For hiv (A61P31/18)

A   Human necessities(312083)
A61P31/18                     For hiv(228)

Therapeutic application of compounds // 2640596
FIELD: pharmacology.SUBSTANCE: invention refers to the application of a compound of formula R1-COOH (I), where R1 is an alkyl group with a main chain of 7-11 carbon atoms, possibly branched in any position of the carbon atom in the main chain, where branching is a side C1-6 alkyl group. The alkyl group of the main chain and/or the side alkyl groups optionally contain one or more heteroatoms. The specified compound is selected from 4-ethyl octanoic acid, 2-butyl octanoic acid, 4-methyl nonanoic acid and 3-methyl undecanoic acid or its pharmaceutically acceptable salt, amide or ester, for treatment or prevention of disease or biomedical state, selected from disorders associated with cramps.EFFECT: increased efficiency of the composition and treatment method.2 cl, 9 dwg, 3 tbl

Synthesis of carbamoil-pyridone inhibitors of hiv integrase and intermediate compounds // 2638923
FIELD: pharmacology.SUBSTANCE: invention relates to new crystalline forms of sodium salt or sodium salt monohydrate of a compound of the general formula (AA). The compound has inhibitory activity against HIV integrase. The AA compound corresponds to the following structural formula: . The crystalline form of the sodium salt of the AA compound has (a) characteristic diffraction peaks at 2-theta angles of 6.4±0.2°; 9.2±0.2°; 13.8°±0.2°; 19.2±0.2° and 21.8°±0.2°, in the X-ray powder diffraction pattern and/or (b) the characteristic infrared absorption spectra at 1641 cm-1 ± 2 cm-1, 1536 cm-1 ± 2 cm-1, 1503 cm-1 ± 2 cm-1 and 1424 cm-1 ± 2 cm-1 and/or (c) 13C-NMR spectra in the solid state, substantially as shown in Fig. 3. The crystalline form of the sodium salt monohydrate of the AA compound has (d) characteristic diffraction peaks at 2-theta angles equal to 8.0°±0.2°; 9.3°±0.2°; 11.3°±0.2°; 16.0°±0.2° and 22.8°±0.2°, in the X-ray powder diffraction pattern and/or (e) characteristic infrared absorption spectra at 1637 cm-1 ± 2 cm-1, 1536 cm-1 ± 2 cm-1, 1501 cm-1 ± 2 cm-1 and 1422 cm-1 ± 2 cm-1 and has substantially X-ray diffraction patterns, as shown in Fig. 4. The invention also relates to a pharmaceutical composition comprising the said crystalline forms, as well as to a process for preparation of the crystalline form of the sodium salt monohydrate of the AA compound. The method includes stages: a) dissolution of the sodium salt compounds of the formula (AA) in a solution of THF (tetrahydrofuran)-water, b) addition of aqueous NaOH to the obtained solution, c) stirring of the obtained mixture, d) filtering of the obtained sediment, washing it with a THF solution - water and THF and drying.EFFECT: crystalline forms of the sodium salt and its monohydrate show high solubility in water or saline, have high bioavailability, increased stability to heat and light, and simplify compound application.13 cl, 7 dwg, 3 ex

Cenicriviroc compositions and methods for their production and application // 2633069
FIELD: pharmacology.SUBSTANCE: composition contains Cenicriviroc or its salt and fumaric acid. A method of preparation of the said composition, a pill, a method for preparation of the said pill and a method for treatment of a disease, disorder or condition, comprising administration of a therapeutically effective amount of the said composition or pill, is described.EFFECT: group of inventions can be used to treat viral infection, inflammation, fibrosis or graft-versus-host syndrome.138 cl, 14 dwg, 36 tbl

Compositions and methods for therapeutic means delivery // 2632445
FIELD: pharmacology.SUBSTANCE: invention group is a nanoparticle for retroviral infection suppression, comprising at least one therapeutic agent and at least one surfactant, wherein the said nanoparticle is crystalline, wherein the said surfactant covers a crystal of the said therapeutic agent, wherein the said therapeutic agent is selected from the group consisting of atazanavir (ATV), efavirenz (EFV), indinavir (IDV) and ritonavir (RTV), wherein the said surfactant is an amphiphilic block copolymer, wherein the said nanoparticle is obtained by wet grinding or high pressure homogenization, and wherein the said nanoparticle contains at least 95% of a therapeutic agent; composition for retroviral infection suppression; method for HIV infection treatment or suppression.EFFECT: invention provides steady drug delivery to the serum and tissue and improved antiviral efficacy relative to the equivalent dose of the free drug.18 cl, 5 ex, 4 tbl, 25 dwg
Combination of traditional chinese medicine for immune function regulation and method for its production // 2630056
FIELD: pharmacology.SUBSTANCE: composition of traditional Chinese medicine for immunity regulation, which contains the following raw materials in parts by weight: 1-100 parts of Radix Panacis Quinquefolii, 1-100 parts of Ganoderma, 1-60 parts of Cordyceps sinensis fermented powder, 1-60 parts of Flos Rosae Rugosae and 1-60 parts of Rhizoma Anemarrhenae or one or more of their extracts. A composition of traditional Chinese medicine for immunity regulation. containing the following raw materials in parts by weight: (i) 1-100 parts of any of Radix Et Rhizoma Ginseng, Radix Codonopsis, Radix Pseudostellariae or Radix Astragali, or any of Radix Et Rhizoma Ginseng extract, Extract of Radix Codonopsis, extract of Radix Pseudostellariae or extract of Radix Astragali; (ii) 1-100 parts of Gandorema; (iii) 1-60 parts of Cordyceps or Cordyceps extract; (iv) 1-60 parts of Flos Rosae Rugosae and (v) 1-60 parts of Rhizoma Anemarrhenae. Method for obtaining of a composition of traditional Chinese medicine. Use of the composition in the manufacture of a medicament for allergic diseases prevention and treatment. Allergic diseases include allergic rhinitis, allergic asthma, atopic dermatitis and/or urticaria. Composition application in the manufacture of a medicament for viral diseases prevention and treatment. Viral diseases include hepatitis B and/or AIDS. Composition application for manufacture of a medicament that is effective in increasing of the leukocytes number. Composition application for manufacture of a medicament for radiation injury prevention and treatment. Composition application for manufacture of a medicament to reduce toxic and/or side effects resulting from radiation therapy and chemotherapy. Composition application for manufacture of a medicament for male sexual function improvement. Composition application for manufacture of a medicament for human body immunity enhancement. Composition application for production of a dietary food product or a medicament to alleviate physical fatigue.EFFECT: compositions described above are effective for immunity regulation.18 cl, 19 ex, 13 tbl

