Lactam-containing compound and its derivatives as xa factor inhibitors

FIELD: chemistry.

SUBSTANCE: description is given of a lactam-containing compound-derivative of tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide with formula I , its pharmaceutical salt and pharmaceutical compositions, their content, and their use as Xa factor inhibitors. The given compound can be used for treating thromboembolic diseases.

EFFECT: obtaining a lactam-containing compound, which can be used for treating thromobembolic diseases.

42 cl, 9 tbl, 140 ex

 

The text descriptions are given in facsimile form.

1. The compound of formula 1:

,

or its pharmaceutically acceptable salt.

2. The compound according to claim 1, which represents a compound of formula 1

,

3. The compound according to claim 1 or 2, intended for the treatment of thromboembolic disease.

4. The compound according to claim 1 or 2, intended for the manufacture of medicaments for the treatment of thromboembolic disease.

5. The compound according to claim 3 or 4, wherein the thromboembolic disorder is a disease from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chamber of the heart.

6. The compound according to claim 3 or 4, wherein the thromboembolic disorder is an acute coronary syndrome.

7. The compound according to claim 3 or 4, wherein the thromboembolic disorder is with the battle myocardial infarction, transient ischemic disorders or stroke.

8. The compound according to claim 3 or 4, wherein the thromboembolic disorder is a deep vein thrombosis.

9. The compound according to claim 3 or 4, wherein the thromboembolic disorder is a pulmonary embolism.

10. Pharmaceutical composition for the treatment of thromboembolic disease, containing a pharmaceutically acceptable carrier and a therapeutically effective amount of the compounds of formula (1) according to claim 1 or its pharmaceutically acceptable salt.

11. Pharmaceutical composition for the treatment of thromboembolic disease, containing a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound according to claim 2.

12. The pharmaceutical composition of claim 10 or 11, characterized in that thromboembolic disease is a disease selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chamber of the heart.

13. The pharmaceutical composition of claim 10 or 11, wherein the thromboembolic disorder is an acute coronary syndrome.

14. The pharmaceutical composition of claim 10 or 11, characterized in that tromboembolic the prioritization of disease is a myocardial infarction, transient ischemic disorders or stroke.

15. The pharmaceutical composition of claim 10 or 11, wherein the thromboembolic disorder is a deep vein thrombosis.

16. The pharmaceutical composition of claim 10 or 11, wherein the thromboembolic disorder is a pulmonary embolism.

17. The use of compounds according to claim 1 or 2 for the manufacture of medicaments for the treatment of thromboembolic disease.

18. The use of compounds according to claim 1 or 2 for the treatment of thromboembolic disease.

19. Use 17 or 18, in which thromboembolic disease is a disease from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chamber of the heart.

20. Use 17 or 18, wherein the thromboembolic disorder is an acute coronary syndrome.

21. Use 17 or 18, in which thromboembolic disease is a myocardial infarction, transient ischemic disorders or stroke.

22. Use 17 or 18, wherein the thromboembolic disorder is a deep vein thrombosis.

23. Use 17 or 18, in which thromboembolic for Alemania is a pulmonary embolism.

24. The use of the pharmaceutical composition of claim 10 or 11 for the manufacture of medicaments for the treatment of thromboembolic disease.

25. The use of the pharmaceutical composition of claim 10 or 11 for the treatment of thromboembolic disease.

26. The application of paragraph 24 or 25, in which thromboembolic disease is a disease from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chamber of the heart.

27. The application of paragraph 24 or 25, wherein the thromboembolic disorder is an acute coronary syndrome.

28. The application of paragraph 24 or 25, in which thromboembolic disease is a myocardial infarction, transient ischemic disorders or stroke.

29. The application of paragraph 24 or 25, wherein the thromboembolic disorder is a deep vein thrombosis.

30. The application of paragraph 24 or 25, wherein the thromboembolic disorder is a pulmonary embolism.

31. Pharmaceutical composition for the treatment of thromboembolic diseases containing a compound according to claim 2, and a second therapeutic agent representing at least one agent selected from an inhibitor of factor XA, protivokashleve what about the agent, protivotromboznoe agent, trainingbible agent, thrombolytic agent, and a fibrinolytic agent.

