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Substituted cyclohexyldiamines Invention relates to a compound of general formula (1), in which Y1, Y1', Y2, Y2', Y3, Y3', Y4 and Y4' denote -H; R1 and R2 denote an unsubstituted -C1-8-aliphatic; R3 denotes an unsubstituted -C6-16-aryl; R4 denotes -H or -C(=O)R0, where R0 denotes -C1-8-aliphatic, unsubstituted or mono- or polysubstituted with substitutes independently selected from a group consisting of -F, -Cl, -Br, -I and -CN; Q denotes unsubstituted -C1-8-aliphatic-heteroaryl; X denotes =O, =CR6R7 or =N-R6, wherein R5 denotes -NH2, -NH-(unsubstituted-C1-8-aliphatic) or -N-(unsubstituted-C1-8-aliphatic)2, if X denotes =O, or R5 and R6 together form a 5-member ring in which the remaining ring atoms independently denote C, N, S or O, wherein the 5-member ring denotes 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, oxazolyl or thiazolyl, in each case unsubstituted or monosubstituted with unsubstituted C1-C8aliphatic or =O, or unsubstituted tetrazolyl, if X denotes =N-R6, or R5 and R6 together form unsubstituted phenyl, and R7 denotes -H, if X denotes =CR6R7, where "aliphatic" in each case represents a branched or straight, saturated hydrocarbon residue; "aryl" in each case independently denotes a carboxylic ring system containing at least one aromatic ring which does not contain heteroatoms, where the aryl may be optionally condensed with other saturated, (partially) unsaturated or aromatic ring systems; "heteroaryl" denotes indolyl; in the form of a separate stereoisomer or a mixture thereof, in the form of free compounds and/or physiologically compatible salts thereof. The compound of formula |
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Method of treating alzheimer's disease Group of inventions refers to medicine and concerns using a peptide conjugated with a protein representing a keyhole limpet hemocyanin (KLH) protein used as an immunogen for preparing antibodies specifically recognising any of prevailing versions of beta-amyloid peptide Aβ40 and Aβ42; or using an antibody, or an active fragment, or an antibody derivative of the above peptide in preparing a therapeutic agent for preventing and/or treating a disease characterised by amyloid accumulation in the patient's brain. |
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Present group of inventions refers to medicine, namely to therapy and pharmacology, and can be used to increase pharmacological activity and therapeutic efficacy of drug preparations of activated-potentiated forms of hyperdiluted antibodies. That is ensured by administering a pharmaceutical composition containing activated potentiated pathogenic antigen and endothelial NO-synthase antibodies. |
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Method for optimising mental activity of trainees Invention refers to medicine, namely to neurology and concerns improving t mental activity of trainees. That is ensured by daily administration of caffeine 0.2 g followed by self-massage of the head and neck. Self-massage involves performing stroking, compression and rubbing spiral motions started from the head periphery from the back to front scalp border. That is followed by self-massage of the cervical region started with stroking motions from the shoulder joint to the scalp, then pressing up motions in the same direction and rubbing motions circularly with four fingers from the shoulder joint to the occipital bone. Self-massage of the head and neck finally involves stroking motions. |
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Invention refers to compounds of formula |
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Substituted derivatives of 4-aminocyclohexane Invention relates to novel compounds of general formula (1), which possess affinity for µ-opioid receptor and ORL1-receptor, to medications, containing said compounds, and to application of said compounds for obtaining medications, suitable for treating pain, fear, stress and other diseases or conditions. In general formula (1) Y1, Y1', Y2, Y2', Y3, Y3', Y4 and Y4' stand for -H; R1 and R2 independently on each other stand for -H or -CH3; on condition that R1 and R2 both simultaneously do not stand for -H; Q stands for: -C6-16-aryl, non-substituted or mono- or poly-substituted with -F, -Cl, -Br or -I; or heteroaryl; R3 stands for: -C1-8-alkyl, non-substituted or mono- or poly-substituted -OR0, where R0 stands for non-substituted -C1-3-alkyl; non-substituted -C3-6-cycloalkyl-C1-4-alkyl; non-substituted -C1-4-alkyl-C3-6-cycloalkyl; -C6-16-aryl, non-substituted or mono- or poly-substituted with -F, -Cl, -Br, -I, -CN, -R0 or -OR0, where R0 stands for non-substituted -C1-8-alkyl; or heteroaryl; n stands for 0; X stands for -NRA-; RA stands for -H or -R0; where R0 stands for non-substituted -C1-4-alkyl; and RB stands for -C(=O)R0; where R0 stands for non-substituted -C2-8-alkenyl-C6-16-aryl or non-substituted -C1-8-alkyl-(C6-16-aryl)1-2. |
