Quinolines and isoquinolines (A61K31/47)

Stable pharmaceutical composition for oral administration comprising levocetirizine, or pharmaceutically acceptable salt thereof and montelukast or pharmaceutically acceptable salt thereof // 2614382
FIELD: medicine, pharmacy.SUBSTANCE: this present invention relfers to a pharmaceutical composition in the form of a capsule for oral administration for asthma or allergic rhinitis prevention or treatment. The composition comprises: (a) the first fraction of particles in the form of mini-pill comprising levocetirizine, or pharmaceutically acceptable salt thereof and organic acid; and (b) the second fraction of particles in the form of mini-pill comprising montelukast or pharmaceutically acceptable salt thereof. The organic acid is citric acid, tartaric acid, succinic acid or ascorbic acid. The organic acid is present in the amount of 100 parts by weight per 100 parts of levocetirizine. The said first and second particle fractions are physically separated and filled into the capsule. A method for pharmaceutical capsule composition production is also described. The pharmaceutical composition of this invention inhibits the production of related contaminants of levocetirizine and montelukast and provides good stability.EFFECT: invention expands the product range of drugs for allergic rhinitis or asthma prevention or treatment.9 cl, 3 dwg, 4 tbl, 6 ex
Gelatine capsule of selective vessel destruction in tumours // 2613146
FIELD: medicine.SUBSTANCE: gelatine capsule of selective vessel destruction in tumours relates to field of pharmaceutics and medicine, in particular to oncology, and deals with novel medications, mechanism of action of which consists in their destruction of already existing vessels inside tumour, preventing in such way supply of blood and oxygen, vital for survival of solid tumours with dimensions exceeding 1 mm. The capsule contains approximately 250-900 mg of pharmaceutical composition, which contains anti-tumour compound 7-methoxy-4-nitro-3-(p-methoxyphenyl)isoquinolinone 16-18 wt %, crospovidone 5-8 wt %, hypromellose 2-3 wt %, polysorbate 80 - 1-2 wt %, sodium laurylsulphate 0.7-1.2 wt %, the remaining part - mannitol, in gelatine capsule.EFFECT: invention solves the task of creating novel peroral anti-tumour medication for prevention or treatment of benign or malignant tumours, independently on their origin or size, within the framework of treating mammals, in particular humans, resistant to traditional treatment.3 cl, 1 tbl

New rebamipide prodrugs, method for their preparation and application // 2612509
FIELD: biotechnology.SUBSTANCE: invention relates to a compound of formula 1 that is a new rebamipide prodrug, and to the pharmaceutical composition thereof.EFFECT: new rebamipide prodrug with absorption rate 25 times higher than that of rebamipide, which can be used for prevention or treatment of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.7 cl, 3 tbl, 204 ex, 1 dwg
ethod of increasing the efficiency of treatment of patients with tuberculosis // 2611398
FIELD: medicine.SUBSTANCE: invention relates to medicine, namely to phthisiology, and can be used to improve the efficiency of treatment of patients with tuberculosis. Method includes the determination of the degree of patient’s medication adherence through his questioning, which is performed at the beginning of the main course of treatment. Stens are determined and after its determination diagnose the factors affecting the level of adherence, and then the prediction of medication adherence is determined: if total score is from 35 points and more, 1–2 stens mark the unsatisfactory medication adherence, if it is 16–34 points, 3–5 stens mark satisfactory medication adherence, if it is 4–15 points, 6–8 stens mark good medication adherence, if it is up to 3 points, 9–10 stens mark medication adherence. In case of unfavorable prognosis at 1–5 stens prescribe cycloferon immunomodulator and methods of psychotherapy, as well as the chemotherapy regimen correction is carried out by changing the method of administration of etiotropic drugs, and at a satisfactory medication adherence etiotropic drugs are administered parenterally, and at unsatisfactory medication adherence etiotropic drugs are administered parenterally and inhalationly.EFFECT: use of invention improves efficiency of treatment of patients with tuberculosis by determining the degree of patient’s medication adherence for further treatment correction.1 cl, 2 ex
ethod for production of antiparasitic long acting preparation for animals // 2611387
FIELD: veterinary medicine.SUBSTANCE: praziquantel, ivermectin, copolymer of lactic and glycolic acids are mixed with a solvent with the following ingredient ratio (in wt %): praziquantel - 1.0-15.0, ivermectin - 0.5-8.0, copolymer of lactic and glycolic acids - 6.0-16.5, solvent - the rest. At that,praziquantel and ivermectin are the first to be dissolved in the solvent. The solution is then purged with argon or nitrogen and placed in an ultrasonic bath. The mixture is kept in the ultrasonic bath for 50-60 minutes till complete dissolution of the components. Then the copolymer of lactic and glycolic acids is added. For complete copolymer dilution, the obtained mixture is kept for 4-5 hours with occasional stirring at the rotation speed of 1600-2000 rpm. Then, the resulting solution is subjected to sterile filtration, dispensed into vials and sealed.EFFECT: method can reduce loss of active ingredients during manufacture and provide a harmless, non-toxic, sterile and effective long-acting drug for treating animals against a wide range of parasitic infections.5 cl, 8 ex

Pharmaceutical composition for treating, preventing or relieving movement disorders and its application // 2611376
FIELD: medicine.SUBSTANCE: group of inventions relates to treatment of movement disorders. Application of composition is proposed, which contains zolmitriptan or its pharmaceutically acceptable salt and 5-HT-receptor agonist buspirone or its pharmaceutically acceptable salt for treating, preventing or relieving movement disorders and use of set containing pharmaceutical composition of zolmitriptan or its salt and pharmaceutical composition of 5-HT-receptor agonist buspirone or its salt, at same prescription.EFFECT: technical result is increased efficiency of combined treatment in part of manifestations of delayed dyskinesia and relief of symptoms of Parkinson's disease in its model in rats.13 cl, 4 dwg, 9 ex
Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2 negative allosteric modulators, compositions and use thereof // 2610262
FIELD: pharmaceutics.SUBSTANCE: invention relates to organic chemistry, namely, to quinoline carboxamide derivatives of following structures. Invention also relates to pharmaceutical composition based on one of said compounds, use of said compounds for treating diseases or disorders mediated by mGluR2, such as Alzheimer's disease, cognitive disorder, schizophrenia, mood disorders, painful disorders, and sleep disorders.EFFECT: novel quinoline carboxamide derivatives with useful biological properties.25 cl, 8 tbl, 310 ex
ethod of treating placental insufficiency in pregnant women suffering from vaginal dysbiosis // 2610061
FIELD: medicine.SUBSTANCE: invention refers to medicine, namely to maieutics, and can be used for treating placental insufficiency in pregnant women suffering from vaginal dysbiosis. For this purpose it is combined with complex drug-induced and laser therapy. During 6 days daily pregnant vaginal sanitation with 0.01 % miramystine for 5 minutes. Tablets of fluomizine are introduced at bedtime. Optimum dose of laser exposure is selected based on parameters of ultrasonic examination, doplerography examination and cardiotocography of foetus. In disturbed uterine-placental perfusion of 1a degree, delay of intrauterine growth retardation on 1 week, sum of Fisher indicators of 7 points daily percutaneous exposure on median cubital vein at wave length of 905 nm, frequency 1000 Hz, radiation power 50 W, for 2 minutes, therapeutic course is 5 procedures. In disturbed uterine-placental perfusion 1b degree, gestational delay of 2 weeks and sum of Fisher indicators of 6-7 points daily percutaneous exposure on ulnar vein with laser device at wave length of 905 nm, frequency 1,000 Hz, radiation power 50 W, for 5 minutes, daily therapeutic course is 7 procedures. In disturbed uterine-placental perfusion of 2 degree, delay of intrauterine growth retardation of 3 weeks, evaluation by Fischer of 6 points daily percutaneous exposure on anterior abdominal wall within projection of placenta wavelength 905 nm, frequency 1,000 Hz, power 65 W, for 6 minutes. Daily therapeutic course is 10 procedures.EFFECT: method provides higher clinical effectiveness, reduced length of treatment, reduced drug load on body of pregnant woman.1 cl, 3 tbl, 3 ex
ethod of treating children with acute respiratory infections accompanied with secondary immune deficiency // 2609865
FIELD: medicine.SUBSTANCE: invention relates to medicine, namely to clinical Immunology and allergology, and can be used for treating children suffering frequent episodes of acute respiratory infections accompanied secondary immune deficiency. Method involves the intranasal introduction of "Grippferon" during 5 days a week with underlying nebulization through face mask with 12.5 % solution of "Cycloferon" – 2 ml, 2 times a week and application of medical pepper of patch on skin in projection of thymus, that is performed 2 times a week for time, when in last 3 months episodes of acute respiratory infections are not registered or only one episode is registered.EFFECT: use of invention increases efficiency of antirecurrent therapy of frequent recurrent ARI episodes.1 cl, 1 ex

