Method for normalising function reactivity of cardiovascular system at arterial hypertension, dislipidemia and abdominal obesity

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to cardiology, and concerns normalising functional reactivity of cardiovascular system (CVS) at arterial hypertension and abdominal obesity. To that end, the state of CVS functional reactivity at psychoemotional stress is assessed by recording systolic, diastolic and average dynamic blood pressure (BP av.dyn) and heart rate (HR). These data serve as the basis for determining functional reactivity index (FRI) prior to and after the stress, according to the following formula: FRI = (BP av.dyn. × heat rate)/100 (conv. un.). If FRI value after stress rises by more than 20 conventional units, complex therapy is implemented including individual hypocaloric diet calculated by a formula considering sex and age, sensibly graded static and dynamic physical exercise as well as administration of irbesartan in a dose of 50 mg once a day, in the morning, over at least 4 months.

EFFECT: complex of drug and non-drug treatment combined with empirically chosen course duration ensures normalisation of CVS functional reactivity among the specified group of patients due to potentiation of certain components of the therapeutic complex.

1 ex

 

The invention relates to medicine, cardiology, and can be used in therapeutic departments of clinics and hospitals. Analogues of the method of normalization of the functional reactivity of the cardiovascular system with arterial hypertension (AH), dyslipidemia (D) and abdominal obesity (AO) does not exist.

The aim of the invention is to increase the efficiency of correction of the functional reactivity of the cardiovascular system in AG with D and AO.

The essence of the proposed method of correction of the functional activity of the cardiovascular system is to increase the tolerance of patients with arterial hypertension with D and AO to emotional stress and increase functional reactivity of cardiac-vascular system in the execution of their metered emotional load and reducing the risk of cardiovascular complications during emotional stress, measured after holding dosed emotional load with the ever increasing speed for 18-20 minutes with every minute registration parameters of Central hemodynamics: arterial systolic pressure (SBP), diastolic blood pressure (Add), arterial pressure medium dynamic (Adsin.) and heart rate (HR), determine the value of the indicator function reactionist the (FIU), which is the work of the AD medium dynamic on heart rate, calculate the relative increment values FIU when performing load compared with the value at rest and largest values FIU assess the type of functional reactivity of the cardiovascular system: when the FIU is more than 20 usled reactivity assessed as hyperfunctional (with AG in combination with D, IGT and AO), the FIU is less than 10 usled response to the load estimate as Hypo-functional and, when values of the FIU from 10 to 20 usled type functional reactivity assessed as normal.

Time psychoemotional load no more than 20 minutes For the normalization of the indicator functional reactivity in patients with hypertension, with D and AO uses a combination of individualized low-calorie diet, rationally dosed static and dynamic physical loads and irbesartana for at least 4 months.

The inventive method is carried out as follows. The value of the FIU is determined by Lebedeva OD, Radziejewski S.A., Bugaeva S.A. Method of assessment of the functional reactivity of the cardiovascular system, EN 2207044. The patient is seated in front of the screen. The patient on the left shoulder impose cuff for measuring blood pressure systolic blood what about the diastolic pressure, blood pressure average dynamic and heart rate prior to loading and during loading. The patient offer two sets of 4 letters: 'ÀNEU and BLOG, of which he must choose to remember one. After registration of hemodynamic parameters during 3 min and memory (30) of the selected set of letters begin conducting psycho-emotional loads, namely, that the subject pressing notes scattered letters from the selected set of progress on the monitor screen square frames situated in a random sequence the letters of the alphabet. The speed of advancement of the frames in the series of letters in the process of conducting samples increases with 3 letters 1 at the beginning of the load up to 6 letters 1, starting from 6 min load, and this provides a gradual vrabatavaemomu patient. Errors in elevation of letters from a selected set of auditory signals, for which the subject may be oriented in the proper execution of the load and try to adjust its execution. After the load calculates the average value of the BPA, Add, Adsin. and heart rate in the periods prior to loading and during loading. HELL the average dynamic calculated by the formula: Adsin.=Add+[0,42(SBP-Add)].

HELL the average dynamic is a complex resultant of all variables HELL. When Prov is Denia samples with emotional stress in healthy individuals the HELL the average dynamic changes slightly, and heart rate usually increases. According to studies, increased heart rate and HELL leads to increased demand of oxygen and increase its energy costs. In pathology, for example, when AG with D and AO, the vessels in a state of spasm, unable to provide the required increased amount of oxygen, which can increase hypoxia, be coming the cerebral circulation, etc.

