Antineoplastic agents (A61P35)

A   Human necessities(312083)
A61P35                 Antineoplastic agents(3496)
A61P35/02 - Specific for leukemia(103)
A61P35/04 - Specific for metastasis(103)
2-aminopyrasine derivatives as csf-1r kinase inhibitors // 2642777
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group; R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl; n is 1; X is NH; V is -N=, W is -C(Z)=; Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl; ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group; [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3; x is 0 or 1; Alk1 is an unsubstituted C1-3 alkylene group; X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3; R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring; and R17 represents a hydrogen atom; where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring; R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group; ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or prevention of diseases or disorders mediated by CSF-1R kinase, as well as application of the said compounds for preparation of a medicament useful for treatment of such diseases.EFFECT: increased application efficiency.18 cl, 59 ex
Packaged product of solid preparation containing 5-hydroxy-1h-imidazole-4-carboxamide, or its salt, or its hydrate // 2642670
FIELD: medicine.SUBSTANCE: invention relates to a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or its salt, or its hydrate and a medium regulating agent, as well as a method for solid preparation stabilizing. The packaged product of the present invention is characterized by the colour differences of the solid preparation being no more than 3, when evaluating the solid preparation surface before and after storage for 3 months under conditions of 40°C and relative humidity of 75%, or for four weeks under conditions of 60°C.EFFECT: invention provides a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or its salt, or its hydrate, with excellent stability of solid preparation during storage.6 cl, 1 tbl, 15 ex

Cancer treatment using targeted antibodies in vivo // 2642305
FIELD: biotechnology.SUBSTANCE: antibody binding to claudine 6 (CLDN6) and inhibiting tumor growth in vivo is claimed. The antibody can be used as part of a pharmaceutical composition, in a method for treatment of tumor related to cells expressing CLDN6. The invention also relates to hybridomas producing antibodies to CLDN6 deposited under the accession numbers DSM ACC3059 (GT512muMAB 36A), DSM ACC3058 (GT512muMAB 27A), DSM ACC3057 (GT512muMAB 5F2D2).EFFECT: invention effectively inhibits the growth of CLDN6-positive germ cell tumors, improves survival and prolongs life of patients with tumors.17 cl, 18 dwg, 5 ex

Immunotherapeutic compositions on the basis of yeast-muc1 and methods of their use // 2642300
FIELD: biotechnology.SUBSTANCE: fusion protein is produced which contains the MUC1 antigen having an amino acid sequence that is at least 85% identical to the sequence of SEQ ID NO: 25 or at least 95% identical to the positions 92-566 of the sequence of SEQ ID NO: 25, and where MUC1 antigen contains 2, 3, 4, 5, 6, 7, 8, 9, 10 or 11 of the following amino acids L184, Y232, L233, V240, V241, L242, Y483, V497, L335, F536 and Y551.EFFECT: invention allows to effectively treat Mucin-1-expressing carcinomas, and also to prevent their metastatic progression.14 cl, 3 dwg, 5 tbl, 10 ex

P53 peptidomimetic macrocycles // 2642299
FIELD: biotechnology.SUBSTANCE: stable cross-linked p53 peptidomimetic macrocycle, a method for its preparation and its use are proposed. The p53 peptidomimetic macrocycle has a structure represented in the formula, and interferes with binding of p53 to MDM2 and/or p53 to MDMX. The P53 peptidomimetic macrocycle can be used to prepare pharmaceutical compositions for treatment of cancer characterized by undesirably low or low p53 activity and/or for the treatment of cancer characterized by undesirably high levels of MDM2 or MDMX activity.EFFECT: proposed cross-linked p53 macrocycle has cell permeability that is at least twice as high as that of the corresponding macrocycle without cross-links.50 cl, 7 dwg, 9 tbl, 22 ex

