Antineoplastic agents (A61P35)

A   Human necessities(303198)
A61P35                 Antineoplastic agents(3286)
A61P35/02 - Specific for leukemia(96)
A61P35/04 - Specific for metastasis(101)
Novel pyrrole compounds, synthesis method thereof and pharmaceutical compositions containing same // 2607788
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I) possessing inhibitory activity on Bcl-2 family proteins. In formula (I) (I) A1 is hydrogen, (C1-C6)polyhaloalkyl group or (C1-C6)alkyl group, A2 is hydrogen, (C1-C6)polyhaloalkyl group, (C1-C6)alkyl group or cycloalkyl group, T denotes a hydrogen atom, (C1-C6)alkyl group, optionally substituted with one-three halogen atoms, group (C1-C4)alkyl-NR1R2 or group (C1-C4)alkyl-OR6, R1 and R2 each independently from each other is a hydrogen atom or (C1-C6)alkyl group, or R1 and R2 form with a nitrogen atom bearing them, heterocycloalkyl, R3 is (C1-C6)alkyl group, cycloalkyl group, heterocycloalkyl group, aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R4 is an aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R5 is hydrogen or halogen atom, R6 is a hydrogen atom or a linear or branched (C1-C6)alkyl group, Ra, Rb, Rc and Rd each independently from other represents hydrogen, linear or branched (C1-C6)alkyl, halogen atom, a linear or branched (C1-C6)alkoxy group, hydroxy group, R7-CO-NH-(C0-C6)alkyl-, R7-SO2-NH-(C0-C6)alkyl-, R7-NH-CO-NH-(C0-C6)alkyl-, R7-O-CO-NH-(C0-C6)alkyl-, or substitutes of pair (Rb, Rc) form together with carbon atoms carrying them, a ring consisting of 5–6 ring members, which may contain 1–2 oxygen atoms, R7 is hydrogen, linear or branched (C1-C6)alkyl, aryl or heteroaryl. Invention also relates to methods of producing compounds of formula (I), to a pharmaceutical composition, use of a pharmaceutical composition for preparing a drug, use of compound of formula (I) for preparing a drug.EFFECT: obtaining novel compounds of formula (I) possessing inhibitory activity on Bcl-2 family proteins.37 cl, 2 tbl, 473 ex

Transdermal therapeutic system for 5-aminolevulinic acid hydrochloride // 2607657
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine. Disclosed is transdermal therapeutic system, which includes active substance impermeable back layer, containing active substance, polymer matrix and separable protective layer, wherein active substance is represented by 5-aminolevulinic acid hydrochloride and polymer matrix basic polymer is adhesive polyacrylate. Transdermal therapeutic system is applicable for diagnosing and treating of skin cancer pre-stages, such as actinic keratosis, as well as skin oncological diseases.EFFECT: transdermal therapeutic system is fairly well sticks to skin and does not cause irritation thereof.15 cl, 1 dwg, 4 ex
N-9-substituted purine compounds, compositions and methods of use // 2607635
FIELD: chemistry.SUBSTANCE: present invention relates to novel compounds of formula I-A, having properties of inhibitors of kinase of phosphoinositide-3-kinase family mTOR and PI3K, for use in treating cancer, as well as for preparing drugs for treating cancer. In compounds of formula I-A R1 is selected from a group comprising cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, oxetan-2-yl, oxetan-3-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl and tetrahydropyran-4-yl, oxepan-2-yl, oxepan-3-yl, oxepan-4-yl, phenyl pyrrol-2-yl, pyrrol-3-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, furan-2-yl, furan-3-yl, thien-2-yl, thien-3-yl, thiazol-2-yl, thiazol-3-yl, thiazol-4-yl, imidazol-1-yl, imidazol-4-yl, pyrid-2-yl, pyrid-3-yl, pyrid-4-yl, pyrimidin-1-yl, pyrimidin-2-yl, pyrimidin-3-yl, pyrazin-2-yl, pyridazin-2-yl, pyridazin-3-yl and triazin-2-yl, where R1 substituted by 0-3 substitutes RR1, selected from a group consisting of halogen, F, Cl, Br, I, -ORa, -C(O)Ra, -Rc; where Ra is selected from hydrogen or C1-6alkyl, Rc is C1-6alkyl; R2 is selected from a group comprising hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl; R3 is a morpholine-4-yl, where group R3 is substituted with 0–3 substitutes RR3, selected from a group consisting of -Ri, halogen, where Ri is selected from C1-6alkyl, C1-6haloalkyl; D is -NR4C(O)NR5R6 or -NR5R6, where R4 and R5 each denotes hydrogen and R6 is C1-6alkyl, C1-6haloalkyl oxetan-3-yl and pyridyl-on.EFFECT: treatment of cancer.11 cl, 1 tbl, 26 ex

Romidepsin solid forms and use thereof // 2607634
FIELD: chemistry.SUBSTANCE: invention relates to novel crystalline form C of romidepsin, a pharmaceutical composition containing form C of romidepsin.EFFECT: treatment of skin T-cell lymphoma.3 cl, 12 dwg, 19 tbl, 16 ex

Combined anticancer therapy // 2607596
FIELD: medicine.SUBSTANCE: present invention relates to combined therapy with {3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4difluorophenyl} amide of propane-1-sulphonic acid (compound 1) or its pharmaceutically acceptable salt and EGFR inhibitor, selected from erlotinib and cetuximab, for treating cancer, containing b-Raf with V600 mutation, namely colorectal cancer, melanoma and thyroid cancer.EFFECT: combination of compound 1 with EGFR inhibitor leads to improved anti-tumor effects, which considerably exceed the results, obtained for each compound separately, without increasing the toxicity.20 cl, 6 ex, 15 tbl, 9 dwg
Combination of ozogamicin inotuzumab and torizel for treating cancer // 2607594
FIELD: medicine.SUBSTANCE: invention relates to therapeutic method of treating cancer, which is non-Hodgkin’s lymphoma; method involves stage of introducing simultaneously or successively effective number of ozogamicin inotuzumab (SMS-544) in dose of 0.4 mg/m2 up to 1.8 mg/m2 every 4 weeks throughout 6 cycles and temsirolimus in dose of 5 to 175 mg/week during disease progression.EFFECT: invention provides low toxicity, associated with treatment using ozogamicin inotuzumab or temsirolimus.7 cl, 8 ex, 11 tbl