32. The pharmaceutical composition according p, wherein the second therapeutic agent selected from warfarin, nefrackzionirovannam heparin, low molecular weight heparin, synthetic pentasaccharide, irudina, argatroban, aspirin, ibuprofen, naproxen, sulindaka, indometacin, mefenamic, droxicam, diclofenac, sulfinpirazon, piroxicam, ticlopidine, clopidogrel, tirofibana, eptifibatida, abciximab, melagatran, desulfatohirudin, tissue plasminogen activator, modified plasminogen activator, tissue, anistreplase, urokinase and streptokinase.

33. The pharmaceutical composition according p, wherein the second therapeutic agent represents at least one protivotrevozhny agent.

34. The pharmaceutical composition according p, wherein the second therapeutic agent is selected from aspirin and clopidogrel.

35. The pharmaceutical composition according to clause 34, wherein protivotrevozhny agent represents clopidogrel.

36. The pharmaceutical composition according to clause 34, wherein protivotrevozhny agent is an aspirin.

37. The use of pharmaceutical compositions for p for and is for drinking, preparing tools for the treatment of thromboembolic disease.

38. The application of clause 37, wherein the second therapeutic agent selected from warfarin, nefrackzionirovannam heparin, low molecular weight heparin, synthetic pentasaccharide, irudina, argatroban, aspirin, ibuprofen, naproxen, sulindaka, indometacin, mefenamic, droxicam, diclofenac, sulfinpirazon, piroxicam, ticlopidine, clopidogrel, tirofibana, eptifibatida, abciximab, melagatran, desulfatohirudin, tissue plasminogen activator, modified plasminogen activator, tissue, anistreplase, urokinase and streptokinase.

39. The application of clause 37, wherein the second therapeutic agent represents at least one protivotrevozhny agent.

40. The application of clause 37, wherein the second therapeutic agent is selected from aspirin and clopidogrel.

41. The application of clause 37, wherein protivotrevozhny agent represents clopidogrel.

42. The application of clause 37, wherein protivotrevozhny agent is an aspirin.



 

Same patents:

FIELD: chemistry, pharmaceutics.

SUBSTANCE: claimed invention relates to novel azaheterocycles of general formula 1.1-13 and 2, as well as their pharmaceutically acceptable salts, which possess anti-carcinogenic activity, pharmaceutical composition with their application and combinatorial and focused libraries including novel azaheterocycles. In general formulae 1.1-1.3 and 2.

.

For compounds 1.1-1.3 each of R1a R2a independently on each other represent possibly substituted C1-C6alkyl; each of R1d, R2d, R3d, R4d, R5d, R6d and R7d independently on each other represent substitutes of cyclic system, preferably hydrogen atom, or for compounds 1.1 and 1.3 independently R1d and R2d, R3d and R4d, R5d and R6d together with atoms with which they are bound can form through R1d and R2d, R3d and R4d, R5d and R6d respectively, possibly substituted aromatic cycle, such as benzole, 5-6-member heterocycle which includes, at least, one of heteroatoms, selected from S; or for compounds 1.2 independently R1d and R2d, R3d and R4d, R4d and R5d, R6d and R7d together with atoms with which they are bound can form through R1d and R2d, R3d and R4d, R4d and R5d, R6d and R7d respectively, possibly substituted aromatic cycle, such as benzole, 5-6-member heterocycle which includes, at least, one of heteroatoms, selected from S; for compound 2 R1a represents amino group substitute, excluding hydrogen atom, such as possibly substituted C1-C6alkyl, possibly substituted phenyl; R2a represents possibly substituted C1-C6alkyl; R3a represents amino group substitute, such as hydrogen atom, possibly substituted C1-C6alkyl; Rnd represents one or two substitutes of cyclic system, preferably hydrogen atom, solid line with accompanying it dotted line represent single or double bond.

