Antineoplastic agents (A61P35)

Method of treating bone tumours and tumour-like bone disorders

Invention refers to medicine, namely bone oncology, and can be used for treating bone tumours and tumour-like bone disorders. That is ensured by separating a pathological focus, excising the tumour or tumour-like disorder, performing a cryoexposure on the post-excision bone defect three times and closing the wound. The cryoexposure is ensured by 'Medical Cryoapplicator' by placing its balls on a surgical suture into the post-excision bone defect and cooling with liquid nitrogen for 10-60 s. That is followed by thawing in normal saline heated to plus 38°C. After the three cryoexposures, 'Medical Cryoapplicator' is removed. A post-excision defect is repaired if indicated.

Bcg-based immunobiological medication for urinary bladder cancer therapy and method for thereof application

Group of inventions deals with BCG-based immunobiological medication of treating urinary bladder cancer, which additionally contains enzyme or enzymes with provision of cleavage of secretion of urinary bladder mucosa membrane and buffer, taken in therapeutically effective ratio. Group of inventions also deals with method for application of immunobiological medication for treating urinary bladder cancer, consisting in introduction of said immunobiological medication into urinary bladder.

Novel compounds and compositions for targeting at malignant stem cells

Invention relates to polymorphs, namely to polymorph 2-acetyl-4H,9H-naphto [2,3-b]furane-4,9-dione, characterised by X-ray diffraction pattern, in fact similar to the one on fig.2, and polymorph of 2-acetyl-4H,9H-naphto [2,3-b]furane-4,9-dione, characterised by X-ray diffraction pattern, in fact similar to the one, given on fig. 3, naphthofurane compounds in form of particles, pharmaceutical compositions for treating cancer, containing one or several naphthofurane compounds, purified compositions for treating cancer, containing one or several said naphthofurane polymorphs in form of particles, methods for obtaining said naphthofurane polymorphs, method for treating cancer in subjects requiring it and method for prolongation of progression-free survival (PFS) in patient with cancer with application of said naphthofurane compounds.

Method and composition

Group of inventions refers to pharmaceutics. What is described is an aqueous pharmaceutical solution containing 2-(hydroxymethyl)-2-(methoxymethyl)quinuclidin-3-one or its pharmaceutically acceptable salt and pH-controlling agent. The above agent is specified in pharmaceutically acceptable organic or inorganic acids, pharmaceutically acceptable acid buffers or any mixture thereof. What is also described is using the above aqueous pharmaceutical solution for producing a drug for treating a disease specified in hyperproliferative diseases, autoimmune diseases and cardiac diseases.

Specific combined therapy of malignant tumours with cytostatic agent and its modifying agent

One or more cytostatic agents are administered in an amount of 1/4 to Ѕ of a standard therapeutic dose, which is followed by a subcutaneous administration of N-acetyl-D-glucoaminyl-β-(1-4)-N-acetylmuramyl-L-alanyl-D-glutamic acid (GMDP-A) in an effective amount once a day for 4-20 days.

Humanized immune bodies for cxcr5, their secondaries, and their use

Options of selected immune body or its fragment are suggested, they are specifically linked with outer domain CXCR5 of person. Described: pharmaceutical composition and options of the patient treatment using said immune body or its fragment for treatment of the disease or state being result of or linked with CXCR5 of person. The selected coding molecule of nucleic acid, expression vector of its bases, and host cell for expression of the immune body or its fragment containing the said vector are suggested.

New therapeutic methods for using inecalcitol

What is presented is using inecalcitol for treating and/or preventing rachitis, osteoporosis, osteomalatia, psoriasis, autoimmune diseases, such as multiple sclerosis, type I diabetes mellitus, hyperparathyroid, benign prostate hyperplasia, any kinds of cancer in doses containing from 1.5 mg/day to 4 mg at intervals specified in: every second day, once a day or twice a day.

Humanised antibodies to cdcp1

Claimed invention relates to the field of biotechnology and discloses a group of humanised recombinant antibodies, which specifically bind with human CDCP1. The claimed invention also discloses a nucleic acid, which codes an antibody, an expression vector, which contains the claimed nucleic acid and a prokaryotic or eukaryotic host cell, intended for obtaining the claimed antibodies. The method of obtaining the claimed antibodies with the application of the claimed host cell is described. A pharmaceutical composition for cancer treatment, characterised by the super-expression of CDCP1, is obtained by the application of the said antibody as the active one.

Specific linking agents against b7-h1

Variational extracted antibodies 2.9D10, 2.7A4, 2.14H9 and 2.14H9-opti and their antigen-binding fragments are presented which specifically link with B7-H1 where each antibody or its antigen-binding fragment contains the set of 6 CDRs the sequences of which are presented in the description. The following is described: nucleinic acid, coding the named antibody, and the host cell producing the named antibody against B7-H1, transfected by the vector containing the named nucleinic acid. The compositions containing the effective amount of the antibody according to the present invention and pharmaceutically acceptable carrier for use in repression of B7-H1-mediated inhibition of animal T-cells are described. The following is offered: the method of repression of B7-H1-mediated inhibition of animal T-cells and the method of treatment of malignant tumour of animals connected with B7-H1, comprising injection to the animal which needs it of effective amount of the named composition.

