3-phenylpyrazolo[5,1-b]thiazole derivative

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) and salts thereof wherein R1 represents -A11-A12-; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 3,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl containing methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine. Also, the invention also refers to a pharmaceutical composition possessing corticotrophin-releasing factor (CRF) receptor antagonist activity, containing a compound of formula (I), to a therapeutic/preventive agent, and a method of treating the diseases specified in the patent claim.

EFFECT: there are presented the compounds of formula (I) as corticotropin-releasing factor (CRF) receptor antagonists.

20 cl, 2 dwg, 2 tbl, 51 ex

 

The text descriptions are given in facsimile form.

1. The compound of the following formula (I) or its salt

where R1represents the formula-A11-And12-;
R2is tetrahydrofuranyl, tetrahydropyranyl or tetrahydropyranyl;
And11represents the t of a simple link, methylene or 1,2-ethylene;
And12represents C1-6alkyl or C3-6cycloalkyl, or C3-6cycloalkyl containing methyl;
R3represents methoxy, cyano, cyclobutylmethyl, methoxymethyl or ethoxymethyl; and
R4represents methoxy or chlorine.

2. The compound or its salt according to claim 1, where R2represents tetrahydropyran-4-yl, tetrahydropyran-3-yl, (tetrahydropyran-4-yl)methyl or (tetrahydrofuran-3-yl)methyl.

3. The compound or its salt according to claim 1 or 2, where R1represents n-propyl, n-butyl, n-pentyl, cyclopropylmethyl, cyclobutylmethyl, 2-(cyclopropyl)ethyl or 2-methylcyclopropyl)methyl.

4. Drug or prophylactic agent for depression, depressive symptoms, anxiety, irritable bowel syndrome, sleep disorders, insomnia, alcohol dependence, withdrawal symptoms of alcohol, drug dependence, withdrawal symptoms of drugs, functional disorders of the gastrointestinal tract associated with stress, anorexia nervosa, disorders of food intake, postoperative ileus, ischemic neuropathy, apoplexy, exitotoxicity neuropathy, convulsion, epilepsy, hypertension, schizophrenia, bipolar disorder or dementia, containing the compound or its salt according to claim 1.

5. N-Butyl-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-meth is XI-N-(tetrahydro-2H-Piran-4-yl)pyrazolo[5,1-b][1,3]thiazole-7-amine or its salt.

6. N-Butyl-3-[4-(ethoxymethyl)-2,6-acid]-6-methoxy-N-(tetrahydro-2H-Piran-4-yl)pyrazolo[5,1-b][1,3]thiazole-7-amine or its salt.

7. N-(2-Cyclopropylethyl)-3-[4-(ethoxymethyl)-2,6-acid]-6-methoxy-N-(tetrahydro-2H-Piran-4-yl)pyrazolo[5,1-b][1,3]thiazole-7-amine or its salt.

8. 3-[4-(Ethoxymethyl)-2,6-acid]-6-methoxy-N-propyl-N-(tetrahydro-2H-Piran-3-yl)pyrazolo[5,1-b][1,3]thiazole-7-amine or its salt.

9. N-(Cyclobutylmethyl)-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-(tetrahydro-2H-Piran-4-yl)pyrazolo[5,1-b][1,3]thiazole-7-amine or its salt.

10. N-(Cyclopropylmethyl)-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-(tetrahydro-2H-Piran-4-yl)pyrazolo[5,1-b][1,3]thiazole-7-amine or its salt.

11. 3-[2,6-Dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-propyl-N-(tetrahydro-2H-Piran-4-yl)pyrazolo[5,1-b][1,3]thiazole-7-amine or its salt.

12. 3-[2-Chloro-6-methoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-propyl-N-(tetrahydro-2H-Piran-4-yl)pyrazolo[5,1-b][1,3]thiazole-7-amine or its salt.

13. 4-{7-[(Cyclopropylmethyl)(tetrahydrofuran-3-ylmethyl)amino]-6-methoxypyrazine[5,1-b][1,3]thiazol-3-yl} - for 3,5-dimethoxybenzonitrile or its salt.