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Method of modulating transporters of atp-binding cassette Invention relates to methods of treating or relieving severity of disease in patient, where disease is selected from mucoviscidosis, hereditary emphysema, chronic obstructive pulmonary disease (COPD), "dry eye" disease. Methods include introduction of effective amount of N-(5-hydroxy-2,4-di-tert-butylphenyl)-4-oxo-1H-quinoline-3-carboxamide or pharmaceutical composition, containing said compound, to patient. |
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Pharmaceutical composition in form of solution for injection and method for production thereof Invention discloses a pharmaceutical composition in the form of a solution, having nootropic and neuromodulating activity, characterised by that it contains N-carbamoylmethyl-4-phenyl-2-pyrrolidone as an agent, hydroxyethyl starch as an auxiliary substance and water for injection. The invention also relates to a method of producing such a pharmaceutical composition, which includes adding hydroxyethyl starch to the water for injection which is preheated to 85-90°C and mixing until complete dissolution, adding N-carbamoylmethyl-4-phenyl-2-pyrrolidone powder and mixing at temperature of 75-85°C until complete dissolution, adding water for injection to obtain the end volume of the solution and mixing once more, holding the obtained solution for 35-40 minutes at temperature of 75-85°C, cooling to 20-30°C, sterilising by filtering through filters with pore diameter of 0.22 mcm and packing in ampoules, which are further sterilised for 8 minutes at temperature of 120°C. |
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Method of post-surgical treatment of cerebral tumour For the purpose of post-surgical treatment of cerebral tumours, memantine is prescribed in a dose of 10 mg daily for 5-7 days before radiation therapy, and in a dose of 20 mg during radiation therapy 4-6 hours before the radiation session. On completing the course of radiation therapy, memantine is prescribed in patients aged up to 60 years old in a dose of 10 mg for 2-3 months daily, in patients aged 60 and older in a dose of 20 mg for 5-6 months daily. |
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Orally soluble and/or effervescent compositions, containing at least one s-adenosylmethyonine (sam) Claimed invention relates to a pharmaceutical, dietary, nutritional orally soluble composition for peroral intake, which contains at least one S-adenosylmethyonine (SAMe) salt in a combination with physiologically acceptable excipients and optionally other active ingredients. The physiologically acceptable excipients include light magnesium oxide. |
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Orally disintegrating tablet temazepam compositions Invention relates to the chemical-pharmaceutical industry and represents an orally disintegrating tablet composition, which includes particles of a therapeutic preparation, containing: a therapeutically effective quantity of, at least, one therapeutic preparation; 0.5-3% ODT binding polymer; sugar alcohol and/or saccharide; and a disintegrant, with particles of the therapeutic preparation being prepared by granulation of, at least, one therapeutic preparation, sugar alcohol and/or saccharide and the disintegrant in the presence of the ODT binding polymer, where the composition mainly disintegrates within approximately 30 seconds after contact with saliva in the oral cavity or in testing by a disintegration test <USP 701>. |
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Invention relates to novel 3-phenyl-3-methoxypyrrolidine derivatives of formula , to any of its enantiomers or any mixture of its enatiomers, or its N-oxides, or its deuterated analogues, or its pharmaceutically acceptable salts, where R1 stands for F, Cl; R2 stands for F, Cl; R3 stands for H, CH3 or CH2CH3; on condition that the said compound does not represent 3-(2,4-difluorophenyl)-3-methoxypyrrolidine and 3-(3,5-difluorophenyl)-3-methoxypyrrolidine. |
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Pharmaceutical drug forms, containing poly-(epsilon-caprolactone) Invention relates to pharmaceutics, namely to pharmaceutical drug forms, containing poly-ε-caprolactone, and methods of obtaining them, an application and methods of treatment with their application. |
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Prevention and treatment of cerebral amyloid angiopathy Invention relates to medicine and deals with an application of an antibody, which binds with residues of 1-5 or 3-7 A-beta, to reduce vascular amyloid in a patient with cerebral amyloid angiopathy, with the antibody being introduced intravenously or subcutaneously. |
