Method of decrease of blood plates activity at methabolic syndrome

FIELD: medicine; haematology.

SUBSTANCE: for 24 weeks they use individually selected low-caloric diet calculated in kcal at the formula: for women of 18-30 years old (0.0621 × body weight, kg + 2.0357) × 240. 31 - 60 years old (0.0342 × body weight, kg + 3.5377) × 240, older than 60 years old (0.0377 × body weight, kg + 2.7545) × 240, for men 18-30 years old (0.0630 × body weight, kg + 2.8957) × 240, 31 - 60 years old (0.0484 × body weight, kg + 3.6534) × 240, older than 60 years old (0.0491 × body weight, kg + 2.4587) × 240. Additionally Eprosartan 800 mg once a day and Preductal MB 35 mg twice a day are administered. The method provides potentiation of the diet complex effect and particular drugs from the selected pharmacological groups at empirically specified duration of treatment and as a consequence normalising of thrombocyte hemostasis and decrease of risk of thrombotic complications.

EFFECT: decrease of blood plates activity at methabolic syndrome.

1 ex

 

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

The closest analogue to the proposed method of correction of platelet aggregation in patients with metabolic syndrome (MS) may be the method described in EN 2268041 C1, 20.01.2006, including the appointment of individualized low-calorie diet and a beta-blocker nebivolol 1 time per day, which provides effective correction of disorders of platelet aggregation in the 6-month course of treatment.

Distinctive features of the proposed method from known are: use instead of nebivolol combination of two drugs: eprosartan 800 mg 1 time per day and Preductal MB 35 mg 2 times a day. It should be noted that nebivolol used in the prototype can be applied not every patient with metabolic syndrome due to the individual characteristics of the drug. In addition, a large proportion of patients with metabolic syndrome shows the use of blockers angiotensin receptor without impairing lipid and carbohydrate metabolisms. In this category of patients with a high risk of developing heart attacks, justified the use of cardioprotective drug Preductal MB. In this regard, the task was to develop a more massively used a method of reducing the activity of the centre is acetow in the metabolic syndrome using widely prescribed for patients with metabolic syndrome blocker angiotensin receptor as antihypertensives and cardioprotector Preductal MB.

When ever medical complex, consisting of individually low-calorie diet and drugs eprosartan and Preductal MB, was not used in patients with metabolic syndrome to normalize platelet hemostasis (adhesive function of blood platelets, platelet aggregation with ADP, collagen, thrombin, ristomycin, hydrogen peroxide, epinephrine -, and combinations of inductors - ADP+epinephrine, ADP+collagen, adrenaline+collagen, as well as optimization of intravascular platelet activity, level of lipid peroxidation and antioxidant protection of blood platelets).

The aim of the invention is to increase the efficiency of correction of disorders of platelet aggregation in patients with metabolic syndrome.

The essence of the proposed method lies in the fact that for the correction of platelet aggregation in patients with metabolic syndrome permanently assigned individually selected low-calorie diet, drugs eprosartan 800 mg 1 time per day and Preductal MB 35 mg 2 times a day.

The method allows to adjust the primary hemostasis in patients with MS within six months, putting it on a level close to that of healthy people. Subject to the subsequent recommendations of the proposed method can be maintained primary hemostasis optimally in the mode of operation, that 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 MS from a 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 individually for each patient with MS is calculated in kcal by the formula:

for women 18-30 years (0,0621 × body mass, kg +2,0357)×240,

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

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

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

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

over 60 formed (0,0491 × body mass, 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 MS, the level of physical activity low).

It is recommended that 3 main meals and 2 intermediate. With regular skipping one meal significantly increases the frequency times the development of obesity, there was also 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 g guidelines 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 - the purpose of eprosartan 800 mg 1 time per day and Preductal MB 35 mg 2 times a day.