On the basis of the data used to calculate the functional reactivity, which allows an integrative measure of the increase in hemodynamic load on the heart and, consequently, the risk of developing cardiovascular complications, defined as follows:

FIU=(Adsis)·/100(used).

The increment values FIU during the transition from rest to execution of the load determines the index:

FIU=PFR-PFR,

where the FIU is the dierence between the values of the FIU before and during loading

PFR - averaged value of the index before load

PFR - averaged value of the index under load.

The relative increment values FIU assess the type of functional reactivity of the cardiovascular system: if the value is *, then divide by 100 to obtain conventional units (used - the double digits).

When you study in the dynamics of treatment Bo is gnome give to remember another set of letters in order to prevent addiction.

When the increment values after conducting dosed emotional load FIU from 10 to 20 usled functional type of reactivity is assessed as normal. When the FIU to load more than 20 usled type functional reactivity assessed as hyperfunctional. In this case the patient AG with D and AO must be assigned at least 4 months a combination of individualized low-calorie diet, measured static and dynamic physical loads and irbesartan 150 mg in the morning 1 times.

To create a negative energy balance in the body of patients they can as an option be recommended following an individually customized 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 (as a rule, patients physical activity level low).

Rekomenduu the Xia 3 main meals and 2 intermediate. With regular skipping one meal significantly increases the incidence of obesity, also revealed a positive 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 - proteins (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, the use of which can be as one of the options in the form below.

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 Agroskin different muscle groups (arms, legs and 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, patients are recommended treatment and preventive exercises. Depending on the initial fitness may use first lightweight option, physical activity, and subsequently enhanced option.

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

2.1. A lightweight version of the treatment-and-prophylactic guy who nastika

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 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. Breath to agree with the movement to the receiving corps and hands. 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.

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 e is scurvy 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 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 step is. 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 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 is energetic, when 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 to touch the right hand to the 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 implement the best 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 to 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. Legs not smesiteli 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 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 RA is doing - 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

A patient with hypertension, D. and AO is the patient with a number of related disorders, primarily the cardiovascular system. This circumstance limits the simultaneous application of a high physical load during morning exercises, as well as in the main lesson, curative gymnastics. This is why increasing the physical activity of persons suffering from hypertension with D and AO should be implemented by the distribution of physical activity in small doses throughout the day. This method of increasing the physical activity of patients should be considered as a method of fractional loads.

Depending on the real conditions of life of patients suffering from varying degrees of abdominal obesity, 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 Bo is isim turning your body - 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).

Timely and effective correction of the FIU in patients with AH and AO will allow in the short term to normalize the functional reactivity of the cardiovascular system that will reduce these patients the period of temporary disability, renders prophylactic action against strokes and heart attacks, reduce the number of outputs on disability and reduce mortality among patients with hypertension with D and AO.

Example. Examined the patient L., 42 years old, suffering the AG II degree, Stage II with D, JSC for 5 years. In the study of hemodynamics in the initial state before conducting psycho-emotional loads the BPA was equal to 140 mm Hg, Add - 91 mm Hg, Adsin. - 111,6 mm Hg, heart rate of 74 beats per 1 minute FIU before psychoemotional load was equal (8256)/100 - 82,5 used When conducting psycho-emotional loads BPA increased to 168 mm Hg, Add - 105 mm Hg, Adsin. to 131, 5mm mm Hg, heart rate up to 94 beats per 1 minute, the FIU is increased to (12361)/100=123,6 used, i.e. the increment of the FIU on the load or what is the same, FIU, made up 41.1 used (82,5 used to 123.6 used), which can be considered as a manifestation of hyperthyroidism cardiovascular system. The patient is assigned to a combination of individualized low-calorie diet, rationally dosed static and dynamic physical loads and irbesartan 150 mg in the morning. After 4 months of treatment, the magnitude of the FIU fell before the load compared to the same before the treatment: the BPA - up to 126 mm Hg, Add up to 78 mm Hg, Adsin. up to 98.2 mm Hg, heart rate up to 68 beats per 1 minute, FIU - to 66.7 used When performing load marked decrease compared with the condition before treatment the increase in value of the BPA - up to 138 mm Hg, Add - up to 87 mm Hg, Adsin. to 108,4 mm Hg, heart rate is 78 beats per 1 minute, FIU - up to 84.6 used, that is marked increment values FIU, or FIU, 17.9 used (before treatment - 1.1 usled), that may be indicative of increased tolerance of the cardiovascular system to psycho-emotional stress, about the reduction of hyperthyroidism cardiovascular system and, consequently, about the economization of cardiac activity.