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Methods for maintenance or increase of growth or cognitive development Invention relates to compositions for maintenance or increase of growth and cognitive development of a foetus, baby or child; the compositions contain one or more complex lipid(s) where the complex lipid(s) include(s) at least approximately 0.1% of gangliosides of dry substance weight. Additionally, the invention relates to application of the complex lipid(s) for production of the said compositions wherein the said lipids include at least approximately 0.1% of gangliosides of dry substance weight. Additionally, the invention relates to methods for maintenance or increase of growth and cognitive development of a foetus, baby or child; the methods involve the said compositions administration to a foetus, baby or child in need thereof. Additionally, the invention envisages providing a pregnant woman with the said compositions and informing her that the composition will maintain or increase growth or maintain or increase cognitive development of the foetus. |
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Present group of inventions refers to medicine, namely to therapy, and concerns treating vegetovascular dystonia (VVD). That is ensured by administering a pharmaceutical composition containing activated potentiated angiotensin II receptor antibodies and activated potentiated endothelial NO-synthase antibodies. |
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Substituted pyrazolo[1,5-a]pyrimidine compounds as tropomyosin-related kinase inhibitors In formula R1 is H or (1-6C alkyl); R2 represents NRbRc, (1-4C)alkyl, (1-4C)fluoroalkyl, CF3, (1-4C)hydroxyalkyl, -(1-4Calkyl)hetAr1, -(1-4Calkyl)NH2, -(1-4C alkyl)NH(1-4Calkyl), -(1-4Calkyl)N(1-4Calkyl)2, hetAr2, hetCyc1, hetCyc2, phenyl substituted where applicable by NHSO2(1-4Calkyl) or (3-6C)cycloalkyl, substituted where applicable by (1-4C alkyl), CN, OH, OMe, NH2, NHMe, N(CH3)2, F, CF3, CO2(1-4C alkyl), CO2H; C(=O)NReRf or C(=O)ORg; Rb is H or (1-6C alkyl); Rc represents H, (1-4C)alkyl, (1-4C)hydroxyalkyl, hetAr3 or phenyl, wherein the above phenyl is substituted where applicable by one or more substitutes independently from halogen, CN, CF3 and -O(1-4C alkyl); Re represents H or (1-4C)alkyl; Rf represents H, (1-4C)alkyl or (3-6C)cycloalkyl; Rg represents H or (1-6C)alkyl; X is absent or represents -CH2-, -CH2CH2-, -CH2O- or -CH2NRd; Rd represents H or (1-4C alkyl); R3 represents H or (1-4C alkyl); and n is equal to 0-6. The radical values NRbRc, Y, hetAr1, hetAr2, hetAr3, hetCyc1, hetCyc2, NReRf, R4 are specified in the patent claim. The invention also refers to a pharmaceutical composition containing the above compounds, to a method of treating Trk kinase mediated diseases and conditions, such as pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection, osteolytic disease, and to a method of preparing the above compounds. |
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Kynurenine-3-monooxygenase inhibitors Invention refers to organic chemistry and medicine and concerns new compounds of formula , a based pharmaceutical composition containing the above compounds, and a method of treating a condition or a disorder mediated by the kinurenine-3-monooxygenase activity. |
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Compounds for treating peripheral neuropathies Invention refers to using 1-{4-[1-(4-cyclohexyl-3-trifluoromethylbenzyloxyimino)-ethyl]-2-ethylbenzyl}azetidine-3-carboxylic acid or its pharmacologically acceptable salt in treating demyelinated peripheral neuropathy specified in chronic inflammatory demyelinated polyradiculoneuropathy, multifocal motor neuropathy with conduction block or paraproteinemic demyelinated peripheral neuropathy. |
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Method of therapy of remittent multiple sclerosis Invention refers to medicine, namely neurology, and is applicable for treating damaged remitting multiple sclerosis. That is ensured by introducing autologous regulatory T-cells of CD4+CD25+Foxp3+ grown ex vivo at 4.5-5.5 mln cells per 1 kg of a patient's body weight in the remitting multiple sclerosis remission stage. |
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Present group of inventions refers to medicine, namely to neurology, and concerns treating infectious diseases accompanied by neurotoxic disorders. That is ensured by administering a pharmaceutical composition containing an activated-potentiated form of human gamma-interferon (IFN-γ) antibodies and an activated-potentiated form of brain-specific protein S-100 antibodies. |
