Method for tumour growth inhibition induction in experiment
SUBSTANCE: invention refers to medicine and may be used for tumour growth inhibition induction in experiment. For this purpose, the Pliss's lymphosarcoma cells 1 ml in the concentration of 20x106/ml proincubated for 30 min at 37°C with 100 mcl with a one-wall carbon nanotube suspension of the length of 100-200 nm functionalised by MH2-groups in the concentration of 10 mcg/ml. The tumour growth inhibition is specified as 97% for 20 days and prolonged life length is stated to increase in 1.68 times as compared to reference tumour carrier animals.
EFFECT: invention induces the tumour growth inhibition and prolongs life length of experimental animals ensured by the combined incubation of tumour cells and one-wall carbon nanotubes.
The invention relates to medicine, namely to experimental research in Oncology, and can be used to assess antitumor activity werdnig nanotubes (NT).
Carbon is the basis of biological macromolecules, which prompted researchers to develop new biocompatible materials carbon nature (fullerenes, graphenes, carbon nanotubes). Functionalization of their different chemical groups allows them to react in vivo and show various kinds of biological activity depending on their properties.
Known cytotoxic effect of nanosized particles of different nature (patent RU №2392668, publ. 20.06.2010,, bull. No. 17), in particular, single-walled carbon HT on the tumor cell culture (Amoopi, P.Drockery, U.Greiser, M.Murphy, V.Barren. Carbon nanotubes and mesenchimal stem cells: biocompatibility, proliferation and differentiation // nano-letters, 2008. V.8. No. 8. 2137-2143). Other authors report the absence of such action (III, Rahmaninov, Asselineau, Reapedgerne, Oaapn. Research proliferative activity and cell viability of fibroblasts and glioblastoma on different types of carbon nanotubes // bull. the experimental. Biol. and the honey. 2012. T. No. 2. S-231). A well-known effect of the destruction of tumor cells under combined action of carbon nanoblock, covered with gold, and various physical factors (.Loo,A.Lowery, N.Halas, J.West, R.Drezek. Immunotargeted nanoshells for integrated cancer imaging and therapy // nano-letters, 2005. V.5. No. 4, 709-710). There is information about selective absorption of different nanosized particles of tumor cells (Acheh, G.Khaled, J.Fang, H.Maeda Exploiting the enhanced permeability and retention effect for tumor targeting // Drug Discov. Today, 2006. No. 11, 812-818). A definite answer, whether single-walled carbon HT cytotoxic or antiproliferative action, the literature provides no; perhaps it depends on the length, functionalization, and other characteristics of the nanotubes. Is the development and experimental study of the effect of conjugates of HT drugs for targeted delivery to the tumor (Jinjun Shi, A.R.Votruba, O.C.Farokhzad, R.Langer. Nanotechnology in drug delivery and tissue engineering: from discovery to application // nano-letters, 2010. 10. 3223-3230).
In the above works do not consider the possibility of inhibition of tumor growth in vivo under the action of short otnoshenij carbon HT, functionalized groups, allowing them to react with protein molecules (NH2and COOH).
As a prototype we have used the work (Ashwin A. Bhride, Vyomesh Patel, Julie Gavard, et al. Targeted killing of cancer cells in vivo and in virto with EGF-directed carbon nanotube-based drug delivery // ACS NANO. 2009. V.3. No. 2. 307-316), which examined the effect of single-walled carbon HT length 50-300 (110±50) nm and a diameter of about 10 nm, functionalized cisplatin and EGF on tumor growth in vivo. The authors floor is constrained 10-day growth inhibition of transplantable tumors HN12, overexpressing EGF, after preprocessing of functionalized nanotubes and intravenous inoculation of Nude mice. However, this method requires complex design nanoconjugates and has a specific focus against EGF-expressing tumors. In addition, the complexity of the model is to use tumor, perelivayuschiesya on Nude mice, which, if you keep in mind the further stages of the study of the effects of NT in a clinical setting, they do not match.
The aim of the invention is the induction of inhibition of growth of transplantable tumors in the experiment using functionalized NH2groups of carbon nanotubes.