As a result of application of the proposed method of correction of functional reactivity of the cardiovascular system in patients with hypertension, with D and AO is achieved normalization of the functional reactivity of the cardiovascular system for dosed psycho-emotional stress, which allows you to use the way for the normalization of the tolerance of patients with arterial hypertension with D and AO to psycho-emotional stress, which can reduce the degree of hemodynamic load when exposed to stress, reducing the risk of development of psycho-emotional loads adverse cardiovascular reactions (angina, myocardial infarction, ischemic, and others).

The method of normalization of the functional reactivity of the cardiovascular system (CVS) with arterial hypertension, dyslipidemia and abdominal obesity, including assessment of functional reactivity SSS during emotional load, which record systolic, diastolic, srednetehnicheskoe pressure (BP Srdan.), heart rate (HR), on the basis of these indicators identify elaut indicator functional reactivity (FIU) before and after exercise, using the formula: FIU=(Adsin.×HR)/100(used), and with increasing values FIU after load of more than 20 facilities. units perform a complex therapy, including a personalised low-calorie diet, calculated by the formula:
for women: 18-30 years of age (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 of age (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,
rationally dosed static and dynamic physical loads, and the introduction of irbesartan at a dose of 150 mg 1 every morning for at least 4 months.



 

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1 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to cardiology, and concerns normalising functional reactivity of cardiovascular system (CVS) at arterial hypertension and abdominal obesity. To that end, the state of CVS functional reactivity at psychoemotional stress is assessed by recording systolic, diastolic and average dynamic blood pressure (BP av.dyn) and heart rate (HR). These data serve as the basis for determining functional reactivity index (FRI) prior to and after the stress, according to the following formula: FRI = (BP av.dyn. × heat rate)/100 (conv. un.). If FRI value after stress rises by more than 20 conventional units, complex therapy is implemented including individual hypocaloric diet calculated by a formula considering sex and age, sensibly graded static and dynamic physical exercise as well as administration of losartane in a dose of 50 mg once a day, in the morning, over at least 4 months.

EFFECT: complex of drug and non-drug treatment combined with empirically chosen course duration ensures normalisation of CVS functional reactivity among the specified group of patients due to potentiation of certain components of the therapeutic complex.

1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a free base (R)-3-[1-(2,6-dichloro-3-fluoro-phenyl)- ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine in crystalline form, having a powder X-ray diffraction pattern with peaks at diffraction angles (2θ) 15.7±0.1, 17.3±0.1 and 19.7±0.1. The invention also relates to a pharmaceutical composition, to methods of treating cancer in mammals, as well as to a method of treating abnormal cell growth in mammals in need of such treatment.

EFFECT: obtaining an novel biologically active compound having the said inhibitory activity.

12 cl, 1 ex, 3 tbl, 2 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound or its salt of formula 1: , where A, E, D, R0, R1-R4 and a assume values given in the formula of invention. The invention also relates to an antioxidant medicinal agent.

EFFECT: effectiveness during treatment of ischemic diseases of organs, during treatment of diseases caused by oxidation cell disorders and when inhibiting disorders of the retina.

4 cl, 1 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

or

or to their pharmaceutically acceptable salts, where ring A, R2, R3, R4 and X are as defined in the description. The disclosed compounds are useful as 11βHSD1 inhibitor. The invention also relates to a pharmaceutical composition, an agent for treating or preventing pathology related to glucocorticoids, a 11βHSD1 inhibitor containing the disclosed compound or its pharmaceutically acceptable salt, and use of the disclosed compounds.

EFFECT: compounds are highly effective.

40 cl, 48 tbl, 191 ex

FIELD: chemistry.

SUBSTANCE: invention proposes 5-member heterocyclic inhibitors of kinase p38, including kinase p38α and kinase p38β, based on pyrazoles and imidazoles, with the general formula given below , in which ring B is phenyl, and C is a pyrazole or imidazole ring, and the rest of the symbols assume values given in paragraph 1 of the formula of invention.