Spiroindolinone pyrrolidines, useful when treating malignant growths

Invention relates to organic chemistry, and specifically to novel spiroindolinone pyrrolidine derivatives of general formula or pharmaceutically acceptable salts and enantiomers thereof, where X is selected from a group which includes Cl and Br, Y is selected from a group which includes F, Cl and Br, R1 is a substituted lower alkyl selected from: where R9, R10 are both a methyl; R11 is (CH2)q-R12; R12 is selected from hydrogen, hydroxyl; q = 1 or 2; R2 is selected from a group which includes phenyl, phenyl substituted with 1-3 substitutes, heteroaryl and heteroaryl substituted with 1-2 substitutes, where the heteroaryl is selected from pyrrolyl, pyrazolyl, furanyl, thiophenyl, thiazolyl, pyridinyl, pyrimidinyl, benzothiophenyl; where the substitutes for the substituted phenyl and the substituted heteroaryl are selected from a group which includes hydrogen, lower alkyl, halogen, CN, NH2, N(H, lower alkyl), N(lower alkyl)2, aminocarbonyl, lower dialkylaminocarbonyl, carboxy, NO2, lower alkoxy, lower alkylsulphonyl, lower alkylcarbonyl, lower alkoxycarbonyl, lower alkylcarbonyl-NH, lower alkoxycarbonyl-lower alkoxy, lower alkylcarbonyl-oxy-lower alkoxy, carboxy-lower alkoxy, hydroxy-lower alkoxy, lower alkyl-thio-lower alkoxy, lower alkylsulphonyl-lower alkoxy, aminocarbonyl-lower alkoxy, lower alkylthionyl-lower alkoxy, halogen-lower alkoxy, dimethylmorpholine, morpholine, tetrazole, lower alkylsulphonylamino, hydroxy-lower alkylcarbonyl, morpholine-4-sulphonyl, tetrahydropyranoxy, -NH-CH2-COOH, -NH-CH2-COOEt, -CONH-CN, oxo-group and lower alkyl, which is substituted with one substitute selected from hydroxy, lower alkoxycarbonyl, lower alkylcarbonyl, carboxy, aminocarbonyl; R3, R4, R5 are selected from H or F under the condition that at least two of R3, R4, R5 are hydrogen; R6, R7, R8 are selected from H or F under the condition that at least two of R6, R7, R8 are hydrogen. The invention also relates to a compound of formula where the values of radicals are given in the claim, specific spiroindolinone pyrrolidinyl derivatives, a pharmaceutical composition based on spiroindolinone pyrrolidinyl derivatives, use thereof and a method of treating malignant growths.

Therapeutic dll4-binding proteins

Present invention refers to immunology. Presented are an antibody and its antigen-binding fragment able to bind to human delta-like ligands 4 (DLL4), including in the form of a labelled antibody or its antigen-binding fragment, a structure with a constant domain of immunoglobulin, a conjugate with a therapeutic or cytotoxic agent and in the crystallised form. Besides, disclosed are: an isolated nucleic acid coding the antibody or its fragment according to the invention, an expression vector, a host cell and a method for producing the antibody or its antigen-binding fragment; as well as a pharmaceutical composition for modulating a disease or a disorder, a method for reducing human DLL4 activity and a method of treating a patient suffering a disorder associated with the negative effect of DLL4.

New (acyloxymethyl)acrylamide esters, pharmaceutical composition containing them, and using them as thioredoxin - thioredoxin-reductase system inhibitors

Invention refers to compounds of formula (1) or their pharmaceutically acceptable salts, wherein in formula (1) R1 means a linear or branched C1-C8 alkyl group, phenyl or benzyl; R2 means hydrogen or C1-C8 alkyl-2-formamide acetate group; R3 means acyl group of carboxylic acid specified in groups of 2,6-dichlorbenzoic or 2,6-di(trifluormethyl)benzoic acid. The invention also refers to using the compounds of formula (1) and a pharmaceutical composition containing them.

Hjurp peptides and vaccines containing them

Invention relates to the extracted peptide which has an inducibility of cytotoxic T-lymphocytes (CTL), and also to its use. The offered peptide can be used in anticarcinogenic immunotherapy, namely, in anticarcinogenic vaccines.

Affinity-matured humanised anti-cea monoclonal antibodies

Invention relates to biochemistry, particularly to an antigen binding molecule (ABM) which specifically binds with membrane-bound human carcinoembyronic antigen (CEA). Also disclosed is an ABM-coding polynucleotide, a coded ABM expression vector, a host cell for ABM expression and a composition for treating cancer, for which abnormal CEA expression is typical. The invention discloses methods of inducing cell lysis of tumour tissue, a disease diagnosis method, a method of prolonging life, a method of inducing tumour regression, a method of treating and a method of inducing CEA-mediated tumour cell adhesion.

Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one

Invention relates to camsilate and maleate salts of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one and to a pharmaceutical composition having activity which is mediated by poly(ADP-ribose)polymerase (PARP), which contains a therapeutically effective amount of the disclosed salt.

Method of obtaining water-soluble polymer complexes of radioisotopes

First polymer carrier with grafted biological vector and chelate units for radiometal binding is obtained. Then, procedure of radio-marking is carried out. Interaction of polymer carrier of chelate units with radioactive component is carried out in alcohol, in water or water-alcohol solution in inert gas atmosphere at temperature 70°C for 20 minutes. As polymer carrier applied is water-soluble copolymer of N-vinylpyrrolidone with N-allylamine with molecular weight 5000-50000 Da, content of chelate units in from of iminodiacetate fragments of iminodiacetic acid 1-20 mol %, content of vinylpyrrolidone m = 99-80 mol % and allylamine n = 1-20 mol %. As radioactive component applied are compounds of transition metals and lanthanides in form of following line [99mTc(CO)3]+, [188Re(CO)3]+, [161Tb(CO)3]+.

Method of treating patients with nodular and radioresistant malignant tumours

Photosensitiser Photosens in a dose in 0.3-0.4 mg/kg is administered into the patient once. A first session of a gamma-ray teletherapy covering the tumour is performed 24 hours later in a single boost dose of 3 Gy. A first session of a remote exposure of the tumour and surrounding healthy tissues to laser light at wave length 670 nm is performed 2-3 hours later in a single light dose Ws of 50-100 J/cm2 at power density Ps 40-50 mW/cm2. That is combined with a session of a contact direct exposure of the tumour to laser light at wave length 670 nm from 2-5 positions depending on a tumour size at a light guide output power P of 100-200 mW and a light dose W of 100 J per each position. The treatment involve 8-10 sessions of the combined gamma-ray teletherapy and photodynamic therapy every 24 hours in the same sequence. That is followed by the gamma-ray teletherapy during 2-4 days.

Pyrazoline dione derivatives as nadph-oxidase inhibitors

Invention relates to pyrazoline dione derivative of formula

Pharmaceutical composition, containing block-copolymer, including boronic acid compound

Block-copolymer includes hydrophilic segment, including polyethyleneglycol, hydrophobic segment, which includes polyamino acid chain; and boronic acid compound residue, bound with side chain of hydrophobic segment via binding unit, which includes heterocyclic structure. Heterocyclic structure is presented by the following chemical structure: , in which B stands for boron atom, formed by boronic acid compound; R1, R2, R3 and R4 each independently stands for hydrogen atom, linear or branched alkyl group with 1-16 carbon atoms, or organic group, containing aromatic group as structure for protection of bond of boronic acid ester, formed by binding of boron atom and oxygen atom, given in chemical structure. The following conditions are observed: (i) at least, one of R1, R2, R3 and R4 represents organic structure, containing aromatic group, and (ii) R1 is not hydrogen atom. Aromatic ring, obtained from aromatic group, is bound with carbon atom, forming cyclic skeleton of heterocyclic structure directly or by means of 1 or 2 atoms.

Purine derivatives applicable for treating fap-related (fibroblast activator protein) diseases

Invention concerns using a compound representing 1-[(4-methylquinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-aminopiperidin-1-yl)-xanthine or its salt for producing a pharmaceutical composition applicable for treating hyperproliferative diseases responding to FAP (fibroblast activator protein) inhibition specified in a group consisting cirrhosis, or healing wounds, treating acne and proliferative skin diseases, such as e.g. psoriasis.

Anti-tumour preparation

Preparation contains Nδ-nitroso-Nδ-[(2-chloroethyl)carbamoyl]-L-ornithine, low molecular polyvinylpyrrolidone Mm=7000-11000 and hydrochloric acid.