14. N-(Cyclopropylmethyl)-6-methoxy-N-(tetrahydro-2H-Piran-4-ylmethyl)-3-(2,4,6-trimethoxyphenyl)pyrazolo[5,1-b][1,3]thiazole-7-amine or its salt.

15. Pharmaceutical composition having antagonistic activity against receptor corticotropin-visualaid the factor (CRF), containing the compound or its salt according to one of claims 1 to 3 as an active ingredient and suitable additives.

16. Drug or prophylactic agent for depression, depressive symptoms, anxiety or irritable bowel syndrome, containing the compound or its salt according to one of claims 1 to 3.

17. A method of treating or preventing depression, depressive symptoms, anxiety, irritable bowel syndrome, sleep disorders, insomnia, alcohol dependence, withdrawal symptoms of alcohol, drug dependence, withdrawal symptoms of drugs, functional disorders of the gastrointestinal tract associated with stress, anorexia nervosa, disorders of food intake, postoperative ileus, ischemic neuropathy, apoplexy, exitotoxicity neuropathy, convulsion, epilepsy, hypertension, schizophrenia, bipolar disorder or dementia, including introduction to the patient compound or its salt according to one of claims 1 to 3.

18. A method of treating or preventing depression, depressive symptoms, anxiety or irritable bowel syndrome, comprising the administration to a patient compounds or salts thereof according to one of claims 1 to 3.

19. The compound or its salt according to one of claims 1 and 2 for treating or preventing depression, depressive symptoms, anxiety, irritable bowel syndrome, disorders of SN is, insomnia, alcohol dependence, withdrawal symptoms of alcohol, drug dependence, withdrawal symptoms of drugs, functional disorders of the gastrointestinal tract associated with stress, anorexia nervosa, disorders of food intake, postoperative ileus, ischemic neuropathy, apoplexy, exitotoxicity neuropathy, convulsion, epilepsy, hypertension, schizophrenia, bipolar disorder or dementia.

20. The compound or its salt according to one of claims 1 and 2 for treating or preventing depression, depressive symptoms, anxiety or irritable bowel syndrome.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula 1 , where X and T are N or C, Q is a (3-7)-member aromatic ring which contains 0-3 nitrogen atoms as ring members, and which is optionally benzo-condensed and is substituted with oxo; C1-C6-alkyl; halogen- C1-C6-alkyl; hydroxy-C1-C6-alkyl; C1-C6-alkoxy; C6-C10-aryl; or a (3-7)-member heteroaryl containing 1-3 oxygen atoms, P is C1-C6-alkyl, optionally substituted with a halogen, and R is a group selected from: (i) -C1-C6-alkyl-R1, (ii) -NR2R3, (iii) -O-R4, (iv) -S-R5, (v) -C (=O))-R6, (vi) optionally substituted (3-7)-member heteroaryl containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (vi) optionally substituted (3-7)-member heteroatom containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (vii) optionally substituted, saturated or partially unsaturated, separate or condensed (3-10)-member heterocyclic ring containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (viii) azido; where each R1, R2, R3, R4, R3, R6, is as described in the claim. The invention also relates to a pharmaceutical composition for preventing and treating a vascular disease, which contains a compound of formula 1.

EFFECT: compounds of formula 1 with inhibitory activity with reference to aggregation of thrombocytes.

7 cl, 7 dwg, 2 tbl, 519 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a 2-aza-bicyclo[3.3.0]octane derivative of formula , with stereogenic centres in a (1S,3S,5S)-configuration, where A is a thiazolyl which is unsubstituted or monosubstituted, where the substitute is independently selected from a group comprising C1-4alkyl, C3-6cycloalkyl and NH2; B is phenyl which is unsubstituted or mono- or disubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl, trifluoromethyl, NHC(O)CH3 and halogen; and R1 is an imidazo[2,1·b]thiazolyl or benzoisoxazolyl group, where said groups are independently unsubstituted or monosubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl; or R1 is a 2,3-dihydrobenzofuranyl group; or a pharmaceutically acceptable salt. The 2-aza-bicyclo[3.3.0]octane derivative of formula (I) is as a medicinal agent having the activity of orexin receptor antagonists.