Gp41-neutralizing antibodies and their application // 2624046
FIELD: biotechnology.SUBSTANCE: monoclonal neutralizing antibodies, that specifically bind to the membrane-proximal external region (MPER) of HIV-1 gp41, are described. Also, compositions, comprising the antibodies described herein, that specifically bind to gp41; nucleic acids encoding these antibodies; expression vectors containing nucleic acids; and isolated host cells expressing such nucleic acids are described. The antibodies and compositions described herein can be used to detect the presence of HIV-1 in biological sample or detect the presence of HIV-1 infection or diacrisis of AIDS in an individual. In addition, the antibodies described herein, due to their broad spectrum of neutralizing activity, are an ideal tool for treating an individual with HIV infection.EFFECT: methods described herein may be used to treat or prevent HIV infection.41 cl, 61 dwg, 8 ex
Pharmaceutical composition for hiv infection treatment // 2619840
FIELD: pharmacology.SUBSTANCE: pharmaceutical composition for HIV infection treatment includes lopinavir, ritonavir in an effective amount and a polymer. At that, the pharmaceutical composition is prepared by extrusion. The composition comprises a matrix polymer consisting of PEG 6000/vinylcaprolactam/vinyl acetate of 5 to 25% by weight of the pharmaceutical composition in combination with copovidone of 45 to 65% by weight of the pharmaceutical composition. The composition is extruded at a temperature of 105 to 145°C.EFFECT: invention allows to expand the arsenal of drugs with enhanced pharmacokinetic properties.9 cl, 3 dwg, 11 ex
Derivatives of 5-substituted quinazolinone, compositions containing them and methods of application thereof // 2617989
FIELD: pharmaceutics.SUBSTANCE: compounds of formula (I) R1 is halogen atom; (C1-C6) alkyl, optionally substituted with one or more halogen atoms; (C1-C6) alkoxy group, optionally substituted with one or more halogen atoms, or -(CH2)nNHRa, where Ra represents hydrogen atom; -C(O)-(CH2)n-phenyl or -C(O)-(CH2)n-pyridyl, where phenyl is optionally substituted with one or more substitutes of halogen atom; -SCF3; (C1-C6)alkyl, optionally substituted with one or more halogen atoms, or (C1-C6)alkoxy group, optionally substituted with one or more halogen atoms; -C(O)-(C1-C8)alkyl, where alkyl is optionally substituted with one or more halogen atoms; -C(O)-(CH2)n-(C3-C10-cycloalkyl); -C(O)-(CH2)n-NRbRc, where Rb and Rc are hydrogen atoms independently of each other; (C1-C6)alkyl; or phenyl, optionally substituted with one or more substitutes of halogen atom or (C1-C6)alkyl; -C(O)-(CH2)n-O-(C1-C6)alkyl; or -C(O)-(CH2)n-O-(CH2)n-phenyl; R2 is hydrogen atom; OH; phenyl or (C1-C6) alkyl, optionally substituted with one or more halogen atoms; R3 is hydrogen atom; or (C1-C6) alkyl; and n takes values 0, 1 or 2.EFFECT: method is disclosed of treating or controlling diseases or disorders, such as cancer involving administering 5-substituted quinazoline compound of formula (I) or its pharmaceutically acceptable salt, solvate or stereoisomer.32 cl, 59 ex

Adapted recombinase for asymmetric target site recombination in a variety of retroviruses strains // 2617968
FIELD: biotechnology.SUBSTANCE: inventions relate to a method for preparation of an expression vector encoding an adapted recombinase capable of asymmetric target sequences recombination within the long terminal repeat (LTR) of the multiple HIV-1 strains proviral DNA built into the host cell genome, as well as the resulting expression vector, cells transfected by this vector, the expressed recombinase and a pharmaceutical composition comprising an expression vector, cell and/or recombinase.EFFECT: possible use for treatment or prevention of HIV-1 infection in a subject.28 cl, 5 dwg, 2 ex
Novel compounds and compositions for inhibiting nampt // 2617643
FIELD: chemistry.SUBSTANCE: present invention relates to compounds of formula II: .EFFECT: novel compounds of formula II are obtained, which can be used in method of inhibiting nicotinamide-phosphoribosyltransferase "NAMPT", as well as pharmaceutical compositions based thereon.17 cl, 3 tbl, 11 ex
Propenoate betulin derivatives // 2613554
FIELD: pharmacy.SUBSTANCE: invention relates to a compound or a pharmaceutically acceptable salt thereof, having the following structure: The invention also relates to other individual compounds and pharmaceutically acceptable salts thereof, the structural formulas of which are indicated in the claims, a pharmaceutical composition for HIV replication inhibition and to a method for HIV infection treatment.EFFECT: new propenoate betulin derivatives are obtained, that inhibit HIV replication.20 cl, 2 tbl, 35 ex
Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use // 2611437
FIELD: chemistry; pharmaceutics.SUBSTANCE: invention relates to novel compounds of formula (I) or its pharmaceutically acceptable salt or solvate, which have inhibiting activity lysine specific demethylase-1 (LSD1). In compounds of formula (I) (A) means phenyl or pyridyl, where said phenyl or pyridyl comprises n substitutes (R3); (B) means -O-CH2-phenyl or phenyl, where said phenyl or phenyl fragment, contained in the above -O-CH2-phenyl, comprises n substitutes (R2); (D) means a monocyclic heteroaryl group containing 5 or 6 ring members, where one to three said ring members are heteroatoms, selected from O, S and N, where said heteroaryl group contains one substitute (R1) and, besides, where said heteroaryl group is covalently bonded to molecules through circular carbon atom; (R1) means -NH2; each (R2) is independently selected from a group comprising C1-C6alkyl, hydroxy group, halogen, C1-C6haloalkyl, C1-C6haloalkyl oxy group or C1-C6alkoxy group; each (R3) is independently selected from a group comprising C1-C6alkyl, a hydroxy group, halogen, C1-C6haloalkyl, C1-C6haloalkyl oxy group or C1-C6alkoxy group; and n independently equal to 0, 1, 2 or 3.EFFECT: compounds can be used for treatment or preventing cancer, selected from a prostate cancer, breast cancer, lung cancer, colorectal cancer, cerebral cancer, blood cancer or leukemia; neurological diseases, including depression, Alzheimer's disease, Huntington's disease, Parkinson's Disease, amyotrophic lateral sclerosis, frontal-temporal dementia or dementia with Lewy bodies; or viral infection caused by herpes virus, or selected from a group of HSV-1, HSV-2, and Epstein-Barr virus.66 cl, 2 tbl, 38 ex
Organic compounds // 2610094
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula IV, wherein R6 and R7 are independently halogen, -SO2NH2, -COOH or H; R2 and R5 represent H; in free form or in form of a pharmaceutically acceptable salt. Compound of formula IV binds to nicotinic acetylcholine receptor with high affinity. Invention also relates to a pharmaceutical composition and method of treating, or preventing a disease or disorder, characterised by activation of acetylcholine receptor pathway.EFFECT: for example, compounds and methods of treating function as blocking activity of certain acetylcholine receptors and their subtypes and are used to treat diseases and conditions mediated by irritation of nicotinic receptors, for example small cell lung cancer, symptoms of cognitive impairment, such as Alzheimer's disease.26 cl, 2 tbl, 13 ex

