Spontaneous erithrocite aggregation reduction method in patients with stable angina pectoris fuctional class i-ii
SUBSTANCE: invention belongs to medicine, notably to haematology and cardiology and refers to reduction of spontaneous erythrocytes aggregation in patients with stable effort angina functional class I-II. To achieve this complex treatment including hypolipidemic diet, controlled activity, at least 30 minutes swimming daily and 20 mg of simvastatin once daily after supper is administered.
EFFECT: method allows spontaneous erythrocytes aggregation correction during 2 months providing blood rheological properties enhancement and, correspondingly, thrombotic complication risk decrement in this group of patients.
2 ex, 1 tbl
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 stable angina I-II functional class (SS I-II FCL) does not exist.
For the correction of SS I-II FCL often be prescribed statins, including simvastatin in the treatment of patients with SS I-II F. cells are often included lipid-lowering diet, 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 SS I-II F. class. that would solve the problem of correction of coronary atherosclerosis with simultaneous normalization of SAE and thereby prevention in a wide number of patients with SS I-II F. CL development of myocardial infarction, cerebral stroke and thrombosis of different localization.
When ever medical complex consisting of lipid-lowering diet, individually tailored physical training, swimming and drug simvastatin, were not used in patients with SS I-II F. class. to normalize SAE.
The aim of the invention is to increase the efficiency of correction of violations SAE in patients with SS I-II F. class.
The essence of the proposed method lies in the fact that for the correction SAE patients with SS I-II F. CL glutelin is assigned a complex of lipid-lowering diet, dosed physical exercise, daily swimming for at least 30 min a day in the middle of the day and of the drug simvastatin 20 mg 1 time in the evening after a meal.
The method allows to correct SAE in patients with SS I-II F. cells within 2 months, translating it to a level close to that of healthy people. Subject to the subsequent recommendations of the proposed method can be maintained SAE, and therefore, the rheology of blood in an optimal state, which will significantly reduce the risk of thrombotic complications, reduce the number of cases of temporary disability, to accelerate and improve the quality of patient treatment, reduce disability, and also to prolong the life and reduce mortality of patients with SS I-II F. cells from a heart attack, stroke and thrombosis of different localization.
The inventive method is carried out as follows. Taking 9 ml of blood is produced in the morning after a 14-hour fast from Vienna through the thick needle by gravity into a test tube with sodium citrate in the ratio of 9:1 to assess the aggregation of erythrocytes.
Erythrocyte aggregation is assessed by the degree of ability of erythrocytes to spontaneously aggregate (Pokrova O.A., Grineva MR, Ivanov K.S. Methodology and clinical significance of the study the rheological properties of blood // Bulletin of the Ivanovo medical Academy. - 2008. - T13, No. 1-2. - s.89-98).
To assess agreg the tion of erythrocytes blood from a vein taken in sodium citrate in the ratio of 9:1 and centrifuged 10 min at 3000 rpm/min In 96-well pad fill 2 holes 0.2 ml plasma of the subject. From the tube removed all the plasma and the layer of leukocytes. Erythrocytes 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. The average unit size (CPA):
Sea - the sum of all cells in the aggregates
KA - the number of units
2. Parasitological (PA):
CTU - free red blood cells
3. The percentage of non-aggregated RBCs (PNA):
Normative values for CPA are 4-5; for 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 in patients with SS I-II F. CL should be treated according to the claimed method.
The inventive method is carried out as follows.
To reduce the level of lipids in blood of patients assigned patients lipid-lowering diet, the basic principles of which are set out in the table below.