EFFECT: obtaining novel 2-aza-bicyclo[3,3,0]octane derivatives as orexin receptor antagonists.

8 cl, 1 tbl, 26 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of general formula:

or its pharmaceutically acceptable salt wherein the ring A represents a phenyl group which can contain 1-3 substitutes specified in a group of substitutes, or a thienyl group which can contain 1-3 substitutes specified in a group of substitutes α; L represents a single bond or a group of formula -NRC CO- (wherein Re represents a hydrogen atom), the ring B represents C6-14 aryl group which can contain 1-3 substitutes specified in a group of substitutes α, or a 5-10-member heterocyclic group which can contain 1-3 substitutes specified in a group of substitutes α; the X, Y, Z , R1 and R2 , R3, R4, R5 and R6 radical values are presented in cl.1 of the patent claim which possess an effect of Aβ protein production inhibition or an effect of BACE1 inhibition.

EFFECT: preparing the compound which is applicable as a preventive or therapeutic agent for neurodegenerative disease caused by Aβ.

13 cl, 35 tbl, 285 ex

FIELD: chemistry.

SUBSTANCE: invention relates to bicyclosulphonyl acid (BCSA) compounds of formula: where: where each of -Rpw, -Rpx, -RPY, and -RPZ independently denotes H or -RRS1; each -RRS1 independently denotes -F, -Cl, -Br, -I, -RA1, -CF3, -OH, -OCF3 or -ORA1; where each RA1 independently denotes C1-4alkyl, phenyl or benzyl; and additionally, two neighbouring -RRS1 groups can together form -OCH2O-, -OCH2CH2O- or -OCH2CH2CH2O-; -RAK independently denotes a covalent bond, -(CH2)- or -(CH2)2-; -RN independently denotes -RNNN, or -LN-RNNN; the rest of the values of the radicals are given in claim 1, which act as inhibitors of inhibitors of tumor necrosis factor-α converting enzyme (TACE).

EFFECT: compounds are useful in treating TNF-α mediated conditions.

36 cl, 303 ex

FIELD: chemistry.

SUBSTANCE: invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of formula , where R1 and R2 are hydrogen, C1-4alkyl or fluorine; R3 is a phenyl which is unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl, C1-4alkoxy group, trifluoromethyl, trifluoromethoxy group and halogen; 2,3-dihydrobenzofuranyl; 2,3-dihydrobenzo[1,4]dioxynyl; or isoxazolyl, pyridyl, indazolyl, benzofuranyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl, benzoisothiazolyl, pyrrolo[2,1b]thiazolyl, imidazo[ 1,2-a]pyridinyl or imidazo[2,1-b]thiazolyl, where said groups are unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl, C1-4alkoxy group, halogen and trifluoromethyl; A is or ; R4 is C1-4alkyl or -NR6R7; R6 is hydrogen or C1-4alkyl; R7 is hydrogen or C1-4alkyl; and D is a phenyl which is unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C1-4alkyl, C1-4alkoxy group, trifluoromethyl and halogen; or a pharmaceutically acceptable salt of such a compound. 3-aza-bicyclo[3.3.0]octane derivatives or a pharmaceutically acceptable salt thereof are used as a medicinal agent having the activity of orexin receptor antagonists.

EFFECT: novel 3-aza-bicyclo[3,3,0]octane derivatives as nonpeptide antagonists of human orexin receptors.

9 cl, 1 tbl, 85 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new antibacterial compounds of formula I

wherein R1 represents halogen or alkoxy group; each U and W represents N; V represents CH, and R2 represents H or F, or each U and V represents CH; W represents N, and R2 represents H or F, or U represents N; V represents CH; W represents CH or CRa, and R2 represents H, or also when W represents CH, may represent F; Ra represents CH2OH or alkoxycarbonyl; A represents group CH=CH-B, a binuclear heterocyclic system D, phenyl group which is mono-substituted in the position 4 by C1-4 alkyl group, or phenyl group which is di-substituted in positions 3 and 4 wherein each of two substitutes is optionally specified in a group consisting of C1-4 alkyl and halogen; B represents mono- or di-substituted phenyl group wherein each substitute is a halogen atom; D represents group

wherein Z represents CH or N, and Q represents O or S; or to salts of such compounds.