Example. Patient K., 47 years old, with body weight 82,0 kg, BMI of 29.5 kg/m2suffering from metabolic syndrome for 12 years when the survey was identified thrombocytopathies with increasing adhesive - 45%, aggregation activity (ADP - 26 North, with collagen - 29 S., thrombin - 43 S., ristomycin-25 C., with N2About2- 32 S., adrenaline 70 C., with ADP+adrenaline 21 S., ADP+collagen 22 S., adrenaline+collagen - 19th C.) and high intravascular platelet activity (discocyte - 61%, disco echinocyte - 22%, ferocity - 14,0%, sphere-echinocyte - 3,0%, biopolar form is 0%, the amount of active forms of 39%, the number of platelet aggregates - 14.0 percent, the number of small units - 17.0 per 100 loose platelets, the number of medium and large units - 11,0 100 free is easy platelets) if the sensitivity of patient platelets to aggregation inducers: when a stand-alone application of the minimum necessary concentration of inducers was for ADP 9,1× 10-6M, for adrenaline 8,2×10-7M, for collagen 1:2,8 cultivation of the main suspension for thrombin 0,114 IU/ml, with a dual combination of inductors for ADP 7,1×10-8M, for adrenaline 5,0×10-9M, for collagen 1:7 dilution of the primary suspension for thrombin 0,080 IU/ml

The patient was observed impaired glucose tolerance and hyperlipidemia II b type (total lipids of 9.2 g/l) with mild hypercholesterolemia (total cholesterol - 5.8 mmol/l). The level of acylhydrazines platelets was 3,9 D233/109platelet malondialdehyde (MDA) platelet - 1,61 nmol/109platelets in catalase activity of platelet - 3300,0 IU/109platelets and the activities of superoxide dismutase platelets of 850.0 IU/109platelet count.

The patient was assigned individually selected low-calorie diet (1974,9 kcal), eprosartan 800 mg 1 time per day and Preductal MB 35 mg 2 times a day. The patient was examined every week after starting treatment. Simultaneously with the inspection was carried out biochemical and hematological analysis of blood.

As a result of treatment, the patient to 5.5 months were normalized sensitivity of platelets to aggregation inducers: when a stand-alone application of the minimum concentration of inducer was for ADP 5,0×10-4M, for adrenaline 5,0×10-6M for collagen 1:2 dilution of the primary suspension, for thrombin with 0.125 IU/ml, with a dual combination of inductors for ADP 10-6M, for adrenaline 2,5×10-7M, for collagen 1:4 dilution of the primary suspension for thrombin 0,100 IU/ml

To week 24 of treatment, the patient had normal body weight (70,0 kg) and body mass index of 25.2 kg/m2), was achieved full normalization of lipid profile (total lipids of 5.2 g/l, total cholesterol - 4.7 mmol/l), test glucose tolerance, the adhesive functions of blood platelets in 35%, platelet aggregation with ADP-47 C., the collagen-35 S., thrombin-59 S., ristomycin-43 C., hydrogen peroxide-54 S., adrenaline - 98 C. and combinations of inductors - ADP+adrenaline-33s., ADP+collagen-23 S., adrenaline+collagen-25 C., and optimization of intravascular platelet activity (discocyte - 88,0%, disco echinocyte - 7,8%, ferocity - 2,3%, sphere-echinocyte - 1,6%, biopolar forms of 0.3%, the amount of active forms is 12%, the number of platelets in aggregates of 5.0%, the number of small units - 5.0 per 100 loose platelets, the number of medium and large units is 0.5 to 100 loose platelets) during normal sensitivity of platelets to the inductors, the normal level of peroxide oxidation of lipids (level acylhydrazines platelets was 2.0 D233/109platelet MDA platelets of 0.62 nmol/109platelets) and antioxidant protection of blood pressure as the s records (catalase platelets 9700,0 IU/109platelets, platelet superoxide dismutase - 1520,0 IU/109platelets). The patient is asked to comply with these recommendations in future.

The use of the proposed method of correction of platelet disorders in Hematology, cardiology and endocrinology will help to avoid many of vascular complications in patients with metabolic syndrome, to reduce their number of cases of temporary disability, to reduce the duration of hospitalization, reduce morbidity and mortality.

A method of reducing activity of blood platelets in the metabolic syndrome, including the use of individualized low-calorie diet, calculated in kcal by the formula

for women 18-30 years (0,0621 · body mass, kg +2,0357)·240;

31 - 60 years (0,0342 · body mass, kg +3,5377)·240;

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

for men 18-30 years (0,0630 · body mass, kg +2,8957)·240;

31 - 60 years (0,0484 · body mass, kg +3,6534)·240;

over 60 years of age (0,0491 · body mass, kg +2,4587)·240,

eprosartan 800 mg 1 time per day and Preductal MB 35 mg 2 times a day for 24 weeks.



