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Crystalline forms of fingolimod hydrochloride Invention refers to a new hydrate of 2-amino-2-(2-(4-octylphenyl)ethyl)propane-1,3-diol hydrochloride salt in the crystalline form with the characteristics below. The hydrate can be used for producing a drug or for treating or preventing a transplanted organ or tissue rejection, or autoimmune diseases in a therapeutically effective amount. The above hydrate is characterised by an X-ray powder diffractogram having peaks at approximately 2.9, 17.2, 30.6, 28.2, 24.4, 8.6 and 25.9 degrees 2-Theta with a limit of error of ±0.2 degrees for each value of 2θ, having a purity of 90% or more, and containing 5.2 to 5.9% of water. |
![(e)-2-(4-{ [3-(2,4-dimethoxyphenyl)acrylamido]methyl} -1h-1,2,3-triazole-1-yl)-2-isopropyl-9-(4-methyl piperazine-1-yl)-3,7-dioxo-3,7-dihydro-2h-furo[3,2-g]chromen, having analgesic activity](http://img.russianpatents.com/img_data/1203/12039841-s.jpg)
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Invention relates to a low-toxic (E)-2-(4-{[3-(2,4-dimethoxyphenyl)acrylamido]methyl}-1H-1,2,3-triazole-1-yl)-2-isopropyl-9-(4-methyl piperazine-1-yl)-3,7-dioxo-3,7-dihydro-2H-furo[3,2-g]chromen of formula (I) , having the analgesic activity in the test "acetic acid-induced writhing". The said property enables to use this compound in medicine. |
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Invention relates to organic chemistry, novel biologically active substances of the class of N-hetarylamides of 4-aryl-2,4-dioxobutanoic acids, and specifically to 2-(5-ethyl-1,3,4-thiadiazolyl)amide of 2-(4-bromophenyl)-4-oxo-4-phenyl-2-butenoic acid. The compound is obtained by reacting 4-bromophenyl-5-aryl-3-imino-3H-furan-2-one with 2-amino-5-ethyl-1,3,4-thiadiazole with equimolar ratio of reactants in a medium of anhydrous toluene while boiling, followed by separation of the end product. |
![Method for producing methyl 1-[(1,3-dioxo-2,3-dihydro-1h-inden-2-yl)-(4-methylphenyl)methyl]cyclohexane carboxylate showing analgesic activity](http://img.russianpatents.com/img_data/1203/12039793-s.jpg)
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Invention refers to organic chemistry, namely to a method for producing methyl 1-[(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)-(4-methylphenyl)methyl]cyclohexane carboxylate (I) consisting in the fact that 1-bromcyclohexane carboxylic acid methyl ester is boiled with zinc and 2-(4-methylbenzylidene)-1H-indene-1,3(2H)-dione in the medium of benzol - ethylacelate - hexamethylphosphotriamide (10:5:1) for 8 hours with 67% yield. |
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Diazahomoadamantane derivatives and methods of using them In general formula (I), X means CH2 or C=O; R means hydrogen, Ar1, Ar2-Ar3, -(CH2)qAr3, -C(O)Ar3, C(O) - (CRxRy)q-Ar3, -C(O) - (CRxRy)q-O-Ar3 or -C (O)-Ar2-AR3; each of the fragments Ar1, Ar2 and Ar3 means C6-10aryl or 5-13-merous heteroaryl containing 1, 2 or 3 heteroatoms specified in N, O or S; q means 1, 2 or 3; Rx and Ry independently mean hydrogen or alkyl; wherein each aryl or heteroaryl are independently unsubstituted or substituted by 1, 2 or 3 substitutes specified in a group of alkyl, halogen, cyano, -OR1a, -O-(CR4aR5a)p-O-, -C(O)R1a, -H(Rb)(R3a), -H(Ra)C(O)R1a and halogenalkyl; wherein R1a and R3a independently mean hydrogen or alkyl; and R4a and R5a mean hydrogen; Ra and Rb independently mean hydrogen or alkyl; p means 1 or 2. |
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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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Sustained release solid therapeutic agent Invention refers to medicine, and represents a sustained release solid therapeutic agent containing a combination of praziquantel with emodepside, polyvinylpyrrolidone and/or a polyvinylpyrrolidone derivative in an amount of 10 to 50 wt %, polyvinylpyrrolidone and/or the polyvinylpyrrolidone derivative is a mixture of one short-chain polyvinylpyrrolidone and one polyvinylpyrrolidone or the polyvinylpyrrolidone derivative with longer chains, and at least one excipient in an amount of 5 to 80 wt %. |