Hpv chimeric particle // 2642287
FIELD: biotechnology.SUBSTANCE: chimeric virus-like particle (VLP) of human papilloma virus (HPV), and method for its production and extraction, methods for prevention or treatment of HPV infection or cervical cancer, and for induction of an immune response in the patient, including the administration of proposed HPV VLP, as well as the application of the proposed HPV VLP in these methods and in production of pharmaceuticals to implement these methods, are proposed. The proposed chimeric HPV VLPS has a diameter of about 30 nm and contains a chimeric polypeptide HPV 16 L1/L2, which consists of a polypeptide HPV 16 L1, in which the peptide HPV 16 L2 from the amino acid residue 414 is inserted. The peptide contains from 13 to 26 amino acids. The amino acids of the inserted HPV 16 L2 peptide replace the corresponding amino acids of the HPV 16 L1 polypeptide. A method is also provided for the production of said HPV VLP in a plant in which successful assembly of small chimeric HPV VLPs, having a diameter of 30 nm, takes place.EFFECT: proposed group of inventions can be used in medicine for the prevention or treatment of HPV infection or in antitumor therapy for cervical cancer.28 cl, 32 dwg, 11 tbl, 3 ex
Application of composition in medical products or drug manufacture for prevention and treatment of leukopenia caused by radiation and chemotherapy // 2642256
FIELD: pharmacology.SUBSTANCE: invention relates to application of a composition made from raw materials consisting of Radix Panacis Quinquefolii Ganoderma, or Radix Et Rhizoma Ginseng and fermented Cordyceps synesis powder and/or from Cordyceps, taken in a certain amount, in manufacture of medical products or drugs for prevention and treatment of radiation therapy or chemotherapy induced leukopenia in which the composition is obtained by raw materials mixing and extracting them with water and/or alcohol (versions).EFFECT: compositions described above are effective in the manufacture of medical products or drugs for prevention and treatment of radiotherapy or chemotherapy-induced leukopenia.25 cl, 36 tbl, 56 ex
N-pyperonyl derivatives of daunorubicine, with antiprofliferative properties // 2642068
FIELD: pharmacology.SUBSTANCE: invention relates to the N-piperonyl derivatives of daunorubicine, which can be used in medicine, of general formula I where R=H, OCH3.EFFECT: new daunorubicine derivatives with antiproliferative properties and relatively low acute toxicity are proposed for cancer treatment, including non-small cell lung cancer, rhabdomyosarcoma, bowel carcinoma, breast adenocarcinoma.2 cl, 1 tbl, 2 ex
3-aminocyclopentancarboxamide derivatives // 2641913
FIELD: chemistry.SUBSTANCE: invention relates to the individual compounds selected from the group: 4-(1,3-benzoxazole-2-yl)]-N-[(1R,3S)-3-(ethylcarbamate)cyclopentyl]-N-methylbenzamide, N-((1R,3S)-3-ethylcarbamoylcyclopentyl)-N-methyl-4-(1-methyl-1H-benzoimidazol-2-yl)-benzamide, 4-benzothiazol-2-yl-N-((1R,3S)-3-ethylcarbamoylcyclopentyl)-N-methylbenzamide, ((1R,3S)-3-ethylcarbamoylcyclopentyl)-methylamide4'-[(R)-(tetrahydrofuran-3-yl)oxy]-biphenyl-4-carbon acid, 4-benzoxazole-2-yl-N-((1R,3S)-3-isopropylcyclopentadienyl)-N-methylbenzamide, and other compounds that are specified in the claims. The invention also relates to medicinal means having an inhibiting activity against fatty acid synthase (FAS) containing therapeutically effective amount of the compound of the invention.EFFECT: new compounds are obtained that have an inhibiting activity against the synthesis of fatty acids.2 cl, 2 tbl, 12 ex

New salicylic acid derivatives, their pharmaceutically acceptable salt, compositions and method for application // 2641903
FIELD: pharmacology.SUBSTANCE: invention relates to a number of other similar specific compounds, pharmaceutical compositions, comprising these compounds and their application to obtain a drug to inhibit the STAT3 and/or STAT5 activity or to treat cancer, where the cancer cells contain activated STAT3 or STAT5. , , , .EFFECT: preparation of a drug for STAT3 and STAT5 activity inhibition or for cancer treatment where the cancer cells contain activated STAT3 or STAT5.20 cl, 21 dwg, 6 tbl, 76 ex
N-[3-oxolup-20(29)-ene-28-oil]-2,2,6,6-tetramethylpiperidine-4-ylamine with cytotoxic activity in respect of human tumour cells // 2641900
FIELD: pharmacology.SUBSTANCE: invention relates to N-[3-oksolup-20(29)-ene-28-oil]-2.2,6,6-tetramethylpiperidine-4-ylamine of the structural formula with cytotoxic activity against human tumour cells.EFFECT: new compound is obtained that has an ability to suppress the growth of human tumour cells.2 tbl, 3 ex
5-(pyridine-2-ylamino)-pyrasin-2-carbonitrile compounds and their therapeutic application // 2641693
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula , as well as to pharmaceutical compositions based thereon for use in the treatment of a disease or condition mediated by SNK1.EFFECT: new compounds are obtained that inhibit the kinase function of kinase 1 of the control point.37 cl, 2 dwg
New anti-invasive compounds // 2641650
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula or pharmaceutically acceptable salts thereof, which can be used to prevent, and/or inhibit, and/or treat cancer. In formula (I) A and A' independently represent phenyl or pyridylene group; R2 represents a hydrogen or alkyl group (C1-C4); R3 represents a 2-pyridyl group, 3-pyridyl group, 4-pyridyl group, 2-pyrimidinyl group, 4-pyrimidinyl group or 5-pyrimidinyl group; R4 represents a carbonyl group or sulfonyl group; R5 is a -NH-(CH2)(a)-NR6R7 group or a 4-methylpiperazinyl group and a is an integer from 1 to 4, R6 and R7 independently represent a nalkyl group (C1-C4) or R6 R7 together with nitrogen atom they are bounded to form a heterocyclic group selected from 4-methylpiperazinyl group, morpholine group, pyrrolidinyl group and piperidine group. The invention also relates to a method for preparation of compounds of formula (I) and a pharmaceutical composition containing them.EFFECT: improved compounds properties.16 cl, 6 tbl, 17 ex

Pharmaceutical composition for cancer treatment and prevention // 2641260
FIELD: pharmacology.SUBSTANCE: invention relates to an antibody or a binding fragment thereof that specifically binds to the CAPRIN-1 protein and has immunological reactivity to the partial CAPRIN-1 polypeptide. Also a conjugate, as well as a pharmaceutical composition and a pharmaceutical combination for treatment or prevention of a malignant tumour expressing CAPRIN-1 are disclosed. The invention also relates to a method for treatment or prevention of a cancer expressing CAPRIN-1 using the above antibody or a fragment thereof, a conjugate, a composition or a combination.EFFECT: invention enables efficient treatment or prevention of cancer expressing CAPRIN-1.19 cl, 12 ex