This objective is achieved in that white outbred rats weighing 200-250 g contained in standard vivarium conditions, under the skin of the back perejivaut 1 ml suspension of tumor cells lymphosarcoma (LSA) Plissa containing 20×106cells in 1 ml, incubated at 37°C for 30 min with 100 µl of the suspension of NT NH2or NT COOH, 10 µg/ml in 4% proxanol is chosen, preventing their aggregation, thus, for each tumor cell has 5×10-5ng HT. Control rats perform a similar perepevku LCA, incubated at 37°C for 30 min with 100 ál of 4% aqueous solution of proxanol is chosen-268, - nonionic surfactants, is what the student component of the commercial product of perftoran. Assess the dynamics of tumor growth and life expectancy of animals-carriers of tumour. In the animals studied groups show statistically significant differences on these indicators: perebivka tumors, preincubating with HT NH2contributes to the inhibition of its growth and increase in life expectancy of animals-carriers of tumour compared with control animals and rats, which transplanted tumor cells, proinsurance with HT COOH.
Thus, objective, namely the induction of inhibition of growth of transplantable tumors (LCA plisse) using carbon HT, functionalized NH2groups, seems to be reached.
The invention "Method of induction inhibition of tumor growth in the experiment is new, because it is unknown in medicine, in particular in Oncology, experimental studies to evaluate the antitumor activity of carbon NT.
The novelty of the invention lies in the fact that rats experimental groups subcutaneously in the region of the back perejivaut 1 ml suspension of tumor cells LCA Plissa containing 20×106cells in 1 ml, incubated at 37°C for 30 min with 100 µl of the suspension of NT, functionalized NH2or COOH, HT concentration is 10 μg/ml; determine the impact of the introduction of HT on growth LCA Plissa, the duration of the ity of life of rats and reveal in the control group, where the transplantable material incubated with proxanol is chosen, there is a gradual increase in tumors with subsequent necrotization, decay and death of animals-carriers of tumour after 22 days after inoculation; in the experimental group, where perepevku conducted after inactivated with HT COOH, differences from control were observed, while in the experimental group, where perepevku conducted after inactivated with HT NH2comes inhibition of tumor growth, the death of the animal occurs later (after 38 days after inoculation).
Thus, in the experiment it is shown that under the action of NT NH2is inhibition of the release of transplantable tumors, and NT COOH such activity do not show.
The invention is industrially applicable as it can be used in biomedical research while conducting experiments in the field of Oncology.
The method of induction inhibition of tumor growth in the experiment is as follows: HT, functionalityand NH2or COOH-groups before the experiment were bred 4% proxanol is chosen up to a concentration of 1 μg/ml, and to prevent aggregation was treated with ultrasound for 1 min, a frequency of 44 kHz, the amplitude of 30-50 μm; rats-males (weight 200-250 g) experimental groups subcutaneously in the back area transplanted 1 ml suspension of tumor cells LCA Square the SSA, containing 20×106cells in 1 ml, incubated at 37°C for 30 min with 100 µl of the suspension HT; control animals were injected transplantable material after incubation with proxanol is chosen; HT concentration is 10 μg/ml, i.e. for each tumor cell has 5×10-5ng HT. Assess the dynamics of growth LCA Plissa and reveal that in control rats and in animals in which the tumor transplanted after inactivated with HT COOH, there is a gradual increase in tumors with subsequent necrotization, decay and death of animals-carriers of tumour through 22-23 days after inoculation, and animals, which transplantable material was administered after inactivated with HT NH2is inhibition of tumor growth, the death of the animal occurs at a later date (after 38 days after inoculation). As can be seen from the data presented in table 1, the braking index (it) tumor growth in animals of the experimental group when perebivke LCA Plissa, incubated with HT NN2is 88,9% after 10 days, which is 97.6% 13 days and 97% after 20 days, and when perebivke LCA Plissa, incubated with HT COOH, inhibition is observed only after 10 days after inoculation, whereas it significantly less (44%), and then the tumor grows as well as in the control group.
