Compositions and medicinal forms on basis of gastrinum, application and reception methods
SUBSTANCE: invention concerns area of medicine and concerns compositions and medicinal forms on the basis of Gastrinum, application and reception methods. The essence of the invention includes the bond of Gastrinum representing conjugates of fragments of amino-acid sequence of Gastrinum, possessing functional ability to contact Gastrinum/SSK receptor, with various carriers, including application amino-acid spacers, and application of bifunctional sewing agents, and also a method of treatment by the compositions including bond of Gastrinum, sick of diabetes.
EFFECT: advantage of the invention consists in action prolongation.
7 cl, 8 ex, 3 tbl, 2 dwg
The text descriptions are given in facsimile form.
1. Connection gastrin, including amino acid sequence containing the amino-end Z-Ym-X-Tyr-Gly-Trp-Leu-Asp-Phe-NH2,
where Z is a human serum albumin or polyethylene glycol;
Y means (Gly-Ala);
m is 0 or 5;
X is Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala, and the cysteine residue at amino ends of the Y, when m is 5, or the amino ends of X, when m is 0,
provided that the connection gastrin binds to the receptor gastrin/Sscv.
2. Connection gastrin according to claim 1, in which Z stands for human serum albumin.
3. Connection gastrin according to claim 1, where m is equal to 5.
4. Connection gastrin according to claim 1, where m is 0.
5. A pharmaceutical composition comprising a compound of gastrin p is any one of the preceding paragraphs and pharmaceutically acceptable carriers or excipients.
6. A method of treating diabetes in a patient, which consists in the introduction of this patient the pharmaceutical composition according to claim 5.
7. The way to maintain over a long period of time a higher level of gastrin in serum compared to the level of a peptide having the amino acid sequence of gastrin in serum, introducing a pharmaceutical composition according to claim 5.
SUBSTANCE: invention concerns compounds of the formula M-N-O-P-G, where M is a metal-chelating agent (in a complex with a radioactive metal nuclide or not), N-O-P is a linker, and G is a peptide for target transportation to a GRP receptor. Also the invention concerns methods of visualisation for a patient with the help of the claimed compounds, methods of obtaining a diagnostic visualisation and radiotherapeutic medium.
EFFECT: improved compounds for application in diagnostics visualisation or therapy.
49 cl, 51 dwg, 8 tbl, 58 ex
SUBSTANCE: present invention pertains to new compounds with formula , in which R represents H, (C1-C12)-alkyl or (C1-C4)-alkyl-(C6-C12)-aryl. In the alkyl, one or more CH2-groups can be substituted with -O-. The invention also relates to the method of obtaining these compounds. The method involves reacting dimethylbenzoic acid ester with formula where R assumes values given above, with a chlorinating agent in an inert solvent or without a solvent at temperature above 40°C, and then cleaning, if necessary. Formula (I) compounds are essential intermediate products during synthesis of PPAR agonists with formula , in which R represents H, (C1-C12)-alkyl or (C1-C4)-alkyl-(C6-C12)-aryl. In the alkyl, one or more CH2-groups can be substituted with -O-; Y represents -(CH2)3-, 1,3-phenylene, 1,3-cyclohexanediyl; R' represents H, F, Br, CF3, (C1-C6)-alkyl, O-(C1-C6)-alkyl, phenyl; CF3; obtained from reaction of compounds with formula with formula (I) compounds in toluene, N-methylpyrrolidone or other aprotic solvents, in the presence of a suitable base, at temperature lying in the -78°C - +50°C interval, with subsequent extractive processing and, if necessary, crystallisation of the end product.
EFFECT: obtaining new compounds.
8 cl, 5 ex
SUBSTANCE: in novel compounds of formula (I) R1 is selected from , R2 stands for hydrogen or (lower) alkoxy; R3, R4, R5 and R6 are selected each independently from hydrogen, (lower) alkyl, halogenated (lower) alkyl, haloid or cycloalkyl; on condition that R2, R3, R4, R5 and R6 do not all stand for hydrogen; R7, R8 and R9 stand each independently for hydrogen, (lower) alkyl, (lower) alkoxy, (lower) hydroxyalkyl or halogenated (lower) alkyl; on condition that R7, R8 and R9 do not all stand for hydrogen; R10 stands for (lower) alkyl or halogenated (lower) alkyl.
EFFECT: obtaining novel biologically active compounds with improved properties.
16 cl, 38 ex
FIELD: medicine, pharmacology.
