Drugs for disorders of the cardiovascular system (A61P9)

A   Human necessities(312083)
A61P9                 Drugs for disorders of the cardiovascular system(2552)
2-aminopyrasine derivatives as csf-1r kinase inhibitors // 2642777
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group; R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl; n is 1; X is NH; V is -N=, W is -C(Z)=; Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl; ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group; [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3; x is 0 or 1; Alk1 is an unsubstituted C1-3 alkylene group; X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3; R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring; and R17 represents a hydrogen atom; where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring; R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group; ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or prevention of diseases or disorders mediated by CSF-1R kinase, as well as application of the said compounds for preparation of a medicament useful for treatment of such diseases.EFFECT: increased application efficiency.18 cl, 59 ex

Concentrated therapeutic phospholipide compositions // 2642653
FIELD: pharmacology.SUBSTANCE: composition for treatment or prevention of cardiometabolic disorders, a metabolic syndrome, neurodegenerative disorders comprises a concentrated therapeutic phospholipid extract comprising compounds of Formula I wherein the total amount of the phospholipid compounds of Formula I from the extract is in a concentration of 60 wt % to 90 wt % of the total weight of the composition and the extract includes astaxanthin; to a capsule containing a concentrated therapeutic extract of krill oil that contains the phospholipid compounds of Formula I and the extract includes astaxanthin; to application of a composition that includes a concentrated therapeutic phospholipid extract containing compounds of Formula I for preparation of therapeutic compositions for serum triglyceride levels lowering; to application of a concentrated therapeutic phospholipid extract that contains compounds of Formula I for preparation of pharmaceutical compositions for treatment of cardiovascular diseases.EFFECT: increased mass percentage of phospholipids in the composition.20 cl, 35 dwg, 2 tbl, 7 ex

System delivery and regulated expression of paracrine genes for treatment of cardiovascular and other diseases // 2642605
FIELD: medicine.SUBSTANCE: group of inventions can be used to treat heart failure with congestive heart failure (CHF), diabetes or prediabetes in vivo in a patient in need thereof. To this end, a vector is administered to a subject comprising a nucleic acid encoding a paracrine polypeptide or a peptide selected from the group consisting of cardiotonic peptide, urocortin-2 (UCn-2), urocortin-1 (UCn-1), urocortin-3 (UCn-3), brain natriuretic peptide and prostacyclin synthase, wherein the said nucleic acid encoding a paracrine polypeptide or peptide is operably linked to a promoter, wherein the vector is an adeno-associated virus (AAV), and wherein the paracrine polypeptide or peptide is expressed in a cell.EFFECT: group of inventions provides treatment or improvement of CHF, diabetes or prediabetes in a patient.24 cl, 20 dwg, 3 tbl
ethod for treatment of alcoholic cardiomyopathy // 2642298
FIELD: medicine.SUBSTANCE: method includes introduction of metabolitotropic cardioprotector represented by (S)-2,6-diaminohexanoic acid 3-methyl-1,2,4-triazolyl-5-thioacetate in a dose of 100 mg/kg a day for 30 days. Invention application allows to increase therapeutic efficiency due to cardioprotective activity and low toxicity of (S)-2,6-diaminohexanoic acid 3-methyl-1,2,4-triazolyl-5-thioacetate.EFFECT: increased efficiency of treatment.2 tbl,1 ex
ethod for selection of perindopril dosage forpatients with ischemic heart disease on background of arterial hypertension // 2642284
FIELD: medicine.SUBSTANCE: polymorphism of the AGTR2 rs1403543 gene is determined. In case of detection of a homozygous version of GG, perindopril dose is 1.3 times lower than in individuals with allele version AA.EFFECT: increased therapy effectiveness and safety.4 tbl, 3 ex

Cells derived from cardial tissue // 2642282
FIELD: biotechnology.SUBSTANCE: invention relates to a method for improving the contractility of the heart, increasing the capillary density, or reducing myocardial hypertrophy in a patient with a damaged myocardium, which can be used in medicine. This method includes an administration of a purified cell pool, derived from cardial tissue of a human, where these cells do not express telomerase, heavy chain of myosin, CD31, CD45 and CD16 and express GATA4, Nkx2.5, CD105, CD90, CD59 and CD54.EFFECT: invention allows you to effectively improve the contractility of the heart, increase capillary density or reduce myocardial hypertrophy in patients after acute myocardial infarction.16 cl, 39 dwg, 30 tbl, 20 ex
Spiro-fused piperidine derivatives for application as inhibitors of external medullar layer potassium channel // 2642066
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula I .EFFECT: new compounds of formula I are obtained which are inhibitors of the ROMK channel and which can be used in hypertension treatment.11 cl, 5 tbl, 85 ex