Pharmaceutical composition for preventing and/or treating hiv disease in humans // 2609769
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine and can be used for preventing and/or treating HIV-disease in human, who requires it. Oral pharmaceutical composition contains mixture of coarse antigen, which contains one or more epitopes of HIV proteins Gag and/or Pol, and non-pathogenic recombinant bacterium, selected from group consisting of bacteria Lactobacillus and BCG. Kit for preventing and/or treating HIV-disease in humans is also disclosed.EFFECT: group of inventions provides prevention and/or treatment of HIV-disease in human by capacity of said composition to provide “Ts” anti-HIV immune tolerance, as result specified virus is not able to replicate in host organism.11 cl, 16 dwg, 1 tbl, 1 ex

Ingenol derivatives for reactivation of latent hiv virus // 2609512
FIELD: chemistry.SUBSTANCE: present invention relates to use certain ingenol derivatives as reactivators of latent HIV virus in viral reservoirs. In particular, invention relates to use of one or more ingenol derivatives of formula I in obtaining a product for reactivation of latent HIV virus in viral reservoirs of human body, where Z is Z1 or Z2 so that when Z = Z1, x and y are integers, x varies from 2 to 10 and y varies from 2 to 7; and when Z = Z2, A is phenyl, CH3- or CH2=CH- and B represents -CH=CH-, [-CH2-]q or [-CH2-]w, where q is an integer ranging from 1 to 10 and w is an integer ranging from 1 to 10, provided that: if A is phenyl, B is -CH=CH-; if A is CH3-, B is [-CH2-]q; if A is CH2=CH-, B is [-CH2-]w, and provided that ingenol derivative of formula (I) does not include 3-(2,4,6-dodecatrienoyl)-ingenol or 3-(2,4,6,8-tetradecatetranoyl)-ingenol.EFFECT: in another aspect, present invention relates to a combination including said ingenol derivatives and antiretroviral agents, which exhibit considerable activity against actively replicating virus.11 cl, 12 dwg, 11 ex

Composition for preventing and/or treating infection, caused by hiv-1 // 2603262
FIELD: biochemistry.SUBSTANCE: present invention relates to biochemistry, namely to immunogenic compositions against HIV-1, containing pharmaceutically acceptable carrier and antigenic peptide, selected from group consisting of PWNASASNKSLDDIW, PWNASWANKSLDDIW, PWNASWSAKSLDDIW and PWNASWSNKALDDIW. Said antigenic peptide can be covalently bound to carrier-molecule. Present invention also discloses method of using said antigenic peptides for detecting antibodies to above antigenic peptides in sample and kit, containing said antigenic peptides, for implementation of said method. Method involves contacting antigenic peptides, according to invention, with sample and detection of formation of complexes between said antigenic peptides and antibodies. Present invention also discloses method and kit for quantitative determination of antibodies to antigenic peptides, according to invention.EFFECT: present invention widens range of products for treating or preventing infection, caused by HIV-1.12 cl, 6 dwg, 4 tbl, 5 ex

Solid pharmaceutical compositions containing integrase inhibitor // 2602865
FIELD: medicine.SUBSTANCE: described are compressed tablets for oral administration containing Raltegravir in form of pharmaceutically acceptable salt. Tablet contains: (A) intra-granular component containing (i) effective amount of Raltegravir potassium salt, (ii) first super-expander, and (iii) binding agent; and (B) extra-granular component containing (i) second super-expander, (ii) excipient, and (iii) lubricating agent. Super-expander represents sodium croscarmellose, excipient represents microcrystalline cellulose or combination of microcrystalline cellulose and dibasic calcium phosphate, lubricating agent is magnesium stearate. Tablet contains neither atazanavir nor its pharmaceutically acceptable salt.EFFECT: compressed tablets according to invention are characterized by high load by medicinal substance at acceptable size tablet.11 cl, 1 dwg, 3 ex

ethod of treating and preventing hiv infection of type 1 subtype a // 2600162
FIELD: medicine.SUBSTANCE: invention refers to medicine and concerns a method of treating and preventing HIV infection of type 1 subtype A (HIV-1A), in which HIV-1A genome structure is extracted from infected patient, primary structure of 14 N-terminal amino acids of Tat-protein in extracted HIV-1A genome is determined, personalized drug is created in the form of 6-peptidyl substituted with aminopenicillanic acid derivatives (6-peptidil - APA) peptide, having amino acid sequence, coinciding with the first 14 N-terminal amino acids of Tat-protein in extracted HIV-1A genome of infected patient, and obtained personalized preparation is administrated to patient.EFFECT: invention provides effective treatment and prevention of HIV-1A, minimized side effect of vaccination process.3 cl, 9 ex, 7 dwg, 1 tbl