 

Same patents:

FIELD: medicine, haematology.

SUBSTANCE: patient with metabolic syndrome is prescribed with individual low-calorie diet calculated in kcal by formula: for women aged 18-30 years old - (0.0621 × body weight, kg + 2.0357) × 240; aged 31-60 years old - (0.0342 × body weight, kg + 3.5377) × 240; over 60 years old (0.0377 × body weight, kg + 2.7545) × 240; for men aged 18-30 years old - (0.0630 × body weight, kg + 2.8957) × 240; aged 31-60 years old - (0.0484 × body weight, kg + 3.6534) × 240; over 60 years old (0.0491 × body weight, kg + 2.4587) × 240. Diet effect is combined with introduction of Zofenopril dosed 60 mg in the morning. Therapy length is 6 months.

EFFECT: method provides potentiated complex effect of diet and specified medicine with fitted therapy length; normalisation of platelet haemostasis and lowered risk of platelet complications.

1 ex

FIELD: medicine, hematology.

SUBSTANCE: individually selected low-calorie diet is administered, combined with reasonably graduated static and dynamic exercise. Concurrently, preparations are administered as follows: 500 mg methformin twice a day after meal, 30 mg zophenopril every morning, 35 mg preductal MB by 1 pill twice a day, and duovit 1 red pill + 1 blue pill every day. Course of treatment is continued for 6 months. The method provides complex effect potentiation of the diet and of particular preparations from selected pharmacological groups during empirically determined treatment period.

EFFECT: normalisation of platelet hemostasis, lowering risk of thrombosis complications.

1 ex

FIELD: medicine, hematology.

SUBSTANCE: method consists in long-term complex administration of low-calorie diet, 200 mg of labetalole twice a day, and 2 mg of lacidipine every morning, to correct platelet hemostasis in metabolic syndrome patients. The method allows primary hemostasis normalisation in metabolic syndrome patients during 2 months, due to ADP and ATP levels normalisation, as well as actin and myosin level and assemblage normalisation in platelets.

EFFECT: primary hemostasis normalisation in metabolic syndrome patients.

1 ex

Carbonyl compounds // 2337099

FIELD: chemistry, pharmacology.

SUBSTANCE: claimed invention relates to novel compounds of general formula(I) , where D represents phenyl, pyridyl or tienyl, each of which is single-substituted or double-substituted with Hal; R1 represents H, =O, COOR3, OH, OA, NH2, alkyl, which has 1, 2, 3, 4, 5 or 6 carbon atoms, N3, ethinyl, vinyl, allyloxy, -OCOR3, NHCOA or NHSO2A; R2 represents H, =O, OH, OA or alkyl, which has 1, 2, 3, 4, 5 or 6 carbon atoms; R1 and R2 together alternatively represent spirocyclically linked 3-6-member carbocyclic ring, R3 represents H or A, R4 represents H or A; represents pyrrolidine-1,2-diyl, piperidine-1,2-diyl, oxazolidine-3,4 or 3,5-diyl, thiazolidine-3,4-diyl, 2,5-dihydro-1H-pyrrol-1,5-diyl, 1,3-dioxolane-4,5-diyl; G represents (CH2)n or (CH2)nNH-; X represents CONH; Y represents 1,3- or 1,4-phenylene, which is not substituted or is single-substituted with methyl, trifluoromethyl, ethyl, propyl, Cl or F; T represents morpholine-4-yl, which is single-substituted or double-substituted with carbonyl oxygen; A represents non-branched or branched alkyl, which has 1-10 carbon atoms and in which 1-7 hydrogen atoms can be substituted with F; Hal represents F, CI, Br or I, n represents 0, 1 or 2; and their pharmaceutically acceptable derivatives, solvates, salts or sterioisomers, including their mixtures in all ratios. Invention also relates to method of obtaining formula I compounds, to medication based on formula I compound and application of formula I compounds for preparation of medication, which has inhibiting activity with respect to coagulation factors Xa and VIla.

