(A61K31/496)

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

New derivative of 3-(4-(benzyloxy)phenyl)hex-4-ine acid, method for its production and pharmaceutical composition for metabolic disease prevention and treatment including it as effective ingredient // 2628077
FIELD: pharmacology.SUBSTANCE: invention relates to a compound represented by formula 1, its optical isomer or a pharmaceutically acceptable salt thereof: [Formula 1] , as well as to methods for its preparation and a pharmaceutical composition based on it.EFFECT: new connections are obtained, with the ability to activate the GPR40 enzyme, suitable for use for metabolic disease prevention or treatment.10 cl, 7 tbl, 77 ex, 2 dwg
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

Derivatives of hinoline, visualizing tau protein // 2627694
FIELD: pharmacology.SUBSTANCE: invention relates to a new quinoline derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is or , R1 is halogen or , in which R4 and R5 each independently represents hydrogen, a lower alkyl group, or R4, R5 and the nitrogen atom to which they are attached together form a 6-member nitrogen-containing aliphatic ring (where the nitrogen atom may be substituted by a lower alkyl group), or R4 and the nitrogen atom to which it is attached together with ring A form a 10-membered nitrogen-containing fused bicyclic ring (one carbon atom constituting the nitrogen-containing condensed bicyclic ring can be replaced by the oxygen atom), and R5 is a lower alkyl group where a line crossed by a dashed line means a bond of the above general formula with another structural moiety, R2 or R3 each independently represents NRaRb or -O-lower alkyl group (each alkyl group may be substituted with 1 to 2 substituents selected from halogen, hydroxy groups), ring A is unsubstituted or substituted by R6 (where R6 is one substituent selected from halogen and an -O-lower alkyl group (each alkyl group may be substituted with 1 to 2 substituents selected from halogen, hydroxy, Ra and Rb each represents hydrogen or a lower alkyl group, m and n denote an integer from 0 to 1, wherein at least one of R2, R3 and R6 is an -O-lower alkyl group substituted with one hydroxy group and one halogen. The invention also relates to a pharmaceutical composition, a composition for conformational disease diagnosis, treatment or prevention, a diagnostic kit based on a compound of formula (I), a method of treatment, a method for detection or staining of a protein-layer β-structure, a process for preparation of a compound of formula (I) and intermediates.EFFECT: new compounds are obtained that can be used to diagnose and treat conformational diseases, in particular, a disease having such a cardinal symptom as intracerebral accumulation of tau protein, for example, Alzheimer's disease.17 cl, 29 dwg, 26 tbl, 2 ex

Pharmaceutical compositions comprising water-insoluble antipsychotic agent and sorbitan esters // 2627469
FIELD: pharmacology.SUBSTANCE: invention relates to an injectable pharmaceutical composition for treatment of central nervous system disorders, comprising: (a) compound A-7: ,wherein component (a) is present in an amount of 15-35 wt %; (b) sorbitan laurate in an amount of 0.2-1 wt %; (c) polysorbate 20 in an amount of 0.05-0.8 wt %, and (d) an aqueous carrier. The invention also relates to a method for central nervous system disorders treatment, comprising administration of an effective amount of the said composition to a subject in need of such treatment.EFFECT: invention provides a composition which can be easily re-suspended, reduces local tissue response to antipsychotic means in sustained release formulations, and improves drugs compliance.11 cl, 4 tbl, 5 ex, 10 dwg

New pyrazole derivative // 2625790
FIELD: pharmacology.SUBSTANCE: in particular, invention relates to a compound represented by the following general formula (I): [wherein Ar1 is 2-methoxy-4-(2-pyridylmethoxy)phenyl, etc. and Ar2 is 1H-indole-6-yl group, etc.] or to salt thereof.EFFECT: increased efficiency of treatment.19 cl, 4 dwg, 1 tbl, 112 ex

