Method of biological age reduction in arterial hypertension with abdominal obesity

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to gerontology and cardiology, and concerns biological age reduction in arterial hypertension combined with abdominal obesity. That is ensured by the integrated treatment including a low-calorie diet, reasonable graduated static and dynamic physical activity, daily swimming in a pool for at least 30 minutes, and the introduction of lisinopril in dosage 10 mg once a day in the morning and metformin in dosage 500 mg twice a day for the therapeutic course of 7 weeks.

EFFECT: complex of drug-induced and drug-free therapy combined with empirically prescribed treatment length provides biological age reduction in the case patients estimated by the relation of electronegative cells to total count in a buccal epithelium scrape due to normalised DNA repair and chromosome fragility level.

2 ex

 

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

Analogues of the proposed method of reducing biological age in patients with arterial hypertension (AH) with abdominal obesity (AO) does not exist.

In the literature there are recommendations for the appointment of a balanced diet, swimming and physical exercise to delay age-related changes (Podkolzin A.A., Dontsov V.I. Aging, longevity and bioactivity, Moscow, 1996. - 144 C.) to a greater extent focused on slowing the development of age-related changes in relatively healthy people. There is also information about applying rational diet (Savelyeva L. Modern approaches to treatment of obesity. // The doctor, 2000, No. 12 - p.12-14; Kadyrov, BC, Salhanov B.A. Nutrition in obesity. Alma-ATA, Kazakhstan, 1990) or physical training (V. Moshkov. Exercise in obesity. M.: Medicine, 1976.-56 C.) in patients with various components of the metabolic syndrome.

For the correction of AG is applied lisinopril, and when AO is used Metformin.

However, never before medical complex, consisting of a low-calorie diet, dosed physical activity, swimming and drugs Metformin and lisinopril, have not been applied in patients with AO to reduce their pathologically increased biological age.

The aim of the invention is the reduction of petal the cally increased biological age of the patients with AH and AO.

The essence of the proposed method lies in the fact that to reduce pathologically increased biological age of the patients with AH and AO for a long period of time is assigned to a low-calorie diet, measured static and dynamic exercise, daily swimming in the pool at least 30 minutes a day and drugs lisinopril at a dose of 10 mg 1 time a day, morning and Metformin 500 mg 2 times a day.

The method allows to align biological and chronological age in patients with AO for 7 weeks. Subject to the subsequent recommendations of the proposed method may reduce the biological age below chronological, which will significantly improve the quality of life of patients with arterial hypertension with AO, to reduce their pathological burden, reduce the number of cases of temporary disability, to accelerate and improve the quality of patient treatment, to exclude disability, as well as extend the life and reduce mortality of patients with arterial hypertension with AO from heart attack and stroke.

The inventive method is carried out as follows.

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

Calorie daily diet for each individual AG with AO is calculated (kcal) by the formula:

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

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

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

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

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

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

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

It is recommended that 3 main meals and 2 intermediate. With regular skipping one meal significantly increases the incidence of obesity, 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, protein (1 g contains 4 kcal), fat (9 kcal), carbohydrates (4 kcal) and alcohol (7 kcal).

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

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

1. Morning hygienic gymnastics (charging).

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

The sequence of the exercises involves the alternation of load on different muscle groups (arms, legs, body). Exercises are performed with gradually increasing excursion breathing, stretching, limited use of power conditions. Breathing exercise should be free, rhythmic, without delay, mainly 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.

When bad samochustvie and, the development of 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 with JSC recommended treatment and preventive exercises. Depending on the initial fitness may apply at the beginning of the lightweight option, physical activity, and subsequently enhanced option.

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

2.1. The lightweight version of preventive and curative gymnastics.

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

Exercise 2. Circular motion in the shoulder joints. When breeding - breath, when the 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.

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

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

Exercise 7. Standing, hands free. The walk free 1 min, then with high flexion of the hips, 10-20 movements with subsequent transition to a peaceful walk, 1-2 minutes Breathing rhythmic, 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, feet apart W is poco, hands on waist. Turns the body right and left, 6-10 times alternately. The head does not turn, to look forward.

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

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

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

Exercise 15. Lying on the Mat to put under your head with a pillow. Go to a half-sitting position and bent to hug the hips, exhale, 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, and stand on all fours; b) to move into position on his knees; hands up - inhale, tilt tolow the school, and the 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 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 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 upwards, 12-16 times. When the fold is NII - exhale, when the alignment of breath.

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

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

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

Exercise 6. The quiet walk 1-2 minutes

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

Exercise 8. 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

pragnienie 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 the 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 and 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. 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 hands, 20-30 steps; g) to sit on the Mat; C) lie on your back, relaxing breath. The whole complex repeat 3-4 times.