SUBSTANCE: invention concerns area of biopharmacology, medicine and medical products. Composition, a set, application and the obtaining method of a preparation insulin - of cosecreting cells is revealed. Thus the composition contains Gastrinum or its active analogue, or its fragment, ligand a receptor of glucagon-like peptide-1 (GLP-1) and a pharmaceutically comprehensible carrier.
EFFECT: provocation of insular neogenesis or augmentation of number of pancreatic insulin-cosecreting β-cages at a mammal at diabetes.
17 cl, 2 tbl, 3 ex
FIELD: medicine; cardiology.
SUBSTANCE: scheme of examination and treatment of patients with a metabolic syndrome (MS) consists in the following. In the presence of AG with average degree of cardiovascular risk in a combination to visceral adiposity and: overweight<27 kg/m2, during 3-6 month prescribe non-medicament actions referred on treatment of adiposity, at achievement of AD target level after the specified term, non-medicament actions continue; with overweigth≥27 kg/m2 or combination of overweigth≥27 kg/m2 and hyperglycemias on an empty stomach, during 3-6 month, prescribe Orlistat and-or Metforminum, at achievement after the specified term of target level of a AD, continue the therapy; with combination overweigth≥27 kg/m2, hyperglycemias on an empty stomach and glucose tolerance during 3-6 month, prescribe acarbose or Orlistat and acarbose in a combination with Metforminum, at achievement after the specified term of target AD level, continue the therapy; in combination of overweight≥27 kg/m2, hyperglycemias on an empty stomach, glucose intolerance and lipidemia during 3-6 month, prescribe Orlistat in a combination with Metforminum or acarbose, at achievement of AD target level after the specified term, continue the therapy. In the presence of AG with high degree of cardiovascular risk in combination with visceral adiposity and: overweight<27 kg/m, prescribe non-medicament actions referred on treatment of obesity, and the antihypertensive combined therapy; overweight≥27 or combination of overweight≥27 kg/m2 and hyperglycemias on an empty stomach, prescribe Orlistat and-or Metforminum, and the antihypertensive combined therapy; with overweight≥27 kg/m2, hyperglycemias on an empty stomach and glucose intolerance, prescribe the antihypertensive combined therapy in a combination with acarbose or Orlistat and acarbose together with Metforminum; with overweight≥27 kg/m2, hyperglycemias on an empty stomach, glucose intolerance and lipidemia, prescribe the antihypertensive combined therapy in combination with Orlistat and Metforminum or acarbose; with lipidemia, glucose intolerance, prescribe the antihypertensive combined therapy in a combination with Orlistat or acarbose; SD 2, and also lipidemia, glucose intolerance, a plasma glucose on an empty stomach < 6,0 mmol/l, prescribe the antihypertensive combined therapy in a combination with orlistate or akarbose; SD 2, and also a lipidemia broken by tolerance to a glucose, plasmatic glucose on an empty stomach > 6,0 mmol/l, prescribe the antihypertensive combined therapy in a combination with preparations decreasing amount of sugar in blood. Affecting only on one of the MS components, it is possible to achieve appreciable improvement due to indemnification of changes in other links of its pathogenesis.
EFFECT: use of the offered algorithms of treatment of patients with a metabolic syndrome will allow optimising their treatment.
12 cl, 2 tbl, 2 ex
FIELD: medicine; pharmacology.
SUBSTANCE: invention refers to medicinal agents containing combined inhibitor of dipeptidylpeptidase IV (DPPIV) and biguanide agent. Offered application of pharmaceutical agent implies production of preventive and therapeutic agent and method of intensified effects of active circulating GLP-1 and/or active circulating GLP-2. Besides, invention concerns method of prevention or treatment of disease connected with active circulating GLP-1 and/or active circulating GLP-2, specifically diabetes, obesity, hyperlipidemia, gastrointestinal diseases. Combined inhibitor DPPIV of formula (I) and biguanide agent, specifically phenformine, methformin or buformine stimulates action of active circulating glucagon-like peptide-1 (GLP-1) and/or active circulating glucagon-like peptide -2 (GLP-2) and, therefore inhibits destruction of GLP-1 and GLP-2, with their levels raised up with biguanide agent.
EFFECT: agent has improved efficiency.
17 cl, 12 tbl, 425 ex
SUBSTANCE: invention can be used in treatment of hyperglycemic ketoacidic coma in patients with diabetes. For this purpose, the solutions of reamberin, ozonised saline and mexidole, and alpha-lipoic acid and cytoflavin are injected intravenously in particular dosage and regimen, developed for different severity of pathologic process.
EFFECT: method provides efficient treatment due to correction of metabolism by administrating the described solutions in optimal dosage and regimen.
FIELD: medicine, endocrinology, pharmacy.