Salt of nitrogen-containing heterocyclic compound or its crystalline form, pharmaceutical composition and flt3 inhibitor // 2641106
FIELD: pharmacology.SUBSTANCE: invention relates to new salts of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide selected from succinate, fumarate, pamoate, hydrochloride, phosphate, sulfate and hydrobromide, as well as crystalline salt forms. The compounds possess the properties of FLT3 (Fms-like tyrosine kinase 3) inhibitor and can be used to treat blood carcinoma including various forms of leukemia, for example acute lymphatic leukemia (ALL), acute myeloid leukemia (AML), acute promyelocytic leukemia (APL), chronic lymphocytic leukemia (CLL), and others. Crystalline α succinate of (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide on a powder X-ray diffractogram shows diffraction peaks at diffraction angles of (2θ) 10.5, 17.1, 19.1 and 22.4°; crystalline β succinate of this compound demonstrates diffraction peaks at diffraction angles of (2θ) 12.8, 16.1, 21.4 and 28.0°. Crystalline fumarate of the said compound on a powder X-ray diffractogram shows diffraction peaks at diffraction angles of (2θ) 8.6, 13.7, 17.8 and 23.0°.EFFECT: salts have storage stability or high solubility.9 cl, 6 dwg, 10 tbl, 13 ex

Salts of 4-((2-(6-(4-methylpiperazine-1-carbonyl)-naphthalen-2-yl)ethyl) amino)quinazoline-6-carbonitrile and pharmaceutical composition // 2641001
FIELD: pharmacology.SUBSTANCE: invention relates to the salts of 4-((2-(6-(4-methylpiperazine-1-carbonyl)naphthalen-2-yl)ethyl)amino)quinazoline-6-carbonitrile, which have the properties of a cyclin-dependent CDK8/CDK19 kinase inhibitor, and to pharmaceutical compositions comprising these salts, and to the use of such salts or such compositions for treatment of diseases or disorders mediated by the cyclin-dependent CDK8/19 kinase.EFFECT: new salts are obtained, which have improved solubility compared to the free base.13 cl, 5 tbl, 23 ex, 5 dwg

Combination liposomal compositions for cancer treatment // 2640934
FIELD: pharmacology.SUBSTANCE: method of delivery includes: (a) introduction to the subject of liposomes containing a therapeutic agent, isolated from the group consisting of cisplatin, oxaliplatin, carboplatin, gemcitabine, 5-fluorouracil, doxorubicin and taxane; and (b) introduction to the subject of lipid nanoparticles containing non-ionic substance that triggers the release of therapeutic agent from specified liposomes containing a therapeutic agent in the specified non-ionic substance isolated from the group consisting of D-α-tokopherolpolyethyleneglycol-succinate (TPGS), polyoxyethylene 40 stearate, polyethylene glycol p-(1,1,3,3 tetramethylbutyl) phenyl ester, polyoxyethylene-(2)-isooctylphenyl ether, polyoxyethylene-(150)-dinonylphenyl ether, 2,3-dihydroxipropyl ether of dodecanoic acid, polyoxyethylene-(20)-including sorbitan-monolaurate, polyoxyethylene-(20)-sorbitan-monopalmitate, polyoxyethylene-(20)-sorbitan monostearate, polyoxyethylene-(20)-including sorbitan-monooleate. The set for delivery includes: (a) the first composition containing liposome, comprising of a therapeutic agent; and (b) the second composition containing lipidic nanoparticle that includes non-ionic substance that triggers the release of the therapeutic agent from the specified liposome containing the therapeutic agent, where the first and second compositions are stored separately prior to introduction to the subject.EFFECT: increase in the release of the therapeutic agent from therapeutic liposomes through the use of attacking liposomes containing non-ionic substance that triggers the release of the therapeutic agent.23 cl, 12 dwg, 24 tbl, 12 ex

eans and methods for cancer treatment and/or prevention depending on natural ahr ligand // 2640913
FIELD: medicine.SUBSTANCE: group relates to the treatment and/or prevention of cancer, dependent on the natural AHR ligand. To this end, a therapeutically effective amount of an arylhydrocarbon receptor (AHR) inhibitor is administered.EFFECT: possibility of effective treatment or prevention of a brain tumour, the pathogenesis of which is justified by unbalanced production of kynurenin.15 cl, 24 dwg, 4 ex
Heterocyclic compounds, effective for kinase inhibition // 2640862
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I)or a pharmaceutically acceptable salt thereof, wherein Q is O; W is phenyl; X is absent; Y is NH; Z1 and Z2 are N; Z3 is NR5, where R5 is hydrogen; R1 is pyridine or pyrimidine; optionally substituted with C1-C6alkyl, C1-C6alkoxy, -NR10R11 or -SOmR12, where R10 and R11 are hydrogen, R12 is C1-C6alkyl; and m is 0; R3 is C1-C6alkyl; R2 is C1-C6alkyl when p is 1; or one R2 is C1-C6alkyl and one R2 is halogen when p is 2; or one R2 and R3 combined with formation of a five- to seven-membered carbocycle; R4 is hydrogen; p=1 or 2; and n is 1.EFFECT: heterocyclic compounds designed for cancer treatment.12 cl, 1 tbl, 8 ex

