Spontaneous erythrocite aggregation reduction method in patients with arterial hypertension

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. This is ensured by the integrated treatment including graduated static and dynamic physical loads, including daily swimming for at least 20 minutes in the middle of the day, daily, and administration of lisinopril 10 mg once a day in the morning and amlodipine 10 mg once a day in the morning.

EFFECT: combined drug-free and drug therapies during empirically fitted period ensure effective reduction of spontaneous aggregation of erythrocytes, which, in turn, allows to improve blood's rheological properties and reduce risk of thrombotic complications in patients with arterial hypertension.

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) does not exist.

For the correction of arterial hypertension is often prescribed ACE inhibitors, including lisinopril and calcium antagonists, including amlodipine, in the correction pattern of patients with hypertension 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 hypertension, which would solve the problem of correction of arterial hypertension with a simultaneous normalization of SAE and thereby prevention in a wide range of patients with hypertension in the development of myocardial infarction, cerebral stroke and thrombosis of different localization.

When ever medical complex, consisting of individually selected physical training, swimming and drugs lisinopril and amlodipine has been used in patients with arterial hypertension to normalize SAE.

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

The essence of the proposed method lies in the fact that for the correction SAE patients with AH long is assigned a complex of dosed physically the training, daily swim at least 20 minutes a day in the middle of the day and drugs lisinopril at a dose of 10 mg 1 time a day, morning and amlodipine 10 mg 1 time in the morning.

The method allows to correct SAE in patients with hypertension within 1.5 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 hypertension 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. - V.13, №1-2. - s.89-98.).

To assess the aggregation of erythrocytes blood the C 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 resuspendiruetsa 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) Average unit size (CPA):

CPA=sea/KA

Sea - the sum of all cells in the units;

KA - the number of units.

2) Show the l 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% talks about increasing the SAE. In case of violation of at least one of these three indicators to patients with hypertension should be treated according to the inventive method.

The first 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 during exercise is supposed to 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, patients with hypertension 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 persons suffering from hypertension.

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 is 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 - 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 spokojnu is a 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.

Exercise 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. The walk is quiet with a steady breath average depth of 1-2 minutes

Exercise 15. Lying on the Mat to put under your head with a pillow. Go to position floor is sitting 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 tilted 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 min; 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 hundred the ONU.

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 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 pubescent. 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. Magic cube MOV is I am energetic. 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 - exhalation. 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 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 n 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 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. Reduce the giving of the total load. 1-2 minutes

3. Fractional exercise during the day.

Depending on the real conditions of life of patients with hypertension 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 different prolonged the tee depending on conditions (cleaning, home services, cleaning, gardening work, and others).

The second component of the claimed method is a daily swim in the sea, the river or the pool at least 20 minutes a day in the middle of the day.

The third component of the way of leveling advanced SAE in patients with hypertension is the appointment of lisinopril at a dose of 10 mg 1 time a day, morning and amlodipine 10 mg 1 time in the morning.

Example 1. Patient S. 45 years old, suffering from hypertension for the last 7 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=5,6, PA=1,48, PNA=69,1%), indicating that the increase of the AOC.

The patient was recommended dosed physical load, swimming in the pool at least 20 minutes a day in the middle of the day, the reception of lisinopril 10 mg in the morning and amlodipine 10 mg in the morning with strict control of blood pressure.

After 1 month it is established that the patient SAE (CPA=4,5, PA=1,12, PNA=88,4%) is normalized.

Example 2. Patient W. 59 years old, suffering from hypertension for the last 12 years, were examined during the follow up inspection regarding arterial hypertension. The patient was taken to the blood in a plastic tube with a subsequent study aggregation activity is of eritrotsitov (CPA=5,8, PA=1,60, PNA=58,3%), indicating a sharp increase in the SAE and the risk of thrombosis.

The patient was recommended dosage of static and dynamic exercise, daily swimming at least 20 minutes a day in the middle of the day, lisinopril 10 mg in the morning and amlodipine 10 mg in the morning.