Therapeutic application of compounds // 2640596
FIELD: pharmacology.SUBSTANCE: invention refers to the application of a compound of formula R1-COOH (I), where R1 is an alkyl group with a main chain of 7-11 carbon atoms, possibly branched in any position of the carbon atom in the main chain, where branching is a side C1-6 alkyl group. The alkyl group of the main chain and/or the side alkyl groups optionally contain one or more heteroatoms. The specified compound is selected from 4-ethyl octanoic acid, 2-butyl octanoic acid, 4-methyl nonanoic acid and 3-methyl undecanoic acid or its pharmaceutically acceptable salt, amide or ester, for treatment or prevention of disease or biomedical state, selected from disorders associated with cramps.EFFECT: increased efficiency of the composition and treatment method.2 cl, 9 dwg, 3 tbl
Pyridine derivative // 2640588
FIELD: pharmacology.SUBSTANCE: invention relates to a pyridine derivative of formula (I) , a prodrug thereof, wherein A is a single bond or an oxygen atom; R1 represents a nitrogen atom or CH; one of X1-X5 is a nitrogen atom, and the remaining four are CR2; R2 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, an alkynyl group having 2 to 6 carbon atoms, a halogen atom, a trifluoromethyl group, a difluoromethyl group, a cyano group, an alkylcarbonyl group having 2 to 7 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, a nitro group, an amino group, a dialkylamino group having 1 to 6 carbon atoms which optionally can form a ring, a formyl group, an alkoxy group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group, a phenyl group, a cyclohexyl group and a halogen atom), an alkylthio group having 1 to 6 carbon atoms, a phenyl a group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom) or a phenoxy group (which may optionally have one or more substituents selected from an alkyl group having 1-6 carbon atoms, an alkoxy group having 1-6 carbon atoms, and a halogen atom), provided that when two CR2 are located side by side, two R2 substituents can be optionally combined with cycle formation; R3 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group, an amino group, a dialkylamino group having 1 to 6 carbon atoms which can optionally form a ring, an imidazole ring, a pyrazole ring, a pyrrolidine ring, a piperidine ring, a morpholine ring and a piperazine ring (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms and alkylsulfonyl group containing from 1 to 6 carbon atoms), an alkenyl group having 2 to 6 carbon atoms, an alkynyl group having 2 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group and a halogen atom), an alkylcarbonyl group having 2-7 carbon atoms, an alkylthio group having 1-6 carbon atoms, an alkylsulfinyl group having 1-6 carbon atoms, a halogen atom, a trifluoromethyl group, a difluoromethyl group, a cyano group, a phenyl group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a pyridyl group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a phenoxy group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a carboxyl group, or -CO2 R5; R4 represents a carboxyl group, a tetrazolyl group, -CONHSO2R5, -CO2R5 or any of the following substituents: , provided that when R3 represents an alkyl group having 1 to 6 carbon atoms substituted by a hydroxyl group, and when R4 represents a carboxyl group, then R3 and R4 can optionally be combined to form a lactone cycle; R5 in R3 and R4 each independently represents an alkyl group having 1 to 6 carbon atoms; Z is any of the following substituents, designated as Z1-Z7 (their meanings are defined in claim 1) that can be used to treat or prevent diseases associated with URAT1 such as gout, hyperuricemia, hypertension, kidney diseases such as interstitial nephritis, diabetes, arteriosclerosis and Lesch-Nyhan syndrome.EFFECT: compound application efficiency increase.23 cl, 55 tbl, 303 ex
5-potassium hydroxinicotinate with cardioprotective activity // 2640580
FIELD: pharmacology.SUBSTANCE: invention relates to a potassium salt of 5-hydroxynicotinic acid of the formula C6H4NO5K, , which has cardioprotective activity.EFFECT: increased compound activity.2 tbl, 1 ex
Bicyclic compound // 2640416
FIELD: pharmacology.SUBSTANCE: in the general formula (1) (1), A is an unbranched C1-C3 alkylene group, wherein one methylene group is optionally substituted with O or S; n is an integer from 3 to 5; each of X1 and X2 is independently CH or N; each of W1 and W2 is independently a carboxyl group or W1 is a carboxyl group and W2 is a tetrazolyl group; V is a linear or branched C1-C8 alkylene group in which one methylene group is optionally substituted by O or S; R is a group selected from the following , , where R1, R2, R3, R4 and R5 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group which may have a substituent group, a C1-C6 alkoxy group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkoxy group, a halogen C1-C4 alkyl group, a halogen C1-C4 vinyl group which may have a substituent group, an ethynyl group which may have a substituent group, a phenyl group which may have a substituent group on the aromatic ring, a phenoxy group which may have a substituent group on the aromatic ring, a benzyl group, which may have a substituent group on the benzene ring, a phenethyl group which may have a substituent group on the benzene ring, a benzyloxy group which may have a substituent group on the benzene ring, a benzylsulfanyl group which may have a substituent group on the benzene ring, a benzylamino group which may have a substituent group on the benzene ring, a phenyloxymethyl group which may have a substituent group on the benzene ring, a phenylsulfanylmethyl group which may contain a substituent group on the benzene ring, or a phenylaminomethyl group which may have a substituent group on the benzene ring, wherein the substituent group is indicated in the claims, m is an integer of 1 or 2 and each of Y1 and Y2 independently represents methylene, O or S, provided that they both do not represent S.EFFECT: compounds can be used to prevent or treat disorders associated with soluble guanylate cyclase, such as hypertension, pulmonary hypertension, heart failure, endothelial dysfunction, atherosclerosis, peripheral vascular disease, angina pectoris, thrombosis, myocardial infarction, erectile dysfunction or impaired renal function.9 cl, 41 tbl, 213 ex

Vaccine // 2640258
FIELD: biotechnology.SUBSTANCE: vaccine to reduce cholesterol levels is presented, including two proprotein convertase fragments subtilisin/kexin type 9 (PCSK9), connected to a pharmaceutically acceptable carrier, in which these two fragments are: PEEDGTRFHRQA and SIPWNLERITP; EEDGTRFHRQASK and SIPWNLERITP; EEDGTRFHRQASK and SIPWNLERIT; or EEDGTRFHRQAS and SIPWNLERIT. Application of the specified vaccine for treatment and/or prevention of disorders caused by hyperlipidemia, hypercholesterolemia and/or atherosclerosis, preferably for cardiovascular disease, stroke or peripheral vessels disease is presented.EFFECT: group of inventions allows to decrease total cholesterol when using these combinations of fragments more efficiently than by using each fragment separately.8 cl, 2 dwg, 4 tbl, 3 ex

