG with D must be treated according to the inventive method.

The inventive method is carried out as follows.

To reduce the level of lipids in blood of patients assigned patients lipid-lowering diet, the basic principles of which are set out in the table below.

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 institutions which m is exempt from state of inhibition of 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 through the 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, sick AG to Dr. recommended treatment and preventive exercises. Depending on the initial fitness may apply at the beginning of the lightweight option, physical activity, and subsequently reinforced Varian is A.

2. Complexes of preventive and curative gymnastics for persons suffering from hypertension with D.

2.1. The lightweight version of preventive and curative gymnastics.

Exercise 1. Standing. A quiet walk with a gradual acceleration and deceleration of 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 note - 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 - the DOH. 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, medium 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.

pragnienie 13. Standing, feet together, hands pubescent. 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, return to the starting position and inhale. 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 you is if you plan 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. A peaceful walk with the breath of the 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 up - 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 pubescent. Circular motion direct hand in the shoulder joints, 6-10 times with a maximum excursion, breathing is not zaderjyvat is.

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. Standing 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. The quiet walk with the transition to the 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 of paperman is. 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 the movement of the hand - 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 Tali is. 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 sick AG with D. you 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 course is BA quiet - 1 minutes

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 at least 40 minutes a day in the middle of the day.

The fourth component of way of leveling advanced SAE in patients with AH D is the appointment of lisinopril at a dose of 10 mg 1 time a day, morning and simvastatin 20 mg 1 time in the evening after a meal.

Example 1. Patient R., 41, suffering AG with D for 5 years, were examined during the follow up inspection regarding arterial hypertension. The patient was taken to the blood in a plastic tube with subsequent study of the aggregation activity of erythrocytes (CPA=5,7, PA=1,60, PNA=68,9%), indicating that the increase of the AOC.

The patient was recommended lipid-lowering diet, dosed physical load, swimming in the pool at least 40 min in d is Ni in the middle of the day, reception of lisinopril 10 mg in the morning and simvastatin 20 mg 1 time in the evening after a meal.

After 1.5 months. it is established that the patient SAE (CPA=4,4, PA=1,12, PNA=89,2%) is normalized.

Example 2. Patient I., 52 years old, suffering from hypertension with D. for 9 years, were examined during the follow up inspection regarding arterial hypertension. The patient was taken to the blood in a plastic tube with subsequent study of the aggregation activity of erythrocytes (CPA=6,2, PA=1,96, the PNA=40,2%), indicating a sharp increase in the SAE and the risk of thrombosis.

The patient was recommended lipid-lowering diet, measured static and dynamic exercise, daily swimming at least 40 minutes a day in the middle of the day, lisinopril 10 mg in the morning and simvastatin 20 mg 1 time in the evening after a meal.

After 2 months. treatment indicators aggregation of erythrocytes (CPA=4,5, PA=1,19, PNA=87,1%) normalized, indicating a normalization of the AOC of the patient.

The use of the proposed correction method SAE in Hematology and cardiology will help to avoid many of vascular complications in patients with Dr, they reduce the 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 arterial hypertension with dyslipidemia, including the use of hypol epidemically diet dosed static and dynamic physical loads, daily swimming at least 40 minutes a day in the middle of the day, the reception of lisinopril at a dose of 10 mg 1 time a day, morning and simvastatin 20 mg 1 time in the evening after meals for 2 months.



 

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55 cl, 6 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula: I, where R1 is selected from group, consisting of ethyl, 2-fluorethyl and isopropyl; R2 is selected from group, consisting of hydrogen, C1-7-alkyl, hydroxy, C1-7-alkoxy, C3-7-cycloalkyl, halogen, -C(O)OR6, where R6 represents C1-7-alkyl, amino, phenyl, phenyl, substituted with 1-3 substituents, selected from group, consisting of halogen, halogen-C1-7-alkyl and halogen-C1-7-alkoxy, pyridyl, imidazolyl, triazolyl and pyrrolyl; R3 is selected from group, consisting of hydrogen, C1-7-alkoxy, amino, -O-benzyl and -o-tetrahydropyranyl; or R2 and R3 are bound to each other with formation of cycle together with carbon atoms to which they are bound, and R2 and R3 together represent -CH=CH-NH-; R4 is selected from group, consisting of hydrogen, halogen, pyridyl and pyrimidyl; R5 and R5' independently on each other are selected from hydrogen or methyl; A is selected from group, consisting of isphenyl; phenyl, substituted with 1-3 substituents, selected from group, consisting of C1-7-alkyl, C3-7-cycloalkyl, C1-7-alkylsulfonyl, -O-C1-7-alkylsulfonyl, hydroxy, C1-7-alkoxy, hydroxy-C1-7-alkyl, hydroxy-C2-7-alkoxy, dihydroxy-C3-7-alkoxy, C1-7-alkylamino, di-C1-7-alkylamino, amino-C2-7-alkoxy, amino-C1-7-alkyl, -C(O)NR10R11, -O-C1-7-alkylene-C(O)NR10R11, -C(O)OR10, -C1-7-alkylene-C(O)OR10, -O-C1-7-alkylene-C(O)OR10, halogen, halogen-C1-7-alkoxy, cyano- C1-7-alkoxy, fluorphenyl, pyridyl, tetrazolyl and tetrazolyl- C1-7-alkoxy; 1,3-benzodioxolyl; naphtyl; pyrimidinyl; pyridyl, substituted with one or two substituents, selected from group, consisting of C1-7-alkyl, C1-7-alkoxy, amino, C1-7-alkylamino, di-C1-7-alkylamino, C3-7-cycloalkylamino, halogen, cyano, morpholinyl, imidazolyl and -NH-C(O)-R9, where R9 represents C1-7-alkyl or C3-7-cycloalkyl, and indolyl; R10 and R11 independently on each other represent hydrogen or C1-7-alkyl; and to their pharmaceutically accdeptable salts. Invention also relates to pharmaceutical compositions.