Use of sigma ligands in diabetes type-2 associated pain // 2608943
FIELD: chemistry.SUBSTANCE: invention relates to use of a sigma ligand, which is a 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine or a pharmaceutically acceptable salt thereof.EFFECT: prevention and/or treatment of pain associated with type 2 diabetes and related symptoms.6 cl, 9 dwg, 4 ex

Serotonin 5-ht3 receptor antagonists for application in treatment of lesional vestibular disorders // 2608458
FIELD: medicine.SUBSTANCE: invention relates to medicine and consists in application of serotonin 5-HT3 receptor antagonist for treatment of damages during vestibular disorders, wherein, mentioned damage is characterized by damage of internal ear cells and/or vestibular nerve cells, wherein, serotonin 5-HT3 receptor antagonist is selected from a group comprising ondansetron, palonosetron, tropisetron, lerisetron, alosetron, granisetron, dolasetron, bernesetron, ramosetron, azasetron, itasetron, zakoprid and cilansetron; and mentioned serotonin 5-HT3 receptor antagonist is introduced to the patient, at least during 5 days.EFFECT: treatment of damages during vestibular disorders.4 cl, 4 ex, 6 dwg

Deuterium-enriched 4-hydroxy-5-methoxy-n,1-dimethyl-2-oxo-n-[(4-trifluoro-methyl)phenyl]-1,2-dihydroquinoline-3-carboxamide // 2608306
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoromethyl)-phenyl]-1,2-dihydroquinoline-3-carboxamide. Invention also relates to a pharmaceutical composition based on deuterium-enriched carboxamide, method for production thereof and method of treating malignant hyperproliferative disorder or autoimmune disease, based on use of deuterium-enriched carboxamide.EFFECT: technical result is obtaining deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoromethyl)-phenyl]-1,2-dihydroquinoline-3-carboxamide, having useful biological properties.25 cl, 7 dwg, 10 tbl, 1 ex
Novel pyrrole compounds, synthesis method thereof and pharmaceutical compositions containing same // 2607788
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I) possessing inhibitory activity on Bcl-2 family proteins. In formula (I) (I) A1 is hydrogen, (C1-C6)polyhaloalkyl group or (C1-C6)alkyl group, A2 is hydrogen, (C1-C6)polyhaloalkyl group, (C1-C6)alkyl group or cycloalkyl group, T denotes a hydrogen atom, (C1-C6)alkyl group, optionally substituted with one-three halogen atoms, group (C1-C4)alkyl-NR1R2 or group (C1-C4)alkyl-OR6, R1 and R2 each independently from each other is a hydrogen atom or (C1-C6)alkyl group, or R1 and R2 form with a nitrogen atom bearing them, heterocycloalkyl, R3 is (C1-C6)alkyl group, cycloalkyl group, heterocycloalkyl group, aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R4 is an aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R5 is hydrogen or halogen atom, R6 is a hydrogen atom or a linear or branched (C1-C6)alkyl group, Ra, Rb, Rc and Rd each independently from other represents hydrogen, linear or branched (C1-C6)alkyl, halogen atom, a linear or branched (C1-C6)alkoxy group, hydroxy group, R7-CO-NH-(C0-C6)alkyl-, R7-SO2-NH-(C0-C6)alkyl-, R7-NH-CO-NH-(C0-C6)alkyl-, R7-O-CO-NH-(C0-C6)alkyl-, or substitutes of pair (Rb, Rc) form together with carbon atoms carrying them, a ring consisting of 5–6 ring members, which may contain 1–2 oxygen atoms, R7 is hydrogen, linear or branched (C1-C6)alkyl, aryl or heteroaryl. Invention also relates to methods of producing compounds of formula (I), to a pharmaceutical composition, use of a pharmaceutical composition for preparing a drug, use of compound of formula (I) for preparing a drug.EFFECT: obtaining novel compounds of formula (I) possessing inhibitory activity on Bcl-2 family proteins.37 cl, 2 tbl, 473 ex

Combined anticancer therapy // 2607596
FIELD: medicine.SUBSTANCE: present invention relates to combined therapy with {3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4difluorophenyl} amide of propane-1-sulphonic acid (compound 1) or its pharmaceutically acceptable salt and EGFR inhibitor, selected from erlotinib and cetuximab, for treating cancer, containing b-Raf with V600 mutation, namely colorectal cancer, melanoma and thyroid cancer.EFFECT: combination of compound 1 with EGFR inhibitor leads to improved anti-tumor effects, which considerably exceed the results, obtained for each compound separately, without increasing the toxicity.20 cl, 6 ex, 15 tbl, 9 dwg

Encapsulated dosage form, containing montelukast and levocetirizine // 2606857
FIELD: pharmaceutics.SUBSTANCE: invention relates to capsule dosage form for preventing or treating allergic rhinitis and asthma, which consists of two separate layers: (1) montelukast layer, containing montelukast or its pharmaceutically acceptable salt; and (2) levocetirizine layer, containing levocetirizine or its pharmaceutically acceptable salt, in which said montelukast layer and levocetirizine layer contain water in amount of 5 % and less; and their production method.EFFECT: encapsulated dosage form, according to invention, can completely separate two active ingredients, minimizing so reaction activity between them and improving stability of product with respect to ageing effect and thus optimizing therapeutic action.20 cl, 5 tbl, 9 ex
Compounds having antagonistic activity towards muscarinic receptors and agonist activity to beta2-adrenoreceptors // 2606121
FIELD: chemistry.SUBSTANCE: present invention relates to compounds of general formula (I), acting as muscarinic receptors antagonists or beta2-adrenoreceptors agonists, as well as to pharmaceutical compositions based thereon and to therapeutic applications for preparing a medicine to prevent and treat diseases, such as asthma, chronic bronchitis, etc.EFFECT: obtained are novel compounds of formula (I) having activity towards muscarinic receptors or beta2-adrenoreceptors.13 cl, 5 tbl, 39 ex, 2 dwg

Quinoline and quinoxaline derivatives effective as cysteinyl-leukotriene antagonists // 2605929
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to a heterocyclic compound of formula (IA) or to a pharmaceutically acceptable salt thereof, where in each case R1 and R3 are independently selected from a group comprising hydrogen, halogen, -OH, -C1-2alkyl, -O-C1-2alkyl, -O-C1halogenalkoxy, -N(C1alkyl)2; R2 represents hydrogen; W represents a group selected from -CH= or -N=; X represents a group selected from -CH=CH- or -N=CH-, where nitrogen from -N=CH- is directly bonded with ring 'a'; Y represents a group selected from -CH=CH- or -C≡C-; Z denotes a bond or group selected from -(CH2)n- and -CH=CH-; A is a group selected from -OR, -O(CH2)nphenyl, -O(CH2)nthiophene; P is selected from a group comprising -O-; Q is a group selected from -COOH; where R is selected from a group comprising hydrogen, -C1-6alkyl, -C3-6cycloalkyl, -C1alkyl (C3-6cycloalkyl), -C3-6alkenyl and -C3-6alkynyl; 'n' in each case represents an integer, selected from 1, 2 or 3; 'm' in each case represents an integer, selected from 0-3, inclusive. Invention also relates to a compound of formula (Id), where radicals are described in patent claim.EFFECT: obtaining novel heterocyclic compounds effective as antagonists of cysteinyl-leukotriene.9 cl, 1 dwg, 2 tbl, 67 ex
Injection preparation based on drotaverine and preparation method thereof // 2605826
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical industry and represents pharmaceutical preparation in form of solution for intravenous and intramuscular administration, containing drotaverine hydrochloride, sodium disulphite, buffer agent and solvent. According to invention, preparation as buffer agent contains ammonium acetate and 30 % aqueous solution of acetic acid, and solvent is 95 % ethanol and water for injections highly purified in following proportions: drotaverine hydrochloride (in terms of anhydrous substance) - 18-22 mg, sodium disulphite - 0.9-1.1 mg, ethanol 95 % (in terms of anhydrous) - 0 59.4-72.6 mg, ammonium acetate - 0.66-1.0 mg, 30 % aqueous solution of acetic acid - 0.54-1.0 mg, water for injections - up to 1.0 ml, pH - 4.0-5.5, as well as method of producing of preparation.EFFECT: invention provides high stability of preparation and maintaining pH in process of storage.3 cl, 4 ex