|Featured products (1)||Products, whose consumption should be limited to (2)||The food products that are not recommended (3)|
|Bread||Wholemeal bread, cereals cereals, porridge, pasta, crisp bread, matzo, rice||Croissants, brioches|
|Products every day||Skim milk cheese with a very low fat content, for example: peasant cheese or quark, yoghurt with very low fat content, the white of an egg substitutes eggs||Semi-skimmed milk, cheeses with reduced fat content, for example: Brough, Camembert, Eden, Year, feta, yogurt with ricote, low fat, two whole eggs per week||Whole milk, evaporated milk, cream, milk substitutes, fatty cheeses and yogurt|
|Fish||White fish, oily fish(cooked in the grill, boiled, smoked). Not to eat the skin of the fish (skin sardines, Snetkov)||Fish fried in a suitable oil||Eggs, fish, fried on the unknown or unsuitable oil or fat|
|Sea-products||Oysters, scallops||Clams, lobster, shrimp||Shrimp, including serrate, squid|
|Meat||is ndaka, chicken, veal, venison, rabbit, lamb||Very lean beef, ham, bacon, lamb (one or 2 times a week). Veal, sausages, chicken, liver 2 times per month||Ducks, geese, all kinds of fatty meat, the usual sausages, salami, meat pies, bacon, leather birds|
|Fats||Polyunsaturated oils, such as: sunflower, corn, peanut, soybean; monounsaturated oils (olive, canola). Soft margarine, low fat, made on the basis of these oils||Butter, suet, lard, fat, palm oil, hard Margarines|
|Fruits and vegetables||All fresh and frozen vegetables, especially legumes: beans, dried beans, lentils, peas, corn, boiled potatoes or jacket potatoes; all fresh or dried fruit, canned unsweetened fruit||Fried potatoes, potato flakes, cooked in sunflower oil||Fried potatoes or potato flakes, vegetables or rice, fried on the unknown or unsuitable oil or fat fries, baked chips, pickles (konservirovannyy the vegetables)|
|Dessert||Sorbitol, jellies, puddings, based on skimmed milk, fruit salad, meringue||Ice cream, puddings, dumplings, sauces, prepared on the basis of cream or butter|
|Grocery||Cake, biscuits, cooked in margarine or oil, containing|
|Factory cake, biscuits, cakes, snacks and puddings|
|Pastry||Oriental sweets, nougat, candy||Marzipan, halva||Chocolate, candy sugar and butter, sweet coconut, candy of burnt sugar and butter|
|Nuts||Walnuts, almonds, chestnuts||Brazil nuts, peanuts, pistachios||Cashew, coconut, salted nuts|
|Drinks||Tea, ground and instant coffee, light diet drinks||Alcohol, liquid chocolate with low fat||Liquid chocolate, Irish coffee, solo the new drinks with a high content of fat, brewed coffee|
|Seasoning||Pepper, mustard, spices||Salad sauces with low fat||Douliana food, sauces for salads, mayonnaise for salads|
The second component of the proposed method is feasible regular physical exercise.
In real life you can implement the three forms of physical activity: 1) morning hygienic gymnastics (charging); 2) health care gymnastics; 3) fractional exercise during the day.
1. Morning hygienic gymnastics (charging).
Morning gymnastics should do after waking up to Breakfast in a ventilated room. Under the influence of training the body is released from the state of inhibition of the physiological processes taking place during sleep.
The sequence of the exercises involves the alternation of load on different muscle groups (arms, legs, body). Exercises are performed with gradually increasing excursion breathing, stretching, limited use of power conditions. Breathing exercise should be free, rhythmic, without delay, mainly through the nose; the exhalation should be longer than the inhale (breath in 2-3 sec, exhale 3-5).
When good samochustvie 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 SS I-II F. class. recommended treatment and preventive exercises. Depending on the initial fitness may apply at the beginning of the lightweight option, physical activity, and subsequently enhanced option.
2. Complexes of preventive and curative gymnastics for people with SS I-II F. class.
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'toole is Vishu.
Exercise 3. Standing, hands on his belt. Alternately shifting the weight of the body from one foot to the other with a small bending the legs at the knee joint without lifting the feet from the floor. Exercise done 10-16 times with the muscles of the legs.
Exercise 4. Standing, feet apart at shoulder width, hands on his belt. Bending the trunk forward, touch right hand to left toe. 4-6 times alternately. When straightened position - breath, when the tilt - exhale. To look ahead.
Exercise 5. Standing with arms along the body. At the same time to take straight arm and one leg to the side with alternating lead leg. 4-6 times in each direction in turn. A wave of the hands and feet, breathe freely, do not delay.
Exercise 6. Standing, feet apart, hands in front of chest with palms down. With a turn of the body to dissolve hand in hand with turning the palms up - breath. To return to the original position with a small tilting forward, exhale. 3-5 times in each direction in turn. Breathing to harmonize with the movement of hands and body. By the end of exhalation to engage the wall of the abdomen.
Exercise 7. Standing, hands free. The walk free - 1 min, then with high flexion of the hips - 10-20 movements with subsequent transition to a peaceful walk 1-2 minutes Breathing rhythmic, 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 the 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. 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 keep the Rav is Onesie. Run 4-6 times.
