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Quinolone analogues and related methods Invention refers to a compound of formula , wherein A and V independently represents H or a halogen; Q is absent; R4 independently represents H, a C1-C6 alkyl or C3-C6 cycloalkyl; R7 represents H; and R8 represents a C1-C10 alkyl substituted by OH or C1-C6 alkoxy; or C1-4 alkyl substituted by a 5-6-merous aromatic heterocyclic ring containing 1-2 heteroatoms specified in N and S, wherein the above aromatic heterocyclic ring is optionally substituted by a C1-C10 alkyl; or in -NR7R8, R7 and R8 together with N can form an optionally substituted azacyclic ring containing where applicable an additional heteroatom specified in H, O and S, as a cycle member, optionally substituted by a C1-C10 alkyl, which is substituted by a C1-C6 alkoxy; m is equal to 0; n is equal to 0. The invention also refers to a compound of formula (wherein the substitutes are those as specified in the patient claim), to a pharmaceutical composition containing a therapeutically effective amount of the compounds of formula (VIII), and to a method of treating or relieving a cell-proliferative disorder. |
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Azetidinyl diamides as monoacylglycerol lypase inhibitors Invention refers to a compound of formula , wherein Y and Z are independently specified in a group of a) or b) so that one of Y or Z is specified in the group a), and another one - in the group b); the group a) represents i) substituted C6-10aryl; ii) C3-8cycloalkyl; iii) trifluoromethyl or iv) heteroaryl specified in a group consisting of thienyl, furanyl, thiazolyl, isothiazolyl, oxazolyl, pyrrolyl, pyridinyl, isoxazolyl, imidazolyl, furasan-3-yl, benzothienyl, thieno[3,2-b]thiophen-2-yl, pyrazolyl, triazolyl, tetrazolyl and [1,2,3]thiadiazolyl; the group b) represents i) C6-10aryl; ii) heteroaryl specified in a group consisting of thiazolyl, pyridinyl, indolyl, pyrrolyl, benzoxazolyl, benzothiazolyl, benzothienyl, benzofuranyl, imidazo[1,2-a]pyridin-2-yl, furo[2,3-b]pyridinyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[3,2-b]pyridinyl, thieno[2,3-b]pyridinyl, quinolinyl, quinazolinyl, thienyl and benzimidazolyl; iii) benzofused heterocyclyl attached through a carbon atom, and when a heterocyclyl component contains a nitrogen atom, the carbon atom is optionally substituted by one substitute specified in a group consisting of C3-7cycloalkylcarbonyl; C3-7cycloalkylsulphonyl; phenyl; phenylcarbonyl; pyrrolylcarbonyl; phenylsulphonyl; phenyl(C1-4)alkyl; C1-6alkylcarbonyl; C1-6alkylsulphonyl; pyrimidinyl and pyridinyl; C3-7cycloalkylcarbonyl, phenyl, phenylcarbonyl, phenyl(C1-4)alkyl and phenylsulphonyl are optionally substituted by trifluoromethyl, or by one or two fluor-substitutes; iv) phenoxatiynyl; vi) fluoren-9-on-2-yl; vii) 9,9-dimethyl-9H-fluorenyl; viii) 1-chlornaphtho[2,1-b]thiophen-2-yl; ix) xanthen-9-on-3-yl; x) 9-methyl-9H-carbazol-3-yl; xi) 6,7,8,9-tetrahydro-5H-carbazol-3-yl; xiii) 3-methyl-2-phenyl-4-oxochromen-8-yl; or xiv) 1,3-dihydrobenzimidazol-2-on-5-yl optionally substituted by 1-phenyl, 1-(2,2,2-trifluoroethyl), 1-(3,3,3-trifluoropropyl) or 1-(4,4-difluorocyclohexyl); 1-phenyl is optionally substituted by one or more fluor-substitutes or trifluoromethyl; or xv) 4-(3-chlorophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl; R1 represents C6-10aryl, C1-3alkyl, benzyloxymethyl, hydroxy(C1-3)alkyl, aminocarbonyl, carboxy, trifluoromethyl, spirofused cyclopropyl, 3-oxo or aryl(C1-3)alkyl; or when s is equal to 2 and R1 represents C1-3alkyl, the substitutes C1-3akyl is taken with a piperazine ring to form 3,8-diazabicyclo[3.2.1]octanyl or 2,5-diazabicyclo[2.2.2]octanyl ring system, and its pharmaceutical compositions. |
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Aqueous transparent solutions of fluocinolone acetonide for treatment of ear inflammation Claimed is a pharmaceutical, ear, sterile, preservative-free composition in the form of a transparent aqueous solution, containing 0.01-0.025 % of fluocinilone acetonide optionally in a combination with 0.1-0.8% of ciprofloxacin or its pharmaceutically acceptable salt, a non-ionic surface-active substance, a tonicity-regulating agent and a viscosity-increasing agent. |
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Anti-inflammatory antibacterial wound-healing agent Invention represents an anti-inflammatory antibacterial wound-healing agent containing a polyethylene oxide base with molecular weight 400 (PEO-400) as a forming agent, as well as polyethylene oxide with molecular weight 1,500 (PEO-1500); an active substance is chloramphenicol and methyluracil; the agent is characterised by the fact that it additionally contains rifampicin and/or cycloserine; the cycloserine content in the rifampicin mixture is specified within the range of 18 to 82 wt %, whereas the ingredients are taken in certain ratio, wt %. |
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Chromone derivatives, method for preparing them and therapeutic uses thereof Invention refers to new chromone derivatives of general formula |
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3-benzofuranylindol-2-one derivatives substituted in position 3, preparing and using them in therapy Invention refers to new 3-benzofuranylindol-2-one derivatives substituted in position 3 of formula wherein: R1 means a hydrogen atom; R2, R3, R4 equal or different, found in any accessible position of the phenyl ring, means independently a hydrogen atom or a halogen atom; R5 means (C1-6) alkyl group; n means 1; in the form of the base or acid-additive salt, as well as to a therapeutic agent and a pharmaceutical composition based on the above compounds possessing the ghrelin receptor antagonist activity, and to using this compounds for preparing the therapeutic agent for preventing or treating obesity, diabetes, appetite disorders and overweight. |