Substituted pyridopyrazines as novel syk inhibitors

Invention relates to compounds of formula (I), their racemic mixture, enantiomers, diastereomers and pharmaceutically acceptable salts, possessing properties of Syk inhibitor, pharmaceutical composition and medication based thereof, thereof application, methods of inhibiting and method of treatment with thereof application. In general formula (I) R1 represents hydrogen or C1-C6alkyl, R2 represents phenyl, benzo[d][1,3]dioxolyl, 2,3-dihydrobenzo[b][1,4]dioxinyl, or 5-10-membered heteroaryl, containing 1-2 heteroatoms, selected from N and O, which is optionally substituted with one or several groups, selected from halogen, -NR5R6, -OR7, -S(O)nR8, -C(O)R9, -CN, -C(O)NR5R6, -NR5C(O)R9, -NR5S(O)nR8, -S(O)nNR5R6, C1-C6alkyl, optionally substituted with one, two or three groups, selected from halogen, -OH, -OC1-C4alkyl, -NH2, -NH(C1-C4alkyl), -N(C1-C4alkyl)(C1-C4alkyl), -C(O)N(C1-C4alkyl)(C1-C4alkyl), or 5-8-membered heterocycle, containing 1-2 heteroatoms, selected from N, O, and S, optionally substituted with -SO2(C1-C4alkyl), C3-C6cycloalkyl, 5-8-membered heterocycle, containing 1-2 heteroatoms, selected from N, O and S, optionally substituted with one, two, or three groups, selected from halogen, -OH, C1-C4alkyl, -C1-C4alkyl-OH, ketogroup(oxo), -C(O)C1-C4alkyl, -C(O)C3-C6cycloalkyl, -C(O)C3-C6cycloalkyl-CN, -C(O)C3-C6cycloalkylhalogen, -C(O)NH2, -C(O)NH(C1-C4alkyl), -C(O)N(C1-C4alkyl)(C1-C4alkyl), -C(O)(C1-C4alkyl)-OH, -C(O)(C1-C4alkyl)-O(C1-C4alkyl), -C(O)C1-C4halogenalkyl, -C(O)(C1-C4alkyl)-CN, -C(O)(C1-C4alkyl)-C(O)NH2, -C(O)(C1-C4alkyl)C3-C6cycloalkyl, -C(O)(C1-C4alkyl)-oxetane, C(O)-furanyl, -C(O)-tetrahydrofuranyl, -C(O)(C1-C4alkyl)-SO2(C1-C4alkyl), -O(C1-C4alkyl)-OH, -SO2(C1-C4alkyl), -SO2NH(C1-C4alkyl), -SO2(C1-C4alkyl)(C1-C4alkyl), -SO2C3-C6cycloalkyl, -N(C1-C4alkyl)C(O)(C1-C4alkyl), and 5-6-membered heteroaryl, containing 1-2 nitrogen atoms, optionally substituted with C1-C4alkyl, R3 and R4 are independently selected from hydrogen, C1-C6alkyl, C3-C6cycloalkyl, phenyl, 1,3-dihydroisobenzofuranyl, and 5-6-membered heterocycle, containing 1 nitrogen atom, each of which, except hydrogen, is optionally substituted with one or several groups, selected from halogen, -NR5R6, -OR7, -C(O)OR7, -CN, -C(O)NR5R6, -S(O)nNR5R6, C1-C6alkyl, C3-C6cycloalkyl, 5-6-membered heteroaryl, containing 1-2 nitrogen atoms, and 4-7-membered heterocycle, containing 1-2 heteroatoms, selected from N, O, and S, optionally substituted with one, two or three groups, selected from halogen, hydroxyl, ketogroup(oxo) C1-C4alkyl, -C1-C4alkyl-OH, -C1-C4halogenalkyl, -C(O)NH2, -C(O)NH(C1-C4alkyl), -C(O)N(C1-C4alkyl)(C1-C4alkyl), -C(O)C1-C4alkyl, -C(O)(C1-C4alkyl)-C3-C6cycloalkyl, -C(O)C3-C6cycloalkyl, -C(O)C1-C4halogenalkyl, -C(O)(C1-C4alkyl)-CN, -C(O)(C1-C4alkyl)-OH, -C(O)(C1-C4alkyl)-O-(C1-C4alkyl), -C(O)(C1-C4alkyl)N(C1-C4alkyl)2, -C(O)(C1-C4alkyl)-SO2-(C1-C4alkyl), -C(O)(C1-C4alkyl)-C3-C6cycloalkyl, -SO2(C1-C4alkyl), -SO2(C1-C4halogenalkyl), -SO2C3-C6cycloalkyl, -SO2NH2 and pyrimidinyl, or R3 and R4 together with N atom, which they bind to, can form 5-10-membered monocyclic, fused bicyclic or spirocyclic ring, optionally containing 1 additional nitrogen atom, which is optionally substituted with one or several groups, selected from -NR5R6, -C(O)OR7, -C(O)NR5R6, -NR5S(O)nR8, -NR5C(O)NR10R11, and C1-C6alkyl optionally substituted with hydroxyl, amino, -NHSO2(C1-C4alkyl), -NH(C1-C4alkyl), -N(C1-C4alkyl)(C1-C4alkyl), or -NHC(O)NH2, m equals 0 or 1, n equals 2.

Crystalline form of 2-chloro-4-methoxy-n-[4-(8-methyl-imidazo[1,2-a]pyridin-2-yl)-phenyl]-benzamide, active component, pharmaceutical composition and medicinal agent

Invention relates to a crystalline form of 2-chloro-4-methoxy-N-[4-(8-methyl-imidazo[1,2-a]pyridin-2-yl)-phenyl]-benzamide of formula 1 . The invention also relates to a pharmaceutical composition and a medicinal agent based on a compound of formula 1, which can be used to prevent and treat a proliferative disease associated with the triggering of Hedgehog (Hh) embryonic signalling cascade.