SUBSTANCE: invention relates to treatment of diabetes mellitus and complications associated with diabetes mellitus. Invention proposes using a pharmaceutical composition for prophylaxis and treatment of diabetes mellitus and associated complications. Pharmaceutical composition comprises an enhancer for sensitivity to insulin (but excluding troglitazone) in combination with at least component from group consisting of aldose reductase inhibitor, biguanide, statin compound and angiotensin-converting enzyme inhibitor. Proposed pharmaceutical composition offers the strong inhibitory effect with respect to diabetic hyperglycemia.
EFFECT: valuable medicinal properties of pharmaceutical composition.
FIELD: biology, medicine.
SUBSTANCE: claimed method includes dissociation of laboratory animal pancreas tissue by homogenizator. Substance with antiprotease activity, such as contrical is added into solution for homogenization. Obtained cell elements are placed in cultural medium containing DMEM medium 80 %; non-inactivated embryo calf serum 20 %; glucose 10 g/l; L-glutamine 500 mg/l; gentamicin 50 mg/l; heparin 5000 IU/l; insulin 50 mg/g; stem cell growth factor 10 ng/ml; epidermal growth factor 30 ng/ml; leucosis-inhibiting factor 10 ng/ml; interleukin-6 10 ng/ml; fibroblast growth factor 10 ng/ml; and incubated in CO2-incubator at 37°C, 5 % CO2 and air humidity of 100 % for 14-21 days.
EFFECT: new method for cloning of regional pancreas stem cells.
1 ex, 2 dwg
FIELD: medicine, cardiology, endocrinology, hematology.
SUBSTANCE: the present innovation deals with matching differentiated therapy of thrombopathy in patients with metabolic syndrome. One should detect thrombocyte aggregation index in three transfer tests - collagen, collagen-aspirin and collagen-imidazole. Depending upon the value of collagen test and the ratios of collagen-aspirin and collagen, and, also, collagen-imidazole and collagen tests one should prescribe differentiated therapy. Such therapy deals with hypocaloric diet, dosed physical loading and introduction of metformin at the dosage of 500 mg twice daily at different combinations. Such differentiated approach provides efficient correction of thrombopathy in case of metabolic syndrome.
EFFECT: higher efficiency.
4 ex, 1 tbl
FIELD: medicine, endocrinology.
SUBSTANCE: invention relates to a method for treatment diabetes mellitus of type 2. Method involves using a birch bark extract in addition to usually used preparations. Method provides enhancing the effectiveness of treatment based on sugar-decreasing, antioxidant and hypolipidemic properties of biologically active components of birch extract.
EFFECT: improved and enhanced method of treatment.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention concerns vaccines, particularly vaccines for meningococcal infections and diseases. Invention claims immunogenic composition for transport via mucosa, including capsular saccharides of at least two of the following serological groups: A, C and W135 and Y N. Meningitidis, as well as trialkylated chitosan.
EFFECT: enhanced production of immune response to meningococci in mucosa, possible balance shift of Th1/Th2 type responses.
16 cl, 24 dwg
SUBSTANCE: invention pertains to modified polysaccharide in particular to modified polysaccharide Neisseria meningitidis of serogroup A, which preserves immunogenicity, but has improved stability. The modified polysaccharide is obtained from reaction of capsular polysaccharide, or its fragment - oligosaccharide, with CDI type bifunctional reagent, accompanied by reaction with an amino-compound, such as dimethylamine. Description is also given of modified polysaccharide conjugates and vaccines, which are obtained from such conjugates.
EFFECT: obtaining modified saccharide.
70 cl, 17 dwg
FIELD: medicine; veterinary science.
SUBSTANCE: method of higher meat production of broilers provides single injection for day birds of liposomal forms of preparation containing chimeric protein with water insoluble enzyme-inactive chloramphenicol acetyltransferase without 10 S-terminal aminoacids, aminoacid spacer (Sp)n, where n=1, 2, 4, 8 and somatostatin-14 with aminoacid sequence AGCFWKTFTSC, with median size of liposomes 250±50 nm. And preparation is introduced in combination with Marek's disease factor vaccine.
EFFECT: invention allows for higher effective meat production of broilers using single injection of preparation during the whole fattening period.
2 cl, 1 tbl
SUBSTANCE: invention concerns aldehyde derivatives and conjugates of di-, oligo- or polysaccharide, of the general formula (I), methods of obtaining them, and pharmaceutical composition based on them and capable of staying in blood flow for prolonged time. , where R is -CH(CHO)CH2OH, -CH2CHO, -CH(CH2NHR1)CH2OH, -CH(CH2NHNHR1)CH2OH, -CH(CH=NNHR1)CH2OH, -CH2CH2NHR1, -CH2CH=N-NHR1, -CH2CH2NHNHR1; R1 is polypeptide or albumen; GlyO is a sialic acid bond; R3 is H; R4 is OH; n is 2 or more.