EFFECT: obtained novel compounds have inhibiting activity with respect to said coagulation factors.

11 cl, 1 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: invention concerns new anticoagulant compounds of the formula (I): and their pharmaceutically acceptable salts, where R is C1-C8 alkyl substituted by at least one halogen. Invention also concerns pharmaceutical compositions containing compounds of the formula I and its salts, as well as application methods for the compounds, salts and compositions, and methods of coagulability disorder treatment (I).

EFFECT: increased efficiency of preparations.

21 cl, 14 dwg, 2 tbl, 11 ex

FIELD: chemistry.

SUBSTANCE: invention concerns new compounds of the formula I , where A is S(O)2 or C1-6alkylene possibly substituted by one or more fluorine atoms; R1 is (a) C1-10alkyl possibly substituted by one or more substitutes of aryl and Het1, (b) aryl possibly substituted by one or two substitutes selected out of halogeno, C1-4alkyl, CF3 and C1-4alkoxy, or (c) Het3; R2a, R2b, R3a and R3b are independently H or C1-3alkyl; R4 is (a) H, (b) C1-6alkyl; R5 and R6 are independently H, F or methyl; G is (a) -C(O)N(R8a)-[CH(C(O)R9)]0-1-C0-3alkylene-(Q1)a-, (b) -C(O)N(R8b)-C2-3alkenylene-(Q1)a-, R9 is H; Q1 is O; a is 0 or 1; L is (a) C0-6alkylene-Ra, (b) or , (c) ; Ar is phenyl or naphthyl; Het is 5-10-member heterocyclic group including one or two rings and one sulfur or oxygen and/or nitrogen atom as heteroatom; R11a is H or one or more substitute selected out of halogeno, OH, CN, C1-6alkyl and C1-6alkoxy (the last two groups are possibly substituted by one or more substitutes selected out of halogeno, OH, C1-4alkoxy); R11c is independently H or one or more substitute selected out of halogeno, OH, CN, C1-6alkyl, C1-6alkoxy; Ra, Rb and Rd are independently (a) , (b) , (c) , or (d) or Rb and Rd also can be H; Q3 is O; Q4 is O or CH2; a is 0 or 1; R13a-R13b are independently (a) H, (b) C(O)OR16; R16 is C1-10alkyl; R8a-R8b and R14a-R14d are independently (a) H or (b) C1-4alkyl (the last group is possibly substituted by one or more substitutes selected out of halogeno and OH), or R14a and R14b are independently C(O)O-C1-6alkyl, or R14c is (a) C3-7cycloalkyl, (b) C(O)O-C1-6alkyl, or R14c and R14d together are C3-6n-alkylene possibly interrupted by O, S, N(H) or N(C1-4alkyl) and/or substituted by one or more C1-4alkyl groups; each aryl is independently C6-10carbocyclic aromatic group which can contain one or two rings and be possibly substituted by one or more substitutes selected out of (a) halogeno, (b) C1-10alkyl, (c) OR17a, R17a is (a) H, (b) C1-10alkyl; Het1 and Het3 are independently 4-9-member heterocyclic groups including one or more heteroatom selected out of oxygen, nitrogen and/or sulfur, so that heterocyclic groups can contain one, two or three rings and be possibly substituted by one or more substitutes selected out of (a) halogeno, (b) C1-10alkyl, (c) =O, (d) OR19a, R19a is (a) H, (b) C1-10alkyl; n, p and q are independently 0, 1 or 2; or its pharmaceutically acceptable salts. Invention also concerns pharmaceutical composition; application; treatment method; method of obtaining compounds of the formula I; and compounds of the formula II, IV, V, VI.

EFFECT: new biologically active compounds with thrombin inhibition effect.

12 cl, 11 ex

FIELD: medicine, pharmacology.

SUBSTANCE: invention relates to method of thrombocyte aggregation inhibition. Method consists in that therapeutically efficient amount of valsartan metabolite, valeryl-4-hydroxyvalsartan, is introduced to patient who needs it. Invention also relates to pharmaceutical composition including valeryl-4-hydroxyvalsartan, and to its application for prevention, slowing-down development or treatment of disease and disorder mediated by thrombocyte aggregation.