Exercise 22. Standing. Walking quiet breathing 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 legs with re what esteem on her the 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. To tilt the body 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 AO can recommend various exemplary embodiments of the fractional loads to increase physical (motor) activity during the day.

Option 1.

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

Exercise 2. Sitting up with deflection housing and land, 8-10 times.

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

Option 2.

Exercise 1. Standing, walking with high shimoyamate, 16-30 times.

Exercise 2. Standing, circular motions his head 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, moving into a standing position, 10-12 times.

Option 3.

Exercise 1. The quiet walk, 1 min

Exercise 2. Walking fast, 1 min

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

Exercise 4. Walking quiet breathing, 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).

In addition to custom-made non-medical treatment of sick AG with AO should be administered daily swimming in the pool at least 30 minutes per day lisinopril at a dose of 10 mg 1 time a day and Metformin 500 mg 2 times a day.

The biological age of patients is determined by calculating the ratio of the number of electronegative cells to the total number of scraping buccal epithelium when conducting microelectrophoresis (VG Shahbazov, A.L. Nabokov, T.V. Kolupaeva. The method of determining b is a logical a person's age. Description of the invention to author's certificate SU 1169614). The obtained results are evaluated according to the reference curve (see drawing). The essence of this process explain the examples.

Example 1. The patient M, 55 years old, suffering from hypertension with the company for 12 years after a night of rest was taken the sample of buccal cells. A sample of cells, which have previously added to 0.5 μl of water was placed in a cell of microelectrophoresis. Included a constant voltage source, providing on the electrode chamber current of 0.1 ml, and within 5 min were observed under the microscope, by change of polarity, with the offset of cell nuclei in the electric field in five fields of view. The number of electronegative (EA) engines amounted to 39 per 100 cells. Passport age of surveyed persons 55 years. This indicates that the result should be compared with the right branch of the reference curve to determine the biological age. Putting a value on the curve EA and projecting on the abscissa, find age appropriate 61 year. This indicates that this person older than his passport age of 6 years. The patient was assigned to a low-calorie diet, daily physical activity, daily swimming in the pool at least 30 minutes a day, lisinopril 10 mg 1 every morning and Metformin 500 mg 2 times a day. The patient was regularly looked after the start is ecene. Simultaneously with the inspection was carried out the determination of the biological age.

After 7 weeks of treatment, the patient electronegativity nuclei of cells was 48%, testified under biological and chronological age in this patient.

The patient is asked to comply with these recommendations in future.

Example 2. In patient 3, 42 years old, suffering from hypertension with the company for 6 years under examination revealed that the rate electronegative nuclei, defined as in example 1 was 45%. The patient was assigned to a low-calorie diet, daily physical activity, daily swimming in the pool at least 30 minutes a day, lisinopril 10 mg 1 every morning and Metformin 500 mg 2 times a day. The patient was regularly looked after the start of treatment. Simultaneously with the inspection was carried out the determination of the biological age.

After 7 weeks of treatment, the patient was reduced biological age below the calendar. The electronegativity of nuclei was 61%, which indicated that the biological age of the patient was equal to 40 years.

The patient is recommended to follow the instructions given in the following.

The use of the proposed method of correction of biological age in gerontology and cardiology will help to avoid many complications in patients with AH and AO, to reduce Niccolo cases of temporary disability, to reduce the duration of hospitalization, reduce morbidity and mortality.

The way to reduce pathologically increased biological age in hypertensive patients with abdominal obesity, including the appointment of a low-calorie diet, a rational dosed static and dynamic physical loads, daily swimming in the pool at least 30 minutes a day and drugs lisinopril 10 mg 1 every morning and Metformin 500 mg 2 times a day for at least 7 weeks.



 

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8 cl, 9 dwg, 9 tbl, 12 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula or its pharmaceutically acceptable salt, where R1 and R2 each independently denotes a hydrogen atom, a halogen atom, a lower alkyl, a hydroxyl group, a cyano group or a lower alkoxy; R3 independently denotes a hydrogen atom, a halogen atom, a lower alkyl, a lower alkoxy, a hydroxyalkyl, trifluoromethyl, lower alkenyl or cyano group; R4 independently denotes a hydrogen atom, a lower alkyl, a lower alkoxy, a halogen atom, trifluoromethyl, hydroxyalkyl optionally substituted with a lower alkyl, aminoalkyl optionally substituted with lower alkyl, alkanoyl, carboxyl group, lower alkoxycarbonyl or cyano group; Q denotes a nitrogen atom; R5 and R6 each independently denotes a hydrogen atom, a lower alkyl, a halogen atom, a lower alkylsulfonyl, a lower alkylsulfanyl, alkanoyl, formyl, aryl, mono- or di-(lower) alkylcarbamoyl or mono- or di-(lower) alkylsulfamoyl; and further as indicated in the formula of invention. The invention also relates to a glucokinase activator containing the compound in paragraph 1 and to a therapeutic agent based on said compounds.