Exercise 16. Lying down, arms at sides, legs apart. A semi-circular motion right straight leg to the left with the rotation of the pelvis - exhale - return to the starting position and inhale. 3-5 times in each direction. Alternately left and right, with the greatest possible excursion movement of the leg, keeping the emphasis brushes the floor.
Exercise 17. Sitting on the floor; a) to stand on all fours; b) to move into position on his knees; hands up - breath, torso, and hands to take back - exhale. When the tilt pull the stomach. Repeat 4-6 times; d) to go into a standing position, and then in the supine position; (e) self-massage of the abdomen small polukrugom movements clockwise - 1-2 minutes Rest 2 min; W) quiet breathing; C) exercise the protrusion (calm) and retraction (active) abdominal wall. The retraction of the abdomen combined with exhale through the mouth. Repeat 4-6 times.
Exercise 18. Standing with arms bent. Energetic walking on the spot or area of high flexion of the hips and waving of hands - 20-30 steps. Breathing is not to delay.
Exercise 19. Sitting on a chair, legs apart, hands on the waist or rest against the edge of a chair. The circular motion of the pelvis with the retraction of the abdomen when moving the pelvis back. 4-6 times in each direction.
Exercise 20. Standing. A peaceful walk with the breath of the average depth of 2-3 minutes
When the source sufficient trained is whether incurred during the course of tolerance to physical activity, 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. 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 possibly the information 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 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 to spokojnu is walking with the breath of medium depth. 2-5 minutes
Exercise 15. Lying on the Mat. Simultaneous lifting of the body and legs on the exhale. 4-6 times. Arms and legs should be straight, to keep the balance.
Exercise 16. Lying on the Mat, the emphasis brushes the floor. Cross movement straight leg - scissors. 4-8 times. Breathing is not to delay.
Exercise 17. With a quick straightening of the legs to move into a sitting position, then to lie down. You can help stroke 4-6 times.
Exercise 18. Lying on your back, legs bent. Calm breathing 4-6 times.
Exercise 19. Lying on his back, hands diluted with emphasis brushes the floor. With the rotation of the pelvis to the left, bend the legs, rotate the pelvis with legs crossed to the right and stretch the legs. To repeat such a circular motion feet 3-6 times in each direction alternately. Hands not off the floor. Breathing is not to delay.
Exercise 20. Lying on your back, arms and legs separated. Alternate turns the body right and left laying one hand to the other. Feet are not slipping. When divorced hands - breath, turning exhale. Performed 3-6 times.
Exercise 21. Lying on your back, arms along the body: a) turn on your left side; b) to turn on the right side; C) switch to lying on his stomach; to kneel; d) to move in a standing position; (e) walking on the spot with high flexion of the hips and the movement of the hand - 20-30 steps; g) to sit on the Mat; C) lie on your back, calm yanie. The whole complex repeat 3-4 times.
Exercise 22. Standing. Walking the quiet breathing of the average depth of 1-2 minutes
Exercise 23. Standing, feet apart on the width of the foot, hands on waist. Circular motion of the pelvis, right and left 6-8 times. Breathing is not to delay.
Exercise 24. Standing with legs wide apart, hands in front of chest. Alternately bending the legs with the transfer to it of gravity of the body with stretching hand to toe of the bent leg. 4-6 times in each direction. The other leg is straight. When straightening - breath, when the tilt - exhale.
Exercise 25. Standing, feet apart at shoulder width, hands on waist. Circular head movements by 4-10 times in each direction.
Exercise 26. Standing, feet apart at shoulder width, hands on waist. Bend trunk to the right, pulling the left arm up-breath. Return to starting position - exhale. 4-6 times alternately.
Exercise 27. The same hands to the shoulders. Circular motion of the brushes with the maximum excursion in the shoulder joints, when breeding - breath during the mixing and retraction of the abdominal wall exhale. Breathing deep.
Exercise 28. Standing. A peaceful walk and breath the average depth. The reduction of the total load. 1-2 minutes
3. Fractional exercise during the day.
Depending on the real conditions of life in patients with SS I-II F. class. you can recommend various exemplary embodiments d is one exercise for improving physical (motor) activity during the day.
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.
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.
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
Walk the pedestrian varying length.
Physical work in different ways and with different duration depending on the conditions (cleaning, home services, cleaning, gardening work, and others).
