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Having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole (A61K31/41)

Using ep4 receptor antagonists in treating il-23-mediated diseases

Invention refers to a compound with EP4 receptor antagonist activity or its pharmaceutically acceptable salt, which is effective in treating an immune disease or allergy. This invention also refers to a compound of formula (I), (II), (III), (IV), (Va) or (Vb) or its pharmaceutically acceptable salt with EP4 receptor antagonist activity, which is effective in treating an immune disease or allergy. This invention also refers to a pharmaceutical composition for treating an immune disease or allergy, which contains a therapeutically effective amount of the compound of formula (I), (II), (III), (IV), (Va) or (Vb) or its pharmaceutically acceptable salt.

Drugs for treatment of helminthiasis of animals

Drug for treatment of helminthiasis of animals comprises albendazole sulphoxide, butafosfan and water for injections with the following mass ratio of components, %: albendazole sulphoxide (n-[6-(propan-1-sulphinyl)-1H-1,3-benzodiazole-2-yl] methoxy carboximide acid) 5.0-10.0; butafosfan (1-butylamino-1-methyl) ethylphosphonic acid) 10.0-20.0; water for injections - the rest.

Pesticide composition

Pesticide composition contains a compound of formula one:

1-[ω-aryloxyalkyl(benzyl)]-substituted 2-aminobenzimidazoles, having activity on influenza virus

Invention relates to organic chemistry and particularly to novel benzimidazole derivatives of formula 1a-f:

Method of external treatment of skin mycosis

Method of external treatment of skin mycosis

Loci of skin affection are successively processed first with eliminating solution, which represents 10-20% hypertonic solution of sodium chloride, then - 1% water solution of carbol fuchsin and after 10-15 minutes composition, which consists of 20-30 parts of tisolium and 80-70 parts of antimycotic, selected from the group: pimafucin, travogen, fungoterbine-neo, zalain, is applied, with processing being carried out twice per day for 14 and more days, daily alternating all 5 mentioned antimyotics in composition.

Method of treating cardiovascular diseases

Invention refers to pharmaceutical industry and represents a pharmaceutical dosage form for treating cardiovascular diseases and introduced once a day, containing a combination of fixed doses of metoprolol or its pharmaceutically acceptable salt in the sustained-release form, amlodipine, or valsartan, or olmesartan, or lisinopril, or enalapril, or their pharmaceutically acceptable salts, and one or more speed-control polymeric excipients containing cellulose polymers or their derivatives, and acrylic acid polymers or their derivatives, which form two layers on metoprolol or their pharmaceutically acceptable salt,wherein the dosage form possesses such a solution profile that less than 6% of metoprolol or its pharmaceutically acceptable salt releases for 1 hour.

1,6-diazabicyclo[3,2,1]octan-7-onА derivatives and using them in treating bacterial infections

1,6-diazabicyclo[3,2,1]octan-7-onА derivatives and using them in treating bacterial infections

Invention refers to a new heterocyclic compound of general formula (I) or its stereoisomer, or its pharmaceutically acceptable salt, wherein Q means oxadiazol, thiadiazole or tetrazole; R1 means: (b) (CO)n-R3 or (c) COOR4, n=0 or 1; R2 means SO3M, M means hydrogen or cation; R3 means: (a) C1-C6-alkyl optionally substituted by one or more substitute independently specified in halogen, NR6R7, heterocyclyl or aryl, (b) NR6R7, (c) CONR6R7, (d) aryl, (e) heterocyclyl, or (f) heteroaryl optionally substituted by CONR6R7, R4 means (a) hydrogen, or (b) C1-C6-alkyl; each R6 and R7 independently means (a) hydrogen or (b) R6 and R7 are coupled together to form a four- to seven-merous ring, wherein cycloalkyl represents 3-7-merous cyclic hydrocarbon radical; heterocyclyl represents 4-7-merous cycloalkyl group containing one or more heteroatoms specified in nitrogen, oxygen or sulphur; aryl represents monocyclic or polycyclic hydrocarbon containing 6-14 atoms in the ring; heteroaryl represents monocyclic or polycyclic heteroaryl, wherein one or more carbon atoms are substituted by heteroatoms specified in nitrogen, oxygen or sulphur. The invention also refers to a pharmaceutical composition based on the compound of formula (I) and a method for preventing or treating a bacterial infection based on using the compound of formula (I).

Method for obtaining losartan potassium nanocapsules in xanthan gum

Method for obtaining losartan potassium nanocapsules in xanthan gum

Invention relates to method for obtaining losartan potassium nanocapsules in xanthan gum. Claimed method consists in the following: losartan potassium is dissolved in chloroform and obtained mixture is dispersed into xanthan gum suspension in benzene in presence of preparation E472c with mixing, after that acetone and water are poured in, obtained suspension is filtered and dried, with envelope/core ratio in nanocapsules constituting 3:1 or 1:5.