Bispecific anti-vegf/anti-ang-2 antibodies // 2640253
FIELD: biotechnology.SUBSTANCE: invention relates to a bispecific antibody specifically binding to a human vascular endothelial growth factor-VEGF and human angiopoietin-2-ANG-2, a pharmaceutical composition containing it, as well as a method for its preparation. Also a nucleic acid encoding the above antibody and a vector or host cell containing the aforementioned nucleic acid are disclosed.EFFECT: invention allows effective treatment of cancer and/or vascular diseases.12 cl, 19 dwg, 18 tbl, 20 ex
Pharmaceutical compositions of substituted quinazolinones // 2640115
FIELD: pharmacology.SUBSTANCE: composition according to this invention contains an active ingredient selected from a series of substituted quinazolinones and their pharmaceutically acceptable salts, stereoisomers, tautomers or hydrates, and additionally contains approximately 10 wt % to approximately 85 wt % of microcrystalline cellulose; approximately 4.0 wt % of sodium starch glycolate; approximately 0.5 wt % of magnesium stearate; and approximately 2.5 wt % of colloidal silicon dioxide; and prepared for peroral introduction and immediate release.EFFECT: creation of new compounds that increase the bioavailability of substituted quinazolinones while maintaining stability, possibility of treatment and prevention of the abovementioned diseases.15 cl, 1 tbl, 1 ex
Liquid composition // 2640023
FIELD: pharmacology.SUBSTANCE: invention is an oral bio-available non-aqueous liquid composition containing at least 7 wt % of propylene glycol in the total composition weight, a cardiotonic means, or angiotensin-converting enzyme inhibitor, or combination of cardiotonic means and angiotensin-converting enzyme inhibitor. Invention discloses a method for obtaining the composition described above, by mixing at least 7 wt % of propylene glycol by the total composition weight with a cardiotonic means, or angiotensin-converting enzyme inhibitor, or a combination of cardiotonic means with angiotensin-converting enzyme inhibitor.EFFECT: treatment of heart disease and hypertension.34 cl, 11 dwg, 17 tbl, 2 ex
Phenyl derivative // 2639875
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the general formula (I) having a high antagonistic activity with respect to human S1P2, and can be used to prepare a drug for treatment of a disease mediated by S1P2, such as a disease caused by vasoconstriction, fibrosis and respiratory disease.EFFECT: compound application efficiency increase.14 cl, 2 tbl, 9 ex
Hetero-aromatic methylic derivative of cyclic amine // 2639869
FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the formula (IA), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; Y is any structure from the following group of formulas (a); n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group; R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 an alkyl group; or a pharmaceutically acceptable salt thereof. The invention also relates to a compound represented by the formula (I), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; any one of Y1 and Y2 is a nitrogen atom, and the other is CH; n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group;R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 alkyl group; or a pharmaceutically acceptable salt thereof. The compounds of the invention are intended for the production of a pharmaceutical composition having antagonistic activity against OX1 and OX2 orexin receptors.EFFECT: hetero-aromatic methyl derivative of cyclic amine, which has antagonistic activity against OX1 and OX2 orexin receptors.9 cl, 6 tbl, 85 ex

Azadecalins condensed with heteroarylketones - glucocorticoid receptor modulators // 2639867
FIELD: medicine.SUBSTANCE: invention provides azadecalin compounds of formula ondensed with heteroarylketones, which are modulators of glucocorticoid receptors. The radicals and symbols in formula I have the definitions given in the claims. In some embodiments of the present invention, pharmaceutical composition is provided comprising a pharmaceutically acceptable excipient and a compound of formula (I). In some embodiments of the present invention, a method is provided for modulation of glucocorticoid receptors that comprises glucocorticoid receptors contacting with a compound of formula I, thereby modulating the glucocorticoid receptors, as well as a method for treatment of diseases by glucocorticoid receptors modulation, which comprises administration of a therapeutically effective amount of a formula I compound to a subject in need thereof, as a result, disease treatment takes place.EFFECT: increased efficiency of treatment.24 cl, 2 dwg, 1 tbl, 22 ex

Pharmaceutical combined drug // 2639818
FIELD: pharmacology.SUBSTANCE: invention relates to a drug for prevention or treatment of cardiovascular diseases comprising a granulated portion of fimsartan and a mixed portion of rosuvastatin, as well as meglumine.EFFECT: excellent effect in treatment of cardiovascular disease due to improved dissolution and dilution of the active substances, which provides better bioavailability and safety of the drug.19 cl, 5 ex, 3 tbl, 1 dwg
ethod for endothelioprotection in adma-similar gestosis model by arginase ii inhibitor // 2639415
FIELD: pharmacology.SUBSTANCE: method involves reproduction of gestosis in laboratory pregnant Wistar rats by daily intraperitoneal administration of the NO-synthase inhibitor L-NAME from day 14 to day 20 of pregnancy at a dose of 25 mg/kg/day. At that, correction of endothelial dysfunction is performed daily by intragastric administration of a selective inhibitor of arginase II-KUD975. Inhibitor administration is performed 30 minutes prior to the administration of L-NAME at a dose of 1 mg/kg of animal body weight.EFFECT: pronounced correction of dysfunction under the conditions of specific mechanisms of the pathological process in pregnant women, with elimination of side effects typical for low- and nonselective arginase inhibitors.1 ex

ethods and compositions for treating inflammation and ischemic damage // 2638807
FIELD: pharmacology.SUBSTANCE: following are proposed: method for treating a subject suffering from ischemic damage or an acute ischemic event, comprising administering cysteamine, cystamine or a salt thereof, simultaneously with or immediately after the ischemic event, in an amount effective to reduce the ischemic damage, wherein the subject does not suffer from hypercholesterolemia or diabetes of II type, where the administration of cysteamine, cystamine or a salt thereof leads to an increase in adiponectin level with low molecular weight (LMW) (versions) in subjects; a method for increasing (versions) adiponectin levels with LMW in the mentioned patient group comprising contacting the subject with an effective amount of cysteamine, cystamine or a salt thereof (versions); the use of cysteamine, cystamine or a salt thereof in the manufacture of a medicament in the above mentioned treatment of a subject suffering from the acute ischemic event and not suffering from hypercholesterolemia or diabetes of II type.EFFECT: levels of all adiponectin multimers are increased, within 1 hour after cysteamine exposure in the blood serum, LMW of adiponectin was rapidly and significantly increased, cysteamine administration 2 hours before the ischemic stroke significantly reduced the infarction area and the number of ischemic damages.28 cl, 18 dwg, 2 tbl, 3 ex

Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods for application // 2638552
FIELD: pharmacology.SUBSTANCE: invention relates to pyrazol-4-yl-heterocyclylcarboxamide compounds of Formula I , including their stereoisomers, tautomers and pharmaceutically acceptable salts, wherein X is a thiazolyl, pyrazinyl, pyridinyl or pyrimidinyl group, R1 and R2 have the meanings indicated in the claims. The compounds of formula I are useful for Pim kinase inhibition and for treatment of disorders such as cancer mediated by Pim kinase. Methods for application of formula I compounds for in vitro, in situ and in vivo diagnosis, prevention or treatment of such diseases in mammalian cells or acssociated pathological conditions are disclosed.EFFECT: increased efficiency of treatment.26 cl, 4 tbl, 528 ex
Pyrazolo [3,4-c] pyridines and methods of application thereof // 2638116
FIELD: pharmacology.SUBSTANCE: subject of the invention is pyrazolo [3,4-c] pyridines of the formula I ,including their stereoisomers, geometric isomers, tautomers and pharmaceutically acceptable salts, wherein R1 and R2 have the values disclosed in the claims. These compounds are useful for inhibiting Pim-kinases and for treating disorders such as cancer, mediated by Pim-kinase. Methods for using compounds of formula I for in vitro, in situ and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells or related pathological conditions are disclosed.EFFECT: increased application effeciency.4 cl, 3 tbl, 328 ex
Enantiomers-2-hydroxy-derivatives of fatty acids // 2637937
FIELD: pharmacology.SUBSTANCE: invention relates to the enantiomer [-] of the formula: [-]NaOOC-HOCH-(CH2)6-(CH=CH-CH2)1-(CH2)6-CH3 and a pharmaceutical composition for treatment of a pathology caused by an abnormally low level of sphingomyelin and/or an abnormally high level of dihydrofolate reductase (DGFR) containing a therapeutically effective amount of an enantiomer of the following formula: [-]HOOC-HOCH-(CH2)6-(CH=CH-CH2)1-(CH2)6-CH3 and/or at least one of its pharmaceutically acceptable salts and, optionally, a pharmaceutically acceptable carrier. The invention also relates to a method for treatment of pathologies, the common etiology of which is an abnormally low level of sphingomyelin, and/or an abnormally low level of glycophelial acid protein (GPAP) and/or an abnormally high level of dihydrofolate reductase (DHFR), comprising administration of a therapeutically effective amount of the enantiomer of the following formula: [-]HOOC-HOCH-(CH2)6-(CH=CH-CH2)1-(CH2)6-CH3 and/or at least one of its pharmaceutically acceptable salts or composition comprising the said enantiomer and/or at least one of its pharmaceutically acceptable salts to the patient.EFFECT: increased efficiency of treatment.9 cl, 10 dwg, 5 tbl, 9 ex

yocardial infarction treatment using tgf-beta antagonists // 2637088
FIELD: medicine.SUBSTANCE: TGF-β antagonist is introduced, which is an antibody containing the VH-domain of PET1073G12 (SEQ ID NO: 2) and the VL-domain of PET1073G12 (SEQ ID NO: 7). Introduction is carried out within 72 hours from the onset of myocardial ischemia.EFFECT: reduced fibrosis, improved remodeling and myocardial function.20 cl, 2 tbl, 30 dwg, 6 ex
Ubiquinol composition for parenteral administration and method for its production // 2635993
FIELD: pharmacology.SUBSTANCE: ubiquinol composition is intended for treatment of cardiovascular system diseases and includes a medicinal substance (ubiquinol), surfactants, anti-oxidants (direct and indirect) and solvents, allowed for parenteral administration.EFFECT: composition and the method allow to obtain a storage stable ubiquinol solution suitable for injectable administration.10 cl, 6 dwg, 1 tbl, 24 ex

Composition for treatment of hypertension and/or fibrosis // 2635564
FIELD: pharmacology.SUBSTANCE: invention relates to the compound of the formula (I) or its pharmaceutically acceptable salt. The invention also relates to a pharmaceutical composition having effects that reduce blood pressure and/or antifibrotic effects comprising a compound of the invention or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient. The compound of the invention is intended for therapeutic treatment of hypertension or prehypertension, prophylactic treatment of fibrosis, therapeutic treatment of fibrosis, therapeutic treatment of hypertension and fibrosis, and treatment of prehypertension and fibrosis in a subject.EFFECT: reduces blood pressure, has antifibrotic effects.16 cl, 12 dwg, 3 ex
Bruton's tyrosine kinase inhibitors // 2634723
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of general formula I: , as well as to pharmaceutical compositions based thereon, and to application for treatment of inflammatory or autoimmune diseases associated with aberrant B-cell proliferation.EFFECT: new compounds with inhibitory activity against Btk are obtained.27 cl, 2 tbl, 34 ex
New solid forms of type 5 phosphodiesterase inhibitors // 2634713
FIELD: pharmacology.SUBSTANCE: invention relates to new solid forms of type 5 phosphodiesterase inhibitors (PDE-5), namely to crystalline compounds consisting of a tadalafil of formula T and coformer Y in which Y is selected from 3-hydroxybenzoic acid, 2,3-dihydroxybenzoic acid, 2,5-dihydroxybenzoic acid, 3,4,5-trihydroxybenzoic acid, D-malic acid and L-tartaric acid, especially to complex cocrystals and their solvates, as well as to pharmaceutical compositions containing the above compounds as a useful active ingredient.EFFECT: high permanent storage stability.14 cl, 20 dwg
V1a-receptors agonists // 2634617
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I) , their salts, pharmaceutical compositions, and their use as vasopressin V1a-receptor agonists in the treatment of, for example, complications of cirrhosis, including bacterial peritonitis, HRS2 (type II hepatorenal syndrome) and refractory ascites.EFFECT: increased efficiency of composition application.39 cl, 3 tbl