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New phenol derivatives and their pharmaceutical or cosmetic application Invention refers to compounds of structural formula (I), which can be used for treating diseases mediated by an androgen receptor. In formula (I), R1 means (C2-6)alkyl, (C1-6)alkyloxy, -S(O)m-(C1-6)alkyl, (C1-6)fluoroalkyl, CN or halogen, R2 and R3 are identical or different and mean a hydrogen atom or (C1-9)alkyl, R4, R5, R6, R7 are identical or different and mean a hydrogen or halogen, X means CH or N, Y means either a nitrogen atom, or a carbon atom substituted by (C1-6)alkyl, (C1-6)alkyloxy, (C1-6)fluoroalkyl, a hydrogen atom or halogen; m is equal to 0, 1 or 2. |
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N-pyridin-3-yl or n-pyrazin-2-yl carboxamides as agents increasing level of hdlp cholesterol Invention relates to field of organic chemistry, namely to heterocyclic compounds of formula I |
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Method of preventing cerebral form of radiation sickness Invention relates to medical radiology and can be used for prevention of cerebral form of acute radiation sickness. Claimed is application of officinal drug pyrazinamide as medication for prevention of cerebral form of acute radiation sickness. Pyrazinamide has been used for treating tuberculosis. |
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Apoptosis inducing agents for treating malignant new growth, and immune and autoimmune diseases Invention refers to compounds of formula |
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Apoptosis-inducing agents for treatment of cancer and immune and autoimmune diseases Invention relates to particular derivatives of N-(phenylsulphonyl)benzamide, given in i.1 of the invention formula. The invention also relates to a pharmaceutical composition, possessing an inhibiting activity with respect to anti-apoptotic proteins Bcl-2, containing an effective quantity of one of the said compounds or a therapeutically acceptable salt of such a compound. |
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Invention relates to the field of organic chemistry, namely to compounds of N-phenyl(pyperazinyl or homopyperazinyl)benzenesulphonamide or benzenesulphonylphenyl(pyperazine or homopyperazine), or to their physiologically acceptable acid addition salts, described by general formulas (I) and (I'), where X is a chemical bond or a group N-R4; R1 is hydrogen or methyl; R2 is hydrogen or methyl; R3 is hydrogen, C1-C3alkyl, fluorine, C1-C2alkoxy or fluorinated C1-C2alkoxy; R4 is hydrogen, C1-C4alkyl or C3-C4cycloalkyl-CH2-; R5 is hydrogen, fluorine, chlorine, C1-C2alkyl, C1-C2alkoxy or fluorinated C1-C2alkoxy; R6 is hydrogen and n is 1 or 2. The invention also relates to a pharmaceutical composition based on the compound of formula |
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Group of inventions relates to medicine, in particular to a composition, the application of the composition and a method of treating abuse with substances, causing painful addiction in a subject. The composition contains a carbamoyl compound, or its pharmaceutically acceptable salt, or an ester as an active ingredient and the method includes the introduction of a therapeutically effective quantity of the carbamoyl compound, or its pharmaceutically acceptable salt, or the ester. |
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Lambertianic acid amides, possessing analgesic activity and stimulating action Invention relates to lambertianic acid amides of formula (Ia, b), which have expressed analgesic activity and stimulating action, manifested in increase of motor and investigation activity of animals, absence of anxiety, etc. In formula I ; (Ib). |
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What is presented is a group of inventions involving a pharmaceutical composition for preventing or treating diabetes mellitus, diseases related to diabetes mellitus, or complications of diabetes mellitus containing a combination of (A) (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol, or its salt, hydrate or hydrate salt, and (B) metformine or an agent intensifying insulin secretion, and a combination of the same formulation and for the same application. |
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Invention refers to compounds of formulas I, II, III, IV, V, VIII or to their pharmaceutically acceptable salts, wherein: Z represents , or phenyl; D represents or ; X represents N(R9), O, S, S(=O) or S(O)2; each Y independently represents O or S; G represents or ; the other radical values are described in the patent claim. The invention also refers to pharmaceutical compositions based on the above compounds. |
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Method of treating chronic tonsillitis Palatal tonsils are daily sanitated with antibacterial preparations selected in accordance with the bacteriological examination of oral smears for pathogenic microflora and antibiotic sensitivity with the tonsil lacunae washed for 10 days. Pre-anaesthesia is followed by the tonsil lacunae exposure to an ultrasonic disintegrator at a depth of a probe working area at an amplitude of 23-26 mc every second day for 5 days. That is followed by paratonsil administration of polyoxidonium in an adult dose of 6 mg every second day for 5 days; the therapeutic course is performed once a year. |