The third component of the claimed method is a daily swim in the sea, the river or the pool for at least 30 minutes a day in the middle of the day.>
The fourth component of way of leveling advanced SAE in patients with SS I-II F. CL is the purpose of simvastatin 20 mg 1 time in the evening after a meal.
Example 1. Patient K., 45 years old, suffering from stable angina functional class I for 5 years, were examined during the follow up inspection regarding stable angina. The patient was taken to the blood in a plastic tube with subsequent study of the aggregation activity of erythrocytes (CPA=5,7, PA=1,69, PNA=65,6%), indicating that the increase of the AOC.
The patient was recommended lipid-lowering diet, dosed physical load, swimming in the pool at least 30 minutes a day in the middle of the day, simvastatin 20 mg 1 time in the evening after a meal.
After 1.5 months found that the patient SAE (CPA=4,9, PA=1,16, PNA=82.7 per cent) is normalized.
Example 2. Patient L., 66 years old, suffering from stable angina II functional class for 15 years, were examined during the follow up inspection regarding stable angina. The patient was taken to the blood in a plastic tube with subsequent study of the aggregation activity of erythrocytes (CPA=5,9, PA=1,99, PNA=40,0%), indicating a sharp increase in the SAE and the risk of thrombosis.
The patient was recommended lipid-lowering diet, measured static and dynamic physical activity daily swimming for at least 30 min a day in the middle of the day, simvastatin 20 mg 1 time in the evening after a meal.
After 2 months of treatment indicators aggregation of erythrocytes (CPA=4,6, PA=1,15, PNA=80,9%) normalized, indicating a normalization of the AOC of the patient.
The use of the proposed correction method SAE in Hematology and cardiology will help to avoid many of vascular complications in patients with SS I-II F. CL, 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 erythrocytes in stable angina voltage I-II functional class and hypertension, including use of lipid-lowering diet, measured static and dynamic physical loads, daily swimming for at least 30 minutes a day in the middle of the day and simvastatin 20 mg 1 time in the evening after meals for 2 months.
SUBSTANCE: there is described a new compound - 1-(β-phenylethyl)-4-amino-1,2,4-triazolium bromide exhibiting cardioprotective, anti-ischemic, antihypertensive, antioxidant, protein synthetic and energotropic action.
EFFECT: improved clinical effectiveness.
1 cl, 5 ex, 4 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed invention relates to compounds of formula IB , where radicals R1-R5 have values, given in invention formula. In range of claimed invention also described are pharmaceutical compositions, which include compounds of IB formula, and methods of application of such compounds and compositions for treatment of different malfunctions, mainly selected from immune response reactions.
EFFECT: compounds by claimed invention have inhibiting action with respect to proteinkinases and, in particular with respect to JAK-3, ROCK or Aurora kinases.
55 cl, 6 tbl, 4 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: there are described novel acylsulfonamide peri-substituted condensed bicyclic compounds of general formula (I), values of radicals are given in invention formula. Also described is pharmaceutical composition based on formula (I) compound.
EFFECT: compounds can be used for inhibition of prostaglandin E2 binding with receptor EP3.
30 cl, 371 ex, 4 tbl
SUBSTANCE: there are offered a pharmaceutical composition for prevention or treatment of cardiovascular disturbances, containing Amlodipine or its pharmaceutically acceptable salt and Losartan or its pharmaceutically acceptable salt wherein Amlodipine or its pharmaceutically acceptable salt and Losartan or its pharmaceutically acceptable salt are physically separated from each other, and a method for preparing thereof. The method includes the following stages: a) wet granulation and drying of mixed Amlodipine or its salts and pharmaceutically acceptable excipients to prepare a portion containing Amlodipine granules; and b) mixing of the portion containing Amlodipine granules prepared at the stage a) and pre-mixed Losartan or its salt and pharmaceutically acceptable excipients.
EFFECT: improved preventive and therapeutic effects in cardiovascular disturbances, better stability, solubility, absence of hygroscopicity in making the tablets.