EFFECT: there are described pharmaceutical compositions containing said compounds, as well as methods of using the compounds and compositions, including a method of treating, preventing or suppressing one or more symptoms of diseases and conditions mediated by kinase p38 which include, but not limited to, inflammatory diseases and conditions.

31 cl, 6 tbl, 175 ex

Pyrazoles // 2381217

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I), where one of R1 and R2 is hydrogen or alkyl, and the other is (CH2)PY, where p=0 or 1, Y is a saturated mono-, bi- or tricyclic 5-10-member cycloalkyl ring optionally substituted with alkyl, or R1 and R2 together with N form a 7-10-member saturated bicyclic ring Z, optionally substituted with halogen, or a 5-7-member monocyclic ring Z, optionally substituted with alkyl, phenyl, phenylalkyl or pyridinyl; R3 is [2,2']bithiophenyl, 1-methylindole, 2,3-dihydrobenzo[1,4]dioxin, benzo[1,3]dioxole, benzothiophene, dibenzofuran, furan, naphthalene, quinoline, thianthrene, thiophene or pyrrole, or biphenyl substituted with halogen, or phenyl optionally substituted with one or more amino, cyano, formyls, halogens, hydroxyl, hydroxymethyls, acyls, acylamino, alkoxy, nitro, trifluoromethoxy, trifluoromethyls, phenoxy or benzyloxy, or R3 is a group, where Ar is phenyl substituted with halogen; and R4 is alkyl; and pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical composition with inhibitory activity towards the 11β-hydroxysteroid dehydrogenase1 (11(β-HSD1) enzyme.

EFFECT: pyrazole composition is disclosed.

22 cl, 1 tbl, 116 ex

FIELD: medicine.

SUBSTANCE: invention is related to antagonists of serotonin 5-HT6 receptors of common formula 1 and their pharmaceutically acceptable salts and/or hydrates, pharmaceutical compositions, dosage forms and methods of production. Invention also includes new compounds of formula 1.1. In formulae 1 and 1.1 , Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur and heteroatom; R1 represents atom of hydrogen, unnecessarily substituted C1-C5 alkyl; Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur as heteroatom; R1 represents atom of hydrogen, which is unnecessarily substituted C1-C5 alkyl; R21,R22, R31, R32 independently from each other represent atom of hydrogen or substituent of aminogroup, selected from unnecessarily substituted C1-C4 alkyl, unnecessarily substituted phenyl, or R31 and R32 together with atom of nitrogen, to which they are bound, create unnecessarily substituted saturated 6-member heterocycle, possibly containing atom of nitrogen in cycle; or R1 together with atom of nitrogen, to which it is bound, and R21 and R22 together with atom of nitrogen, to which they are bound, create substituted pyrimidine cycle. In formula 1.1 R4, R5 and R6 independently from each other represent atom of hydrogen, unnecessarily substituted C1-C3 alkyl or phenyl.

EFFECT: compounds of invention may find application for treatment and prevention of development of conditions and disorders of central nervous system.

13 cl, 11 dwg, 4 tbl, 11 ex

FIELD: medicine.

SUBSTANCE: invention is related to new derivatives of common formula (I) , in which: A, if available, means (C1-C6)-alkyl; R1 means group NR6R7, (C4-C7)-azacycloalkyl, (C5-C9)-azabicycloalkyl, besides, these groups, unnecessarily, are substituted with one or more substituents, selected from (C1-C5)-alkyl or halogen; A-R1 is such that nitrogen of radical R1 and nitrogen in position 1 of pyrazole are necessarily separated at least by two atoms of carbon; R3 means radical H, OH, NH2, ORc, NHC(O)Ra or NHSO2Ra; R4 means phenyl or heteroaryl, unnecessarily, substituted with one or more substituents, selected from halogen, CN, NH2, OH, ORc, C(O)NH2, phenyl, polyfluoroalkyl, linear or ramified (C1-C6)-alkyl, besides these substituents, unnecessarily, are substituted with halogen, and moreover, heteroaryl radicals are 3-10-member, containing one or more heteroatoms, selected from sulphur or nitrogen; R5 means radical H, linear or ramified (C1-C6)-alkyl; Ra means linear or ramified (C1-C6)-alkyl; Rc means linear or ramified (C1-C6)-alkyl, (poly)fluoroalkyl or phenyl; R6 and R7, independently from each other, means hydrogen, (C1-C6)-alkyl; R6 and R7 may create 5-, 6- or 7-member saturated or non-saturated cycle, which includes one heteroatom, such as N, and which, unnecessarily, substituted with one or more atoms of halogen; to its racemates, enantiomers, diastereoisomers and their mixtures, to their tautomers and their pharmaceutically acceptable salts, excluding 3-(3-pyridinyl)-1H-pyrazole-1- butanamine, 4-(3-pyridinyl)-1H-pyrazole-1-butanamine and N-(diethyl)-4-phenyl-1H-pyrazole-1-ethylamine. Invention is also related to methods for production of compounds of formula (I) and to pharmaceutical composition intended for treatment of diseases that appear as a result of disfunction of nicotine receptors α7 or favorably responding to their modulation, on the basis of these compounds.