Quinoline-2-amine derivatives, useful for treating aids // 2598845
FIELD: chemistry.SUBSTANCE: present invention relates to organic chemistry, namely to new quinoline-2-amine derivatives of general formula (I) or pharmaceutically acceptable salts thereof, where X represents CR0 or N, i.e. together with the ring it belongs to it forms respectively a benzene or a pyridine group, R0, R1, R2, R3, R4, R7 and R8 independently represent a hydrogen atom , a halogen atom or a group selected from a (C1-C5)alkyl group, a (C1-C5)fluoroalkyl group, a (C1-C5)alkoxy group, a (C1-C5)fluoroalkoxy group, a -NRaRb group, a -NRa-SO2-NRaRb group, a -NRa-SO2-Ra group and may additional represent a group selected from (IIa) or (IIIa); A represents an oxygen atom, B is a covalent bond, n equals 1, 2 or 3, m equals 1, 2 or 3, R, R′, Rand R andb independently represent a hydrogen atom or (C1-C5)alkyl group, R and R′ can further form with a nitrogen atom, to which they are bonded, saturated 5-or 6-member heterocycle, possibly containing one more heteroatom O, R5 is a hydrogen atom or (C1-C5)alkyl group, R10 is a hydrogen atom or a chlorine atom, and R11 is a hydrogen atom under the conditions specified in CL. 1. Invention also relates to specific quinoline-2-amine derivatives and a pharmaceutical composition based on the compound of formula (I).EFFECT: technical result: there are new quinoline-2-amine derivatives, useful for treating AIDS.14 cl, 2 tbl, 6 ex , ,

ethods and compositions for preventing transmission of hiv infection // 2594249
FIELD: medicine. SUBSTANCE: group of inventions refers to medicine and concerns composition for preventing HIV transmission including polyclonal antibodies or fragments thereof, capable to bind with protein of human immunodeficiency virus (HIV) viral envelope (Env) or its fragment, wherein polyclonal antibodies or fragments thereof (i) are capable to bind with Env protein from HIV heterologous strain and (ii) are present in hyperimmune animal milk or obtained from hyperimmune animal milk, are present in hyperimmune colostrum animal or obtained from hyperimmune animal colostrum or are present in bird egg or obtained from bird eggs. Group of inventions also concerns using said composition for producing drugs for preventing HIV transmission; method of preventing HIV transmission, including topical introduction of said composition. EFFECT: group of inventions provides prevention of HIV transmission. 45 cl, 12 ex, 6 dwg, 6 tbl

ethod of inhibiting hiv replication in cells of mammals and humans // 2593948
FIELD: biochemistry. SUBSTANCE: invention relates to the field of biochemistry. Method of inhibiting replication of human immunodeficiency virus (HIV), involving treatment of mammalian cells with agent selected from group of peptides, interfering RNA or anti-sense oligonucleotide destructive structure proteins vimentin and/or keratin-10 of cytoskeletal intermediate filaments (IF) in mammal cell. Invention also relates to use of said agent for preparing drug for treating of HIV-infection. Besides, there are presented pharmaceutical compositions for treating of HIV-infection, containing said agent. EFFECT: invention increases HIV replication inhibition. 10 cl, 11 dwg, 2 tbl, 12 ex

Immunogenic compositions based on synthetic peptides mimicking actual determinants of hiv1 gp120 // 2577132
FIELD: medicine.SUBSTANCE: invention relates to immunology, and can be used to create a vaccine against HIV/AIDS. To do this, the immunogenic composition comprises synthetic peptides that mimic the consensus sequence of M V1-, V2-, V3 - loop and V3 - loop isolate Russia RU A022a2 casing HIV1 gp120 protein and peptide-loaded immunoadjuvant or dendritic cells.EFFECT: use of the present invention is to provide an immunogenic composition elicits response to each antigen composition comprising synthetic peptides which replicate relevant antigenic determinants of HIV.1 cl, 2 ex, 2 tbl

Compounds applicable for treating aids // 2575845
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to using a compound of formula or any of its pharmaceutically acceptable salts, wherein means an aromatic ring, wherein V represents C or N, and when V represents N, V is found in meta- or para-position to Z, R independently represents a hydrogen atom, halogen atom or group specified in -CN group, hydroxyl group, -COOR1 group, (C1-C3)fluoralkyl group, (C1-C3)fluoralkoxy group, -NO2 group, -NR1R2 group, (C1-C4)alkoxy group, phenoxy group and (C1-C3)alkyl group, wherein the above alkyl is optionally monosubstituted by a hydroxyl group, R1 and R2 independently represent a hydrogen atom or (C1-C3)alkyl group, n is equal to 1, 2 or 3, n′ is equal to 1 or 2, R′ represents a hydrogen atom, halogen atom or group specified in (C1-C3)alkyl group, -NO2 group, -NR1R2 group, morpholinyl group, N-methylpiperazinyl group, (C1-C3)fluoralkyl group and (C1-C4)alkoxy group, R″ represents a hydrogen atom, Z, Y, X, W, T and U represent N or C, and wherein at most four of V, T, U, Z, Y, X and W groups represent N, and at least one of T, U, Y, X and W groups represents N, for producing a medicinal preparation for preventing, inhibiting or treating AIDS. The invention also refers to using specific compounds, new quinoline derivatives, a pharmaceutical composition based on the new quinoline derivatives.EFFECT: new quinoline derivatives are produced, and new biological activity of known compounds is stated.15 cl, 2 tbl, 11 ex

Anti-cxcr4 antibodies for treatment of hiv infection // 2573902
FIELD: medicine, pharmaceutics.SUBSTANCE: claimed invention relates to field of immunology. Claimed is antibody against human CXCR4 or its functional fragment, which are characterised by the fact that they contain light and heavy chains, which each contain 3 respective CDR. Described are versions of nucleic acids for antibody expression; vector for antibody expression, based on said NA, host cell for obtaining antibody, which contains said vector, and method for obtaining antibody, using cell cultivation. Disclosed is pharmaceutical composition, capable of binding human CXCR4 based on antibody. Described is method of screening and/or identification of molecules as anti-viral medications, CXCR4-antagonists.EFFECT: application of invention provides antibodies, which can be applied in therapy of HIV infection.13 cl, 22 dwg, 11 tbl, 16 ex

Treating and preventing hiv infection // 2569058
FIELD: medicine.SUBSTANCE: group of inventions refers to the long-term use of an parenteral formulation for producing a medicinal preparation for treating a HIV-infected individual with the above preparation applicable for subcutaneous or intramuscular injections and consists of brecanavir, or its salt in the form of an aqueous micro- or nanoparticle suspension containing Polysorbate 20, and is administered at regular intervals from 6 to 12 months, and to the above pharmaceutical composition.EFFECT: reducing the number of injections of the composition (preparation) in the absence of the additional agent ritonavir.7 cl, 4 dwg, 4 tbl