Derivatives of vitamine b6 nucleotides, acyclic nucleotides and acyclic nucleoside phosphonates // 2640582
FIELD: pharmacology.SUBSTANCE: invention relates to compounds, compositions thereof, for treatment of infections and neoplasms with structures , where R1 is the residue of a compound selected from the group consisting of cytarabine, fludarabine, gemcitabine, clofarabine, cladribine, vidase, dacogen, pentostatin and cladribine or aristermycin, acyclovir, ganciclovir, penciclovir, adefovir, cidofovir, tenofovir, zidovudine and lamivudine; X and Y are independently O, S or NH; and R2 and R3 are independently selected from the group consisting of H, alkyl, phenyl, heteroaryl and the remainder of the vitamin B6 fragment selected from wherein heteroaryl is an aromatic ring containing from 1 to 3 heteroatoms selected from oxygen, sulfur and nitrogen, and wherein at least one of R2 and R3 is the residue of a fragment of vitamin B6, L is alkyl.EFFECT: new effective substances for treatment of viral and oncological diseases.16 cl, 4 dwg, 2 tbl, 6 ex

Combination treatment of cancer // 2640485
FIELD: pharmacology.SUBSTANCE: proposed: a combination for application as a drug for cancer treatment, containing: (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363) or a salt thereof with an androgen receptor signal modulator selected from 4-{3-[4-cyano-3-(trifluoromethyl)-phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluoro-N-methylbenzamide (MDV-3100) and N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)-sulfonyl]-2-hydroxy-2-methylpropanamide (bicalutamide) or a salt thereof, a set of these components for application in cancer treatment (versions).EFFECT: greater inhibition of tumour growth by combining the said compound against monotherapy of castration-resistant prostate cancer, the combination showed good tolerability.9 cl, 3 dwg, 1 tbl
odulators of atp-binding cartridge transporters // 2640420
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula II , where R is H, OH, OCH3, or two R taken together form -OCH2O- or -OCF2O-; R1 is H or up to two C1-C6alkyls; R2 is H or halogen; and R3 is H or C1-C6 alkyl; R3 is H or C1-C6 alkyl; Y is O or NR4; and R4 is H or C1-C6 alkyl, and their pharmaceutical compositions useful as modulators of ATP-binding cassette ("ABC") transporters, or fragments thereof, including a cystic fibrosis transmembrane conduction regulator ("CFTR"). This invention also relates to methods for treatment of diseases mediated by ABC transporters using the compounds of the invention.EFFECT: increased efficiency of treatment.19 cl, 2 tbl, 1 ex

Stable crystalline form of typiracyl hydrochloride and method for its crystallization // 2640417
FIELD: pharmacology.SUBSTANCE: invention relates to a new crystalline form of hydrochloride of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)pyrimidinedione of the formula (I) indicated below. The crystalline form of the compound of the formula (1) shows characteristic peaks of powder X-ray diffraction at 11.6°, 17.2°, 17.8°, 23.3°, 27.1° and 29.3° angles, as the diffraction angle (2θ±0.1°) in anhydrous form and an endothermic peak determined by thermogravimetry and differential thermal analysis at a temperature of about 262 °C. The crystal shows, following crystal data in the analysis of single crystals: crystal system: monoclinic system, spatial group: P2l/n (No. 14), the crystal lattice constant: a=11.6006 (9) , b=10.3106 (11) , c=10.3036 (10) , α=90°, β=101.951 (7)°, γ=90° and unit lattice cell volume: 1205.7 (2) .EFFECT: compound has the properties of a thymidine phosphorylase inhibitor and can be used as an antitumor agent.13 cl, 3 dwg, 3 tbl, 7 ex
Derivatives of 1,4-dioxide of quinoxaline-2-carbonitrile inhibiting tumour cells growth // 2640304
FIELD: pharmacology.SUBSTANCE: invention relates to derivatives of 1,4-dioxide of quinoxaline-2-carbonitrile, corresponding to the formula: , as well as pharmaceutical compositions based on them.EFFECT: new compounds are obtained that have antiproliferative activity and can be used to inhibit the growth of tumour cells.9 cl, 2 tbl, 48 ex

at40 antibody binding with domain i of extracellular part of epidermal her2/cd340 growth factor receptor, and its application for cancer treatment // 2640259
FIELD: biotechnology.SUBSTANCE: antibody that binds to the epidermal HER2/CD340 growth factor receptor is disclosed. Application of this antibody to treat cancer with HER2 overexpression is also considered. The antibody of the present invention binds to domain I of the extracellular portion of HER2.EFFECT: high efficiency of cancer treatment.3 cl, 4 dwg, 2 tbl, 8 ex

Bispecific anti-vegf/anti-ang-2 antibodies // 2640253
FIELD: biotechnology.SUBSTANCE: invention relates to a bispecific antibody specifically binding to a human vascular endothelial growth factor-VEGF and human angiopoietin-2-ANG-2, a pharmaceutical composition containing it, as well as a method for its preparation. Also a nucleic acid encoding the above antibody and a vector or host cell containing the aforementioned nucleic acid are disclosed.EFFECT: invention allows effective treatment of cancer and/or vascular diseases.12 cl, 19 dwg, 18 tbl, 20 ex

Bis-met-histones // 2640247
FIELD: biotechnology.SUBSTANCE: nucleic acid molecule encodes a polypeptide consisting of two methionine residues as the first and second N-terminal amino acid residues linked through a peptide bond to the mature eukaryotic histone H1. 3. A polypeptide is prepared by culturing a host cell transformed with an expression vector comprising the said nucleic acid molecule. The polypeptide is used as part of a pharmaceutical composition for treatment of cancer, bacterial, viral or fungal infections. Also, the polypeptide is used as part of a composition for diagnosing a patient with respect to the presence of a response to a pharmaceutical composition containing the said polypeptide, or with respect to curability thereof.EFFECT: invention allows to increase the efficiency of recombinant expression and facilitate the determination of the said polypeptide in the presence of endogenous histones while maintaining biological activity of the mature eukaryotic histone.16 cl, 3 dwg, 6 tbl, 7 ex