After 1.5 months of treatment indicators aggregation of erythrocytes (CPA=4,6, PA=1,20, PNA=by 83.4%) were normal, 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 the vascular complications in patients with hypertension, 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 arterial hypertension, including use of metered static and dynamic physical loads, daily swimming at least 20 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 amlodipine 10 mg 1 every morning for 1.5 months.



 

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30 cl, 136 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: in formula (I') , R5 is any group selected from a group comprising C1-C6 alkoxy group, which can be substituted with one group selected from a group of β substitutes, phenyloxy group which can be substituted with one group selected from a group of γ substitutes, C1-C6 halogenalkoxy group and C3-C6 cycloalkyloxy group; R6 is a substitute in a benzene ring which is selected from a group of α substitutes; R7 is a hydrogen atom, C1-C6 halogenalkyl group, C1-C6 hydroxyalkyl group which can be substituted with a hydroxy-protective group, C1-C6 alkyl group which can be substituted with one group selected from a group of β substitutes, or a phenyl group which can be substituted with one hydroxy group; m equals 1; n equals 1 or 2; numbers in each benzene ring denote the number of the position of each substitute; the group of substitutes includes hydroxyl groups, nitro groups, cyano groups, C1-C6 dialkylamino groups, acetamide groups, halogen atoms, C1-C6 alkyl groups, which can be substituted with one group selected from a group of β substitutes, C1-C6 halogen alkyl groups, C3-C10 cycloalkyl groups, 6-member heterocyclic groups with an N atom or O atom as a heteroatom, C3-C6 cycloalkenyl groups, phenyl group which can be substituted with one group selected from a group of γ substitutes, 5-6-member heteroaryl groups with 1-3 N atoms as heteroatoms which can be substituted wit one or more groups selected from a group of γ substitutes, C1-C6 alkoxy groups, C1-C6 halogenalkoxy groups, C3-C10 cycloalkoxy groups, phenyloxy group, C1-C6 alkylthio groups, C1-C6 halogenalkylthio groups, C1-C6 alkylsulphonyl groups and C1-C6 alkylcarbonyl groups; the group of β substitutes includes C1-C6 alkoxycarbonyl groups, C3-C10 cycloalkyl groups which can be substituted with one group selected from a group of γ substitutes, C3-C6 cycloalkenyl groups, C6-C10 aryl groups which can be substituted with one or more groups selected from a group of γ substitutes, 5-6-member heteroaryl groups with one N, O or S heteroatom, 9-member heteroaryl groups with two heteroatoms selected from N and S, C1-C6 alkoxy group and C6-C10 aryloxy group; and the group of γ substitutes include cyano groups, C1-C6 dialkylamino groups, C1-C6 cyclic amino groups, halogen atoms, C1-C6 alkyl groups, C3-C10 cycloalkyl grous, C1-C6 halogenalkyl groups, C1-C6 alkoxy groups and C1-C6 alkylenedioxy groups. The invention also relates to compounds or pharmaceutically acceptable salts thereof, selected from: 4-(2-cyclopropylethoxy)-N-(2-(4-ethoxyphenyl)-1-{[(2-hydroxyethyl)amino]carbonyl}vinyl)benzamide, 4-(2-cyclopropylethoxy)-N-(2-[4-(cyclopropyloxy)phenyl]-1-{[(2-hydroxyethyl)amino]carbonyl}vinyl)benzamide, 4-(2-cyclopropylethoxy)-N-(2-[4-(difluoromethoxy)phenyl]-1-{[(2-hydroxyethyl)amino]carbonyl}-vinyl)-benzamide. Other compounds are given in the formula of invention. The invention also relates to a pharmaceutical composition which can inhibit bone resorption, which contains the disclosed compound, to use of the disclosed compound as a medicinal agent for inhibiting bone resorption, for preparing a medicinal agent for lowering concentration of calcium in the blood, for preparing a medicinal agent for inhibiting reduction of bone mass, to a medicinal agent for inhibiting bone resorption in form of the disclosed compound, to a method of inhibiting bone resorption, a method of lowering concentration of calcium in the blood, a method of inhibiting reduction of bond mass, involving addition of an effective amount of the disclosed compound.