EFFECT: compounds are used for treating bacterial infections.

13 cl, 2 tbl, 25 ex

FIELD: medicine.

SUBSTANCE: invention refers to an agent for activation of lipoprotein lipase containing a benzene derivative of general formula (1) which is used for preventing and treating hyperlipidemia and obesity. The invention also refers to the benzene derivatives of general formula (1a).

EFFECT: composition improvement.

8 cl, 6 tbl, 9 ex

FIELD: chemistry.

SUBSTANCE: method is realised by mixing a compound of formula (B) with p-toluenesulphonic acid or a monohydrate of toluenesulphonic acid in less than 1 molar equivalent with respect to the compound of formula (B), in a solvent while heating. An additional amount of p-toluenesulphonic acid or monohydrate of p-toluenesulphonic acid is then added to the mixed solution while cooling in such an amount that their total molar equivalent with p-toluenesulphonic acid or monohydrate of p-toluenesulphonic acid at the mixing step is equal to 1 molar equivalent or more with respect to the compound of formula (B). At the last step, the obtained solution is crystallised to separate a compound of formula (A).

EFFECT: obtaining a compound of formula (A) with stable high output.

12 cl, 1 dwg, 3 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention describes the pyrrolo- and thiazolopyridinium compounds and their pharmaceutically acceptable salts covered by general structural formula I: wherein the values A, B, R1, R2, R3, R4, R5, R6, R7 and R8 are those as presented in cl.1, and a pharmaceutical composition based on the given compound for inhibition of hypoxia-inducible factor (HIF) hydroxylase activity.

EFFECT: there are produced and described new compounds able to modulate hypoxia-inducible factor (HIF) stability and/or activity.

29 cl, 178 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula I , and pharmaceutically acceptable salts thereof, where L denotes O, S, or CH2; Y denotes N or CH; Z denotes CR3; G denotes CH; R1 denotes a heteroaryl ring of formula , where D1 denotes S, O; D2 denotes N or CR12; D3 denotes CR12; R2 denotes (C6-C10)-aryl; 5-9-member mono- or bicyclic heteroaryl with 1 or 2 heteroatoms independently selected from N or S; a saturated or partially saturated (C3-C7)-cycloalkyl; or a saturated 5-6-member heteocyclyl with 1 heteroatom selected from N, where said aryl, heteroaryl, cycloalkyl and heterocyclyl are optionally substituted with one or two groups independently selected from (C1-C6)-alkyl, F, Cl, Br, CF3, CN, NO2, OR6, C(-O)R6, C(=O)OR6, C(=O)NR6R7, saturated 6-member heterocyclyl with 2 heteroatoms independently selected from N or O, and S(O)2R6, and where said alkyl is optionally substituted with one -OR8 group; R3 denotes H; (C1-C6)-alkyl; (C2-C6)-alkenyl; Cl; Br; OR6; SR6; phenyl; or a 6-member heteroaryl with 1 heteroatom selected from N, where said alkyl and alkenyl are optionally substituted with one group selected from C(=O)OR8, -OR8, -NR8R9; or a saturated 6-member heterocyclyl with 1 heteroatom selected from N or O.

EFFECT: disclosed compounds are used in treating and preventing diseases mediated by insufficient level of glucokinase activity, such as sugar diabetes.

16 cl, 479 ex

FIELD: medicine.

SUBSTANCE: claimed invention relates to field of medicine, namely to cardiology, and deals with treatment of ischemic heart disease with distal or diffuse affection of coronary arteries. For this purpose 5-oxymethyluracyl in dose 25 mg per kg of weight was introduced 3 times per day during 2 weeks in experiments on male rabbits of Shilshilla breed.

EFFECT: method ensures improvement of myocardium blood supply due to stimulation of neoangiogenesis and prevention of thrombosis development.