Pharmaceutical composition for liver cancer treatment and/or prevention // 2640245
FIELD: pharmacology.SUBSTANCE: pharmaceutical composition for treatment and/or prevention of liver cancer with surface expression of a CAPRIN-1 protein, that contains an anti-CAPRIN-1 protein is provided. In addition, a pharmaceutical kit and a method for treatment and/or prevention of liver cancer expressing the CAPRIN-1 protein are observed.EFFECT: invention can find further application in liver cancer therapy.9 cl, 16 ex
New compounds // 2640200
FIELD: pharmacology.SUBSTANCE: invention relates to a new compound of the formula (I) or a pharmaceutically acceptable salt thereof having interferon α (IFN-α) and tumour necrosis factor α (TNF-α) inducer properties. The compounds may be useful as vaccine adjuvants. In the formula (I) R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl; m is an integer having a value of 1 to 4.EFFECT: compounds can be used for treatment of allergic diseases and inflammatory conditions, for example, allergic rhinitis and asthma, infectious diseases and cancer.15 cl, 7 ex
ethod for adjuvant therapy of cancer // 2640180
FIELD: medicine.SUBSTANCE: methods of the invention include administration of therapeutically effective doses of dabrafenib and trametinib. The composition of the invention comprises a combination of dabrafenib and trametinib.EFFECT: application of inventions allows to improve disease-free survival in patients with melanoma.8 cl, 1 tbl
Pharmaceutical compositions of substituted quinazolinones // 2640115
FIELD: pharmacology.SUBSTANCE: composition according to this invention contains an active ingredient selected from a series of substituted quinazolinones and their pharmaceutically acceptable salts, stereoisomers, tautomers or hydrates, and additionally contains approximately 10 wt % to approximately 85 wt % of microcrystalline cellulose; approximately 4.0 wt % of sodium starch glycolate; approximately 0.5 wt % of magnesium stearate; and approximately 2.5 wt % of colloidal silicon dioxide; and prepared for peroral introduction and immediate release.EFFECT: creation of new compounds that increase the bioavailability of substituted quinazolinones while maintaining stability, possibility of treatment and prevention of the abovementioned diseases.15 cl, 1 tbl, 1 ex

ethod for biological material obtaining for creation of autological antitumour vaccines // 2640017
FIELD: medicine.SUBSTANCE: invention can be used to isolate tumour antigens for tumour immunotherapy. For this, 1 gram of tumour is chopped on a cooled surface, 9 ml of buffer (pH 7.0) consisting of 10 mM of NaHCO3, 10 mM of EDTA, 2 mM of PMSF is added, and homogenized. Then it is centrifuged first at 20,000 g at 4°C for 30 minutes, and then at 100,000 g at 4°C for 90 minutes. The supernatant is subjected to ultra-/diafiltration using a membrane with a cut-off limit of 50 kDa, using a formulation buffer (pH 7.0) consisting of 10 mM of NaHCO3 and 150 mM of sodium chloride.EFFECT: obtaining of a fraction consisting of complexes represented by different classes of heat shock proteins, which determines a wide range of associated tumour peptides.1 ex, 2 tbl, 2 dwg