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Stable formulations of bortezomib Storage-stable pharmaceutical composition represents a liquid formulation containing bortezomib and a system of anhydrous solvents and applicable for injection. A primary ingredient of the system of anhydrous solvents is propylene glycol. Bortezomib is found in the concentration of at least 1 mg/ml. The pharmaceutical composition contains a total amount of aqueous buffer of 10 vol. % or more. |
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1, 2-dihydrocyclobutanedione derivatives as nicotinamide phosphoribosyltransferase inhibitors Invention relates to compound of formula (I) , where A is selected from -C(=O)-, -S(=O)2-, and -P(=O)(R5)-, where R5 is selected from C1-6-alkyl, C1-6-alkoxy and hydroxy; B is selected from single bond, -O-, and -C(=O)-NR6-, where R6 is selected from hydrogen; D is selected from single bond, -O-, and -NR9, where R7, R8 and R9 are independently selected from hydrogen; m equals integer number 0-12 and n equals integer number 0-12, where the sum m+n equals 1-20; p equals integer number 0-2; R1 is selected from optionally substituted heteroaryl, where heteroaryl represents aromatic carbocyclic ring, where one carbon atom is substituted with heteroatom; R2 is selected from hydrogen, optionally substituted C1-12-alkyl, and substituents are selected from phenyl, morpholine, halogen and pyridine; C3-12-cycloalkyl, -[CH2CH2O]1-10-C1-6-alkyl); and R3 is selected from optionally substituted C1-12-alkyl, and substituents are selected from morpholine, phenyl, dialkylamine and C3-12-cycloalkyl, optionally substituted with halogen aryl; or R2 and R3 together with adjacent atoms form optionally substituted with alkylcarbonyl or alkyl N-containing heterocyclic or heteroaromatic ring; each of R4 and R4* independently represents hydrogen; and their pharmaceutically acceptable salts, as well as to application of said compounds for treatment of diseases/states, induced by increased level of nicotinamide phosphoribosyltransferase (NAmPRTase). |
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New benzene sulphonamide compounds, methods for preparing and using them in therapy and cosmetics Invention refers to new benzene sulphonamide compounds, wherein the compounds are specified in a group of the following compounds, including additive salts with pharmaceutically acceptable acid, additive salts with pharmaceutically acceptable base and enantiomers of these compounds: 1) 3-[(4-but-2-inyloxybenzenesulphonyl)-methylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 2) (S)-3-(4-but-2-inyloxybenzenesulphonylamino)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 3) (S)-3-(4-benzyloxybenzenesulphonylamino)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 4) (S)-3-[(4-benzyloxybenzenesulphonyl)-methylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 5) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 6) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(naphthalen-1-ylmethoxy)-benzenesulphonylamino]-propionamide, 7) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-(4-propoxybenzenesulphonylamino)-propionamide, 8) (S)-3-[4-(3-cyanobenzyloxy)-benzenesulphonylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 9) (S)-3-[4-(4-cyanobenzyloxy)-benzenesulphonylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 10) benzyl-4-{(S)-1-hydroxycarbamoyl-2-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-entyl}-piperazine-1-carboxylate, 11) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-phenylpiperidin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 12) (R)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 13) (S)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-2-piperazin-1-ylpropionamide, 14) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide hydrochloride, 15) tert-butyl-3-{4-[(S)-2-hydroxycarbamoyl-2-(4-methanesulphonylpiperazin-1-yl)-ethylsulphamoyl]-phenoxymethyl}-2-methylindole-1-carboxylate difluoroacetate, 16) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(quinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 17) (S)-2-(4-benzylpiperazin-1-yl)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 18) (S)-2-[4-(4-fluorobenzyl)-piperazin-1-yl]-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino-propionamide, 19) (S)-2-(4-ethulpiperazin-1-yl)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 20) (S)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-2-[4-(4-trifluoromethylbenzyl)-piperazin-1-yl]-propionamide, 21) (S)-N-hydroxy-2-[4-(4-methylbenzyl)-piperazin-1-yl]-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 22) (S)-3-[4-(benzoisoxazol-3-ylmethoxy)-benzenesulphonylamino]-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-propionamide, 23) (S)-N-hydroxy-2-(4-isobutyrylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 24) (S)-N-hydroxy-2-[4-(2-methylpropane-1-sulphonyl)-piperazin-1-yl]-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-propionamide, 25) (S)-N-hydroxy-2-(4-methanesulphonylpiperazin-1-yl)-3-[4-(2-trifluoromethylpyrazolo[1,5-a]pyridin-3-ylmethoxy)-benzenesulphonylamino]-propionamide, 26) (S)-N-hydroxy-3-[4-(2-methylquinolin-4-ylmethoxy)-benzenesulphonylamino]-2-[4-(propane-2-sulphonyl)-piperazin-1-yl]-propionamide, and 27) (S)-2-(4-benzylpiperazin-1-yl)-N-hydroxy-3-[4-(2-trifluoromethylpyrazolo[1,5-a]pyridin-3-ylmethoxy)-benzenesulphonylamino]-propionamide. The invention also refers to pharmaceutical and cosmetic compositions on the basis of the above compounds possessing TNFα-converting enzyme (TACE) activity. |
