(A61K31/4375)

Salts and crystalline forms of apottosis-inducing agent // 2628560
FIELD: pharmacology.SUBSTANCE: invention relates to a compound having the systematic name 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy) benzamide (compound 1) in the form of a free base crystalline anhydrate, a free base hydrate of crystalline form, a solvate of crystalline form, a hydrochloride salt of crystalline form, or a sulfate salt of crystalline form. The invention also relates to a pharmaceutical composition having an inhibitory activity against anti-apoptotic proteins of the Bcl-2 family comprising a therapeutically effective amount of the compound of the invention and one or more pharmaceutically acceptable excipients.EFFECT: crystalline forms of compound 1 suitable for use as an active pharmaceutical ingredient.21 cl, 14 dwg, 14 tbl, 17 ex
Compound as wnt signal inhibitor, its compositions and application // 2627712
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic compound of the general formula (I) or an N-oxide thereof, wherein X1, X2, X3 and X4 independently represent CR4 or N, where 0 or 1 of X1-X4 can be N; Y1, Y2 and Y3 are hydrogen; R1 is selected from hydrogen, , C6 aryl, 6-member heterocycloalkyl containing 2 heteroatoms selected from N and O, and 5- or 6-member heteroaryl containing 1-4 heteroatoms selected from N, O and S, wherein each of C6 aryl, 6-member heterocycloalkyl and 5- or 6-member heteroaryl may be optionally substituted with one R4; R2 is selected from hydrogen, halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl and 6-member heteroaryl may be optionally substituted with one R4. If X5 is N, R2 is selected from halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl, and 6-member heteroaryl may be optionally substituted with one R4; each R4 Is independently selected from hydrogen, halogen, cyano, oxo, C1-6 alkoxy, -C(O)OR5, -C(O)R5, C1-6 alkyl. Moreover , C1-6 alkyl may be optionally substituted with 1 to 3 substituents selected from halogen and cyano; R5 is C1-6 alkyl; and where the central structure of Formula I, limited by X5, X6, X7 and X8, is: or The invention also relates to particular compounds, a method for inhibiting the secretion of WNT signalling in a cell, use of a compound of formula (I), a method for treatment of a disorder mediated by WNT. .EFFECT: new heterocyclic compounds have been obtained that are useful for treatment of cancer, fibrosis and osteoarthritis.22 cl
Aza-aryl-1-h-pyrazol-1-yl-sulphonamides // 2627268
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I) ,in which radicals and characters have values specified in the claims and their versions. The proposed compounds act as potent antagonists of CCR (9) receptor. Animal testing has shown that these compounds are useful for treatment of inflammation, disease with a hallmark for CCR (9). The compounds as a whole are arylsulfamide derivatives and are used in pharmaceutical compositions, methods for treatment of CCR (9) mediated diseases and as a control in assays for identification of CCR (9) antagonists.EFFECT: increased efficiency of compounds application.26 cl, 2 tbl, 33 ex
Adamantyl derivatives useful for treatment of jnk-mediated disorder // 2626890
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to the heterocyclic compound of I formula or a pharmaceutically acceptable salt thereof, wherein R represents phenyl optionally substituted with one or more R'; R' is halo or methoxy; X represents CH; X1 represents C(=O)OCH3; Y represents N; Y1 It is OH, N(Y1')2, NHS(=O)2Y1', NHC(=O)Y1', NHC(=O)C(CH3)2OH or NHC(=O)C(CH3)2OC(=O)Y1'; each Y1' independently represents H, C1-6-alkyl or lower cycloalkyl; Y2 It is H. The invention also relates to formula I based on the compound of the pharmaceutical composition and the use thereof.EFFECT: new heterocyclic compounds useful for treating JNK-mediated disorder are obtained.12 cl, 5 tbl, 31 ex
ethod for macular area morphometric changes treatment in case of polymorbide somatic conditions // 2622759
FIELD: medicine.SUBSTANCE: optical coherent tomography of the retina is used for research. When the macular area relief is flattened and the average central thickness of the retina is increased beyond 300 mcm, diabetic macular edema is diagnosed. In the presence of cystic cavities in the nuclear and plexiform layers of the retina, cystic macular edema is diagnosed. Treatment by a 2.0% dorsopt solution is prescribed every morning and evening in the eye, continuously. In the presence of uneven retina contour and retina folds of irregular shape, membrane epiretinality is additionally diagnosed and instillation of 0.1% diclofenac solution three times a day in the eye during the month is additionally prescribed. Then rest for a month and repeated treatment with diclofenac solution of according to the scheme above. A course of: vinpocetine, pyracetam, detralex is prescribed again with repetition 6 months later.EFFECT: use of the invention makes it possible to increase the effectiveness of treatment of morphometric changes in the macular area with improved state of vitreomacular interface, reduced edema and decreased risk of vitreomacular complications.2 dwg, 1 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

Pure tetrahydrate l-arginine salt s-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidine-1-yl)-5-methyl-1-oxo-1h,-5h-benzo[i,j]hinolizin-2-carboxylic acid and method for production thereof // 2594166
FIELD: chemistry. SUBSTANCE: invention relates to method of producing substantially pure tetrahydrate of L-arginine salt S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidine-1-yl)-5-methyl-1-oxo-1H,-5H-benzo[i,j]hinolizine-2-carboxylic acid, having purity of at least 99% wt/wt as defined by HPLC, above method involves: (a) dissolution of L-arginine in mixture of acetone and water; (b) addition of S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidine-1-yl)-5-methyl-1-oxo-1H,-5H-benzo[i,j]hinolizine-2-carboxylic acid to solution obtained at step (a); (c) heating solution obtained at step (b) to obtain transparent solution; (d) optional treatment warm solution obtained at step (c), with activated carbon and filtering treated solution through 5 mcm filter and, finally, through 0.2 mcm filter; (e) dilution of hot solution obtained at step (d), with acetone and heating of diluted solution with reflux condenser for 30 minutes; (f) cooling solution obtained at step (e) at a temperature of 10-15°C to produce solid tetrahydrate of L-arginine salt S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidine-1-yl)-5-methyl-1-oxo-1H,-5H-benzo[i,j]hinolizine-2-carboxylic acid; (g) collecting tetrahydrate of S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidine-1-yl)-5-methyl-1-oxo-1H,-5H-benzo[i,j]hinolizin-2-carboxylic acid L-arginine salt obtained at step (f) by means of filtration and optional washing of it with acetone; and (h) of vacuum drying tetrahydrate of L-arginine salt S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidine-1-yl)-5-methyl-1-oxo-1H,-5H-benzo[i,j]hinolizin-2-carboxylic acid obtained at step (g), at temperature of 30-40 °C. EFFECT: method of producing tetrahydrate of L-arginine salt S-(-)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidine-1-yl)-5-methyl-1-oxo-1H,-5H-benzo[i,j]hinolizin-2-carboxylic acid of high purity (at least 99 % wt/wt) with high output, disclosed method of producing is accessible for large-scale synthesis. 1 cl, 1 tbl, 1 ex