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Co-crystals of tramadol and coxibs Claimed invention relates to novel co-crystal, containing (rac)-tramadol HCl and celecoxib, with respective molecular ratio 1:1. Co-crystal can be used for treating pain, preferably acute pain, chronic pain, neuropathic pain, noticetive pain, minor and from severe to moderate pain, hyperalgesia, pain, associated with central sensitisation, allodynia or cancer pain, including diabetic neuropathy or diabetic peripheral neuropathy and osteoarthritis, fibromyalgia; rheumatois arthritis, ankylosing spondilitis, glenohumeral periarthritis or ischias. Co-crystal is characterised by peaks of powder X-ray diffraction, obtained with application of copper (CuKα1 1.54060 E), and irradiation and absorption bands of infrared spectra. Co-crystal has orthorhombic elementary cell with the following dimensions: a=11.0323 (7) E,b=18.1095 (12) E,c=17.3206 (12) E, as well as endothermic acute peak, corresponding to melt point, with start at 164°C. |
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Present invention refers to immunology. There are presented an antibody and its antigen-binding fragment specifically binding human colony-stimulating factor-1 receptor (CSF-1R) characterised by sequences of complementary-determining regions (CDR). There are also disclosed a nucleic acid coding the antibody according to the invention or its antigen-binding fragment, a vector providing the expression of the antibody and its antigen-binding fragment, and a pharmaceutical composition applicable in treating the diseases associated with an inflammation or an autoimmunity, or cancer. |
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Aminotetraline derivatives containing their pharmaceutical compositions and using them in therapy Invention refers to new aminotetraline derivatives of formula (I) and their physiologically tolerable salts. In formula |
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Medication includes 7.0-9.0 wt % of a dried thick fraction of a product of hazel dry sublimation, 0.025-0.033 wt % of hydrochloride anaprilin, 36.0-38.0 wt % of sodium hydrocarbonate, 24.5-25.5 wt % of boric acid, 12.0-16.0 wt % of phthalic acid, 5.5-7.5 wt % of sodium carboxymethylcellulose, 0.8-1.0 wt % of sodium dodecylsulphate, 0.45-0.55 wt % of calcium stearate and 5.5-10.8 wt % of glucose. |
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Suppositories for treating hemorrhoid, proctitis and other proctologic inflammations Invention refers to an agent for treating hemorrhoid, proctitis and other proctologic inflammations. The above agent represents a suppository 1,35 - 3,65 g containing diosmin 0,3 - 0,65 g, dexpanthenol 0,05 - 0,2 g, green tea extract 0,05 - 0,2 g as active substances, and emulsifier 0,0135 - 0,1825 g and fatty acid glycerides as additives. |
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Method for producing glycolised polypeptide agent Method for producing an anti-inflammatory glycolised polypeptide agent with the use of commercial sea urchin (Strongylocentrotus droebachiensis) waste. A method involves extracting sea urchin inners in ethanol, separating the extract in a separator or a centrifuge, evaporating it, filtering the concentrate, performing gel chromatography, separating a fraction having molecular weight 5.5-7.0 kDa and drying it in the certain environment. The produced agent possesses the pronounced anti-inflammatory action. |