12 cl, 5 dwg, 1 tbl, 15 ex
SUBSTANCE: invention relates to novel crystalline modifications of [6-methoxy-5-(2-methoxyphenoxy)-2-pyridin-4-ylpyrimidin-4-yl]amide-5-methylpyridine-2-sulfonic acid, which produces an endothelial antagonistic effect and is suitable for treating diseases associated with abnormal vascular tone and endothelial dysfunction, such as heart failure, pulmonary hypertension etc. The crystalline modification which is denoted modification B is characterised by a powder X-ray diffractogram with characteristic peaks expressed through the d-parametre value (interplanar distance) (Å) obtained on a conventional X-ray powder diffractometre using Cuka radiation: 10.7 (m), 9.4 (m), 8.6 (vs), 8.3 (m), 7.6 (m), 6.7 (m), 6.4 (m), 6.0 (m), 5.69 (m), 5.30 (m), 5.17 (m), 4.95 (vs), 4.76 (m), 4.56 (m), 4.43 (s), 4.13 (vs), 3.80 (s), 3.45 (s), 3.41 (s), 3.37 (s) and 3.03 (m). The invention also relates to crystalline pseudopolymorphous modifications of [6-methoxy-5-(2-methoxyphenoxy)-2-pyridin-4-ylpyrimidin-4-yl]amide-5-methylpyridine-2-sulfonic acid selected from: a) pseudopolymorphous modification, solvate with ethanol, denoted modification D; b) pseudopolymorphous modification, polysolvate with acetone, denoted modification E; c) pseudopolymorphous modification, solvate with tetrahyrofuran, denoted modification F; d) pseudopolymorphous modification, solvate with methanol, denoted modification G; e) pseudopolymorphous modification, solvate with isopropanol, denoted modification H; f) pseudopolymorphous modification, solvate with dichloromethane, denoted modification I; and g) pseudopolymorphous modification, solvate with 2-butanol, denoted modification J. The invention also relates to a method of obtaining crystalline modification B, a pharmaceutical composition and use.
EFFECT: wider field of use of the compounds.
8 cl, 9 dwg, 9 tbl, 12 ex
SUBSTANCE: invention refers to pharmacology. A solid pharmaceutical dispersion contains bazedoxifene acetate dispersed in a dispersant, and said dispersant contains polyvinylpyrrolidone, poloxamer, polyethylene glycol, or a mixture or copolymer of said substances. The invention refers also to the compositions containing said dispersion, to methods for making the solid pharmaceutical dispersion containing bazedoxifene acetate and the composition and a dosage form containing the solid pharmaceutical dispersion containing bazedoxifene acetate for treatment of a disease or a syndrome associated with oestrogen hunger or excess, a disease or a disorder associated with proliferation or pathological development of endometrial tissues, cholesterol reduction, bone loss inhibition and breast cancer treatment. Besides the invention covers the methods of treating mammals suffering a disease or a syndrome associated with oestrogen hunger or excess, or a disease or a disorder associated with proliferation or pathological development of endometrial tissues, or cholesterol reduction in a mammal, bone loss inhibition in a mammal or breast cancer treatment in a mammal, treatment of one or more vasomotor disorders in postmenopausal women, including the introduction of therapeutically effective amounts of the solid pharmaceutical dispersion, and also to the application of the solid pharmaceutical dispersion containing bazedoxifene acetate for preparing a drug for treatment of a disease or a syndrome associated with oestrogen hunger or excess, a disorder associated with proliferation or pathological development of endometrial tissues, cholesterol reduction, bone loss inhibition and breast cancer treatment.
EFFECT: invention provides higher clinical effectiveness.
38 cl, 6 tbl, 2 dwg, 4 ex
SUBSTANCE: invention refers to medicine, namely to cardiology and concerns normalising functional responsiveness of cardiovascular system (CVS) in stenocardia function classes I-II. That is ensured by estimating the condition of functional responsiveness of the CVS in psychoemotional load by recording systolic, diastolic, average dynamic pressure. These data are used to evaluate a functional responsiveness index (FRI) before and after load by formula: FRI=(BPav.dyn. × HR)/100 (standard units). The post-load FRI gain by more than 20 standard units requires the administration of lisinopril in a dose 20 mg a day in the morning and metoprolol in a dose 50 mg a day in the morning.
EFFECT: method provides normalising functional responsiveness of the cardiovascular system and higher psychoemotional load tolerance in the given group of patients within two-month therapeutic course.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to new compounds of formula I , where: R1, R2, R3 and R4 independently from each other mean hydrogen, F, CI, Br, I; R5 designates hydrogen, alkyl with 1, 2, 3, 4, 5 or 6 C atoms, or cycloalkyl with 3, 4, 5 or 6 C atoms; R6 designates hydrogen; R7 and R8 independently from each other mean hydrogen, W means CrH2r or CsH2S-2; and one or more CH2-groups in C2H2r and CsH2s-2 can be substituted with NR17, oxygen or S; R17 means hydrogen, alkyl with 1, 2, 3 or 4 C atoms; r means 1, 2, 3, 4, 5 or 6; s means 2, 3 or 4; X designates-with C(O)- or -S(O)2-; Z means -C(O)- or a bond; and also to their pharmaceutically acceptable salts and trifluoroacetates. The invention also concerns application of the compounds of formula I, and also to a pharmaceutical composition.