EFFECT: reduction of thrombocyte ability to aggregate.

3 cl, 4 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns medicine, particularly cardiology and endocrinology. The method involves prescription of individual hypocaloric diet and administration of 50 mg of Losartane medication once in the morning for at least 24 weeks. In comparison to other angiotensin receptor antagonist medications, administration of Losartane in the said dosage allows total normalisation of thrombocyte homeostasis in patients with metabolic syndrome by elimination of thrombocyte aggregation, adhesion and intravascular activity disorders.

EFFECT: possibility of total normalisation of thrombocyte homeostasis in patients with metabolic syndrome.

1 ex

FIELD: medicine.

SUBSTANCE: invention concerns medicine, particularly cardiology and endocrinology. The method involves prescription of individual hypocaloric diet and administration of 4 mg of Trandolapril medication once in the morning for at least 24 weeks. In comparison to other ACE inhibitor medications, administration of Trandolapril in the said dosage allows total thrombocyte homeostasis normalisation for patients with metabolic syndrome by elimination of thrombocyte aggregation, adhesion and intravascular activity disorders.

EFFECT: possibility of total thrombocyte homeostasis normalisation in patients with metabolic syndrome.

1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the agent strongly inhibiting thrombocyte aggregation, it doesn't inhibit COX-1 or COX-2. The invention offers the compounds of formula (I) or their pharmaceutically acceptable salts, where residuals and groups in the specified structure of the compounds have the values denoted in the formula of the invention. The pharmaceuticals containing any of the compounds of formula (I) or their pharmaceutically acceptable salts, and phylactic and/or therapeutic agents for coronary heart disease, which contain any of the compounds of formula (I) or their pharmaceutically acceptable salts are suggested. Moreover, application of the compounds and their pharmaceutically acceptable salts for preparation of the medicine having anti-thrombotic potency, and method of the treatment of coronary heart disease are suggested.

EFFECT: production of the medicines having anti-thrombotic potency on basis of pyrazole.

12 cl, 1 tbl, 171 ex

FIELD: medicine, haematology.

SUBSTANCE: patient with metabolic syndrome is prescribed with individual low-calorie diet calculated in kcal by formula: for women aged 18-30 years old - (0.0621 × body weight, kg + 2.0357) × 240; aged 31-60 years old - (0.0342 × body weight, kg + 3.5377) × 240; over 60 years old (0.0377 × body weight, kg + 2.7545) × 240; for men aged 18-30 years old - (0.0630 × body weight, kg + 2.8957) × 240; aged 31-60 years old - (0.0484 × body weight, kg + 3.6534) × 240; over 60 years old (0.0491 × body weight, kg + 2.4587) × 240. Diet effect is combined with introduction of Zofenopril dosed 60 mg in the morning. Therapy length is 6 months.

EFFECT: method provides potentiated complex effect of diet and specified medicine with fitted therapy length; normalisation of platelet haemostasis and lowered risk of platelet complications.

1 ex

FIELD: medicine, hematology.

SUBSTANCE: individually selected low-calorie diet is administered, combined with reasonably graduated static and dynamic exercise. Concurrently, preparations are administered as follows: 500 mg methformin twice a day after meal, 30 mg zophenopril every morning, 35 mg preductal MB by 1 pill twice a day, and duovit 1 red pill + 1 blue pill every day. Course of treatment is continued for 6 months. The method provides complex effect potentiation of the diet and of particular preparations from selected pharmacological groups during empirically determined treatment period.

EFFECT: normalisation of platelet hemostasis, lowering risk of thrombosis complications.

1 ex

FIELD: medicine; cardiology.