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Method for producing pigment complex of bisnaphthazarin Method for producing a pigment complex of bisnaphthazarin for preventing inflammatory diseases, involving demineralising commercial sea urchins' crusts and needles in an organic acid solution, separating organic acid salts and protein, applying pigment solution on a chromatographic column, washing the column with diluted mineral acid and distilled water, eluting the pigment complex, combining fractions containing the pigments, removing ethanol, lyophilising concentrate in the certain environment. The complex of pigments bisnaphthazarins for preventing inflammatory diseases. |
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Method for entero- and pancreactoprotective action of non-steroid anti-inflammatory preparations Invention refers to medicine, namely to experimental medicine and gastroenterology, and can be used for the entero- and pancreatoprotective action of non-steroid anti-inflammatory preparations in simulating the gastric ulcer and/or pancreatitis experimentally. To this effect, the simulation is preceded by administering courses of Ketanov, Celebrex or Ketonal. The preparations are administered parenterally. A dose for the first three days is 2.5-3.1 mg/kg. A dose for the following three days is 1.5-2.4 mg/kg. That is followed by four days in a dose of 0.5-1.4 mg/kg with the therapeutic course repeated 1.5-2 months later. For the first three days of the repeated course, a dose of the preparation makes 0.7-2.0 mg/kg. A dose for the following three days makes 2.1-2.6 mg/kg. And for the final four days, a dose of the preparation makes 2.7-3.1 mg/kg. |
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Anti-inflammatory and analgesic agent of 1,2-dihydro-1h-2-oxocinchoninic acid isopropylamide Invention refers to an anti-inflammatory and analgesic agent of 1,2-dihydro-1H-2-oxocinchoninic acid isopropylamide of formula |
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Invention relates to N-hetaryl-substituted 4-hydroxy-1-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamides of general formula: , where R=5-methyl-1,3-thiazol-2-yl, or 4-ethoxycarbonylmethyl-1,3-thiazol-2-yl, or 6-methylpyridin-2-yl, or 5-chloropyridin-2-yl, or pyrimidin-2-yl. Novel N-hetaryl-substituted 4-hydroxy-1-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide derivatives which exhibit analgesic activity are obtained. |
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Invention refers to new 2-amino-2-[2-(4-C2-20alkylphenyl)ethyl]propan-1,3-diol salts specified in tartrate, lactate benzoate, succinate, malonate, acetate and propionate in the crystalline form. Each of the above salts is characterised by powder X-ray pattern data. Compounds in the therapeutically effective amount can be used in treating autoimmune diseases. |
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Methyluracil derivative and organic acid complex and method for production thereof Invention relates to a novel complex of 5-hydroxy-6-methyluracil with 5-aminosalicylic acid of formula . The compound has anti-inflammatory activity and can be used as a basic active substance when producing novel medicinal preparations having anti-inflammatory action. The invention also relates to a method of obtaining said complex. The method includes reacting 5-hydroxy-6-methyluracil with 5-aminosalicylic acid in equimolar amounts in an aqueous medium at room temperature for 24 hours, followed by removal of water from the reaction mixture and obtaining the product. |
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Andolina preparation possessing anti-inflammatory, analgesic and wound-healing action Invention refers to the pharmaceutical industry, particularly to a preparation possessing anti-inflammatory, analgesic and wound-healing action. The preparation possessing the anti-inflammatory, analgesic and wound-healing action represents a mixture of an alcoholate of lilac blossom and plantain leaves with honey and extracted juice of unpeeled pomegranate. |