Pyrazolopyridine derivatives as nadph oxidase inhibitors

Invention relates to organic chemistry, particularly to a novel pyrazolopyridine derivative of formula (I), as well as to a tautomer, geometric isomer and optically active forms thereof, such as enantiomers, diastereomers and racemates, and to pharmaceutically acceptable salts thereof, where G1 is selected from -C(O)-R1; R1 is selected from C1-C6-alkoxy-C1-C6-alkyl; C1-C6-alkyl; substituted C6-aryl-C1-C6-alkyl; substituted piperidine; G2 is selected from optionally substituted C6-aryl; G3 is selected from C1-C6-alkyl; G4 is selected from pyridine-C1-C6-alkyl; G5 is selected from H; where the term "substituted" denotes groups substituted with one substitute selected from a group which includes "C1-C6-alkyl", "C1-C6-alkoxy", "C1-C6-alkoxycarbonyl" and "halogen". The invention also relates to a specific compound and a pharmaceutical composition based on a pyrazolopyridine derivative.

Compositions for kinase cascade modulation and methods of their application

Invention relates to polymorph of mesylate salt of 2-(5-(4-(2-morpholinethoxy)phenyl)pyridine-2-yl)-N-benzylacetamide, possessing properties of Syk inhibitor, method of its synthesis, based on it pharmaceutical composition and its application for treatment and prevention of cell proliferation.

Antibodies against human angiopoietin-2

Invention relates to the field of biochemistry, in particular to antibodies against human angiopoietin-2, coding them nucleic acids and host cells. An antibody is characterised by the fact that it does not bind with human angiopoietin-1. Also claimed is a pharmaceutical composition, which contains the antibody against human angiopoietin-2, intended for cancer treatment, prevention of metastases or treatment of vascular diseases.

Anti-cd3*cd19 flexibody-based pharmaceutical compositions for treating b-cell diseases

Group of inventions refers to medicine and pharmaceutics, particularly to a pharmaceutical composition containing an effective amount of anti-CD3*CD19 recombinant monoclonal antibody specified in a group containing the antibody SEQ ID No. 1 or the antibody SEQ ID No. 2, as well as phosphate-buffer saline, surfactant and mannitol in the concentration of 1.5-3.0%, as well as to using these compositions for treating B-cell malignancies or B-cell depletion.

Anti-cancer therapy, directed against cancer stem cells and forms of cancer, resistant to treatment by medications

Group of inventions relates to medicine, namely to oncology, and can be applied for application of sodium metaarsenite for production of therapeutic agent for treatment of taxane- and cisplatin-resistant forms of cancer. For this purpose composition, which contains sodium metaarsenite and composition, which contains paclitaxel, decetaxel or cisplatin, is included into therapeutic agent. Anti-tumour agents for treatment of taxane- and cisplatin-resistant forms of cancer are also claimed.

Kinase inhibitors, prodrug forms thereof and use thereof in therapy

Invention relates to pyrido[3,4-d]pyrimidine compounds of formula (III), having Pan-erbB kinase inhibiting properties. In the compound of formula

Apoptosis inducing agents for treating cancer, immune and autoimmune diseases

Invention refers to new compounds specified in a group shown below. The compounds contain at least 5 rings including a fragment with a bridge structure with a carbon side of the central group C(O)-NH-SO2, piperidinyl, or piperazinyl, or phenyl; phenyl attached to each carbon and sulphur atom of the group C(O)-NH-SO2, wherein phenyl from the sulphur atom side is substituted by a nitro group and NH-CH2(tetrahydro-2H-pyran-4-yl or cyclohexyl) group. The compounds possess the properties of Bcl-2 antiapoptotic protein activity inhibitor and can be used in treating the diseases expressing Bcl-2 protein. These diseases are malignant diseases specified in bladder cancer, cerebral cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukaemia etc. The compounds of the present invention are specified in a group consisting of 4-(4-{acetyl[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}piperidin-1-yl)-N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)benzamide; 4-(4-{benzoyl[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}piperidin-1-yl)-N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)benzamide; N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)-3′-{[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}biphenyl-4-carboxamide; N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)-4-(4-{(phenylacetyl)[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}piperidin-1-yl)benzamide; N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulphonyl)-4-(4-{2-[(1R,4R)-1,7,7-trimethylbicyclo[2.2.1]hept-2-en-2-yl]benzylidene}piperidin-1-yl)benzamide; 4-[4-(2-{5-[8-azabicyclo[3.2.1]oct-8-ylmethyl]-2-thienyl}benzyl)piperazin-1-yl]-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulphonyl)benzamide; N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)-4-(4-{(3-phenylpropanoyl)[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}piperidin-1-yl)benzamide; 4-{4-[adamantan-1-ylmethyl]piperazin-1-yl}-N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)benzamide; 4-(4-{2-[adamantan-1-yl]-2-oxoethyl}piperazin-1-yl)-N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)benzamide; N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)-4-{4-[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]piperazin-1-yl}benzamide and other compounds or their therapeutically acceptable salts listed in the patent claim.

