Osteotropic radiopharmaceuticals for pet imaging

FIELD: medicine.

SUBSTANCE: invention relates to the field of nuclear medicine, namely to radiopharmaceuticals (RF) for metastatic bone lesions imaging using the positron emission tomography (PET) techniques and radiation therapy planning. This goal is achieved by application of a composition representing a solution containing gallium-68 in the form of a complex with oxa-bis (ethylene-nitrile)tetrametylene-phosphonic acid and sodium chloride, sodium hydroxide and a phosphate buffer containing sodium phosphate and sodium hydrogen phosphate, as the preparation for PET imaging of metastatic bone lesions and radiation therapy planning. Preparation is obtained from a lyophilized composition at the room temperature during 1-2 minutes, radiochemical purity of the preparation is more than 90%, pH range is from 4.5 to 8.0, maximum accumulation of drug in a pathological bone shall be reached 1.5 hours after introduction, and is 40-45% of the introduced activity, differential callus/blood accumulation factor is more than 10, accumulation of the drug in blood is less than 0.30%/year.

EFFECT: invention expands the number of nuclear medicine devices, particularly for metastatic bone lesions imaging using the positron emission tomography (PET) techniques and radiation therapy planning.

3 dwg, 4 ex, 1 tbl

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to synthesis of N-mono fluoroalkyl tropanes with application of fluoroalkyliodides, as well as to application of such method for obtaining non-radioactive tropane intermediate compound of formula and its further conversion into 123I-labelled radiopharmaceutical substance DaTSCAN (123I-ioflupane). Method consists in alkylation in presence of base of formula compound with alkylating agent of formula F-(CH2)mX, where m equals 2, 3 or 4, X represents I. .

EFFECT: obtaining non-radioactive tropane intermediate compound of formula and its further conversion into 123I-labelled radiopharmaceutical substance DaTSCAN (123I-ioflupane).

10 cl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a radioindicator for PET, which possesses improved properties with respect to visualisation of peripheral benzodiazepine receptors (PBR) in comparison with known radioindicators for PET. In accordance with the claimed invention also claimed are: a predecessor compound for obtaining the radioindicator for PET in accordance with the invention and methods of obtaining the said predecessor compound and the said radioindicator for PET.

EFFECT: claimed is a radiopharmaceutical composition, containing the radioindicator for PET in accordance with the invention and methods for the application of the radioindicator for PET and the radiopharmaceutical composition .

23 cl, 8 dwg, 12 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to chemotherapy of cancer and represents a composition for hepatic cancer in individuals and containing a complex of formula [M(RCS3)2(RCS2)], wherein M represents 188Re having an activity of more than 3.7 GBq and a lipophilic organic phase emulsified with a water phase; as well as a method for preparing the above composition.

EFFECT: invention provides higher stability and efficacy of the composition for treating hepatic cancer in the individuals.

17 cl, 1 dwg, 9 ex

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining biocompatible highly disperse polylactide particles for in situ manufacturing of diagnostic means for positron-emission tomography by combination of said particles with solution, containing cations of gallium 68 (III). Claimed method includes combination of solution of bidentate aromatic ligand, namely quercetin, quinalizarin, alizarin or 8-hydroxyquinoline in polar solvent with solution, containing lactic acid copolymers in low-polar solvent and intensive mixing of obtained mixture with obtaining highly homogenous mixture. After that, at least three volumes of water solution of polyvinyl alcohol with molecular weight 9.080 kDa are added and intensively mixed with obtaining highly homogenous mixture. Obtained mixture is evaporated with obtaining suspension, which is filtered by filter with pore size less than 30 mcm with obtaining filtrate, with further addition of lyoprotector, freezing and lyophilisation. Invention also relates to biocompatible highly disperse particles for manufacturing radiopharmaceutical preparation for positron-emission tomography, their application for carrying out positron-emission tomography and to diagnostic composition, containing effective amount of gallium-68 (III), bound with said particles.

EFFECT: obtaining biocompatible highly dispersive polylactide particles for in situ manufacturing of diagnostic means for positron-emission tomography.

33 cl, 8 tbl, 6 dwg, 2 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to a kit for targeted medical imaging and/or clinical medicine, and to a method for using the kit. The declared kit comprises a pre-guide probe and an effector probe, wherein the pre-guide probe comprises a primary guide fragment and a first bio-orthogonal reactive group, and wherein the effector probe comprises an effector element, such as a label or a pharmaceutically active compound, and a second bio-orthogonal reactive group. Any of the first and second bio-orthogonal reactive groups represents dienophile in the form of stressed 8-merous cycle (cyclooctene or cyclooctine), while diene represents electron-deficient tetrazine or other applicable diene. A method for using the kit involves administering the pre-guide probe into the individual and enabling the probe circulating in the individual system for a period of time effective to achieve binding of the primary guide fragment with the primary target with the unbounded substance discharge from the body, with the effector probe to be inserted.