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Bruton's tyrosine kinase inhibitors Present invention refers to compounds having formula III such as below, wherein: Q represents C(Y3) or N; R represents H, -R1, -R1-R2-R3, -R1-R3 or -R2-R3; R1 represents heteroaryl or heterocyclyl each of which is optionally substituted by one or more C1-6alkyls, hydroxyC1-6alkyls, oxogroups or halogenC1-6alkyls; R2 represents -C(=O), -O, -C(R2')2, -C(R2')2C(=O), -C(R2')2C(=O)NR2', C(R2')2 N(R2')C(=O), -C(=NH), -C(R2')2NR2' or -S(=O)2; each R2' independently represents H or C1-6alkyl; R3 represents H or R4; R4 represents C1-6alkyl, C1-6alkoxygroup, aminogroup, C1-6alkylaminogroup, di(C1-6alkyl)aminogroup, heterocyclyl, C1-10alkylheterocycloalkyl, heterocycloalkylC1-10alkyl each of which is optionally substituted by one or more C1-6alkyls, C1-6alkylaminogroups, di(C1-6alkyl)aminogroups, hydroxygroups, hydroxyC1-6alkyls, C1-6alkoxygroups, oxogroups or halogenC1-6alkyls; X represents CH; X' represents CH; and the rest symbols have values as specified in the patent claim. The compounds of formula III inhibit Bruton's tyrosine kinase (Btk). There are also described compositions containing the compounds of formula III, and at least one carrier, thinner or excipient, and a method for producing the compound of formula X in accordance with the following procedure. |
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Method for producing agent possessing anti-inflammatory, diuretic and antioxidant activity Method for preparing an agent possessing anti-inflammatory, diuretic and antioxidant activity, involving milling Spiraea salicifolia shoots representing a mixture of leaves, blossom and shoots, extracting them three times by gradual maceration, mixing in infusing, filtering, condensing, separating, drying in the certain environment. |
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Pharmaceutical compositions containing diacerein Invention refers to medicine and represents a controlled-release preparative form of diacerein administered once a day for treating or autoimmune diseases or their complications. The preparative form contains a core, an active layer, a sustained-release film layer and a delayed-release film layer, wherein the active layer is followed by the sustained-release film, and the delayed-release film layer thereafter. The sustained-release film layer contains ethyl cellulose polymer, povidone, triethylacetate and talc; the delayed-release film layer contains Eudragit polymer, triethylacetate and talc. |
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Short-time high-temperature processing for microbial preparations with anti-inflammatory properties Present invention refers to microbiology, namely to using bacteria, and describes a composition containing microorganisms, a method for preparing probiotics with the anti-inflammatory action and a method for preparing an anti-inflammatory composition containing the probiotics. The composition according to the invention is characterised by the microorganism count subject to the short-time high-temperature processing at 120-140°C for 5-15 seconds. |
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Invention refers to new compounds of formula I, such as below, or its pharmaceutically acceptable salts. What is described is a method for preparing them. |
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Analgesic agent of peptide structure of undercapeptide containing d-octaarginine vector Group concerns using undecapeptide - H-Tyr-Pro-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-Gly-OH·9HCl as an analgesic agent. The group of inventions also concerns a dosage form containing the above peptide as an active substance for treating acute and chronic pain syndromes. |
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Water-soluble salamide derivative possessing tranquilising, nootropic and analgesic activity Invention can be used in chemical-pharmaceutical industry for preparing effective tranquilising salamide preparations and analgesics. What is presented is using salicyloyl morpholine sodium salt of formula (I) as a tranquilising, nootropic and analgesic agent possessing low gastric toxicity. |