Photosensitiser and method for producing it

Invention is applicable to produce lyophilised trismethyl glucamine salt of chlorine e6, which is used as a high-effective photosensitiser (PS) for the purpose of photodynamic therapy (PDT) of cancer and other new growths of various origins, as well as for fluorescent diagnosing of cancer cells. The method for producing the PDT photosensitiser involves dissolving methylfeoforbide in acetone, processing the produced solution with aqueous alkali NaOH or KOH, and neutralising the reaction mixture with diluted hydrochloric acid, separating precipitated chlorine e6, washing, processing the precipitation with aqueous solution and lyophilising. Implementing the invention enables eliminating pseudocolloidal precipitation, and producing fine and dense precipitation of the photosensitise low in foreign matters.

Method for primary cancer prevention

Method for detection of cancer proneness involves studying a cell immunity by basic lymphocyte subpopulations by CD markers: a) CD3+; b) CD4+; c) CD8+; d) CD16+; e) CD56+, whereas a method for primary cancer involves using the complex herbal preparations 'Pletnev's Drops', which recover metabolism and energy supply of tissues and organs, containing β-carotene, vitamins P, C, PP, ursolic acid, chlorophyl.

Method for prevention of cancerogenic effect of diethylnitrosamine in experimental animals

Method includes introduction of diethylnitosamine with drink in dose 100 mg/l for 4 months. As chemopreventive preparation applied are polysaccharides of Calamus for 6 months with food in dose 75 mg/kg.

Interferon beta immunobiological agent for bladder cancer therapy and method for using same

Group of inventions refers to an immunobiological agent for bladder cancer treatment on the basis of an adenoviral vector containing a promoter-controlled interferon beta gene, wherein the above adenoviral vector is human adenovirus; the agent additionally contains an enzyme, which provides bladder mucosa secretion splitting. The group of inventions also concerns a method for using the immunobiological agent for bladder cancer treatment involving administering the above immunobiological agent into the bladder.

Substituted quinoline compounds and methods of their application

Claimed invention relates to novel substituted quinolines of general formula (I), where R1 stands for hydroxyC2-6 alkoxy and R2 is H, C1-10alkoxy or hydroxyC1-10alkoxy; R3 is H or F, R4 is H, F, Cl, Br, I or CN; and X is CH or N, or to their stereoisomers, tautomers, or pharmaceutically acceptable salts. Invention also claims pharmaceutical compositions, which include such compounds and methods of applying compounds and compositions in treatment of hyper-proliferative disorders in mammals, especially humans.

Cyclopentyl- and cycloheptylpyrazole as fxr modulators

Claimed invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of formula I, where A and R1-R4 are determined in formula of invention, or their pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition containing them and application of claimed compounds.

Targeting cancer tumours by application of inhibitors of carbonic anhydrase ix isoforms

Invention relates to field of organic chemistry, namely to novel nitroimidazole derivatives of formula (1) and to its pharmaceutically acceptable salts, where Z represents Z1 with formula (2a), or Z represents Z2 with formula (2b): (CH2)nCH2X, or Z represents Z3 with formula (2c), and R1 and R2 each independently can represent H or CH3, R3, R4, R6 and R7 each independently can represent H, sulphonamide, sulphamate or sulphamide, R5 can represent H, sulphonamide, sulphamate or sulphamide, X = sulphonamide, sulphamate or sulphamide Y = S, and n = 0, 1 or 2, and where, if n = 0, R2 = 2-CH3, Z = Z1, R3 = R4 = R6 = R7 = H and R5 = SO2NH2, then NO2 is not in position 4, and where if R5 represents H, at least one of R3, R4, R6 and R7 is not H. Invention also relates to application of formula (1) compound and method of treating disease, characterised by superexpression of one or several carbonic anhydrases.

Antibodies against fgfr3 and methods of their application

Invention relates to the field of immunology. Claimed are a separated antibody-antagonist against FGFR3 and its functional fragment, as well as a polynucleotide, vector of expression, host cell and method of obtaining the antibodies against FGFR3 or its functional fragment. In addition, analysed are pharmaceutical compositions and the application of the antibody or its functional fragment by the invention for the treatment or prevention of cancer and a skeleton disease, as well as for the inhibition of cell proliferation and/or reduction of the quantity of cancer cells.

Pyrrolo[2,3-b]pyridine derivatives inhibiting activity of anti-apoptotic bcl-2 proteins

Invention refers to organic chemistry, namely to new heterocyclic compounds of general formula (IIIa) or its therapeutically acceptable salt, wherein A1 represents C(A2); A2 represents H; B1 represents OR1 or NHR1, wherein R1 represents C1-alkyl substituted by R10; D1 and E1 represent H; and Y1 represents NO2; G1 represents C1-alkyl substituted by OP(O)(OH)(OH); R10 represents C6-cycloalkyl, each of which has one CH2 fragment either unsubstituted, or substituted by means of independently specified O; wherein the fragment representing R10 is either unsubstituted, or substituted by one, or two, or three, or four, or five substitutes independently specified in a group consisting of R50, OR50, F, Cl, Br, and I; and R50 represents C1-alkyl. The invention also refers to specific compounds, a pharmaceutical composition based on the compounds specified in claims No. 1-3, and a method of treating cancer.