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Methods of treating chronic pain Invention refers to biochemistry, particularly to using an anti-CGRP antagonist antibody for producing a therapeutic agent for preventing and/or treating chronic pain and/or chronic pain symptoms, and wherein the therapeutic agent is produced for peripheral administration. |
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Methods and compositions for improved delivery of macromolecules Group of inventions relates to biopharmacology and represents a composition, a method and a set, which include a single-chain antibody scFv and a penetration-enhancing substance, selected from amino acid sequences, with a peptide being bound with a protective group with N-terminus, and the penetration-enhancing substance facilitates delivery of large macromolecules (i.e. larger than 10 kDa) through intercellular contacts. |
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Oxicodon and naloxon-containing pharmaceutical compositions with instant release Claimed are: a peroral pharmaceutical composition with an instant release for treating pain in patients or for titration of a dose for the patients, suffering from pain, which contains at least oxicodon or its pharmaceutically acceptable salt and naloxon or its pharmaceutically acceptable salt in an approximate weight ratio oxicodon or its pharmaceutically acceptable salt: naloxon or its pharmaceutically acceptable salt 2:1 (versions), its application for obtaining medication for titration of the dose for the patients, suffering from pain, its application for obtaining medication for treatment of breakthrough pain, a method of titration of the dose in the patient, suffering from pain, and a method of treating breakthrough pain. |
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Embryonated egg isolate and using it Group of inventions refers to medicine, namely to psychiatry, and may be used for treating and preventing disorders specified in a group consisting of depressive, affective and anxious disorders, particularly a major depressive disorder. For this purpose, a patient's therapy is added with a stage of administering a therapeutically effective amount of embryonated egg isolate. |
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Invention refers to the chemical-pharmaceutical industry and represents a compound having a structure according to formula I: |
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Agent for managing alcohol abstinence syndrome Invention refers to medicine, particularly to the addiction pharmacology, and concerns new application of threonyl-lysyl-prolyl-arginyl-prolyl-glycyl-prolyl-diacetate (Selank) as an agent for managing alcohol abstinence syndrome (AAC). It has been stated that Selank eliminates anxiety induced by withdrawal of ethanol. Selank has been detected to recover a threshold of tactile sensation reduced in the period of alcohol withdrawal to the level observed in intact animals. |
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Pharmaceutical composition for preventing and treating vascular disorders and neuropathies Pharmaceutical composition contains a combination of dalargin in an amount of 0.1-4 mg and vitamin specified in B1 (thiamine hydrochloride or thiamine bromide) or vitamin B6 (pyridoxine hydrochloride) or a mixture thereof in an amount of 25-100 mg. |
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Injectable dosage form for treatment of parkinson's disease, method for preparing and using it Invention refers to pharmaceutics and medicine, and presents a pharmaceutical composition for injections for acute forms of parkinsonian syndrome characterised by the fact that an active substance is presented by a therapeutically effective amount of N-(2-adamantyl)-hexamethylenimine hydrochloride (hymantan), and additive substances are presented by water for injections or a physiological solution. The invention also concerns a method for preparing the pharmaceutical composition. |
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Invention relates to buprenorphine analogues of formula , where R1 is selected from -(C1-C10)alkyl, -(C2-C12)alkenyl, -(C3-C12)cycloalkyl, ((C3-C12)cycloalkyl)-(C1-C6)alkyl-; any of which is optionally substituted with 1 or 2 substitutes selected from OH and -(5-12-member)heterocycle, wherein at least one carbon atom is substituted with a nitrogen heteroatom; R2 and R8 each independently is hydrogen, -(C1-C10)alkyl, -(C2-C12)alkenyl, -(C2-C12)alkynyl, -(C3-C12)cycloalkyl, -(5-9-member)heteroaryl, where in the 5-9-member heteroaryl, at least one carbon atom is substituted with a nitrogen, oxygen or sulphur heteroatom, phenyl and naphthyl; any of which is optionally substituted with one or two substitutes selected from OH, halo, -C(halo)3, -(C1-C6)alkyl, phenyl, NH2, CN, OR4 and COOR7; at least one of R2 or R8 is not hydrogen; R3a and R3b are independently selected from hydrogen and -(C1-C6)alkyl; R4 is selected from -(C1-C6)alkyl, -C(halo)3 and phenyl; R7 is hydrogen; X is selected from (C1-C6)alkoxy or OH; Z is (CH2)m; Y is (CH2)n-CH or a direct bond, under the condition that when Y is a direct bond, R8 is absent; m equals 1 and n equals 0. The invention also relates to a pharmaceutical composition which modifies opioid receptor function and is intended to treat pain, which contains compounds of formula I, a method of preparing said composition, a method of modulating an opioid receptor and a method of treating pain. |