![Bridged spiro[2,4]heptane derivatives as alx and/or fprl2 receptor agonists](http://img.russianpatents.com/img_data/1193/11931717-s.gif)
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Bridged spiro[2,4]heptane derivatives as alx and/or fprl2 receptor agonists Invention refers to bridged spiro[2.4]heptane derivatives of formula (I), wherein W means -CH2CH2- or -CH=CH-; Z means -C(O)NR3-* or -CH2NR4C(O)-*, Y means a bond or (C1-C4)alkane diyl group, R1-R4 are those as specified in the description, to preparing and using them as ALX and/or FPRL2 receptor agonists applicable for treating inflammatory and obstructive respiratory diseases. |
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Imidazopyrazine or imidazodiazepine derivatives, active with respect to receptor cb2 Invention relates to field of organic chemistry, namely to heterocyclic compound of general formula (I) or to its pharmaceutically acceptable salt, acid salt or stereoisomer, where Y: NRa and N+R1R2X-; Z: bond, -(CH2)p, -CHOH, -CH=CH-, -C≡C-, -CONH- and -CO-; Rb: C1-C8 alkyl, C2-C8 alkenyl, C6-C10 aryl, -NR5R6,: , and ; with each alkyl, alkenyl and aryl, representing Rb, possibly, contains 1-3 substituents, selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C6 cycloalkyl, C1-C4 alkoxy, C6-C10 aryl, 5-, 6- and 7-membered heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur, halogen, -OH, -NH2, -CN and -NO2; Rc: halogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkinyl, C3-C10 cycloalkyl, C3-C8 cycloalkenyl, C1-C4 alkoxy, C6-C10 aryl, 5-, 6-, 7- and 8-membered monocyclic heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur, 9- and 10-membered bicyclic heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; with C1-C6 alkyl, C2-C6 alkenyl C2-C6 alkinyl, C3-C10 cycloalkyl, C3-C8 cycloalkenyl, C6-C10aryl, 5-, 6-, 7-, 8-membered monocyclic heterocyclyl and 9- and 10-membered bicyclic heterocyclyl, representing Rc, possibly contain 1-5 substituents, selected from the group, consisting of C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C3-C6 cycloalkyl, C4-C8 cycloalkenyla, halogen, -OH, -NH2, C6-C10 (A)(A')(A")(A'")aryl, (A)(A')(A")(A'")heterocyclyl, containing 1-3 heteroatom, selected from nitrogen, oxygen and sulphur, NR14R15, (CH2)pNR14R15, -CN, -NO2, oxo, -COOR14, SOR14, SO2R14, SO2NR14R15, NR15SO2R16, COR14, CONR14R15 and NR15COR16; with each (A), (A'), (A") and (A'")independently absent or representing C1-C4 alkyl, and each heterocyclyl (A)(A')(A")(A'")heterocyclyl is independently selected from the group, consisting of 5-, 6-, 7- and 8-membered monocyclic heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur, and 9- and 10-membered bicyclico heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; the remaining radicals have values given in i.1;and on condition that, if Rc represents heterocyclyl, said heterocyclyl is bound directly through carbon atom of heterocyclyl ring. Invention also relates to particular compounds and to pharmaceutical composition based on formula (I) compound. |
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Invention refers to compounds of formula (I) - oxytocin receptor agonists, to their pharmaceutical compositions containing them. |
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Isoxazoline as fatty acid amide hydrolase inhibitors Present invention refers to isoxazoline FAAH inhibitors of formula (I) or their pharmaceutically acceptable forms, wherein each of G, Ra, Rb, Rc and Rd has a value described in the present application, to pharmaceutical compositions, and methods of treating a FAAH-mediated condition. |
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Co-crystalline form of 2-hydroxybenzamide with salicylic acid In claimed co-crystalline form molar ratio of 2-hydroxybenzamide and salicylic acid constitutes 1:1. Co-crystalline form is characterised by peaks at 2θ(°) 11.5, 14.8, 16.7, 18.8, 22.2, 23.5, 27.0 by the data of measurement of X-ray radiation diffraction on powder, and has endothermic peak from 116 to 124°C by the data of measurement by means of differential scanning calorimetry. Claimed co-crystalline form can be applied for manufacturing pharmaceuticals. |