EFFECT: preparation of new biologically active compounds exhibiting NHE3 inhibiting activity.
16 cl, 64 ex, 1 tbl
SUBSTANCE: invention relates to medicine, namely to cardiology and can be used to predict degree of restenosis development in coronary stent. For this purpose rate of nitrogen-containing preparation metabolism is determined by introduction the preparation into the test. As test-preparation introduced is caffeine in dose 150-300 mg orally once. After 6 hours ratio of N-acetyl-derivative of the preparation to non-metabolised preparation in urine is determined. If value of said ratio equals 73 % and lower favourable outcome of stenting is predicted.
EFFECT: said procedure ensures increase of accuracy in predicting degree of risk of restenosis development in coronary stent.
SUBSTANCE: invention relates to medicine and can be used for treatment of vascular depression. For this purpose efficient amount of cholinesterase inhibitors is introduced.
EFFECT: in addition to improvement of cognitive and executive functions method ensures reduction of depression symptoms in patients with cerebrovascular disorders.
SUBSTANCE: invention relates to novel substituted tetracyclic derivatives of tetrahydropyran, pyrrolidine and tetrahydrothiophene of general formula (I), their pharmaceutically acceptable addition salts, their stereochemically isomeric forms, their N-oxide forms, in which all substitutes are defined in claim 1 of the formula of invention. These compounds have binding affinity to serotonin receptors, particularly 5-HT2A and 5-HT2C receptors, and to dopamine receptors particularly D2 dopamine receptors, and have norepiniphrine reuptake inhibition properties. The invention also relates to a pharmaceutical composition containing said compounds, method of preparing said composition and use of said compounds as medicinal agents, particularly for preventing and/or treating several psychiatric and neurological disorders.
EFFECT: new compounds have useful biological properties.
12 cl, 3 tbl, 49 ex
SUBSTANCE: invention describes a compound of formula I or its pharmaceutically acceptable salt , where R, R9, Z, X, Q and Y are defined in the formula of invention. The compounds are chemokine receptor 2 and chemokine receptor 5 antagonists and can be used as a medicinal agent for preventing, relieving or treating autoimmune or inflammatory diseases or conditions.
EFFECT: obtaining a formula (I) compound, a pharmaceutical composition based on the formula (I) compound, use of the compound in paragraph 1 to prepare a medicinal agent for treating an autoimmune or inflammatory disease or condition, as well as use of the compound in paragraph 1 to prepare a medicinal agent for treating HIV infection or AIDS.
11 cl, 181 ex
SUBSTANCE: invention relates to use of a therapeutic agent which is an α-amino-amide compound of formula (I):
, in which R is a phenyl ring which is optionally substituted with one or two substitutes independently selected from halogen, hydroxy, cyano, C1-C6-alkyl, C1-C6-alkoxy or trifluoromethyl; R1 is hydrogen or C1-C6-alkyl; R2 and R3 are independently selected from hydrogen, C1-C4-alkyl; R4 and R5 independently denote hydrogen, C1-C6-alkyl; X is O or S; Y and Z, taken together with X and a phenyl ring bonded to Y and X, form a 5-7-member saturated heterocycle containing O or S atoms, or Y and Z denote hydrogen; or its isomers, mixtures and pharmaceutically acceptable salts for preparing a medicinal agent for treating lower urinary tract disorders.
EFFECT: obtaining a pharmaceutical composition based on the said compounds.
8 cl, 6 ex
SUBSTANCE: invention refers to medicine and pharmaceutics and concerns an agent gastrointestinal stimulation, specifically for prevention or treatment of functional gastric distresses, appetite regulation etc., containing TIR agonist representing cyclamate or amide derivative of formula as an active agent, a based pharmaceutical composition or a foodstuff and a method for gastrointestinal stimulation.
EFFECT: present invention provides improved life quality of the patients.
27 cl, 7 dwg, 3 tbl, 6 ex
FIELD: chemistry; pharmaceutics.