ethod of combination treatment of non-small cell lung cancer stage 1b-111 with customization of adjuvant chemotherapy // 2593342
FIELD: medicine. SUBSTANCE: invention refers to medicine, namely to oncology, and can be used for combination treatment of non-small cell lung cancer (NSCLC) IB-stage III. Method involves a neoadjuvant chemotherapy and before tumour biopsy material is sampled, from which the total RNA and gene expression level monoresistance of RRM1, TYMS, ABCC5, ERCC1, TOP1, TOP2a, TUBB3 in tumour tissue are determined. Second stage involves courses of neoadjuvant chemotherapy, at the third stage a combination therapy involves radical pneumonectomy or lobectomy, during which the tumour tissue sample is taken as well as visually intact lung tissue/bronchus, in which determination of monoresistance gene expression levels is repeated, then, in the postoperative period on 15 day adjuvant chemotherapy is given with carboplatin dosed AUC6 in 2-5th day cycle at the level of monoresistance gene expression ERCC1 less than 0.5, in combination with one of the cytostatics, selection of which depends on the level of expression of analysed genes monoresistance. EFFECT: using the invention enables higher clinical effectiveness of treatment in NSCLC IB-stage III. 1 cl, 1 dwg, 4 ex

ethods of applying (+)-1,4-dihydro-7-[(3s, 4s)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(thiazolyl)-1,8-naphthiridine-3-carboxylic acid for cancer treatment // 2592231
FIELD: medicine. SUBSTANCE: to treat acute myologenic leukaemia (+)-1,4-dihydro-7-[(3S, 4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(thiazolyl)-1,8-naphthiridine-3-carboxylic acid in doses from approximately 30 mg/m2 to less than 50 mg/m2 and from more than 90 to 100 mg/m2 is introduced to patient, suffering from acute myelogenic leukaemia. EFFECT: treatment of acute myelogenic leukaemia with introduction of said compound in effective and safe doses. 11 cl, 20 dwg, 16 tbl, 11 ex

Inhibitors of akt activity // 2579513
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula , where each R1 and R2 is independently selected from hydrogen, C1-C10alkyl, optionally substituted OH and OR3, where R3 represents C1-C10alkyl, or R1 and R2 together represent oxo or optionally C1-C10alkyl O-substituted oxime; W represents O, NR′ or CRaRb, where R′ represents either hydrogen, or C1-C10alkyl; X is either absent or represents CR4R5, where each Ra, Rb, R4 and R5 are independently selected from substituents, given for R1 and R2; Y and Z independently represent substituted or non-substituted nitrogen or carbon (substituents for which are given in i. 1 of the invention formula), or Y and Z together form optionally substituted pyrazolyl, imidazolyl, pyriminidyl, 1,2,4-triazolyl (substituents for which are given in i. 1 of the invention formula); R7a and R7b represent H; R6a and R6b represent H or R6a and R6b can be combined with formation of C3-C6cycloalkyl, optionally substituted with one or two substituents, selected from C1-C6alkyl and OH; Cy is selected from C1-6alkyl(C3-C8)cycloalkyl, phenyl, pyridinyl and thienyl; m equals 0 or 1; R8 represents F. the invention also relates to particular compounds, given in i. 1 of the invention formula, to pharmaceutical composition and method for treating malignant tumour.EFFECT: novel methods for Akt inhibition.19 cl, 1 dwg, 153 ex

Novel crystalline acid-addition salts of tricyclic derivative or their hydrates and method for thereof obtaining // 2572820
FIELD: chemistry.SUBSTANCE: invention relates to novel crystalline acid-addition salt of tricyclic derivative in form of its hydrate, represented by the following chemical formula 2: , method for thereof obtaining, and based on its pharmaceutical composition for prevention and treatment of diseases, caused by PARP overactivity.EFFECT: obtained is novel crustalline acid-addition salt of tricyclic derivative in form of its hydrate, which is stable with respect to hygroscopicity and therefore useful in supporting quality in medication obtaining.4 cl, 3 dwg, 2 tbl, 22 ex

Tetrahydrocarboline derivative // 2572818
FIELD: chemistry.SUBSTANCE: claimed invention relates to field of organic chemistry, namely to novel heterocyclic compounds of general formula (I) and to its pharmaceutically acceptable salt or its solvate, where R1 represents halogen atom, C1-4 alkyl group, C1-4 alkoxygroup, C1-4 halogenalkyl group, cyanogroup, carbamoyl group, R2 represents hydrogen atom, R3 represents C1-4 alkyl group, R4 represents hydrogen atom or C1-4 alkyl group, ring A represents (i) C3-6 monocyclic carbon ring, including phenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cyclohexene, (iii) 5-6-membered monocyclic heterocyclic ring, containing one-two heteroatoms, selected from oxygen atom, nitrogen atom and sulphur atom, including thiophene, furan, isoxazole, imidazole, pyrazole, thiazole, pyridine or (iv) 9-membered bicycic heterocyclic ring, including indole, X represents nitrogen atom or carbon atom, T represents bond or linear C1-4 alkylene group, C2-4 alkenylene group or C2-4 alkinylene group, optionally substituted with two R5 (where R5 represents C1-4 alkyl group or aminogroup), U represents (i) methylene group, (ii)oxygen atom, (iii) -NR6- (where R6 represents hydrogen atom or methyl group) or (iv) 3-6-membered monocycle, including cyclobutane, cyclopentane, cyclohexane, phenyl, thiophene, pyrrolidine, pyrazole, imidazole, triazole, oxazole, piperazine, piperidine, tetrahydropyridine C7-8 bridge carbon ting, including bicyclooctane, bicycloheptane and imidazolidine, optionally substituted with one-three R7 (where R7 represents halogen atom, C1-4 alkyl group; hydroxygroup, C1-4 alkoxygroup or benzyloxy group), Y represents (i) bond or (ii) linear C1-3 alkylene group, optionally substituted with one or two R8 (where R8 represents methyl group), W represents bond or linear C1-3 alkylene group; Z represents methylene group, oxygen atom or sulphur atom, q represents integer number 1, r represents integer number from 0 to 5, and t represents integer number from 0 to 2, on condition that groups, represented by set R1, R2, R3, R5, R7 and R8, can be similar or different, respectively, and two R3 or R5, bound with one and the same carbon atom, can be taken together with carbon atom with formation of C3cycloalkyl, respectively. Invention also relates to pharmaceutical composition, pharmaceutical preparation and ENPP2 inhibitor, based on formula (I) compound.EFFECT: novel compounds, possessing inhibiting activity with respect to ENPP2, have been obtained.29 cl, 2 dwg, 3 tbl, 937 ex

Inhibitors of cell cycle checkpoint kinase 1 for amplification of dna-damaging agents // 2567044
FIELD: medicine, pharmaceutics.SUBSTANCE: claimed is application of inhibitor of cell cycle checkpoint kinase 1 (CHK1), representing some derivatives of N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrole[2,3-b]pyridine-3-yl), or N-(5-bromo-4-(3-(methylamino)piperidin-1-yl)-5-bromo-1H-pyrrole[2,3-b]pyridine-3-yl)nicotinamide, for amplification of DNA-damaging agent, with first dose of said inhibitor being introduced 1 day after DNA-damaging agent, and second dose - two days after DNA-damaging agent.EFFECT: claimed compounds amplified effect of DNA-damaging agent irinotecan or gemcitabine on tumour cells.30 cl, 13 dwg, 8 tbl, 12 ex

Using levofloxacin in aerosol form for treating mucoviscidosis // 2563809
FIELD: medicine.SUBSTANCE: group of inventions refers to medicine and can be used for treating mucoviscidosis in an individual suffering from P. aeruginosa pulmonary infection. That is ensured by administering an aerosol solution containing levofloxacin or ofloxacin in the concentration from approximately 50 mg/ml to approximately 200 mg/ml, and a bivalent or a trivalent cation in the concentration from approximately 50 mM to approximately 400 mM into the individual. That provides reducing expectoration P. aeruginosa density by min. 40%. There are also provided methods of treating mucoviscidosis and a method of reducing small airway resistance.EFFECT: group of inventions enables reducing bronchial obstruction in the mucoviscidosis patients.25 cl, 17 dwg, 32 tbl, 5 ex