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Biologically active food additive Biologically active food additive strengthening the organism adaptive power and body defences and having anti-inflammatory and antioxidant activity contains vegetal origin components represented by a complex extract of devil's-club root, Rhaponticum carthamoides root, Hedysarum neglectum Ledeb root, celery roots and leaves, rhodiola rosea root, Japanese angelica tree roots, boschniakia rossica roots, Hungarian sainfoin herb, magnolia-vine fruits; additionally the additive contains chitosan, trepang fermentative hydrolysate, ascorbic acid, taurine, glutathione, nicotinamide, vitamin B1, vitamin B2, vitamin B6, vitamin B12, folic acid, anhydrous calcium chloride, magnesium chloride, zinc chloride, bee honey at preset ingredients ratio. |
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Invention relates to medication, representing betulin bis-isonicotinoate . |
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Invention refers to compounds of formula I wherein R means C1-6alkyl, C1-6halogenalkyl, hydroxy-C1-6alkyl, hydroxygroup or halogen; m, n is equal to 0 or 1; Z1 means CH or NH; Z2 means CH or N; Z3 means CR1, N or NR2; R1 means H, C1-6alkyl, C3-7cycloalkyl, cyanogroup, cyano-C1-6alkyl or halogen; R2 means H or C1-6alkyl; X means CH, CR' or N; X' means CH, CR' or N; r is equal to 1; Y means CH or CR'; R' means R'a or R'b; R'a means a halogen or cyanogroup; R'b means C1-6alkyl, heterocycloalkyl specified in piperazinyl, morpholinyl, piperidinyl, thiomorpholinyl, azetidinyl, pyrrolidinyl, OR", SR", S(=O)2R" or NR"R", optionally substituted by one or more R'c; R'c means a hydroxygroup, oxogroup, cyanogroup, C1-6alkyl, pyridinyl, carboxy-C1-6alkyl, aminocarbonyl-C1-6alkylaminogroup, C1-6alkylaminogroup, C1-6dialkylaminogroup or C1-6alkoxygroup; R" means H, C1-6alkyl, hydroxy-C1-6alkyl, piperidinyl, C3-7cycloalkyl or pyridinyl; Q means S(=O)2Q1, C(=O)Q2, C(=O)OQ3 or Q4; Q1 means C1-6alkyl, C3-7cycloalkyl-C1-6alkyl, C1-6alkylaminogroup or C1-6dialkylaminogroup optionally substituted by one or more Q1'; each Q1' independently means C1-6alkyl or cyanogroup; Q2 means C1-6alkyl optionally substituted by one or more Q2'; each Q2' independently means a cyanogroup; Q3 means C1-6alkyl; Q4 means C1-6alkyl, oxetanyl optionally substituted by one or more Q4'; each Q4' independently means a halogen, cyanogroup, cyano-C1-6alkyl; p is equal to 0, 1 or 2; q is equal to 1 or 2; each means a single bond or a double bond; provided one of Z1 and Z2, and Z3 and Z3 bonds are double and single. |
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Invention relates to novel derivatives of N-(5-brompyridyl)amide of 4-aryl-4-oxo-2-(oxo-1,2-diphenylethylidene hydrazone)butanoic acid of general formula R=Me (1), MeO (2), Cl (3), having analgesic action. |
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Invention refers to medicine, and consists in using compounds that are sigma-1 receptor antagonists. |
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Preparation for treatment and prevention of mastitis in cows Invention relates to field of veterinary and is intended for treatment and prevention of postpartum acute mastitis in cows. Medication contains antimicrobial, anti-inflammatory preparations and distilled water. Medication additionally contains licorice root. As antimicrobial preparation it contains metronidazole. as anti-inflammatory preparation it contains ciprofloxacin, with the following component ratio, g/l: licorice root 80-85 g; metronidazole 3.5-4.0 g; ciprofloxacin 2.0-2.5 g; distilled water - the remaining part. |
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![2-methylsulphanyl-6-nitro-oxo-1,2,4-triazolo[5,1-c] [1,2,4]triazinide l-argininium dihydrate, possessing antiviral activity, method of its obtaining and application for prevention and treatment of west nile fever](http://img.russianpatents.com/img_data/1189/11895113-s.gif)