Pyrazolopyrimidines and related heterocycles as ck2 inhibitors // 2607453
FIELD: chemistry.SUBSTANCE: invention relates to novel compounds of formula (II) or (II') or pharmaceutically acceptable salts thereof. Compounds inhibit activity of protein kinase CK2 (casein kinase II) or PIM kinase and can be used for treating proliferative diseases selected from cancer of various cell lines, such as breast cancer, lung, skin cancer etc, angiogenesis, as well as other kinase related conditions, including inflammation, vascular diseases, pathogenic infections, neurodegenerative diseases, some immunological diseases. In compounds of formula (II) or (II') or Z3 denotes N and Z4 denotes CR5; or Z3 denotes CR5 and Z4 denotes N; or Z3 and Z4 both denote N; each R5 is independently selected from halo, -CN and -R, where each R is independently selected from H and optionally substituted C1-C4 alkyl; each R2, R3 and R4 is independently selected from H and optionally substituted C1-C10 alkyl; X denotes S or NR2; Y is O or S; Z is O or S; L is a bond, -CR7=CR8-, -C≡C- or -(CR7R8)m-, and W is optionally substituted C1-C10alkyl, optionally substituted with 1-10-member heteroalkyl, optionally substituted C6-C12aryl, Optionally substituted 5-12-member heteroaryl, -NR7R8, -OR7, -S(O)nR7, -CONR7R8, optionally substituted 3-10-member heterocyclyl, optionally substituted with C3-C10carbocyclyl, optionally substituted C2-C10alkenyl, optionally substituted C2-C10alkynyl or -CR7R8R9; or L is a bond, -NR7-, -O-, -S(O)n-, -(CR7R8)m- or -(CR7R8)m-NR7-; and W is selected from optionally substituted C6-C12aryl, optionally substituted 5-12-member heteroaryl and -NR7R8; where each R7 and R8 and R9 is independently selected from H, optionally substituted C1-C10alkyl, optionally substituted 1-10-member heteroalkyl, optionally substituted C3-C10carbocyclyl, optionally substituted 3-10-member heterocyclyl, optionally substituted C3-C10carbocyclylalkyl, optionally substituted 3-10-member heterocyclylC1-C8-alkyl, optionally substituted C6-C12aryl, optionally substituted C7-C12arylalkyl, optionally substituted 5-12-member heteroaryl and optionally substituted 5-12-member heteroarylC1-C8alkyl; or R8 and R9, taken together with carbon atom to which they are bonded form =O(oxo); or R7 and R8, taken together and arranged on one carbon atom or on adjacent bonded atoms (CR7R8)m, either alone, or as part of another group, form a 3-8-member carbocyclic ring or a heterocyclic ring; or R7 and R8, taken together with a nitrogen atom to which they are bonded, form an optionally substituted 5-10-member heterocyclic or heteroaryl ring, which optionally contains one or more additional ring heteroatoms selected from N, O and S; provided that no more than one group from R7 and R8 in -NR7R8 is selected from a group consisting of alkoxy, alkylamino, dialkylamino and heterocyclyl; each n is independently equal to 0, 1 or 2; each m is independently equal to 1, 2, 3 or 4; and R1A is selected from H, optionally substituted C1-C10alkyl; and R1B each is independently selected from H, optionally substituted C1-C10alkyl, optionally substituted 3-10-member heterocyclyl, optionally substituted C3-C10carbocyclyl, optionally substituted C3-C10carbocyclylalkyl, optionally substituted 3-10-member heterocyclyl-C1-C8alkyl, optionally substituted C6-C12aryl, optionally substituted C7-C12arylalkyl, optionally substituted 5-12-member heteroaryl or optionally substituted 5-12-member heteroaryl-C1-C8alkyl.EFFECT: substitutes for saturated and unsaturated carbon atoms are selected from corresponding groups specified in patent claim.58 cl, 14 dwg, 113 tbl, 299 ex
Cancer antigen // 2607379
FIELD: biotechnology.SUBSTANCE: invention relates to biotechnology, specifically to antigen expression induction on cancer cells, and can be used in medicine. Treatment of cancer cells with agent selected from Mycobacterium w, cisplatin, paclitaxel, Gemcitabine and combinations thereof, obtaining cancer antigens: protein 45 kDa, expressed by pancreatic cancer cells, and protein 36 kDa, expressed by melanoma cells.EFFECT: invention enables to obtain tumor-specific antigen expressed by cancer cells treated by said agent, capable of immune response inducing on homologous and heterogeneous cancer cells, originating from same tissue/same organ.5 cl, 4 dwg, 1 tbl, 8 ex

New antibody to c-met // 2607377
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry, namely to monoclonal antibody, which is capable of inhibiting dimerization of c-Met. Composition for preventing and treating cancer, associated with c-Met, containing said antibody is also disclosed. Application of said antibody and composition is disclosed for preparing therapeutic agent against cancer, associated with c-Met.EFFECT: invention is capable of total inhibiting dimerization of c-Met, which enables effective treatment of cancer, characterized by ligand-independent c-Met activation.19 cl, 39 dwg, 4 tbl, 20 ex
Substituted n2-(4-amino-2-methoxyphenyl)-n4-[2-(dimethylphosphoryl)-phenyl]-5-chloro-pyrimidine-2,4-diamines as modulators of alk and egfr, applicable for treating cancer // 2607371
FIELD: chemistry.SUBSTANCE: invention relates to novel substituted N2-(4-amino-2-methoxyphenyl)-N4-[2-(dimethylphosphoryl)-phenyl]-5-chloro-pyrimidine-2,4-diamines of general formula 1 and their stereoisomers, N4-[2-(dimethylphosphoryl)-phenyl]-N2-{4-[4-(1-methyl-1,8-diaza-spiro[4.5]dec-8-yl)-piperidin-1-yl]-2-methoxyphenyl}-5-chloro-pyrimidine-2,4-diamine and their pharmaceutically acceptable salts. Compounds have anti-cancer effect and can be used for preparing a drug for preventing or treating cancer, in particular, non-small cell lung cancer (NSCLC), including with metastases in brain. In compounds of general formula 1 1, R denotes a substitute, selected from a series (a)-(o): (a)-(c), (e)-(i), (k)-(l), (m)-(o), in which R2, R3, R4 and R5 are optionally identical C1-C4alkyls; n is an optionally identical number 1 or 2; arrow indicates binding point of substitute. Invention also relates to a method of producing compounds of formula 1.EFFECT: method comprises reacting compounds of general formula 2, 1_1(17) where R is a substitute selected from corresponding substitutes given above, with N-[2-(dimethylphosphoryl)phenyl]-2,5-dichloro-pyrimidine-4-amine of formula 1_1(17).12 cl, 2 tbl, 4 ex