Combination contact-type herbal medicinal product // 2561593
FIELD: medicine.SUBSTANCE: herbal medicinal product contains Sanguiritrine, Alpuizarine and additives: acetic acid 98%, chitosan, dimethyl sulphoxide, glycerol and water taken in certain amounts.EFFECT: combination contact-type herbal medicinal product has the effective prolonged antimicrobial and antiviral action.7 dwg, 2 tbl
Agent possessing lymphokinetic activity // 2560518
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry, particularly to an agent possessing lymphokinetic activity. The agent possessing lymphokinetic activity contains dihydroquercetin and arabinogalactan in ratio (weight parts) 1:5.EFFECT: agent described above possesses the synergic lymphokinetic activity.1 tbl, 4 ex
Pharmacological composition for treating secondary amyloidosis // 2557906
FIELD: medicine.SUBSTANCE: oral pharmacological composition for treating secondary amyloidosis contains alkaloid curcumin, betulin and piperine taken in certain proportions.EFFECT: composition is effective for treating secondary amyloidosis.

Purinoreceptor antagonists based on novel pyridoxin derivatives // 2554885
FIELD: chemistry.SUBSTANCE: invention relates to synthetic biologically active heterocyclic substances having antagonist activity on purinoreceptors and which are products of modifying pyridoxin, particularly n-(1,5-dihydro-3-R-8-methyl-9-hydroxy-[1,3]dioxepino[5,6-c]pyridinyl-6-azo)phenyl sulphonic acid and salt forms thereof of general formula I , where is selected from: a hydrogen atom, ethyl, heptyl or octyl.EFFECT: compounds of the given formula have high antagonist activity on purinoreceptors and can be used in medicine and veterinary.2 tbl, 5 ex

Using pyridoxin acetals derivatives as purinoreceptor antagonists // 2554883
FIELD: chemistry.SUBSTANCE: invention relates to use of synthetic biologically active heterocyclic substances as purinoreceptor antagonists, said substances having antagonist activity on purinoreceptors and being a product of modifying pyridoxin, particularly n-(1,5-dihydro-3-R1-3-R2-8-methyl-9-hydroxy-[1,3]dioxepino[5,6-c]pyridinyl-6-azo)phenyl sulphonic acid and salt forms thereof of general formula I , where R1 is a hydrogen atom or methyl, R2 is methyl, isopropyl.EFFECT: compounds of the given formula have high antagonist activity on purinoreceptors and can be used in medicine and veterinary.2 tbl
Alkaloid encapsulation method // 2554503
FIELD: chemistry.SUBSTANCE: invention relates to a method of encapsulating alkaloids. Said method is characterised by that an alkaloid is dissolved in dioxane, dimethyl sulphoxide or dimethyl formamide, then dispersed in a mixture of sodium carboxymethyl cellulose and acetone in the presence of E472c, adding distilled water, filtering and drying the obtained suspension of microcapsules, wherein the core/polymer ratio in the microcapsules is 1:3.EFFECT: invention provides a simple and fast process of producing alkaloid microcapsules and increases mass output.19 ex
ethod of alkaloid encapsulation // 2552323
FIELD: chemistry.SUBSTANCE: invention relates to method of encapsulation of alkaloids. Method of encapsulation of alkaloids consists in the fact that sodium alginate is used as envelope for microcapsules. Alkaloid is dispersed in dioxane and obtained mixture is dispersed into sodium alginate suspension in butanol, which contains polymer in presence of E472c, with the following mixing under specified conditions, after which distilled water is added, and then obtained suspension is filtered and dried at room temperature.EFFECT: method provides simplification and acceleration of process of obtaining microcapsules, reduction of loss in the process of their obtaining, and increase of output by weight.19 ex
Condensed heteroaryls and their application // 2552114
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of formula (1) and/or to their pharmaceutically acceptable salts, where A1 represents CH; A4and A5 independently represent CR2 or N; A2 and A3 together with ring B represent 5-membered heteroaryl or heterocycle, with said 5-membered heteroaryl or heterocycle being selected from where t represents 1 or 2; and R3 is independently selected from H, C1-C6 alkyl, C6-aryl, C3-C6-membered cycloalkyl, C(O)NRcRd, -ORb, heteroaryl, representing pyridine, and heterocycle, representing piperidine and tetrahydropyran; and each of said alkyl, aryl, cycloalkyl, heteroaryl and heterocycle can be substituted with one group, independently selected from C1-C6 alkyl, possibly substituted with one substituent, selected from -CONMe2, C3-membered cycloalkyl, -CN, -OMe, -pyridine, tetrahydropyran, -CO-morpholine, -CO-pyrrolidine, (3-methyl)oxetane; -OH; -C(O)Ra; -CN; -C(O)NRcRd; -NRcRd; -ORb; -S(O)nRe; halogen, and substituted with one group -COMe heterocycle, representing piperidine, on condition that when A4 represents CR2, A2 and A3 together with ring B are selected from structure (3), (5) or (6); represents single bond or double bond; R1 represents heteroaryl, representing 6-membered or 9-10-membered aromatic mono- or bicyclic ring, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; possibly substituted with one or two groups, independently selected from C1alkyl, C2alkinyl, -NRcRd, -NRcS(O)nRe, -ORb, halogen, halogenalkyl; R2 is independently selected from H; each Ra, Rb, Rc, Rd, and Re is independently selected from H; C1-C4alkyl, possibly substituted with one substituent, selected from -OH, -OMe, -CN, -NH2, -NMe2, C3-cycloalkyl; C2-C3alkenyl; C3alkinyl; C6aryl, possibly substituted with one or more substituents, selected from fluorine or methyl group; C3-membered cycloalkyl, possibly substituted with one substituent, selected from -OH and -CN; halogenalkyl; heteroaryl, representing pyridine; and substituted with one methyl group heterocycle, representing piperidine, or Rc and Rd together with atom (atoms) which they are bound to form 5-6-membered heterocyclic ring, representing pyrrolidine or morpholine; and in each case n is independently equal 2. Invention also relates to particular compounds, pharmaceutical composition, based on claimed compounds; method of inhibiting PI3K and/or mTOR activity and to application of claimed compounds.EFFECT: novel compounds, useful for inhibiting PI3K and/or mTOR activity have been obtained.15 cl, 16 ex