3-carboxy-4-aminoquinoline derivates, useful as sweet taste modifiers // 2605549
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry and specifically to novel quinoline derivatives of general formula (IIIb) or ingestible salt thereof, where A is NH2; B is C1-C4 alkyl; C is -CO2R7; R7 is hydrogen; L1 is C1-C8 alkylene, C6-cycloalkylene or -CH2-C6-cycloalkylene; L2 is -O-, NR34-C(O)-, -C(O)-NR34-, -(3-6-member heterocyclylene-C(O))-group, where heterocyclylene contains one nitrogen atom; R33 is C1-C6 alkyl, optionally substituted C1-C6 alkoxy or hydroxy, C3-C10 carbocyclyl, optionally substituted with one C1-C6 alkoxy, C6-C10 aryl, optionally substituted with one or two substitutes, selected from -OH, halogen, -C(=O)NH2, -C(=O)NHC1-6 alkyl, C1-C6 alkoxy, C1-C6 alkyl-OH and O-C1-C6 alkyl-OH, C6-C10 aryl C1-C4 alkyl, optionally substituted C1-C6 alkoxy, 5-10-member heterocyclyl containing 1 or 2 oxygen atoms, pyridine or pyridine-C1-C4 alkyl; and R34 is hydrogen. Invention also relates to quinoline derivatives of formula (IIIc) and (IIIc'), specific quinoline derivatives, ingestible composition based on compounds of formula (IIIb), (IIIc) and (IIIc'), method of enhancing sweet taste of ingestible composition, method of producing intermediate compounds of formulae (IV) and (IVc).EFFECT: novel quinoline derivatives, useful as sweet taste modifiers.23 cl, 23 tbl, 133 ex, , ,

Nuclear receptor binding agents // 2604666
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine, namely, to gastrology and endocrinology, and can be used for prevention, treatment, delay of the onset, reduction of the incidence or reduction of the severity of a condition associated with high fat diet consumption, fatty liver infiltration, post-menopausal obesity, to increase energy consumption in a patient, to increase lean body mass. For this purpose, the patient in need thereof, administering a therapeutically effective amount of an estrogen receptor ligand compound, wherein the compound represents 4-bromo-6,8-dihydroxy-2-(4-hydroxyphenyl)isoquinoline-1-(2H)-on (12u) or 4-cyano-6,8-dihydroxy-2-(4-hydroxyphenyl)isoquinoline-1-(2H)-on (14m).EFFECT: group of inventions provides increase in treatment efficacy of said states within its safety.13 cl, 10 tbl, 33 dwg, 41 ex

Novel class of selective agonists of somatostatin receptors // 2603962
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I or its pharmaceutically acceptable salt, wherein R1, R5 are independently selected from H; R2, R3 and R4 are selected from H and ring A, wherein one of R2, R3 or R4 independently represents ring A; ring A is a 6-member monocyclic or 10-member bicyclic aromatic ring which optionally contains 1 heteroatom, which is N, wherein ring A can be optionally substituted with 1-3 substitutes independently selected from halogen, OH, COOH, C1-C6-alkyl, C1-C6-alkoxy, -C(O)C1-C6-alkyl, -NO2; ring B is a 5-6-member non-aromatic ring, optionally containing 1 heteroatom, which is O, wherein ring B can be optionally substituted with 1-3 substitutes independently selected from -C1-C6-alkyl, -C(O)C1-C6-alkyl, -C1-C6-alkoxy; R6 is selected from H or C1-C6-alkyl, R7 denotes H or-(Z)m-(D)p, where independently m=0-1, p=0-1, wherein m=p=0 does not hold; Z is selected from C1-C6-alkyl; D is a 5-6-member non-aromatic ring, optionally containing one N heteroatom, wherein ring D can be optionally substituted with one substitute selected from C1-C6-alkyl, C1-C6-alkoxy. Compound of formula I or pharmaceutically acceptable salt thereof are intended for use as sst4 receptor agonist for preparing a pharmaceutical composition for treating and/or preventing a pathological condition or disease involving somatostatin receptors subtype 4 (sst4). Invention also relates to a pharmaceutical composition for treating and/or preventing a pathological condition or disease, treatment and/or prevention of which requires use of somatostatin receptor agonist subtype 4 (sst4), containing a therapeutically effective amount of compound of formula I or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, solvent and/or filler.EFFECT: chemical compounds, which are selective agonists of human sst4 receptors.15 cl, 4 dwg, 3 tbl, 6 ex

Aerosolized fluoroquinolones and uses thereof // 2603638
FIELD: medicine.SUBSTANCE: invention relates to using levofloxacin or ofloxacin in a dose from 20 mg to 400 mg per day for treating microbial infection in the patient.EFFECT: technical outcome: invention relates to the use of levofloxacin or ofloxacin in effective dosages for treating a microbial infection.14 cl, 53 dwg, 37 tbl, 13 ex

New derivatives of 3,3-dimethyltetrahydroquinoline // 2603276
FIELD: chemistry.SUBSTANCE: invention is related to organic chemistry and specifically to new tetrahydroquinolin derivatives of general formula (I) or pharmaceutically acceptable salts or esters where R1 represents hydrogen, halogen, carboxyl, alkoxycarbonyl, alkilsulphonylaminocarbonyl or cycloalkylalkilsulphonylaminocarbonyl; R2 represents hydrogen, halogen or carboxyl; R3 represents hydrogen, halogen, carboxyl, halogenalkyl, cyano, alkoxycarbonyl, alkylsulphonyl, alkylsulphonylaminocarbonyl, cycloalkylalkilsulphonylaminocarbonyl, carboxylalkylamino(alkyl)carbonyl, alkyl(hydroxy)pyrrolidinylcarbonyl or carboxylpyrrolydincarbonyl; R4 is hydrogen, carboxyl, alkilsulphonylaminocarbonyl or cycloalkylalkilsulphonylaminocarbonyl; R5 is pyridinyl, substituted pyridinyl, morphonylpyrinidil, phenyl or substituted phenyl, where substituted pyridinyl and substituted phenyl represent pyridinyl and phenyl, substituted with one or two substitutes given in the patent claim; where the alkyl, one or in combination, is saturated alkyl group with linear or branched chain containing 1 to 6 carbon atoms; alkoxy, one or in combination, denotes a group of alkyl-O-, where the alkyl such as defined above; cycloalkyl, one or in combination, relates to saturated carbon ring, containing from 3 to 6 carbon atoms; provided that 3,3-dimethyl-2-phenyl-1,2,3,4,6-hydroxyl-2,2,4-trimethyl-1,2,3,4-tetrahydroquinline is excluded. Invention is also related to specific compounds, pharmaceutical composition based on compound of formula (I), use of formula (I) and a method of treating or preventing diseases based on use of compounds of formula (I).EFFECT: technical result is obtaining novel tetrahydroquinolin derivatives, useful as activator AMR-activated protein kinase (AMPK).17 cl, 236 ex