Method for thermochemoradiation therapy of malignant cerebral glioma

Postoperative period involves a remote radiation therapy and a chemotherapy. That is combined with a local hyperthermia (LH) beginning simultaneously with the chemoradiation therapy. The sessions are performed at temperature 42-44°C for 60 min with a 15-20-minute break between a session of the radiation therapy and the local hyperthermia, 3 times a week, 10 sessions in total. The LH exposure area is supposed to cover a postoperative area and perifocal oedema areas.

Inhibition of dissemination of tumour using bv8 or g-csf antagonists

Method of inhibition of metastasis G-CSF of secrete primary tumour in vivo is suggested. The individual is injected with effective number of antibodies against G-CSF or its antigen-binding fragment after removal of the primary tumour.

Arylmethoxy isoindolin derivative, compositions including thereof and methods of their application

Invention relates to compounds of formula (I), (III) and (VI), possessing properties of TNF-α inhibitors, and their pharmaceutical salts and stereoisomers, as well as to a based on them pharmaceutical composition and a method of treatment with their application. In the general formulae (I), (II), (III) and (VI) X stands for C=O or CH2; R1 stands for -Y-R3; R2 stands for H or (C1-C6)alkyl; Y stands for a 6-10-membered aryl, heteroaryl or heterocycle, each of which can be substituted with one or more halogens; R3 stands for -(CH2)n-aryl, -O-(CH2)n-aryl or -(CH2)n-O-aryl, in which the aryl can be substituted with one or more of the following substituents: (C1-C6)alkyl, which itself can be substituted with one or more halogens; (C1-C6)alkoxy, which itself is substituted with one or more halogens; oxo; amino; carboxyl; cyano; hydroxyl; halogen; deuterium; 6-10-membered aryl or heteroaryl, in case of necessity substituted with one or more (C1-C6)alkyls, (C1-C6)alkoxy or halogens; -CONH2; or -COO-(C1-C6)alkyl, where the alkyl can be substituted with one or more halogens; -(CH2)n-heterocycle; -O-(CH2)n-heterocycle or -(CH2)n-O-heterocycle, where the heterocycle can be substituted with one or more of the following substituents: (C1-C6)alkyl, itself in case of necessity substituted with one or more halogens; (C1-C6)alkoxy, itself substituted with one or more halogens; oxo; amino; carboxyl; cyano; hydroxyl, halogen; deuterium; 6-10-membered aryl or heteroaryl, in case of necessity substituted with one or more (C1-C6)alkyls, (C1-C6)alkoxy or halogens; -CONH2; or -COO-(C1-C6)alkyl, where the alkyl can be substituted with one or more halogens; or -(CH2)n-heteroaryl, -O-(CH2)n-heteroaryl or -(CH2)n-O-heteroaryl, where the heteroaryl can be substituted with one or more of the following substituents: (C1-C6)alkyl, itself in case of necessity substituted with one or more halogens; (C1-C6)alkoxy, itself substituted with one or more halogens; oxo; amino; carboxyl; cyano; hydroxyl; halogen; deuterium; 6-10-membered aryl or heteroaryl, in case of necessity substituted with one or more (C1-C6)alkyls, (C1-C6)alkoxy or halogens; -CONH2; or -COO-(C1-C6)alkyl, where the alkyl can be substituted with one or more halogens; and n=0, 1, 2 or 3.

Compounds suitable for cancer treatment

Invention relates to application of formula

Preparation for selective apoptotic elimination of tumour cells

Invention relates to microbiological industry and can be used in biotechnology, genetic engineering, medicine and veterinary. Claimed is application of RNAase Bacillus sp. VKPM B-9862 as preparation for selective apoptotic elimination of tumour cells.

Pharmaceutical composition for treating and/or preventing cancer

Invention refers to biochemistry, particularly to a medicinal product for treating or preventing cancer, containing an antibody as an active ingredient, which possesses an immune responsiveness to CAPRIN-1 protein. There are also disclosed an antibody, which possesses an immune responsiveness to CAPRIN-1 protein, a pharmaceutical combination containing the above medicinal product for treating or preventing cancer. Disclosed is a method for treating or preventing cancer with the use of the above medicinal product and the pharmaceutical combination.

Anti-vegf antibodies and applications thereof

Inventions refer to biotechnology. Presented are: variants of a monoclonal anti-VEGF antibody or its antigen-binding fragment, which are characterised by the fact that they contain 6 CDRs and optionally T51A substation in CDR-L2, and also have one or a combinations of substitutions as compared to the antibody bevacizumab, namely: 1. K64S in CDR-H2; 2. K64Q in CDR-H2; 3. Y53F and K64Q in CDR-H2; 4. Y53F and K64S in CDR-H2; 5. H97E in CDR-H3; 6. Y98F in CDR-H3; 7. H97E and Y98F in CDR-H3; 8. H97P and Y98F in CDR-H3. Described are: a conjugate of the antibody and a medicinal product neutralising VEGF activity based on the antibody or its antigen-binding fragment; a pharmaceutical composition also based on the antibody or its antigen-binding fragment, or the conjugate, which neutralizes VEGF activity. Disclosed are a method of treating a cancer disease, and also a method of treating age-related macular degeneration or an immune disorder on the basis of the above antibody or its antigen-binding fragment, or the conjugate.