Oxoazetidine derivatives, method for producing them and using them in medicine and cosmetic medicine

Oxoazetidine derivatives, method for producing them and using them in medicine and cosmetic medicine

Invention refers to organic chemistry, namely new oxoazetidine derivatives of general formula

Method of correction of mineral metabolism of dictyocaulosis of sheep

Method comprises dehelminthisation using alben and administering of immunomodulators of T-activin and B-activin and probiotic of lactoferon. The course of treatment is repeated three times at intervals of 7 days.

Pharmaceutical compositions containing beta-lactam antibiotic, sulbactam and beta-lactamase inhibitor

Pharmaceutical compositions containing beta-lactam antibiotic, sulbactam and beta-lactamase inhibitor

Group of inventions refers to medicine and may be used in treating infectious diseases. A pharmaceutical composition contains one beta-lactam antibiotic or its pharmaceutically acceptable salt, sulbactam or its pharmaceutically acceptable salt and trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide or its pharmaceutically acceptable salt. The methods according to the invention concern treating a bacterial infection by administering the above composition.

Sigma-ligands for application in prevention and/or treatment of postoperative pain

Sigma-ligands for application in prevention and/or treatment of postoperative pain

Group of inventions relates to the application of a sigma-ligand of formula (I) for the prevention and/or treatment of acute and chronic pain, developed as a result of a surgical operation; to the application of the sigma-ligand of formula (I) for obtaining a medication for the prevention and/or treatment of the said pain and to a respective method of prevention and/or treatment.

Daktarin therapy of candida-associated chronic processes in oral mucosa

Invention represents using Daktarin preparation for treating Candida-associated chronic processes in the oral mucosa in the form of local applications on the mucosal surface having lesion elements, and per os in a dose of 0.5 g 2 times a day after meals for 10 days.

Antispasmodic medication

Antispasmodic medication

As compound, possessing antispasmodic activity claimed is dihydrochloride 9-dialkylaminoethyl-2-(4-chlorophenyl)imidazol[1,2-a]benzimidazole of general formula I where Ia NR2= dimethylamino- Ib NR2 = diethylamino-. Therapeutic index of dihydrochloride 9-dialkylaminoethyl-2-(4-chlorophenyl)imidazol[1,2-a]benzimidazole was in 10 times higher than of sodium valproate.

Cyclopentyl- and cycloheptylpyrazole as fxr modulators

Cyclopentyl- and cycloheptylpyrazole as fxr modulators

Claimed invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of formula I, where A and R1-R4 are determined in formula of invention, or their pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition containing them and application of claimed compounds.

Targeting cancer tumours by application of inhibitors of carbonic anhydrase ix isoforms

Targeting cancer tumours by application of inhibitors of carbonic anhydrase ix isoforms

Invention relates to field of organic chemistry, namely to novel nitroimidazole derivatives of formula (1) and to its pharmaceutically acceptable salts, where Z represents Z1 with formula (2a), or Z represents Z2 with formula (2b): (CH2)nCH2X, or Z represents Z3 with formula (2c), and R1 and R2 each independently can represent H or CH3, R3, R4, R6 and R7 each independently can represent H, sulphonamide, sulphamate or sulphamide, R5 can represent H, sulphonamide, sulphamate or sulphamide, X = sulphonamide, sulphamate or sulphamide Y = S, and n = 0, 1 or 2, and where, if n = 0, R2 = 2-CH3, Z = Z1, R3 = R4 = R6 = R7 = H and R5 = SO2NH2, then NO2 is not in position 4, and where if R5 represents H, at least one of R3, R4, R6 and R7 is not H. Invention also relates to application of formula (1) compound and method of treating disease, characterised by superexpression of one or several carbonic anhydrases.

Nucleoside inhibitors of rna-polymerase hcv ns5b, methods for production and use thereof

Nucleoside inhibitors of rna-polymerase hcv ns5b, methods for production and use thereof

Invention relates to C3alkyl ethers (S)-2-{[(2R,3R,5R)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-4,4-difluoro-3-hydroxy-tetrahydrofuran-2-ylmethoxy]phenoxy-phosphoryl amino}-propionic acid of general formula 1 and pharmaceutically acceptable salts thereof. The compounds have properties of nucleoside inhibitors of RNA-polymerase HCV NS5B and can be used to treat and prevent viral diseases such as hepatitis C. In formula R1 is C1-C4alkyl. A pharmaceutical composition based on a compound of formula 1 may further contain an inhibitor of RNA-polymerase NS5A, such as Ribavirin, Ribamidin or methyl ether hydrochloride [(S)-1-((S)-2-{5-[4-(4-{2-[(S)-1-((S)-2-methoxycarbonylamino-3-methyl-butyryl)pyrrolidin-2-yl-3H-imidazol-4-yl]buta-1,3-diinyl)phenyl]-1H-imidazol-2-yl}pyrrolidin-1-carbonyl)-2-methyl-propyl]}-carbamic acid (AV-4025).