Pharmaceutical composition for treatment and/or prevention of cancer // 2607366
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry, particularly to an antibody which specifically binds with CAPRIN-1 protein and having immunological reactivity with respect to a partial polypeptide of CAPRIN-1 protein, wherein said antibody has cytotoxic activity against a cancer cell expressing CAPRIN-1 protein, as well as a medicinal agent containing same. Invention also relates to a method of treating or preventing CAPRIN-1 expressing cancer using said antibody or composition.EFFECT: invention provides effective treatment or prevention of CAPRIN-1 expressing cancer.17 cl, 3 dwg, 6 ex
Dichloroacetates of substituted n4-[2-(dimethylphosphoryl)phenyl]-n2-(2-methoxy-4-piperidin-1-ylphenyl)-5-chloropyrimidine-2,4-diamines as modulators of alk and egfr, intended for treating cancer // 2606951
FIELD: chemistry.SUBSTANCE: invention relates to novel compounds – dichloroacetates of substituted N4-[2-(dimethylphosphoryl)phenyl]-N2-(2-methoxy-4-piperidin-1-ylphenyl)-5-chloropyrimidine-2,4-diamine of general formula 1, which are modulators of ALK and EGFR and can be used for preventing and/or treating cancer, in particular for treating non-small cell lung cancer (NSCLC), including with metastases in brain. In formula 1 R represents dimethylamine group or 4-methylpiperazin-1-yl fragment, and k is a number 1, 2 or 3. Invention also relates to a pharmaceutical composition, containing said compound as an active component in therapeutically effective amount in combination with pharmaceutically acceptable diluent and/or carrier. Composition can be made in form of tablets, capsules or injections, placed in a pharmaceutically acceptable packaging.EFFECT: invention also relates to a method of producing a compound of formula 1 by reacting a compound of general formula 2, where R is a dimethylamine group or 4-methylpiperazin-1-yl fragment, with 1, 2 or 3 equivalents of 2,2-dichloroacetic acid.11 cl, 2 tbl, 10 ex
Substituted n-{3-[4-(1-methyl-1h-indol-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}-amides as modulators of egfr, applicable for treating cancer // 2606949
FIELD: chemistry.SUBSTANCE: invention relates to novel substituted N-{3-[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}-amides of general formula 1 and pharmaceutically acceptable salts thereof, having properties of modulators of EGFR and suitable for treating cancer, for example small cell lung cancer. In general formula 1 R1 represents CH2=C(R3)-, R3CH=CH-; R2 is (2-dimethylaminoethyl)-methylamino, 3-dimethylaminopiperidin-1-yl; R3 is fluorine, trifluoromethyl, dimethylcarbamoyl; or R2 is 3-dimethylaminopiperidin-1-yl; R3 is H; or mesylate compound 1, where R1 is C(CH3)≡C-, R2 is (2-dimethylaminoethyl)-methylamino. Preferable compounds are N-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-2-fluoro-acrylamide (1.2); N-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-4,4,4-trifluorobut-2-enamide (1.6); (E)-3-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenylcarbamoyl}-N,N-dimethylacrylamide (1.8); N-{2-(3-dimethylaminopiperidin-1-yl)-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-acrylamide (1.11); mesylate N-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-2-butynamide (1.14⋅CH3SO3H) or mesylate N-{2-(3-dimethylaminopiperidin-1-yl)-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-acrylamide (1.11⋅CH3SO3H). Invention also relates to a method of producing compounds of formula 1.EFFECT: method involves reacting a compound of formula 2 or its salt with activated derivative of corresponding organic acid, such as an acid, ester or organic acid anhydride.15 cl, 2 tbl, 14 ex

Substituted purine and 7-deazapurine compounds // 2606514
FIELD: pharmaceutics.SUBSTANCE: invention relates to compound of formula (IV) or its N-oxide, or pharmaceutically acceptable salt of such compounds, where A is O or CH2; Q is NH2, NHRb, NRbRc or OH, where each Rb and Rc independently represent C1-C6 alkyl; X is N or group CRx, where Rx is H; Y is H or Rd, where Rd is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C8 cycloalkyl, and Rd is optionally substituted with one or more substitutes, selected from group consisting of halogen and C3-C8 cycloalkyl; each of R1 and R2 is H; each of Re, Rf, Rg and Rh independently represent group -M2-T2, where M2 is bond or O-C1-C4 alkyl linker, and T2 is H, halogen or RS4, where RS4 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl or oxetanyl, and each of O-C1-C4 alkyl linker and RS4 is optionally substituted with one or more substitutes, selected from group consisting of halogen, hydroxyl, cyano, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl and C1-C6 alkoxyl; and m equals to 0, 1 or 2. Invention relates to specific compounds. Disclosed compounds are intended for producing pharmaceutical composition with antiproliferative activity, including therapeutically effective amount of compound and pharmaceutically acceptable carrier. Besides compound is applied for treating leukemia and inhibiting DOT1L-mediated protein methylation.EFFECT: substituted purine or 7-deazapurine compound effective in treating leukemia and inhibiting DOT1L-mediated protein methylation.24 cl, 1 tbl, 3 dwg, 11 ex