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Isoindoline compounds used for treating cancer Invention refers to isoindoline compounds, such as compounds of Formula or to their pharmaceutically acceptable salts or stereoisomers, wherein X represents CH2; Y represents O, cyanamido (N-C≡N) or amido (NH); m represents an integer of 0 or 1; R1 represents hydrogen or C1-6 alkyl; R2 represents hydrogen, C1-10 alkyl, C0-6alkyl-(5-10-merous heteroaryl containing one, two or three heteroatoms independently specified in O, S or N), C0-6alkyl-(6-merous heterocyclyl which represents morpholinyl or piperazinyl), C0-6alkyl-OH, -NHCO-C1-6alkyl, -OR21 or - (CH2-Z)-(6-merous heteroaryl which represents pyridinyl), wherein each heteroaryl and heterocyclyl is optionally substituted by one or more C1-6 alkyls; R3 represents hydrogen, halogen, -NO2, C0-6alkyl-OH, C0-4 alkyl-NH2 or -OR21; R21 represents phenyl, pyridinyl, piperidinyl or -CO(CH2)R22; R22 represents -NH2 or piperazinyl; and Z represents O; provided R1 represents hydrogen, then R2 is other than hydrogen or C1-10alkyl; provided R3 represents halogen, then R2 represents C0-6alkyl-(5-6-merous heterocyclyl). The invention also refers to pharmaceutical compositions for controlling angiogenesis or inhibiting the TNFα production on the basis of the above compounds. |
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Method includes preparation of a hydrochloric acid solution of tin (II) chloride dehydrate with tin concentration of 7 mg/ml, for which purpose 0.07 g of tin (II) chloride dehydrate and 0.2 ml of 1 M hydrochloric acid are slowly mixed, dissolution is carried out in an inert gas (argon) medium, when dissolution finishes, distilled water is added and the solution volume is brought to 10 ml. Then 0.015-0.025 ml of the prepared solution are taken and mixed with 5-6 mg of a ciprofloxacin hydrochloride substance, the obtained solution is frozen at a temperature of liquid nitrogen, placed into a sublimator chamber and subjected to freeze-drying at a temperature of -50°C, vacuum 0.09 Torr for 24 hours, after which it is transferred into an upper freeze-drying chamber and after-dried at a temperature of +15°C for 4.5 hours. |
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Tablets and granulated powders containing 6-fluor-3-hydroxy-2-pyrazincarboxamide Invention discloses a tablet for treating or preventing viral infections which contains 50-95% of 6-fluor-3-hydroxy-2-pyrazincarboxamide or its salt; it has a size facilitating ingestion; it possesses excellent release characteristics of the active principle and has hardness. |
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Apoptosis-inducing preparations for treatment of cancer and immune and autoimmune diseases Invention relates to compound of formula or to its therapeutically acceptable salt, where A1 represents N or C(A2); A2 represents H; B1 represents H, OR1 or NHR1; D1 represents H; E1 represents H; Y1 represents CN, NO2, F, Cl, Br, I, R17 or SO2R17; R1 represents R4 or R5; Z1 represents R26 or R27; Z2 represents R30; Z1A and Z2A both are absent; L1 represents R37; R26 represents phenylene; R27 represents indolyl; R30 represents piperasinyl; R37 represents R37A; R37A represents C2-C4 alkylene; Z3 represents R38, R39 or R40; R38 represents phenyl; R39 represents benzodioxilyl; R40 represents C4-C7cycloalkenyl, heterocycloalkyl, which represents monocyclic six- or seven-member ring, containing one heteroatom, selected from O, and zero of double bonds, or azaspiro[5.5]undec-8-ene; the remaining values of radicals are given in i.1 of invention formula. Invention also relates to pharmaceutical composition, based on claimed compound. |
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Benzene or thiophen derivative and using it as vap-1 inhibitor Invention refers to a compound presented by formula |
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Diaminoheterocyclic carboxamide compound Compounds can find application for preventing or treating cancer, lung cancer, non-small cells lung cancer, small-cell lung cancer, EML4-ALK hybrid polynucleotide-positive cancer, EML4-ALK hybrid polynucleotide-positive lung cancer or EML4-ALK hybrid polynucleotide-positive non-small cells lung cancer. In formula (I) -X-: group of formula , A represents chlorine, ethyl or isopropyl; R1 represents phenyl wherein carbon in the 4th position is substituted by the group -W-Y-Z, and carbon in the 3rd position can be substituted by a group specified in a group consisting of halogen, R00 and -O-R00; R00: lower alkyl which can be substituted by one or more halogen atoms; -W-: a bond, piperidine-1,4-diyl or piperazine-1,4-diyl; -Y- represents a bond; Z represents a monovalent 3-10-membered monocyclic non-aromatic heterocyclic ring which contains 1 to 4 heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, which can be substituted by one or more substitutes R00; R2 represents (i) an optionally bridged saturated C3-10cycloalkyl which can be substituted by one or more groups specified in -N(lower alkyl)2, lower alkyl, -COO-lower alkyl, -OH, -COOH, -CONH-RZB and morpholinyl, or (ii) a monovalent 3-10-membered monocyclic non-aromatic heterocyclic ring which contains 1 to 4 heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, which can be substituted by one or more groups specified in a group consisting of lower alkyl, -CO-lower alkyl, oxo, -CO-RZB and benzene; and RZB: phenyl which can be substituted by a group consisting of halogen and -O-lower alkyl; R3 represents -H. |