2-[3-(5-nitrofuran-2-yl)-1-phenyl-1h-1,2,4-triazole-5-yl] hexanoic acid and method of its manufacturing

2-[3-(5-nitrofuran-2-yl)-1-phenyl-1h-1,2,4-triazole-5-yl] hexanoic acid and method of its manufacturing

Invention relates 2-[3-(5-nitrofuran-2-yl)-1-phenyl-1H-1,2,4-triazole-5-yl] hexanoic acid of the formula I and method of its manufacturing.

Phosphodiesterase 10 modulators

Phosphodiesterase 10 modulators

Invention relates to formula compound, in which X and X1 independently represent CR4 or N; Y and Y1 independently represent C or N; Z and Z1 independently represent CR6, NR7, N, O or S; R1 and R2 are independently selected from C1-C7-alkyl, C3-C8-cycloalkyl, or R1 and R2, together with nitrogen atom, they are bound to, form spirobicyclic saturated ring system, including from 5 to 12 ring atoms, including heteroatoms, selected from N, O, or 4-, 5- or 6-membered heterocycloalkyl, containing 1 or 2 heteroatoms, selected from N, O, S, which can contain from 1 to 3 substituents, independently selected from halogen; R3 represents C1-C7-alkyl; R4 represents hydrogen, C1-C7-alkyl, C1-C7-halogenalkyl or halogen; R5 represents phenyl or heteroaryl, with both groups probably containing C1-C7-alkyl, halogen, C1-C7-alkoxygroup as substituent; R6 represents hydrogen, C1-C7-alkyl or R5 and R6, together with Y1 and Z atom, which they are bound to, form phenyl ring, possibly substituted with C1-C7-alkyl, halogen; R7 represents C1-C7-alkyl, C3-C8-cycloalkyl, C1-C7-halogenalkyl, C1-C7-alkoxyalkyl, phenyl, heteroaryl or C1-C7-alkyl, possibly substituted with phenyl or C3-C8-cycloalkyl, or R5 and R7, together with Y1 and Z atom, which they are bound to, form heteroaryl, possibly substituted with C1-C7-alkyl, C1-C7-halogenalkyl; W is selected from ethylene, possibly substituted with C1-C7-alkyl, and to its physiologically acceptable salts.

Preparation for skin care, possessing antifungal properties (versions)

Preparation for skin care, possessing antifungal properties (versions)

Invention represents preparation for skin care, possessing antifungal properties and contains hydrochloride of 2-benzimidazolylcarbamic acid methyl ether, salicylic acid, dimethylsulphoxide and ethanol, with components in preparation being in specified ratio in wt %.

1,2,4-triazolone derivative

1,2,4-triazolone derivative

Invention relates to 1,2,4-triazolone derivatives and pharmaceutically acceptable salts thereof. The disclosed compounds have antagonistic activity with respect to the arginine vasopressin V1b receptor. In formula (IA): R1 is C1-5 alkyl (the C1-5 alkyl is optionally substituted with 1-3 groups selected from a group consisting of hydroxy, halogen atoms, and C3-7 cycloalkyl), C3-7 cycloalkyl or a 4-8-member saturated heterocycle, containing one heteroatom selected from an oxygen atom; R2 is a hydrogen atom; R3 is a phenyl or pyridyl (the phenyl or pyridyl is optionally substituted with 1 or 2 groups selected from a group consisting of C1-5 alkoxy, halogen atoms, cyano and C1-5 alkylsulphonyl); R4 and R5 can be identical or different, and each is a hydrogen atom or C1-5 alkyl (the C1-5 alkyl is optionally substituted with one hydroxy), or R4 and R5 optionally, together with a nitrogen atom with which they are bonded, form a 4-8-member saturated or unsaturated heterocycle, optionally containing one nitrogen, oxygen or sulphur atom, in addition to the nitrogen atom with which they are bonded, in a ring (the 4-8-member saturated or unsaturated heterocycle is optionally substituted with one or two groups selected from a group consisting of hydroxy, C1-5 alkyl ( the C1-5 alkyl is optionally substituted with one hydroxy), C1-5 alkoxy, halogen atoms, cyano, C2-5 alkanoyl, aminocarbonyl, trifluoromethyl and amino (the amino is optionally substituted with one or two groups selected from a group consisting of C1-5 alkyl and C2-5 alkanoyl), and the 4-8-member saturated heterocycle optionally has a C1-5 alkylene group which crosslinks two different carbon atoms in the ring, or form 2-oxa-6-azaspiro[3.3]hept-6-yl or 7-oxa-2-azaspiro[3.5]non-2-yl; A is phenylene, pyridinediyl or pyrimidinediyl (the phenylene, pyridinediyl and pyrimidinediyl are optionally substituted with one group selected from halogen atoms and C1-5 alkoxy); X is a single bond or -O-; Ra is a hydrogen atom or a C1-5 alkyl and n equals 0 or 1. The invention also relates to 1,2,4-triazolone derivatives, the structural formulae and values of radicals of which are given in the claim, to a pharmaceutical composition and to a therapeutic or preventive agent containing a 1,2,4-triazolone derivative or a pharmaceutically acceptable salt thereof.