EFFECT: obtaining novel biologically active compounds, which are antagonists of somatostatin receptor subtype 5 (SSTR5).

26 cl, 266 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described novel compounds of formula (I), where R1 represents hydroxymethyl; R2 is selected from -C(O)NR4R5; HET-1 represents 5- or 6-member heteroaryl ring, bound by atom C; R3 represents halogeno; R4 and R5 together with nitrogen atom, to which they are bound, can form heterocyclyl ring system, as it is defined for HET-3; HET-3 represents possibly substituted azetidinyl; m equals 1; n equals 0, 1 or 2; or their pharmaceutically acceptable salt, which can be applied as glucokinase (GLK) activators or active ingredient of pharmaceutical compositions, also described are methods of obtaining them.

EFFECT: creation of novel compounds applied as glucokinase (GLK) activators in treatment of diabetes.

13 cl, 40 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: method of obtaining dry diketopiperaxine powder includes obtaining diketopiperazine solution, stage of diketopiperazine-containing particles formation and removal of solvent by drying by means of dispersion. Method can include additional stage of loading diketopiperazine particles with active agent, which represents peptide or protein, preferably, insulin. Diketopiperazine preferably is fumaryldiketopiperazine. Diketopiperazine particles, obtained by invention method, possess improved aerodynamic characteristics, active agent, in particular insulin, is more stable and is delivered in more efficient way in comparison with composition of diketopiperazine-insulin, dried by means of sublimation.

EFFECT: dry powders are used as compositions of pharmaceutical preparations for delivery in pulmonary way.

16 cl, 10 dwg, 5 tbl, 8 ex

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine and deals with stimulator of pancreatic beta-cell regeneration and insulin production in pancreatic beta-cells. Essence of invention includes pharmaceutical composition for stimulation of neogenesis or regeneration of pancreatic beta-cells, producing and secreting insulin, and for stimulation of insulin production in beta-cells, where said composition contains ghrelin or its derivative as an effective component.

EFFECT: advantage of invention lies in elaboration of method for stimulation of neogenesis or regeneration of pancreatic beta-cells.

18 cl, 5 ex, 6 tbl, 10 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to pyrrole derivatives of formula (I): , where R1 denotes hydrogen; R2 denotes adamantine which is unsubstituted or substituted with a hydroxy group or halogen; R3 denotes trifluoromethyl, pyrazole, triazole, piperidine, pyrrolidine, hydroxymethylpiperidine, benzylpiperazine, hydroxypyrrolidine, tert-butylpyrrolidine, hydroxyethylpiperazine, hydroxypiperidine or thiomorpholyl group; R4 denotes cyclopropyl, tert-butyl, -CH(CH3)2CH2OH, methyl, -CF3 or -(CH2)nCF3 group, where n equals 1 or 2; R5 denotes hydrogen or lower alkyl which is unsubstituted or substituted with a halogen, as well as pharmaceutically acceptable salts thereof.

EFFECT: compounds and pharmaceutical compositions containing said compounds can inhibit 11β-hydroxysteroid dehydrogenase of the form 1 (11-BETA-HSD-1) and can be used to treat diseases such as type II sugar diabetes type and metabolic syndrome.

17 cl, 99 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmacy. An aqueous-alcoholic tincture exhibiting hypolipidemic and hypotensive activity is prepared by infusion and filtration. The raw materials are mistletoe shoot, leaves, berries collected in autumn in the ratio 1:1:1 extracted in 60% alcohol in the ratio of raw materials to extractant 1:2 for 4 days followed by triple heating to 60°C and cooling, filtration to prepare the first fraction, the oil cake is soaked once again in 90% alcohol in the ratio 1:2, infused for 10 days to produce the second fraction, then the dried mistletoe leaves collected in January are placed in distilled water in the ratio of raw materials to extractant 1:10 with 10% ascorbic acid added, kept for 24 o'clock, filtered to produce aqueous tincture, the fractions are mixed together and added with aqueous mistletoe tincture to alcohol concentration 60%.

EFFECT: invention allows improving hypolipidemic and hypotensive activity of the product.

1 ex

FIELD: chemistry.

SUBSTANCE: use of compounds of formula (I): where: X denotes >CR1R2 or, when R6 denotes H, X denotes >SO2; Y denotes >CR1R2; Z denotes >C=O, >CH2, single bond; R1 denotes H, R2 denotes H, -COOH, -OH; or R1 and R2 together denote =O, ethylenedioxy or hydroxyimino group; R3 denotes H, lower alkyl group; R4 denotes two H, =O, hydroxyimino group; R5 denotes H, lower alkyl group, halogen; R6 denotes H, lower alkoxy, COOH; R7 and R8 are identical or different from each other and each denotes H, lower alkyl, halogen; and pharmaceutically acceptable salts thereof and esters for preparing a medicinal agent.

EFFECT: agent having neuroprotective action against hypoxia.

2 tbl, 24 ex, 13 cl

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