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Invention refers to medicine, namely to therapy, and can be used for treating arthritis in a mammal, involving administering N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulphanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulphonyl)benzene sulphonamide (ABT 263). |
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Heterocyclic compounds and methods of application Invention relates to compounds or their pharmaceutically acceptable salts, where compound has formula 1-a, in which R1 and R3 are absent, m represents integer number from 1 to 2, n represents integer number from 1 to 3, A represents , B represents or , where X2 represents O or S, R4a is absent, R4b is selected from the group, consisting of: , , , , and ; Rk is selected from C1-6alkyl and C1-6halogenalkyl, L and E are such as given in i.1 of the invention formula; or compound is such as given in b) of i.1 of the invention formula. Invention also relates to pharmaceutical composition, which contains said compounds. |
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Method of obtaining indolinone derivative Invention relates to method of obtaining 3-Z-[1-(4-(N-((4-methylpiperazin-1-yl)methylcarbonyl)-N-methylamino)-anilino)-1-phenylmethylene]-6-methoxycarbonyl-2-indolinone of formula including stage of reaction of compound of formula, , obtained by dechloroactilation of compound of formula catalysed by base, with compound of formula . |
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Thieno[3,2-d]pyrimidine derivatives, possessing inhibiting action with respect to proteinkinase Invention relates to thieno[3,2-d]pyrimidine derivative of formula (I) or to its pharmaceutically acceptable salt: (I), where Y stands for -CH=CR1-, -C≡C- or -C(=O)NR1-; L stands for -C(=O)NR2-, -NR2C(=O)- or -NR2C(=O)NR2-; R1 and R2, each independently stands for H; R stands for H, a halogen atom, methyl or methoxy; E stands for phenyl or C3-10heteroaryl, which is non-substituted or substituted with 1-2 substituents, consisting of a group, which includes a halogen atom, -CF3, C1-6alkyl, hydroxy-C1-6alkyl, C3-8cycloalkyl, -(CH2)n-C1-6alkylamino, -(CH2)n-diC1-6alkylamino, -(CH2)nC1-6alkoxy, -(CH2)n-OS(=O)2-C1-6-alkyl, -(CH2)n-phenyl, -(CH2)n-C2-5heteroaryl and -(CH2)n-C4-6heterocycloalkyl, where C3-10heteroaryl represents pyridine, isoquinoline, indole or isoxazole, C2-5heteroaryl of radical -(CH2)n-C2-5heteroaryl represents imidazole or pyrrol, C4-6heterocycloalkyl of radical -(CH2)n-C4-6heterocycloalkyl represents piperazine, morpholine, diazepam, pyrrolidine or piperidine, and phenyl, heteroaryl and heterocycloalkyl each independently, is non-substituted or substituted with substituent selected from a group, which consists of C1-6alkyl, hydroxy-C1-6alkyl, a halogen atom and diC1-6alkylamino, n is equal to 0 or 1; and Z stands for H, -C(=O)R3, C1-6alkyl, hydroxyC1-6alkyl, C3-8cycloalkyl, piperidine, phenyl or pyridine, where piperidine, phenyl and pyridine, each independently, is non-substituted or substituted with C1-6alkyl, C1-6alkoxy or R3-piperazinyl and R3 represents C1-6alkyl or phenyl. The invention also relates to an intermediate compound for obtaining the claimed final compound of formula (I). |
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Claimed is a group of inventions, which includes a method of treating a hyperproliferative disorder by introduction to a mammal of a therapeutic combination in the form of a combined composition or by alternation, and the therapeutic combination contains a therapeutically effective quantity of formula compound 4-(2-(1H-indasol-4-yl)-6-((4-(methylsulphonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine, or formula (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, or their stereoisomers, geometrical isomers, tautomers, or their salts and a therapeutically effective quantity of a chemiotherapeutic agent, selected from erlotinib, docetaxel, 5-FU, gemcitabine, PD-0325901, cisplatin, carboplatin, paclitaxel, bevacizumab, trastuzumab, pertuzumab, temozolomide, tamoxifen, doxorubicin, Akti-1/2, HPPD, rapamycin and lapatinib; a pharmaceutical composition of the same purpose and composition, application of the said therapeutic combination for manufacturing of medication for treatment of cancer, selected from breast cancer, cervical cancer, cancer of large intestine, endometrium, glioma, lung cancer, melanoma, ovarian cancer, cancer of pancreas and prostate, a product for treatment of a hyperproliferative disorder, including the said composition and an instruction and the product, containing the said combination for separate, simultaneous or successive application in treatment of a hyperproliferative disorder. |
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Substituted aminoindans and analogues thereof to be used in pharmaceutics Invention refers to compounds of formula , wherein A means a six-merous aryl radical or a five-merous heteroaryl radical which contains one heteroatom specified in oxygen and sulphur; one or more hydrogen atoms in the above aryl or heteroaryl radicals can be substituted by substituting groups R1 which are independently specified in a group consisting of: F, Cl, Br, I, (C1-C10)-alkyl-, (C1-C10)-alkoxy-, -NR13R14; B means a radical with mono- or condensed bicyclic rings specified in a group consisting of: six-ten-merous aryl radicals, five-ten-merous heteroaryl radicals and nine-fourteen-merous cycloheteroalkylaryl radicals, wherein cycloheteroalkyl links can be saturated or partially unsaturated, while the heterocyclic groups can contain one or more heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, one or more hydrogen atoms in the radical groups B can be substituted by substituting groups R5 (as specified in the patent claim), L means a covalent bond, X means the group -O-, R2 is absent or means one or more substitutes specified in F and (C1-C4)-alkyl radical; R3 and R4 independently mean (C1-C10)-alkyl, (C3-C14)-cycloalkyl, (C4-C20)-cycloalkylalkyl, (C2-C19)-cycloheteroalkyl, (C3-C19)-cycloheteroalkylalkyl, (C6-C10)-aryl, (C7-C20)-arylalkyl, (C1-C9)-heteroaryl, (C2-C19)-heteroarylalkyl radicals, or R3 and R4 together with nitrogen attached whereto can form a four-ten-merous saturated, unsaturated or partially unsaturated heterocyclic compound which can additionally contain one or more heteroatoms among -O-, -S(O)n-, =N- and -NR8-; other radicals are such as specified in the patient claim. Also, the invention refers to using the compound of formula I for preparing a drug. |