Inhibitors of hepatitis c virus having rodlike chain and comprising {2-[4-(biphenyl-4-yl)-1h-imidazo-2-yl]pyrrolidin-1-carbonylmethyl}amine fragment // 2625787
FIELD: pharmacology.SUBSTANCE: invention relates to compound of formula (IV) or to pharmaceutically acceptable salt thereof, wherein R1 is selected from C1-6alkyl, optionally substituted with hydroxy or methoxy, and tetrahydropyran; R2 is a hydrogen atom; R3 is -C(O) OC1-6alkyl; R4 is methyl, methoxy or -CH2OCH3; R7 is selected from atom of fluoro, chloro, -CF3 and -OCF3; R8 independently represents methyl or hydroxymethyl; R9 is selected from -NHCH3, cyclopropyl, 2.2-dimethylcyclopropyl, tert-butyl, C1-6alkyl substituted with -OH, and imidazolyl; R10 is hydrogen atom or hydroxymethyl; a takes on a value of 1 or 2; and b takes on a value of 1 or 2. The invention also relates to heterocyclic compound of formula (V), specific compound, pharmaceutical composition based on compound of formulas (IV) or (V), method for preparing a target compound, intermediate compound, as well as to application of the produced compounds and method for inhibiting hepatitis C virus replication.EFFECT: new heterocyclic compounds are obtained, useful in the treatment of a viral infection of hepatitis C virus.15 cl, 1 dwg, 29 tbl, 24 ex
ethod for obtaining of rifampicine polymeric complexes with reduced toxicity and high antituberculosis activity // 2623877
FIELD: pharmacology.SUBSTANCE: invention relates to medicine and is a method for production of rifampicine polymeric complexes with reduced toxicity and high antituberculosis activity by rifampicine complexing with anionic polyelectrolyte in its aqueous solution. Poly-2-acrylamido-2-methylpropanesulphonic acid with a molecular weight of 20,000-40,000 is used as an anionic polyelectrolyte, complexation is performed at a weight ratio of polymer:antibiotic equal to 1.9-4.0.EFFECT: decreased rifampicin toxicity while preserving high level of anti-TB activity.1 tbl, 4 ex
ethod for complex treatment of infectious acute optical neuritis // 2623870
FIELD: medicine.SUBSTANCE: to treat infectious acute optical neuritis, retrobulbar infusions of dexamethasone and emoxipin are performed for 10 days via an irrigation system. Simultaneously, three immunomodulating preparations are used: 6 mg of polyoxidonium dissolved in 200.0 ml of physiological solution are injected intravenously every day; endonasal electrophoresis with 0.25% derinat solution at a current strength of 0.5-1 mA for 8 to 10 minutes; 2 ml of 12.5% of cycloferon are injected intramuscularly according to the scheme: the first 2 days - daily, the next 3 injections - every other day and the remaining 5 injections - every 3 days.EFFECT: use of the invention allows to restore the antibacterial and antiviral functions of the immune system, normalize the mechanisms of antioxidant protection, neuro-trophic activity, prevent the negative effects of GCS therapy, shorten the periods of inflammatory reaction arrest in the optic nerve and restore visual functions.2 ex
Azole derivatives // 2622639
FIELD: pharmacology.SUBSTANCE: invention relates to azole derivative of formula (I) or its pharmaceutically acceptable salt, wherein R1 is hydrogen atom or C1-5alkyl; R2 is hydrogen atom or C1-5alkyl; R3 is phenyl or pyridyl (where phenyl or pyridyl is optionally substituted with one or two fragments selected from the group consisting of C1-5alkoxy, halogen and trifluoromethyl atoms); each of R4 and R5, which can be the same or different, represent hydrogen atom or C1-5alkyl (where C1-5alkyl is optionally substituted with one fragment selected from the group consisting of hydroxy and C1-5alkoxy), or R4 and R5 together with nitrogen atom joining them form 4-7-membered saturated or unsaturated heterocycle, optionally compirsing one cyclic nitrogen, oxygen or sulfur atom, aside from the mentioned above joining nitrogen atom (where 4-7-membered saturated and unsaturated heterocycle is optionally substituted with one or two fragments, selected from the group consisting of hydroxy C1-5alkyl (where C1-5 alkyl is optionally substitued with one or two hydroxyl group), C1-5alkoxy, halogen atoms, cyano, C2-5alkanoyl, aminocarbonyl, mono-C1-5alkylaminocarbonyl, di-C1-5 alkylaminocarbonyl, trifluoromethyl, amino, mono-C1-5alkylamino, di-C1-5alkylamino and C2-5alkylamino, wherein the mentioned 4-7-membered saturated or unsaturated heterocycle optionally has C1-5alkylene fragment, joining two different cyclic carbon atoms), or form 2-oxa-6-azaspiro[3.3]hept-6-yl or 7-oxa-2-azaspiro[3.5]non-2-yl; azole cycle represented by formula (α) has any structure of group (II) formula, contained in invention formula, and wherein Ry is hydrogen atom or C1-5alkyl; X1 and X2 are such that: (i) if X1 means an ordinary link or fragment -CO-, X2 means -C1-5alkylene- or -O-C1-5alkylene-; and (ii) if X1 means a fragment -CONRx1-, X2means an ordinary link; Rx1 is hydrogen atom or C1-5alkyl; and cycle A is benzol cycle, pyridine cycle (where benzol cycle is optionally substituted with one or two fragments, selected from the group consisting of halogen atoms and C1-5alkoxy), 5-6-membered saturated or partly unsaturated heterocycle, containing one or two nitrogen atoms (where 5-6-membered saturated or unsaturated heterocycle is optionally substituted with one oxo group) or C3-7cycloalkane. The invention also relates to a pharmaceutical composition having antagonistic effect against V1b arginine-vasopressin receptor, and to agent for treating or preventing mood disorders, anxiety disorders or drug addiction, comprising azole derivative of formula (I) or its pharmaceutically acceptable salt as an active agent.EFFECT: azole derivative having antagonistic effect against V1b arginine-vasopressin receptor.12 cl, 22 tbl, 361 ex
Inhibitors of nonprilyzine // 2622288
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula , wherein R1 is selected from -OR7 and -NR8R9; R2 is H; X is -C1-9heteroaryl, selected from pyrazole, imidazole, triazole, benzotriazole, furan, tetrazole, pyrazine, thiophene, oxazole, isoxazole, thiazole, oxadiazole, pyridazine, pyridine, pyrimidine, benzoxazole, pyridylimidazole and pyridyltriazole; R3 is absent or is selected from H; Halogen; -C0-5alkylene-OH; -NH2; -C1-6alkyl; -CF3; -C3-7cycloalkyl; -C0-2alkylene-O-C1-6alkyl; -C(O)R20; -C0-1alkylene-COOR21; -C (O) NR22R23; -NHC(O)R24; =O; -NO2; -C(CH3) =N(OH); Phenyl optionally substituted with one or two groups independently selected from halogen, -OH, -CF3, -OCH3, -NHC(O)CH3 and phenyl; Naphthalenyl; Pyridinyl; Pyrazinyl; Pyrazolyl optionally substituted with methyl; Thiophenyl, optionally substituted by methyl or halogen; Furanyl; and -CH2-morpholinyl; and R3, when present, is attached to a carbon atom; R4 is absent or is selected from H; -HE; -C1-6alkyl; -C1-2alkylene-COOR35; -OCH2 O(O)CH (R36)NH2; -OCH2O(O)CH3; -CH2CH(OH)CH2OH; and phenyl or benzyl optionally substituted with 1 to 3 groups selected from halogen, -COOR35, -OCH3, -OCF3 and -SCF3; and R4, when present, is attached to a carbon or nitrogen atom; or R3 and R4 are taken together to form -phenylene-O- (CH2) 1-3- or -phenylene-O-CH2-CHOH-CH2-; A is 0 or 1; R5 is halogen; B is 0 or an integer of 1 to 3; Each R6 is independently selected from halogen, -OH, -CH3 and -OCH3; R7 is selected from H, -C1-8alkyl, -[(CH2)2O]1-3CH3, -C1-6alkylene-OC(O)R10, -C0-6alkylenemorpholinyl, -C1-6alkylene-SO2-C1-6alkyl and the structure of formula (a); R10 is -O-C3-7cycloalkyl; and R32 is -C1-6alkyl; R8 and R9 are H; R20, R21 and R35 are independently selected from H and -C1-6alkyl; R22 and R23 are independently selected from H, -C1-6alkyl, -CH2COOH, -(CH2)2OH, -(CH2)2OCH3, - (CH2)2SO2NH2, -(CH2)2N(CH3)2, -C0-1alkylene-C3-7-cycloalkyl and -(CH2)2-imidazolyl; or R22 and R23 are taken together to form a ring; R24 is selected from -C1-6alkyl; -C0-1alkylene-O-C1-6alkyl; Phenyl optionally substituted by halogen or -OCH3; and pyridinyl; and R36 is -CH (CH3) 2; and wherein the methylene linker on the biphenyl is optionally substituted with one or two -C1-6 alkyl groups; or a pharmaceutically acceptable salt thereof. Compounds of formula (I) are prepared by combining a compound of formula with a compound of formula 2 to provide a compound of formula I; Where P1 is also H. Also, the invention relates to an intermediate of formula 1, wherein P1 is H. The compounds of formula (I) are intended for the preparation of a medicament or pharmaceutical composition having inhibitory activity against non-prolamin (NEP). (a).EFFECT: compounds that have a non-lysine inhibitory enzyme activity.28 cl, 61 tbl, 25 ex