EFFECT: obtaining pharmaceutical composition based on aldehyde derivatives of sialic acid capable of staying in blood flow for prolonged time.
20 cl, 7 tbl, 22 dwg, 10 ex
FIELD: medicine; pharmacology.
SUBSTANCE: invention group refers to compositions containing hapten-carrier conjugate within arranged and repeating matrix, and method of related composition production. Offered hapten-carrier conjugate used for induction of agent-specified immune reaction in case of addiction or abuse, contains cortex particle including at least one first apposition site, where specified cortex particle is virus-like particle of RNA-phage, and at least one nicotine hapten with at least one second apposition site, where specified second apposition site is associated by at least one covalent non-peptide bond with specified first apposition site, thus forming arranged and repeating hapten-carrier conjugate. Offered conjugates and compositions under this invention can include virus-like particles connected to various haptens including hormones, toxins and agent, especially agents causing addiction, as nicotine and can be applied for induction of hapten immune reaction for therapeutic, preventive and diagnostic purposes.
EFFECT: vaccines can induce stable immune reactions for nicotine and fast reduce nicotine availability for brain absorbing.
31 cl, 6 dwg
FIELD: medicine, virology, immunology, molecular biology.
SUBSTANCE: invention involves a composition comprising a regulated and repeated matrix of antigens or antigen determinants and, in particular, matrix comprising RANKL protein, RANKL fragment or RANKL-VLP peptide. Invention relates to a composition comprising viral-like particle and at least one RANKL protein, RANKL fragment or RANKL peptide bound with its, and to a method for preparing conjugates and regulated and repeated matrices, respectively. Proposed compositions can be used for preparing vaccines used in treatment of bone diseases and as a pharmaceutical vaccine used for prophylaxis or treatment of bone diseases, and for effective induction of immune responses, in particular, humoral responses. The advantage of invention involves enhancing induction of immune responses to RANKL protein.
EFFECT: valuable biological and medicinal properties of matrices.
28 cl, 7 dwg, 20 ex
FIELD: medicine, polymers.
SUBSTANCE: invention relates to conjugates consisting of a water-soluble polymer of molecular mass from 200 to 20000 Da and representing polyethylene glycol or alkyl chain to which two molecules of synthetic peptides, not less, are bound by reactive functional group and wherein each peptide comprises amino acid sequence originating from region HR1 or HR2 of human immunodeficiency virus (HIV) gp41. Invention relates to methods for using these conjugates for delivery inhibition of to HIV target-cell by addition of indicated conjugates in the amount providing effective inhibition of cell infection with indicated virus. Also, invention relates to methods for preparing conjugates by functional adding of each molecule of synthetic peptide to polymer through reactive functional group.
EFFECT: valuable biological properties of conjugates.
27 cl, 2 dwg, 6 tbl, 6 ex
FIELD: chemical and pharmaceutical industry.
SUBSTANCE: invention relates to lyophilized pharmaceutical immunocytokine composition including immunocytokine and containing as cytokine component interleukin-2 (IL-2), sugar or aminosugar, amino acid and surfactant, wherein said composition contains: immunocytokines from 0.1 to 25 mg/ml; sugar or aminosugar 1-200 mg/ml; amino acid 1-200 mMol/l; and surfactant 0.001-1 mass %.
EFFECT: composition for parantheral administering with prolonged storage time even at increased temperatures.
13 cl, 8 ex, 4 tbl, 2 dwg
SUBSTANCE: method involves carrying out single-stage conjugate synthesis having stereospecific (affine) compound conjugated in covalent way to suspensoid carbon particles.
EFFECT: enabled direct analyte observation on solid phase surface as back spots; increased sensitivity of diagnosticum for performing immunochemical, gene-hybridizing and ligand-receptor studies and creating instrumentless rapid diagnosis test systems.
FIELD: chemical-pharmaceutical industry, proteins.
SUBSTANCE: invention concerns to cytokine-containing fused proteins showing the enhanced therapeutic index, and methods for enhancing the therapeutic index of these fused proteins. Fused proteins are able for binding with cytokine receptors of more one type expressed on cells and to bind with cells of more one type also. Except for, fused proteins possess a half-time value in blood stream of a patient as compared with that of corresponding natural cytokines.
EFFECT: improved and valuable properties of cytokines.
21 cl, 3 tbl, 11 ex