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Invention describes a group of substituted N-phenylbipyrrolidincarboxamides of formula (I), where m equals 1 or 2; n equals to 1 or 2; p equals to 1 or 2; R1 is hydrogen, (C1-C4)-alkyl, CF3, (C1-C4)-alkoxy-(C1-C4)-alkyl; and R2 is hydrogen, halogen, (C1-C4)-alkyl or CF3; or their salt, or enantiomer, or diastereomer. In particular, compounds in accordance with the invention are modulators of H3 receptors and, therefore, are suitable for application as pharmaceutical preparations, in particular, in treatment and (or) prevention of different diseases, modulated by H3 receptors, including diseases associated with the central nervous system. |
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Antipsychotic agent and method for preparing it Invention concerns an antipsychotic agent representing the amino acid glycine immobilised on the detonation-synthesised nanodiamond particles of 2-10 nm in size, and a method for preparing it. |
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Antidepressant drug and method for preparing it Invention concerns an antidepressant drug representing the amino acid glycine immobilised on the detonation-synthesised nanodiamond particles of 2-10 nm in size, and a method for preparing it. |
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Anxiolytic and method for preparing it Invention concerns an anxiolytic representing the amino acid glycine immobilised on the detonation-synthesised nanodiamond particles of 2-10 nm in size, and a method for preparing it. |
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Invention relates to a method of enhancing cognitive function in an animal or human being. Said method includes administering a compound which is selected from a group consisting of: steviol, isosteviol, and a mixture of steviol and isosteviol in a cognitive function enhancing amount. The invention also relates to a composition and nutraceutic agent containing one of said compounds or a mixture thereof. |
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Medication for treating attention deficit disorder and method of treating attention deficit disorder Group of inventions relates to medicine, namely to neurology, and deals with treatment of attention deficit disorder. For this purpose introduced is a pharmaceutical composition, containing potentiated form of antibodies to brain-specific protein S-100 and as an additional enhancing component - an activated-potentiated form of antibodies to endothelial NO-synthase. |
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Tetrodotoxin-based lyophilised preparation and method of its production Group of inventions relates to methods of obtaining a lyophilised preparation of tetrodotoxin and to a tetrodotoxin preparation for relief of the drug withdrawal in case of addiction to opiates. The method of obtaining the lyophilised preparation of tetrodoxin includes the following stages: 0.1-20 mcg/dose of tetrodotoxin is dissolved with 0.1% solution of citric acid to regulate pH within the range of 3.5-4.5 in injection water and filtered to remove pyrogen; separately dissolved are: a stabiliser - dextran or trehalose - and a filling agent, representing an isotonic solution of sodium chloride or mannit in injection water. After that, 0.1% solution of citric acid is added to regulate pH within 3.5-4.5, then, activated carbon is added with keeping at a temperature of 60°C and mixing for more than 30 minutes, filtering to remove pyrogen and cooling to room temperature. After homogeneous mixing of the obtained solutions and realisation of ultrafiltration, lyophilic drying is carried out. Lyophilic drying consists in preliminary freezing, drying under vacuum at reduced temperature, drying under vacuum at increased temperature, with each drying being performed at a certain temperature for the specified time period. After that, filling with inert gas is performed with control of water content at 3% level, with further sealing. Another version includes addition of additional solution of lidocaine chloride to the solution of tetrodotoxin and citric acid at the first stage. Also disclosed is the tetrodotoxin preparation for relief of the drug withdrawal in case of addiction to opiates, obtained by the said method, which is characterised by the weight ratio tetrodotoxin:filling agent:stabiliser, equal to 1:(150-3000):(50-6000). |