Antagonists of trpv1, containing dihydroxy group as substitute, and their use // 2621708
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, in which R1 represents -halo or -CF3; R4 represents -H or -CH3; each of R8 and R9 independently represents -H, -halo, -CH3 or -OCH3, each halo independently represents -F, -Cl, -Br or -I; and m means an integer of 0 or 1; (1) provided that if R4 represents -H, the m means 1; and (2) provided that if R4 represents -H and the carbon atom in the position a of the a-b bond is in (S)-configuration, the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group, a (S)-3-methyl group or a (R)-3-methyl group; (3) provided that if R4 represents -H, the carbon atom in position a of the a-b bond is in (S)-configuration, R8 represents -H and R9 represents -halo, then the methyl group connected to piperazinonyl ring represents a (R)-3-methyl group; (4) provided that if R4 represents -H, the carbon atom in position a of the a-b bond is in (S) configuration, R8 represents -F and R9 represents -F, then the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group or a (S)-3-methyl group; and (5) provided that if R4 represents -CH3, each of the carbon atoms in positions a and c and the a-b bond and the c-d bond is in (S) configuration,R8 represents -H, R9 represents -halo, and m means 1, the methyl group connected to piperazinonyl ring is a (S)-3-methyl group or a (R)-3-methyl group. Invention also relates to a compound of formula (II) or a pharmaceutically acceptable salt thereof, a specific compound of formula (Ia) or a pharmaceutically acceptable salt thereof and / or a co-crystal of fumaric acid. Invention also relates to specific compounds of formula (Ib) or a pharmaceutically acceptable salt thereof. The compounds as per invention are intended to inhibit the function of TRPV1 in a cell and to treat pain, pain associated with osteoarthritis, osteoarthritis, urinary incontinence (UI), ulcer, inflammatory bowel disease (IBD) or irritable bowel syndrome (IBS) in an animal.EFFECT: compounds having an affinity for the receptor TRPV1.38 cl, 11 tbl, 3 dwg, 16 ex

