Method for accelerated optimisation of platelets activity in metabolic syndrome

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

 

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

As the closest analogue of the proposed method (EN 2272628 C1, 27.03.2006). This method also alleviates platelet dysfunction in the metabolic syndrome and is carried out by setting a low-calorie diet, as well as the introduction of amlodipine and Metformin.

The claimed method differs from the known fact that instead of Metformin is administered β-blocker labetalol dose of 200 mg 2 times a day, and instead amlodipine - lacidipine 2 mg in the morning. Scientific research leading to the establishment of the claimed method was dictated by the fact that amlodipine is used in the prototype can be applied not every patient with metabolic syndrome due to possible individual characteristics of patients. Furthermore, among patients with metabolic syndrome high proportion of patients requiring concomitant antihypertensive therapy with a calcium antagonist and β-blocker. In this regard, the task was to develop a method of correction of thrombocytopathy in patients with metabolic syndrome, need for antihypertensive treatment with calcium antagonist and β-blocker.

Never before medical complex, consisting of individually low-calorie diet and drugs labetalola and lacidipine, was not applied at the Aulnay arterial hypertension 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 accelerate the 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 and drugs labetalol 200 mg 2 times a day and lacidipine 2 mg in the morning.

The method allows to adjust the primary hemostasis in patients with MS within two 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 in the optimal mode of functioning, which will significantly reduce the risk of thrombotic complications/decrease 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 Insa is it.

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 years of age (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 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%.

For the preparation of the menu of the patient are special the 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 - assignment labetalola 200 mg 2 times a day and lacidipine 2 mg in the morning.

Example. Patient S., 58 years old, with body weight 78,0 kg, BMI of 31.1 kg/m2suffering from metabolic syndrome over 10 years when the survey was identified thrombocytopathies with increasing adhesive activity is 51%, the aggregation ability (ADP - 24, with collagen - 20 with thrombin - 32, ristomycin - 25, H2About2- 30 with adrenaline 71, ADP + adrenalina 16, ADP + collagen 18 with adrenaline + collagen -19 C) and intravascular platelet activity (discocyte - 62%, disco echinocyte - 21%, ferocity to 12.0%, sphere-echinocyte - 2,0%, biopolar form is 0%, the amount of active forms 38%, and the number of platelet aggregates to 15.7%, the number of small units - 21 100 loose platelets, the number of medium and large units - 12 100 loose platelets) in the background of impaired glucose tolerance and hyperlipidemia type II 6 (total lipids of 9.7 g/l) with mild hypercholesterolemia (total cholesterol - 5.7 mmol/l). The level of acylhydrazines platelets were 4,1D233/109platelet malondialdehyde (MDA) platelet - of 1.62 nmol/109platelets, Catala is s platelets 3000 IU/109platelets, platelet superoxide dismutase - 900 IU/109platelets in blood platelets ATP was before secretion 6,03 mmol/1011Tr., ADP was to secretion of 3.99 mmol/1011Tr., the level of secretion of ATP was 48.0%and secretion of ADP to 58.6%. The content of actin in intact platelets were $ 30.1% of the total protein content in the cell, changing the background ADP-aggregation to 39.9% of the total protein content in the cell, against thrombin-aggregation, it increased to 48.3% of the total protein content in the cell. The content of myosin in intact platelets, the patient was 22.6% of the total protein content in the cell when the content grows on the background ADP-aggregation to 36.6% of the total protein content in the cell and on the background of the thrombin-aggregation of 41.5% of the total protein content in the cell.

The patient was assigned individually selected low-calorie diet (1931,2 kcal), labetalol 200 mg 2 times a day, lacidipine 2 mg in the morning. The patient was examined after 4 and 8 weeks after starting treatment. Simultaneously with the inspection was carried out biochemical and hematological analysis of blood.

To 8 week of treatment, the patient began to decline body weight (72,0 kg) and body mass index (28,8 kg/m2), was achieved by improving the lipid profile (total lipids - 6.0 g/l, total cholesterol 5.2 mmol/l), normalization test glucose tolerance, edge the positive functions of blood platelets - 37%, platelet aggregation with ADP - 45, collagen - 38 C, thrombin - 62, ristomycin - 49, hydrogen peroxide - 52, adrenaline - 104 and combinations of inductors - ADP + adrenaline - 29, ADP + collagen-27, adrenaline + collagen-28, as well as optimization of intravascular platelet activity (discocyte 89%, discogenic - 7,9%, ferocity - 2,2%, sphere-echinocyte - 1,5%, biopolar forms of 0.4%, the amount of active form 11%, the number of platelet aggregates to 4.0%, the number of small units - 5 100 loose platelets, the number of medium and large units - 0.2 per 100 loose platelets), level of lipid peroxidation (level acylhydrazines platelets 1.7 D233/109platelet MDA platelets 0.61 nmol/109platelets) and antioxidant protection of blood platelets (catalase platelet - 9200 IU/109platelets, platelet superoxide dismutase - 1500 IU/109platelet count.