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Treatment of alzheimer's disease with cytokines Invention relates to the field of biotechnology and medicine. Claimed is a method of treating Alzheimer's disease, associated with low production of IL-10. The method includes increase of IL-10 level in an individual by introduction of efficient quantity of IL-10 or a molecule, increasing IL-10 production. Beta-amyloid can be one version of such a molecule. The claimed group of inventions can be used in medicine. |
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Therapeutic agent for treating pathological syndrome and method of treating multiple sclerosis Present group of inventions refers to medicine, namely neurology, and concerns treating pathological syndrome specific for multiple sclerosis. That is ensured by administering a pharmaceutical composition containing an activated-potentiated form of human gamma-interferon (IFN-γ) antibodies and an activated-potentiated form of brain-specific protein S-100 antibodies. |
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Medication, possessing anxiolytic activity Claimed is application of potassium salt 2-[1-(1,1-dioxothietanyl-3)benz-imidazolyl-2-thio]acetic acid (known as immunomodulator) as medication, possessing anxiolytic action. It is demonstrated that action of claimed medication on different anxiety components is comparable with effect of standard anxiolytics phenazepam and afobazole, but it is not accompanied by myorelaxant action characteristic of benzodiasepin anxiolytics (phenazepam). |
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What is presented is a group of inventions involving a pharmaceutical composition, a method of preparing it, a method of treating Parkinson's disease and a method of reducing a 'wear' effect in the given patients by administering the same. The pharmaceutical composition in the form of a single oral dose for treating Parkinson's disease consists of a mixture of a) Levodopa or its salt in an amount of 50 mg to 300 mg in the form of prolonged release, b) Carbidopa or its salt in an amount of 10 mg to 100 mg in the form of prolonged release, wherein the prolonged release is ensured by coating or mixing Levodopa and Carbidopa with one or more rate control polymers, and c) Entacapone or its salt in an amount of 100 mg to 1000 mg in the form of prolonged release, optionally with other pharmaceutically acceptable excipients. |
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Method for prevention of ixodic tick-borne borreliosis in children Method for prevention of ixodic tick-borne borreliosis in children by an antibacterial therapy consists in the fact that after establishing the fact of Borrelia infected tick suction, ceftriaxone 50 mg/kg a day is injected intramuscularly for 3 days in a combination with a single intramuscular injection of bicillin 5 in a dose of 50 thousand IU/kg; anaferone is also prescribed in a dose of 1 tablet 3 times a day for 30 days. |
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There are presented: a combination possessing analgesic action of at least one sigma ligand and at least one opioid or opiate compound specified in morphine and its structural derivatives, phentanyl and tramadol for simultaneous, separate or sequential administration; the sigma ligand has the general formula ; |
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Invention refers to using an oxadiazolyl compound of the formula I |
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Advanced glycation end product (rage) receptor antibodies and using them Invention refers to biotechnology, more specifically to recovered monoclonal antibodies, particularly CDR-grafted humanised antibodies binding to an epitope of human RAGE molecule, and particularly possess an ability to inhibit RAGE binding to various ligands. The invention also refers to a method for preparing the above antibodies, a recovered nucleic acid coding them, an expression vector, a host cell and a pharmaceutical composition. |
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Il-1beta-binding antibodies and fragments thereof Present invention refers to immunology and biotechnology. What is presented is an IL-1β-binding antibody or its IL-1β-binding fragment containing V heavy and light chain regions. The above antibody binds to human IL-1β with dissociation constant less than 1pM. Versions of the antibody are described. There are disclosed corresponding coding nucleic acids (NA), as well as: a NA passage vector to a host cell, the host cell producing a coded polypeptide. What is described is using the antibody for preparing the other format of the above antibody: "camel-like", VHH antibody, nanobody. What is disclosed is a pharmaceutical composition for treating or preventing an IL-1β-related disease in a mammal on the basis of the antibody, as well as a method of treating or preventing the IL-1β-related disease in a mammal. |