1 dwg, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of general formula (I), wherein A represents a pyrrole group or a pyrazole group, and X represents a carbon atom or a nitrogen atom; R1 represents a carboxy group; R2 independently represents a group specified in a substitute group α; R3 independently represents phenyl(C1-C6alkyl)group substituted by, phenyl(C1-C6alkyl)group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α); m is equal to 0, 1, 2 or 3, n is equal to 0 or 1; each of R4, R5, R6 and R7 independently represents a hydrogen atom, C1-C6alkyl group or a halogen atom; B represents a substituted naphthyl group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α), or the group represented by formula (II), wherein B1, B2 and α are those as specified in the patent claim. Also, the invention refers to a pharmaceutical composition possessing lipolysis inhibiting activity, to the use of the compounds of formula (I) in preparing a drug preparation for treating hyperlipidemia, dislipidemia, abnormal lipid metabolism, arteriosclerosis or type II diabetes mellitus and to a method of treating or preventing the mentioned diseases.

EFFECT: preparing the compounds of formula (I) possessing lipolysis inhibiting activity.

36 cl, 1 dwg, 1 tbl, 69 ex

Antioxidant // 2481116

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to an antioxidant containing a cyclolanostan derivative selected from 9,19-cyclolanostan-3-ol and 24-methylene-9,19-cyclolanostan-3-ol, and a lophenol derivative selected from 4-methylcholest-7-en-3-ol, 4-methylergost-7-en-3-ol and 4-methylstigmast-7-en-3-ol, in the concentration of min. 0.0001 wt %, as an active ingredient. The invention also concerns a method for preparing the specified antioxidant. The antioxidant may be used as a drug preparation, a food or a beverage, a food additive, a drug preparation for topical skin application.

EFFECT: mentioned antioxidant provides the inhibition of lipid peroxide formation.

28 cl, 2 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula 1 , where X and T are N or C, Q is a (3-7)-member aromatic ring which contains 0-3 nitrogen atoms as ring members, and which is optionally benzo-condensed and is substituted with oxo; C1-C6-alkyl; halogen- C1-C6-alkyl; hydroxy-C1-C6-alkyl; C1-C6-alkoxy; C6-C10-aryl; or a (3-7)-member heteroaryl containing 1-3 oxygen atoms, P is C1-C6-alkyl, optionally substituted with a halogen, and R is a group selected from: (i) -C1-C6-alkyl-R1, (ii) -NR2R3, (iii) -O-R4, (iv) -S-R5, (v) -C (=O))-R6, (vi) optionally substituted (3-7)-member heteroaryl containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (vi) optionally substituted (3-7)-member heteroatom containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (vii) optionally substituted, saturated or partially unsaturated, separate or condensed (3-10)-member heterocyclic ring containing 1-4 heteroatoms selected from a nitrogen atom, an oxygen atom and a sulphur atom, (viii) azido; where each R1, R2, R3, R4, R3, R6, is as described in the claim. The invention also relates to a pharmaceutical composition for preventing and treating a vascular disease, which contains a compound of formula 1.

EFFECT: compounds of formula 1 with inhibitory activity with reference to aggregation of thrombocytes.

7 cl, 7 dwg, 2 tbl, 519 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to an oral solid dosage form containing a therapeutically effective amount of aliskiren or its pharmaceutically acceptable salt wherein an active ingredient makes more than 46 wt % of total weight of the oral dosage form. The oral dosage form is presented in the form of a tablet or a film-coated tablet, and contains an internal phase containting aliskiren or its pharmaceutically acceptable salt, an excipient, a binding agent and a disintegrant, and an external phase containing a disintegrant, an excipient, a glidant and a lubricant.

EFFECT: invention provides administration of the active ingredient aliskiren in the small oral dosage form; it is characterised by an acceptable disintegration time.

32 cl, 2 ex

FIELD: medicine.

SUBSTANCE: correction of ischemic disorders caused by reperfusion liver injury in experiment in white Wistar male rats involves modelling an ischemic and reperfusion liver injury. 30 Minutes before, L-norvalin arginase blocker 10 mg/kg is introduced intraperitoneally, and distant ischemic pre-conditioning is conducted. Then, another dose of L-norvalin arginase blocker is introduced immediately after liver ischemia.