Pyridoxin and acetone derivatives with antitumor activity // 2639879
FIELD: pharmacology.SUBSTANCE: invention relates to pyridoxine and acetone derivatives of the general formula I , where R1=R2=CH3; R1=H, R2=C2H5; R1=H, R2=C3H7; R1=H, R2=C4H9; R1-R2=spiro-C4H8; R1-R2=spiro-C5H10; R1= H, R2= CH (CH3) C9H19.EFFECT: these compounds have expressed antitumor activity against cells of predominantly malignant neoplasms and provide high security in relation to the conditionally normal and normal cells and high value of lethal dose LD50, and may have applications in medicine.3 dwg, 14 ex
Phenyl derivative // 2639875
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the general formula (I) having a high antagonistic activity with respect to human S1P2, and can be used to prepare a drug for treatment of a disease mediated by S1P2, such as a disease caused by vasoconstriction, fibrosis and respiratory disease.EFFECT: compound application efficiency increase.14 cl, 2 tbl, 9 ex
Anti-cancer benzopyrazines acting through fgfr-kinases inhibition // 2639863
FIELD: pharmacology.SUBSTANCE: invention relates to benzopyrazine derivatives of the general formula (I) , including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof, wherein W is -N(R3)-; R2 is C1-4alkoxy; Y is -CR18=N-OR19 or -E-D; E is bond, C2-4alkynediyl, -CO-(CR22R23)s-, -NR22-(CR22R23)s-, -(CR22R23)s-CO-NR22-(CR22R23)s- or -(CR22R23)s-NR22-CO-(CR22R23)s-; D is phenyl, 3-6 membered cycloalkyl or 5-9 membered mono- or bicyclic saturated, partially saturated or aromatic heterocyclyl containing 1-4 heteroatoms selected from N, O or S, wherein the said phenyl, cycloalkyl and heterocyclyl can each optionally being substituted with 1-2 R1-groups; with the exception of the compounds indicated in the formula; R1 is halogen, cyano, C1-6alkyl, C1-6alkoxy, -C(=O)-O-C1-6alkyl, hydroxyC1-6alkyl, -NR4R5 , C1-6alkyl substituted by -O-C(=O)-C1-6alkyl, C1-6alkyl substituted by -NR4R5, -C(=O)-NR4R5, R6, C1-6alkyl substituted by R6, -C(=O)-R6; R3 is halogenC1-6alkyl, optionally substituted by -O-C(=O)-C1-6alkyl, hydroxyC1-6alkyl, hydroxyhalogenC1-6alkyl, C1-6alkoxyC1-6alkyl, where each C1-6alkyl may optionally be substituted by one hydroxyl group or -O-C(=O)-C1-6alkyl, C1-6alkyl substituted by R9, C2-6alkynyl substituted with R9, C1-6alkyl substituted by -NR10R11, C1-6alkyl substituted by -O-C(=O)-NR10R11; R4 and R5 are hydrogen, C1-6alkyl, C1-6alkyl substituted by -NR14R15, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, where each C1-6alkyl may optionally be substituted by one hydroxyl group, -C(=O)-NR14R15, -C(=O)-O-C1-6alkyl, -C(=O)-R13; R6 is a 6-membered saturated or aromatic monocyclic heterocyclyl having 1 to 2 heteroatoms selected from N or O; the said heterocyclyl is optionally substituted by 1 substituent selected from C1-6alkyl, halogen, C1-6alkyl-O-C(=O)-; R9 is C3cycloalkyl or 3-6 membered monocyclic saturated, partially saturated or aromatic heterocyclyl containing 1-2 heteroatoms selected from N or O, the said heterocyclyl is optionally substituted by 1 substituent selected from =O, hydroxyC1-4alkyl, C1-4alkyl-C(=O)-, C1-4alkyl substituted by -NR14R15, C1-4alkoxy; R10 and R11 are hydrogen, C1-6alkyl, halogen C1-6alkyl, hydroxyC1-6alkyl or C1-6alkyl substituted by carboxyl; R13 is a saturated 6-membered monocyclic heterocyclyl containing 1-2 heteroatoms selected from N and O; R14 and R15 are hydrogen or C1-4alkyl; R18 and R19 are C1-6alkyl; R22 and R23 are hydrogen; n=2; s=0, 1, 2, or 3. Invention also relates to a pharmaceutical composition and a product based thereon, the use of a compound of formula (I) and a method of prevention or treatment of conditions mediated by FGFR kinase.EFFECT: new derivatives of benzopyrazine, useful for cancer treatment.28 cl, 4 tbl, 54 ex

Antibodies and immunoconjugates and their applications // 2639543
FIELD: biotechnology.SUBSTANCE: humanized antibody specific for STEAP-1 and its antigen-binding fragment are proposed. A polynucleotide encoding an antibody or an antigen-binding fragment thereof, a vector, a host cell, a method for anti-STEAP-1 antibody production are described. A method for tumour visualization, a pharmaceutical composition, a medicament for cell proliferative disorder treatment, immunoconjugates and a cysteine-based antibody based on the said antibody are also disclosed.EFFECT: invention provides new antibodies to STEAP-1 and can be used in medicine.30 cl, 29 dwg, 2 tbl, 9 ex

Pharmaceutical composition for cancer treatment and/or prevention // 2639522
FIELD: pharmacology.SUBSTANCE: invention relates to an antibody that specifically binds to the CAPRIN-1 protein, as well as to a conjugate for treatment or prevention of CAPRIN-1 expressing cancer containing it. A pharmaceutical composition for CAPRIN-1 treatment or prevention, as well as a pharmaceutical combination for CAPRIN-1treatment or prevention containing the above antibody or conjugate is also described. The invention also relates to a method for treatment or prevention of a CAPRIN-1 expression cancer comprising administration of the above antibody, conjugate, composition or combination.EFFECT: invention allows effective treatment or prevention of CAPRIN-1 expressing cancer.12 cl, 8 ex

Immunity inducing agent // 2639518
FIELD: medicine.SUBSTANCE: invention refers to the immunity inducing agent containing the effective number of at least one polypeptide with inducing immune system activity, which induces cytotoxic t-cells capable to destroy tumour cells expressing polypeptide CAPRIN-1. Also, method is represented to obtain the selected antigen-presenting cell in vitro, which presents polypeptide fragment CAPRIN-1 for class I molecule RENAMO t-cells, as well as in vitro method for obtaining selected cytotoxic t-cells specific to protein CAPRIN-1. The invention also relates to a method of induction of immunity, including the introduction of individual effective amount of at least one polypeptide with inducing immune system activity, which induces cytotoxic t-cells capable to destroy tumour cells expressing polypeptide CAPRIN-1.EFFECT: effectively destroys tumour cells expressing the CAPRIN-1 polypeptide.13 cl, 5 dwg, 6 ex

