Romidepsin solid forms and use thereof

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

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention describes a method of producing cyclic depsipeptides of formula (I) via intramolecular cyclisation.

EFFECT: improved method.

14 cl, 31 ex

FIELD: chemistry.

SUBSTANCE: invention discloses lysobactin derivatives, synthesis method thereof, as well as use thereof to prepare medicinal agents for treating and/or preventing diseases caused by bacteria. The lysobactin derivatives are distinguished from natural substance by presence of an N-terminal peptide chain which contains a 3-(3-pyridyl)alanyl residue.

EFFECT: compositions are highly effective.

10 cl, 1 tbl, 10 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel anti-tumour compounds which are kahalalide F derivatives, pharmaceutical compositions containing said derivatives and their use in preparing an anti-tumour medicinal agent.

EFFECT: obtaining novel anti-tumour compounds.

4 cl, 9 tbl, 17 ex

FIELD: organic chemistry, antibiotics, medicine, oncology.

SUBSTANCE: invention relates to novel derivatives of aplidine possessing anti-tumor activity and represented by the general formula:

EFFECT: valuable medicinal property of compound, improved methods of synthesis and preparing.

28 cl, 3 tbl, 121 ex

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: declared invention refers to veterinary science and aims at treating the diseases caused by giardia. The declared drug as an active substance contains Nifurtimox.

EFFECT: using the declared drug is high effective in treating the diseases caused by giardia.

3 cl, 2 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention discloses lysobactin derivatives, synthesis method thereof, as well as use thereof to prepare medicinal agents for treating and/or preventing diseases caused by bacteria. The lysobactin derivatives are distinguished from natural substance by presence of an N-terminal peptide chain which contains a 3-(3-pyridyl)alanyl residue.

EFFECT: compositions are highly effective.

10 cl, 1 tbl, 10 ex

FIELD: medicine.

SUBSTANCE: invention relates to application of emodepside and PF1022A for obtaining medications for prevention of vertical infections in animals, in particular in dogs, caused by endoparasites.

EFFECT: invention ensures increased efficiency of preventing vertical infection in animals.

2 cl, 5 ex

FIELD: medicine.

SUBSTANCE: antiendoparasitic contains emodepside as an active substance, PF1022 and/or praziquantel, a pyrrolidone solvent, limonene as a penetration booster. The preparation can additionally contain aliphatic fatty acid as an accessory penetration booster, e.g., linoleic or oleic acids.

EFFECT: preparation is transdermally applied and provides effective endoparasite control.

5 cl, 2 tbl, 19 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel anti-tumour compounds which are kahalalide F derivatives, pharmaceutical compositions containing said derivatives and their use in preparing an anti-tumour medicinal agent.

EFFECT: obtaining novel anti-tumour compounds.

4 cl, 9 tbl, 17 ex

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