Apoptosis inducing agents selective for bcl-2 for cancer and immune diseases treatment // 2621052
FIELD: pharmacy.SUBSTANCE: invention relates to specific heterocyclic compounds containing the sulphonyl amino carbonyl group. The invention also relates to a pharmaceutical composition based on this compound.EFFECT: new heterocyclic compounds with inhibitory activity in terms of anti-apoptotic Bcl-2 proteins are obtained.2 cl, 3 tbl, 481 ex
Pyrazole quinolinone derivatives, their preparation and therapeutic application // 2621037
FIELD: pharmacy.SUBSTANCE: invention relates to compounds according to formula (I) , wherein R1, R2 and R3 are as defined in claim cl. 1. The compounds of this invention are reversible and selective inhibitors of type 2 methionine aminopeptidase (MetAP2). The invention also relates to intermediates for preparing the compounds of formula (I), drug and pharmaceutical compositions based on the compounds of formula (I) and their therapeutic application.EFFECT: increased efficiency of compounds application.24 cl, 2 tbl, 25 ex
Antimicrobial composition based on siloxane rubber // 2619836
FIELD: pharmacology.SUBSTANCE: invention is an antibacterial composition intended for the manufacture of implantable medical products based on polydimethylmethylvinylsiloxane rubber, comprising an aerosil, an anti-structuring additive, a silicic hydride, a platinum catalyst and an antimicrobial additive, characterised by composition containing rifampicin as an antimicrobial additive, the components in the composition are in a certain ratio, in parts by weight.EFFECT: invention provides high biocompatibility and long-lasting antimicrobial effect.2 tbl, 1 ex
Piperazine derivatives, their preparation and their use in treatment of insulin resistance // 2619110
FIELD: chemistry.SUBSTANCE: invention relates to the heterocyclic compound of the formula and its enantiomer, diastereoisomer and addition salts of the pharmaceutically acceptable bases or acids, where R1 refers to the group of -C(O)CR3R4CR5R6C(O)OH or the group of ; n and m refer to 0 or 1; L1 - group C (O) -; -C (O) O- or -S (O)2-; R2 refers to the carbocyclic aromatic group having 6 members, unsubstituted or substituted with one or more substituents, identical or different, selected from the alkoxy group having 1-6 carbon atoms, linear or branched, of halogen, CF3, the cyano-group (-CN), the sulfonylmethyl group (-S (O)2-methyl); the heterocyclic aromatic group with 5 or 6 members containing 1 or 2 heteroatoms, identical or different, selected from nitrogen and sulfur; the polyheterocyclic aromatic group with 9 members, with 3 heteroatoms, identical or different, selected from nitrogen and sulfur; the L2 is - carbocyclic group, wherein the carbocycle refers to the aromatic cycle with 6 members ; or the hydrocarbon group, linear or branched, with 1 to 5 carbon atoms; L2 refers to alkyl, linear or branched, with 1 to 5 carbon atoms; R3, R4, R5 and R6 refer to hydrogen atom; R7, identical or different, refers to alkyl, linear or branched, with 1 to 5 carbon atoms. The invention also relates to the process for preparing a compound of the formula (1) and the pharmaceutical composition based on the compounds of the formula (1).EFFECT: new heterocyclic compounds are obtained, useful in the treatment of pathologies associated with insulin resistance syndrome.11 cl, 1 tbl 5 ex
ethod of treating and preventing chronic inflammatory diseases of nasopharynx associated with inhalation exposure to benzene and formaldehyde in children // 2618469
FIELD: medicine.SUBSTANCE: invention can be used to treat and prevent chronic inflammatory diseases of nasopharynx (CIDN) in children aged 4 through 10 years old, living in area of industrial enterprises impact in conditions of atmospheric air pollution with benzene and formaldehyde. Treatment is carried out by combined administration of the following medicinal products to children: "Tonsilgon N" preparation orally in a dose for children aged 4 through 6 years old - 10 drops 3-4 times a day; for children over 6 years - 1 pill 3-4 times a day, for 21 days course; "Multi-Tabs Junior" 1 tablet once a day for 21 days; "Eslidine" 1 capsule twice a day before meals in the morning and evening for 21 days; "Zodac" preparation 5 mg once a day in a dose for children aged 4 through 6 years old; 10 mg once a day for children over 6 years old, for 21 days course, and simultaneously with children medical treatment, starting from the third day of drug administration, pulsed low-frequency magnetotherapy is employed for 10 minutes daily or every other day for 10 days course on nose sinuses or submandibular regions in the form of two-inductor technique with transverse arrangement of inductors and feedback sensor position at right supraclavicular region.EFFECT: invention provides treatment and prevention of chronic inflammatory disease of nasopharynx associated with exposure to benzene and formaldehyde in children.5 cl, 5 tbl