Carboxamide compounds and use thereof as calpain inhibitors // 2567392
FIELD: chemistry.SUBSTANCE: 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).EFFECT: obtaining novel carboxamide compounds which are useful as calpain inhibitors (calcium-dependent cysteine proteases).27 cl, 4 tbl, 34 ex

acrocyclic integrase inhibitors // 2567385
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a macrocyclic compound of general formula to its stereochemically isomer form, wherein R1 represents F; R2 represents H, F or Cl; R3 represents C1-4alkyl or cyclopropyl; R4 represents methyl; J represents ---N(R5)-SO2-, ---C(=O)-N(R5)-, ---N(R5)-, or wherein a dashed line means an attachment point to a pyridazinone ring; K represents -(CHR6)P, or *-(CH2)q-CH=CH-CH2-, wherein * means an attachment point to the group J; L represents -O-, -O-CH2-* or -N(R5)-C(=O)-*, wherein * means an attachment point to a phenyl ring; and R5 represents hydrogen, C1-4alkyl or C3-5cycloalkyl; each R6 independently represents hydrogen or C1-3alkyl; p is equal to 3, 4, 5 or 6; q is equal to 2 or 3. The invention also refers to a pharmaceutical composition based on the compound of formula I and using the compound of formula I.EFFECT: produced are the new macrocyclic compounds effective in treating or preventing HIV-infection.13 cl, 6 tbl, 169 ex

Inhibitors of hiv replication // 2564445
FIELD: medicine.SUBSTANCE: invention relates to compounds of formula (I) , where: R1 represents CH3, CH2CH3, Cl, Br, CHF2 or CF3; R2 represents H, OH or F; X represents CH2 or O on condition that when R1 represents CH3 and R2 represents H, then X represents O; and to application of such compounds as inhibitors of HIV replication.EFFECT: possibility of applying said compounds as inhibitors of HIV replication.15 cl, 52 ex

Double vector for suppression of human immunodeficiency virus // 2562868
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of biotechnology, genetic engineering and virology. Recombinant retrovirus vector codes inhibitor of HIV coreceptor, such as CCR5 or CXCR4, and protein, inhibiting fusion of HIV with target-cell or HIV replication. Pharmaceutical compositions, containing such constructions, and methods of thereof application for prevention or treatment of HIV infection in patients are also described. Claimed group of inventions can be used in medicine.EFFECT: described is expression vector for prevention or suppression of HIV penetration, fusion or replication in mammalian cells.57 cl, 24 dwg, 9 tbl, 11 ex

Triterpene derivatives of lupeol type as antiviral preparations // 2561604
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to novel triterpene derivatives of formula and formulaactive with respect to HIV, as well as HIV-mediated diseases, and to an intermediate compound of formulaIn the general formula (I) R stands for H, substituted or non-substituted C1-6 alkyl, benzyl or substituted or non-substituted C4-5 cycloalkyl and preferably R is substituted with Ra; R' stands for H, substituted or non-substituted C1-6 alkyl, substituted or non-substituted C4-5 cycloalkyl, substituted or non-substituted C4-5 cycloalkenyl,substituted piperazinyl, substituted piperidinyl, substituted 8-azabicyclo[3.2.1]octane, 4-ethyl-2,2,6-trimethyl-1.3-dioxane, hexane-2,4-diol or (S)-1-((4aS,8aS)-octahydroisoquinolin-2(1H)-yl)-4-phenylbutan-2-ol and preferably R′ can be substituted with Ra; X is selected from a bond and -C(O)-; X1 is selected from -C(O)-, -C(O)2- or -C(O)NR"-; Z stands for -O-; Z1 stands for a bond; Z' stands for H; n equals 0; m equals 1, ″″ stands for a single bond; R1 stands for H; R2 stands for -C(=CH2)(CH3); Ra stands for cyano, phenyl, benzyl, ethyl, 3-isopropyl-5-methyl-1,2,4-triazole, -C(O)2R", -C(O)R", -CH2OR", -C(O)N(R)"2 or substituted or non-substituted C1-6 alkyl, where the substituent is selected from -OH, morpholinyl, benzyl, -COOMe, piperazinyl, optionally substituted with ethyl, piperidinyl, optionally substituted with methyl, -COOH, or benzyl; and each R" is independently selected from H, substituted or non-substituted C1-6 alkyl, methyl 3-methylbutanoate, 3-methylbutanic acid, 4-methylpentanic acid, methyl 4-methylpentanoate, methyl propionate, propanoic acid, 1-morpholinopropan-1-one, 1-(pyrrolidin-1-yl)propan-1-one, 4-ethylpiperazinyl, morpholinyl, piperidinyl, optionally substituted with -COOEt, pyrrolidinyl or benzyl. In formula (2A) XA1 stands for a bond or -C(O)-; XA2 stands for a bond, O or NH; RA1 stands for Rb stands for substituted or non-substituted C1-6 alkyl; RA2 stands for substituted or non-substituted amine, substituted or non-substituted C4-5 cycloalkyl, substituted or non-substituted C4-5 cycloalkenyl, 4-ethyl-2,2,6-trimethyl-1,3-dioxane, hexane-2,4-diol, (S)-1-((4aS,8aS)-octahydroisoquinolin-2(1H)-yl)-4-phenylbutan-2-ol or substituted piperazinyl, substituted piperidinyl, substituted 8-azabicyclo[3.2.1]octane, and RA2 is preferably substituted with R'"; and each R'" represents substituted nitrogen-containing heterocycloalkyl (where alkyl is bound to a nitrogen atom in a heterocycle), where the substituent is selected from methyl, ethyl, -CN, phenyl, benzyl, 3-isopropyl-5-methyl-1,2,4-triazole, -COOH, -COOEt, -COOtBu, -CONHtBu, -CH2OH or phenyl.EFFECT: obtaining novel triterpene derivatives.14 cl, 1 tbl, 105 ex