EFFECT: invention involves using the [4+2] Diels-Alder retrochemical reaction with electron reuptake to bind the pre-guide probe and the effector probe that enables fast in vivo reaction behaviour.

12 cl, 12 dwg, 1 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound presented by formula OR or its pharmaceutically acceptable salt or solvate. The radical values are as follows: Rt - H, C1-C8 alkyl group, ammonium ion, alkali or alkali-earth ion; R84 - substituted C1-8 alkyl; R - C1-8 hydroxyalkyl, C1-8 alkoxyalkyl, C1-8 aminoalkyl, (CH2)8(NHC(S)NH)Ph(SO2NH2), (CH2)dPh(SO2NH2), (CH2)5C(O)NH-(1-acetylpyrrolidin-2-yl)boric acid, (1-acetylpyrrolidin-2-yl)boric acid, (CH2)4CH(NH2)CO2H, (CH2)3CH(NH2)CO2H, (CH2)2CH(NH2)CO2H, -(CH2)d-R80, -C(O)(CH2)d-R80, or amino acid radical; R80 is carboxylate, C6-10 aryl, 3-6-merous heterocyclyl, amino acid; d represents an integer within 0 to 12 inclusively; and R82, R83, R85 and R86 are hydrogen, substituted or unsubstituted alkyl, ether, ester, CH2CH2OCH2CH3, CH2CH(OCH3)2, -(CH2)d-R80, or (CH2)dR87; wherein R87 represents phosphonate or phosphorinate. What is also presented is a complex containing the above compound and a radionuclide.

EFFECT: compound can be used as diagnostic or therapeutic agents.

11 cl, 13 dwg, 10 tbl, 23 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula I , II or IV , wherein the radical values W, V, Ra, Rb, X, L, Rt, A are presented in the patent claim.

EFFECT: declared compounds identify and bind the CA-IX protein; they can contain a radioactive element for radionuclide imaging or therapeutic application.

27 cl, 1 tbl, 5 dwg, 25 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new radiopharmaceutical compounds of structural formula

.

In formula I, R means H or a (C1-C8)alkyl group; W means a bond, -CH(NH2)-, -C(O)-NH-CH(COOH)-, -O-(CH2)n-O-(CH2)n- or -(CH2)nO(CH2)nO(CH2)n; Z means -NHC(O)-, -NH-C(O)-CH(NH2)- or -C(O)-NH-CH(COOH)-; e is an integer from 1 to 4; f is an integer from 0 to 10; g is an integer from 0 to 10; n is an integer from 0 to 2; the radical NRaRb values are presented in the patent claim.

EFFECT: invention refers to the radionuclide complex containing a radioactive metal and the above compounds, to a pharmaceutical compound for visualising and to a method for visualising any patient's region, e.g. a tissue specified in the spleen tissue, kidney tissue or PSMA-expressing tumour tissue.

21 cl, 6 dwg, 1 tbl, 18 ex

FIELD: medicine.

SUBSTANCE: 90-minute kinetics of an intravenously administered 99mTc hepatobiliary tracer is studied. The maximum activity time of the tracer in the common bile duct is recorded. Choleretic breakfast is introduced 45 minutes after the beginning of the study. An Oddi's sphincter incompetence index is calculated by formula: N=x/y, wherein N is the Oddi's sphincter incompetence index, x is time of introducing choleretic breakfast, minutes, y is the tracer maximum activity time in the common bile duct from the beginning of the study, minutes. If N is more than 1 unit, the Oddi's sphincter incompetence is diagnosed.

EFFECT: higher sensitivity, accuracy and facilitation of the technique applicable in patients with postcholecystectomy syndrome.