Stabilised voriconazole composition

Stabilised voriconazole composition

Group of inventions refers to medicine, namely to pharmacology, and is applicable for producing a stabilising composition containing voriconazole. Stabilising a lyophilised composition is ensured by using lactose, wherein its amount required for the stabilisation process on a lactose monohydrate basis makes at least 3 weight fractions in relation to voriconazole. A method for stabilising the composition involves the stages of providing an aqueous solution containing voriconazole and hydroxypropyl-beta-cyclodextrine, adding at least 3 weight fractions of lactose, and lyophilising the produced composition. The stabilised composition for intravenous administration contains one weight fraction of voriconazole, 10-30 weight fractions of 2-hydroxypropyl-beta-cyclodextrine and at least 3 weight fractions of lactose on the lactose monohydrate basis.

Method of treating patients with chronic alcohol intoxication

Method of treating patients with chronic alcohol intoxication

Combination drug Thiocetam is administered in a dose of 100 mg/kg a day expressed as piracetam during 14 days.

2-aryl-substituted n-arylimidazolines, selective cyclooxygenase-2 inhibitors, methods for production and use thereof

2-aryl-substituted n-arylimidazolines, selective cyclooxygenase-2 inhibitors, methods for production and use thereof

Compounds have selective cyclooxygenase-2 inhibitor properties and can be used to treat inflammatory diseases. The diseases can be selected from: articular syndrome with rheumatism and acute gout, rheumatoid arthritis, psoriatic arthritis, osteoarthrosis, radiculitis, in inflammatory processes of ligaments, tendons, ischias, lumbago, menstrual pain or inflammation, associated with inflammations caused by sunburn, skin damage by ultraviolet light, different forms of cancerous diseases of the skin. In formula 1 R is C1-C3 alkyl or an amino group, R' is hydrogen or C1-C3 alkyl, Ar is optionally substituted with a halogen, C1-C3 alkyl, C1-C3 alkoxy group or CF3 aryl; or a 5- or 6-member hetaryl containing one nitrogen, oxygen or sulphur atom in the ring. The invention also relates to a method of producing said compounds. The method includes reaction of a compound of general formula 3 with a substituted ethylenediamine of general formula 4, followed by reaction of the compound of general formula 5: with a compound of general formula 6 to form a compound 1.1, or with a compound of general formula 7 to form a compound 1.2 through an intermediate step of removing the protective group in the compound of general formula 8 according to the scheme where R and R' assume values given above.