Combination of sirosingopin and mitochondrial inhibitors for treatment of cancer and for immunosuppression // 2602937
FIELD: medicine.SUBSTANCE: group of inventions is related to medicine, pharmacology, pharmaceutics, and involves a pharmaceutical composition and combination of sirosingopin (SS) and mitochondrial inhibitor (MI), where the said mitochondrial inhibitor represents metformin or fenformin. Ratio of the amount of (wt/wt) CC and MI can range from 1 to 10-1 to 1000. This combination can be used in treating such types of cancer as carcinoma, sarcoma, leukaemia, myeloma, lymphoma, various types of cancer of the nervous system or autoimmune diseases of skin, nervous system, connective tissue, muscles, blood, bone tissue and internal organs, as immunosuppressive therapy. Group of inventions also includes the method of determining if the cancer cell is sensitive to the SS. For this purpose, (a) a suspension of single cells cultivated cancer cells in acceptable media is received; (b) the cancer cell is incubated with SS; (c) the cancer cell obtained at step (b) is incubated with positively charged fluorescent dye; (d) the fluorescence excited intensity is measured; and (e) fluorescence intensity, measured at step (d) is compared with the intensity of fluorescence of the cancer cell to be incubated only with positively charged fluorescent dye. Relative increase in fluorescence intensity of cancer cells, preliminary incubated with SS, means that cells are sensitive to treatment with SS. Group of inventions also includes a method of treating cancer or autoimmune disease by administration of a combination or a composition of SS and the said MI to a warm-blooded animal in the amount effective with respect to the aforementioned disease.EFFECT: said combination and composition provide a synergetic effect when used regarding the aforementioned disorders, the prognosis of which, in its turn, can be provided for implementation of the above method for prognosis of cancer cell sensitivity to SS.14 cl, 12 dwg, 1 ex, 1 tbl

Cyanoquinoline derivatives // 2600928
FIELD: chemistry.SUBSTANCE: invention relates to novel cyanoquinoline derivatives of general formula I, as well as to stereoisomers, cis-trans-isomers or pharmaceutically acceptable salts thereof, where R1 is selected from a group consisting of 4-bromobut-2-enamide, 4-(dimethylamino)but-2-enamide, acrylamido, but-2-enamide, 3-methylbut-2-enamide, 2-(1-tert-butoxycarbonylpiperidin-4-ylidene) acetamide, 2-(piperidin-4-ylidene)acetamide, 2-(1-methylpiperidin-4-ylidene) acetamide, 2-(1-ethylpiperidin-4-ylidene) acetamide, 2-(1-benzylpiperidin-4-ylidene) acetamide, 2-(1-(2-methoxyethyl) piperidin-4-ylidene)acetamide, 2-(1-(2-methoxycarbonylmethylene)piperidin-4-ylidene)acetamide, 2-(1-isopropylpiperidin-4-ylidene) acetamide, 2-(1-(2-hydroxyethyl)piperidine-4-ylidene)acetamide, 2-(pyrrolidin-3-ylidene)-acetamide, N-(N-(2-(2-(dimethylamino)ethoxy)ethyl)amino)fumaramide, 2-(1-(2-(2-(2-hydroxyethoxy)ethylamino)acetyl) piperidin-4-ylidene)acetamide, 2-((1-methylsulphonyl)piperidin-4-ylidene) acetamide, 4-(piperidin-1-yl)but-2-enamide, 4-(morpholin-4-yl)but-2-enamide, 4-(tert-butylamino)but-2-enamide, 4-(benzylamino)but-2-enamide, 4-(6-hydroxyhexylamino)but-2-enamide, 4-(N-methylbenzylamino)but-2-enamide, 4-(diethylamino)but-2-enamide, 4-(2-methoxyethylamino)but-2-enamide, 4-(diethanolamino)but-2-enamide, 4-(N-methylmethoxyethylamino) but-2-enamide, 4-(N-methyl-ethanolamino)but-2-enamide, 4-(dimethoxyethylamino)but-2-enamide, 4-(N-methyl-6-amino-1-hexanolyl)but-2-enamide and propylamide; one of R2 and R3 is H, while other is selected from unsubstituted C6-aryl-C1-2-alkyl, substituted with 1-2 substitutes or unsubstituted C6-aryl and substituted with 1 substitute or unsubstituted 6-9-member heteroaryl, where, when R2 or R3 is selected from a substituted C6-aryl, substitute is selected from C2-C6-alkynyl, halogen, C6-aryl-C1-alkyloxy (where said C6-aryl can be substituted with 1 substitute selected from halogen, cyano, C1-C6 alkyl, C1-C-6 alkoxy), and 6-member heteroaryl-C-1-alkyloxy, and when R2 or R3 are selected from a substituted heteroaryl, substitute is selected from a group comprising C6-aryl-C1-alkyl (where said C6-aryl is optionally substituted with 1 substitute selected from halogen and cyano, methoxy group), C6-arylamido (where the said C6-aryl can be unsubstituted or substituted with 1 dimethylamino group), C6-arylsulphonylamino, C5-heteroarylamido, C6-cycloalkylamido, C6-arylaminocarbonyl (where said C6-aryl is substituted with 1 methoxy group), C6-aryl-C1-alkyloxy and C6-aryloxy; or R2 and R3, together with a nitrogen atom to which they are bonded, form a substituted or unsubstituted 9-10-member heterocyclyl, where heterocycyl substitutes are selected from halogen, C1-C-6 alkyl, CF3, C6-aryl-C1-alkoxy, -COOMe, -CH2OH and pyrrolyl; and R4 is substituted with 1 methyl or unsubstituted 5-6-member heterocyclyl or unsubstituted 6-member heteroaryl. Invention also relates to specific compounds, pharmaceutical composition based on compound of formula I and use of formula I.EFFECT: technical result is obtaining novel cyanoquinoline derivatives which are useful in treating tumours.33 cl, 20 tbl, 228 ex

Form of pharmaceutical composition multi-layer coating for oral administration containing omega-3 fatty acid or its alkyl ester, as well as medicinal agent based on statin // 2600804
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutics. Pharmaceutical composition for oral administration is described containing: gelatine capsule core, coated with first and second layers of coating. Gelatine capsule core contains omega-3 fatty acid or its alkyl ester. First coating layer contains hydroxypropyl methylcellulose and copolymer of butyl methacrylate, (2-dimethylaminoethyl)methacrylate and methyl methacrylate with weight ratio of 1:2:1; where weight ratio of hydroxypropyl methylcellulose to said copolymer ranges from 1:0.8 to 1:10. Second coating layer contains medicinal agent based on statin as inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme (HMG-CoA) reductase.EFFECT: invention prevents sticking of gelatine capsules' cores to each other and deformation of gelatin capsules' cores, which can occur in process of aqueous coating application, invention also provides pharmaceutical composition disintegration and stability requirements compliance.13 cl, 9 tbl, 7 ex

Tissue regeneration stimulating agent // 2599289
FIELD: medicine.SUBSTANCE: invention refers to medicine, more specifically to pharmacology, cell technologies and regenerative medicine. Task solved by this invention, is increasing of effective agents range stimulating tissue regeneration. Assigned task is solved by using as tissue regeneration stimulating agents, of pharmacological substances having direct action on PI3K-, PKB-, PKC-, NF-κB-, MAPK-, JAK/STAT, cAMP-, PKA/CREB-mediated signaling in progenitor cells.EFFECT: proposed agents allow to efficiently stimulate regeneration of tissues impaired by pathological process, due to activation of resident (regional) progenitor cells functions by effect on intracellular signal transduction.8 cl, 24 tbl, 7 ex