EFFECT: obtaining novel azaheterocycles and their pharmaceutically acceptable salts, which possess anti-carcinogenic activity.

9 cl, 4 dwg, 3 tbl, 7 ex

FIELD: chemistry, pharmaceutics.

SUBSTANCE: invention relates to novel derivatives of pyridine [2,3-d] pyrimidine of general formula (I) and their pharmaceutically acceptable salts, which possess properties of KDR and FGFR inhibitors. Compounds can be applied to produce medications for treatment of cancer, for instance, of mammary gland, large intestine, lungs and prostate gland. In general formula (I) , Ar and Ar' independently on each other are selected from group that includes phenyl; phenyl substituted with 1-3 substituents selected from group C1-C4alkyl, hydroxy, halogen, halogen-substituted C1-C4alkyl, C1-C4alkoxy; 6-member nitrogen-containing heteroaryl and 6-member nitrogen-containing heteroaryl substituted with C1-C4alkoxygroup, on condition that Ar standing for heteroaryl does not represent 2-pyridyl, and standing for substituted heteroaryl does not represent substituted 2-pyridyl, R1 is selected from group including phenyl, C1-C10alkyl, C1-C10alkyl independently containing substituents selected from group that includes phenyl, C3-C6cycloalkyl. Invention also relates to intermediate compounds for compounds of general formula (I) and to pharmaceutical compositions.

EFFECT: obtaining derivatives and their pharmaceutically acceptable salts which possess properties of selective KDR and FGFR inhibitors.

21 cl, 2 tbl, 20 ex

FIELD: chemistry.

SUBSTANCE: described is obtaining and pharmaceutical application of substituted derivatives of arylalkane acid of formula I , where ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1 and Ar2 are such as determined in said description. Said compounds, as selective agonists activating (RAPPs) receptors, activated by peroximal proliferator, in particular, RXRs/RAPPs-alfa, RXRs/RAPPs-gamma and RXRs/RAPPs-delta heterodimers, are applied in treatment and/or prevention of type 2 diabetes and connected with it metabolic syndrome, such as hypertension, obesity, insulin-resistence, hyperlipidemia, hyperglycemia, hyperolesterinemia, artheriaslerosis, coronary artery disease, and other cardio-vascular disorders, and possess improved profile of side effects, connected with common RAPPs-gamma agonists.

EFFECT: obtaining compunds, which possess improved profile of side effects, connected with common RAPPs-gamma agonists.

22 cl, 38 ex, 2 tbl, 10 dwg

FIELD: chemistry.

SUBSTANCE: novel compounds are selected from group, consisting of: 4-(2-cyclopropyl-ethyl)-piperazine-1-carboxylic acid 2-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 3-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 3-fluorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-(2-hydroxymethyl-cyclopropylmethyl)-piperazine-1-carboxylic acid 2-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopentylmethyl-piperazine-1-carboxylic acid 2-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 3-chlorine-4-(3-methyl- 4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 3-chlorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 2-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-(2-cyclopropyl-ethyl)-piperazine-1-carboxylic acid 3-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 3-methyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 3-fluorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 2-fluorine-4-(3-methyl-4,10-dihudro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 2-fluorine-4-(3-methyl-4,10-dihydro-3H-2,3,4;9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 3-ethyl-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclobutylmethyl-piperazine-1-carboxylic acid 2-chlorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide; 4-cyclopropylmethyl-piperazine-1-carboxylic acid 2-chlorine-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzylamide and 4-cyclobutylmethyl-piperazine-1-carboxylic acid 3-methoxy-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-benzylamide. Invention also relates to pharmaceutical composition and to application of compounds of general formula 1.

EFFECT: obtaining novel biologically active compounds and based on them pharmaceutical composition, possessing antagonistic activity with respect to vasopressin receptors.

60 cl, 153 ex

FIELD: chemistry.