Pharmaceutical composition // 2606510
FIELD: pharmaceutics.SUBSTANCE: present invention relates to compounds of formula (I), in which one of R1a and R1b is hydrogen and the other is methyl; or R1a and R1b together form a cyclopropyl ring; R2 denotes methyl or monofluoromethyl, difluoromethyl or trifluoromethyl; R3 denotes methyl; R4 denotes hydrogen, halogen, monofluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy, monofluoromethoxy, difluoromethoxy or trifluoromethoxy; R5 denotes hydrogen, halogen, monofluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy, monofluoromethoxy, difluoromethoxy or trifluoromethoxy; R6 is hydrogen; R7 means hydrogen; and X denotes oxygen; or pharmaceutically acceptable salts thereof.EFFECT: compound of formula (I) inhibit the transmission of PGE/EP4 signal and can be used for treating autoimmune pathologies, such as rheumatoid arthritis, multiple sclerosis, psoriasis, cancer and other; invention also relates to pharmaceutical compositions containing these compounds, and methods for using them in the case of individuals in need of treatment.50 cl, 2 dwg, 3 tbl, 113 ex
Thiazolylphenyl-benzenesulfonamido derivatives as kinase inhibitors // 2606497
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I), where each of n and m independently equals 1; R1 is halogen or a group selected from a straight or branched (C1-C8)alkyl and heterocyclyl, selected from piperidinyl and tetrahydropyranyl, where piperidinyl is optionally substituted with (C1-C6)alkyl and (C3-C6)cycloalkyl; or R1 is NR7R8, where each R7 and R8 independently represents hydrogen or a group, selected from a straight or branched (C1-C8)alkyl, heterocyclyl, selected from piperidinyl and optionally substituted methyl; or, taken together with a nitrogen atom with which they are bonded, R7 and R8 can form optionally substituted 3-8-member heterocyclyl, optionally having one additional heteroatom or heteroatomic group selected from O, N and NH, optionally substituted with halogen; each of R2 and R3 independently represents hydrogen, halogen or optionally substituted group, selected from a straight or branched (C1-C8)alkyl and heterocyclyl, selected from imidazolidine, substituted -COCH3, -C=O, -CH2-OCH3, -CH3; or each of R2 and R3 independently represents NR17R18, where R17 and R18 independently denote hydrogen or optionally substituted group, selected from a straight or branched (C1-C8)alkyl, optionally substituted -NH-COCH3, -NHCOOCH3, -N(CH3)2; or R17 represents hydrogen and R18 represents COR22, where R22 denotes OR23 or optionally substituted group, selected from a straight or branched (C1-C8)alkyl, where R23 is straight or branched (C1-C8) alkyl, each of R4 and R5 is independently hydrogen or halogen; Rx is hydrogen; R6 denotes phenyl, optionally substituted with halogen; or a pharmaceutically acceptable salt thereof. Invention relates to a method of inhibiting activity in vitro of Raf, which involves bringing said receptor into contact with an effective amount of compound of formula (I). Compound of formula (I) or a pharmaceutically acceptable salt thereof are intended for use as a medicinal agent or in a pharmaceutical composition, with activity against a malignant tumour.EFFECT: technical result is thiazolylphenyl-benzenesulfonamido derivatives as Raf kinase inhibitors.10 cl, 1 tbl, 22 ex
ethod of measuring absorbed dose in boron neutron capture therapy of malignant tumors // 2606337
FIELD: medicine.SUBSTANCE: method relates to nuclear medicine, neurooncology, can be used in boron neutron capture therapy (BNCT) of malignant tumors. Performed an introduction to the patient a preparation of targeted delivery of boron, irradiating by the flow of epithermal neutrons and measurement of gamma-spectrometer spatial distribution of radiation intensity of gamma-quanta. Note here that preliminary preparation of targeted delivery is marked with stable atomic nucleus, which under irradiation by epithermal neutrons is activated and splits with electron emission. At the same time for measuring of spatial distribution of the absorbed dose is calculated ratio of intensity of activation of stable atomic nucleus to intensity of neutron absorption with boron, using measurement of ratios of boron concentrations and target nucleus for radiation capture of neutrons and measurement induced activity after irradiation. Gamma-spectrometer can be located outside the room, where irradiation is carried out. As a reagent with a stable atomic nucleus, activated under action of epithermal neutrons is used gold or indium.EFFECT: method provides the accurate determination of the absorbed dose of neutrons and its spatial distribution in the tumor.3 cl, 1 tbl
Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors // 2606131
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula I given below, or to their stereoisomers, tautomers or pharmaceutically acceptable salts thereof. R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and ring C are as defined by the invention formula. Wherein the Y-B moiety and the NH-C(=X)-NH moiety are in the trans configuration.EFFECT: compounds of formula I are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.56 cl, 31 tbl, 649 ex
ethod of brachytherapy for localised prostate cancer // 2606108
FIELD: medicine.SUBSTANCE: invention refers to medicine, oncology, urology, radiology, methods of registration auto fluorescence of tissues for more efficient use of low-dose brachytherapy of localised forms of malignant tumors of the prostate gland. Implantation is carried out at ultrasound control of microcapsules with radionuclide I-125 by trans-perineal access in prostate tumor tissue by template with holes with a pitch of 5 mm. Previously at the beginning of operation through the holes of the template is introduced in prostate tissue a diagnostic catheter for registration of auto fluorescence. Determined amount of centers of auto fluorescence typical for tumor tissue, and their boundaries. According to this data is determined the radiation dose, number of microcapsules and nature of their distribution at implantation.EFFECT: method allows more precise and specifically explore a whole volume of the body, exclude the possibility of passage of prostate parenchyma sections at its complex anatomical structure or considerable dimensions, as well as use the obtained value for target distribution of micro sources and calculation of necessary doses to avoid bringing excess radiation effect on the surrounding healthy tissues, reduce rate of developing early and late radiation complications.1 cl, 3 ex

Aldehyde marked immunoglobulin polypeptides and methods of their application // 2606016
FIELD: biotechnology.SUBSTANCE: present invention relates to biotechnology, namely to producing aldehyde marked antibody for conjugation with drug of interest, and can be used in medicine. Obtained antibody can be modified with formylglycine-forming enzyme to make 2-formylglycine modified (FGly) antibody, which can be covalently and site specificly is conjugated with target fragment.EFFECT: invention enables to obtain conjugate, capable of directed delivery in antigen expressing body tissues.60 cl, 33 dwg, 3 ex

Therapeutic dll4-binding proteins // 2605928
FIELD: medicine.SUBSTANCE: present invention relates to immunology. Antibody and its antigen-binding fragment specifically binding human delta-like ligand 4 (DLL4) are presented, characterized by sequences determining sections complementarity (CDR). Besides, there are disclosed: isolated antibody coding nucleic acid under the invention or its antigen-binding fragment; expression vector and host cell; as well as, pharmaceutical composition and application of antibody or antigen-binding fragment according to the invention in preparing a drug for reducing human DLL4 activity in an individual human.EFFECT: present invention can find further application in therapy of diseases associated with Notch signaling.29 cl, 30 tbl, 13 ex

N,n'-bis(3-bromopropionyl)-n,n'-dimethyl-1,2-ethylenediamine, method for production thereof and use thereof as water-soluble reagent, having anti-tumour properties // 2605603
FIELD: chemistry.SUBSTANCE: invention relates to N,N'-bis(3-bromopropionyl)-N,N′-dimethyl-1,2-ethylenediamine of formula 1. Disclosed compound is obtained by treatment of derivatives of 3-bromopropionic acid with N,N′-dimethyl-1,2-ethylenediamine in presence of bicarbonates of alkali metals.EFFECT: technical result is N,N'-bis(3-bromopropionyl)-N,N′-dimethyl-1,2-ethylenediamine as water-soluble anticancer agent.2 cl, 5 tbl, 8 ex

Salts of 4-methyl-n-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-ylpyrimidine-2-ylamino)benzamide // 2605551
FIELD: chemistry.SUBSTANCE: invention relates to novel salts of 4-methyl-N-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-yl-pyrimidine-2-ylamino)benzamide (nilotinib), which have protein kinase inhibitor properties and can be used for treating diseases responding to protein kinase activity inhibition. Salts are selected from hydrochloride, diphosphate, sulphate, methanesulphonate, ethanesulphonate, benzolesulphonate and n-toluene sulphonate. Method involves the stage for reacting 4-methyl-N-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-yl-pyrimidine-2-ylamino)benzamide in the form of a free base with the corresponding acid of formula HB selected from the said acids in a solvent medium. Invention also relates to a pharmaceutical composition containing: (a) a therapeutically effective amount of the salt and (b) at least one pharmaceutically acceptable carrier, a diluent, an adjuvant or an excipient.EFFECT: method of treating involves introducing a patient requiring such treatment a therapeutically effective amount of the said salt, or monohydrate of monohydrochloride, or a monophosphate salt of 4-methyl-N-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-yl-pyrimidine-2-ylamino)benzamide.13 cl, 8 dwg, 17 tbl, 11 ex