Bicyclic pyridines and analogues as sirtuin modulators // 2550821
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to a compound of formula (I), or its tautomer, or a pharmaceutically acceptable salt, where each of Z1 and Z2: N and CR, where at least, one of Z1 and Z2 represents CR, and each R: H, C1-C4 alkyl and -N(R3)(R3); W: -O-, -N(C1-C4) alkyl and -C(R6)(R6) -, and each R6: H and C1-C4 alkyl, or two R6, bound with the same carbon atom, are taken together with the formation of =O, R1: a phenyl and heterocycle, which represents a saturated or unsaturated 5-6-member monocyclic ring, containing 1-3 heteroatoms, selected from atoms N, S and O, or a 8-12-member bicyclic ring, each cycle of which is selected from a saturated, unsaturated and aromatic cycle, containing 1-2 nitrogen atoms, where R1 is optionally substituted with one or more substituents, independently selected from halogen, C1-C4 alkyl, =O, fluorosubstituted C1-C2 alkyl, -O-R3, -(C1-C4 alkyl)-N(R3)(R3), -N(R3)(R3) and -C(O)-N(R3)(R3), R2: a phenyl and heterocycle, which represents an unsaturated 5-6-member monocyclic ring, containing 1-2 heteroatoms, selected from atoms N and O, or represents dihydrobenzofuranyl, where R2 is optionally substituted with 1-2 substituents, independently selected from a halogen, -C≡N, C1-C4 alkyl, C1-C2 fluorosubstituted alkyl, -O-R3, -(C1-C4 alkyl)-N(R3)(R3) and -N(R3)(R3); each R3: -C1-C4 alkyl; or two R3 are taken together with a nitrogen atom, which they are bound with, with the formation of a 4-8-member unsaturated heterocycle, optionally containing one additional heteroatom, selected from N and O, where in case when R3 represents an alkyl, the said alkyl is optionally substituted with two -OH groups, and when two R3 are taken together with a nitrogen atom, which they are bound with, with the formation of a 4-8-member saturated heterocycle, the said saturated heterocycle is optionally substituted with fluorine by any carbon atom; and is substituted with hydrogen by any capable of substitution nitrogen atom; p equals 1, 2 or 3; X2 is selected from -C(=O)-♣, -C(=O)-O-♣, -C(=O)-NH-♣, -S(=O)2-NH-♣ and -C(=O)-NH-CR4R5-♣, where: ♣ represents a site, by which X2 is bound with R1; and each R4 and R5 represents hydrogen. The invention also relates to compounds of formulas (IV), (V), (VI), particular the compounds, a pharmaceutical composition based on the compound of formulas (I), (IV)-(VI) and to a method of treatment, based on the application of the said compounds.EFFECT: novel heterocyclic compounds, possessing sirtuin-modelling activity are obtained.26 cl, 2 tbl, 40 ex

Quinolone analogues and related methods // 2549895
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound of formula , wherein A and V independently represents H or a halogen; Q is absent; R4 independently represents H, a C1-C6 alkyl or C3-C6 cycloalkyl; R7 represents H; and R8 represents a C1-C10 alkyl substituted by OH or C1-C6 alkoxy; or C1-4 alkyl substituted by a 5-6-merous aromatic heterocyclic ring containing 1-2 heteroatoms specified in N and S, wherein the above aromatic heterocyclic ring is optionally substituted by a C1-C10 alkyl; or in -NR7R8, R7 and R8 together with N can form an optionally substituted azacyclic ring containing where applicable an additional heteroatom specified in H, O and S, as a cycle member, optionally substituted by a C1-C10 alkyl, which is substituted by a C1-C6 alkoxy; m is equal to 0; n is equal to 0. The invention also refers to a compound of formula (wherein the substitutes are those as specified in the patient claim), to a pharmaceutical composition containing a therapeutically effective amount of the compounds of formula (VIII), and to a method of treating or relieving a cell-proliferative disorder.EFFECT: compound of formula (VIII) inhibiting cell proliferation or cell apoptosis.12 cl, 1 dwg, 14 tbl, 55 ex

ethod of obtaining (+)-1,4-dihydro-7-[(3s,4s)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid // 2548031
FIELD: chemistry.SUBSTANCE: invention relates to method of obtaining (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, including: i) opening of epoxy cycle of Compound 3 by means of methylamine with obtaining compound 4, ii) separation of Compound 4 by means of chiral acid, selected from L-(-)-malic acid and L-(-)-pyroglutamic acid with obtaining Compound 5A or 5B, or iii protection of secondary amine of Compound 5A or 5B with tert-butoxycarbonyl protective group with obtaining compound 6 iv) methylation of free hydroxyl group of Compound 6 with methylating agent, v) removal of protection from amino groups by means of monohydrate of p-toluenesulphonic acid with obtaining Compound 8 and vi) interaction of Compound 8 with compound 10 with the following obtaining (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid.EFFECT: method improvement.29 cl, 3 tbl, 4 ex

New 2,3,4,5-tetrahydro-1-pyrido[4,3-b]indole derivatives and methods for using them // 2544856
FIELD: medicine, pharmaceutics.SUBSTANCE: given invention refers to new 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole derivatives, which can be used for modulating histamine receptors in individuals or for treating neurodegenerative diseases. The above derivatives have formula , wherein R1 is specified in an alkyl, substituted alkoxy or phenyl, and aralalkyl; R2 is specified in an alkyl, C6-C14-aryl optionally substituted by 1 to 5 substitutes specified in alkoxy and alkyl; R3 is an alkyl; and R4 is an alkyl.EFFECT: presented are the new compounds effective as histamine receptor modulators, and a based pharmaceutical composition.20 cl, 1 tbl, 1 ex

2,6-diaminopyridine compounds for treating amyloid protein related proteins and for treating ocular diseases // 2538208
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula , wherein pyridine rings A, B and C are independently unsubstituted or substituted by one or more substitutes independently specified in a group consisting of: C1-6-alkyl, halogen alkyl having 1-6 carbon atoms, Hal or OR13; L1 and L2 are independently specified in residues having formula or , wherein at least one of L1 or L2 has formula (b); R1 and R2 are independently specified in a group consisting of hydrogen, C1-6-alkyl and phenyl; R3 is specified in hydrogen and C1-6-alkyl; R4, R5, R6 and R7 are independently specified in a group consisting of hydrogen and C1-6-alkyl; R8, R9, R10 and R11 are independently specified in a group consisting of hydrogen and C1-6-alkyl; R12 is specified in a group consisting of hydrogen and C1-6-alkyl; R13 is independently specified in a group consisting of hydrogen, C1-6-alkyl and phenyl; p is equal to 1 or 2; q is equal to 0, 1 or 2, and Hal is specified in a group consisting of F, Cl, Br, and I, which can be used in treating a group of amyloid protein related disturbances and disorders.EFFECT: preparing the compounds which can be used in treating a group of amyloid protein related disturbances and disorders.17 cl, 1 dwg, 6 tbl, 13 ex

Compositions containing berberine or its analogues for treating skin diseases related to rosacea or blush // 2533458
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to the pharmaceutical industry and represents a local pharmaceutical composition for treating rosacea containing at least 0.02% berberine or a biologically equivalent berberine analogue, such as palmatine, and an ingredient specified in a group consisting of water, methanol, ethanol and dimethylsulphoxide, wherein berberine or the biologically equivalent berberine analogue represents the major pharmaceutically active ingredient.EFFECT: invention provides extending the range of products for treating rosacea.4 cl, 6 ex, 2 dwg