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Described is novel biologically active compound 2-methylsulphanyl-6-nitro-7-oxo-1,2,4-triazolo[5,1-c][1,2,4]triazinide L-argininium dehydrate of formula , which has antiviral action, method of its obtaining and application for prevention and treatment of West Nile fever. |
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Invention relates to a compound of formula wherein each of R1 and R2 is independently selected from a group consisting of a hydrogen atom, nitro and NR6R7; R3 is C1-C8alkyl; each of R4 and R5 is independently selected from a group consisting of C1-C8alkoxy, phenoxy and phenyl(C1-C8alkylene)oxy; each of R6 and R7 is independently selected from a group consisting of a hydrogen atom, C1-C8alkyl, C(O)R8 and SO2R8;R8 is selected from a group consisting of a hydrogen atom, C1-C8alkyl, halogen-substituted C1-C8-alkyl, C1-C8-alkyl, substituted (C1-C8-alkylsubstituted amino), C1-C8-alkyl, substituted with piperidine and C1-C8-alkyl, substituted with morpholine. |
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Cocrystalline form of niflumic acid with isonicotinamide ot caffeine Invention relates to novel cocrystals of niflumic acid with isonicotinamide or caffeine, where molar ratio of niflumic acid with isonicotinamide or caffeine constitutes 1:1, and cocrystal of niflumic acid with isonicotinamide has entothermic peak from 152 to 162°C according to the data of measurement by means of differential scanning calorimetry and peaks at 2θ(°) 6.3, 7.4, 12.5, 14.5, 19.2, 23.2, 25.0 by the data of measurement of X-ray radiation difraction on powder, and cocrystal of niflumic acid with caffeine has endothermic peak from 155 to 165°C by the data of measurements by means of differential scanning calorimetry and peaks at 2θ(°) 9.7, 12.0, 13.26, 14.3, 17.0, 18.1, 22.5, 26.2 and 26.9 by the data of measurement of X-ray radiation diffraction on powder. |
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Arylamide derivatives as ttx-s blockers Invention refers to compounds of formula (I) and (II), which possess the blocking activity on voltage-sensitive sodium channels, such as TTX-S channels, and their pharmaceutically salts. In general formula (I) and (II), R1 represents -CF3, -CHF2, -OCF3, -OCHF2, -OCH2CHF2/ -OCH2CF3, -OCF2CHF2; -OCF2CF3, -OCH2CH2CF3, -OCH(CH3)CF3, -OCH2C(CH3)F2, -OCH2CF2CHF2, -OCH2CF2CF3, OCH2CH2OCH2CF3, -NHCH2CF3, -SCF3, -SCH2CF3, -CH2CF3 -CH2CH2CF3, -CH2OCH2CF3 and -OCH2CH2OCF3; R2 is specified in (1) hydrogen, (2) halogen (3) -On-C1-6 alkyl, (4) -On-C3-6 cycloalkyl, (5) -On-phenyl, (6) -On-heterocyclic group, (7) -NR7 (C=O)R8; wherein n is equal to 0 or 1, p is equal to 1, 2; R3 and R4 represents hydrogen or C1-6 alkyl, X represents carbon atom; Y represents hydrogen or C1-6 alkyl; Ar represents 4-pyridyl, 4-pyrimidyl or 6-pyrimidyl, which is substituted in the 2nd position by a substitute, which is independently specified in (1) -(C=O)-NR7R8, (2) -NR7(C=O)R8; R9 is specified in: (1) hydrogen, (2) halogen, (3) -On-C1-6 alkyl, wherein alkyl is unsubstituted or substituted by hydroxyl; q is equal to 1, 2 or 3; R10 independently represents hydrogen, C1-6 alkyl, C2-6alkenyl, C3-7 cycloalkyl or phenyl, which is unsubstituted or substituted by one or substitutes independently specified in hydroxyl, -On-C1-6 alkyl and -C3-7 cycloalkyl. |
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Enantiomers of spiro-oxindole compounds and using them as therapeutic agents Invention refers to a new compound, namely to (S)-enantiomer of 1'-{[5-(trifluoromethyl)furan-2-yl]methyl}spiro[furo[2,3-f][1,3]benzodioxol-7,3'-indole]-2'(1'H)-one of formula (I), and a method for preparing it which is effective for treating diseases and conditions, such as pain, an intensity of which can be reduced or relieved by modulating potential-dependent sodium channel gatings. |