The content of ADP and ATP, the level of secretion, the content values and the Assembly of actin and myosin, in blood platelets returned to normal. Thus, platelet ATP began to reach secretion 5,69 mmol/1011Tr ADP to secretion 3.50 mmol/1011Tr, when the level of secretion of ATP and 33.4% and the level of secretion of ADP to 44.0%. The content of actin in intact platelets of the patient after treatment is 20.3% of the total containing the s protein in the cell, changing the background ADP-aggregation to 29.2% of the total protein content in the cell, against thrombin-aggregation 35,8% of the total protein content in the cell. The content of myosin in intact platelets of the patient after treatment ranged from 15.0% to the total protein content in the cell when the content grows on the background ADP-aggregation to 27.0% of the total protein content in the cell and on the background of the thrombin-aggregation of 35.0% to the total protein content in the cell. Treatment was discontinued.

The results allowed us to save over the next 2 months indicators of platelet hemostasis in the patient at a normal level. Thus, the adhesive function of blood platelets was equal to 36.2 percent, while platelet aggregation with ADP 44,0 with collagen 38,2 with thrombin 61,0 with ristomycin 50,0 with hydrogen peroxide 50,0 with adrenaline 99,9 s and combinations of inductors with ADP + adrenaline 32,2 with ADP + collagen 30,0 with adrenaline + collagen 29,0 with, the normal level of intravascular platelet activity: discocyte of 84.0%, disco echinocyte 10,0%, ferocity 4,0%, sphere-echinocyte 2.0%) and bipolar forms of 1.0%the number of platelets in units of 3.0%, the number of small aggregates 2.1 per 100 loose platelets, medium and large units 0,17 100 loose platelets. Thus remained stable levels of ADP and ATP, the level of secretion, indicators sod is Rania and Assembly of actin and myosin, in blood platelets. Thus, platelet ATP to the secretion contained 5,70 mmol/1011Tr ADP to secretion 3.54 mmol/1011Tr, the level of secretion of ATP was 33.9%to the level of secretion of ADP to 45.6%. The content of actin in intact platelets, the patient was 20.9% of the total protein content in the cell, changing the background ADP-aggregation to 29,7% of the total protein content in the cell, against thrombin-aggregation to 35.9% of the total protein content in the cell. The content of myosin in intact platelets, the patient was 15.5% of the total protein content in the cell when the content grows on the background ADP-aggregation to 28.6% of the total protein content in the cell and on the background of the thrombin-aggregation 35,8% of the total protein content in the cell.

The level of acylhydrazines platelets was 1.8 D233/109platelet MDA platelets of 0.60 nmol/109platelet antioxidant protection of blood platelets was normal (catalase platelet - ME/109platelets, platelet superoxide dismutase - ME/109platelet count.

The patient is asked to observe her earlier recommendations in the following.

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, decrease in h is x number of cases of temporary disability, to reduce the duration of hospitalization, reduce morbidity and mortality.

Method for optimizing the 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 of age (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 of age (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,

labetalola 200 mg 2 times a day and lacidipine 2 mg in the morning for 8 weeks.



 

Same patents:

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: chemistry, pharmaceutics.

SUBSTANCE: invention proposes a lipid compound with formula (I): , where PHG is a polar head group, obtained from one of the following: phospholipid, lysophospholipid, ceramides, monoacylglycerine, diacylglycerine and triacylglycerine, or -W-Linker-HG, p is a number from 1 to 3, X is independently chosen from C6-24alkenyl, containing one or more double bonds and, possibly, one or more triple bonds, or C6-24alkyl, which are can be substituted with at least one of the following: F, hydroxy, C1-C4alkoxy, C1-C4alkylthio, C2-C5acyloxy and C1-C4alkyl; Y chosen from at least one of S, Se, SO2, SO, O and CH2; and Z is a C1-C10alkyl residue, where each of the X, Y and Z groups is chosen independently, when p is 2 or 3, under the condition that, at least one Y does not represent CH2. Description is also given of the use of formula (I) compound or its pharmaceutical salt in the production of medicinal preparations for curing and/prevention of different conditions, pharmaceutical composition, containing formula (I) compound and the method of obtaining a lipid compound with formula (I).