Tricyclic oxazolidinone antibiotic compounds // 2530884
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to a compound of formula (I)CE, wherein "-----" means a bond, V represents CH, and U represents CH or N, or "-----" means a bond, V represents CR6 and U represents CH, or also "-----" means a bond, V represents N and U represents CH, or "-----" is absent, V represents CH, and U represents CH2, NH or NR9; R0 represents H, or provided "-----" means a bond, can also represent C1-3alkoxygroup; R1 represents H, halogen, cyanogroup, C1-3alkyl or ethinyl; R2 represents H, acetyl or a group of formula -CH2-R3; R3 represents H, C1-3alkyl or C1-3hydroxyalkyl; R4 represents H, or provided n is other than 0, and R5 means H, can also represent OH; R5 represents H, C1-3alkyl, C1-3hydroxyalkyl, C1-3aminoalkyl, C1-3alkoxyC1-3alkyl, carboxyl group or C1-3alkoxycarbonyl; R6 represents C1-3hydroxyalkyl, carboxyl group, C1-3alkoxycarbonyl or a group -(CH2)q-NR7R8, wherein q is 1, 2 or 3 and each of R7 and R8 independently represents H or C1-3alkyl, or R7 and R8 together with a nitrogen atom to which they are attached, form a pyrrolodinyl or piperidinyl ring; R9 represents C1-3alkyl, 2-hydroxyethyl, 2-hydroxypropyl or 3-hydroxypropyl; A represents -(CH2)p-, -CH2CH2CH(OH)- or -COCH2CH(OH)-; G represents a phenyl group which is mono- or disubstituted in m- and/or n-position(s)by substitutes independently specified C1-4alkyl, C1-3alkoxygroup and halogen, or G means a group of one of formulas below G1 and G2, wherein Q means O or S, and X means CH or N; and each Y1, Y2 and Y3 represents CH, or one of Y1 and Y3 represents N, and the other one represents CH; and n is equal to 0, provided A represents -CH2CH2CH(OH)- or -COCH2CH(OH)-, and n is equal to 0, 1 or 2, provided A represents (CH2)p, wherein p is equal to 1, 2, 3 or 4, provided a sum of n and p is then equal to 2, 3 or 4; or a pharmaceutically acceptable salt of this compound.EFFECT: compound of formula (I)CE or its pharmaceutically acceptable salt are applicable as a therapeutic agent for preventing or treating a bacterial infection.29 cl, 2 tbl, 202 ex

5-hydroxymethyloxazolin-2-one derivatives for treating bacterial intestinal diseases // 2527769
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula wherein A means N or CH; and n is equal to 0 or 1; or their pharmaceutically acceptable salts for preventing or treating intestinal diseases caused by a bacterium specified in Clostridium difficile, Clostridium perfringens or Staphylococcus aureus.EFFECT: present invention possesses a high activity on the agents of intestinal infections, reduces a toxin load, spore production inducing thereby the minimum effect on the flora produced in the intestine.9 cl, 1 dwg, 3 tbl, 10 ex

5-amino-2-(1-hydroxyethyl)tetrahydropyran derivatives // 2525541
FIELD: chemistry.SUBSTANCE: invention relates to antibacterial compounds of formula , where R1 is an alkoxy group; R2 is H or F; each of R3, R4, R5 and R6 is independently H or D; V is CH and W is CH or N, or V is N and W is CH; Y is CH or N; Z is O, S or CH2 and A is CH2, CH2CH2 or CD2CD2; or a salt of said compound. The invention also describes a antibacterial pharmaceutical composition which contains the compound of formula (I) as a basic component, and use of the compound of formula (I).EFFECT: obtaining novel compounds possessing useful biological properties.25 cl, 2 tbl, 24 ex

Quinazolinone, quinolone and related analogues as sirtuin modulators // 2519779
FIELD: chemistry.SUBSTANCE: invention relates to a compound of structural formula or a salt thereof, where each of Z1, Z2 and Z3 is independently selected from N and C(R9), where not more than one of Z1, Z2 and Z3 is N; each R9 is hydrogen; and is a second chemical bond between either W2 and C(R12), or W1 and C(R12); W1 is -N=, and W2(R14) is selected from -N(R14)- and -C(R14)=, such that when W1 is -N=, W2(R14) is -N(R14)- and is a second chemical bond between W1 and C(R12); R11 is selected from phenyl and a heterocycle which is selected from a saturated or aromatic 5-6-member monocyclic ring, which contains one or two or three heteroatoms selected from N, O and S, or an 8-member bicyclic ring which contains one or more heteroatoms selected from N, O and S, where R11 is optionally substituted with one or two substitutes independently selected from halogen, C1-C4 alkyl, =O, -O-R13, -(C1-C4 alkyl)-N(R13)(R13), -N(R13)(R13), where each R13 is independently selected from -C1-C4alkyl; or two R13 together with a nitrogen atom to which they are bonded form a 5-6-member saturated heterocycle, optionally containing an additional heteroatom selected from NH and O, where if R13 is an alkyl, the alkyl is optionally substituted with one or more substitutes selected from -OH, fluorine, and if two R13 together with the nitrogen atom to which they are bonded form a 5-6-member saturated heterocycle, the saturated heterocycle is optionally substituted on any carbon atom with fluorine; R12 is selected from phenyl, a 4-6-member monocyclic saturated ring and a heterocycle, which is selected from an aromatic 5-6-member monocyclic ring which contains one or two heteroatoms selected from N and S, where R12 is optionally substituted with one or more substitutes independently selected from halogen, -C≡N, C1-C4 alkyl, C1-C2 fluorine-substituted alkyl, -O-R13, -S(O)2-R13, -(C1-C4 alkyl)-N(R13)(R13), -N(R13)(R13); R14 is selected from hydrogen, C1-C4 alkyl, C1-C4 fluorine-substituted alkyl, C1-C4 alkyl-N(R13)(R13), C1-C4 alkyl-C(O)-N(R13)(R13); and X1 is selected from -NH-C(=O)-†, -C(=O)-NH-†, -NH-S(=O)2-†, where † denotes the point where X1 is bonded to R11. The invention also relates to a pharmaceutical composition having sirtuin modelling activity based on said compounds.EFFECT: obtaining novel compounds and a pharmaceutical composition based on said compounds, which can be used in medicine to treat a subject suffering from or susceptible to insulin resistance, metabolic syndrome, diabetes or complications thereof.18 cl, 2 tbl, 52 ex

[4-(1-aminoethyl)cyclohexyl]methylamine and [6-(1-aminoethyl)tetrahydropyran-3-yl]methylamine derivatives // 2515906
FIELD: chemistry.SUBSTANCE: invention relates to antibacterial compounds of formula (I), where R1 represents alkoxygroup; U, V and W each represents CH or one of U, V and W represents N, and each other represents CH; A represents CH2 or O; G represents CH=CH-E, where E represents phenyl group, mono- or di-substituted with halogen, or G represents group of one of the formulas given below , , where Z represents CH or N, Q represents O or S and K represents O or S; or salt of such compound. In addition, invention also relates to pharmaceutical composition based on formula (I) compound for prevention or treatment of bacterial infection, as well as to application of claimed compounds for obtaining medication for prevention or treatment of bacterial infection.EFFECT: novel compounds, which can be applied in treatment of bacterial infection, are obtained and described.23 cl, 1 tbl, 13 ex

Novel chemical compounds - 2,4-diamino-1,3,5-triazine derivatives for preventing and treating human and animal diseases // 2509770
FIELD: chemistry.SUBSTANCE: invention relates to a 2,4-diamino-1,3,5-triazine derivative of general formula I, having protein kinase inhibitor properties, use thereof and a pharmaceutical composition based thereon. In general formula I Y is CH2, CHR', O, S, S(O) or S(O)2; X1, X2, X3 are independently selected from a CH groups or N; R1 is a C1-8 aliphatic group, C3-8 cycloalkyl, C6-10 aryl, ethylene-dioxyphenyl, methylene dioxyphenyl, pyridyl, each of which is optimally substituted with one or more identical or different groups R"; R' is hydrogen, OH, halogen, such as F, Cl, Br, I, or carboxyl or carboxamide, optimally N-substituted with (C1-6)alkyl, or cyano or halo(C1-8)alkyl, (C1-8)alkoxy, piperidinyl, optimally substituted with methyl; R" is R' or RD; R21, R22, R23, R24 are independently selected from groups F, Cl, Br, I, CN, (C1-16)alkyl; furthermore, R21 and R22 and/or R23 and R24 can be combined and represent one oxo (=O) group or together with a carbon atom can form a spirocycle containing 3 to 7 carbon atoms; furthermore, R21 and R24 together with two carbon atoms can form an aliphatic or aromatic ring containing 4 to 8 atoms, optionally substituted with one or more groups R'; RD is an oxo group =O or =S.EFFECT: invention can be used to treat autoimmune or cancerous diseases, rheumatoid arthritis and non-Hodgkin lymphoma.13 cl, 12 ex