ethod for treatment of lower limbs chronic arterial insufficiency of i-iia degree // 2634419
FIELD: medicine.SUBSTANCE: for treatment of lower limbs chronic ischemia, lumbar chemical sympathectomy is carried out by introducing an ethanol solution. The basal level of the transcutaneous oxygen tension and the ankle-brachial index (ABI) are determined. With basal ABI less than 0.90, the need for limb revascularization is determined. With basal ABI of 0.90 or more, a stress test is performed, with a decrease in the load ABI of less than 0.90, or 15% or more compared to basal, sympathectomy is performed. The volume of ethyl alcohol 70% for sympathectomy is determined by the height and body mass index of the patient. After 1 day, the transcutaneous oxygen tension is determined, with an increase of 15% or more from the basal level, therapy including calf muscles electrostimulation within 60 minutes by pulses of less than 0.05 W, stimulation rate of 60-75 muscle contractions per minute is recommended. If no increase by 15% or more from the basal level in the transcutaneous oxygen tension is observed after chemical sympathectomy, indications for revascularization are determined, the transcutaneous oxygen tension is examined monthly.EFFECT: method allows to increase the treatment effectiveness for patients with lower limbs chronic ischemia, due to the timely detection of patients with clinically not-manifested lower limbs chronic ischemia.1 dwg, 1 ex
ethod for preventing postinfarction cardiac remodeling in experiment // 2634375
FIELD: medicine.SUBSTANCE: method comprises dressing the upper third of the left coronary artery and administering the Alloplant biopreparation into the stenosed artery circulation. The administration is carried out by intramyocardial injection of 3.0 mg of a biopreparation diluted in physiological saline. Injections are performed immediately after stenosing the artery at 6 points, by 0.5 mg each.EFFECT: effective stimulation of endogenous mechanisms of myocardial regeneration, preventing postinfarction cardiac remodeling.2 tbl, 1 ex

Compositions of the complexes of omega-3 fatty acids // 2633862
FIELD: pharmacology.SUBSTANCE: invention is a method of treating a cardiovascular disease or condition in a patient comprising administering to said patient, orally or parenterally, a pharmaceutical composition that independently forms micelles upon contact with an aqueous medium to form spherical micelles that have an average diameter of 1 mcm to 10 mcm And ensure the absorption of omega-3 fatty acid esters practically independently of any food influence, or stable micelles pre-formed from mentioned composition in an amount therapeutically effective to reduce one or more of the symptoms of said cardiovascular disease or condition. Mentioned pharmaceutical composition comprises: (a) from 60% (w/w) to 85% (w/w) of at least one omega-3 fatty acid ester selected from the group consisting of an all-Z omega-3)-5,8,11,14,17-eicosapentaenoic acids (EPA), ester (all-Z omega-3)-4,7,10,13,16,19-docosahexaenoic acids (DHA), hexadecatrienic acid ("NTA" or 16:3 (n-3) or all-Z-7,10,13-hexadecatrienoic acid), α-linolenic acid ("ALA" or 18:3 (n-3) or all-Z-9,12,15-octadecatrienoic acid), stearidonic acid ("SDA" or 18:4 (n-3) or all-Z-6,9,12,15-octadecatetraenoic acid Slots), eicosatrienoic acid ("ETA" or 20:3 (n-3) or all-Z-11,14,17-eicosatrienoic acid), eicosatetraenoic acid ("ETA" or 20:4 (n-3)), ("HPA" or 21:5 (n-3) or all-Z-6,9,12,15,18-geyeykozapentaenoic acid), docosapentaenoic acid ("DPA", or clupanodonic acid, or 22:5 (n-3), or all-Z-7,10,13,16,19-docazapentenoic acid); Tetrakosapentaenoic acid (24:5 (n-3) or all-Z-9,12,15,18,21-tetrakosapentaenoic acid) and tetracosahexaenoic acid (nisic acid or 24:6 (n-3) or all-Z-6 , 9,12,15,18,21-tetracosahexaenoic acid); And (b) a surfactant which contains, in combination, at least one non-ionic polyoxyethylene glycol and sorbitan alkyl ester (polysorbate) selected from the group consisting of polyoxyethylene (20) sorbitan monolaurate (polysorbate 20), polyoxyethylene (20) sorbitan monopalmitate (Polysorbate 40), polyoxyethylene (20) sorbitan monostearate (polysorbate 60), and polyoxyethylene (20) sorbitan monooleate (polysorbate 80); and a block copolymer of polyethylene glycol and polypropylene glycol having the formula [(HO[(HO(C2H4O)64(C3H6O)37(C2H4O)64H] (Poloxamer 237); wherein said polysorbate is present in an amount of 0.5% (wt/wt) to 5% (wt/wt) of smentioned composition. This combination of surfactants is effective for forming said stable micelles upon contact with said aqueous medium, and wherein said composition for the oral or parenteral administration that self-forms micelles when administered to a human in equal dosage provides substantially the same bioavailability when administered with food or without food to the person who needs it. The mentioned composition, which independently forms micelles, independently forms micelles in an aqueous medium, thereby forming spherical micelles having an average diameter of from 1 mcm to 10 mcm, which ensure the absorption of said omega-3 fatty acid esters practically independently of any food effect; and wherein said pharmaceutical composition is administered orally or parenterally in an amount that is therapeutically effective to reduce one or more of the symptoms of said cardiovascular disease or condition..EFFECT: invention provides compositions that are less influenced by food, have high efficacy at low doses, minimize and eliminate an unpleasant odor, taste or eructation in the patient.89 cl, 5 ex, 5 tbl, 4 dwg
ethod for treatment of lower limbs ischemic diseases // 2633487
FIELD: medicine.SUBSTANCE: method includes intramuscular administration of a suspension of autologous peripheral blood stem cells (PBSC) into several points of the muscle mass in the ischemic zone. Three to four days after PBSC administration, vascular endothelial growth factor (VEGF) is introduced into the same muscular mass, depth, place of injection in the muscle mass and the fact of PBSC and VEGF spread is determined and fixed by ultrasound control.EFFECT: use of the invention makes it possible to reduce the number of complications with introduction of peripheral blood stem cells.2 ex