EFFECT: more effective use of the compounds.

22 cl, 6 tbl, 116 ex

FIELD: chemistry.

SUBSTANCE: disclosed compounds can be used as a medicinal agent having CXCR2 inhibiting properties. In formula I , X denotes -CR3=CR4-, -CR5=N-, -N=CR6-, -NR7- or -S-; R3, R4, R5 and R6 independently denote hydrogen, F, CI, Br, I; R7 denotes hydrogen; Y1, Y2, Y3 and Y4 independently denote -CR8- or nitrogen, provided that at least two of Y1, Y2, Y3 and Y4 denote -CR8-; where R8 denotes hydrogen, F, CI, Br, I; A denotes a cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms; a bicyclic partially saturated 9-member cycloalkyl; a bicyclic partially saturated 9-10-member heterocycle in which two atoms in the ring are oxygen atoms; phenyl; naphthyl; a 5-6-member heteroaryl in which 1-3 atoms in the ring are oxygen, sulphur and nitrogen atoms; a 9-10-member bicyclic heteroaryl in which 1-3 atoms in the ring are nitrogen, oxygen and sulphur atoms; a 6-member heterocycle in which one atom in the ring is a nitrogen atom and which can be unsubstituted or substituted with alkyl having 1, 2, 3 or 4 carbon atoms, -C(O)CH3, -C(O)CH2CH3, -C(O)cyclopropyl, -C(O)CF3 and -C(O)OC(CH3)3; where phenyl, heterocyclic or heteroaryl radical is substituted with 1, 2 or 3 radicals selected from a group consisting of F, O, Br, I, OH, CN, NO2, SCF3, SF3, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, where 1, 2, 3 hydrogen atoms may be substituted with fluorine atoms; cycloalkyl having 3, 4, 5 or 6 carbon atoms; alkoxy having 1, 2, 3, 4, 5 or 6 carbon atoms, where 1, 2, 3 hydrogen atoms may be substituted with fluorine atoms; -S-alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, where 1, 2, 3 hydrogen atoms may be substituted with fluorine atoms; -NR9R10, C(O)R44, S(O)SR47, -(CH2)k-phenyl, 5-6-member heteroaryl, in which 1-3 atoms in the ring are nitrogen and sulphur atoms; where the phenyl radical may be substituted with F, CI, Br, I; R9 is an alkyl having 1, 2, 3 or 4 carbon atoms; R10 is an alkyl having 1, 2, 3 or 4 carbon atoms; R44 is an alkyl having 1, 2, 3 or 4 carbon atoms, where 1, 2, 3 hydrogen atoms may be substituted with fluorine atoms; alkoxy having 1, 2, 3 or 4 carbon atoms, cycloalkyl having 3, 4, 5 or 6 carbon atoms; R47 is an alkyl having 1, 2, 3 or 4 carbon atoms; k equals 0, 1, 2 or 3; s equals 1 or 2; B is -O-C(R11R12), -C≡C-, -CR52=CR53-, -C(R13R14)C(R15R16), -NR17-C(R18R19); R11, R12, R13, R14, R15, R16, R17, R18, R19, R52, R53 independently denote hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; D is C(O)OH, C(O)NHR21 or C(=NR58)NHR22; R21 and R22 independently denote hydrogen, -SO2-alkyl having 1, 2, 3 or 4 carbon atoms, -SO2-phenyl; R58 is OH; R1 and R2 independently denote an alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, where the alkyl radicals are unsubstituted or substituted with 1 radical selected from a group consisting of F, Cl, Br, I, phenyl substituted with OH; or R1 and R2, taken together with a carbon atom with which they are bonded form a 3-, 4-, 5- or 6-member carbocycle. The invention also relates to use of formula I compounds in preparing a medicinal agent which has CXCR2 inhibiting properties, to a medicinal agent which containing an effective amount of the disclosed compound and having CXCR2 inhibiting properties, as well as to use of formula II compounds (formula and values of radicals are given in the formula of invention) in preparing a medicinal agent having CXCR2 inhibiting properties.