|Groups of rats||Days after inoculation, tumor volume (cm3)|
|Control (proxanol is chosen)||0,09±0,0198||22,97±2,8||49,55±4,95|
|Experienced (NT NH2)||0,01±0,0022*||0,55±0,26*||1,42±0,62*||of 4.44±2,0*||22,3±3,38|
|% inhibition =(V K-V/V)×100%||88,9||97,6||97||-||-|
|Experienced (NT COOH)||0,05±0,009||19,23±2,3||54,83±5,5||-||-|
|% inhibition =(V K-V/V)×100%||44||16||-10||-||-|
|Note. * - statistically significant differences from control (P<0,05)|
As can be seen from the data presented in table 2, the tumor is slower than in the control, is formed in rats of the experimental group after inoculation of the cells, incubated with HT NH2while the death of rats of this group occurs at a later date. In the control group, the tumor has formed all 5 rats 10 days after inoculation, their downfall started on the 20th and ended on the 27th day. In the experimental group after inoculation of tumor cells, incubated with HT NH2after 10 days the swelling was gone in 3 rats from 5, then another 1, and 1 - never came out; the death of 4 rats came from 33 to 40 days, 1 animal lived without tumor 6 months and were killed for another reason. After inoculation of tumor cells, incubated with HT COOH, LCA Plissa develops what I similar to control.
|The impact of the introduction of tumor cells, incubated with HT NH2for 30 min at 37°C, on the death of rats-carriers of tumour|
|Groups of rats||The number of rats with tumors/number of live rats|
|Control (proxanol is chosen)||5/5||5/5||4/4||0||0||0|
|Experienced (NT NH2)||3/5||4/5||4/5||4/5||4/5||0/1|
|Experienced (NT COOH)||5/5||5/5||4/4||2/2||0||0|
As can be seen from the data presented in table 3, long is th life carriers of tumour maximum in the experimental group after inoculation of the cells, incubated with HT NH2and statistically significantly higher than that in control group than in animals after inoculation of tumor cells, incubated with HT COOH.
|The life span of rats after inoculation LCA Plissa, incubated with tumor cells 30 min 37°C|
|Groups of rats||Lifetime (days)|
|Control (proxanol is chosen)||22,6±1,54|
|Experienced (NT NH2)||38±1,0*|
|Experienced (NT COOH)||23,3±1,85|
|Note. * - statistically significant differences from control (P<0,05)|
Thus, preincubate tumor cells with HT ML causes growth inhibition LCA Plissa 97% for 20 days and the increase in life expectancy of animals-carriers of tumour 1.68 times; HT COOH show no such effect.
Technical and economic efficiency "Method of induction inhibition of tumor growth in the experiment is that preincubation NT NH2with transplantable tumor cells you which indicates the inhibition of its growth and the increase in life expectancy of animals-carriers of tumour.
The method of induction inhibition of tumor growth in the experiment, including perepevku tumor cells after incubation in vitro with single-walled carbon nanotubes, characterized in that the experimental rats subcutaneously previvous 1 ml of tumor cells LCA Plissa at a concentration of 20·106/ml, preincubating for 30 min at 37°C With 100 µl of suspended single-walled carbon nanotubes with a length of 100-200 nm, functionalized NH2groups, in a concentration of 10 μg/ml, establish the inhibition of tumor growth by 97% within 20 days and the increase in life expectancy of animals 1.68 times as compared with the control animals-carriers of tumour.
SUBSTANCE: invention relates to cosmetology, particularly a composition enriched with silver nanoparticles and a method of producing said composition. The composition is intended to replace water as the basic component for producing cosmetic products (shampoos, Balsams, masks, intimate hygiene agents, creams etc). The composition contains a dry 65% whey protein concentrate, a micellar solution of silver nanoparticles in form of an aqueous solution having concentration of 500 mg/l in amount of 0.01-0.5% and additionally water. The method of producing said composition involves heating water to temperature of 50-55°C, adding the whey protein concentrate to the heated water in portions, recirculating the obtained mixture for 15 minutes using a cam-driven pump, adding the micellar solution of silver nanoparticles to the stirred mixture and cooling the obtained mixture to 30°C.
EFFECT: invention enables to obtain cosmetic material which protects skin from inflammatory processes and ageing, controls and maintains the skin water-oil balance.
2 cl, 2 ex
FIELD: process engineering.