EFFECT: obtaining sulphur containing phospholipid compounds, with useful biological properties.

58 cl, 8 tbl

FIELD: medicine.

SUBSTANCE: invention relates to pharmacology and medicine, particularly: the set applied to treatment for thrombosis, which includes compound with formula and aspirin; pharmaceutical composition, which includes compound with formula (1) and aspirin; and application of pharmaceutical composition, which includes compound with formula (1), and pharmaceutical composition, which includes aspirin to treatment for thrombosis.

EFFECT: providing of increased thrombosis therapy efficacy.

6 cl, 1 dwg, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to application of compounds with formula R2=R1-X, where R1 and R2 have 23 to 35 carbon atoms in sum, X represents primary alcohol functional group -CH2OH or carboxyl group -COOH, R1 is saturated linear hydrocarbon chain with 9 carbon atoms, and R2 is linear hydrocarbon chain, which is saturated or unsaturated, including 1 to 4 unsaturated double links.

EFFECT: producing formulations suited for application to hypercholesterolemia therapy and prophylaxis.

3 cl, 4 tbl, 6 ex

FIELD: medicine.

SUBSTANCE: within 12 weeks therapy including individually prescribed low-calorie diet, individually prescribed physical activity, lovastatin introduced in dose 20 mg once for the night, amlodipine 10 mg once at the same time and oligovit one tablet 2 times a day.

EFFECT: decreased risk of thrombotic complications is provided due to the most complete normalisation of cholesterol content in thrombocyte membranes.

2 ex

FIELD: medicine; cardiology.

SUBSTANCE: in case patient is diagnosed with increased thromboxane development resulted from three transfer tests while level of thrombocyte aggregation restoration within simple transfer test is higher than 37.0%, indicators of collagen-aspirin test are higher than 69.0% and/or of collagen-imidazole test is higher than 59%, for purposes of thromboxane development correction associated with arterial hypertension and metabolic syndrome, low-calorie diet, graduated physical activity, intake of Lovastatin 20 mg for the night and Amlodipine 10 mg once a day are prescribed for patient within 4 months.

EFFECT: provided normalisation of thromboxane formation in thrombocytes.

1 tbl, 3 ex

FIELD: medicine; cardiology.

SUBSTANCE: thrombocyte aggregation is evaluated within in three transfer tests. If aggregation indicators are found in single transfer test in amount 37.1% and more, and/or in collagen-aspirin test - in amount 69.1% and more, and/or in collagen-imidazole test - in amount 59.1% and more, complex treatment is prescribed for 2 months as follows: low-calorie diet, graduated physical exercises, introduction of Atorvastatin in dosage10 mg for the night, Nitrendipine 0.02 g once a day, Metformin in dosage 500 mg 2 times a day and Duovit 1 red and 1 dark blue tablets per day.

EFFECT: thrombus formation risk is decreased due to fast and effective normalisation of arachidonic acid thrombocyte metabolism.

1 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically to haematology, cardiology and endocrinology, and concerns thrombocyte intravascular activity normalisation for patients suffering from arterial hypertension associated with metabolic syndrome. For this purpose individually prescribed low-calorie diet is used within 12 weeks combined with Essentiale Forte dosed 1 capsule 3 times a day, amlodypine dosed 10 mg in the morning and Duovit dosed 1 red and 1 dark blue tablet a day. Such method realisation in particular choice of specific polyvitaminic agent provides conditions for therapeutic components potentiating that is manifested in reduction of thrombocyte content in blood and in normalisation of ADF and ATP content in thrombocyte.

EFFECT: development of effective method of thrombocyte intravascular activity normalisation for patients suffering from arterial hypertension associated with metabolic syndrome.

2 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: claimed composition contains (i) aliskiren; (ii) amplodipin; and (iii) hydrochlorotiazid. Invention is useful in treatment of condition or disease such as hypertension, heart failure, angina pectoris, Alzheimer's disease, stroke, etc.

EFFECT: composition of prolonged therapeutic effect and synergetic action.