EFFECT: high effectiveness of application.

10 cl, 384 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: claimed invention relates to compound of general formula (I) and its pharmaceutically acceptable salts. In general formula (I) , Y represents group -CONH(Q)- or -NHCONH(Q)-; Q represents 6-member aromatic ring or 5-10-member heteroaromatic ring, containing one or two N heteroatoms or two O heteroatoms; R represents hydrogen, halogen, linear or branched (C1-C6)alkyl; (C1-C6)alkoxy; di-(C1-C6)alkylamino, 5-member heteroaromatic ring, containing one O or S heteroatom; 6- or 9-member heteroaromatic ring, containing one or two N heteroatoms; phenyl, mono- or disubstituted with halogen, (C1-C6)alkyl, halogeno(C1-C6)alkyl, (C1-C6)alkoxy, acyl; hydroxy; piano; di-(C1-C6)alkylamino, acylamino' carbamoyl; X represents group : where Z represents CH2, N or O; m represents integer number from 1 to 3; p is equal 0, 1; R" is selected from group, consisting of di-( C1-C6)alkylaminocarbonyl, (C1-C6)alkyl, acyl. Invention also relates to pharmaceutical composition, containing as active ingredient, invention compound, to application of invention compound for manufacturing pharmaceutical composition, to method of inhibition of nicotinic acetylcholine receptor α7.

EFFECT: obtaining compound, which possesses agonistic activity with respect to nicotinic acetylcholine receptor (nAChR) α7.

7 cl, 2 tbl, 4 dwg, 270 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compound of general formula (I) or its pharmaceutically acceptable salt, mediated by glutamate receptor, and to based on them pharmaceutical composition. (I), where R1 stands for C1-6alkyl; R2 and R3 stand for hydrogen; p stands for 0; n stands for 1; R5 and R6 stand for hydrogen, and Het stand for thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, pyrazolyl, imidozolyl, each of which can be substituted with one or two groups, independently selected from the list, which consists of C1-6alkyl, C1-6alkoxy, acetyl, halogen, halogenC1-6alkyl, cyano.

EFFECT: creation of compound which has property to enhance response reaction.

4 cl, 2 tbl, 6 dwg, 38 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to (S)-(-)-amlodipine camsylate of formula , where camphorsulfonic acid represents (1S)-(+)-10- camphorsulfonic acid or (±)-10- camphorsulfonic acid, as well as to its hydrate and to pharmaceutical composition, including them, which can be applied in treatment of cardiovascular diseases.

EFFECT: high photostability and solubility.

8 cl, 3 ex, 5 tbl, 4 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of pharmaceutics and medicine and concerns method of improvement of pharmakinetic characteristics of peroral medication, directly metabolised by UGT1A1, of formula (I), which includes peroral introduction to mammal, which needs drug treatment, of combination of medication, or its pharmaceutically acceptable salt, and atasanavir, or its pharmaceutically acceptable salt.

EFFECT: improvement of pharmakinetic characteristics of medication.

13 cl, 2 dwg, 14 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: invention relates to the field of medicine, in particular to ophthalmology, and may be intended for treatment of hemodynamics abnormalities in visual nerve vessels in case of their atherosclerotic lesion. Medical therapy is administered with established treatment regimen. At the same time lipid spectrum of blood plasma is investigated, and if level of total cholesterol is more than 5.1 mmole/l, treatment with pentoxifylline in tablet form, 0.2 g 3 times a day after food intake, piracetam in pills, 40 mg 3 times a day before food intake, simvastatin, 10 mg per day, in tablet form, once, in the evening time, treatment is administered for 6 months. Afterwards hemodynamic indices are investigated by means of ultrasound Doppler sonography.

EFFECT: improved blood circulation in vessels of carotid system and regional vessels of visual nerve.

3 tbl, 1 dwg, 1 ex

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