Derivatives of oxazolidine antibiotics // 2506263
FIELD: chemistry.SUBSTANCE: invention relates to compound of formula I in which R1 represents halogen, methoxy group or cyano group; each of Y1 and Y2 represents CH, and one or two from U, V, W and X represent N, and each remaining one represents CH, or in case X, cam also represent CRa, or Ra represents halogen; A represents CH2CH(OH), CH2CH(NH2), CH(OH)CH(NH2) or CH(NH2)CH2, B represents CH2CH2, CH2NH or CONH, and D represents CH2, or A represents CH(OH)CH2, and B represents CH2NH, N(R2)CO or CONH, and D represents CH2, or B represents N(R2a)CH2, and D represents CH(OH), or A represents CH(OH)CH(OH), B represents CH2NH or CONH and D represents CH2, or A represents CH2CH2, and B represents CH2CH2, CH2NR3, NHCO, CONR4, CH2O, COCH2 or CH2CH2NH, and D represents CH2, or B represents CH2NH, and D represents CO, or A also represents CH2CH2, B represents NR4bCH2 and D represents CH(OH), or A represents CH=CH, B represents CH2NR5 or CONR6, and D represents CH2, or A represents C≡C, B represents CH2NH and D represents CO, or A represents COCH2, B represents CONH and D represents CH2, or A represents CH2N(R7), and B represents CH2CH2, a D represents CH2, or B represents CH2CH(OH), a D represents CH(OH), or A represents NHCH2, and B represents CH2NH, a D represents CH2, or B represents CH2NH, a D represents CO, or A represents NHCO, B represents CH(R8)NH or CH2CH2, and D represents CH2, or A represents OCH2, B represents CH=CH or CONH, and D represents CH2; R2 represents (C1-C4)alkyl; R2a represents hydrogen; R3 represents hydrogen, CO-(CH2)p-COOR3', (CH2)p-COOR3, (C2-C5)acyl or amino(C1-C4)alkyl, or also R3 represents (C1-C4)alkyl, which can be one or two times substituted with hydroxygroup, p stands for integer number from 1 to 4, and R3 represents hydrogen or (C1-C4)alkyl; R4 represents hydrogen or (C1-C4)alkyl; R4b represents hydrogen; R5 represents hydrogen or (C2-C5)acyl; R6 represents hydrogen or (C1-C4)alkyl; R7 represents hydrogen or (C1-C4)alkyl, which can be one or two times substituted with group, independently selected from hydroxygroup and aminogroup, R8 represents hydrogen or (C1-C4)alkyl; E represents one of the following groups (a-a1) where Z represents CH or N, and Q represents O or S, or E represents phenyl group, which is one or two times substituted in meta- and/or para-position with substituents, each of which is independently selected from group, including halogen, (C1-C3)alkyl and trifluoromethyl; or pharmaceutically acceptable salt of such compound. Formula I compound or its pharmaceutically acceptable salt is applied for obtaining medication or pharmaceutical composition for prevention or treatment of bacterial infection.EFFECT: derivatives of oxazolidine antibiotics for obtaining medication for treatment of bacterial infections.15 cl, 2 tbl, 214 ex

Antiviral compounds // 2505539
FIELD: chemistry.SUBSTANCE: in formula III: , each of X1 and X2 is independently selected from a bond, -CH2-, -O- or -S- and at least one of X1 and X2 is selected from -CH2-, -O- or -S-; each of R7 and R8 is independently selected from hydrogen or C6aryl, optionally substituted with one or more Ra and at least one of R7 and R8 is selected from C6aryl, optionally substituted with one or more Ra; each of Z1 and Z2 is selected from -N(RB)-, each of W1, W2, W3, W4, W5, W6, W7 and W8 is independently selected from N or C(Rd), where Rd in each case is selected from hydrogen; each of R1, R2, R9, R11, R12, R14, R15 and R16 in each case is independently selected from hydrogen or Ra; each of m and n is 0; Ra in each case is independently selected from halogen, hydroxy group, amino group, -LA and -Ls-Re; La in each case is selected from C1-C6-alkyl; values of radicals T, Rb, Rb', Re are given in the claim. The invention also relates to a pharmaceutical composition containing said compounds, a method of inhibiting HCV replication, a method of treating HCV infection and a method of producing said compounds.EFFECT: high efficiency of using compounds.7 cl, 6 tbl, 28 ex

Combined drug preparation // 2500415
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry, particularly to an oral preparation, possessing antihypoxic, nootropic and hypolipidemic action. The oral preparation possessing antihypoxic, nootropic and hypolipidemic action contains a combination of vinpocetine and gingko extract in the relation of 1:(3.5 -16).EFFECT: preparation possesses the pronounced antihypoxic, nootropic and hypolipidemic action.2 cl, 6 tbl

5-aminocyclylmethyloxazolidin-2-one derivatives // 2492169
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to antibacterial compounds of formula (I) , where one or two of U, V, W and X represent N, the remaining ones represent CH or, in case X, can also represent CRa, where Ra represents fluorine; R1 represents alcoxygroup, halogen or cyanogroup; R2 represents H, CH2OH, CH2N3, CH2NH2, alkylcarbonylaminomethyl or triazol-1-ylmethyl; R3 represents H or, when n=1, R3 can also represent OH, NH2, NHCOR6 or triazol-1-yl; A represents CR4; K represents O, NH, OCH2, NHCO, NHCH2; CH2NH5 CH2CH2, CH=CH, CHOHCHOH or CHR5; R3 represents H or together with R5 forms bond, or R4 can also represent OH, when K is not O, NH, OCH2 or NHCO; R5 represents OH or together with R4 forms bond; R6 represents alkyl; m=0 or 1 and n=0 or 1; and G is specified in i.1 of the formula; and to salt of such compound.EFFECT: obtaining antibacterial compounds.19 cl, 1 tbl, 44 ex

Hydrated crystalline camptothecin esters for treating cancer // 2483071
FIELD: medicine, pharmaceutics.SUBSTANCE: invention describes a crystalline hydrate of camptothecin esters, namely the crystalline hydrates of camptothecin aliphatic esters, a pharmaceutical composition containing the crystalline hydrates of camptothecin aliphatic esters for treating cancer or malignant tumours, as well as a method for treating cancer or malignant tumour.EFFECT: what is prepared and described is the new crystalline form of the hydrate of camptothecin aliphatic ester possessing low toxicity and good absorbability in a living body.19 cl, 5 ex, 10 tbl, 5 dwg

edication, possessing wound-healing activity // 2481836
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to medicine, in particular to pharmacology, to medication, possessing wound-healing activity. Application of hipaconitine as medication, possessing wound-healing activity is disclosed.EFFECT: hipactonitin possesses expressed wound-healing activity.6 tbl, 1 ex