SUBSTANCE: scheme of examination and treatment of patients with a metabolic syndrome (MS) consists in the following. In the presence of AG with average degree of cardiovascular risk in a combination to visceral adiposity and: overweight<27 kg/m2, during 3-6 month prescribe non-medicament actions referred on treatment of adiposity, at achievement of AD target level after the specified term, non-medicament actions continue; with overweigth≥27 kg/m2 or combination of overweigth≥27 kg/m2 and hyperglycemias on an empty stomach, during 3-6 month, prescribe Orlistat and-or Metforminum, at achievement after the specified term of target level of a AD, continue the therapy; with combination overweigth≥27 kg/m2, hyperglycemias on an empty stomach and glucose tolerance during 3-6 month, prescribe acarbose or Orlistat and acarbose in a combination with Metforminum, at achievement after the specified term of target AD level, continue the therapy; in combination of overweight≥27 kg/m2, hyperglycemias on an empty stomach, glucose intolerance and lipidemia during 3-6 month, prescribe Orlistat in a combination with Metforminum or acarbose, at achievement of AD target level after the specified term, continue the therapy. In the presence of AG with high degree of cardiovascular risk in combination with visceral adiposity and: overweight<27 kg/m, prescribe non-medicament actions referred on treatment of obesity, and the antihypertensive combined therapy; overweight≥27 or combination of overweight≥27 kg/m2 and hyperglycemias on an empty stomach, prescribe Orlistat and-or Metforminum, and the antihypertensive combined therapy; with overweight≥27 kg/m2, hyperglycemias on an empty stomach and glucose intolerance, prescribe the antihypertensive combined therapy in a combination with acarbose or Orlistat and acarbose together with Metforminum; with overweight≥27 kg/m2, hyperglycemias on an empty stomach, glucose intolerance and lipidemia, prescribe the antihypertensive combined therapy in combination with Orlistat and Metforminum or acarbose; with lipidemia, glucose intolerance, prescribe the antihypertensive combined therapy in a combination with Orlistat or acarbose; SD 2, and also lipidemia, glucose intolerance, a plasma glucose on an empty stomach < 6,0 mmol/l, prescribe the antihypertensive combined therapy in a combination with orlistate or akarbose; SD 2, and also a lipidemia broken by tolerance to a glucose, plasmatic glucose on an empty stomach > 6,0 mmol/l, prescribe the antihypertensive combined therapy in a combination with preparations decreasing amount of sugar in blood. Affecting only on one of the MS components, it is possible to achieve appreciable improvement due to indemnification of changes in other links of its pathogenesis.

EFFECT: use of the offered algorithms of treatment of patients with a metabolic syndrome will allow optimising their treatment.

12 cl, 2 tbl, 2 ex

FIELD: chemistry, pharmacology.

SUBSTANCE: compound of formula [I]: is described, where the ring A represents halogen substituted benzene ring; the ring B represents benzene ring substituted with two lower, 1 to 4 carbon atoms, alcoxy-groups; the ring C represents benzene ring or five-member aromatic heterocyclic ring, that may be optionally substituted with substitute as follows: carboxyl group, C1-4-alkyl group, C2-7-alkanoiloxy-C1-6-alkyl group, phenyl-C1-4-alkyl group, phenyl group, optionally substituted with carboxyl group, or oxo-group; R1 represents C1-6-alkyl group, optionally substituted with hydroxyl group, that optionally substituted with C2-20-alkanoil or C1-7-alkyl group; X1a represents bound or C1-6-alkylen, optionally substituted with hydroxyl or oxo-group; X1b represents bound or C1-6-alkylen, optionally substituted with hydroxyl or oxo-group; X2 represents bound, -O- or -S- ; X3 represents bound or group, formed by one hydrogen atom elimination from either straight or branched chain C1-7-alkyl, or C2-6-alkenyl group, that optionally substituted with hydroxyl or oxo-group; and Y represents optionally etherified carboxyl group; or its salt. Benzoxazepin derivatives production method, medicine based on them, and their application are also described.

EFFECT: novel compounds have high lipids-decreasing effect and are helpful as hyperlipidemia prevention and treatment medicine.

20 cl, 168 ex

FIELD: chemistry, pharmacology.