SUBSTANCE: in general formula I

R1 is phenyl or 5-6-member heterocycle, containing one N atom and/or one O atom; R2 is imidazole or annelated imidazole, selected from group, including a), b), c), d) and e); and R3 stands for hydrogen, phenyl, 2,3-dihydrobenzo[1,4]dioxin-6-yl, benzo[b]thiophen-3-yl, 3-methylbenzo[b] thiophen-2-yl, thiophen-2-yl or thiophen-2-ylmethyl, R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, halogen, morpholinyl, -NR'R", piperydinyl, optionally substituted with hydroxy-group, or is pyrrolidin-1-yl; R6 is hydrogen or -(CH2)nO-lower alkyl, R7 is hydrogen, -C(O)O-lower alkyl, -C(O)-C6H4-halogen, -C(O)-C6H4-lower alkyl, -C(O)-lower alkyl, -C(O)-cycloalkyl, -C(O)-NR'R", -C(O)-(CH2)nO-lower alkyl, -S(O)2-lower alkyl, -(CH2)nO-lower alkyl, -C(O)-pyridin-4-yl, whose ring can contain as substituents lower alkyl, halogen-lower alkyl or pyrrolidin-1-ylmethyl or is -(CH2)n-C(O)-NR'R"; R'/R" independently on each other stand for hydrogen, lower alkyl or -(CH2)n-tetrahydropyran-4-yl, X is -CH2-, -NR'''- or -O-; R''' is hydrogen, -C(O)-lower alkyl, -C(O)O-lower alkyl, -C(O)-C6H4CH3 or benzyl; n is 1 or 2.

EFFECT: increase of composition and treatment method efficiency.

14 cl, 56 ex

FIELD: chemistry.

SUBSTANCE: claimed are novel pyrazole derivatives of formula II or its pharmaceutically acceptable salts, where C ring is selected from phenyl or pyridinyl ring and R2, R2', Rx and Ry are such as said in given description. C ring has ortho-substituent and is optionally substituted in non-ortho positions. R2 and R2' , optionally taken with their intermediate atoms, form condensed ring system, such s indazole ring, and Rx and Ry, optionally taken together with their intermediate atoms, form condensed ring system, such a quinazoline ring.

EFFECT: possibility to use compositions as inhibitors of protein kinases as inhibitors GSK-3 and other kinases and apply them for protein kinase-mediated diseases.

41 cl, 8 tbl, 423 ex

FIELD: chemistry.

SUBSTANCE: in substituted with carbamate groups pyrazolpyridines of general formula (I): R1 stands for group -NR3C(=O)OR4, R2 stands for hydrogen atom or NH2, R3 stands for hydrogen atom or alkyl group with number of carbon atoms from one to four, R4 stands for alkyl group with number of carbon atoms from one to six, as well as to their salt, isomers and hydrates; to methods of their obtaining, medication based on them, as well as to application of said compounds for manufacturing medications for cardio-vascular diseases.

EFFECT: useful biological properties of compounds.

13 cl, 9 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention concerns new histamine receptor blockers in the form of 2,3,4,5-tetrahydro-1H-pyrido-[3,4-b]indoles of the general formula 1 , where: R1 is an aminogroup substitute selected out of optionally substituted C1-C5alkyl; R2i is one or several same or different substitutes selected out of hydrogen, halogen, C1-C3 alkyl, CF3; Ar is phenyl or 5-6-member heterocycle containing 1-2 nitrogen or sulphur atoms in the cycle, unsubstituted or substituted by halogen, C1-C5alkyl, C1-C5alkoxy, substituted aminogroup or trifluormethyl; W is CH2 group optionally substituted CH2CH2 group or optionally substituted CH=CH group.

EFFECT: enhanced antiallergic and autoimmune effect.

4 tbl

FIELD: chemistry.

SUBSTANCE: in novel compounds of formula (I) R1 is selected from , R2 stands for hydrogen or (lower) alkoxy; R3, R4, R5 and R6 are selected each independently from hydrogen, (lower) alkyl, halogenated (lower) alkyl, haloid or cycloalkyl; on condition that R2, R3, R4, R5 and R6 do not all stand for hydrogen; R7, R8 and R9 stand each independently for hydrogen, (lower) alkyl, (lower) alkoxy, (lower) hydroxyalkyl or halogenated (lower) alkyl; on condition that R7, R8 and R9 do not all stand for hydrogen; R10 stands for (lower) alkyl or halogenated (lower) alkyl.