3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel in vivo visualising agents of formula I, where R1stands for C1-3alkyl, C1-3fluorinealkyl; R2 stands for H, OH, halogeno, C1-3alkyl, C1-3alkoxy, C1-3fluoroalkyl, C1-3fluoroalkoxy; R3 and R4 independently stand for C1-3alkyl, C7-C10aralkyl or R3 and R4 together with nitrogen atom, to which they are bound, form nitrogen-containing C4-6aliphatic ring; Y1 stands for CH2; Y2 stands for CH2, CH2-CH2, CH(CH3)-CH2 or CH2-CH2-CH2; and where formula I, as it is determined, contains atom, which represents radioactive isotope, suitable for visualisation in vivo, selected from 11C, 18F, 77Br, 123I, 124I and 131I. Claimed compounds bind with PBR with high affinity, have good absorption in brain after introduction. Described is method of obtaining in vivo visualising agent and set for claimed method realisation.

EFFECT: radio-pharmaceutical composition, which contains in vivo visualising agent, is described.

21 cl, 13 dwg, 18 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to biochemistry, particularly to a recovered monoclonal anti-LOXL2 antibody or its antigen-binding fragment, as well as conjugates containing them. What is disclosed is a pharmaceutical composition for treating a disease related to angiogenesis, fibrosis, tumour or metastases, containing the above recovered monoclonal anti-LOXL2 antibody or its antigen-binding fragment in an effective amount. The invention also refers to a method for determining and/or measuring LOXL2 in a biological sample, to a method for inhibiting LOXL2 activity, to a method for reducing growth of LOXL2-expressing tumour in an individual in need thereof, to a method for inhibiting angiogenesis in the individual in need thereof, to a method for suppressing a fibrous disease in the individual in need thereof, as well as to a method for monitoring an individual's response to an anti-LOXL2 therapy with using the above antibody or its antigen-binding fragment and the above conjugate.

EFFECT: invention enables treating the LOXL2-related diseases effectively.

28 cl, 6 dwg, 6 tbl, 9 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine and can be used for detection of urease-producing microorganisms, in particular Helicobacter pylori. For this purpose express-analysis is carried out on diagnostic discs to determine urease activity of samples. Discs are made from filter paper, on which urea, acid-base indicator, muromidase and conditioning substances are preliminarily applied. In case if urease activity is present in sample colouration of disc takes place.

EFFECT: invention provides increased sensitivity of method of Helicobacter pylori diagnostics.

3 ex

FIELD: medicine.

SUBSTANCE: diagnostic technique for initial dental caries consists in applying 1% Rodamin C fluorescent dye on a segment of the changed dental tissues after tartar removal, and fixing the dye for 1-3 min, rubbing the dye simultaneously with a microapplicator; the excessive dye is washed off with water; the moisture is removed; the dye is developed by means of a dental polymerisation lamp, and the presence of red colour visualised through an orange ophthalmic filter shows initial caries.

EFFECT: using the technique enables the reliable detection of initial caries in a relatively short time without the need of using special instruments.

2 ex, 4 dwg

FIELD: medicine.

SUBSTANCE: method is used to treat a retinal hole with the use of an intravitreal dye. That is ensured by performing a microinvasive vitrectomy. A posterior hyaloid membrane (PHM) is isolated and excised. An irrigation fluid is shut off from the vitreal cavity. A silicone tipped cannula is used to drop a perfluorogranic compound (PFOC) directly on the through macular retinal hole. A PFOC drop diameter makes 1.5-2.0 diameters of the macular hole. Further, an internal limiting membrane (ILM) is coloured with the irrigation fluid shut off. After the membrane is coloured, the ILM is exfoliated by performing a maculorhexis. The PFOC drop is removed. The retina is plugged completely with gas air mixture.

EFFECT: conservation of neuroepithelium and retinal pigment epithelium cells within the macular hole ensured by such relation of the PFOC and macular hole diameters that in turn enables fixing the PFOC within the macular hole reliably.

5 cl, 2 ex

FIELD: chemistry.

SUBSTANCE: claimed invention relates to a method of obtaining a chelate compound of metal or its salt, used as a diagnostic reagent. The method includes the following stages: a) contact of a liquid composition, containing a metal ion, with a cation-exchange solid carrier, modified by functional groups of iminodiacetic acid or thiourea, to obtain a metal-chelate carrier; and b) contact of the said metal-chelate carrier with a liquid composition, containing an aminocarboxylic chelating reagent or its salt. The said metal in the chelate compound or ion component represents a lanthanide. Also claimed is a method of obtaining gadobenate dimeglumine.

EFFECT: method makes it possible to selectively obtain the chelate metal compound with the high output in the form, which in fact does not contain by-products or a material that has not reacted.

11 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new radiopharmaceutical compounds of structural formula

.