Novel thieno-pyrimidine derivatives, method for production thereof and pharmaceutical compositions containing them // 2605403
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I): (I), in which: A is a linear or a branched (C1-C6)alkyl group, a linear or a branched (C1-C6)alkoxy group, a -S-(C1-C6)alkyl group, a linear or a branched (C1-C6)polyhalogen-alkyl group, a hydroxy group, a cyano group or a halogen atom; R1, R2, R3, R4 and R5 independently denote a hydrogen atom, a halogen atom, a linear or a branched (C1-C6)alkyl group, a linear or a branched (C2-C6)alkenyl group, a linear or a branched (C2-C6)alkynyl group, a linear or a branched (C1-C6)polyhalogen-alkyl group, a hydroxy group, a linear or a branched (C1-C6)alkoxy group, a -S-(C1-C6)alkyl group, a nitro group, -alkyl(C0-C6)-NR8R8′, -O-Cy1, -alkyl(C0-C6)-Cy1, -alkenyl(C2-C6)-Cy1, -alkynyl(C2-C6)-Cy1, -O-alkyl(C1-C6)-R9, -C(O)-OR8, -O-C(O)-R8, -NR8-C(O)-R8′, -NR8-C(O)-OR8′, -alkyl(C1-C6)-NR8-C(O)R8′; X represents a carbon or a nitrogen atom; R6 represents hydrogen, a linear or a branched (C1-C8)alkyl group, an aryl group, heteroaryl-alkyl(C1-C6); R7 is a linear or a branched (C1-C6)alkyl group, a linear or a branched (C2-C6)alkenyl group, a linear or a branched (C2-C6)alkynyl group, -Cy3, -alkynyl(C2-C6)-Cy3,-Cy3-Cy4, -alkynyl(C2-C6)-O-Cy3, -Cy3-alkyl(C0-C6)-O-alkyl(C0-C6)-Cy4, a halogen atom, a cyano group, -C(O)-R11, -C(O)-NR11R11′, values of other radicals are defined in cl.1 of the formula.EFFECT: compounds can be used as pro-apoptotic agents.50 cl, 2 tbl, 871 ex

Bispecific antibodies specific for t-cell activating antigens and a tumor antigen and methods of use // 2605390
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine and concerns a bispecific antibodies that specifically bind a T-cell activating antigen and a tumor antigen (TA), comprising a first Fab fragment and a second Fab fragment, wherein either the variable regions or the constant regions of the second Fab heavy and light chain are exchanged; and wherein the bispecific antibody does not comprise a Fc domain, so that the constant region of the heavy chain consists of one or more CH1 domains. Group of inventions also relates to a host cell, comprising vectors comprising nucleic acid molecules, encoding the light chains and heavy chains of the bispecific antibody; application of bispecific antibody in preparing a drug for treating cancer.EFFECT: group of inventions provides inducing T cell-mediated apoptosis of target cells.19 cl, 9 ex, 23 dwg, 1 tbl

Agent for inhibiting human tyrosyl-dna-phosphodiesterase 1 enzyme // 2605329
FIELD: biochemistry.SUBSTANCE: invention relates to molecular biology, biochemistry, biotechnology and chemical-pharmaceutical industry, and represents an agent, which is one of enamine derivatives of usnic acid of general formula I; , where R - an aromatic substitute, which contains a halogen or hydroxy and tert-butyl substitutes, attached to the nitrogen atom directly or via ethyl or propyl linker, showing inhibitory activity against enzyme tyrosyl-DNA-phosphodiesterase of 1 person.EFFECT: invention provides increasing of inhibitory activity on enzyme tyrosyl-DNA-Phosphodiesterase of 1 person (Tdp1) and wider range of inhibitors of this enzyme.1 cl, 1 dwg, 1 tbl, 13 ex

Fraction of dna-hydrolyse secretory immunoglobulins of class a, with selective apoptotic activity in relation to human cancer cells // 2605321
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry. Purposed a fraction of DNA-hydrolyse secretory immunoglobulins of class A (sIgA), having molecular weight 380 kDa, processing selective apoptotic activity in relation to human cancer cells, extracted from milk of healthy donors by affinity chromatography on protein-A-sepharose, then ion-exchange chromatography on DEAE-cellulose, then by affinity chromatography on DNA-cellulose.EFFECT: invention enables to inhibit cancer cell growth on the way of apoptosis without inducing death of normal (non-tumorous) cells.1 cl, 7 dwg, 1 tbl, 3 ex

Formulation, kit and a pharmaceutical composition containing decitabine derivatives, production and use thereof // 2605289
FIELD: medicine.SUBSTANCE: series of inventions relates to medicine. Derivatives of decitabine with superior chemical stability and shelf life, with similar physiological activity are described. Methods for treating one or more myelodysplastic syndromes, leukemia, or solid tumours using the formulations are described. Derivatives of decitabine are provided in a non-aqueous formulation, which further stabilizes the derivatives.EFFECT: derivatives of decitabine are described.34 cl, 4 dwg, 5 tbl, 4 ex

New combination comprising n-acetyl-l-cysteine and its use // 2605287
FIELD: pharmaceutics.SUBSTANCE: group of inventions refers to pharmaceutics and concerns a medical agent containing a combination of N-acetyl-L-cysteine, selenium in the form of selenomethionine and melatonin. Described product can be used for treating carcinoma, dermatological diseases, chronic obstructive pulmonary disease (COPD), amyloidosis, endometriosis and bacterial infections caused by E.coli., for cosmetic treatment of skin, as well as an antibacterial agent with medical device adapted for use in contact with body fluids.EFFECT: group of inventions provides a synergetic effect at preservation of N-acetyl-L-cysteine, favorable effect on treating COPD, endometriosis, amyloidosis, dermatological diseases and skin states, such as vitiligo, psoriasis, alopecia, seborrheic dermatitis, as well as improved oral absorption.12 cl, 9 dwg, 1 tbl, 5 ex

Biomarkers based on tumor tissue for combined therapy with bevacizumab // 2605282
FIELD: medicine.SUBSTANCE: group of inventions refers to medicine, namely to oncology, and is intended for increasing survival without progression of disease in patient suffering colon or rectum metastatic cancer. For implementation of method, tissue samples are obtained from above patient, VEGFA and/or CD31 expression is determined, and Bevacizumab combined with chemotherapy schedule is administered to patient. Patient therein has higher level of VEGFA and/or CD31 relative to reference levels defined in patients with colon or rectum metastatic cancer. Said chemotherapy schedule represents oxalic platinum chemotherapy schedule. Also, in vitro method is provided for detecting patients responding or sensitive to adding Bevacizumab for treatment to chemotherapy schedule.EFFECT: application of invention group allows to increase survival rate of patients with colon or rectum metastatic cancer without progression of disease.15 cl, 8 dwg, 4 tbl, 1 ex