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Agent possessing anti-inflammatory, antipyretic and antimicrobial action Agent possessing the anti-inflammatory, antipyretic and antimicrobial action representing a dry extract of drug hedge hyssop leaves and blossom by grinding them, extracting in 96% alcohol on a water bath to a boil, and boiling, evaporating, diluting the evaporated residue by distilled water first, adding chloroform then, cooling to a room temperature and centrifuging, separating a water fraction and drying it in the certain environment. |
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Composition containing bacterial waste products useful for human body Invention is a composition having antibacterial, immunostimulating, anti-allergic and anti-inflammatory action, containing bacterial waste products useful for human body, in the form of exometabolites and fermentolysis products, characterised in that it is a culture medium of lactic acid bacteria, containing laxarane in an amount of 5-10 g/ml, caseicyne, isracydine or their mixture and lectins in an amount of 0.05-2.5 mol/l, histamine in an amount of 0.8-2.0 mmol/l and monocarboxylic fatty acid with an unbranched chain, namely, acetic acid, propionic acid, butyric acid and valeric acid - in an amount of 10-20 mg/ml. |
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Presented group of inventions refers to medicine. What is presented is a method of treating visceral pain and/or one or more symptoms of visceral pain, involving administering a therapeutically effective amount of an antagonist antibody against calcitonin gene-related peptide (CGRP) into an individual suffering visceral pain, or an individual suffering a risk of visceral pain, wherein the CGRP agonist antibody is applicable for peripheral administration. What is also presented is a pharmaceutical composition containing the CGRP agonist antibody and a pharmaceutically acceptable carrier, applicable for peripheral administration. |
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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). |
![Substituted [1,2,4]triazolo[4,3-a]pyridines, demonstrating properties of antagonists of adenosine a2a receptors, and their application](http://img.russianpatents.com/img_data/1186/11869468-s.gif)
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In general formula |
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Synthesis and new saline forms of (r)-5-((e)-2-(pyrrolidin-3-ylvinyl)pyrimidine Present invention refers to new crystalline forms of acid addition salts of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, wherein the acid is specified in methanesulphonic, maleic, fumaric, citric, orotic, 10-camphor sulphonic acids and fencifose. The salts possess the agonist properties of neuronal nicotine receptor (NNR) and can be used for managing or preventing pain, an inflammation or a CNS disorder. Each of the crystalline salts is characterised by an X-ray powder diffraction diagram. The invention also involves an amorphous form of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine monocitrate and polymorphic forms of the above crystalline salts. |
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Condensed triazolamines as p2x7 modulators There are described new compounds of formula I or their pharmaceutically acceptable salts, wherein R1 means phenyl once or twice substituted by C1-6 alkyl, C1-6 alkoxy, halogen or 5-6-merous heteroaryl; R2 is phenyl once or twice substituted by C1-6 alkyl, C1-6 alkoxy, halogen, halogen-C1-6alkyl, halogen-C1-6alkoxy, C1-6 alkylsulphonyl, nitrile, etc. R3 means H or C1-6 alkyl; X - -O-, -NRa-,-S(O)m- or CRbRc, wherein Ra - H, C1-6 alkyl or C1-6 alkylcarbonyl; Rb and Rc mean H or together with the atom to which they are attached, form 5-merous cycle additionally containing 2 oxygen atoms; m is equal to 0-2; Y means -NRc-, wherein Rc - H or C1-6 alkyl. |
Another patent 2551157.