Bir domain iap binding compounds

Invention relates to compounds of formula 1, where G represents a group (1) , where R9 represents an aryl, optionally substituted with C1-C3alkoxy or halogen; or (2) a substituded or non-substituted azole or pyrrole ring, condensed with a substituted or non-substituted aryl, heteroaryl, C5-C6cycloalkyl or heterocyclyl, or to its pharmaceutically acceptable salts, methods of its obtaining and application in the treatment of proliferative disorders, such as cancer.

Crystal anhydrous delta modification of n-(2-chlorine-6-methylphenyldiazomethane)-2-[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pirimidinyl]amino]-5-thiazolcarboxamide, method of its production and pharmaceutical composition based on it

Invention relates to crystal anhydrous δ-modification of N-(2-chlorine-6-methylphenyldiazomethane)-2-[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pirimidinyl]amino]-5-thiazolcarboxamide, characterized by the following set of interplanar distances (d, E) and the intensities corresponding to them (Irel., %): 9.637-69.1%; 7.928-29.2%; 6.415-100%; 5.819-39.4%; 5.529-3.0%; 4.941-27.2%; 4.887-5.6%; 4.549-72.6%; 4.092-3.8%; 4.037-3.2%; 3.847-35.0%; 3.782-5.8%; 3.751-5.2%; 3.642-3.9%; 3.607-2.7%; 3.442-16.6%; 3.383-3.0%; 3.183-27.4%; 3.122-21.7%; 3.099-5.6%; 2.958-6.9%; 2.905-3.4%; 2.763-7.5%; 2.757-7.8%; 2.694-9.2%; 2.551-12.6%; 2.516-2.6%; 2.463-3.9%; 2.292-3.9%; 2.270-5.0%; 2.137-4.0%; 2.112-3.5%; 2.024-3.7%; 1.906-3.4%; 1.867-3.0%; 1.780-6.0%. Crystal anhydrous delta modification of N-(2-chlorine-6-methylphenyldiazomethane)-2-[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pirimidinyl]amino]-5-thiazolcarboxamide is obtained by dissolving of N-(2-chlorine-6-methylphenyldiazomethane)-2-[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pirimidinyl]amino]-5-thiazolcarboxamide in organic solvent. Crystallites are extracted from the solution using the solvent switch method of replacement or by cooling with subsequent filtering, washing, the crystallites are frozen and subjected to sublimation drying during 22-27 hours at the final temperature on the product 25°C minimum. Crystal anhydrous δ-modification of N-(2-chlorine-6-methylphenyldiazomethane)-2-[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pirimidinyl]amino]-5-thiazolcarboxamide, which is characterized by inhibitory activity with reference to the tyrosine kinase, for preparation of pharmaceutical composition for treatment of immunological and oncological diseases.

Crystalline ε-modification of n-[2-(diethylamino)ethyl]-5-[(z)-(5-fluor-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrol-3-carboxamide malate, method for producing same and based pharmaceutical composition

Invention refers to a new crystalline ε-modification of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluor-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrol-3-carboxamide malate, to a method for producing it and using the same for preparing a pharmaceutical composition as an antitumour agent, tyrosine kinase inhibitor for treating oncological diseases.

Carboxamide compounds and use thereof as calpain inhibitors

Invention relates to organic chemistry, particularly to novel carboxamide compounds of formula and to pharmaceutically acceptable salts thereof, where R1 is phenyl-C1-C6-alkyl, where the phenyl can be unsubstituted or substituted with 1 radical R1c; where R1c is independently selected from halogen, C1-C6-alkyl, C1-C6-alkoxy, where the C1-C6alkyl groups can be partially or completely halogenated or can have 1, 2 or 3 substitutes R1a, and -(CH2)p-NRc6Rc7, where p=0, 1, where R1a is independently selected from NRa6Ra7, Ra6 is C1-C6-alkyl, Ra7 is C1-C6-alkyl, or two radicals Ra6 and Ra7, or Rc6 and Rc7 together with a N atom form a nitrogen-containing 6-member saturated heterocycle, which can optionally have 1 additional O heteroatom as a ring member, R2 is phenyl, pyridyl, where the phenyl can be unsubstituted or can have 1 substitute R2c; where R2c has one of the values given for R1c; R3 is C1-C6-alkyl, C3-C6-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, where C1-C6alkyl, is unsubstituted or has 1 substitute Rxa, where Rxa has one of the values given for R1a; R5 is a halogen or C1-C2-alkyl, where m equals 0 or 1; n equals 0. The invention also relates to specific compounds and a pharmaceutical composition based on the compound of formula (I).