Combined anticancer therapy

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

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: present invention relates to biotechnology and provides a α1,6-glucan-containing compound of Helicobacter pylori. The present invention also discloses a conjugate for inducing immune response against H.pylori, which contains said compound conjugated with a carrier protein. The present invention also discloses an immunogenic composition, use of said composition and a method of inducing immune response against H.pylori using said composition. The present invention also discloses immune serum for neutralising H.pylori in mammals, which is obtained by immunising said mammal with an immunogenic composition containing said immunogenic composition. The present invention discloses an antibody which recognises said α1,6-glucan-containing compound of H.pylori, use of said antibody and a method of inducing complement-mediated bacteriolysis of H.pylori strains which express α1,6-glucan using said antibody.

EFFECT: invention improves the effectiveness of immunogenic compositions against Hpylori.

27 cl, 8 dwg, 21 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-carboxamide. As well as to a pharmaceutical composition containing the above compound, to the use thereof and a set for treating.

EFFECT: 2-(3-amino-1-(2,4-difluorophenyl)-1H-1,2,4-triazol-5-yl)-N-methyl-4,5-dihydrobenzo[b]thieno[2,3-d]oxepin-8-carboxamide inhibiting PI3 kinase (PI3K).

6 cl, 15 dwg, 1 tbl, 610 ex

FIELD: medicine.

SUBSTANCE: claimed invention relates to the field of biotechnology. Claimed are versions of a humanised anti-CD79b antibody, each of which is characterised by the presence of a light and heavy chain and a set of 6 CDR with a determined amino acid sequence. An epitope of the antibody from 11 amino acids is determined by the Biacore method. Disclosed are: an immunoconjugate of the antibody with a medication or means for inhibiting cell growth, where the antibody is bound with means covalently, and versions of the composition, based on an effective quantity of the immunoconjugate or the antibody, used for inhibiting B-cell proliferation; as well as a method of determining CD79b in a sample with the application of the antibody. Described are: an antibody-coding polynucleotide, as well as an expression vector and an isolated cell, containing the vector for obtaining the antibody. Disclosed are versions of applying the antibody or immunoconjugate for obtaining the medication for inhibiting the growth of CD79b-expressing cells for the treatment of an individual, affected with cancer, for the treatment of proliferative disease or for inhibiting B-cell proliferation.

EFFECT: invention provides novel antibodies, which can find further application in the therapy of proliferative CD79b-associated diseases.

91 cl, 8 tbl, 9 ex, 20 dwg

FIELD: medicine.

SUBSTANCE: invention refers to biotechnology, virology and medicine. The method provides administering a pox virus containing the defect F2L gene into a host body or a cell. What is also described is using this pox virus for producing a drug preparation for treating proliferative diseases or diseases accompanied by osteoclast hyperactivity. The invention can be used in medicine.

EFFECT: what is presented is the method of treating proliferative diseases or diseases accompanied by osteoclast hyperactivity.

28 cl, 10 dwg, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to methods of obtaining heteroaryl compounds, represented by structural formulae (I) or (II): where R1-R4 have values, given in subcl. 1,14 of the formula.

EFFECT: compounds can be used for treatment or prevention of cancer, inflammatory states, immunological states, etc.

29 cl, 20 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel choline salt of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid, corresponding to formula and to its crystalline form. Crystalline form of salt (A) has characteristic peaks at diffraction angles (2θ(E)) 7.1, 11.5, 19.4, 20.3, 21.5, 22.0, 22.6, 23.5 and 26.2 in diagram of powder diffraction of X-rays, characteristic peaks of values of chemical shifts (δ(ppm)) 155.8, 149.8, 145.3, 118.0, 113.7, 111.6, 110.3, 98.1, 69.8, 58.7, 57.1 and 55.5 in solid-state 13C NMR spectrum and characteristic peaks of values of chemical shifts (δ(ppm)) -131.6, -145, and -151.8 in solid-state 19F NMR spectrum, as well as endothermic peak about 213°C in diagram of differential-thermal analysis.

EFFECT: compound has excellent solubility and stability in storage.

5 cl, 5 dwg, 3 tbl, 8 ex

FIELD: chemistry.

SUBSTANCE: invention relates to biotechnology, specifically to novel hetero-multimeric proteins obtained from modified ubiquitin, and can be used in medicine to treat or diagnose diseases associated with hyperprodution of the extradomain B of fibronectin (ED-B). The protein includes two monomeric ubiquitin links which are differently modified through substitutions of at least 6 amino acids in positions 4, 6, 8, 62, 63, 64, 65 and 66 of SEQ ID NO: 1. In the first monomer link the substitutions include: F4W, K6(H, W or F), Q62N, E64(K, R or H), S65(L, F or W), T66(S or P), and in the second monomer link: K6(T, N, S or Q), L8(Q, T, N or S), Q62(W or F), K63(S, T, N or Q), E64(N, S, T or Q), S65(F or W), T66(E or D).

EFFECT: invention enables to obtain a modified heterodimeric ubiquitin protein, capable of binding with ED-B with high affinity.