ethods and compositions for raynaud disease treatment // 2633236
FIELD: medicine.SUBSTANCE: semi-solid composition of prostaglandin E1 for topical administration to a subject in need is used, wherein the treatment method comprises topical application of an effective amount of this prostaglandin E1 composition to the surface of the affected body part. At that, the total daily dose of prostaglandin E1, applied to the surface of the affected body part, is approximately 0.5 to 5.7 mg. Prostaglandin E1 for production of such semi-solid composition, which may also include suitable thickeners and penetration enhancers such as dodecyl-2(N,N-dimethylamino)-propionate (DDAIP). Preferably, the semi-solid topical composition has a room temperature at the time of application to the affected body part surface to avoid vasospasm triggering or exacerbation characteristic of the Raynaud phenomenon secondary to systemic sclerosis. The total daily dose of the semi-solid composition can be applied as needed or divided by 2-4 times a day.EFFECT: no complications of systemic administration and the desired relief of the secondary Raynaud phenomenon in systemic sclerosis, improvement of quality of life, patient functions, reduction of finger ulceration, prevention of new finger ulcers, improvement of existing ulcers healing.39 cl, 2 dwg, 4 tbl, 2 ex

Dyetered diaminopyrimidine compounds and pharmaceutical compositions containing such connections // 2632907
FIELD: pharmacology.SUBSTANCE: invention relates to novel deuterated diaminopyrimidines of the general formula (I) and their pharmaceutically acceptable salts. In the general formula (I) R1a, R1b, R1c, R2a, R2b, R2c, R3, R4, R6, R7, R9, R10, R11, R12, R13a, R13b, R13c, R14a, R14b, R14c, R15a, R15b, R15c, R16, R17a, R17b, R18a, R18b, R19a, R19b, R20a and R20b independently hydrogen or deuterium; R5 is hydrogen, deuterium or halogen, R8 Represents a halogen; Provided that at least four of R1a, R1b, R1c, R2a, R2b, R2c, R3, R12, R13a, R13b, R13c, R14a, R14b, R14c, R19a, R19b, R20a or R20b are deuterium. The invention also relates to a process for the preparation of compounds of general formula (I) by reacting compound A6 with compound XV and to intermediates A6 and XV. In this case, in compound A6 R10, R11, R12, R13a, R13b, R13c, R14a, R14b, R14c, R15a, R15b, R15c, R16, R17a, R17b, R18a, R18b, R19a, R19b, R20a or R20b are independently selected from deuterium or hydrogen and at least one of them is deuterium; In compound XV R1a, R1b, R1c, R2a, R2b, R2c, R3, R4, R6, R7, R9 are independently selected from hydrogen or deuterium and at least one of them is deuterium; and R5 is hydrogen, deuterium or halogen; and R8 represents a halogen; X2 is selected from F, Cl, Br, I.EFFECT: compounds have ALK protein kinase inhibitory properties and can be used to treat or prevent cancer, impair cell proliferation, cardiovascular diseases, inflammation, infection, autoimmune diseases, organ transplantation, viral diseases, cardiovascular diseases or metabolic diseases.18 cl, 4 dwg, 1 tbl
Pyrazole derivative // 2632884
FIELD: pharmacology.SUBSTANCE: in the above formula , A represents a phenyl group which may be unsubstituted or substituted by 1 to 3 Q groups which are identical or different and are selected from the group consisting of a halogen atom, C1-6alkyl, C3-7cycloalkyl, C1-6haloalkyl, phenyl, -O-R2 and -O-C1-6haloalkyl; X and Z are CH and Y is a nitrogen atom; R is a hydrogen atom; R1 is a hydrogen atom and R2 is a hydrogen atom or C1-6alkyl group.EFFECT: compound has an inhibitory effect on xanthine oxidase, is well suited for treatment or prevention of diseases associated with xanthine oxidase such as gout, hyperuricemia, tumor lysis syndrome, stones in the urinary tract, hypertension, dyslipidemia, diabetes, cardiovascular disease, kidney disease, respiratory tract disease, autoimmune diseases, inflammatory bowel disease.10 cl, 7 tbl, 112 ex