Antibodies against vascular endothelial growth factor (vegf) // 2639506
FIELD: biotechnology.SUBSTANCE: method is described for blocking or reducing recurrent tumour growth or recurrent growth of cancer cells, comprising administering an effective amount of an anti-VEGF antibody to a subject in need of such treatment, wherein the anti-VEGF antibody comprises: HVR-H1 comprising the amino-acid sequence of SEQ ID NO: 1; HVR-H2 comprising the amino-acid sequence of SEQ ID NO: 2; HVR-H3 comprising the amino-acid sequence of SEQ ID NO: 3; HVR-L1 comprising the amino-acid sequence of SEQ ID NO: 4 or 5; HVR-L2 comprising the amino-acid sequence of SEQ ID NO: 6; and HVR-L3 comprising the amino-acid sequence of SEQ ID NO: 7, or wherein the anti-VEGF antibody comprises a heavy chain variable domain comprising the amino-acid sequence of SEQ ID NO: 43 and a light chain variable domain comprising an amino-acid sequence of SEQ ID NO: 44 or 45. A method of treating a non-neoplastic condition is also described is, comprising administering an effective amount of an anti-VEGF antibody to a subject in need of such treatment, wherein the anti-VEGF antibody is an antibody according to the above method.EFFECT: increased efficiency.19 cl, 16 dwg, 5 ex
Oral antitumour drugs and method for oncological diseases treatment // 2639479
FIELD: pharmacology.SUBSTANCE: group of inventions is an oral agent for oncological diseases treatment, comprising: a therapeutically effective amount of (S)-3-[(3-amino-1-pyrrolidinyl)carbonyl]-4,11-dihydroxy-2-methylanthra[2,3-b]furan-5,10-dione, represented by the formula: and a liquid pharmaceutically acceptable carrier comprising one or more solvents selected from water, polyethylene glycol, 1,2-polypropylene glycol, ethanol, glycerol. The oral agent may be a solid dispersion. The group of inventions includes a method for treatment of an oncological disease, comprising oral administration of a therapeutically effective amount of the described agent to a patient in need.EFFECT: pharmaceuticals according to the invention provide high solubility of anthrafuran, rapid release of the active ingredient from pills or capsules, are stable during storage.13 cl, 1 dwg, 8 tbl, 7 ex
Oral pharmaceutical composition // 2639473
FIELD: pharmacology.SUBSTANCE: invention represents a medicinal form of a non-coated pill containing α,α,α-trifluorothymidine and hydrochloride 5-chloro-6-(2-iminopyrrolidine-1-yl)methyl-2,4(1N,3N)pyrimidinedione as active ingredients and, as such, not containing additives, including salt metals. The invention also includes a method for stabilization of an oral pharmaceutical composition containing the active ingredients described above.EFFECT: increased stability of the medicinal form.11 cl, 18 ex, 5 tbl
ethod for acute radiation esophagitis treatment // 2639463
FIELD: medicine.SUBSTANCE: for treatment of acute radiation esophagitis during radiation therapy, 25-30 g of "Koleteks gel DNA-l" is taken orally before a radiation therapy session. At that, during the radiotherapy session, placement of the "Kolegel-DNA-disk" material in the oral cavity is assigned with complete gradual dissolution. After completion of radiation therapy, inhalations with "Koleteks-Beta", hydrogel which is mixed with inhalation solution "Fluimucil" and water at a ratio of 3:5:2 accordingly are prescribed 2 times a day, 5-10 min. within 5-7 days. Inhalations are continued for the next 3-4 months, 5-7 days per month with a break of 20-25 days.EFFECT: invention reduces the frequency and severity of early and late radiation reactions in patients.3 ex

Apoptosis-inducing means // 2639459
FIELD: pharmacology.SUBSTANCE: group of inventions refers to a pharmaceutical composition for induction of apoptosis in a cell with a mutated KRAS containing an effective amount of a drug that suppresses GST-π; and an effective amount of a drug that suppresses autophagy. A method for apoptosis induction in a cell with a mutated KRAS, in particular in a cancer cell with a KRAS mutation, is also claimed.EFFECT: increased efficiency of apoptosis in the cell.8 cl, 18 dwg, 6 ex

Pharmacutical, containing recombinant mistletoe lectin, for treatment of melanotic cancer // 2639445
FIELD: pharmacology.SUBSTANCE: pharmaceutical comprises of a recombinant mistletoe lectin including the amino acid sequences ID SEQ No. 1 and SEQ ID No. 4. The group of inventions also relates to a pharmaceutical composition.EFFECT: effectiveness of treatment is increased, increasing the survival of patients.12 cl, 1 dwg, 1 tbl
Oxothioimidazoline derivatives, methods for their production and application in medicine as androgen receptor inhibitors // 2639145
FIELD: pharmacology.SUBSTANCE: invention relates to an oxothioimidazoline derivative of the formula or to its mesomer, racemate, enantiomer, diastereomer, or a mixture thereof, wherein A is -CR' or N; R' is hydrogen or halogen; Z1 and Z2 each independently represents methyl; R1 and R2 each is independently selected from the group consisting of S or O; R3 is selected from the group consisting of C1-C3-alkyl, heterocyclyl selected from tetrahydrofuran, tetrahydropyran, piperidine, dioxo-tetrahydrothiopyran, azetidine, pyrrolidine, oxetane; C6-aryl and -S(O)mR6; when R3 is selected from heterocyclyl selected from tetrahydrofuran, tetrahydropyran, piperidine, dioxo-tetrahydrothiopyran, azetidine, pyrrolidine, oxetane; or C6-aryl, each of the heterocyclyl and aryl is optionally substituted by one or more groups selected from the group consisting of C1-alkyl, -OR6, -C(O)NR7R8, -S (O)mR6 and -C(O)R6; when R3 is C1-C3alkyl, alkyl is substituted by one or more groups selected from the group consisting of halogen, cyano, amino, C3-cycloalkyl, tetrahydrofuran, -OR6, -C(O)NR7R8, -S(O)mR6 and -C(O)OR6, wherein the cycloalkyl is optionally substituted by one group selected from cyano, amino, -OR6, -C(O)NR7R8 and -C(O)OR6; R4 and R5 are each independently selected from the group consisting of cyano, C1-alkyl, halogen and -CF3; R6 is hydrogen, C1-alkyl or -CF3; R7 and R8 are each independently selected from the group consisting of hydrogen and C1-alkyl, and m is 2. The invention also relates to intermediates, a process for preparation of a compound of formula (I), a pharmaceutical composition based on the compound of formula (I) and its application.EFFECT: new oxothiohydantoin derivatives, useful for treatment of androgen receptor mediated diseases.18 cl, 51 ex
Indasole inhibitors of wnt signal path and their therapeutic applications // 2638932
FIELD: medicine.SUBSTANCE: invention relates to a indasole derivative that has the following formula , or its pharmaceutically acceptable salt, as well as a pharmaceutical composition containing it. The invention relates to methods for treatment of disorders characterized by the activation of Wnt-signalling pathways (e.g., cancer, abnormal cell proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), including introduction of a therapeutically effective amount of this compound or pharmaceutically acceptable salt thereof. This compound can also be used in modulation of cellular events, mediated by Wnt-signalling, as well as for treatment of genetic diseases and neurological conditions/disorders/diseases due to mutations or disregulation of the Wnt pathway and/or one or more components of Wnt-signalling.EFFECT: inhibits the Wnt signalling pathway and can be used to treat various diseases and pathologies.28 cl, 8 tbl, 8 ex