Arry-520 application for treatment of cancer for patients with low acs // 2617392
FIELD: medicine.SUBSTANCE: group of inventions relates to medicine, namely to oncology and can be used to treat cancer for patients with low concentrations of human α 1-acid glycoprotein (ACS). The methods of the invention include biological sample obtaining from a patient to determine the concentration of ACG and ARRY-520 administration to a patient with low concentration of ACG.EFFECT: increased efficiency of treatment due to a better response to the introduction of ARRY-520 at low ACG.57 cl, 6 tbl, 10 dwg, 10 ex
Preoperative preparation of patient with pheochromocytoma // 2616896
FIELD: medicine.SUBSTANCE: prior to operation, doxazosin is administered orally at the initial daily dose of 2 mg daily with subsequent daily dose increasing by 2-4 mg to normalize the blood pressure. The maximum daily dose of doxazosin is 16 mg. Daily intake of individualized therapeutic dose is continued until normalization of rheovasography readings - total peripheral vascular resistance index and photopletismography amplitude.EFFECT: method allows to stabilise hemodynamics for this patient group.2 ex
Solid drug form of indinavir with immediate release and method of obtaining thereof // 2616267
FIELD: pharmacology.SUBSTANCE: group of inventions relates to a solid form of indinavir sulfate, which is a capsule containing 67-79 wt % of indinavir sulfate, 10-20 wt % of lactose monohydrate, 7.7-15 wt % of Prosolv, 0.5-3 wt % of sodium croscarmellose (primellose) 0.5-1 wt % of stearic acid and/or its salt; and a method for its production, according to which indinavir sulfate, lactose monohydrate, croscarmellose sodium and Prosolv are mixed, dusted with stearic acid and/or its salt, encapsulated with simultaneous capsules dedusting and polishing.EFFECT: prompt active agent release and reduced timing of therapeutic effect.5 cl, 3 tbl
Pharmaceutical composition for nasal administration containing corticosteroid and quinolone or fusidic acid // 2614716
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutical composition in single dosage form in form of nasal spray for treating upper airway diseases. Pharmaceutical composition contains corticosteroid for local application and quinolone or fusidic acid, wherein weight ratio of corticosteroid for local application to quinolone or fusidic acid ranges from 0.02 to 20, and amount of quinolone or fusidic acid is less than 1 mg. Preferably composition can be used for treating acute or chronic sinusitis and nasal polyp. Invention also relates to pharmaceutical preparation in form of nasal spray containing several single doses; dosage form of pharmaceutical composition containing from 50 to 300 mcg of corticosteroid for local application and from 150 to 400 mcg of quinolone; use of composition for treating upper airway diseases.EFFECT: pharmaceutical composition under invention provides higher clinical effectiveness, reduced toxicity and minimization of used amount of active substances.19 cl, 2 ex

ethod of using 4-((1r,3s)-6-chloro-3-phenylindane-1-yl)-1,2,2-trimethylpiperazine and salts thereof in treating schizophrenia // 2613177
FIELD: medicine.SUBSTANCE: group of inventions relates to treating central nervous system diseases. Use of 4-((1R,3S)-6-chloro-3-phenylindane-1-yl)-1,2,2-trimethylpiperazine or its salt is disclosed for treating schizophrenia, schizophreniform disorder, schizo-affective disorder, delusional disorder, short-term psychotic disorder, induced psychotic disorder or bipolar disorder, every week or twice a week in form of immediate release composition (IR-composition), long, controlled or delayed release for peroral administration in dose of 20 mg/week up to 50 mg/week in terms of free base of 4-((1R,3S)-6-chloro-3-phenylindane-1-yl)-1,2,2-trimethylpiperazine and application of 4-((1R,3S)-6-chloro-3-phenylindane-1-yl)-1,2,2-trimethylpiperazine (cikronapine) or its salt for preparing drug for above treatment.EFFECT: introduction 1 time a week of declared dose is effective in reducing total PANSS score relative to daily administration of 10 mg; it can lead to increase of consent of patient.10 cl, 1 dwg, 1 tbl

Agent improving process of training, memory and cognitive functions, as well as for symptomatic therapy at autistic disorders // 2612791
FIELD: pharmaceutics.SUBSTANCE: invention relates to agent with nootropic and anti-autistic activity, representing tetrazole-containing derivative of 4-amino-3-phenyl-butyric acid of general formula (I): in which X=O, N, R2=H, CH3, X=O, R1=methyl, ethyl, H, X=N, R1=2-(pyridin-4-yl)ethyl, isopropyl. Invention also relates to pharmaceutical composition, medicinal agent and method of improving training processes, memory, cognitive functions.EFFECT: technical result: obtaining agent effective in treating disorders of cognitive functions, as well as for symptomatic therapy at autistic disorders.4 cl, 3 dwg, 16 tbl, 16 ex
Novel pyrazine derivatives // 2612138
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I), a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) modulate activity of cannabinoid receptor 2 (CB2). . In formula (I) R1 is a halophenyl or C3-C6-cycloalkyl-C1-C6-alkoxy; R2 is a C3-C6-cycloalkyl, azetidinyl or difluoroazetidinyl; one of R3 and R4 is hydrogen, and other is -(CR5R6)-R7 or -A-R7; or R2 is a C3-C6-cycloalkyl, and R3 and R4 together with a nitrogen atom, to which they are bonded, form piperidinylamine; R5 and6 are independently selected from hydrogen, C1-C6-alkyl, halogen-C1-C6-alkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C6-alkyl, phenyl, phenyl-C1-C6-alkyl and halophenyl; or R5 and6 together with carbon atom, to which they are bonded, form C3-C6-cycloalkyl or oxetanyl; R7 is cyano, carboxy, 5-methyl-[1,2,4]oxadiazol-3-yl, 5-amino-[1,2,4]oxadiazol-3-yl, thiazolyl, C1-C6-alkylthiazolyl, pyridinyl, C1-C6-alkylaminocarbonyl, hydroxy-C1-C6-alkyl, C1-C6-alkoxy-C1-C6-alkyl, aminocarbonyl, C1-C6-alkoxycarbonyl, di-C1-C6-alkylaminocarbonyl, phenyl-C1-C6-alkyl, pyridinyl-C1-C6-alkyl, halogen-C1-C6-alkylaminocarbonyl, 5-phenyl-2-methyl-oxazol-4-yl-alkyl, aminocarbonyl-C1-C6-alkyl or halogen; and A is cyclohexyl or thiophenyl, under condition specified in patent claim. Invention also relates to individual compounds, pharmaceutical composition, use of compounds and to a method of modulating CB2 receptor activity.EFFECT: technical result is obtaining novel compounds of formula (I) modulating activity of cannabinoid receptor 2 (CB2).19 cl, 111 ex