Sustained-release pharmaceutical composition containing asparaginates // 2632715
FIELD: pharmacology.SUBSTANCE: sustained-release pharmaceutical composition includes potassium asparaginate hemihydrate, magnesium asparaginate dihydrate, matrix-forming polymer, which is an Eudragit polymer, ethyl cellulose, polyvinylpyrrolidone or a combination thereof, a disintegrant such as aerosil, methylcellulose, hydroxypropylmethylcellulose or hydroxypropyl cellulose, an antifriction substance that is talc or starch in the amounts indicated in the claims. The composition is in the form of a solid dosage, preferably in the form of a pill. The composition is characterized by an immediate onset of release and a prolonged, sustained maintenance of the active substances concentration for 12 hours. The pill core can be coated. What is also presented is a method for pharmaceutical composition production.EFFECT: expanded arsenal of drugs used in cardiology and sports medicine, the composition of the invention provides a reduction in the frequency of drug intake, its manufacturing technology is economically advantageous.23 cl, 2 dwg, 1 tbl, 2 ex
Delayed release pharmaceutical composition containing asparaginates // 2632713
FIELD: pharmacology.SUBSTANCE: drug can be used in therapy, in particular in cardiology, and in sports medicine. Preferably, the pharmaceutical composition for oral use in the form of a pill contains hemihydrate, magnesium aspartate dihydrate, microcrystalline cellulose, sodium croscarmellose, aerosil, stearic acid in the potassium asparaginate; the pill shell contains the pH-dependent polymer Eudragit, polyethylene glycol, talc, titanium dioxide. A method for manufacture of a tablet with asparaginates is also described. The composition is characterized by delayed, after 2 hours, release of active ingredients and subsequent rapid release of these active substances in a therapeutically active concentration within 20-30 minutes.EFFECT: reduced side effects on the gastric mucosa.16 cl, 11 dwg, 1 tbl, 11 ex
Complex of zinc acetate with 1-propargylimidazol with anti-hypoxic activity // 2632682
FIELD: pharmacology.SUBSTANCE: invention is a complex of bis(1-propargylimidazole)zinc diacetate, which has antihypoxic properties under conditions of acute hypoxia (hypobaric, hemic, hypoxia with hypercapnia).EFFECT: antihypoxic effect is superior to that of etimerzole, mexidol, nooglutil and hypoxen.1 tbl
ethod for treatment of patients with arterial hypertension // 2632619
FIELD: medicine.SUBSTANCE: once a day, during breakfast, a colloidal preparation of Cardio Support, 3-5 ml, diluted in 200 ml of drinking catholyte with a total mineralization of 300 to 600 ppm with a redox potential of -200 mV to -700 mV and a hydrogen pH from 8 to 11 is introduced. Before lunch, an exercise complex is performed for 15 minutes, manual classical massage or mechanical massage of the cervical collar zone is performed for 15 minutes, repeated exercise complex is performed for 15 minutes. Further, a contrast shower of the upper and lower limbs and the whole body is performed, as well as an anolyte shower or rubbing of the whole body with an anolyte with a redox potential of +450 mV to +800 mV and a pH of 6.0 to 4.0 for 5 minutes, respectively, with anolyte temperature of +37°C - +40°C. Next, a catholyte bath or a shower with a redox potential of -200 mV to -700 mV and a hydrogen pH of 8 to 11 is performed for 15 minutes with a catholyte temperature of +37°C - +40°C. After that, rubbing and resting take place for 15 minutes, then an exercise complex is performed for 15 minutes, manual classical massage or mechanical massage of the neck-collar zone is performed for 15 minutes and repeated exercise complex is performed for 15 minutes. Then again, a catholyte bath or catholyte shower, rubbing and resting take place for 15 minutes. Before eating, 200 ml of drinking catholyte is introduced into the meal. Between lunch and dinner, an exercise complex is performed for 15 minutes, manual classical massage or mechanical massage of the cervical collar zone is performed for 15 minutes, repeated exercise complex is performed for 15 minutes. Then a contrast shower of the upper and lower limbs and the whole body is performed, as well as an anolyte shower or rubbing of the whole body with an anolyte for 5 minutes. Then a catholyte bath or a catholyte shower is performed. After bath, rubbing and resting take place for 15 minutes. After that, once again, an exercise complex is performed for 15 minutes, manual classical massage or mechanical massage of the neck-collar zone is performed for 15 minutes and repeated exercise complex is performed for 15 minutes. Then again a catholic bath or a catholyte shower takes place. After bath, rubbing and resting take place for 15 minutes. After this, 200 ml of drinking catholyte is administered for dinner before meals. The introduction of catholyte for dinner is performed till 2000.EFFECT: effective treatment of arterial hypertension, prevention of the development of pathogenic bacteria and fungi on the body.5 tbl, 5 dwg, 2 ex
N-(acetylsalicyloyl)pyrazol with cerebroprotector action in case of cerebral circulation insufficiency // 2632005
FIELD: pharmacology.SUBSTANCE: invention can be used to obtain effective cerebroprotective agents based on pyrazole and 2-acetoxybenzoic acid (acetylsalicylic acid, aspirin). A pyrazole derivative with the formula given below is proposed. .EFFECT: derivative has a cerebroprotective effect, effectively and in small doses improves cerebral circulation in the model of one-stage irreversible bilateral occlusion of common carotid arteries, surpasses the action of pyracetam.3 tbl, 2 ex
Healing cream with anti-inflammatory and venotonic action // 2630977
FIELD: pharmacology.SUBSTANCE: invention is a therapeutic cream with anti-inflammatory and venotonic action, comprising a therapeutically effective amount of a dry extract of red grape leaves, wax emulsion, propylene glycol, vaseline oil, peach oil, glycerin, nipagin, triethanolamine and purified water, the components in the cream being at certain ratio, wt %.EFFECT: expansion of the arsenal of drugs with anti-inflammatory and venotonic action.1 dwg
eans with antiarrhythmic action // 2630967
FIELD: pharmacology.SUBSTANCE: means with antiarrhythmic action is a substance isolated from plants of the Aconitum genus of the Ranunculaceae (buttercup) family containing lappaconitine, N-acetylsepaconitine alkaloids. 1-desmethyl-l-paconitine, ranaconitine, N-desacetyl-l-paconitine, isolappaconitine, 9-deoxylpaconitine or pharmaceutically acceptable salts thereof. A pharmaceutical composition for oral administration with an antiarrhythmic effect. The above described agent is an effective and safe antiarrhythmic drug, reduces the risk of sudden cardiac death, can be used in the treatment of arrhythmia in patients with chronic obstructive pulmonary disease (COPD) and epilepsy, and has high antiarrhythmic activity in various forms of arrhythmia.EFFECT: broncholytic, antiepileptic, anti-inflammatory and local anesthetic properties.9 cl, 19 tbl, 15 ex
ethod for conservative treatment of acute haemorrhoid // 2630615
FIELD: medicine.SUBSTANCE: Detralex is applied, 2-3 pills 2 times a day; Gepatrombin G and Levomecol ointments are topically applied to affected areas 2-3 times a day until the inflammation symptoms disappear and Gepatrombin G ointment is applied once a day for a week after their disappearance. The total period of treatment is 8 days, during which the patient is additionally injected with Sulodexide daily intramuscularly at a dose of 600 EBU.EFFECT: increased efficiency of treatment.1 cl
ethod for selecting tactics of carrying out complex therapy in patients with arterial hypertension and obesity // 2630603
FIELD: medicine.SUBSTANCE: presence or absence of dyslipidemia is revealed for treatment in patients with obesity of II degree and controlled AH of I and II degree. Diet and exercise are chosen differentially for patients with AH of I and II degree without dyslipidemia and with dyslipidemia. The complex of daily physical exercises is performed in the morning, in the afternoon and in the evening in a sitting position with wrist and ankle weights.EFFECT: effective weight and blood pressure loss in the absence of side effects from the musculoskeletal system.2 cl, 1 ex, 3 tbl
Neprilysin inhibitors // 2629930
FIELD: pharmacology.SUBSTANCE: invention relates to formula I compounds, or pharmaceutically acceptable salts thereof, which have the ability to inhibit neprilysin activity (NEP). In formula I, R1 is selected from H, -C1-8alkyl, -C1-6alkylene-OC(O)R10, -CH2-pyridinyl, -(CH2)2-pyridinyl and ; R10 is selected from -C1-6alkyl, -OC1-6alkyl and -CH(R15)-NHC(O)O-C1-6alkyl; R14 is -C1-6alkyl; R15 is -CH(CH3)2; R2 is -OR21 or -CH2OR21; and R3 is H or -CH3; where R21 is H; or R2 is taken with R3 to form -CH2-CH2-; Z is selected from -CH- and -N-; R4 is selected from H, -C1-8alkyl, -C1-3alkylene-O-C1-8alkyl, -C1-3alkylene-C6-10aryl, -[(CH2)2O]1-3CH3 and ; R44 is-C1-6alkyl; A is 0 or 1; R5 is selected from halogen, -CH3, -CF3 and -CN; b is 0 or an integer of 1 to 3; each R6 are independently selected from halogen, -OH, -CH3, -OSN3, -CN and -CF3. Each alkyl group in R1 and R4 is optionally substituted with 1 to 8 fluorine atoms and the methylene linker on biphenyl is optionally substituted with one or two -C1-6alkyl groups. The invention also relates to a method for the preparation of formula I compounds containing their pharmaceutical composition and application of the said compounds for preparation of a medicament for treatment of hypertension, heart failure or kidney disease.EFFECT: improved compounds properties.40 cl, 16 ex