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Given invention refers to a compound of formula its stereoisomers, including R and S isomers, wherein: 'A' represents N; Y and Y' represent O; '---' is absent; R1 and R2 are identical or different, and independently represent hydrogen or C1-12 alkyl; R3 represents hydrogen; R4 represents heteroaryl which can be optionally substituted in any acceptable position by one or more substitutes Ra; Z represents -(CH2)n-heteroaryl which can be optionally substituted in any acceptable position by one or more substitutes Ra; T, U, V and W are identical or different, and independently represent hydrogen or halogen; Ra is independently specified in hydrogen, halogen, C1-12 alkyl, C1-12 haloalkyl, -C(=Y)OR7, -(CH2)nYR7, each of which can be optionally substituted in any acceptable position by halogen; R7 represents hydrogen or C1-12 alkyl; m represents 1; m′ represents 0; n represents 1; wherein: the above heteroaryl is specified in 1,2,3-triazolyl, pyridinyl, 1-oxypyridinyl (pyridinyl-N-oxide), pyrazinyl, isoxazolyl, imidazo[1,2-α]pyrimidinyl, imidazo[1,2-α]pyrazinyl. The compounds of the given invention are applicable to prevent, relieve and/or treat bacterial infections in an individual. The bacterial infection is caused by the drug-resistant species Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H. influenza, Moraxella, acid-resistant species like Mycobacterium tuberculosis, as well as linezolid-resistant species Staphylococcus and Enterococcus. |
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Method of obtaining a reagent for preparation of a radiopharmaceutical based on technetium-99m-labelled ciprofloxacin consists in preparation of a hydrochloric acid solution of tin (II) chloride dehydratate with tin concentration 7 mg/ml by careful mixing of 0.07 mg of tin (II) chloride dehydratate and 0.2 ml of 1M hydrochloric acid and carrying out dissolution in an inert gas (argon) medium with further bringing the volume to 10 ml with distilled water after completion of dissolution, sampling 0.015-0.025 ml of the prepared solution and its mixing with 5-6 mg of a ciprofloxacin hydrochloride substance, the obtained solution is frozen at a temperature of liquid nitrogen, placed in a sublimator chamber and subjected to freeze drying at specified parameters of lyophiliser: T=-50°C, vacuum - 0.0015 Torr, for 20.5 hours, with further placement in the upper lyophilic chamber and after-drying for 5.5 hours at a temperature of+15°C. |
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Cocrystalline form of fenbufen Claimed is a cocrystalline form of fenbufen with pyrazinamide, where molar ratio of fenbufen with pyrazinamide constitutes 1:1, which has an endothermal peak from 148 to 152°C by the data of measurements by means of differential scanning calorimetry and peaks at 2θ(°) 7.38, 10.43, 11.04, 21.67 by the data of measurement of polycrystal X-ray radiation diffraction. |
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Methods for increasing stabilisation of hypoxya induced factor-1 alpha There are presented: using a compound of formula (1) or its salt for preparing a drug for increasing HIF-1α stabilisation in a cell, as well as for preparing a drug enhancing the immune response in an individual, for preventive management of a wound to avoid an infection, for treatment of the microbial infection, for improvement of efficacy of a vaccine for management of the wound in the individual. What is presented is a pharmaceutical composition containing the above HIF-1α prolyl hydroxylase inhibitor and one or more additives. What is shown is achieving the declared applications by using the new compound of formula (1) with the HIF-1α prolyl hydroxylase (HIFPH2 (EGLN1)) inhibitor. It makes it applicable for treating HIF-1 alpha activity related diseases, conditions and/or syndromes. |
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Therapeutic compositions containing macitentan There are presented: a product for treating pulmonary arterial hypertension containing macitentan or its pharmaceutically acceptable salt in a combination with a prostacyclin receptor (IP) agonist specified in iloprost, beraprost, 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulphonyl)acetamide, {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid or their pharmaceutically acceptable salt (versions), a pharmaceutical composition for the same application and formulation of the active agents. What is also presented is using macitentan or its salt in a combination with the above agonist for preparing the therapeutic agent for treating pulmonary arterial hypertension. |