Cyclopentylacrylamide derivative

Cyclopentylacrylamide derivative

Invention relates to compound, represented by general formula or its pharmaceutically acceptable salt, in which R1 and R2 independently represent hydrogen atom, C1-C6alkylsulphonyl group, which includes cyclopropylsulphonyl group, or C1-C6alkoxy- C1-C6alkylsulphonyl group, and A is selected from group which includes: thiazolyl group, 1,2,4-thiadiazolyl group, pyrazolyl group, pyridyl group, pyrazinyl group, isooxazolyl group, benzothiazolyl group and thiazolo[5,4-b]pyridyl group, and A can be mono-substituted by substituent, selected from group, which includes halogen atom; C1-C6alkyl groups, optionally substituted with halogen atom or hydroxyl group; C1-C6alkoxyl groups, optionally substituted with halogen atom or hydroxyl group; C1-C3alkoxy-C1-C2alkoxyl groups; C1-C3alkoxycarbonyl-C1-C2alkoxyl groups; C1-C6alkylsulphanyl groups; C1-C6amino-alkylsulphanyl group, optionally substituted with C1-C3alkyl group; C1-C6alkylsulphanyl-C1-C6alcoxyl groups; phenyl group; 1,3-dipxolane, substituted with two C1-C6alkyl groups; piperazinesulphonyl is substituted with methyl group; 1,3-dioxolanemethyl, substituted with two methyl groups; piperazinemethyl, substituted with methyl group; tetrahydropyranyloxy-C1-C3alkoxy group; aminosulphonyl groups, optionally substituted with C1-C3alkyl group; C1-C6 hydroxyalkylsulphanyl groups; -(O)(CH2)C(O)O-C1-C6alkyl group; -C(O)O-C1-C6 alkyl group; as well as groups, represented by general formula -(CH2)mP(O)R4R5 (where R4 and R5 independently represent C1-C3alkoxyl group; m is integer number from 0 to 1). Compound of formula (1) is intended, as active ingredient, for production of pharmaceutical composition, which has effect for activation of glucokinase (GK) or hypoglycaemic action. Invention also relates to intermediate compounds, represented by formula in which R1 and R2 independently represent hydrogen atom, C1-C6alkylsulphonyl group, which includes cyclopropylsulphonyl group, or C1-C6alkoxy-C1-C6alkylsulphonyl group.

Method of treating chronic erosive gastritis associated with helicobacter pylori

Invention concerns treating chronic erosive gastritis associated with Helicobacter pylori (HP). The oral mucosa HP content is pre-assessed by means of plaque urease test. The oral mucosa HP content is shown by discoloration of Zakse medium. The treatment starts with removing the dental plaque. That is followed by anti-Helicobacter therapy and gingival applications of metronidazole for 30 minutes after tooth brushing after breakfast and at bedtime. If the Zakse medium colour changes from yellow to raspberry red for the first 20 minutes, the high bacterial content is stated. The treatment involves the four-component anti-Helicobacter therapy and the gingival applications for the period of 14 days. If the Zakse medium colour changes in between the 21st and 40th minutes, the moderate bacterial content is stated. The treatment involves the 10-day three-component anti-Helicobacter therapy and the gingival applications for the period of 7 days. If the Zakse medium changes its colour by the end of the first hour, the mild bacterial content is detected. The treatment involves the 7-day three-component anti-Helicobacter therapy. During the month following the treatment, the oral cavity is sanitated. The sanitation involves tooth brushing after breakfast and at bedtime for 2 minutes with Mexidol toothpaste with Metrogil Denta gel added in a match head sized amount and mouthwash with 0.05% chlorhexidine bigluconate 15 minutes after tooth brushing. The sanitation is repeated one month before the expected aggravation of the disease.

Treatment of hypertension and/or prevention and treatment of heart failure in mammal, receiving anticoagulant therapy

Treatment of hypertension and/or prevention and treatment of heart failure in mammal, receiving anticoagulant therapy

To treat heart failure in individual, receiving anticoagulant therapy introduced are: a) pharmaceutical composition, including therapeutically effective quantity of trisodium [3-((1S,3R)-1-diphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl-{2″-(tetrazol-5-ylate)diphenyl-4′-ylmethyl}amino)butirate]semi-pentahydrate and pharmaceutically acceptable carrier or b) pharmaceutical composition, including therapeutically effective quantity of (i) valsartan or its pharmaceutically acceptable salt; (ii) ethyl ester of N-(3-carboxy-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methylbutanoic acid or 2R,4S)-5-diphenyl-4-yl-4-(3-carboxypropyonylamino)2-methylpentanoic acid or its pharmaceutically acceptable salt; and (iii) pharmaceutically acceptable carrier.

New ep4 agonist

New ep4 agonist

Invention refers to a compound presented by formula (1)

N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thien-2-yl)amide 1-(4-bromobenzoyl)-5-hydroxy-3-(4-methylphenyl)-4,5-dihydro-1h-pyrazole-5-carboxylic acid, having analgesic activity

N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thien-2-yl)amide 1-(4-bromobenzoyl)-5-hydroxy-3-(4-methylphenyl)-4,5-dihydro-1h-pyrazole-5-carboxylic acid, having analgesic activity

Invention relates to novel biologically active substances of the class of N-acyl-derivatives of 2-aminothiophene, specifically to N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thien-2-yl)amide of 1-(4-bromobenzoyl)-5-hydroxy-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazole-5-carboxylic acid having the formula given below. The disclosed compound is obtained by reacting 2-[5-(4-methylphenyl)-3-oxofuran-2(3H)-ylideneamino]-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile with 4-bromobenzoylhydrazine in anhydrous toluene at 60°C and stirring for 2 hours, followed by separation of the end product using existing methods.