2-amino-1-aryl-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-n-(thiazol-5-yl)-4,5-dihydro-1h-pyrrole-3-carboxamides, exhibiting antitumour and antiradical activity, synthesis method thereof and pharmaceutical composition based thereon // 2605091
FIELD: chemistry.SUBSTANCE: invention relates to compounds of general formula I, where R represents a C6-C10 aryl, optionally substituted with one or more halogen atoms, or its pharmaceutically acceptable salts. Compounds of general formula I are obtained by reacting 4-R-amino-2-tert-butyl-2,5-dihydro-5-oxofuran-2-ylacetate (III) and 2-cyano-N-(thiazol-2-yl)acetamide in the presence of triethylamine. Initial reagents 4R-amino-2-tert-butyl-2,5-dihydro-5-oxofuran-2-ylacetate (III) and 2-cyano-N-(thiazol-2-yl)acetamide are taken in equimolar amount. Triethylamine is taken in an amount from equimolar to two-fold excess with respect to 2-cyano-N-(thiazol-2-yl)acetamide and 4R-2-tert-butyl-2,5-dihydro-5-oxofuran-2-ylacetate. Reaction takes place in a medium of benzene. Invention also relates to a pharmaceutical composition having antitumour and antiradical activity, containing as an active ingredient a compound of general formula I or its pharmaceutically acceptable salt in a pharmaceutically active amount and a pharmaceutically acceptable filler. Compounds of formula I are intended for producing drug preparations for treating oncological diseases.EFFECT: 2-amino-1-aryl-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-N-(thiazol-5-yl)-4,5-dihydro-1H-pyrrol-3-carboxamides, exhibiting antitumour and antiradical activity.17 cl, 2 tbl, 2 dwg, 5 ex

Chemical synthesis and anticancer and antimetastatic effects of dual functional conjugate // 2604718
FIELD: chemistry.SUBSTANCE: invention relates to dual functional conjugate of formula i, where docetaxel is linked with muramyl dipeptide derivative, which enables to achieve anticancer and antimetastatic effect. Method of producing conjugate is carried out by combination of solid-phase and liquid-phase synthesis.EFFECT: invention also discloses a pharmaceutical composition and use of conjugate for producing anti-tumour drugs.21 cl, 29 dwg, 13 tbl, 51 ex

Design of stable heterodimeric antibody with mutations in fc domain // 2604490
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry. Carcasses are described, which contain heavy chains, being asymmetric in different domains (for example, CH2 and CH3), to achieve selectivity between different Fc receptors involved in modulation of effector function, higher selectivity than selectivity, achieved when using natural homodimeric (symmetrical) Fc molecules, and increased stability and purity of produced alternative Fc homodimers as a result.EFFECT: these new molecules contain complexes of heterogeneous components formed in order to change the behavior of natural antibodies and their use in medicinal agents.80 cl, 38 dwg, 12 tbl, 8 ex
ethod of therapy of malignant growths // 2604409
FIELD: medicine.SUBSTANCE: invention relates to medicine, namely to oncology, and can be used in treating malignant growths. Method involves chemotherapy and subcutaneous injection of Enoxaparin sodium. Before the beginning of chemotherapy patient's peripheral blood is examined to determine the level of D-dimer and if its value in the range of 1-3, 8 mcg/kg introduction of Enoxaparin sodium is prescribed in an amount of 15-25 mg for 7-10 days, and if a value of 3.9-6.5 mcg/ml introduction of Enoxaparin sodium is prescribed in an amount of 35-45 mg for 7-10 days, in determining the pre-therapeutic value of D-dimer above 6.5 mcg/ml, prescribed the introduction of Enoxaparin sodium in an amount of 35-45 mg/kg for 10-14 days. Then on the last day of injection of Enoxaparin sodium is again determined level of D-dimer and if the value below 1 mcg/ml, further therapy by Enoxaparin sodium not continued, if determining the level of d-dimer equal to and above 1 mcg/ml, repeated therapy by Enoxaparin sodium is described in accordance with the above values of D-dimer.EFFECT: using the invention enables to increase clinical effectiveness of treatment ensured by individual daily dosage of Enoxaparin sodium and reduce a risk of profuse bleeding.1 cl, 3 ex

Antibodies to cd70 // 2604196
FIELD: medicine.SUBSTANCE: present invention relates to immunology. Antibody and its antigen-binding fragment are proposed, binding to human CD70, which are characterized by amino acid sequences of CDR variable domains of heavy and light chains. Extracted polynucleotide, coding antibody or antigen-binding fragment according to invention, as well as expression vector, host cell, cell-free expression system and method of producing antibody or its antigen-binding fragment, according to the invention are disclosed. Pharmaceutical composition, method of tumor cell growth inhibiting and method of exhaustion of CD70-expressing cells in patient are also disclosed.EFFECT: present invention can find further application in therapy and diagnosis of diseases, namely cancer and autoimmune diseases characterized by CD70 expression.27 cl, 24 dwg, 29 tbl, 21 ex

Pyrazine derivatives used as atr kinase inhibitors // 2604066
FIELD: chemistry.SUBSTANCE: present invention relates to pyrazine compounds , used as inhibitors of ATR protein kinase, pharmaceutical compositions containing compounds according to invention, and use of compounds according to present invention to increase cell sensitivity to DNA damaging agents and as a radio-sensitiser and a chemo-sensitiser.EFFECT: high sensitivity of cells to DNA damaging agents, radio-sensitiser and chemo-sensitiser.115 cl, 98 dwg, 18 tbl, 77 ex
ethod for producing preparation on basis of interaction between trans-dichlorodiammineplatinum (ii) with arabinogalactan // 2604030
FIELD: pharmaceutics.SUBSTANCE: invention relates to production of chemical-pharmaceutical preparations with biological activity. Method of producing preparation is described on basis of interaction of aqueous solution of platinum complex compound with 50 % water solution of arabinogalactan, while heating in water bath, filtration and settling in alcohol, characterized by fact, that trans-dichlorodiammineplatinum (II) is used as complex compound, wherein reaction is carried out, while heating for 30 minutes, in molar ratio of initial substances 1:1.EFFECT: technical result is obtaining medication on basis of interaction between trans-dichlorodiammineplatinum (II) and arabinogalactan with anticancer activity, higher water solubility and low toxicity.1 cl, 2 ex