Antiretroviral agents based on azidothymidine derivatives // 2561501
FIELD: chemistry.SUBSTANCE: invention relates to antiretroviral azidothymidine derivatives of formula 1 and can be used as a medicinal agent. , where: R1+R2=-CH2(CH2)2CH2-, R1+R2=-CH2(CH2)3CH2-, R1=H, R2=CH3, R1=H, R2=CH2CH2CH3, R1=H, R2=C(CH3)3, R1=H, R2=CH2(CH2)6CH3.EFFECT: novel effective agents with low toxicity against retroviral infections.16 ex, 2 tbl

ethod of preventing sexually transmitted viral diseases, medication, method of obtaining medication, pharmaceutical composition for local application and condom // 2560879
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to the application of a pharmaceutical composition for local application for the prevention of sexually transmitted viral diseases, which includes an effective quantity of a formula (I) compound. The composition is applied locally into the vagina, anus or oral cavity. In formula (I) R1, R2 and R3 represents hydrogen. The invention also relates to the application of the pharmaceutical composition, made in the form of a vaginal cream, and to the application of a condom, covered with the said pharmaceutical composition.EFFECT: obtaining the pharmaceutical composition for local application for the prevention of sexually transmitted viral diseases.16 cl, 6 dwg, 1 tbl, 13 ex

Aminotetraline derivatives containing their pharmaceutical compositions and using them in therapy // 2546649
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new aminotetraline derivatives of formula (I) and their physiologically tolerable salts. In formula,A means a benzene ring or a ring specified in a group consisting of a 5-merous ring , R means the group R1-W-A1-Q-Y-A2-X1-; R1 means hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl-C1-C4-alkyl, halogenated C1-C6-alkyl, tri-(C1-C4-alkyl)-silyl-C1-C4-alkyl, C1-C6-alkoxy-C1-C4-alkyl, amino-C1-C4-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl, an optionally substituted phenyl, C1-C6-alkoxy, di-C1-C6-alkylamino, an optionally substituted 5 or 6-merous heterocyclyl containing 1-3 heteroatoms specified in nitrogen and/or oxygen or sulphur; W means a bond; A1 means a bond; Q means -S(O)2- or -C(O)-; Y means -NR9- or a bond; A2 means C1-C4-alkylene, or a bond; X1 means -O-, C1-C4-alkylene, C2-C4-alkynylene; R2 means hydrogen, halogen, or two radicals R2 together with the ring atom to which they are attached form a benzene ring; R3 means hydrogen. The other radical values are specified in the patent claim. The invention also refers to intermediate products for preparing the compounds of formula (I).EFFECT: compounds possess the properties of glycine transporter inhibitors, particularly GlyT1 and can find application in treating neurological and psychiatric disorders, such as dementia, bipolar disorder, schizophrenia, etc or for managing pain related to glycerinergic or glutamatergic neurotransmission dysfunction.20 cl, 2 tbl, 326 ex
Pharmaceutical composition for treating hiv-infection, method for preparing and method of using // 2543322
FIELD: medicine.SUBSTANCE: invention represents a pharmaceutical composition for treating the HIV infection in the form of a solid dosage form, containing at least one HIV protease inhibitor in a therapeutically effective amount specified in a group of nelfinavir, sacvinavir, tipranavir, darunavir, indinavir, ritonavir, lopinavir, palinavir or fosamprenavir, and pharmaceutically acceptable additives differing by the fact that as the pharmaceutically acceptable additives it contains at least one water-insoluble polymer from 0.39 to 28 wt % of the total dosage form, surfactants, excipients up to 100% of the total dosage form, as well as a method of treating the HIV infection.EFFECT: pharmaceutical composition according to the invention possesses the improved technological properties and improved bioavailability as compared to a prototype therapeutic agent.10 cl, 4 ex, 1 tbl

Herbal composition for treating and preventing viral blood disorders, such as diseases caused by human immunodeficiency virus (hiv) or hepatitis c // 2543319
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a composition for treating or preventing the human immunodeficiency virus (HIV) or hepatitis C. The herbal composition used for treating or preventing the patients infected by the HIV or hepatitis C viruses and containing a herbal ingredient with tannin agents and catechin, and a pharmaceutically acceptable carrier; the herbal ingredient is Agrimonia Eupatoria (GAFT) and/or gambier (Uncaria gambir). A method for preparing the herbal composition for treating or preventing the patients infected by the HIV or hepatitis C viruses.EFFECT: composition is effective for treating or preventing the patients infected by the HIV or hepatitis C viruses.12 cl, 6 dwg, 2 tbl

ethods of obtainment and application of multipotent cell populations // 2535365
FIELD: medicine.SUBSTANCE: invention relates to the field of biotechnology and cell technology. The claimed invention is aimed at the creation of pluripotent, multipotent and/or self-renewing cells, which are able to start differentiating in a culture into various types of cells and are capable of further differentiation in vivo. The claimed invention is also aimed at the creation of populations of the required differentiating cells, which can be transplanted to patients, genetic modification of endogenic cells and treatment of patients, suffering from diseases, intensity of which can be reduced by means of the said methods.EFFECT: invention also claims methods of prevention, treatment or retardation of a disease, associated with an infection of immunodeficiency virus.17 cl, 1 dwg, 13 ex

Improving genetic constructs for providing high efficacy of anti-hiv therapy // 2533817
FIELD: medicine.SUBSTANCE: invention refers to medical and molecular genetics. There are described genetic constructs expressing RNA sequences and genes coding proteins possessing the antiviral activity on human immunodeficiency virus. The genetic constructs contain a sequence coding the human TRIM5a modified protein. The invention can be used in scientific investigations.EFFECT: presented constructs enable providing the higher expression of the modified gene of the human TRIM5a.40 cl, 4 dwg, 3 tbl, 13 ex
Antiretroviral combination // 2531089
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a pharmaceutical composition in a tabletted dosage form which contains the first layer containing ritonavir and a polymer in a ratio of 1:1 - 1:6, and the second layer containing darunavir. The first layer is produced by hot extrusion, and the second layer - by direct extrusion or wet granulation. Also, the invention refers to a method for preparing the above pharmaceutical composition, and to a method of treating HIV or AIDS involving administering the above composition.EFFECT: invention enables overcoming the incompatibility of ritonavir and darunavir, and also provides an optimum dissolution profile of both the active substances.17 cl, 2 tbl, 2 ex