EFFECT: novel compounds which can be useful in treating and preventing diabetes and obesity are obtained and described.

29 cl, 227 ex, 6 tbl

FIELD: medicine.

SUBSTANCE: claimed group of inventions relates to medicine, namely to endocrinology, and deals with regulation of fat in organism. For this purpose stabilisation of alpha subunit of hypoxia-induced factor protein (HIFα) is realised. In order to stabilise HIFα efficient amounts of compound inhibiting HIF hydroxylase activity, representing 2-oxoglutarate-dioxygenase mimetic are introduced.

EFFECT: inventions ensure reduction of fat formation and deposition due to regulation of its metabolism.

31 cl, 11 dwg, 13 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula (I) , where R1 is selected from group, including: phenyl, unsubstituted or mono-, di- or tri-substituted independently with lower alkyl, lower alkoxy group, halogen or lower halogenalkyl; naphtyl; tetrahydronaphtyl; C3-7cycloalkyl; -(CHR3)m-phenyl, where m stands for 1, 2, or 3; and phenyl is unsubstituted or mono-, di- or tri-substituted with lower alkoxy group, and where R3 is independently selected from hydrogen and lower alkyl; -(CH2)n-heteroaryl, where n stands for 1, 2 or 3; term "heteroaryl" relates to aromatic 5- or 6- member ring or bicyclic 9-member aromatic groups, which can include 1, 2 or 3 atoms, selected from nitrogen and/or sulphur; -(CH2)n-heteroaryl, where n stands for 1, 2 or 3; term "heteroaryl" relates to aromatic 5- or 6- member ring or bicyclic 9-member aromatic groups, which can include 1, 2 or 3 atoms, selected from nitrogen and/or sulphur, and heteroaryl is mono-, di- or tri-substituted independently with lower alkoxy group; and R2 is selected from group including: n-butyl; phenyl, unsubstituted or mono-, di- or tri-substituted independently with lower alkyl, halogen or lower alkoxy group; heteroaryl, where term "heteroaryl" relates to aromatic 5-member ring, which can include 1, 2 or 3 atoms, selected from nitrogen and/or sulphur; unsubstituted or mono-, di- or tri-substituted independently with lower alkoxy group; -C(O)-NR4R5; where R4 and R5 stand for lower alkyl or together with nitrogen atom, to which they are bound, form 5-member heterocycle, which can additionally contain heteroatom, selected from N or S, and to their pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition.

EFFECT: obtaining novel biologically active compounds, able to inhibit DPP-IV.

13 cl, 43 ex

Novel compounds // 2395511

FIELD: chemistry.

SUBSTANCE: present invention relates to novel xanthine derivatives of general formula (I) and their pharmaceutically acceptable salts which have HM74A receptor activity, which can be used in therapy for treating diabetic dyslipidemia, combined dyslipidemia, heart failure, hypercholesteremia, atherosclerosis, arteriosclerosis, hypertriglyceridemia, type II sugar diabetes, type I diabetes, insulin resistance, hyperlipidemia, anorexia nervosa, obesity, coronary artery disease, thrombosis, stenocardia, chronic kidney disease, peripherical vascular disease or stroke. In compounds of formula (I) , R1 is hydrogen or methyl; R2 is unsubstituted H-C4-6 alkyl; and R3 is chlorine.

EFFECT: obtaining novel compounds and a pharmaceutical composition based on the said novel xanthine derivatives.

15 cl, 54 ex

FIELD: chemistry.

SUBSTANCE: invention relates to use of existing and novel N-sulfamoyl- N'-arylpiperazines and their physiologically compatible acid-addition salts of formula I , where Ar denotes a monocyclic or bicyclic C6-C10aryl in which ring carbon atoms are optionally substituted with 1-3 nitrogen or oxygen atoms, and/or where the C6-C10aryl ring system optionally contains 3-5 double bonds, and/or where the C6-C10aryl ring system is optionally substituted with 1 or 2 substitutes which can be identical or different and which can be selected from a group containing halogen, trifluoromethyl, cyano group, nitro group, C1-C4alkyl, C1-C4alkoxy group, C1-C4alkylsulfonyl; and two oxygen atoms which are bonded to two neighbouring carbon atoms of the C6-C10aryl ring system and are bonded by a C1-C2alkylene bridge; or where the C6-C10aryl ring system is substituted with phenyl which can optionally be substituted in the phenyl ring by one substitute which can be selected from a group containing halogen; for preventing or treating obesity and related diseases.