SUBSTANCE: present invention relates to novel cyclohexane derivatives of formula (I) or their pharmaceutically acceptable salts having inhibitory effect on Na+-glucose cotranspoter (SGLT2), as well as to pharmaceutical compositions based on the said compounds and their use in preventing or treating diabetes, diabetic complications caused by hyperglycaemia or obesity. , where A is -O-; n is an equal to 0 or 1; R6 and R7 each independently represents a hydrogen atom or a C1-C6alkyl group, m is an integer selected from 1-3; Q is selected from Q1 - Q5, given in formula 2.
EFFECT: obtaining novel cyclohexane derivatives or their pharmaceutically acceptable salts and preparation of a pharmaceutical composition based on the said compounds.
15 cl, 19 dwg, 11 tbl, 86 ex
SUBSTANCE: method involves asymmetric reduction of (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethyleneamine, catalytic reduction of the obtained product at temperature ranging from 40 to 100°C and pH ranging from 3 to 9, propionylation of the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine, and then crystallisation from the reaction mixture.
EFFECT: obtaining optically active amine derivatives of high purity with high output and prevention of formation of by-products.
6 cl, 1 tbl, 3 ex
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
SUBSTANCE: carboxylic acid compounds are presented by formula (I) where R1 represents (1) hydrogen atom, (2) C1-4alkyl; E represents -CO-; R2 represents (1) halogen atom, (2) C1-6 alkyl, (3) trihalogen methyl; R3 represents (1) halogen atom, (2) C1-6alkyl; R4 represents (1) hydrogen atom; R5 represents (1) C1-6alkyl; represents phenyl; G represents (1) C1-6alkylene; represents 9-12-merous bicyclic heterocycle containing heteroatoms, chosen of 1-4 nitrogen atoms, one or two oxygen atoms; m represents 0 or an integer 1 to 4, n represents 0 or an integer 1 to 4, and i represents 0 or an integer 1 to 11 where R2 can be identical or different provided m is equal to 2 or more, R3 can be identical or different provided n is equal to 2 or more, and R5 can be identical or different provided i is equal to 2 or more; both R12 and R13, independently represent (1) C1-4alkyl, (2) halogen atom, (3) hydroxyl or (4) hydrogen atom, or R12 and R13 together represent (1) oxo or (2) C2-5alkylene and where provided R12 and R13 simultaneously represent hydrogen atom, carboxylic acid compound presented by formula (I), represents a compound chosen from the group including the compounds (1) - (32), listed in cl.1 of the patent claim. Besides the invention concerns a pharmaceutical composition based in the compound of formula I and to application of the compound of formula I for making the pharmaceutical composition.
EFFECT: there are produced new carboxylic acid derivatives with antagonistic activity with respect to DP receptor.
14 cl, 74 ex
SUBSTANCE: invention relates to new benzofuran derivatives of formula II or their pharmaceutically acceptable salts, where R1 is H or C1-C10 alkyl; R2 is H or C1-C10 alkyl; n ranges from 0 to 4; p ranges from 0 to 1; R3 and R4 represent H, as well as to pharmaceutical compositions based on said derivatives and methods of treating cardiac arrhythmia using these compositions.
EFFECT: increased effectiveness of composition and method of treatment.
15 cl, 12 dwg, 3 ex
SUBSTANCE: invention concerns medicine, namely haematology, cardiology and endocrinology, and covers correction of blood microvesicle level in arterial hypertension, dyslipidemia and impaired glucose tolerance. It is ensured by complex treatment that involves introduction of fozinopril in a dose 10 mg once a day in the morning, pioglitazone in a dose 30 mg once a day in the morning, simvastatin in a dose 40 mg in the evening in combination with graduated physical activities for therapeutic course at least 6 weeks.
EFFECT: invention provides complete normalisation of blood microvesicle level ensured by potentiation of therapeutic effect of certain components of the complex therapy; that in turn allows reducing risk of thrombotic in the given group of patients.
SUBSTANCE: invention belongs to medicine, notably to physiotherapy, surgery. Method includes course of mechanical pneumocompression on lower extremities before operation. The course of treatment takes 5 sessions. Sinusoidal moderated current therapy starts from the first post-operational day. Electrodes are applied paravertebrally. The course of treatment takes 10 sessions.
EFFECT: method prevents postoperative edema and lymphorrhea from wounds in operated extremity due to speed and volume of lymphatic flow enlargement, reduces pain syndrome intensiveness.