EFFECT: effective correction of the hepatocellular damage ensured by minimising the oxidative stress effects.

1 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine and concerns methods of treating acute cerebrovascular disease. A method of treating acute ischemic and hemorrhagic cerebrovascular disease consists in administering a pharmaceutical composition containing a protein-polypeptide complex taken as a biologically active substance and prepared of fast-frozen embryo brain of hoofed farm animals of a gestation term from the middle of the first one-third to the middle of the last one-third of pregnancy, in the amount of 0.05-0.8 mg/day subcutaneously, intramuscularly, intravenously, intranasally and intrathecally. Said protein-polypeptide complex contains negative weak acid neutral proteins and polypeptides referring to growth/differentiation factors, signal molecules, intercellular adhesion molecule, of molecular weights 5 to 200 kD with min. 80% of total weight of proteins having molecular weight 10 to 120 kDa, and characterised nu a peak at UV wave length 274-284 nm and bands at the pi values of 4.2 to 8.4 at isoelectric focusing in 5% polyacrylamide gel.

EFFECT: protein-peptide complex is safe and tolerable when in use; it is effective in treating the patients with acute cerebrovascular disease that ensures clinically significant effect of survivability, dynamics and recovery length of the lost functions in the patients when using the method.

4 cl, 9 tbl, 23 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to using a compound of formula (I):

wherein R represents a hydrogen atom or CH3, and X represents a physiologically acceptable counter ion for preparing a hepatoprotective agent for treating or preventing a liver injury. The invention also refers to a method for treating or preventing the liver injury which involves a therapeutically or preventive effective amount of said compound of formula (I).

EFFECT: declared group of inventions provides hepatoprotective activity ensured by an ability of the compounds of formula (I) to improve an endothelium function to release endogenic prostacyclin.

14 cl, 7 dwg, 3 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely anaesthesiology, and concerns the early postoperative drug-induced correction of central hemodynamic disorders in oncological patients. That is ensured by measuring a cardiac index (CI), an impact index (II), a LV filling pressure (LVFP), a total peripheral vascular resistance (TPVR), a LV mechanical work index (LVMWI), a systolic blood pressure (SBP); the derived relations of these values in a patient are used to prescribe an individual drug-induced therapy.

EFFECT: method provides reducing a number of hemodynamic complication in this group of patients by taking account of the individual haemodynamic values of the particular patient.

5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly a drug preparation for preventing the development of cardiovascular diseases in individuals of a high-risk group. A capsule for preventing the development of cardiovascular diseases in individuals of a high-risk group which contains acetylsalicylic acid tablets coated by partially hydrolised polyvinyl alcohol (PVA), tablets of simvastatin and pravastatin coated by hydroxypropyl methylcellulose (HPMC) and tablets of lisinopril, ramipril or perindopril coated by partially hydrolised polyvinyl chloride. Using the capsule in producing the drug preparation for preventing the development of cardiovascular diseases in individuals of a high-risk group.

EFFECT: capsule is stable at variable temperature and relative humidity, as well as resistant to decomposition of the active ingredients under exposure to light.

8 cl, 29 tbl, 9 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of general formula

, wherein X represents a halogen atom or C1-6-alkyl; and has the value of 0, 1, 2 or 3; R1 represents H; R2 represents or ; R3 represents C1-6-alkyl, C3-10-cycloalkyl, phenyl, 6-member heterocycloalkyl representing tetrahydropyranyl, or 5-10-member heteroaryl specified in pyridinyl, pyrazinyl, pyrimidinyl, pyridazinyl, benzo[1,3]dioxolyl and 2,3-dihydrobenzo[1,4]dioxynyl; which be substituted and contains one to five substitutes specified in the patent claim. The invention also refers to pharmaceutical compositions possessing high affinity to dopamine D3 receptor and serotonin 5-HT2A receptor containing said compounds, and the use thereof in preparing drugs.

EFFECT: preparing the compounds of formula (I) possessing high affinity to dopamine D3 receptor and serotonine 5-HT2A receptor.

15 cl, 4 dwg, 5 tbl, 78 ex

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