SUBSTANCE: compound of formula [I]: is described, where the ring A represents halogen substituted benzene ring; the ring B represents benzene ring substituted with two lower, 1 to 4 carbon atoms, alcoxy-groups; the ring C represents benzene ring or five-member aromatic heterocyclic ring, that may be optionally substituted with substitute as follows: carboxyl group, C1-4-alkyl group, C2-7-alkanoiloxy-C1-6-alkyl group, phenyl-C1-4-alkyl group, phenyl group, optionally substituted with carboxyl group, or oxo-group; R1 represents C1-6-alkyl group, optionally substituted with hydroxyl group, that optionally substituted with C2-20-alkanoil or C1-7-alkyl group; X1a represents bound or C1-6-alkylen, optionally substituted with hydroxyl or oxo-group; X1b represents bound or C1-6-alkylen, optionally substituted with hydroxyl or oxo-group; X2 represents bound, -O- or -S- ; X3 represents bound or group, formed by one hydrogen atom elimination from either straight or branched chain C1-7-alkyl, or C2-6-alkenyl group, that optionally substituted with hydroxyl or oxo-group; and Y represents optionally etherified carboxyl group; or its salt. Benzoxazepin derivatives production method, medicine based on them, and their application are also described.

EFFECT: novel compounds have high lipids-decreasing effect and are helpful as hyperlipidemia prevention and treatment medicine.

20 cl, 168 ex

FIELD: medicine.

SUBSTANCE: invention concerns biopharmacology and medicine area. The antitumor agent representing a immunoliposome biological structure, including a liposome containing the therapeutic agent, sewed with a vector of peptide nature, thus for treatment of CNS tumors is declared, the liposome contains the therapeutic agent in a water phase, as a vector contains monoclonal antibodies to CD34+, and a linking represents 2-iminotiolan (IT) in 0.1% concentration. As a therapeutic agent, immunoliposome contains the substance chosen from the group: Daunomycin, Carminomycinum, Melphtalan, Methotrexatum, Cytarabinum, Doxorubicinum, Ricine. The method of obtaining of an antitumoral agent and way of inhibition of a tumor of the brain, consisting in agent administering due to item 1 in a pharmaceutically suitable carrier in effective quantity is declared also. Thus preliminary administer parenterally a preparation of hematological stem cells CD34+.

EFFECT: provision of highly effective delivery of an antitumor agent to a CNS tumor.

4 cl, 7 ex, 4 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns medicine. A soft drink on the basis of herbs consists of the concentrated vegetative extract obtained from an admixture of herbs, chosen of Sida sps., Boerhaavia diffusa, Vitis vinifera, Tinospora cordifolia and Withania somnifera, along with green palm sugar, the agent causing a fermentation, and carbonised water, in which proportion Sida sps.: Boerhaavia diffusa: Vitis vinifera: Tinospora cordifolia: Withania somnifera in a powdery admixture makes (15-20 : (5-10 : (15-20 : (5-10 : (5-10); Proportion of wt/wt: green palm sugar: the concentrated vegetative extract makes from 1 : 3 to 1 : 4; wt/wt, a proportion of carbonised water: the admixture of the concentrated vegetative extract, green palm sugar and the agent causing a fermentation, makes from 1 : 3 to 1 : 5. Perform: (a) obtaining of parts of Sida sps., Boerhaavia diffusa, Vitis vinifera, Tinospora cordifolia and Withania somnifera; (b) crushing of parts of plants and their mixing with obtaining of a powdery admixture; (c) water addition to a powdery admixture from a stage (b) for obtaining of a water extract; (d) concentration of a water extract from the stage (c); (e) filtration of the concentrated extract from the stage (d); (f) admixture of green palm sugar to the filtered extract from the stage (e); (g) addition of Sacromyces strain and the agent causing fermentation, to the admixture from the stage (f); (h) fermentation of the admixture from the stage (g) during the period of time from 3 till 6 days; (i) filtration of the fermented admixture from the stage (h); (j) concentration of the fermented filtrate from the stage (i) with obtaining of the basic solution and (k) mixing of the basic solution (j) with the carbonised water in wt/wt proportion from 1 : 3 to 1 : 5 with obtaining of a soft drink on the basis of herbs.

EFFECT: creation of a soft drink on the basis of herbs.