Agent for stimulating reproductive function

Agent for stimulating reproductive function

What is presented is using 2-[1-(1,1-dioxothietanyl-3)benzimidazolyl-2-thio]acetic acid potassium salt (formerly known as an immunotropic and anxiolytic agent) as an agent to stimulate the reproductive function: prolonging an oestrus phase and shortening a proestrus phase of the ovulatory cycle activating receptive sexual motivation and impregnation processes, reducing the pre- and post-implantation embryo death.

Method of treating essential arterial hypertension at background of obesity

Invention relates to medicine, namely to cardiology, and deals with the treatment of essential arterial hypertension at the background of obesity. For this purpose realised is complex treatment, which includes the introduction of candesartan 8 mg/day, amlodipine 5 mg/day, indapamide 2.5 mg/day and sibutramine 10 mg/day in a combination with daily dosed 1-2 km walking for 1 month with the further increase of the distance to 3 km. The patient is taught to calculate the calorie content of the daily diet and control the treatment result by measuring the level of arterial pressure 2 times per week and determining the circumference of the waist and hips, as well as the body weight index 1 time per week on their own.

Method of treating acute and sudden sensorineural hearing loss and deafness

Method of treating acute and sudden sensorineural hearing loss and deafness

Euphylline, trental, nicotinic acid, ascorbic acid, B1 and B6 group vitamins are administered intravenously; papaverine and dibazol are injected intramuscularly in standard doses and combined with intravenous injections of tompasline in an amount of 40 mg daily for 10 days.

Selective antagonists of ep4 receptor for cancer treatment

Selective antagonists of ep4 receptor for cancer treatment

Invention relates to chemical and pharmaceutical industry and represents application of compound, selected from group, including 3-[2-(4-{2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]piridin-1-yl}phenyl)ethyl]-1-[(4-methylebenzene)sulphonyl]urea; 4-((1S)-1-{[5-chloro-2-(4-fluorophenoxy)benzoyl]amino}ethyl)-benzoic acid and 4-[(1S)-1-({[5-chloro-2-(3-fluorophenoxy)piridin-3-yl]carbonyl}amino)ethyl]benzoic acid, or its pharmaceutically acceptable salt for production of medication for production of cancer dimensions, associated with prostaglandin E2 (PGE2) (for instance, gastroenterologic cancer, prostate cancer, lung cancer and breast cancer) in humans or animals.

Novel solvate crystals

Novel solvate crystals

Invention relates to crystals of solvate of trityl olmesartan medoxomil with acetone, which comprise 1 mol of acetone per 1 mol of of trityl olmesartan medoxomil, versions of methods of thereof obtaining, as well as to method of obtaining olmesartan medoxomil with application of crystals of solvate of trityl olmesartan medoxomil with acetone.

Sigma ligands for potentiating analgesic effect of opioids and opiates in postoperative pain and attenuating dependency thereof

Sigma ligands for potentiating analgesic effect of opioids and opiates in postoperative pain and attenuating dependency thereof

Invention relates to simultaneous, separate or sequential administration of a combination, comprising at least one sigma ligand of formula

Pharmaceutical composition with analgesic activity in injection form (versions)

Pharmaceutical composition with analgesic activity in injection form (versions)

Pharmaceutical composition with kappa-opioid agonistic activity, demonstrating an analgesic effect in accordance with the first version contains 9-(2-morpholinoethyl)-2-(4-fluorophenyl)imidazo[1,2-α]benzimidazole dihydrochloride as an active component, and an isotonicity corrigent, selected from salts of organic and inorganic acids, polyols, amino acids, as auxiliary substances. The composition can additionally contain a co-solvent, a corrigent of the solution pH, a cryoprotector, and an antioxidant. In accordance with the second version the pharmaceutical composition contains 9-(2-morpholinoethyl)-2-(4-fluorophenyl)imidazo[1,2-α]benzimidazole dihydrochloride as an active component, and a co-solvent, selected from ethyl alcohol, glycerol, propylene glycol, benzylbenzoate, benzyl alcohol, ethyloleate and fatty oils, including olive oil and peach oil as auxiliary substances. The composition can additionally contain an isotonicity corrigent, a corrigent of the solution pH, a cryoprotector, and an antioxidant.