New substituted quinoline compounds as inhibitors of s-nitrozoglutation-reductase inhibitors // 2599144
FIELD: chemistry.SUBSTANCE: invention is related to organic chemistry and specifically to novel quinoline derivatives of general formula I or pharmaceutically acceptable salts, stereoisomers or N-oxides, where m = 0 and 1; R1 is independently selected from a group consisting of chlorine, fluorine and bromine; R2b and R2 c are independently selected from a group, consisting of hydrogen, halogen, C1-C3 alkyl, fluorinated C1-C3alkyl, cyano and N (CH3)2; X is selected from a group consisting of n is selected from a group consisting of 0 and 1; R3 is independently selected from a group consisting of halogen, C1-C3 alkyl, fluorinated with1-C3 alkyl, cyano, C1-C3alkoxy and NR4R4′, where R4 and R4′ are independently selected from a group consisting of C1-C3 alkyl; and a is selected from a group consisting of .Invention is also related to the use of formula I, pharmaceutical composition based on the compound of formula I, method of treating pulmonary disorders and inflammatory diseases based on use of the compound of formula I, and a method of producing a pharmaceutical composition based on the compound of formula I.EFFECT: technical result is obtaining novel quinoline derivatives, useful as inhibitors of S-nitrozoglutation reductase (GSNOR).17 cl, 64 ex

Triazolopyrine compounds as kinase inhibitors pim // 2598846
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula I, their stereoisomers and pharmaceutically acceptable salts thereof, in which R1, R2, R3, R4 and R10 assume values given in the patent claim. Declared compounds are inhibitors of kinase tyrosine kinases PIM-1, and/or PIM-2, and/or PIM-3 and can be used in treating diseases mediated by said kinase. Invention also relates to a pharmaceutical composition based on them, methods of producing the declared compounds and an intermediate compound used in production of the declared compounds.EFFECT: disclosed are compounds of Formula I, their stereoisomers and pharmaceutically acceptable salts.56 cl, 6 tbl, 11 ex biological researches (A-K), 6 receptions of, 328 ex

Quinoline-2-amine derivatives, useful for treating aids // 2598845
FIELD: chemistry.SUBSTANCE: present invention relates to organic chemistry, namely to new quinoline-2-amine derivatives of general formula (I) or pharmaceutically acceptable salts thereof, where X represents CR0 or N, i.e. together with the ring it belongs to it forms respectively a benzene or a pyridine group, R0, R1, R2, R3, R4, R7 and R8 independently represent a hydrogen atom , a halogen atom or a group selected from a (C1-C5)alkyl group, a (C1-C5)fluoroalkyl group, a (C1-C5)alkoxy group, a (C1-C5)fluoroalkoxy group, a -NRaRb group, a -NRa-SO2-NRaRb group, a -NRa-SO2-Ra group and may additional represent a group selected from (IIa) or (IIIa); A represents an oxygen atom, B is a covalent bond, n equals 1, 2 or 3, m equals 1, 2 or 3, R, R′, Rand R andb independently represent a hydrogen atom or (C1-C5)alkyl group, R and R′ can further form with a nitrogen atom, to which they are bonded, saturated 5-or 6-member heterocycle, possibly containing one more heteroatom O, R5 is a hydrogen atom or (C1-C5)alkyl group, R10 is a hydrogen atom or a chlorine atom, and R11 is a hydrogen atom under the conditions specified in CL. 1. Invention also relates to specific quinoline-2-amine derivatives and a pharmaceutical composition based on the compound of formula (I).EFFECT: technical result: there are new quinoline-2-amine derivatives, useful for treating AIDS.14 cl, 2 tbl, 6 ex , ,

Novel compounds // 2598840
FIELD: pharmaceutics.SUBSTANCE: invention relates to a compound of formula I, , where ring A and ring B are condensed bicyclic group, R1 denotes a substitute selected from hydrogen, halogen or ORf7; each R2a, R2b, R2c, R3 are independently selected from hydrogen, halogen, -CN, -ORf7 or C1-6 alkyl, optionally substituted with one or more substitutes selected from =O and E1; X is a straight bond; Y denotes -arylene-, -heteroarylene-, where -arylene- and -heteroarylene- may be substituted with E3, where E3 denotes halogen, or -heterocycloalkylene-, optionally substituted with one or more substitutes selected from =O and E4, RN denotes hydrogen or C1-6 alkyl, optionally substituted with one or more substitutes selected from =O and E5; Z denotes -C(O)-[T1]- or -C(O)N(Rx3)-[T1]-, where T1 denotes -(CH2)0-4-T2- and T2 denotes a direct bond or -C(O)-N(H)-CH2-; or its pharmaceutically acceptable ester, amide.EFFECT: compounds are suitable for use in treating the diseases in which it is desirable and/or require inhibition of protein-or lipid-kinase (PI3-K, for example, especially class I PI3K kinase family, PIM and/or mTOR), and especially in treating cancer.9 cl, 1 dwg, 4 tbl

N-heteroaryl compounds // 2596185
FIELD: pharmaceutics.SUBSTANCE: invention relates to N-heteroaryl compounds and pharmaceutically acceptable salts, solvates or N-oxides of general formula (I), where R1: halogen, C1-C6-alkyl, C1-C6-alkyloxy, C1-C6-alkylthio, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy-C-1-C6-alkyl, C1-C6-alkyl-carbonyl, SF5, C1-C6-alkylsulphonyl, wherein each carbon-containing radical is optionally substituted with one or more halogen atoms, R2: hydrogen, C1-C6-alkyl, R3, R4 and R7 hydrogen, C1-C6-alkyl, R5: hydrogen, C1-C6-alkyl, C1-C6-acyl or C1-C6-alkyloxycarbonyl, R6: hydrogen, C1-C6-alkyl, C1-C6-alkyloxycarbonyl, phenyl, phenyl-C1-C6-alkyl, n=1-3, X: carbonyl, thiocarbonyl or sulphonyl group, A is a bond, E is a bond or NR9, where R9 - hydrogen, B is N, D is N or CR11, where R11 - hydrogen, Y1 is C or N, where C is substituted with R12, which is hydrogen, C1-C6-alkyl, C1-C6-galoalkilom, nitro, Y2 is C or N, where C is substituted with R13, which is hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, nitrilo, di(C1-C6-alkyl)amino, N-pyrrolidinyl, C1-C6-alkylthio, C1-C6-alkylcarbonyl, aminocarbonyl, C1-C6-alkylamino-carbonyl, C1-C6-alkoxycarbonyl, Y3 is C, where C is substituted with R14, which is hydrogen, C1-C6-alkyl, C1-C6-alkoxy, amino, N-pyrrolidinyl, N-piperidinyl, N-morpholinyl, C1-C6-alkylcarbonyl, 1,3-dioxolane, which is unsubstituted or substituted with C1-C6-alkyl, Y4 is C or N, where C is substituted with R15, which is hydrogen, C1-C6-alkyl, wherein two of Y1, Y2 and Y4 can represent N, or Y3 and Y4 are bonded to form a ring system, selected from phenyl, thiophene, imidazole, pyridine, furan, 1,4-dioxane, triazole, and where at least one of B and D is a nitrogen atom. Invention also relates to a pharmaceutical composition based on compound of formula (I), intermediate compounds of formulae (1-IV), (3-IV), (4-II), method of treating helminth infection, compounds of formula (Ia), use of formula (I) and (Ia).EFFECT: obtaining novel compounds effective in treating parasitic infections.23 cl, 3 tbl, 18 ex

Substituted benzamide derivatives // 2595902
FIELD: chemistry.SUBSTANCE: invention relates to compound of formula (I), where R is hydrogen or C1-7alkyl; R1 represents -(CH2)n-(O)o-5-7-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, except for piperazine, where said heterocycloalkyl group optionally substituted with C1-7alkyl, hydroxy or halogen; n equals to 0, 1 or 2; o equals to 0 or 1; R2 represents CF3, C3-6-cycloalkyl, possibly substituted C1-7alkoxy or halogen, or represents indane-2-yl, or is 6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, optionally substituted with pyrimidinyl, or is 5-6 mono- or 9-10-member bicyclic heteroaryl containing 1-2 heteroatoms selected from N, O and S, where the heteroaryl is not thiazol and where said aromatic ring, is possibly substituted with one or two substitutes selected from C1-7alkyl, halogen, 5-6-member heteroaryl containing 1-2 heteroatoms selected from N and O, hydroxy, CF3, OCF3, OCH2CF3, OCH2-cycloalkyl, OCH2C(CH2OH)(CH2Cl)(CH3), S-C-1-7alkyl, C1-7alkoxy, CH2-C-1-7alkoxy, C2-7alkynyl or cyano, or substituted with -C(O)-phenyl, -O-phenyl, -O-CH2-phenyl, phenyl, and where said phenyl ring may be substituted with halogen, -C(O)OH or -C(O)O-C-1-7alkyl, or said aromatic ring, is possibly substituted with 5-6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, OCH2-oxetane-3-yl or O-tetrahydropyran-4-yl, possibly substituted C1-7alkyl; X is bond, -CH2NH-, -CHR″-, -(CHR″)q-O-, -O-(CHR″)q- or -(CH2)2-; Y is bond; R″ is hydrogen, C1-7alkyl, CF3, C1-7alkoxy; q is equal to 0, 1, 2 or 3; or pharmaceutically acceptable acid addition salt thereof, except for compounds specified in patent claim. Invention also relates to specific compounds specified in patent claim. Compounds are intended for producing medicinal agents, showing affinity to TAAR1.EFFECT: technical result: benzamide derivatives having high affinity to receptors associated with TAAR1 trace amines.9 cl, 1 tbl, 323 ex