EFFECT: obtaining novel biologically active compounds with improved properties.

16 cl, 38 ex

FIELD: chemistry.

SUBSTANCE: invention pertains to new substituted 2,3,4,5-tetrahydro-1N-pyrido[4,3-b]indoles with general formula 1.1, 1.2 or 1.3, their pharmaceutical salts and/or hydrates with antihistamine activity. In general formulae 1.1, 1.2 or 1.3 radicals assume values given below . In 1.1 compounds, R1 represents a substitute, chosen from hydrogen or unsubstituted C1-C5 alkyl; R2 represents a hydrogen atom or C1-C4 alkyl; R3i represents one or more single or different substitutes, chosen from hydrogen, halogen, C1-C3 alkyl or CF3; n=0 or 1-3; in 1.2 compounds R1 represents a substitute of an amino group, chosen from hydrogen or optionally substituted C1-C5 alkyl; R3 represents one or more single or different substitutes, chosen from hydrogen, halogen, C1-C3 alkyl or CF3, and Ar1 represents an aryl or heterocyclyl, containing at least one carboxyl and/or alkoxycarboxyl substitute or R3i represents a carboxyl and/or alkyloxycarboxyl substitute, and Ar1 represents optionally substituted aryl or heterocyclyl; in 1.3 compounds, R2 represents a hydrogen atom or C1-C4 alkyl; R3i represents one or more single or different substitutes, chosen from hydrogen, halogen, C1-C3 alkyl or CF3, and Ar2 represents optionally substituted aryl or heterocyclyl; k=0 or 1-4; m=1 or 2.

EFFECT: compounds can be used for making drug formulation for treating allergies, autoimmune diseases such as pollen allergy, urticaria, bronchial asthma etc.

17 cl, 10 dwg, 2 tbl,13 ex

FIELD: medicine; cardiology and endocrinology.

SUBSTANCE: thromboplastin formation normalisation in patients suffering from metabolic syndrome (MS) is ensured with four-month hypo-calorie diet, graduated static and dynamic physical activity, preparations dosed 30 mg once a day and Lozartan dosed 50 mg once a day.

EFFECT: normalisation of thromboplastin formation activity and time in patients suffering from MS.

1 ex

FIELD: medicine.

SUBSTANCE: essence of claimed inventions lies in local extravascular introduction of vasculoproliferative compound of rapamicyn, which is carried out by means of device, placed on outer vessel surface. Device represents implanted cuff containing flexible matrix material in form of cylindrical tube, which has opening, corresponding to vessel size. Matrix material contains dispersed in it antiproliferative agent - rapamicyn, which being gradually released from cuff, locally goes into vessel wall.

EFFECT: efficient reduction or prevention of vascular proliferation and hyperplasia of unstriped muscle cells due to prolonged supply of constant concentration of rapamicyn locally into vessel wall.

36 cl, 12 tbl, 14 ex, 20 dwg

FIELD: chemistry, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutically acceptable salts of sulfonic acid bonding of compound Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-(S)Aze-Pab(OMe), where Aze - azetidin-2-carboxilate, Ph - phenyl, Pab-p-amidinobenzylamino and Me - methyl, which are useful as pro-medication of competitive inhibitors of tripsin-like proteases such as thrombin, and, thus, in particular, in treatment of conditions which require thrombin inhibition (for instance, thrombosis), or as anticoagulants. Invention also relates to method of obtaining such salts.

EFFECT: obtaining pharmaceutically acceptable salts of sulfonic acid bonding.

7 cl, 12 tbl, 20 ex, 5 dwg

FIELD: chemistry, pharmaceutics.