Diaryl hydantoins // 2638833
FIELD: biotechnology.SUBSTANCE: invention relates to organic chemistry, namely to a new heterocyclic compound [RD93], which may be useful for treatment of hormone-refractory prostate cancer, benign prostatic hyperplasia, breast cancer and ovarian cancer.EFFECT: new heterocyclic compound with useful biological properties is obtained.6 cl, 41 dwg, 11 tbl, 61 ex

Lc-ms/ms method for multiple reactions monitoring to identify therapeutic antibodies in animal species using framework signature peptides // 2638806
FIELD: biotechnology.SUBSTANCE: invention relates to a method for detection of human or humanized antibodies comprising the steps of treatment of a human or humanized biological sample with a digestible enzyme to form a sample of a split antibody, the biological sample being serum, blood plasma, tissue or cells from an animal that has been treated with a human or humanized antibody; and analysis of a sample of the digested antibody using mass spectrometry to identify one or more human framework peptides.EFFECT: invention provides detection of therapeutic antibodies in samples from an animal treated with a therapeutic antibody, while other antibodies present in the sample, such as native animal antibodies, are not detected.12 cl, 4 ex, 25 dwg, 13 tbl

ethod for antitumour agent introduction // 2638795
FIELD: pharmacology.SUBSTANCE: new pharmaceutical product is used that includes compound A at a dose of 800 to 3000 mg per day, daily for 5 days on days 1 to 5 of the treatment cycle followed by a break of 23 days.EFFECT: method allows to increase the effectiveness of treatment.9 cl, 4 tbl, 1 ex, 2 dwg
ethod for treatment of anal cancer with skin transition // 2638616
FIELD: medicine.SUBSTANCE: method includes two induction courses of polychemotherapy (PCT) according to the scheme: mitomycin C 10 mg/m2 intravenously sprayed on days 1 and 29 and 5-fluorouracil 1000 mg/m2 per day by continuous infusion on days 1-4 and 29-32. Three weeks after the second course of PCT, the primary focus and regional lymph nodes are exposed to external radiation of 2.4 Gy daily, 5 fractions per week till the cumulative dose of 44 isoGr, 17 irradiation sessions. At that, during 15 irradiation sessions, a sonodynamic therapy session is performed 2 hours before the start of irradiation, for which an "extempore" formulated mixture containing 5 mg of hydrogel napkin "Coletex SP-1" with propolis based on sodium alginate and 100 mg of gemcitabine is delivered to the perianal area skin. After application of the medicinal mixture, a radiator is fed to the lesion focus and a medium frequency ultrasound treatment session is performed at a frequency of 0.88 MHz, I = 1.0 Bm/cm2, exposure time 10 min. On days free from irradiation, no sonodynamic chemotherapy sessions are performed, while 15 procedures of sonodynamic exposure are performed for the entire course of external exposure. The total dose of gemcitabine for the external exposure course is 1500 mg. After the course of irradiation, a break in treatment for 2-3 weeks is performed. Then a course of endovaginal brachytherapy with a fraction dose of 3 Gy with irradiation frequency one day until a cumulative dose of 15 Gy is conducted. On days of irradiation, 2 hours before the irradiation session, a sonodynamic therapy session is performed. For this purpose, the above-mentioned "extempore" composed mixture is introduced into the anus region. Immediately after its delivery, , the radiator is fed to the focal point of the lesion and a medium frequency ultrasonic exposure session is conducted at a frequency of 0.88 MHz, I=1.0 Bm/cm2, exposure time is 10 min. In days free from irradiation, no sonodynamic chemotherapy sessions are performed. A total of 5 procedures are performed for the course of intracavitary irradiation. The total dose of gemcitabine for the course of combined radiation treatment is 2000 mg, total cumulative dose at the primary focus is 61 isoGr.EFFECT: improved effectiveness of radiation treatment, quality of life of patients with locally advanced anal cancer with transition to the skin, its complete regression.1 ex, 1 tbl
 
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