Substituted 2-oxy-quinoline-3-carboxamides as kcnq2/3 modulators // 2595894
FIELD: chemistry.SUBSTANCE: invention relates to substituted 2-oxy-quinoline-3-carboxamides of general formula (I) in form of free compounds or salts of physiologically acceptable acids or bases, where R1 is C1-6-aliphatic residue; 6-member unsubstituted or mono- or disubstituted aryl or unsubstituted 5-member heteroaryl, selected from a thienyl; R2 is CF3; C1-4-aliphatic residue; O-C1-4-aliphatic residue; R3, R4, R5 and R6 each independently represent H; F; Cl; Br; I; CN; CF3; R7 is C1-6-aliphatic residue, unsubstituted or mono- or trisubstituted; where "aliphatic residue" in each case may be branched or straight, saturated, where "mono- or trisubstituted" with respect to "aliphatic residue" relates, in relation to corresponding residues, to substitution of one or three hydrogen atoms, each independently from other, with at least one substitute selected from a group which includes F, Cl, Br, I, OH, O-C1-4-aliphatic residue, where "mono- or disubstituted" with respect to "aryl" relates, in relation to corresponding residues, to substitution of one or two hydrogen atoms, each independently from other, with at least one substitute selected from a group which includes F, Cl, Br, I, OH, O-C1-4-aliphatic residue C1-4-aliphatic residue. Invention also relates to a pharmaceutical composition based on compound of formula (I) and a method of treating and/or preventing diseases mediated by channels KCNQ2/3 K+.EFFECT: obtaining novel 2-oxy-quinoline-3-carboxamide derivatives having useful biological activity.8 cl, 2 tbl, 53 ex

Composition and method of producing eye drops // 2595837
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutics, particularly to ophthalmology, and invites methods of getting pharmaceutical compositions in the form of eye drops for local treatment of inflammatory eye diseases of microbial genesis and bacterial infections in humans and animals. Methods are characterized by the fact that an aqueous solution of methylcellulose according to method 1 or hydroxypropyl methylcellulose according to method 2 at a temperature of 80-90 °C with further cooling to room temperature. Preparation of a solution of boric acid at a temperature of 75-85 °C with further cooling to 50-60 °C, dissolving fluroquinolone compound and sodium chloride in a solution of boric acid with subsequent cooling to room temperature, introduction of an aqueous solution of methylcellulose, homogenization prepared solution, bringing the solution with sodium hydroxide to pH 6-8, carrying out steps of sterilizing filtration and aseptic filling; as an antibacterial fluroquinolone connection one of quinolone, namely lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacine, or moxifloxacin, or gatifloxacin, or gemifloxacin, or their acceptable salts.EFFECT: preparing the pharmaceutical compositions.2 cl, 9 tbl
ethod of achieving prolonged clinical remission of chronic hpv infection, manifesting pointed condyloma of anogenital region // 2595832
FIELD: medicine.SUBSTANCE: invention relates to medicine, specifically to virology, and can be used for achieving prolonged clinical remission of chronic HPV infection, manifesting condyloma of anogenital region. Method includes triple vaccination of patients against 6, 11, 16 and 18 HPV types with "Gardasil" preparation for 0-2-6 months. Simultaneously applying 5 % Aldara cream on condyloma 3 times a week before bedtime, with subsequent washing in morning with soap until disappearance of visible anogenital warts, but not more than 16 weeks. Aldara 5 % cream is applied on day of first dose of "Gardasil" vaccine.EFFECT: invention provides clinical recovery of pointed condylomas and prevents repeated infection with condyloma types of HPV.1 cl

Pi3-kinase inhibitors and use thereof // 2595718
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds which are irreversible PI3-kinase inhibitors, and conjugates containing one or more PI3-kinases, containing cysteine residue, which is covalently and irreversibly boned with PI3-kinase inhibitor. Invention also discloses pharmaceutical compositions containing said compounds.EFFECT: compounds are intended for treating disorders and diseases associated with PI3-kinase.19 cl, 16 dwg, 26 tbl, 52 ex

Agents causing apoptosis and intended for treating cancer, immune and autoimmune diseases // 2594282
FIELD: chemistry. SUBSTANCE: invention refers to heterocyclic compounds of formula (I) or to therapeutically acceptable salt thereof, where X represents benzo [d] thiazolyl, optionally substituted with one or two R4; Y1 represents a pirrolil, pyrazolyl, triazolyl or pyridinyl; where Y1 is optionally substituted with one or two substitutes independently selected from a group consisting of R5, CO(O)R5, CO(O)H and CN; L1 selected from group comprising (CR6R7)q, (CR6R7)s-O-(CR6R7)r, (CR6R7)s-C(O)-(CR6R7)r, (CR6R7)s-S(O)2-(CR6R7)r and (CR6R7)s-NR6A-(CR6R7)r; and Y2 is selected from a group consisting of C3-4 alkyl with branched chain, C5-7 cycloalkyl, C6-7 cycloalkyl, phenyl, piperidinyl, morpholinyl and tetrahydropiranyl; where the phenyl is optionally condensed with benzene; where Y2 optionally substituted with one, two or three substitutes independently selected from a group consisting of R8, OR8, SO2R8, CO(O)R8, NHR8, N(R8)2, C(O)H, OH, CN, NO2, F, Cl, Br and I; or L1 represents a bond; and Y2 is selected from a group consisting of C5 cycloalkyl, phenyl, tetrahydropiranyl and piperidinyl; where C5 cycloalkyl and tetrahydropiranyl presented by Y2 are optionally condensed with benzene; Z1 is selected from group consisting of or ; R1, R2 and R3 are absent; R4, in each case is independently selected from group consisting of OR12 and halogen; R5, in each case is independently selected from group consisting of C1-6 alkyl, C1-6 hydroxyalkyl, phenyl and cyclopropyl; R6A represents C1-6 alkyl; each R6 and7, in each case are independently selected from group consisting of hydrogen, R15 and CO(O)R15; R8, in each case is independently selected from group consisting of C1-6 alkyl, C2-6 alkynyl, phenyl, piperidinyl and morpholinyl; where R8 C1-6 alkyl and C2-6 alkynyl are optionally substituted with one, two or three substitutes independently selected from a group consisting of R16, OR16, SO2R16, C(O)R16, NHR16, N(R16)2, OH and F; where R8 phenyl is optionally substituted with one Cl; Rk, in each case represents C1-6 alkyl; R12 is C1-4 alkyl; R15, in each case is independently selected from a group consisting of C1-4 alkyl and phenyl; where R15 C1-4 alkyl is optionally substituted with one substitute selected from a group consisting of C1-4 alkoxy, morpholinyl and C6cycloalkyl; R16, in each case is independently selected from a group consisting of C1-4 alkyl, C1-4 hydroxyalkyl, phenyl, tetrahydropiranyl, morpholinyl, 1,4-dioxanyl, dioxydotiomorfolinyl and pyridinyl; q equals to 1, 2 or 3; s, r, m, n and p equals to 0; or where the compound is selected from a group specified in item 1. Invention also relates to pharmaceutical composition based on the above compounds and method of cancer treating. EFFECT: technical result allows obtaining new heterocyclic compounds effective in cancer treating. 9 cl, 3 tbl, 188 ex