SUBSTANCE: invention relates to novel chemical composition from group quaternary ammonium salts of succinic acid, namely, 1-deoxy-1-N-methyl ammonium-D-glucitole succinate (meglumine succinate) .

EFFECT: obtaining chemical composition which acquires ability to impact on complex of pathological changes accompanying sugar diabetes.

4 cl, 6 tbl

FIELD: chemistry.

SUBSTANCE: invention refers to new derivatives of hydrochloride 8-amino-7-(2-hydroxypropyl-1)-1,3-dimethylxanthine of general formula: where . Compounds under this invention display haemorheological activity surpassing that of common pentoxifylline compound. Compounds represent hydrochloride 1,3-dimethy-7-(2-hydroxy-3- piperidinopropyl-1)-8-phenylaminoxanthine or hydrochloride 1,3- dimethy-7-[2-hydroxy-3-(2- chlorophenoxy)-propyl-1]-8- piperazinoxanthine.

EFFECT: production of compounds displaying haemorheological activity.

4 cl, 2 tbl, 4 ex

FIELD: medicine; pharmacology.

SUBSTANCE: new medical product possessing hemorheological and antiplatelet properties represents a dry extract preparation of Amur maackia.

EFFECT: arsenal expansion of the antiplatelet vegetative means, improving rheological properties of blood and an antiplatelet effect.

6 ex, 2 tbl

FIELD: medicine.

SUBSTANCE: method includes application of individually chosen hypohigh-calorie diet, the dosed out physical activities and introduction of Pyoglitazone 30 mg once a day and Valsartane 80 mg, 1 time at the same time of the day. The combined application of a hypohigh-calorie diet, physical activities and Pyoglitazone and Valsartane preparations in the specified dosages allows normalising activity of protein C within three months at patients with metabolic syndrome.

EFFECT: optimisation of activity of protein C at patients with metabolic syndrome.

1 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: method includes application of the hypohigh-calorie diet, the dosed out loads and introduction of Pyoglitazone 30 mg once a day, Irbersartane 150 mg, 1 time in the same time and Lerkanidipine - 10 mg in the morning. The combined application of a diet, physical activities and the given preparations allows normalising fibrinosis level in blood plasma during 3 months.

EFFECT: optimisation of fibrinosis level at metabolic syndrome.

1 ex

FIELD: medicine; pharmacology.

SUBSTANCE: method consists in polymer hydrogel production, containing physiologically active substances, by physiologically active substance immobilisation in cross-linked polymer volume, modified with ovomucoid from duck egg-white; the cross-linked polymer being additionally modified with α-amylase inhibitor from wheat seed; as physiologically active substance heparin or hirudin is used. The cross-linked polymer modified with ovomucoid and α-amylase inhibitor is obtained by chemical modification of polymer with ovomucoid and α-amylase inhibitor mix, in proportion of 0.5 to 15 mg ovomucoid to 1 g swollen cross-linked polymer, and 0.5 to 5.0 mg α-amylase inhibitor to 1 g swollen cross-linked polymer.

EFFECT: hydrogels have anticoagulant activity, are eligible for peroral administration in prevention and treatment for cardiovascular disorders.

2 cl, 20 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: described is novel compound Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-(S)Aze-Pab(2,6-diF)(OH) of formula: or its pharmaceutically acceptable salt.

EFFECT: using compound as active ingredient for preparation of medicine for treatment of condition, which demands inhibiting of trombone.

12 cl, 7 ex

FIELD: chemistry.

SUBSTANCE: description is given of a compound with general formula Ia , where A and Q each represents H and where the asymmetrical centre in position 3 can be in optically active form, R represents formula Ib and where R1 is an alkyl, containing 1 to 4 carbon atoms, in form of a free base or in form of a pharmaceutical acidic additive salt and a pharmaceutical composition, capable of reducing intraocular pressure, based on this compound. Description is also given of the method of treating glaucoma or myopia and use of formula Ia compound for making medicinal preparations for treating glaucoma and myopia.

EFFECT: new method of treating glaucoma or myopia.

6 cl, 6 ex

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