SUBSTANCE: invention relates to water treatment and can be used for water ozone treatment. Proposed device comprises water feed pipeline with strainer, water discharge pipeline, pipeline to feed ozone from ozone generator connected with ejector, means to discharge ozone-bearing gas, discharge pipeline, bypass pipeline with check valve, hydraulic lock, pump, filtration vessel with bed filter, drainage system level indicator, 1st, 2nd, 3rd and 4th shutoff devices, control unit connected with gages and control circuits of ozone generator, pump hydraulic lock and 1st, 2nd, 3rd and 4th shutoff devices. Note here that ozone feed pipeline is connected with ejector. Means to discharge ozone-bearing gas is composed of ozone destructor arranged atop filtration vessel and connected therewith via air shutoff valve. Flushing water discharge pipeline is connected with discharge from filtration vessel via hydraulic lock. 3rd shutoff valve is arranged in water feed line downstream of strainer to connect it with ejector and bypass line with check valve connected via 2nd shutoff valve and pump with drainage system outlet and, via 4th shutoff valve with water discharge line. 1st shutoff valve arranged in branch pipe of water feed line downstream of said strainer connects the latter with drainage system. Bed filter is composed of catalyst consisting of pelletised nano-structured based of natural green earth, thermally expanded graphite without extra binder. Sprayers are arranged at filtration vessel top part and connected with shutoff valve and pump and are automatically controlled along with ozone generator by control unit. Note here that sprayer nozzles are located: One at the center while others are arranged in concentric circles located in one plane, their number being defined by calculation.
EFFECT: higher quality of cleaning and efficient use of ozone.
SUBSTANCE: polarising film is a film of iodised polyvinyl alcohol with a mixture of carbon nanotubes and carbon nanofibres deposited on two sides by laser deposition using p-polarised radiation of a CO2 laser at wavelength 10.6 mcm, as well as orientation the deposited nanostructures in an electric field with strength of 50-200 V/m.
EFFECT: cheaper material for making polarising film, preserving transmission in the visible spectrum range and higher surface mechanical strength.
1 dwg, 1 tbl
SUBSTANCE: apparatus has a microscope attachment with an infinite optical system mounted on a support, an image recording unit, an illumination system and an image processing system, wherein the source for the illumination system is in form of a narrow-band light-emitting diode module; further, between the microscope attachment with an infinite optical system on the side of the optical output and the image recording unit there is a spectral filtration system, and between the illumination system and the image recording unit there is a signal time delay unit, the inputs of which are connected to outputs of the illumination system and the image processing system, and the outputs are connected to inputs of the illumination system, the image processing system and the image recording unit, wherein the spectral filtration system is provided with a set of variable band-pass optical filters with stepped variation of the transmission coefficient.
EFFECT: high sensitivity and information content of imaging.
3 cl, 4 dwg
FIELD: process engineering.
SUBSTANCE: invention relates to welding. Proposed method comprises producing briquette-shape filling material. Briquettes consist of the mix of powders wherein nano-sized hardening particles make 0.1-0.4% of surfacing metal amount. Binding component represents 4-5%-water solution of carboxymethyl cellulose. Then, briquettes are dried to complete hardening. Briquette is placed onto facing surface. Then coating bead is built up by complete dissolution of filler briquette and, partially, of article metal with penetration depth of 0.1-0.5 mm. Every other briquette is placed on facing surface after dissolution of previous briquette. Now, bead after bead is built up to make two and more layers of coating.
EFFECT: higher efficiency owing to continuous surfacing without cooling.
3 cl, 1 tbl, 1 ex
SUBSTANCE: invention refers to a contrast agent for magnetic resonant and X-ray diagnostic agent for magnetic resonant tomography (MRT) and X-ray computed tomography (XRCT). The above agent contains complex ferric oxide in the concentration of 600 mg/ml, citric acid 2.4 mg/l for stabilising the particle size of complex ferric oxide within the range of 5-10 nm, sodium citrate 140 mg/ml for stabilising the contrast agent structure, polyethylene glycol in the concentration of 160 g/l and water for injections 460 mg/ml. The invention also refers to a method for preparing the above contrast agent wherein ferric salts are mixed with ammonium hydrate and citric acid added. That is followed by introducing polyethylene glycol with added water-dissolved sodium citrate while stirring thoroughly; non-dissolved sodium citrate is cooled and filtered.
EFFECT: group of the declared inventions provides more effective diagnostic study ensured by visualising with respect to relaxation time, as well as provides the lower concentration of the administered contrast agent.