ethod for producing a pharmaceutical formulation of rocuronium bromide in the form of a stable lyophilisate and pharmaceutical composition obtained using said method // 2594062
FIELD: pharmaceutics. SUBSTANCE: present invention relates to pharmaceutical industry and to a method for producing a pharmaceutical formulation of rocuronium bromide in the form of a stable lyophilisate for injection or infusion. Method includes placing the solution rocuronium bromide in ampoules or bottles in a sublimation chamber, where the solution is frozen to (-41)-(-49)°C at the rate (-12)-(-13) deg/h during 7-9 hours, held for 6-9 hours, then the ampoules (bottles) are heated at a rate of 7-10 deg/h during 7-9 % to 20-25 °C and kept at this temperature for 5-9 hours. Pharmaceutical formulation includes rocuronium bromide as an active ingredient, sodium chloride or potassium chloride, acid to bring pH to 3.8-4.8 and water for injections. EFFECT: pharmaceutical formulation storage life increases up to 5 years. 2 cl, 3 tbl, 1 ex

Agent intensifying action of anti-cancer agents // 2589713
FIELD: pharmaceutics.SUBSTANCE: invention relates to an agent improving anti-cancer effect of another antitumour agent containing 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide and another antitumour agent, which is selected from a group consisting of paclitaxel, gemcitabine, lapatinib, tegafur-gimeracil-oteracil potassium combination drug and irinotecan. Invention also relates to an antitumour agent based on said components, use of said quinoline carboxamide derivative and a method of treating a tumour, based on use of agent consisting of said quinoline carboxamide derivative and other antitumour agent.EFFECT: technical result is development of an agent enhancing antitumour effect of another antitumour agent.6 cl, 9 dwg, 6 tbl, 7 ex

Dihydrooxazole-2-amine derivatives // 2587512
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I), in which R1 is hydrogen or lower alkyl; R2 represents hydrogen or represents heteroaryl, selected from a pyridinyl, containing as a substitute cyano group; R3 represents hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy group, lower alkoxy group, substituted with halogen, cyano group, S-lower alkyl, S(O)-lower alkyl, S(O)2-lower alkyl, C(O)-lower alkyl or C3-6-cycloalkyl; R4 is hydrogen or lower alkyl; 6-member aromatic ring, possibly containing (N), is a phenyl or pyridinyl, in which N atom can be in different positions; X is a bond or -CH(CF3)-; Ar denotes aryl or heteroaryl, selected from phenyl, naphthyl, quinolinyl, pyridinyl, pyrimidinyl, pyrazinyl, possibly containing one or more as a substitute R3. Invention also relates to a pharmaceutical composition having high affinity for trace amine receptors (TAAR1), containing as an active ingredient a compound of formula (I) and a pharmaceutically acceptable carrier.EFFECT: dihydrooxazole-2-amine derivatives, having high affinity for trace amine receptors (TAAR1), used as therapeutically active substance.14 cl, 1 tbl, 75 ex,

Catechol-o-methyl transferase inhibitors and use thereof in treating psychotic disorders // 2586974
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, namely to derivatives of 4-pyridinone formula I or pharmaceutically acceptable salts thereof, where A is hydrogen, B(OH)2, halogen, C(O)NH(CH2)nC(O)N(R3)2; X is hydrogen or halogen; Y denotes phenyl, benzimidazolil, benztiazolil, benzoksazolil, benzpiperidinil, quinolyl, indolyl, indazolyl or pyridyl, each optionally substituted with 1-3 groups Ra, provided that Y denotes phenyl, then at least one of said Ra selected from OCF3, O(CH2)nC3-6cycloalkyl, NR2C(O)R2, C(O)R2, N(R2)2, (CH2)nC(O)OR2, OR2, (CH2)nheterocyclyl, NH(CH2)nheterocyclyl, (CH2)n(C)6-10aryl, O(CH2)nC6-10aryl or O(CH2)nheterocyclyl, where said heterocyclic ring and aryl optionally substituted with 1-3 groups Rb; R1 represents hydrogen, NR2R3, Si(CH3)3, (CH2)nC6-10aryl, C2alkenyl or C1-4alkyl, said alkyl and alkenyl optionally substituted with 1-3 groups of halogen, OH, C1-6alkyl, O-C1-6alkyl, NR2R3, SOR2, NHSO2R2, CF3, C6-10aryl, heterocyclyl, -C≡C-C6-10aryl, C(O)NR2R3, wherein said aryl and heterocyclyl optionally substituted with 1-2 groups Ra; R2 and R3 independently denote H, C1-6alkyl, (CH2)nheterocyclyl, (CH2)nC6-10aryl, wherein said aryl optionally substituted by group Ra or R2 and R3 together with nitrogen atom to which they are bonded, form a 6-member ring, which contains oxygen; Ra is C1-6alkyl, halogen, CF3, OCF3, C3-6cycloalkyl, O(CH2)nC3-6cycloalkyl, NR2C(O)R2, C(O)R2, CN, N(R2)2, (CH2)nC(O)OR2, OR2, (CH2)nheterocyclyl, NH(CH2)nheterocyclyl, (CH2)nC6-10aryl, O(CH2)nC6-10aryl or O(CH2)nheterocyclyl, wherein said heterocyclyl and aryl optionally substituted with 1-3 groups Rb; Rb is C1-6alkyl, halogen, CHF2, oxo (=O), N(R2)2, CH2OH, S(O)2NR2R3, (CH2)nC6-10aryl, (CH2)nheterocyclyl, NH(CH2)nheterocyclyl, OR2, C3-6cycloalkyl, CF3 or CN; and n equals 0-3; and where heterocycle is aromatic or saturated or partially saturated monocyclic or bicyclic ring containing 5-10 atoms, among which 1-4 atoms are heteroatoms selected from nitrogen, oxygen and sulphur. Invention also relates to pharmaceutical composition based on compound of formula I, method of treating and/or preventing neurological and psychiatric disorders and method of intensifying action of antipsychotic agent based on use of compound of formula I.EFFECT: new compounds are prepared effective in treating diseases associated with catechol-O-methyltransferase (COMT).52 cl, 1 tbl, 17 ex

ethod of creating therapeutic soft contact lenses // 2585746
FIELD: medicine.SUBSTANCE: invention can be used for creating therapeutic soft contact lenses (SCL). Method involves saturation of lens from water solution of levofloxacin. At that, is saturating solution of levofloxacin is additionally include indometacin so that concentration of levofloxacin in this solution is 0.25-0.33 %, and indometacin 0.033-0.05 %. Washed in distilled water lenses are placed in solution in amount of 2.0-2.5 ml of solution per one lens and left for 12-18 hours at room temperature in dark place. Method makes it possible to introduce in lens simultaneously two preparation at increase of indometacin, sorbed by lens, in comparison with sorption of individual solutions.EFFECT: creation of such therapeutic SCL enables increasing efficiency of treating eye diseases and damages.1 cl, 1 tbl, 15 ex

Pharmaceutical composition containing pyridone derivatives // 2585287
FIELD: chemistry.SUBSTANCE: invention relates to a compound of a pyridone derivative of formula I or its pharmaceutically acceptable salt, R or S isomer, where A is a C1-C10-heteroaryl group, which is unsubstituted or substituted with one or two substitutes selected from a group consisting of halogen group C1-C6-alkyl group, C3-C7-cycloalkyl group, C6-C12-aralkyl group, C1-C6-alkoxy group and C6-C12-aryl group; B represents O or NH; and C1-C10-heteroaryl group is selected from a group consisting of thiazolyl, benzothiazolyl, pyridyl, isoxazolyl, isquinolyl, quinolyl, benzothiadiazole, thiadiazole, pyrazolyl and pyrazinyl. Invention also relates to a pharmaceutical composition for preventing or treating cognitive disorders, wherein composition contains a pyridone derivative of formula I, its pharmaceutically acceptable salt, R or S isomer, in a therapeutically effective amount and a pharmaceutically acceptable carrier.EFFECT: technical result is a pyridone derivative as an agonist or partial agonist of α7-nicotinic acetylcholine receptor.6 cl, 2 tbl, 48 ex