Compounds of substituted n-(1h-indazol-4-yl)imidazol [1,2-a]-3-carboxamide as cfms inhibitors

Compounds of substituted n-(1h-indazol-4-yl)imidazol [1,2-a]-3-carboxamide as cfms inhibitors

Invention relates to novel formula I compounds and their pharmaceutically acceptable salts, which are cFMS inhibitors and are useful in treatment of bone diseases, cancer, autoimmune disorders, inflammatory diseases, cardio-vascular diseases and anaesthetics. Invention relates to versions of method of obtaining said compounds, pharmaceutical composition and method of treating bone diseases on their basis. In general formula

Veterinary antiviral drug

Veterinary antiviral drug comprises the active substance as piperidinium 2-[5-(furan-2-yl)-4-phenyl-1,2,4-triazol-3-ylthio]acetate and additionally comprises the esters of 4-hydroxybenzoic acid in a weight ratio of 1:(0.03-0.05), e.g. methyl-4-hydroxybenzoate and/or propyl-4-hydroxybenzoate, and/or butyl-4-hydroxybenzoate. The drug may be produced in the dosage form of a powder or a sterile solution or an ointment. In the manufacture of the drug in the dosage form of a sterile solution it comprises piperidinium 2-[5-(furan-2-yl)-4-phenyl-1,2,4-triazol-3-ylthio]acetate, esters of 4-hydroxybenzoic acid and purified water in the following ratio of ingredients, wt %: piperidinium 2-[5-(furan-2-yl)-4-phenyl-1,2,4-triazol-3-ylthio]acetate - 1.0-20.0; esters of 4-hydroxybenzoic acid - 0.03-1.0; purified water - the rest. In the manufacture of the drug in the dosage form of an ointment, it comprises piperidinium 2-[5-(furan-2-yl)-4-phenyl-1,2,4-triazol-3-ylthio]acetate, esters of 4-hydroxybenzoic acid and lipophilic, or fatty, or hydrophilic ointment base in the following ratio of ingredients, wt %: piperidinium 2-[5-(furan-2-yl)-4-phenyl-1,2,4-triazol-3-ylthio]acetate - 1.0-20.0; esters of 4-hydroxybenzoic acid - 0.03-1.0; the ointment base - 79.0-98.07.

Oxygen-substituted derivatives of 3-heteroaroylaminopropionic acids and their application as pharmaceutical substances

Oxygen-substituted derivatives of 3-heteroaroylaminopropionic acids and their application as pharmaceutical substances

Invention relates to formula compounds and their pharmaceutically acceptable salts, where A represents C(R1); D represents N(R2); E represents N; G are selected from group, consisting of R71-O-C(O)- and R72-N(R73)-C(O)-; R1 are selected from hydrogen, halogen and (C1-C6)-alkyl; R2 are selected from (C1-C7)-alkyl, (C3-C7) cycloalkyl-CsH2s- and Ar-CsH2s-, where s equals 0, 1, 2 and 3; R10 are selected from R11-O-, R12-N(R13)-C(O)-O- and Het2-C(O)-O-; R11 are selected from hydrogen, R14, (C3-C7)-cycloalkyl and Ar; R12 and R13 independently on each other are selected from hydrogen, R15 and Ar; R14 represents (C1-C10)-alkyl, which is optionally substituted with 1-3 similar or different substituents, selected from halogen, HO-, R16-O-, oxo, (C3-C7)-cycloalkyl, optionally substituted with 1-3 fluorine atoms, Ar, Het1, Het3, di((C1-C4)-alkyl)N-C(O)- and Het1-C(O)-; R15 represents (C1-C6)-alkyl; R16 represents (C1-C6)-alkyl, which is optionally substituted with (C1-C4)-alkyl-O-; R30 is selected from group, consisting of R31, R32-CuH2u- and Het3-CuH2u-, where u equals 0; R31, R32 and R33 are such as given in invention formula; R40 represents hydrogen; R30 and R40 together represent (CH2)x, x equals 2, 3, 4 or 5; R50 is selected from group, consisting of hydrogen and HO-; R60 represents hydrogen; R71, R72 and R73 are such as given in invention formula; Ar is selected from group, consisting of phenyl and aromatic 6-membered monocyclic heterocycle, which includes one nitrogen atom, with phenyl and heterocycle being optionally substituted with 1-3 similar or different substituents, selected from halogen (C1-C6)-alkyl, optionally substituted with 1-3 fluorine atoms, (C1-C6)-alkyl-O-, (C1-C6)-alkyl-S(O)m-, H2N-S(O)2- and NC-; Het1, Het2, Het3 and Het4 are such as given in invention formula; m equals 0, 1 and 2. Invention also relates to method of obtaining formula I compounds, pharmaceutical composition and application.