3 cl, 1 dwg, 3 ex
SUBSTANCE: invention refers to medicine, namely otolaryngology, and may be used for treating acute-on-chronic rhinosinusitis. For this purpose, iron-containing ferrihydride nanoparticles prepared by the culture of the bacteria Klebsiella oxytoca recovered from sapropel of Borovoye Lake of the Krasnoyarsk Territory, mixed with a water-dissolved antibiotic, applied on the nasal mucosa and exposed to a magnetic field for 20 minutes.
EFFECT: method enables providing the higher clinical effectiveness ensured by the targeted antibiotic delivery into the tissues with the intensive and prolonged therapeutic action thereof.
2 cl, 2 dwg, 1 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to medicine, pharmaceutics and nanotechnology, more specifically to a pharmaceutical composition of fluconazole that is an antifungal agent from the group of triazole prepared by chemical synthesis, and a method for preparing it. The presented pharmaceutical composition possessing antifungal activity containing fluconazole coating nanotubes of the various external tube diameter - 60-160 nm, the internal diameter - 10-60 nm and the length - 100-5000 nm in the following relations, wt %: fluconazole - 50-60; alumosilicate nanotubes - 40-50. The method for preparing the pharmaceutical composion consists in the fact that fluconazole is mixed with the alumosilicate nanotubes with the aqueous ethanol environment, and mixing the prepared suspension and evaporating ethanol.
EFFECT: using fluconazole applied on the nanotubes enables developing new ointments and gels for treating fungal diseases with the reduced amount of fluconazole.
2 cl, 2 dwg, 1 tbl, 3 ex
FIELD: radio engineering, communication.
SUBSTANCE: in a printed-circuit board for spacecraft on-board radio electronic equipment, which comprises a dielectric substrate and an electric circuit formed thereon, the substrate is made from dielectric material with volume resistivity selected based on the condition 1011 Ohm·cm≥ρv≥105 Rmax • d, where ρv is the volume resistivity of the dielectric material of the substrate of the printed-circuit board, Ohm·cm, Rmax is the maximum resistance of the resistor included in the electric circuit on the printed-circuit board, Ohm, d is the thickness of one dielectric layer of the printed-circuit board. The dielectric material used is a composite dielectric material which contains a conducting additive selected from: fine acetylene soot in amount of 5-6.5% of the weight of binder, molecular fullerene C60 or C70 in amount of 1-2% of the weight of binder, carbon nanotubes in amount of 0.3-0.9% of the weight of binder.
EFFECT: making a printed-circuit board for spacecraft on-board radio-electronic equipment which is resistant to electrostatic charging effects.
SUBSTANCE: according to the invention, heterojunction structure consists of semiconductor layers of n and p type of conductivity, which are located in series on a substrate of n type, homogeneous to semiconductor layers of n type, which are adjacent to it, and having ohmic contact to rear side. With that, on surface of n layer on the side of n-p heteroboundary there located is a massif of nanostructured objects; p layer is made in the form of a diamond film, the thickness of which does not exceed diffusion length of electrons, and concentration of acceptors in it is in the range of 1020-1024 m-3.
EFFECT: possibility of considerable increase of operating currents of a field radiating cathode, or field-emission diodes, increase of stability of devices to degradation and increase of their life cycle.
6 cl, 1 ex, 6 dwg
SUBSTANCE: invention proposes humanised anti-NKG2A antibody obtained from murine antibody Z270, which is characterised through amino-acid sequences of variable domains, and method of its obtainment. Besides, a pharmaceutical composition is described, which contains an antibody according to the invention, a treatment method and application of the antibody in production of a medicine to be injected into a patient who is a human being suffering the disorder chosen from cancer, virus disease, inflammatory disorder and autoimmune disorder.
EFFECT: invention can be further used in therapy.
14 cl, 20 dwg, 2 tbl, 16 ex
SUBSTANCE: nucleic acid molecule codes a polypeptide consisting of two residues of methionine as the first and the second N-end amino-acid residues connected through a peptide link to a mature eucariotic histone. Polypeptide is obtained by cultivation of a host cell transformed by an expression vector including the above molecule of nucleic acid. Polypeptide is used as part of pharmaceutical composition for therapy of cancer, bacterial, virus or fusarium infections. Besides, polypeptide is used as part of composition for diagnostics of a patient in relation to response to pharmaceutical composition containing the above polypeptide, or in relation to curability using it.