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Compositions and methods of treating colitis Group of inventions refers to compositions and methods of treating colitis and other inflammatory intestinal diseases. There are presented: using the compound of the formula (1) or a salt thereof for preparing a drug preparation for treating an inflammatory disease of intestinal epithelial tissue (particularly, indeterminate colitis, Crohn's disease, irritable colon syndrome and ischemic colitis) and a pharmaceutical composition for the same application. What is presented is the pharmaceutical composition for treating colitis containing the compounds of the formula (1) or the salt thereof. |
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Imidazopyridine derivatives as inhibitors of receptor tyrosine kinases Invention relates to novel derivatives of bicyclic heterocyclic compounds of formula (I), which can be applied in prevention or treatment of abnormal or pathological condition, mediated by FGFR kinase, such as cancer. In formula compound, (i) in case when R1 and R2 independently represent hydrogen or C3-8cycloalkyl; A is group Aa, which represents aromatic group, representing phenyl; R3 represents hydrogen or C1-6alkyl; R4 represents group R4a, which represents amino, halogen, C1-6alkyl, -X-R5, phenyl or aromatic heterocyclic group, where said heterocyclic group represents 5- or 6-membered heterocyclyl group and contains 1, 2 or 3 heteroatoms, independently selected from nitrogen, oxygen or sulphur, where said phenyl or said heterocyclyl group can be optionally substituted with one or two Rb groups; or (ii) when R1 represents hydrogen and R2 represents C1-6alkyl or halogenC1-6alkyl; A is group Ab, which represents aromatic 5-membered heterocyclic group; R3 represents hydrogen or C1-6alkyl; R4 is group R4a, which represents halogen; or (iii) when R1 represents hydrogen and R2 represents C1-6alkyl or halogenC1-6alkyl; A is group Ac, which represents aromatic 6-membered heterocyclic group, containing one nitrogen atom as heteroatom; R3 represents hydrogen or C1-6alkyl; R4 is group R4b, which represents halogen, C1-6alkyl, -X-R5 or aromatic heterocyclic group, containing 1, 2 or 3 heteroatoms, independently selected from nitrogen, oxygen and sulphur. Other values of radicals are given in the invention formula. |
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Novel bicyclic heterocyclic compound Claimed invention relates to novel compound of formula (1) or its pharmaceutically acceptable salt, possessing SNS inhibiting properties. In general formula R1 represents (1) hydrogen atom, (2) halogen atom, (3) C1-6alkyl group or (4) C1-6halogenalkyl group (where R1 can be present in any substitutable position of benzene or pyridine ring); L represents (1) simple bond, (2) -O- or (3) -CH2O- (where L can be present in position 5 or 6 of condensed cycle); R2 represents (1) C6-10aryl group (C6-10aryl group is optionally condensed with C3-6cycloalkane), optionally substituted with substituent(s), X represents carbon atom or nitrogen atom. Other values of radicals are given in the invention formula. |
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Invention relates to compounds of general formula or , where Ar1 represents phenyl group, optionally substituted with one or several identical or non-identical halogen atoms; R1 represents hydrogen atom; R4, R5, R6a, R6b represent hydrogen atoms; Y, Z independently represent linear C1-4 alkylene group, optionally substituted with one linear C1-4 alkyl group; Ar2 stands for condensed with benzene 5-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, substituted with one linear C1-4 alkyl group, or derivative of 5- or 6-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, condensed with heteroaromatic 6-memebered ring, containing one or two nitrogen atoms, substituted with one linear C1-4 alkyl group, linear C1-4 alkoxygroup or group -NR7R8, where R7 and R8 independently stand for hydrogen atom, linear or branched C1-4 alkyl group, or R7 and R8 together with nitrogen atom form group of general formula , where R2, R3 represent linear C1-4 alkyl groups, A stands for group -CHR12, oxygen atom or group -NR9, where R12 and R9 stand for hydrogen atom or linear C1-4 alkyl group, m has value 1 or 2, n has value 1 or 2, o has value 0 or 1, p has value 0 or 1, Q stands for group -O-, group -N--H or group -N--CO-R10, where R10 stands for linear C1-4 alkyl group or -NH-R11 group, where R11 represents linear C1-4 alkyl group; and to their salts. Invention also relates to methods of obtaining therein and to based on them pharmaceutical composition, possessing antagonistic activity with respect to receptor CCR3. |
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Phenyl alkyl piperazines, which modulate tnf activity Invention relates to phenyl alkyl piperazines of formula (I) , in which: R1 represents independently on each other hydrogen atom, halogen atom, (C1-C5)alkyl group, (C1-C5)halogenalkyl group, (C1-C2)perfluoroalkyl group, (C1-C5)alkoxyl group or (C1-C2)perfluoroalkoxyl group; R2 stands for (C1-C5)alkyl group or (C1-C5)alkoxyl group, R3 represents (C1-C5)alkyl group; A represents =CH- and =N-; in form of base or additive salt with acid. Invention also relates to pharmaceutical composition for modulation of activity of TNF-alpha, which contains claimed compounds, and to method of their obtaining. |