11 cl, 5 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns medicine. A soft drink on the basis of herbs consists of the concentrated vegetative extract obtained from an admixture of herbs, chosen of Sida sps., Boerhaavia diffusa, Vitis vinifera, Tinospora cordifolia and Withania somnifera, along with green palm sugar, the agent causing a fermentation, and carbonised water, in which proportion Sida sps.: Boerhaavia diffusa: Vitis vinifera: Tinospora cordifolia: Withania somnifera in a powdery admixture makes (15-20 : (5-10 : (15-20 : (5-10 : (5-10); Proportion of wt/wt: green palm sugar: the concentrated vegetative extract makes from 1 : 3 to 1 : 4; wt/wt, a proportion of carbonised water: the admixture of the concentrated vegetative extract, green palm sugar and the agent causing a fermentation, makes from 1 : 3 to 1 : 5. Perform: (a) obtaining of parts of Sida sps., Boerhaavia diffusa, Vitis vinifera, Tinospora cordifolia and Withania somnifera; (b) crushing of parts of plants and their mixing with obtaining of a powdery admixture; (c) water addition to a powdery admixture from a stage (b) for obtaining of a water extract; (d) concentration of a water extract from the stage (c); (e) filtration of the concentrated extract from the stage (d); (f) admixture of green palm sugar to the filtered extract from the stage (e); (g) addition of Sacromyces strain and the agent causing fermentation, to the admixture from the stage (f); (h) fermentation of the admixture from the stage (g) during the period of time from 3 till 6 days; (i) filtration of the fermented admixture from the stage (h); (j) concentration of the fermented filtrate from the stage (i) with obtaining of the basic solution and (k) mixing of the basic solution (j) with the carbonised water in wt/wt proportion from 1 : 3 to 1 : 5 with obtaining of a soft drink on the basis of herbs.

EFFECT: creation of a soft drink on the basis of herbs.

11 cl, 5 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns the pharmaceutical, food and cosmetic industry. Perform extraction of the raw material crushed with water with obtaining of a water extract and pulp. The pulp, obtained after extraction of raw materials by the water, is extracted in two steps with ethyl alcohol. At the first step of extraction the constrictor is extracted within 4-6 hours using the following proportion: ethyl alcohol 1:(5-7) with concentration of alcohol of 30% either 50%, or 70%, at temperature of 60-75°C, obtaining an ethanolic extract of the first step of extraction and pulp; then, this pulp is repeatedly extracted within 4-6 hours with ethyl alcohol using the following proportion: ethyl alcohol 1:(3-5) with concentration of alcohol of 30% either 50%, or 70%, at temperature of 60-75°C, obtaining an ethanolic extract of the second step of extraction and pulp. After that the ethanolic extract of the first step of extraction is aggregated with the ethanolic extract of the second step of extraction.

EFFECT: increase in active substances content in an extract.

1 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns the pharmaceutical, food and cosmetic industry. Perform extraction of the raw material crushed with water with obtaining of a water extract and pulp. The pulp, obtained after extraction of raw materials by the water, is extracted in two steps with ethyl alcohol. At the first step of extraction the constrictor is extracted within 4-6 hours using the following proportion: ethyl alcohol 1:(5-7) with concentration of alcohol of 30% either 50%, or 70%, at temperature of 60-75°C, obtaining an ethanolic extract of the first step of extraction and pulp; then, this pulp is repeatedly extracted within 4-6 hours with ethyl alcohol using the following proportion: ethyl alcohol 1:(3-5) with concentration of alcohol of 30% either 50%, or 70%, at temperature of 60-75°C, obtaining an ethanolic extract of the second step of extraction and pulp. After that the ethanolic extract of the first step of extraction is aggregated with the ethanolic extract of the second step of extraction.

EFFECT: increase in active substances content in an extract.

1 ex, 1 tbl

FIELD: medicine, hematology.

SUBSTANCE: individually selected low-calorie diet is administered, combined with reasonably graduated static and dynamic exercise. Concurrently, preparations are administered as follows: 500 mg methformin twice a day after meal, 30 mg zophenopril every morning, 35 mg preductal MB by 1 pill twice a day, and duovit 1 red pill + 1 blue pill every day. Course of treatment is continued for 6 months. The method provides complex effect potentiation of the diet and of particular preparations from selected pharmacological groups during empirically determined treatment period.

EFFECT: normalisation of platelet hemostasis, lowering risk of thrombosis complications.

1 ex

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