7 cl

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of pyridylcyanoguanidine of the formula (I): wherein X1 and X2 represent independently a bond, linear or branched hydrocarbon diradical; Y1 and Y2 represent independently a bond or -O-; Y3 represents oxygen atom (O), -O-C(O)-, N(R8) wherein R8 represents hydrogen atom; R1 represents hydrogen atom, linear or branched alkyl or phenyl; R2 represents aryl, heteroaryl or nonaromatic heterocyclic hydrocarbon radical wherein each is substituted optionally with tetrahydropyranyloxy-, di-(C1-C4-alkoxy)phosphinoyloxy- and (C1-C4)-alkoxycarbonylamino-group; R3 represents hydrogen atom, linear, branched or cyclic hydrocarbon radical substituted optionally with one or more amino- carboxy-, alkoxy-groups, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkoxycarbonylamine or nonaromatic nitrogen-containing heterocyclic hydrocarbon radical substituted optionally with (C1-C4)-alkoxycarbonyl, or compound of the formula: wherein s represents a whole number from 1 to 10; R6 represents hydrogen or optionally substituted nonaromatic hydrocarbon radical; R7 represents independently hydrogen atom or methyl; R4, R5 and A represent hydrogen atom; Z' represents pharmaceutically acceptable anion, such as chloride, bromide, iodide; m and r represent independently a whole number from 0 to 4; n = 0 or 1. Also, invention relates to compound of the formula (II) given in the invention description, to pharmaceutical composition based on these compounds for preparing a drug used in treatment of proliferative diseases, methods for treatment and using.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

37 cl, 2 tbl, 36 ex

FIELD: medicine, anesthesiology-resuscitation, neuropathology.

SUBSTANCE: it is necessary to carry out oxygenotherapy, intravenous injection of physiological solution and those of hydroxyethyl starch. Also, it is important to inject beta-blocators, heparin, opioids, alpha2-adrenoagonists, antagonists of NMDA-receptors, glucocorticoids, nimotope, actovegin. One should prescribe early enteral nutrition. On stabilizing the parameters of cardio-vascular and respiratory systems it is necessary to inject intravenously the solution of mildronate 10% - 10 ml for 10-14 d once daily and the intake of rheaferon-EC-lipint at the dosage of 10000-15000 U/kg or through a gastric probe for 5 d. The innovation enables to efficiently prevent pneumonia due to adequate immunotherapy of the above-mentioned pathology.

EFFECT: higher efficiency of prophylaxis.

3 ex, 1 tbl

FIELD: medicine, experimental cardiopharmacology.

SUBSTANCE: dysfunction is modeled in experiment by every day intraperitoneal administration to rats of L-arginine nitromethyl ester for 7 days in the dose 25 mg/kg. On this background amlodipine is administrated into stomach in the dose 0.5 mg/kg, and L-arginine is administrated by intraperitoneal route in the dose 200 mg/kg once per 24 h. Method provides effective correction under the definite modeling conditions.

EFFECT: improved method of dysfunction correction.

2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: preparation comprises Amlodipine taken in quantity corresponding to free base content from 6 mg to 10 mg and Benazepril/benazeprilate corresponding to Benazepril hydrochloride content not exceeding 40mg.

EFFECT: enhanced effectiveness of arterial blood pressure control.

28 cl

FIELD: medicine, cardiology, chemical-pharmaceutical industry.

SUBSTANCE: invention relates to an agent used in treatment and prophylaxis of cardiovascular diseases. The claimed agent comprises the following components, wt.-%: foridone as an active substance (3.00-6.00) and pharmaceutically acceptable carrier - gel base (the balance) consisting of a thickening agent, non-aqueous hydrophilic solvents, hydrophobic solvents, preserving agent, neutralizing agent, emulsifier and purified water. Invention provides achievement of high level of prolongation of specific activity of agent, reducing or excluding negative adverse effects.

EFFECT: improved and valuable medicinal properties of agent.

8 cl, 5 tbl, 14 ex

FIELD: medicine; cardiology.

SUBSTANCE: group of inventions includes a method and pharmaceutical composition aimed at heartbeat number reduction of mammals. To that purpose a therapeutically effective dose of adenosine A1 receptor agonist represented by 6-(3-(R)-N-aminotetrahydrofuranyl)purine riboside (CVT-510) or 2-{6-[((lR,2R)-2-hydroxycyclopentyl)amino]purine-9-yl}(4S,5S,3R)-5-[(2-fluorphenylthio)methyl]oxolan-3,4-diol (CVT-3619) in combination with minimal therapeutically effective dose of beta-blocker.

EFFECT: efficient heartbeat frequency reduction due to synergic effect of administered compounds with minimal side effects.

22 cl, 7 tbl, 10 dwg, 6 ex

Up!