EFFECT: invention allows improving efficiency of recombinant expression and simplifying determination of the above polypeptide in presence of endogenic histones at preservation of biologic activity of mature eucariotic histone.
17 cl, 3 dwg, 6 tbl, 7 ex
SUBSTANCE: proposed peptides represent T-cell epitopes of an endothelial marker of a tumour (TEM8), which are able to induce cytotoxic T-lymphocytes (CTL) in presence of antigen-presenting cells or exosome, which carry or contain HLA-A*0201. A pharmaceutical composition is proposed for elimination of cells expressing TEM8, extracted exosome and antigen-presenting cell, which carry a complex containing a peptide as per invention with HLA-A*0201 molecule. Methods for induction of an antigen-presenting cell, which can induce CTL that destroy the cells expressing TEM8, as well as cytotoxic cells induction methods have been considered.
EFFECT: invention can be further used for cancer therapy.
10 cl, 5 dwg, 1 tbl
SUBSTANCE: invention relates to anti-tumour purine derivatives of formula (A) and salts thereof, as well as pharmaceutical compositions based thereon, a method for production thereof where W is an alkyl-substituted amine, a pyrrolidine, piperidine, morpholine or piperazine residue, optionally substituted with C1-C6 alkyl or hydroxy; Y is H or a saccharide residue, Z is H; Q is an optionally substituted quinoline residue. The disclosed method involves reacting a corresponding purine protected at the 9th position with corresponding precursors of groups W and Q.
EFFECT: novel compounds with low toxicity, a wide anticancer range, high anticancer activity, high stability, suitable for producing anti-tumour drugs.
12 cl, 3 tbl, 31 ex
SUBSTANCE: invention relates to imidazopyridines of formula I and to a pharmaceutically acceptable salt thereof, where Z1 is CR1; R1 is H; R1' is H; Z2 is CR2; Z3 is CR3; R2 and R3 are H; R4 is H; Y is W-C(O)-; W is or ; R5 is H; X1 is selected from R11' and -OR11'; R11 is independently H or C1-C6 alkyl, optionally substituted -(CR19R20)nCOR16; X4 is ; R6 is halogen, carbocyclyl or -(CR19R20)n-SR16, wherein said carbocyclyl is cyclopropyl or cyclobutyl; R6' is halogen; p equals 1, 2; n equals 0, 1; each R16 is independently H or C1-C6 alkyl; R19 and R20 are independently selected from H or C1-C6 alkyl. The invention also relates to a pharmaceutical composition based on the compound of formula I and a method of inhibiting anomalous cell growth or treating a hyperproliferative disorder, based on use of the compound of formula I.
EFFECT: obtaining novel imidazopyridine derivatives of formula I, which are useful in treating hyperproliferative disorders.
7 cl, 14 ex
SUBSTANCE: invention relates to novel imidazo[4,5-b]pyridine derivatives of formula I as well as salts, hydrates and stereoisomers thereof, where B-R2 and R4-A-R3 are selected from groups indicated in claim 1, R1 denotes a C1-C6 alkyl group, optionally branched, R5 denotes a hydrogen atom. The invention also relates to a compound of formula II 3-substituted 7-chloro-5-iodo-imidazo[4,5b]pyridine, a method of producing imidazo[4,5-b]pyridine derivatives of formula I, a pharmaceutical composition based on the compound of formula I and use thereof.
EFFECT: obtaining novel derivatives having CDK inhibiting properties.