Triazolopyridine jak inhibitor compounds and methods

Triazolopyridine jak inhibitor compounds and methods

Invention refers to compounds of formula I or its pharmaceutically acceptable salts. The compounds according to the invention possess the properties of JAK2 kinase inhibitor. In formula

Method for correcting neurological disturbances accompanying alcohol intoxication

Method for correcting neurological disturbances accompanying alcohol intoxication

Correcting neurological disturbances accompanying alcohol intoxication in rats is ensured by prescribing a metabolitotropic agent containing both the active substance (S)-2,6-diaminohexanoic acid 3-methyl-1,2,4-triazolyl-5-thioacetate (Angioline), also having a neuroprotective and endothelioprotective action, in a dose of 100 mg/kg a day for 14 days.

Pharmaceutical compositions, containing sulbactam and beta-lactamase inhibitor

Disclosed are pharmaceutical antibacterial composition and methods of treatment or prevention of bacterial infections by its application or by application of combination of its ingredients (versions). Pharmaceutical composition contains pharmaceutically effective quantity of: (a) sulbactam or its pharmaceutically acceptable salt and (b) beta-lactamase inhibitor trans-7-oxo-6-(sulphoxy)-1,6-diazabicyclo-[3.2.1]-octane-2-carboxamide or its pharmaceutically acceptable salt.

Therapeutic preparation and preventive preparation for treating alzheimer's disease

Therapeutic preparation and preventive preparation for treating alzheimer's disease

Claimed invention provides a therapeutic preparation or preventive preparation for treating Alzheimer's disease, with the said preparation containing, preferably, as an effective ingredient a cyclohexane derivative, represented by formula given below, or its pharmaceutically acceptable salt.

Therapeutic preparation or preventive preparation for treating fibromyalgia

Therapeutic preparation or preventive preparation for treating fibromyalgia

Claimed invention provides a therapeutic preparation or a preventive preparation for treating fibromyalgia, with the said preparation containing, preferably, as an effective ingredient a cyclohexane derivative, represented by the formula given below , or its pharmaceutically acceptable salt.

Jak-inhibiting triazolopyridine compounds and methods

Jak-inhibiting triazolopyridine compounds and methods

Invention relates to compounds of formula I or their pharmaceutically acceptable salts. Compounds by invention possess properties of JAK2 kinase inhibitors. In formula I R1 represents phenyl, optionally substituted with 1-3 R6; R2 represents phenyl, optionally substituted with 1-2 R7; R3, R4 and R5 independently represent H. values of the rest of radicals are presented in invention formula. Invention also relates to particular compounds, structural formulae of which are presented in invention formula.

4-[2-[[5-methyl-1-(2-naphthalinyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride polymorph and solvates

4-[2-[[5-methyl-1-(2-naphthalinyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride polymorph and solvates

Invention refers to 4-[2-[[5-methyl-1-(2-naphthalinyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride salt (P027) polymorphs and solvates, methods for producing them, and pharmaceutical compositions containing them.

Method to produce albendazole nanocapsules

Invention describes the method of production of albendazole nanocapsules by method of deposition with a non-dissolvent, where albendazole is added in small portions into a suspension of carrageenan, used as a shell of nanocapsules, in butanol in presence of 0.01 g of preparation E472c and during mixing at 1000 rotations/seconds, then the precipitator is added - butyl chloride, filtered and dried at room temperature.

Salts of 4-[2-[[5-methyl-1-(2-naphthalinyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine

Salts of 4-[2-[[5-methyl-1-(2-naphthalinyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine

Claimed invention relates to field of organic chemistry, namely to hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalinyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine. Invention also relates to method of obtaining said hydrochloride salt, pharmaceutical composition, based on said hydrochloride salt, application of said hydrochloride salt.

Therapeutic agent or preventive agent for treating urine collection disorder

Therapeutic agent or preventive agent for treating urine collection disorder

Present invention represents a therapeutic agent or a preventive agent for treating urine collection disorder(s); the above agent preferentially contains a cyclohexane derivative as an effective ingredient presented by formula such as below , or its pharmaceutically acceptable salt. Due to its anticholinergic activity, this agent is used to correct side effects and possesses analgesic action.

Dental pencil with metronidazole, bactisubtil and large bee moth larvae extract for treating inflammatory periodontal diseases

Dental pencil with metronidazole, bactisubtil and large bee moth larvae extract for treating inflammatory periodontal diseases

As active ingredients, a dental pencil contains metronidazole, bactisubtil and a 10% large bee moth larvae extract, and a base, which consists of bee wax, emulsifier No. 1, methyl parabene, paraffin, peach oil, low-molecular polyethylene, Lutrol F127 and Cremophore RH-40 taken in a certain mixture ratio.

Another patent 2551086.

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