Dichloroacetate of n1,n2-disubstituted n4-[4-(1-methyl-1h-indole-3-yl)-pyrimidine-2-yl]-5-methoxybenzene-1,2,4-triamine as egfr modulator for treating cancer // 2603960
FIELD: chemistry, medicine.SUBSTANCE: invention relates to novel salt - dichloroacetate N-{2-[(2-dimethylaminoethyl)methyl-amino]-5-[4-(1-methyl-1H-indole-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}acrylamide, which has properties of EGFR inhibitor and can be used for treating cancer types, mediated by EGFR and its mutants selected from L858R, 1790M and Exon19. Compound may be used for treating ovarian cancer, cervical cancer, colorectal cancer, breast cancer, pancreatic cancer, glioma, glioblastoma, prostate cancer, melanoma, leukemia, non-Hodgkin lymphoma, stomach cancer, lung cancer and hepatocellular cancer, gastrointestinal stromal tumors (GIST), thyroid cancer, bile duct cancer, endometrial cancer, renal cancer, anaplastic large cell lymphoma, acute myeloid leukemia, multiple myeloma, melanoma and mesothelioma. Preferably compound can be used for preventing and/or treating mutations of epidermal growth factor receptor EGFRm of non-small cell lung cancer (NSCLC), which also have resistent mutation T790M. N-{2-[(2-dimethylaminoethyl)methyl-amino]-5-[4-(1-methyl-1H-indole-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}acrylamide dichloroacetate corresponds to general formula 1.EFFECT: prevention and/or treatment of mutations of epidermal growth factor receptor EGFRm in non-small cell lung cancer (NSCLC).12 cl, 2 tbl, 6 ex

Crystalline γ-modification of n-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinoline amine of bis (4-methylbenzenesulfonate) monohydrate, method of its production and pharmaceutical composition based thereon // 2603943
FIELD: pharmaceutics.SUBSTANCE: invention relates to novel crystalline anhydrous modification N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinoline amine of bis (4-methylbenzenesulfonate) monohydrate (lapatinib ditosylate monohydrate), in particular γ-modification, characterized by certain set of diffraction maxima (d, Å) and their intensity (Irelative, %) and certain thermal effects and their temperatures on curve of differential scanning calorimetry, as well as to method of its production and use in pharmaceutical compositions as reversible selective inhibitor of intracellular tyrosine kinase receptor of epidermal growth factor for treating advanced and/or metastatic breast cancer.EFFECT: increased biological activity.4 cl, 5 dwg, 3 tbl, 4 ex

Pharmaceutical composition of taxoids // 2603833
FIELD: pharmaceutics.SUBSTANCE: present invention relates to a stable oral pharmaceutical composition of taxoid for administering to mammals, comprising: taxoid selected from paclitaxel or docetaxel or pharmaceutically acceptable salts thereof; solubiliser selected from diethylene glycol monoethyl ether (Transcutol HP) and glycofurol; stabilising agent selected from piperine, graft copolymer of polyvinyl caprolactam - polyvinyl acetate - polyethylene glycol (Soluplus), polyvinylpyrrolidone and hydroxypropyl methylcellulose; surfactant selected from capryl/caproyl macrogol glycerides, alpha-tocopheryl-polyethylene glycol 1000 succinate, polysorbate and PEG hydrogenated castor oil and combinations thereof; solvent selected from propylene glycol and ethyl alcohol and combinations thereof; and oil selected from 1) triglycerides of fatty acids with average chain length, such as fractionated coconut oil, caprylic/capric acid triglycerides, 2) esters of fatty acids and monovalent alkanols, selected from isopropyl myristate, isopropyl palmitate, ethyl linoleate and ethyl oleate, and 3) two esters of fatty acids and propylene glycol, selected from propyleneglycol dicaprylate, propyleneglycol dilaurate; where weight ratio of solubiliser: taxoid and stabilising agent: taxoid varies from 3 to 12.5 and from 0.5 to 3.3 respectively.EFFECT: invention enables to produce a stable pharmaceutical composition exhibiting improved bioavailability and solubility.9 cl, 11 ex, 9 tbl, 1 dwg

Family of aryl, heteroaryl, o-aryl and o-heteroaryl carbasugars // 2603769
FIELD: pharmaceutics.SUBSTANCE: present invention relates to a compound and its pharmaceutically or cosmetically acceptable salts, used as an inhibitor of sodium-dependent glucose co-transporter, antioxidant and for depigmenting the skin in medicine and cosmetology, of the following formula (I): , as well as methods of its production and compositions based thereon, where n, m and p are independently 0 or 1, R denotes CH2OH or CH2OR11,R1 and R2 are OH or OR15, R3 is OH or OR18, R4 is a hydrogen atom, when n=1, or a hydrogen atom, a halogen atom or OH group, when n=0; X1 is a hydrogen atom, halogen atom, OH group, (C1-C6)-alkyl or OR24; U, V and W denote phenyl, pyrazolyl, N-(C1-C6)alkyl-pyrazolyl or thienyl optionally substituted by one or more substitutes selected from a halogen atom, OH, (C1-C6)-alkyl and OR24; R11, R15 and R18 are aryl-(C1-C6)-alkyl and R24 is (C1-C6)-alkyl or aryl-(C1-C6)-alkyl. In the proposed methods a compound of formula (II) is fluoridated, or compounds of formulae (VIII) and (XI) , are bound, wherein OH group in position of R4 in the binding product of formula (I) is optionally substituted by halogen, or the compound of formula (I) is bromated with subsequent reconstruction, or a compound of formula (XVI) is associated with a compound of formula (V), where R, R1, R2, R3, X1, U, V, W, n, m and p are given above, A1 is -Li or -Mg-Hal, Hal is a halogen atom, R9 is a leaving group.EFFECT: new agent is disclosed which is suitable for bleaching and depigmentation of skin, as an antioxidant, for inhibition of sodium-dependent glucose co-transporter, such as SGLT1, SGLT2 and SGLT3, and diseases, where such inhibition is effective, in particular in the treatment or prevention of diabetes and diabetes-related complications.21 cl, 69 ex, 11 dwg

Immunoglobulins k human cd52 // 2603743
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry. Disclosed are versions of a monoclonal antibody against human CD52. Invention also discloses isolated nucleic acids and recombinant expression vectors, coding an antibody or a light chain or a heavy chain of antibody against human CD52, host cells, as well as method of producing said antibody. Antibodies against human CD52 can be used for therapeutic purposes for treating, for example, an autoimmune disease, cancer, non-Hodgkin lymphoma, multiple sclerosis and chronic lymphocytic leukaemia.EFFECT: invention increases antibody-dependent cell-mediated cytotoxicity of antibodies against human CD52.45 cl, 246 dwg, 29 tbl, 70 ex