Pharmaceutical composition for treating, preventing or relieving movement disorders and its application // 2611376
FIELD: medicine.SUBSTANCE: group of inventions relates to treatment of movement disorders. Application of composition is proposed, which contains zolmitriptan or its pharmaceutically acceptable salt and 5-HT-receptor agonist buspirone or its pharmaceutically acceptable salt for treating, preventing or relieving movement disorders and use of set containing pharmaceutical composition of zolmitriptan or its salt and pharmaceutical composition of 5-HT-receptor agonist buspirone or its salt, at same prescription.EFFECT: technical result is increased efficiency of combined treatment in part of manifestations of delayed dyskinesia and relief of symptoms of Parkinson's disease in its model in rats.13 cl, 4 dwg, 9 ex
Substituted dihydropyrazolones for treating cardiovascular and hematologic diseases, use thereof, drug and method of treating and/or preventing // 2611012
FIELD: chemistry; pharmaceutics.SUBSTANCE: present invention relates to use of dihydropyrazolone derivatives of formula (I), in which radicals and symbols are defined in p. 1 of patent claim.EFFECT: making drug for treating and/or preventing cardiac diseases of blood circulation, cardiac failure, anemia, chronic diseases of kidneys and renal failure, as well as medicinal agent containing said dihydropyrazolone derivatives, and method of treating and/or preventing said diseases in human and animals.4 cl, 10 tbl, 180 ex

ethod for producing ciprofloxacin hydrochloride nanocapsules // 2609742
FIELD: chemistry.SUBSTANCE: invention relates to a method for producing ciprofloxacin hydrochloride nanocapsules. According to the invention ciprofloxacin hydrochloride powder is added to the suspension of gellan gum in butanol and 0.01 g of E472c agent, followed by chloroform, and the resulting nanocapsule suspension is filtered and dried. The core : shell ratio in the nanocapsules was 1:3, 1:1, 1:5 or 5:1.EFFECT: quick and easy process of producing ciprofloxacin hydrochloride nanocapsules and increase of mass yield.1 dwg, 5 ex

Use of sigma ligands in diabetes type-2 associated pain // 2608943
FIELD: chemistry.SUBSTANCE: invention relates to use of a sigma ligand, which is a 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine or a pharmaceutically acceptable salt thereof.EFFECT: prevention and/or treatment of pain associated with type 2 diabetes and related symptoms.6 cl, 9 dwg, 4 ex

Serotonin 5-ht3 receptor antagonists for application in treatment of lesional vestibular disorders // 2608458
FIELD: medicine.SUBSTANCE: invention relates to medicine and consists in application of serotonin 5-HT3 receptor antagonist for treatment of damages during vestibular disorders, wherein, mentioned damage is characterized by damage of internal ear cells and/or vestibular nerve cells, wherein, serotonin 5-HT3 receptor antagonist is selected from a group comprising ondansetron, palonosetron, tropisetron, lerisetron, alosetron, granisetron, dolasetron, bernesetron, ramosetron, azasetron, itasetron, zakoprid and cilansetron; and mentioned serotonin 5-HT3 receptor antagonist is introduced to the patient, at least during 5 days.EFFECT: treatment of damages during vestibular disorders.4 cl, 4 ex, 6 dwg
ethod of treating patients with x-linked agammaglobulinemia // 2608128
FIELD: medicine.SUBSTANCE: invention relates to medicine, namely to clinical immunology, and can be used for treating patients with X-linked agammaglobulinemia (X-AGG). For this patient gets replacement therapy of intravenous immunoglobulins. In addition from first day of treatment and every next six months after its start for first 10 days of each half of year patient gets 2 times day, in morning and evening, every 12 h oral administration of Polyoxidonium in dose of 12 mg.EFFECT: invention provides reduced number of infectious diseases in said category of patients due to recovery of adaptive capability of phagocytes.1 cl