Naphthyridine derivatives as potassium channel modulators // 2481347
FIELD: medicine, pharmaceutics.SUBSTANCE: given invention refers to a compound of formula I, wherein W and Z represent CH; Y represents CH2; wherein R1 and R2 independently represent H, halogen, CH2F, CHF2, CF3, CF2CF3, or C1-C6alkyl; R' represents H; R3 and R4 independently represent H, or C1-C3alkyl, all mentioned C1-C3alkyl groups and mentioned C1-C6alkyl groups are independently substituted by one or two groups independently substituted by one or two groups independently specified in OH, halogen, C1-C3alkyl, OC1-C3alkyl or trifluoromethyl; q=1 or 0; R5 represents C1-C6alkyl; and to pharmaceutically acceptable salts thereof. Furthermore, the invention refers to a composition, a tablet and pharmaceutical syrup having potassium channel modulation activity and containing the compound of formula I, to a method of preventing and treating diseases that are affected by the activation of potentially opened potassium channels.EFFECT: there are prepared and described the new biologically active compounds which may be effective in the prevention or treatment of diseases or disorders that are affected by potassium channel activity.21 cl, 2 ex, 1 tbl

Octahydropentalene compounds as chemokine receptor antagonists // 2481332
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to new compounds of formula (I) or to its stereoisomers, or to a pharmaceutically acceptable salt, wherein Ra represents H or (C1-C6)alkyl; Rb is specified in an optionally substituted group consisting of -(CH2)n-aryl, -CH(CH3)-aryl, -(CH2)n-arylaryl, -(CH2)n-arylheteroaryl, -(CH2)n-(C3-C8) cycloalkyl, -(CH2)n-heteroaryl, -(CH2)n-heterocyclyl and -(C3-C8) cycloalkylaryl; or Ra and Rb taken together with a nitrogen atom form 2,3-dihydro-1H-isoindolyl, decahydroisoquinolinyl, optionally substituted piperidinyl or optionally substituted pyrrolidinyl; Y is specified in an an optionally substituted group consisting of 5,6,7,8-tetrahydro[1,6]naphthyridinyl, -NH-(CH2)n-heterocyclyl, wherein NH is attached to carbonyl, and -heterocyclylaryl, wherein heterocyclyl is attached to carbonyl; and n is equal to 0, 1 or 2; wherein each heterocyclyl represents an independent non-aromatic ring system containing 3 to 12 ring atoms, and at least one ring atom specified in a group consisting of nitrogen, oxygen and sulphur; wherein each heteroaryl represents an independent non-aromatic ring system containing 3 to 12 ring atoms and at least one ring atom specified in a group consisting of nitrogen, oxygen and sulphur; and wherein the optional substitutes are independently specified in a group consisting of C1-C6-alkyl, C1-C6-alkoxy, halogen, CN, CF3, OCF3, NH2, NH(CH3), N(CH3)2, hydroxy, cyclohexyl, phenyl, pyrrolidinyl, -C(O)-piperidinyl, -N(H)-C(O)-C1-C6-alkyl and N(H)-S(O)2-C1-C6-alkyl. The invention also describes a pharmaceutical composition having chemokine receptor antagonist activity and a method of treating such diseases, such as rheumatoid arthritis, psoriasis, lupus, etc.EFFECT: there are prepared and described new chemical compounds that can be used as chemokine receptor antagonists and, as such, may be used in treating certain pathological conditions and diseases, particularly inflammatory pathological conditions and diseases and proliferative disorders and conditions, eg rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.23 cl, 59 ex, 2 tbl
Foam formulation of immune response modifier, method for preparing based drug preparation (version) and therapeutic kit containing said formulation // 2481108
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry, particularly to a foam formulation of an immune response modifier. The foam formulation of the immune response modifier, which contains: imiquimod; isostearic acid; a propellant; a mixture of preserving agents; sorbitan monostearate; a viscosifying agent taken in a specific ratio. A kit containing a drug preparation and an aerosol bottle. The use of the foam formulation for treating senile keratosis, basal cell skin cancer, anogenital warts, photodamaged skin, or for improving skin characteristics, cervical dysplasia, viral diseases, particularly herpes, skin metastases, skin damages caused by bites, self-healing epithelioma, for inducing interferon biosynthesis (versions).EFFECT: above-described foam formulation of the immune response modifier is stable.24 cl, 8 tbl, 1 ex

Antibacterial compounds based on sulphanilic acid and pyridoxine // 2480471
FIELD: chemistry.SUBSTANCE: invention discloses a product of modification of sulphanilic acid, and specifically n-(1,5-dihydro-3-methyl-8-R1-8-R2-9-hydroxy-[1,3]dioxepino[5,6-c]pyridinyl-6-azo)phenylsulphonic acid and salt forms thereof of general formula I: , where R1, R2 are selected from a group comprising: a hydrogen atom, methyl, a linear or branched alkyl or R1 and R2 together form a spirocycloalkyl group. Compounds of formula (I) have antibacterial activity, are more efficient with respect to both gram-negative bacteria Proteus vulgaris, Pseudomonas aeroginosa and gram-positive bacteria Staphylococcus aureus, and can be used in medicine and veterinary.EFFECT: improved properties.1 cl, 1 tbl, 11 ex
Pharmaceutical composition (versions) and methods for sterilisation thereof // 2474425
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a pharmaceutical composition for local application containing a therapeutic compound of an immune response modifier, sterilisation-resistant and applicable for local application immediately on tissue regions with skin damages wherein said composition is sterilised by electron-beam irradiation, and the therapeutic compound represents 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinoline-4-amine (imiquimod). Also, the invention refers to a packed composition for local application containing a packing material and said pharmaceutical composition.EFFECT: invention provides the sterilisation-resistant pharmaceutical composition.26 cl, 5 tbl, 1 ex

3-amino-6-(1-aminoethyl)tetrahydropyrane derivatives // 2471795
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new antibacterial compounds of formula I wherein R1 represents halogen or alkoxy group; each U and W represents N; V represents CH, and R2 represents H or F, or each U and V represents CH; W represents N, and R2 represents H or F, or U represents N; V represents CH; W represents CH or CRa, and R2 represents H, or also when W represents CH, may represent F; Ra represents CH2OH or alkoxycarbonyl; A represents group CH=CH-B, a binuclear heterocyclic system D, phenyl group which is mono-substituted in the position 4 by C1-4 alkyl group, or phenyl group which is di-substituted in positions 3 and 4 wherein each of two substitutes is optionally specified in a group consisting of C1-4 alkyl and halogen; B represents mono- or di-substituted phenyl group wherein each substitute is a halogen atom; D represents group wherein Z represents CH or N, and Q represents O or S; or to salts of such compounds.EFFECT: compounds are used for treating bacterial infections.13 cl, 2 tbl, 25 ex