Pharmaceutical composition for treatment and/or prevention of cancer // 2603742
FIELD: biochemistry.SUBSTANCE: invention relates to biochemistry, particularly to an antibody which specifically binds to CAPRIN-1 protein. Invention also discloses a monoclonal antibody having immunological reactivity to CAPRIN-1 protein, antibodies which specifically bind with CAPRIN-1 protein, a medicinal agent containing said antibodies for treating or preventing CAPRIN-1 expressing cancer. Disclosed are methods of treating or preventing CAPRIN-1 expressing cancer, using disclosed antibody and said medicinal agent.EFFECT: invention is capable of specifically binding to CAPRIN-1, which provides effective treatment of diseases associated with expression of CAPRIN-1 protein.16 cl, 2 dwg, 7 ex

Treatment of pharmacologically induced hypacidity // 2603462
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine and is intended for treating hyperproliferation diseases and increasing bioavailability of preparation for hyperproliferation disease treating. Patients receiving simultaneously acidity reducing agents, such as proton pump inhibitors, and PI3K inhibitor, compound GDC-0941, on this therapy background preparations for repeated acidification are prescribed.EFFECT: group of inventions allows improving of GDC-0941 bioavailability.10 cl, 10 dwg, 1 tbl, 7 ex

Cyclic peptides with antineoplastic and antiangiogenic activity // 2603286
FIELD: biochemistry.SUBSTANCE: present invention relates to biochemistry, particularly to a cyclic peptide possessing antineoplastic and antiangiogenic activity, having one of SEQ ID NO: 1-76. Present invention discloses a pharmaceutical composition, a pharmaceutical combination and use of said cyclic peptide for treating malignant growths or disorders associated with undesirable cell proliferation or undesirable angiogenesis. Pharmaceutical combination of said cyclic peptide in concentration of 12.5-200 mcM with anticancer drug in concentration of 1-2,000 nM has high antineoplastic activity. Present invention discloses means for diagnosis of malignant new growths, comprising a cyclic peptide and radiopharmaceutical agent, for example fluorescent particle.EFFECT: present invention widens range of means of controlling malignant new growths.14 cl, 21 dwg, 8 tbl, 21 ex

Diethyl(3,5-bis(arylidene)-4-oxopiperidin-1-yl)-(aryl)-methylphosphonates having antiproliferative properties // 2603194
FIELD: chemistry.SUBSTANCE: invention relates to diethyl(3,5-bis(arylidene)-4-oxopiperidin-1-yl) (aryl)methylphosphonates, which can be used in medicine, of general formula 1:in which R1=H, F, OMe; R2=H, F.EFFECT: are disclosed novel diethyl(3,5-bis(arylidene-4-oxopiperidin-1-yl)(aryl)methylphosphonates with antiproliferative properties and low acute toxicity for treating oncological diseases, including rhabdomyosarcoma, intestinal carcinoma, adenocarcinoma of mammary gland.5 cl, 1 tbl, 4 ex

Crystalline form of hidamide, method of its production and use // 2603138
FIELD: chemistry.SUBSTANCE: invention refers to pharmaceutical chemistry and discloses two crystalline forms of hidamide, in particular, crystalline form A of hidamide and crystalline form B of hidamide, as well as a method of producing crystalline forms A and B of hidamide, use thereof and a pharmaceutical composition based thereon.EFFECT: technical result is obtaining crystalline forms A and B of hidamide, which have low toxicity, stability during storage and processing, and also have the advantage in oral use and inhibiting the cell differentiation and proliferation.7 cl, 8 dwg, 8 ex

5-hydroxy-1h-imidazole-4-carboxamide sulphate // 2603137
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to 5-hydroxy-1H-imidazole-4-carboxamide sulphate and its crystalline forms. Invention also relates to a pharmaceutical composition based on α-form, β-form or γ-form of 5-hydroxy-1H-imidazole-4-carboxamide sulphate.EFFECT: obtained crystalline forms of 5-hydroxy-1H-imidazole-4-carboxamide sulphate, having useful biological activity, as well as such characteristics, as reduced blue staining, high degree of purity, low water absorption and excellent stability during storage.10 cl, 10 dwg, 6 tbl, 9 ex

Antibodies to polyubiquitin and methods of application thereof // 2603093
FIELD: medicine.SUBSTANCE: present invention relates to immunology. Monoclonal antibody and its fragment are presented, which bind with K11-associated polyubiquitin, characterized by amino acid sequences of hypervariable sections (HVR). Isolated nucleic acid, which codes antibody, according to invention; expression vector; host cell and method of producing antibody are also described. Moreover, immunoconjugate and pharmaceutical composition for treating disease or disorder, containing antibody, according to invention; use of disclosed antibody for preparing drug; method of treating individual, suffering from disease or disorder, selected from cancer, degenerative muscle or nerve disorder; as well as method of determining presence of K11-associated polyubiquitin or polyubiquitinated protein; method of separating K11-associated polyubiquitinated protein and method of determining function and/or activity of K11-associated polyubiquitin are proposed.EFFECT: present invention can find further application in therapy and diagnostics of diseases, associated with formation of polyubiquitins, containing bond, formed K11 lysine.46 cl, 9 dwg, 5 tbl, 3 ex

Combination of sirosingopin and mitochondrial inhibitors for treatment of cancer and for immunosuppression // 2602937
FIELD: medicine.SUBSTANCE: group of inventions is related to medicine, pharmacology, pharmaceutics, and involves a pharmaceutical composition and combination of sirosingopin (SS) and mitochondrial inhibitor (MI), where the said mitochondrial inhibitor represents metformin or fenformin. Ratio of the amount of (wt/wt) CC and MI can range from 1 to 10-1 to 1000. This combination can be used in treating such types of cancer as carcinoma, sarcoma, leukaemia, myeloma, lymphoma, various types of cancer of the nervous system or autoimmune diseases of skin, nervous system, connective tissue, muscles, blood, bone tissue and internal organs, as immunosuppressive therapy. Group of inventions also includes the method of determining if the cancer cell is sensitive to the SS. For this purpose, (a) a suspension of single cells cultivated cancer cells in acceptable media is received; (b) the cancer cell is incubated with SS; (c) the cancer cell obtained at step (b) is incubated with positively charged fluorescent dye; (d) the fluorescence excited intensity is measured; and (e) fluorescence intensity, measured at step (d) is compared with the intensity of fluorescence of the cancer cell to be incubated only with positively charged fluorescent dye. Relative increase in fluorescence intensity of cancer cells, preliminary incubated with SS, means that cells are sensitive to treatment with SS. Group of inventions also includes a method of treating cancer or autoimmune disease by administration of a combination or a composition of SS and the said MI to a warm-blooded animal in the amount effective with respect to the aforementioned disease.EFFECT: said combination and composition provide a synergetic effect when used regarding the aforementioned disorders, the prognosis of which, in its turn, can be provided for implementation of the above method for prognosis of cancer cell sensitivity to SS.14 cl, 12 dwg, 1 ex, 1 tbl
 
2551396.
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