Composition comprising an antibiotic and a dispersant or an anti-adhesive agent // 2607660
FIELD: medicine.SUBSTANCE: invention relates to products for treating or preventing of bacterial infection, comprising an antibiotic agent and a second agent representing a dispersant or an anti-adhesive agent, where antibiotic is a tobramycin, colistin, gentamycin or ciprofloxacin, and a dispersant or an anti-adhesive agent is a cysteamine.EFFECT: treatment or prevention of bacterial infection.1 cl, 10 dwg, 2 tbl, 2 ex
Ph-modulated compositions for pulmonary delivery // 2606175
FIELD: medicine.SUBSTANCE: invention relates to aerosol composition for delivery into patient's airway by inhalation, consisting of particles with aerodynamic diameter of 2.0-12.0 micron and combined total volume of 0.1–3.0 ml, wherein composition contains ciprofloxacin, pharmaceutically acceptable carrier and agent, affecting pH, which increases solubility of medicinal agent in carrier and is present in molarity, required to vary composition pH from 7.4 by at least 3.0 logarithmic units and no more than 5.4 logarithmic units; where agent, affecting pH, is acetic acid or its pharmaceutically acceptable salt, wherein said composition is characterized by low buffer capacity, such that, when it is in contact with fluid in human respiratory tract during certain period of time and under conditions of medium of human lungs, composition pH approaches pH 7.4 by 3.0 logarithmic units relative to composition pH before its introduction, besides, said composition is characterized by fact, that antibiotic in human lung acquires lower solubility as compared to its solubility in composition before its introduction.EFFECT: composition has low buffer capacity, which enables to change quickly pH of composition and provide formation of crystals, which slow down release of antibiotic in order to increase efficiency of treating infection.1 cl, 2 ex
Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors // 2606131
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula I given below, or to their stereoisomers, tautomers or pharmaceutically acceptable salts thereof. R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and ring C are as defined by the invention formula. Wherein the Y-B moiety and the NH-C(=X)-NH moiety are in the trans configuration.EFFECT: compounds of formula I are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.56 cl, 31 tbl, 649 ex

Oral solid preparation of compound antituberculosis drug and preparation method thereof // 2605388
FIELD: medicine.SUBSTANCE: oral solid preparation of a compound anti-tubercular drug is disclosed, wherein the active ingredients are rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride in weight ratio of 150:75:400:275, respectively. Compound oral solid preparation is a coated tablet with coated core or a coated three-layer tablet, wherein the two active ingredients rifampicin and isoniazid do not come to contact with each other directly. In the coated tablet with coated core in the inner core contains isoniazid or rifampicin and polymer, which is quickly destroyed and is quickly increased in volume during absorption of water, or rifampicin in the inner core is in the form of enteric solid dispersion. In the coated three-layer tablet the top layer and bottom layer separately and independently comprise a layer of rifampicin, including polymer which is quickly destroyed and is quickly increased in volume during absorption of water, and a layer of isoniazid/pyrazinamide, and a central layer is a layer of ethambutol hydrochloride including an inhibitor, which retains fast disintegration or release of ethambutol hydrochloride, or in the layer containing rifampicin, rifampicin is in form of enteric solid dispersion, where the weight ratio of rifampicin and enteric solid carrier is from 2:1 to 1:3.EFFECT: compound oral solid preparation according to the invention is characterized by high stability, higher bioavailability of rifampicin, that enhances treatment efficacy and reduces a probability of drug resistance.19 cl, 11 dwg, 11 tbl, 11 ex

Nasal antimicrobial agent // 2605313
FIELD: pharmaceutics.SUBSTANCE: invention refers to pharmaceutical industry and represents a nasal antimicrobial therapeutic agent containing active and auxiliary materials differing by the fact, that ciprofloxacin hydrochloride antibiotic is selected as active material, and as auxiliary materials are selected - propylene glycol, macrogol glyceryl hydroxystearate, benzalkonium hydrochloride, purified water, wherein the ingredients in the preparation are taken in certain proportions, wt%.EFFECT: invention provides expansion of the range of nasal application antibacterial agents for treating rhinitis, rhinopharyngitis and sinusitis.3 cl

Controlled-release pharmaceutical tablet for oral administration methods for preparation thereof // 2603469
FIELD: pharmaceutics.SUBSTANCE: invention relates to a controlled-release pharmaceutical composition for oral administration. Pharmaceutical composition comprises ciprofloxacin hydrochloride as an active principle. Method for preparation comprises a) granulating the first part of ciprofloxacin and water, b) granulating remaining part of said active ingredient with hydroxypropyl methylcellulose having low molecular weight and water, c) mixing ethyl cellulose and water, d) mixing the granulated material produced at step b) with the ethyl cellulose mixture in a fluidized bed, d) combining both granulated materials with a diluent-binding agent, diluent and sliding substance, e) compacting the produced material. Polymer coating is being optionally applied on a tablet . Also described is a pharmaceutical composition produced using said method. Tablets are characterized in that one part of the ciprofloxacin is released immediately, while another part of the active principle is located in a polymer diffusion matrix system, that allows the active principle to be released in a delayed manner.EFFECT: ciprofloxacin release profile allows administrating ciprofloxacin once a day.6 cl, 1 dwg, 6 tbl

Pyrazole derivatives // 2600983
FIELD: chemistry.SUBSTANCE: pyrazole derivatives are disclosed, which are encompassed by formula (I), in which radicals and groups are defined in patent claim and which are suitable for treating disorders mediated by peripheral cannabinoid 1 receptor 1.EFFECT: invention also discloses pharmaceutical compositions and methods related to use of said compounds.29 cl, 11 ex