Novel tricyclic derivative and pharmaceutically acceptable salts thereof, method for production thereof and pharmaceutical composition containing said derivative // 2470934
FIELD: chemistry.SUBSTANCE: invention relates to a novel tricyclic derivative of chemical formula 1 or pharmaceutically acceptable salts thereof: formula 1, where Y1, Y2 and Y3 independently denote H, C1-C10 alkyl with a straight or branched chain, hydroxy, C1-C10 alkoxy, -CCOR1, -NR2R3 or -A-B; A denotes -O-, -CH2-, -CH(CH3)-, -CH-N- or -CONH-; B denotes -(CH2)n1-Z, -(CH2)n2-NR2R3 or -(CH2)n3-OR1; Z denotes C5-C20 aryl, unsubstituted or substituted with R5 and selectively R6, C3-C10 cycloalkyl, unsubstituted or substituted with R5 and selectively R6, C1-C20 heterocyclic compound, unsubstituted or substituted with R5 and selectively R6; R1 denotes H or C1-C10 alkyl with a straight or branched chain; R2 and R3 independently denote H, C1-C10 alkyl with a straight or branched chain or -(CH2)n4R7; R5 denotes H, C1-C10 alkyl with a straight or branched chain, C5-C20 aryl or C1-C20 heterocyclic compound; R6 denotes H or C1-C10 alkyl with a straight or branched chain; R7 denotes -NR8R9, -COOR1, -OR1, -CF3, -CN, halogen or Z; R8 and R9 independently denote H or C1-C10 alkyl with a straight or branched chain; n1-n4 respectively denote an integer from 0 to 15; Y denotes H or C1-C10 alkyl with a straight or branched chain. The invention also relates to methods of producing a compound of formula 1, compositions containing the described compound and with effective inhibiting activity on poly(ADP-ribose)polymerase (PARP).EFFECT: obtaining and describing novel compounds which can be suitable for preventing or treating diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic neuropathy, inflammatory diseases, osteoporosis and cancer.23 cl, 123 ex, 7 tbl, 2 dwg

Substituted 4-aryl-1,4-dihydro-1,6-naphthyridine amides and use thereof // 2470932
FIELD: chemistry.SUBSTANCE: invention relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, method for production thereof, use thereof to produce a medicinal agent which inhibits MR activity.EFFECT: improved method.11 cl, 9 ex

[1,8]naphthyridine derivatives, useful as inhibitors of hcv virus replication // 2467007
FIELD: chemistry.SUBSTANCE: invention relates to novel derivatives of [1,8]naphthyridine, described by formula I(a), where Z represents -NR41-; A represents phenyl; each R10, R17, R31, R33, R35 and R41 in each case is independently selected from group, consisting of hydrogen, C1-C6alkyl, C1-C6haligenalkyl, phenyl, C3-C6cycloalkyl, -Ls-O-Rs, -Ls-C(O)Rs, -Ls-C(O)ORs and LE-Q-LE-(morpholine); X is selected from group, consisting of bond, -Ls-O-, -Ls-S- and -Ls-C(O)N(Rs)-; R22 is selected from group, consisting of halogen, C1-C6alkyl, phenyl, and phenyl C1-C2alkyl, and, optionally, is substituted with one R26, where R26 in each case is independently selected from group, consisting of halogen, hydroxy, nitro, C1-C6alkyl, -Ls-OSO2Rs; Y is selected from group, consisting of bond, -Ls-O-, -Ls-S(O)-, -Ls-C(O)N(R15) - and -Ls-S-, where R15 represents hydrogen; R50 represents -L1-A1, where A1 is selected from group, consisting of C1-C6alkyl and phenyl and L1 is selected from group, consisting of bond and C1-4alkylene, where A1 is optionally substituted with from one to three R30, and R30 in each case is independently selected from group, consisting of halogen, hydroxy, amino, azido, C1-C6alkyl, -Ls-O-Rs, -Ls-C(O)ORs, -LS-N(RSRS), -Ls-C(=NRs)RS', -Ls-C(O)N(RsRsO, -Ls-N(Rs)C(O)Rs', -LE-Q-LE'- (phenyl or naphthyl) and -LE-Q-LE'-(M5-M6heterocyclyl, which represents pyridine, pyrazine, pyrrolodine, furan, thiophene, piperidine); Ls in each case is independently selected from group, consisting of bond and C1-4alkylene; each RS and Rs' in each case is independently selected from group, consisting of hydrogen, C1-C6alkyl, C3-6alkenyl, C1-6alkoxy, C1-6alkoxyC1-C6alkyl and C1-6alkoxycarbonylC1-C6alkyl; each LE and LE' in each case is independently selected from group, consisting of bond, C1-4alkylene, -C1-4alkylene-NC(O)-C1-4alkylene-; Q in each case is independently selected from group, consisting of bond, -O-, -N(Rs)C(O)-, -C(O)N(Rs)- and -O-SO2-; each R17 and R30 in each case is optionally independently substituted with from one to three substituent(s), selected from group, consisting of halogen and hydroxy; and each heterocyclyl group in -LE-Q-LE'-(M5-M6heterocyclyl) in each case is optionally independently substituted with at least one or two substituents, selected from group, consisting of hydrogen, hydroxy, C1-C6alkyl, C1-6alkoxy, C1-6alkoxycarbonyl, phenyloxy and phenylC1-6alkoxycarbonyl, or to their pharmaceutically acceptable salts. Invention also relates to compounds of formula II(a), pharmaceutical composition based on claimed compounds, application of claimed compounds, method of inhibition of HCV virus replication, method of treating HCV infection.EFFECT: obtained are novel derivatives, useful in treatment of HCV infection.

Dihydroquinone and dihydronaphthyridine inhibitors of jnk kinase // 2466993
FIELD: chemistry.SUBSTANCE: invention relates to novel derivatives of dihydroquinone and dihydronaphthyridinone of formula (I) or to its pharmaceutically acceptable salts, in which X represents group CR11 or N; Y represents group -C(O)R3, oxazolyl or isoxazolyl; Z represents phenyl, pyrrolidinyl, piperidinyl, morpholinyl, tetrahydropyranyl, pyridinyl, pyrimidinyl or pyrazolyl, and is substituted with groups R1 and R2; R1 and R2 each independently represents H, halogen, CN group, C1-6alkyl or group -Y1-Y2-Y3-R8, or R1 and R2 together form group -O(CH2)nO-, where n represents 1 or 2; Y1 represents group -O-, -C(O)-, -C(O)O-, -C(O)NR9-, -NR9C(O), -S-, -SO2- or bond; Y2 represents heterocycloalkylene, C1-6alkylene or bond, where heterocycloalkylene stands for cycloalkylene group, in which one, two carbon atoms are substituted with heteroatoms O or N, where heterocycloalkylene group also contains, at least, two carbon atoms and cycloalkylene represents ; Y3 represents group -O-, -C(O)-, -C(O)O-, -C(O)NR9-, -NR9C(O)-, -SO2- or bond; R8 represents H, C1-6alkyl, C1-6alkoxy, cyclohexyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, tetrahydropyranyl, or group -NR9R10, where R8, different from H, is optionally substituted with C1-6alkyl, halogen, group -CF3 or group -OH; R9 and R10 each independently represents H or C1-6alkyl; R3 represents OH, C1-6alkyl, C1-6alkoxy, (C1-6alkoxy)-C1-6alkoxy; R4 represents C1-6alkyl, phenyl, cyclopropyl, cyclobutyl, cyclobutyl, cyclohexyl, tetrahydropyranyl or tetrahydrothiophene 1,1 -dioxide, and is optionally substituted with C1-6alkyl, hydroxyl group, C1-6alkoxy, halogen, nitro group, amino group, cyano group or halo-lower alkyl; R5 and R6 each independently represents H, halogen, C1-6alkyl, group -CF3, C1-6alkoxy; R7 represents H; R11 represents H. Invention also re4lates to pharmaceutical composition based on formula (I) compound.EFFECT: obtained are novel dihydroquinone and dihydronaphthyridinone derivatives, useful for treatment of disease mediated by JNK kinase.9 cl, 4 tbl, 38 ex
 
2550900.
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