28 cl, 18 dwg, 3 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to field of biotechnology, namely to internalisation of therapeutic molecules into cell, and can be applied in medicine. Obtained is composition for delivering molecules of nucleic acids into cells, containing at least one peptide with at least 92% identity to GAAEAAARVYDLGLRRLRQRRRLRRERVRA (SEQ ID NO: 2); IREIMEKFGKQPVSLPARRLKLRGRKRRQR (SEQ ID NO: 3); or YLKVVRKHHRVIAGQFFGHHHTDSFRMLYD (SEQ ID NO: 4), bound to one or several molecules of nucleic acids.

EFFECT: invention makes it possible to increase efficiency of delivery of molecules of nucleic acids into mammalian cell due to peptide, capable of internalisation into mammalian cell with efficiency, constituting at least 200% of efficiency of internalisation of peptide TAT, which has amino acid sequence GRKKRRQRRRPPQ (SEQ ID NO: 1).

8 cl, 16 dwg, 1 tbl, 8 ex

FIELD: chemistry.

SUBSTANCE: invention relates to field of organic chemistry, namely to polymorphs of form 1 and form 2 of (-)trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolon-I-yl)-4-(1H-indol-3-yl)pyrrolidin-2,5-dione. Invention also relates to methods of obtaining said polymorphs and pharmaceutical composition on their basis.

EFFECT: novel polymorphs of (-)trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolon-I-yl)-4-(1H-indol-3-yl)pyrrolidin-2,5-dione are obtained, useful in cancer treatment.

23 cl, 26 dwg, 2 tbl, 27 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to biotechnology and represents an immunogenic composition for preventing and treating cancer diseases, which contains the non-functional BORIS protein, a sequence of which is free from the zinc finger protein. The present invention also discloses an immunotherapeutic cancer composition containing the above non-functional BORIS protein or a bacterial, mammalian or yeast cell, or a viral particle able to express the above non-functional BORIS protein. The present invention also discloses a method for immunising a patient by administering an effective amount of the above immunotherapeutic composition, as well as using the above immunotherapeutic composition for preparing the cancer vaccine.

EFFECT: invention enables increasing the efficacy of the immunoprophylactic and therapeutic cancer vaccine.

22 cl, 7 dwg, 2 tbl, 8 ex

FIELD: medicine.

SUBSTANCE: invention refers to veterinary science and consists in a method for cell immunity activation in vitro with homeopathic medicines. A leukocyte suspension 0.5 ml is added with a homeopathic medicine 0.5 ml diluted in normal saline; the prepared solution is placed into a thermostat for 1 hour at T=37±0.5°C; the solution is added with a microbial reference strain Staphylococcus albus No.182 suspension 0.5 ml containing 109 CFU in normal saline 1 ml; the new solution is placed into the thermostat for 30 minutes at T=37±0.5°C; after incubation, blood smears are fixed in alcohol-formalin for 10 minutes and stained according to Romanowsky-Giemsa for 30 minutes.

EFFECT: cell immunity activation.

3 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents a method for reducing extracellular matrix producing cells in lungs or suppressing an increase of the extracellular matrix producing cells in lungs, involving administering into an individual a composition containing (i) a carrier containing retinoid as a targeting agent, and (ii) a pro-drug specified in a group consisting of siRNA, RNA enzyme, anti-sense nucleic acid and DNA/RNA chimeric polynucleotide, which is targeted on HSP47, and vectors expressing said siRNA, RNA enzyme, anti-sense nucleic acid and/or DNA/RNA chimeric polynucleotide.

EFFECT: invention provides using retinoic acid as a targeting agent for the drug delivery to the extracellular matrix producing cells in the lungs.

8 cl, 6 dwg, 3 ex

FIELD: medicine.

SUBSTANCE: what is presented is using a complex of tris-(2-hydroxyethyl)amine and zinc bis-(2-methylphenoxyacetate) [cinkatran or citrimin] of formula: (HOCH2CH2)3N·Zn(OOCCH2OC6H4CH3-2)2 as an agent suppressing total activity of basic (alkaline) mononuclear phospholipase A2.

EFFECT: invention enables extending the range of using the substances as an ingredient of new pharmaceuticals for preventing sclerotic vascular injuries.

2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: what is presented is using a complex of tris-(2-hydroxyethyl)amine with bis-(2-methylphenoxy-acetate)zinc[zincatran or citrimine] of formula: (HOCH2CH2)3N·Zn(OOCCH2OC6H4CH3-2)2 as an acidic phospholipase Al inhibitor.

EFFECT: invention enables extending the substance use as a component of new pharmacological preparations for preventing sclerotic involvement of blood vessels.

1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a combination of sigma-receptor ligand of formula (I) or its pharmaceutically acceptable salt, isomer or solvate, and a chemotherapeutic agent specified in a group formed by taxane, vincaalkaloids, platinum-based drugs and thalidomide. In formula (I), the radicals R1-R6 have the values specified in the patient claim, and n is specified in 2, 3 and 4.