Protein phosphatase-1 inhibitors and using them // 2527561
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a pharmaceutical composition for HIV-1 replication inhibition containing a compound of Formula , wherein n is equal to 1 or 2; Ar means phenyl substituted by one substitute specified in a group consisting of OH and NO2, or by two substitutes OR, or thienyl; R1 is specified in a group consisting of R6, C(O)N(R6)2, and C1-C6 alkyl substituted by OR; R2 means H or C1-C6 alkyl; R6 is independently in each specific case specified in H and C1-C6 alkyl; each R independently represents C1-C8 alkyl; or its pharmaceutically acceptable salt, or a compound 1G3, or its pharmaceutically acceptable salt. Also, the invention refers to a method of treating an individual either HIV-1 infected or suffering a high risk of HIV-1 infection involving administration of the above composition, to a method for HIV-1 virus replication inhibition.EFFECT: what is prepared is the new pharmaceutical composition possessing effective biological properties 1G3.11 cl, 6 tbl, 1 ex

Synthesis of carbamoyl pyridone inhibitors of hiv integrase and intermediate compounds // 2527451
FIELD: chemistry.SUBSTANCE: invention relates to improved method of obtaining pyridine compounds (AA),(BB) and (CC) of respective formulas: , , . said compounds possess inhibiting action with respect to HIV-integrase. method consists in carrying out the following stages: P-1) bromination of compound of formula (I-I) with obtaining bromine-compound of formula (II-II), where value R represents -CHO, -CH(OH)2, -CH(OH)(OR4), -CH(OH)-CH2OH or -CH(OR5)(OR6); P1 represents benzyl; P3 represents H or protective group of carboxyl; R4 represents lower alkyl; R5 and R6 independently represent lower alkyl or R5 and R6 can represent alkyl and be connected with formation of 5-, 6- or 7-member ring, P-2) formation of side chain of 2,4-di-fluorophenyl-CH2-NH-C(O)- with application of reagents 2,4-di-fluorophenyl-CH2-NH2 and carbon monoxide, stage of formation of Q ring by means of respective amine, selected from 3-amino-butan-1-ol, 2-amino-propan-1-ol and 2-pyrrolidinyl methylamine, and stage of debenzylation with obtaining compound of formula (AA), (BB) or (CC), where said stage P-2 is carried out after formation of Q ring.EFFECT: method makes it possible to simplify obtaining target compounds due to carrying out regioselective bromination at the first stage.6 cl, 3 ex, 7 dwg

1,2,5-oxadiazole derivatives, having anti-hiv activity, pharmaceutical composition, method of inhibiting hiv-1 integrase // 2515413
FIELD: chemistry.SUBSTANCE: invention relates to use of nucleoside derivatives - 1,2,5-oxadiazoles of general structural formula I where R1 and R2 are selected from phenylsulphonyl, substituted with one or more halogen atoms, nitro groups, carboxy groups, alkyl halides, CH3, OCH3, OCF3; X is selected from N or N→O; or R1 and R2 form a group, where R', R", R'" and R'''' are independently selected from hydrogen; halogens; nitro groups, hydroxy group, carboxy group, CH3; CH2Br; OCH3; phenylsulphonyl; phenylthio group; or the following groups: R' and R" can also be merged into one of the following common rings for inhibiting human immunodeficiency virus (HIV) replication. The invention also relates to a pharmaceutical composition based on compounds of formula I and a method of inhibiting HIV-1 subtypes A and B integrase, including forms which are resistant to raltegravir.EFFECT: detecting novel activity in compounds of formula I, which can be used in medicine as HIV replication inhibitors.3 cl, 5 tbl, 4 ex

Pyrrolodinyl alkylamide derivatives, their obtaining and therapeutic application as ligands of ccr3 receptor // 2514824
FIELD: chemistry.SUBSTANCE: invention relates to compounds of general formula or , where Ar1 represents phenyl group, optionally substituted with one or several identical or non-identical halogen atoms; R1 represents hydrogen atom; R4, R5, R6a, R6b represent hydrogen atoms; Y, Z independently represent linear C1-4 alkylene group, optionally substituted with one linear C1-4 alkyl group; Ar2 stands for condensed with benzene 5-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, substituted with one linear C1-4 alkyl group, or derivative of 5- or 6-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, condensed with heteroaromatic 6-memebered ring, containing one or two nitrogen atoms, substituted with one linear C1-4 alkyl group, linear C1-4 alkoxygroup or group -NR7R8, where R7 and R8 independently stand for hydrogen atom, linear or branched C1-4 alkyl group, or R7 and R8 together with nitrogen atom form group of general formula , where R2, R3 represent linear C1-4 alkyl groups, A stands for group -CHR12, oxygen atom or group -NR9, where R12 and R9 stand for hydrogen atom or linear C1-4 alkyl group, m has value 1 or 2, n has value 1 or 2, o has value 0 or 1, p has value 0 or 1, Q stands for group -O-, group -N--H or group -N--CO-R10, where R10 stands for linear C1-4 alkyl group or -NH-R11 group, where R11 represents linear C1-4 alkyl group; and to their salts. Invention also relates to methods of obtaining therein and to based on them pharmaceutical composition, possessing antagonistic activity with respect to receptor CCR3.EFFECT: obtained are novel compounds and based on them pharmaceutical compositions, which can be applied in medicine for obtaining medication, intended for treating asthma, allergic rhinitis, atopic dermatitis, eczema, inflammatory intestinal diseases, ulcerous colitis, Crohn's disease, allergic conjunctivitis, multiple sclerosis or HIV-infection and AIDS-associated diseases.14 cl, 3 tbl, 26 ex
New antiretroviral combination // 2508105
FIELD: medicine, pharmaceutics.SUBSTANCE: presented group of inventions refers to medicine. What is presented is a pharmaceutical composition representing a tablet formulation containing ritonavir in a first layer and atazanavir in a second layer, and a polymer. What is presented is a method for preparing the above pharmaceutical composition wherein a hot melt of rinonavir is extruded to prepare an extrudate to be placed into the first tablet layer, and atazanavir - into the second layer; the first and second layers are combined providing a single multilayer tablet. What is presented is a composition prepared by the method described above to be used in treating HIV or AIDS, and a method of treating HIV or AIDS.EFFECT: presented group of inventions is effective in creating the multilayer tablet providing a good bioavailability for ritonavir, wherein atazanavir is not degraded in preparation.19 cl, 5 tbl, 4 ex