EFFECT: production of new compounds and pharmaceutically acceptable composition on their basis, which may find application in medicine for treatment, prophylaxis, diagnostics and observance over development of psychiatric or neurological disorders or diseases of central nervous system, when cognitive functions deteriorate or quality of sensor information processing drops.

16 cl, 106 ex

FIELD: medicine.

SUBSTANCE: invention refers to new compounds of formula: I where R1 represents hydrogen or C1-7-alkyl; R2 and R3 independently represent hydrogen; R4 and R5 independently represent hydrogen; R6, R7, R8 and R9 independently represent hydrogen, C1-7-alkyl; and one of R6, R7 and R8 represents where R10 represents hydrogen, C1-7-alkyl; R11 represents hydrogen, C1-7-alkyl; one of R12 or R13 represents hydrogen, C1-7-alkyl or fluorine-C1-7-alkyl; and the other represents undivided electron pair; R14 represents hydrogen, C1-7-alkyl, halogen; R15 represents aryl or aryl substituted with 1-3 groups chosen from C1-7-alkyl C1-7-alkoxy, halogen, fluorine-C1-7-alkyl and fluorine-C1-7-alkoxy; and n has a value 1, 2 or 3; and to all their enantiomers and to pharmaceutically acceptable salts and/or esters. The invention also concerns the pharmaceutical compositions.

EFFECT: production of new biologically active compounds with agonist activity with respect to PPARδ and PPARα.

20 cl, 25 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to antagonists of serotonin 5-HT6 receptors - substituted 4-sulphonylpyrazoles and 3-sulphonyl-pyrazolo[1,5-a]pyrimidines of general formula 1 or general formula 1.2. These compounds can be used for treating and preventing development of different cognitive and neurodegenerative diseases of the central nervous system. In general formulae 1 and 1.2, 1 1.2 respectively, Ar is optionally substituted phenyl or optionally substituted 5-6-member heteroaryl, containing a nitrogen, oxygen or sulphur atom as a heteroatom; R1 is a hydrogen atom, optionally substituted C1-C5 alkyl, lower acyl or optionally substituted phenyl; R2 is an optionally substituted amino group or substituted hydroxy group or R1, together with the nitrogen atom to which it is bonded, and R2, together with the carbon atom to which it is bonded, form a substituted pyrimidine ring; R3 is a hydrogen atom, optionally substituted C1-C5alkyl, substituted hydroxyl group or substituted sulphanyl group, R5 is a hydrogen atom, optionally substituted C1-C5alkyl, substituted hydroxyl group or substituted sulphanyl group, R7 and R9 independently represent a hydrogen atom, C1-C3alkyl or phenyl, R8 is a hydrogen atom.

EFFECT: new compounds have useful biological properties.

13 cl, 2 dwg, 4 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to cardiology, and concerns normalising functional reactivity of cardiovascular system (CVS) at arterial hypertension and abdominal obesity. To that end, the state of CVS functional reactivity at psychoemotional stress is assessed by recording systolic, diastolic and average dynamic blood pressure (BP av.dyn) and heart rate (HR). These data serve as the basis for determining functional reactivity index (FRI) prior to and after the stress, according to the following formula: FRI = (BP av.dyn. × heat rate)/100 (conv. un.). If FRI value after stress rises by more than 20 conventional units, complex therapy is implemented including individual hypocaloric diet calculated by a formula considering sex and age, sensibly graded static and dynamic physical exercise as well as administration of losartane in a dose of 50 mg once a day, in the morning, over at least 4 months.

EFFECT: complex of drug and non-drug treatment combined with empirically chosen course duration ensures normalisation of CVS functional reactivity among the specified group of patients due to potentiation of certain components of the therapeutic complex.

1 ex

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