10 cl, 17 dwg, 6 tbl, 6 ex
SUBSTANCE: invention relates to novel phenylaminopyrimidine compounds of formula I, which are JAK kinase inhibitors. In particular, these compounds selectively act on JAK2 kinase. The compounds can be used to treat diseases such as immunological and inflammatory diseases; hyperproliferative diseases, myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases. In the compound of formula I , Q and Z are independently selected from N and CR1; R1 is independently selected from hydrogen, halogen, R2, OR2, OH, R4, OR4, CN, CF3, (CH2)nN(R2)2, where n equals 1,2 or 3, NO2, R2R4, NR2SO2R3, COR4, NR2COR3, CO2H, CO2R2, NR2COR4, R2CN, R2OH, R2OR3 and OR5R4; or two substitutes R1 together with carbon atoms with which they are bonded form an unsaturated 5- or 6-member heterocyclic ring containing 1-4 N atoms; R2 is C1-4alkyl; R4 is R2, C2-4alkenyl or phenyl; R4 is NH2, NHR2, N(R1)2, substituted or unsubstituted morpholine, CH2morpholine, substituted or unsubstituted thiomorpholine, substituted or unsubstituted thiomorpholino-1-oxide, substituted or unsubstituted thiomorpholino-1,1-dioxide, substituted or unsubstituted piperazinyl, substituted or unsubstituted piperidinyl, substituted or unsubstituted pyridinyl, substituted or unsubstituted pyrrolidinyl, substituted or unsubstituted pyrrolyl, substituted or unsubstituted oxazolyl, substituted or unsubstituted imidazolyl, substituted or tetrahydrofuranyl unsubstituted and substituted or unsubstituted tetrahydropyranyl; R5 is C2-4alkylene; R6-R9 are independently selected from H, RXCN, halogen, substituted or unsubstituted C1-4alkyl, OR1, CO2R1, N(R1)2, NO2 and CON(R1)2, wherein at least one of R6-R9 is RXCN; the rest of the values of the radicals are given in the claim.
EFFECT: high efficiency of treatment.
29 cl, 7 dwg, 2 tbl, 93 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention discloses an antibody (versions) possessing immunologic responsiveness to incomplete polypeptide CAPRIN-1 (the amino acid sequences are presented in the description), and a pharmaceutical composition (versions) for treating and/or preventing a malignant growth, particularly breast cancer, cerebral tumour, leukaemia, lymphoma, lung cancer, or colon cancer. As an active ingredient, the composition contains an antibody or a fragment thereof possessing immunologic responsiveness to the protein CAPRIN-1 or a fragment thereof containing 7 more or more sequential amino acids. The antibody can be monoclonal, polyclonal, human, humanised, chimeric, single-chain or bispecific antibody. What is disclosed is a method of treating and/or preventing a malignant growth with using the antibody or the immunologically active fragment thereof.
EFFECT: antibodies according to the invention show the pronounced antitumour effect particularled ensured by their ability to damage the tumour cells expressing CAPRIN-1, and are attractive for treating the oncological diseases.
22 cl, 10 dwg, 7 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: group of inventions refers to medicine, more specifically to oncology and concerns using neranitib and capecitabine in a combination for treating a new growth (breast cancer); wherein neranitib is administered in the approximate amount of 240 mg a day, and capecitabine is administered in the approximate amount of 1500 mg a day. There are also presented: a pharmaceutical composition, a kit and a method of treating breast cancer which involves administering neranitib and capecitabine.
EFFECT: group of inventions provides a synergetic effect of administering neranitib in the approximate amount of 240 mg a day and capecitabine in the approximate amount of 1500 mg a day in a combination for treating new growths.
19 cl, 2 tbl, 4 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutics and medicine and concerns new radiopharmaceuticals containing a complex comprising a sulphonamide fragment able to bind to an active catalytic site CA-IX, and a radionuclide for radiovisualisation and/or radiotherapy, which can be used for diagnostic visualisation and therapeutic treatment of the diseases characterised by CA-IX overproduction.
EFFECT: preparing the new radiopharmaceuticals.
50 cl, 5 tbl, 47 ex
SUBSTANCE: invention relates to carbon materials. Described is a method of producing porous carbon material from silicon-containing plant material. The method involves carbonising plant material by temperature treatment, treating with acid or alkali, followed by activation. The porous carbon material has nitrogen BET specific surface area of at least 130 m2/g, mesopore and micropore volume of at least 0.1 cm3/g, measured by BJH method and MP method and containing more mesopores smaller than 20 nm than mesopores having size of at least 20 nm. The obtained material is used, for example, as an adsorbent, an adsorbent for oral administration, a medical adsorbent, a creatinine adsorbent, a cap for blood purification columns, a water treatment adsorbent, a mask, an adsorbent sheet, a medicine carrier and a carbon-polymer complex.
EFFECT: invention enables to obtain material with a wide range of applications.
10 cl, 10 dwg, 12 tbl, 8 ex