Agonists of protein tyrosine phosphatase-1 containing homology-2 src domain, and methods of treating using said agonists // 2584986
FIELD: pharmaceutics.SUBSTANCE: in formula I R1 and R3 independently represent hydrogen, and R2 represents , , , , or R1 independently represents hydrogen, R3 is methyl, and R2 represents or or R2 and R3 independently represent hydrogen, and R1 is . Invention also refers to pharmaceutical compositions containing said compound, a method for increasing Src homology-2 containing proteintyrosinephosphatase-1 (SHP-1) expression in a cell, method of treating diseases or pathological condition characterised by low expression SHP-1, and to use of said compounds for preparing a drug for treating diseases or pathological condition characterised by low expression of SHP-1.EFFECT: disclosed are novel compounds of formula I, having Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity.11 cl, 6 tbl, 23 dwg, 2 ex

Synthesis and anticancer activity of derivatives of aryl and heteroaryl quinolines // 2584688
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I and pharmaceutically acceptable salts thereof , where R is hydrogen, RO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2; W represents 2-halogenphenyl, 3-halogenphenyl or 4-halogenphenyl; R5 is (C1-C6)alkoxy, hydroxyl or OR8; R6 is hydroxyl or (C1-C6)alkoxy; R7 represents hydrogen, hydroxyl or O-(C1-C6)alcylenphenyl; R8 represents a RO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2, and m is monovalent metal ion; or where R is hydrogen, RO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2; W represents 2-halogenphenyl, 3-halogenphenyl or 4-halogenphenyl; R5 represents hydrogen, (C1-C6)alkoxy, hydroxyl or OR8; R6 is (C1-C6)alkoxy; R7 is hydroxyl or O-(C1-C6)alcylenphenyl; R8 represents PO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2, and m is monovalent metal ion. Disclosed compounds have anti-cancer activity. Invention also relates to compounds of formula I, radicals of which are presented in patent claim and to using pharmaceutical composition containing effective amount of compound of invention for treating cancer.EFFECT: technical outcome is new compounds possessing anticancer activity.17 cl, 23 dwg, 7 tbl, 4 ex

Pharmaceutically acceptable salt (e)-n-[4-[[3-chloro-4-(2-pyridylmethoxy) phenyl] amino] -3-cyano-7-ethoxy-6-quinolyl] -3-[(2r)- 1- methylpyrrolidin-2-yl] prop-2-enamide, method for production and use thereof in treating cancer // 2583056
FIELD: pharmaceutics.SUBSTANCE: invention relates to a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide (formula (I)), where n equals 1, 2 or 3; and M is a molecule of acid, where said salt is selected from group consisting of hydrochloride, para-toluene sulphonate, methanesulphonate, maleate, succinate and L-malate. Invention also relates to method of producing salt of formula (I), pharmaceutical composition based on salt compound of formula (I) and use of salt compound of formula (I).EFFECT: novel salt of compound of formula (I) effective in treating cancer.10 cl, 7 tbl, 13 ex
Heteroarylsulphonamide derivatives, production and use thereof for human treatment // 2582995
FIELD: chemistry.SUBSTANCE: invention relates to geteroarilsulfonamide derivatives of formula I, where R1 is a substituent of the phenyl nucleus X selected from the group consisting of: hydrogen, F, Cl, Br, trifluoromethyl, trifluoromethoxy group, a linear or branched C1-C4-alkyl, linear or branched C1-C4 alkoxy group; n is 0, 1 or 2; A is oxygen or sulfur; D is -C (=O)-, -CH2O- or -O-; B is a nitrogen atom if n = 1 or 2, and D is -C(=O) -, or B is CH, if n = 0, and Dis -CH2O-, or if n = 1, D is -O-; R2 is hydrogen, and HetAr is pyridyl or quinolyl, optionally containing a substituent which is a linear or branched C1-C4-alkyl or trifluoromethyl; or pharmaceutically acceptable salts thereof. Invention also relates to the methods for producing compounds of formula I and to the pharmaceutical composition containing a therapeutically effective amount of the compound of formula I. EFFECT: technical result is geteroarilsulfonamide derivatives of formula I, with blocking activity to Kv1,5 potassium channels.12 cl, 1 tbl, 35 ex
Quinoline derivatives and melk inhibitors containing same // 2582610
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, namely to a heterocyclic compound of general formula (I) or its pharmaceutically acceptable salt thereof, where: R1 is C1-C6 alkyl sulphonyl or -CO-R5, where R5 is C1-C-6 alkyl or C3-C5 cycloalkyl; R2 represents phenyl which can contain group substitute selected from group of substitutes C, or -NR6AR7A, where R6A is hydrogen atom and R7A is -(CH2)n-R10A (where n equals whole number from 0 to 2 and R10A represents mono- or tricyclic C3-C10 cycloalkyl, which can contain group substitute selected from group of substitutes D, phenyl, which can contain group substitute selected from a group of substitutes E, aliphatic heterocyclic group which is selected from piperidinil, piperazinil and azabicyclooctanil and can be substituted C1-C-6 alkyl, aromatic heterocyclic group which is selected from a pyridinyl, pyrimidinyl and pirazolil and can contain group substitute selected from a group of substitutes I), or R6A and R7A is formed with adjacent nitrogen atom aliphatic heterocyclic group that is selected from piperidinil and piperazinil and may contain group substitute selected from a group of substitutes F; R3 is C6-C10 aryl, which can contain group substitute selected from a group of substitutes G, or aromatic heterocyclic group which is selected from a pyridinyl, pyrimidinyl, tiofenil, isoxazolyl, pyrrolyl and pirazolil and can contain group substitute selected from a group of substitutes H; R4 is hydrogen atom or halogen; R is hydrogen atom or halogen; and R101 is hydrogen atom; where said substitutes C - I are one-three substitutes are given in claim. Invention also relates to pharmaceutical composition, an inhibitor of MELK, agent, which simulates the expression MELK, anticancer agent based on compounds of formula (I), method of treating and/or preventing diseases, which includes MELK overexpression, using compound of formula (I).EFFECT: obtained are novel heterocyclic compounds effective as anti-tumour agent.19 cl, 4 tbl, 1200 ex

Substituted 2-oxo- and 2- thioxo- dihydroquinoline-3-carboxamides as kcnq2/3 modulators // 2581362
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to organic chemistry, namely to derivative 2-oxo- and 2-thioxodihydroquinoline-3-carboxamides of formula in the form of free compounds, or in the form of salts of physiologically acceptable acids or bases, wherein X means O or S, R1 represents an unsubstituted C1-7-aliphatic residue; or aryl specified in phenyl unsubstituted or monosubstituted by at least one substitute specified in a group, which contains F, Cl, Br; R2 represents CF3; C1-4-aliphatic residue or O-C1-4-aliphatic residue, wherein C1-4 aliphatic residue in each case is unsubstituted; each R3, R4, R5 and R6 independently represents H; F; Cl; Br; CN; CF3; OCF3; provided at least one of R3, R4, R5 and R6 does not represent H; R7 represents C1-7-aliphatic residue unsubstituted, or mono- or disubstituted; or 6-merous heterocycloaliphatic residue specified in tetrahydropyrane; wherein the 'aliphatic residue' in each case can be branched or unbranched, saturated; wherein 'mono- or disubstituted' in relation to the 'aliphatic residue' refers in the view of respective residues or groups, to substitution of one or two hydrogen atoms specified in one or two hydrogen atoms, each independently, by at least one substitute specified in a group, which contains OH, O-C1-4-aliphatic residue, COOH or C(=O)-O-C1-4-aliphatic residue. The invention also refers to a pharmaceutical composition based on the compound of formula (I).EFFECT: new compounds effective in treating and/or preventing diseases mediated by KCNQ2/3 K+ canals are produced.8 cl, 2 tbl, 45 ex
 
2551303.
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