EFFECT: declared combination can be used for preventing or treating pain caused by the above chemotherapeutic agents if administered simultaneously, separately or sequentially.

15 cl, 18 dwg, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents using sulphated hyaluronic acid for preparing a therapeutic agent for local administration for treating inflammatory/irritating skin diseases specified in dermatitis, atopic dermatitis, photocontact dermatitis, rash, vitiligo, eczema, psoriasis, all skin irritations related to activation of anti-inflammatory cytokines, such as IL-1, IL-2, IL-7, IL-8, IL-9 and TNF, wherein hyaluronic acid has a molecular weight falling within the ranges of 10000 D to 50000 D, 150000 D to 250000 D and 500000 D to 750000 D, and a sulphatation degree equal to 1.

EFFECT: invention provides stimulating the immune system protein synthesis for eliciting the immune response.

8 cl, 33 ex, 15 dwg, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to immunology. What is presented is a prophylactic or therapeutic agent for IL-31 related itching, containing an effective amount of anti-NR10 antibody, possessing NR10-neutralising (alternative name IL-31RA) activity as an active ingredient, and pharmaceutically acceptable additives, wherein the anti-NR10 antibody represents an antibody, which contains the heavy-chain amino acid sequence SEQ ID NO: 17 and the light-chain amino acid sequence SEQ ID NO: 18, or its humanised antibody. What is presented is using the anti-NR10 antibody containing the heavy- and light-chain amino acid sequences SEQ ID NO: 17 and SEQ ID NO: 18 respectively, or its humanised antibodies for preparing the prophylactic or therapeutic agent for IL-31 related itching. What is described is a method for preventing or treating IL-31 related itching, which involves the stage of administering the anti-NR10 antibody containing the heavy-chain amino acid sequence SEQ ID NO: 17 and the light-chain amino acid sequence SEQ ID NO: 18, or its humanised antibodies.

EFFECT: invention enables suppressing IL-31 overexpression itching.

3 cl, 5 dwg, 2 ex

FIELD: pharmacology.

SUBSTANCE: invention relates to a therapeutical or preventive agent for treatment of hypertension or high blood pressure and to the appropriate method of treatment with its usage. The proposed agent contains (a) and (b) as active ingredients: (a) 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolcarbonic acid (febuxostat) or its pharmaceutically acceptable salt; (b) a compound selected from a group made of blockers of calcium channels, blockers of a receptor of angiotensin II, and inhibitors of an angiotensin-converting ferment and their salts applicable from the point of view of medicine.

EFFECT: synergism of lower blood pressure on a model of spontaneous hypertension.

9 cl, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and represents a method of treating psoriasis or a related symptoms, in an individual, involving the local administration of a local composition containing a therapeutic effective amount of an α2 adrenergic receptor agonist and a pharmaceutically acceptable carrier on an individual's skin area, wherein the skin area is subject to psoriasis or the related symptom, or prone thereto, and wherein the α2 adrenergic receptor agonist is brimonidine.

EFFECT: invention provides developing the effective and safe method for treating or preventing psoriasis with no side effects or small side effects.

10 cl, 1 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine, namely to dermatology, and can be used for treating such diseases, as rosacea, psoriasis, topic dermatitis or acne. That is ensured by a local application on an individual's skin area of a topical composition, which can be an ingredient of a kit and contains a therapeutically effective amount of an α2-adrenergic receptor agonist, wherein the α2-adrenergic receptor agonist is specified in a group consisting of: a compound of formula (Ia) wherein each of R1, R2 and R3 independently means hydrogen, halogen, (C1-C8)alkyl or alkoxy; each of R4 and R5 independently means hydrogen, (C1-C8)alkyl or alkoxy; each of R6 and R7 independently means hydrogen, nitro, (C1-C8)alkyl or alkoxy; alkoxy is specified in methoxy, ethoxy, n-propoxy, sec-butoxy, tret-butoxy, n-hexyloxy; and a therapeutically effective amount of the non-steroid anti-inflammatory agent diclofenac and a pharmaceutically acceptable carrier, wherein the skin area is subject to or can be injured by an inflammatory skin disease or a symptom related to the above disease. The α2-adrenergic receptor agonist can be presented by, e.g. brimonidine.

EFFECT: ensuring the synergetic effect when using the declared combination which shows the synergetic effect by improving the anti-inflammatory action of diclofenac that leads to the complete relief of any symptoms of the inflammatory disease.

21 cl, 3 ex, 6 tbl, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a pharmaceutical composition containing N-[3-chlor-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulphonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine or its pharmaceutically acceptable salt as an active pharmaceutical ingredient in an amount of more than 60 wt % to less than 85 wt % as related to total weight of the composition. The active pharmaceutical ingredient is characterised by a wetting angle of less than 55°.

EFFECT: method for preparing the pharmaceutical composition involves the stage of grinding or milling the above pharmaceutical ingredient in the presence of one or more excipients.

7 cl, 7 dwg, 5 tbl, 6 ex

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