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P38 kinase-inhibiting isoquinoline derivatives Claimed invention relates to isoquinolinone derivatives of formula (I) or to its pharmaceutically acceptable salt, where R1 represents (C1-C5)alkyl, possibly substituted with 1, 2 or 3 groups, independently selected from groups -(C1-C6)alkyl, -(C1-C6)alkyloxy, -OH or -(C1-C6)alkyl-hydroxy, and where one independent substituent of R1 radical, representing -(C1-C6)alkyl, can be possibly condensed with other independent substituent of R1 radical, representing -(C1-C6)alkyl, with formation of saturated (C3-C4)cycloalkyl; R2 represents H; R3 represents (CH2)d-Y and R3 is independently possibly substituted with one or two groups -(C1-C6)alkyl, -NH2, -HN(C1-C6)alkyl, -N-di-(C1-C6)alkyl, -(C1-C6)alkyl-NH2, -(C1-C6)alkyl-hydroxy; Y us selected from heterocycloalkyl, S-(O)e-heterocycloalkyl, S-(O)e-(C1-C6)alkyl- heterocycloalkyl, -SO2NH-(C1-C6)alkyl; d equal 0, 1 and 2; e equals o, 1 or 2; R4 and R5 are independently selected from (C1-C6)alkyl and halogeno; R6 represents H; heterocycloalkyl represents C- or N-bound 5-7-membered non-aromatic cyclic ring, which, when it is C-bound, contains one NR7 atom, and when it is N-bound, contains one N-atom, or one N-atom and one NR7 atom, R7 represents H or (C1-C6)alkyl. Invention also relates to application of formula (I) compound in treatment of chronic obstructive pulmonary disease (COPD) and asthma. |
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8-substituted isoquinoline derivatives and use thereof Invention relates to a compound of formula (1) or a salt thereof, where D1 is a single bond, -N(R11)- or -O-, where R11 is a hydrogen atom or C1-C3 alkyl; A1 is C2-C4 alkylene, or any of divalent groups selected from the following formulae , and , |
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Combined antibacterial preparation for treating acute intestinal infections Invention refers to an antibacterial preparation for treating gastrointestinal diseases, preferentially acute intestinal infections, including unexplained. The declared preparation represents a mixture of an antibiotic and a biological ingredient, wherein the antibiotic is presented by ofloxacin, while the biological ingredient is a complex of immunoglobulins IgG(56-60):IgA(16-22):IgM(22-24) in the following ratio, mg/flask: ofloxacin - 250, the complex of immunoglobulins IgG,IgA,IgM - 300. |
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Using pentaaminofullerenes as antimicrobial agents and antimicrobial composition based thereon In formula 1 , X denotes a negative charge which is localised on a fullerene skeleton, a chlorine atom bonded to a carbon skeleton or a hydrogen atom; the NR1R2 moiety denotes an amine residue, where R1 and R2 are hydrogen atoms or linear or branched alkyl radicals (CmH2m+1; n=1-20) that are substituted with protonated (NH3 +) or unprotonated (NH2) amine groups, or a piperazine residue of general formula 1c-1 , where R, R'1, R'2, R'3 and R'4 are hydrogen atoms or linear or branched alkyl (CmH2m+1; n=1-20) radicals, as well as residues of aliphatic alcohols -(CH2)nOH, ethers -(CH2)nOR'5, thiols -(CH2)nSH, acids -(CH2)nCOOH, esters thereof -(CH2)nCOOR'5 or amides -(CH2)nCONR'5R'6, for which n=0-20, R'5 and R'6 are hydrogen atoms or linear alkyl (CmH2m+1; n=1-20) radicals. |
![Crystalline forms and two solvate forms of lactic acid salts 4-amino-5-fluorine-3-[5-(4-methylpiperazin-1-yl)-1-h-benzimidazol-2-yl]quinoline-2(1h)one](http://img.russianpatents.com/img_data/1153/11536355-s.gif)
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Invention refers to a crystalline anhydrous form II of a 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolinon-2(1H)-one lactic acid salt, as well as to a method for preparing it, and a pharmaceutical composition inhibiting receptor VEGFR2 and FGER3 activity, on the basis of the above compound. |
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Invention refers to pharmaceutics and medicine and concerns a fibrosis inhibitor containing 2-{4-N-(5,6-diphenyl-pyrazin-2-yl)-N-isopropylamino]butyloxy}acetic aci or a pharmaceutically acceptable salt thereof or 2-{4-[N-(5,6-diphenyl-pyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulphonyl)acetamide or a pharmaceutically acceptable salt thereof as an active ingredient for treating interstitial pneumonia, pulmonary fibrosis, scleroderma or hepatic cirrhosis. |
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Intrapulmonary administration of fuoroquinolone Powder composition for intrapulmonary administration contains particles of ciprofloxacin betaine 3,5-hydrate and an excipient. The particles have a mass median aerodynamic diameter making from approximately 1 to approximately 5 mcm; a pulmonary half-life of betaine 3,5-hydrate makes min. 1.5 h; while a roughness of the composition falls within the range of 3 to 10. |
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Piperazine compound inhibiting prostaglandin-d-synthase Present invention refers to a piperazine compound presented by formula , wherein R1 represents C1-6 alkyl; R2 represents hydroxy, C1-6 alkyl which can contain a substitute specified in saturated or unsaturated 5-6 member heterocycle with 1-3 heteroatoms specified in oxygen and nitrogen, -(C=O)-N(R3)(R4) or -(C=O)-OR5; R3 and R4 may be identical or different, and each represents hydrogen or C1-6 alkyl which can contain a substitute specified in saturated or unsaturated 5-6 member heterocycle with 1-3 heteroatoms specified in oxygen and nitrogen, or R3 and R4 bound through a nitrogen atom whereto R3 and R4 are attached, can form a saturated heterocyclic group specified in 5-6 member heterocycle with 1-3 heteroatoms specified in oxygen and nitrogen; R5 represents hydrogen or C1-6 alkyl; and n represents 1 or 2; or a salt thereof. Also, the invention refers to a pharmaceutical compositions and an agent exhibiting prostaglandin-D-synthase activity and based on the compound of formula I, as well as to a method of preventing and treating a disease wherein prostaglandin D2 is involved. |
Another patent 2550921.