In formula I, R means H or a (C1-C8)alkyl group; W means a bond, -CH(NH2)-, -C(O)-NH-CH(COOH)-, -O-(CH2)n-O-(CH2)n- or -(CH2)nO(CH2)nO(CH2)n; Z means -NHC(O)-, -NH-C(O)-CH(NH2)- or -C(O)-NH-CH(COOH)-; e is an integer from 1 to 4; f is an integer from 0 to 10; g is an integer from 0 to 10; n is an integer from 0 to 2; the radical NRaRb values are presented in the patent claim.

EFFECT: invention refers to the radionuclide complex containing a radioactive metal and the above compounds, to a pharmaceutical compound for visualising and to a method for visualising any patient's region, e.g. a tissue specified in the spleen tissue, kidney tissue or PSMA-expressing tumour tissue.

21 cl, 6 dwg, 1 tbl, 18 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a diagnostic and therapeutic agent which is a bombesin analogue peptide antagonist conjugate having the general formula (I), [A-(B)n]x-C, wherein A represents a metal chelator containing at least one radionuclide metal, B represents a spacer bound to N terminal C, or a covalent bond, and C represents a bombasin analogue peptide antagonist, wherein additionally x represents an integer 1 to 3, and n represents an integer 1 to 6.

EFFECT: preparing the therapeutic agent representing the bombesin analogue peptide antagonist conjugate.

17 cl, 12 dwg, 1 tbl, 13 ex

FIELD: medicine.

SUBSTANCE: invention refers to a visualising agent for visualisation of cell oxidative stress in vivo and a precursor compound for a synthesis of the visualising agent. The agent contains a tagged cystine compound having a structure I: wherein one of R and R' contains a tag specified in a fluorescent tag representing Bodipy, or a radioactive tracer specified in 11C, 13N, 15O, 17F, 18F, 75Br, 76Br, 124I, 123I, 131I and 77Br, and the other of R and R' represents hydrogen. Also, the invention refers to a method for visualising a biological sample having a cystine/glutamate transporter with the method involving administering the above visualising agent into the above biological sample through the cystine/glutamate transporter.

EFFECT: invention provides the method for detecting oxidative stress in vivo in apoptotic cells by administering the visualising agent in a cystine/glutamate cell antiporter.

14 cl, 10 dwg, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a solid pharmaceutical product for oral administration which contains a photosensitiser representing a compound of general formula I:

wherein R1 represents a substituted or unsubstituted unbranched, branched or cyclic alkyl group, and each R2 independently represents a hydrogen atom or optionally a substituted alkyl group or its pharmaceutically acceptable salt, and at least one pharmaceutically acceptable carrier or excipient. The above pharmaceutical product is presented in the form of a tablet, a pill or a capsule having an enteric and gastroresistant coating, or in the form of the tablet or the capsule containing a number of balls, drops, granules or mini-pills with an enteric and gastroresistant coating. The above coating disintegrates in the lower gastrointestinal tract. The invention also refers to using the above photosensitiser in preparing the solid pharmaceutical product applicable in photodynamic treatment or diagnostics of a cancer condition in the lower gastrointestinal tract. What is also described is a photodynamic method of treating or diagnosing the cancer condition in the lower gastrointestinal tract by administering the solid pharmaceutical product containing the photosensitiser.

EFFECT: invention provides photosensitiser delivery to the lower gastrointestinal tract, and homogenous distribution of the photosensitiser in the target region, thereby improving the response to photodynamic treatment or diagnostics.

20 cl, 2 dwg, 2 tbl, 54 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to RGD-containing cyclic peptidomimetics, conjugates of the said peptidomimetics and a functional group, selected from fluorescent probes, photosensitisers, chelating agents or cytotoxic agents; and to pharmaceutical compositions, which contain the said conjugates.

EFFECT: conjugates by the invention are suitable both for diagnostic purposes and for treatment of different diseases, disorders and states.

26 cl, 9 dwg, 10 tbl, 13 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry, namely represents composition, which contains mixture of particles of hydrophobic silicon dioxide aerogel, which have specific area of surface per weight unit (Sw) in range from 500 to 1500 m2/g and size, expressed in form of volume mean diameter (D[0.5]), in range from 1 to 1500 mcm, and at least one first linear silicone oil, which has viscosity higher than 50 mm2/s, and at least second and third linear silicone oils, and each of them has viscosity lower than or equal 50 mm2/s.

EFFECT: mixture of particles of silicon dioxide aerogel and linear oils provides possibility of obtaining compositions, which provide comfort and smoothness of skin after application and have dullness and "soft focus"-adding properties.

23 cl, 8 ex

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