ethod for immunocorrection in case of chronic cerebral ischemia // 2629813
FIELD: medicine.SUBSTANCE: immunocorrection method involves administration of 250 mg/day of 2-ethyl-6-methyl-3-hydroxypyridine succinate (Mexicor) for 5 days intravenously and 7 injections of 6 mg intramuscular azoxime bromide (Polyoxidonium) every 48 hours.EFFECT: application of this method allows immunocorrection of patients with chronic cerebral ischemia due to membrane-protective, antihypoxic and immunocorrective action of drugs.1 dwg,1 ex
Cardioprotective pharmaceutical substance and method of its preparation // 2629772
FIELD: pharmacology.SUBSTANCE: invention relates to a method for preparing neopetroside A, which can be used in medicine as an agent inhibiting activity against glycogen synthase-3β and glycogen synthase-3α. The proposed method is characterized in that 2,3-acetonide-D-ribose is acylated with para-acetoxybenzoyl chloride in pyridine to obtain 2,3-O-acetonide-5-O-(4-acetoxybenzoyl)-D-ribose, then the resulting compound is treated with ethyl niconate to form 1-[2,3-O-acetonide-5-O-(4-acetoxybenzoyl)-α-D-ribofuranosyl]pyridinium-3-carboxylate, then the resulting compound is treated with an aqueous solution of ammonia to form 1-[2,3-O-acetonide-5-O-(4-hydroxybenzoyl)-α-D-ribofuranosyl]pyridinium-3-carboxylate, then the resulting compound is treated with an acid to form neopetroside A([5-O-(4-hydroxybenzoyl)-α-D-ribofuranosyl]pyridinium-3-carboxylate) in a salt form.EFFECT: new effective method of a valuable product and its new application as an agent possessing glycogen synthase inhibitory activity are proposed.2 cl, 5 ex, 1 tbl, 10 dwg
Dipeptide prodrug, its application and medicine // 2629558
FIELD: pharmacology.SUBSTANCE: invention relates to a dipeptide prodrug of general formula (I) , which can be used to treat and/or prevent cardiovascular diseases.EFFECT: increased application effeciency.3 cl, 4 tbl, 7 ex
 
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