Alpha-substituted omega-3 lipids, activators or modulators of peroxisome proliferator activated receptor (ppar) // 2507193
FIELD: chemistry.SUBSTANCE: invention relates to novel omega-3 lipid compounds of general formula (I) or to their pharmaceutically acceptable salt, where in formula (I): R1 and R2 are similar or different and can be selected from group of substitutes, consisting of hydrogen atom, hydroxy group, C1-C7alkyl group, halogen atom, C1-C7alkoxy group, C1-C7alkylthio group, C1-C7alkoxycarbonyl group, carboxy group, aminogroup and C1-C7alkylamino group; X represents carboxylic acid or its carbonate, selected from ethylcarboxylate, methylcarboxylate, n-propylcarboxylate, isopropylcarboxylate, n-butylcarboxylate, sec-butylcarboxylate or n-hexylcarboxylate, carboxylic acid in form of triglyceride, diglyceride, 1-monoglyceride or 2-monoglyceride, or carboxamide, selected from primary carboxamide, N-methylcarboxamide, N,N-dimethylcarboxamide, N-ethylcarboxamide or N,N-diethylcarboxamide; and Y stands for C16-C22 alkene with two or more double bonds, which have E- and/or Z-configuration.EFFECT: described are pharmaceutical and lipid compositions, which contain said compounds, for application as medications, in particular, for treatment and/or prevention of peripheral insulin resistance and/or condition of diabetes, for instance, type 2 diabetes, increased levels of triglycerides and/or levels of non-HDL cholesterol, LDL cholesterol and VLDL cholesterol, hyperlipidemic condition, for instance, hypertriglyceridemia (HTG), obesity or condition of excessive body weight, fatty liver disease, for instance, non-alcoholic fatty liver disease (NAFLD) or inflammatory disease or condition.60 cl, 3 tbl, 65 ex

Immunoprophylactic vaccine against hiv based on hiv-specific antibodies // 2505604
FIELD: biotechnologies.SUBSTANCE: there proposed is the method for obtaining vaccine against HIV-1 with the use of method of reverse paning at bacterial virus-presented library of HIV-1 - specific scFv antibodies obtained on the basis of mRNA B-lymphocytes of the patients infected by HIV-1 and enriched via paning on HIV-1 peptides and induced systems of expression of recombinant proteins with eukaryotic glycosylation. There also reviewed is the vaccine against HIV-1 and its use for immunisation of non-infected people against infection and development of HIV infection.EFFECT: HIV-1 vaccine obtained due to this invention provides the appearance of immune response in organism with formation of HIV-1-specific antibodies.12 cl, 27 dwg, 9 tbl, 4 ex

Pharmaceutical composition for treating hiv infection, method for preparing it, and method of treating // 2505286
FIELD: medicine.SUBSTANCE: invention represents a pharmaceutical composition for treating HIV infection as a solid dosage form containing at least one HIV protease inhibitor in a therapeutically effective amount specified in a group of nelfinavir, sacvinavir, tipranavir, darunavir, indinavir, ritonavir, lopinavir, palinavir or fosamprenavir, and pharmaceutically acceptable additives, differing by the fact that the pharmaceutically acceptable additives are presented by at least one water-soluble polymer in the amount of 0.4 to 49 wt % of the weight of the ready dosage form, one water-insoluble polymer in the amount of 0.39 to 28 wt % of the weight of the ready dosage form, surfactants, excipients to the weight of 100% of the ready dosage form, as well as a method of treating HIV infection.EFFECT: composition possesses the improved technological properties and bioavailability as compared to a prototype drug.13 cl, 7 ex, 1 dwg

Replication inhibitors of human immunodeficiency virus // 2503679
FIELD: biotechnologies.SUBSTANCE: invention refers to compounds of formula I: , where X means S or CR5;Y means S or CR7; where one of X or Y means S; each of R2, R5, R6 and R7 has been independently chosen from a group including the following: a) halogen; b) R8, -O-R8, -(C1-C6)alkylene-R8, -(C1-C6)alkylene-O-R8; where in each case R8 has been independently chosen from a group containing H, (C1-C6)alkyl, (C2-C6)alkenyl, (C3-C7)cycloalkyl and aryl; R3 means -W-R31 and bond is an ordinary bond; where W means O and R31 means (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl-; R4 means aryl or Het, where each aryl and Het optionally contains 1 to 5 substitutes, each of which has been independently chosen from a group containing halogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C1-C6)haloalkyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl-, -OH, -O(C1-C6)alkyl, -NH2, -NH(C1-C6)alkyl and -N((C1-C6)alkyl)2, which can be used for treatment of HIV infection.EFFECT: improving compound application efficiency.15 cl, 4 tbl, 55 ex

Application of adapted recombinases for curing of retroviral infections // 2501860
FIELD: biotechnologies.SUBSTANCE: invention proposes a method for obtaining an expression vector coding an adapted recombinase. The above adapted recombinase recombines asymmetric sections-targets in LTR of proviral DNA of retrovirus built into a genome of a host cell and applicable as means for cutout of provirus from genome of the host cell.EFFECT: optimisation of curing of retroviral infection with individual in vitro and use of adapted recombinases for obtaining pharmaceutical compositions for reduction of virus load with the individual infected with retrovirus.21 cl, 11 dwg, 1 tbl, 4 ex

Crystalline form of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile // 2498979
FIELD: chemistry.SUBSTANCE: invention relates to a novel polymorph I 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile, i.e., polymorph I TMC278, which is characterised by X-ray powder diffraction peaks at positions two theta 9.0°±0.2°, 14.3°±0.2°, 17.1°±0.2° and 24.2°±0.2°. In particular, the invention relates to a pharmaceutical composition of micro- or nanoparticles for administration via intramuscular or hypodermic injection. The invention also relates to the method of producing the polymorph I TMC278. The method involves dissolving TMC278 in ketone, heating the solution to boiling point and cooling to temperature below 0°C.EFFECT: polymorph has HIV inhibiting properties and can be used to treat HIV infection or prevent HIV infection in case of risk of HIV infection as an active ingredient of a pharmaceutical composition.15 cl, 8 dwg, 6 ex

Peptides // 2496789
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a conformationally restricted cyclic oligopeptide producing two stable and specific epitopes each of which is able to react with a target ligand, to a pharmaceutical composition comprising the above oligopeptide, and to a method for producing the oligopeptide.EFFECT: producing the conformationally restricted cyclic oligopeptide.19 cl, 8 tbl, 8 ex
 
2551193.
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