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Antigen tau-peptides and their application Invention relates to field of biotechnology, in particular to immunogens based on antigenic tau-peptide, and can be used in medicine. Obtained is immunogen, which contains antigenic tau-peptide, consisting of amino acid sequence, selected from SEQ ID NO:6, 8-19, 21-26, 105 and 108-112, covalently bound with immunogenic carrier by means of linker, represented by formula (G)nC, where n equals 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10. Linker can be located either on C-terminal (peptide -(G)nC), or on N-terminal (C(G)n-peptide) of peptide. Obtained immunogens are used as base for creation of pharmaceutical compositions for treatment of tau-associated neurological disorders. |
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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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2-pyridyl-substituted imidazoles as therapeutic alk5 and/or alk4 inhibitors Described are novel 2-pyridyl-substituted imidazoles of general formula (I) , where Ra is C1-6alkyl; m = 1; A1 = N; A2 = NR1, where R1 is hydrogen; X is bond, -NR2-, -O- or -S-, where R2 is hydrogen or C1-3alkyl; Rb independently is H, halogen, C1-6alkyl, C2-6alkenyl, C2-6alkinyl, -(CH2)q-OR3, where R3 - C1-6alkyl or C1-6halogene alkyl, and q=0,1, -(CH2)q-NR3R4, where R3 and R4 independently are C1-6alkyl or together with nitrogen atom - pyrrolidinyl or morpholinyl, and q=0-2; -SR3, where R3 - C1-6alkyl, -(CH2)q-CN, where q=0 or 1, -COR3 or -CO2R3, where R3 is C1-6alkyl, -CONR3R4, where R3 and R4 is hydrogen, -NHCOR3 or -NHSO2R3, where R3 stands for C1-6alkyl; n equals 0, 1, 2, 3, 4 or 5; or their pharmaceutically acceptable salts, or hydrates and pharmaceutically acceptable compositions for treatment or abatement of metastasis of tumour cells, carcinomas, fibrosis by inhibiting pathways of transmission of signal of TGF-β or activin, or both. |
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Aroylamino- and heteroaroylamino-substituted piperidines as glyt-1 inhibitors Invention relates to a compound of general formula I , where R1 is a hydrogen atom, a lower alkyl, CD3, -(CH2)n-CHO, -(CH2)n-O-lower alkyl, -(CH2)n-OH, -(CH2)n-cycloalkyl or is a heterocycloalkyl (where the heterocycloalkyl is a partially unsaturated ring containing up to 6 carbon atoms, at least one of which is substituted with O); R2 is a hydrogen atom, a halogen atom, hydroxy, lower alkyl, di-lower alkyl, -OCH2-O-lower alkyl or lower alkoxy; or the piperidine ring along with R2 forms a spiro-ring selected from 4-aza-spiro[2,5]oct-6-yl; Ar is an aryl or heteroaryl (where the heteroaryl is a cyclic aromatic hydrocarbon radical consisting of one ring and containing 6 ring atoms, and which contains at least one heteroatom selected from N), optionally having one, two or three substitutes selected from a halogen atom, lower alkyl, lower alkyl having as substitutes, a halogen atom, a lower alkoxy having as substitutes, a halogen atom, cycloalkyl, lower alkoxy, S-lower alkyl, heterocycloalkyl (where the heterocycloalkyl is a partially unsaturated ring containing up to 6 carbon atoms, at least one of which is substituted with N), or optionally having as substitutes, phenyl, optionally having R' as substitutes, and R' is a halogen atom, CF3, lower alkyl, lower alkoxy or a lower alkoxy having as substitutes, a halogen atom, or is a heteroaryl (where the heteroaryl is a cyclic aromatic hydrocarbon radical consisting of one ring and containing 6 ring atoms, and which contains at least one heteroatom selected from N and S); R is a lower alkyl, heterocycloalkyl (where the heterocycloalkyl is a partially unsaturated ring containing up to 6 carbon atoms, at least one of which is substituted with O), aryl or heteroaryl (where the heteroaryl is a cyclic aromatic hydrocarbon radical consisting of one ring and containing 6 ring atoms, and which contains at least one heteroatom selected from N), Where the aryl and heteroaryl optionally have as substitutes, one or two R'; n equals 0, 1, 2 or 3; or to a pharmaceutically acceptable acid addition salt, a racemic mixture or a corresponding enantiomer and/or optical isomer of said compound. The invention also relates to pharmaceutical compositions based on a glycine reuptake inhibitor of a compound of formula I. |
Another patent 2513604.