EFFECT: design of a method of obtaining the said compounds and a pharmaceutical composition based on the said compounds.

25 cl, 9 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula I , where X is N or CH; R1 is -C(O)-NR8R9 or -C(O)-OR10, and R2 is hydrogen; or alternatively R2 is and R1 is hydrogen or halogen; Y is N or CH; R3, R4, R5 and R6 are independently selected from a group consisting of hydrogen, halogen, (lower)alkoxy, (lower)fluoroalkyl, (lower)fluoroalkoxy and (lower)fluoroalkylsulfanyl; or R3 and R4 together with carbon atoms with which they are bonded form a 6-member unsaturated ring which can contain one nitrogen heteroatom; R7 is hydrogen or (lower)alkyl; R8 is hydrogen or NH2; R9 is selected from a group consisting of (lower)alkyl, (lower)alkenyl, (lower)alkoxyalkyl, -(CH2)m-(C3-C7)cycloalkyl, -(CH2)m-piperidinyl, -(CH2)m-phenyl, where the phenyl ring is unsubstituted or substituted with one or two groups selected from halogen, (lower)alkoxy, (lower)fluoroalkyl and (lower)fluoroalkoxy, -(CH2)m-naphthyl and pyridylamino; R10 is (lower)alkenyl; R11 is selected from a group consisting of -C(O)-R12, -SO2-R13 and -SO2-NR14R15; R12 is selected from a group consisting of (lower)alkyl, (lower)alkoxyalkyl, -(CH2)n-(C3-C7)-cycloalkyl, -(CH2)n-phenyl and -(CH2)n-pyridyl, where phenyl or pyridyl are unsubstituted or substituted with one (lower)alkyl; R13 is selected from (lower)alkyl or -(CH2)n-phenyl, where phenyl is unsubstituted or substituted with one (lower)alkyl; R14 is (lower)alkyl; R15 is (lower)alkyl; m equals 0, 1 or 2; n equals 0 or 1; and all their pharmaceutically acceptable salts. The invention also relates to a pharmaceutical composition based on formula I compounds.

EFFECT: novel indole and benzimidazole derivatives which have modulating effect on the CB1 receptor are obtained.

26 cl, 3 tbl, 148 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds of formula Ia and their pharmaceutically acceptable salts, hydrates, solvates, esters and amides. In formula Ia , A is specified from -C(O)OR5 where R5 represents hydrogen; W represents C1-3alkylene; Y is specified from phenyl and 5-6-member heteroaryl containing one heteroatom specified from N, S, O; where any phenyl or heteroaryl Y can be optionally substituted with 1 to 3 radicals specified from halogen, C1-6alkyl, C1-6alkoxygroup, halogen-substituted C1-6alkyl and halogen-substituted C1-6alkoxygroup; Z is specified from: where left and right asterisks Z specify an attachment point between -C(R3)(R4)- and A of formula la; R6 is specified from hydrogen and C1-6alkyl; or R6 can be attached to carbon atom in Y to form a 5-7-member ring; R1 is specified from phenyl and 5-member heteroaryl containing one heteroatom specified from S, O; where any phenyl or heteroaryl R1 is substituted with a radical specified from phenylC0-4alkyl, heteroarylC0-4alkyl where heteroaryl represents 5-6-member heteroary containing one heteroatom specified from N, S, O, C3-8cycloalkylC0-4alkyl, C3-8heterocycloalkylC0-4alkyl which contains nitrogen atom as heteroatom, or C1-6alkyl; where any phenyl, heteroaryl, cycloalkyl or heterocycloalkyl group R1 can be optionally substituted with 1 to 3 radicals specified from halogen, C1-6alkyl, C1-6alkoxygroup, halogen-substituted C1-6alkyl group and halogen-substituted C1-6alkoxygroup; R2 represents C1-6alkyl group; R3 and R4 represent hydrogen.

EFFECT: preparation of the pharmaceutical composition exhibiting EDG/S1P receptor modulating properties, containing therapeutically effective amount of the compound under the invention, development of a method of treating the disease mediated by EDG/S1P receptor activity, application of the compounds for preparing a drug for prevention or treatment of the disease mediated by EDG/S1P receptor activity.

16 cl, 1 tbl, 86 ex

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