Form of pharmaceutical composition multi-layer coating for oral administration containing omega-3 fatty acid or its alkyl ester, as well as medicinal agent based on statin // 2600804
FIELD: pharmaceutics.SUBSTANCE: invention relates to pharmaceutics. Pharmaceutical composition for oral administration is described containing: gelatine capsule core, coated with first and second layers of coating. Gelatine capsule core contains omega-3 fatty acid or its alkyl ester. First coating layer contains hydroxypropyl methylcellulose and copolymer of butyl methacrylate, (2-dimethylaminoethyl)methacrylate and methyl methacrylate with weight ratio of 1:2:1; where weight ratio of hydroxypropyl methylcellulose to said copolymer ranges from 1:0.8 to 1:10. Second coating layer contains medicinal agent based on statin as inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme (HMG-CoA) reductase.EFFECT: invention prevents sticking of gelatine capsules' cores to each other and deformation of gelatin capsules' cores, which can occur in process of aqueous coating application, invention also provides pharmaceutical composition disintegration and stability requirements compliance.13 cl, 9 tbl, 7 ex

Prognostic factors for treating cancer // 2600026
FIELD: medicine.SUBSTANCE: invention refers to medicine and represents a method for prediction of response of oncological patient with non-Hodgkin's lymphoma to anticancer therapy, including bortezomib and rituximab, characterized by that the method involves determination of level or amount of first prognostic factor and determination of presence or amount of second prognostic factor, wherein low level of CD68 or polymorphism of PSMB1 (P11A) correlates with, at least, one positive result. Invention also relates to a diagnostic kit for detecting oncological patients with non-Hodgkin's lymphoma, which are candidates for treating cancer with bortezomib and rituximab, as well as method of treating cancer in oncological patients with non-Hodgkin's lymphoma.EFFECT: invention implementation enables predicting positive response of oncology patient to combination therapy of bortezomib and rituximab.7 cl, 5 ex, 25 tbl, 8 dwg

ethod of producing nanocapsules of ciprofloxacin hydrochloride in sodium alginate // 2599007
FIELD: medicine.SUBSTANCE: invention relates to nanotechnology and medicine. Method of producing nanocapsules of ciprofloxacin hydrochloride in sodium alginate envelope is described. According to the method of invention ciprofloxacin hydrochloride powder is added to sodium alginate suspension in benzene, containing 0.01 g of preparation E472c as surfactant. Then butyl chloride is added. Obtained suspension of nanocapsules is filtered and dried. Process is performed at 25 oC during 15 minutes.EFFECT: method provides simple and fast process of producing nanocapsules and increases mass output.1 cl, 1 dwg, 5 ex

Substituted benzamide derivatives // 2595902
FIELD: chemistry.SUBSTANCE: invention relates to compound of formula (I), where R is hydrogen or C1-7alkyl; R1 represents -(CH2)n-(O)o-5-7-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, except for piperazine, where said heterocycloalkyl group optionally substituted with C1-7alkyl, hydroxy or halogen; n equals to 0, 1 or 2; o equals to 0 or 1; R2 represents CF3, C3-6-cycloalkyl, possibly substituted C1-7alkoxy or halogen, or represents indane-2-yl, or is 6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, optionally substituted with pyrimidinyl, or is 5-6 mono- or 9-10-member bicyclic heteroaryl containing 1-2 heteroatoms selected from N, O and S, where the heteroaryl is not thiazol and where said aromatic ring, is possibly substituted with one or two substitutes selected from C1-7alkyl, halogen, 5-6-member heteroaryl containing 1-2 heteroatoms selected from N and O, hydroxy, CF3, OCF3, OCH2CF3, OCH2-cycloalkyl, OCH2C(CH2OH)(CH2Cl)(CH3), S-C-1-7alkyl, C1-7alkoxy, CH2-C-1-7alkoxy, C2-7alkynyl or cyano, or substituted with -C(O)-phenyl, -O-phenyl, -O-CH2-phenyl, phenyl, and where said phenyl ring may be substituted with halogen, -C(O)OH or -C(O)O-C-1-7alkyl, or said aromatic ring, is possibly substituted with 5-6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, OCH2-oxetane-3-yl or O-tetrahydropyran-4-yl, possibly substituted C1-7alkyl; X is bond, -CH2NH-, -CHR″-, -(CHR″)q-O-, -O-(CHR″)q- or -(CH2)2-; Y is bond; R″ is hydrogen, C1-7alkyl, CF3, C1-7alkoxy; q is equal to 0, 1, 2 or 3; or pharmaceutically acceptable acid addition salt thereof, except for compounds specified in patent claim. Invention also relates to specific compounds specified in patent claim. Compounds are intended for producing medicinal agents, showing affinity to TAAR1.EFFECT: technical result: benzamide derivatives having high affinity to receptors associated with TAAR1 trace amines.9 cl, 1 tbl, 323 ex

Use of nanophospholipid composition of rifampicine together with protionamide or its nanophospholipid form in treatment of tuberculosis // 2595881
FIELD: medicine.SUBSTANCE: invention refers to medicine and pharmacology and concerns using of nanophospholipid composition of rifampicine together with protionamide or its nanophospholipid form for treatment of tuberculosis.EFFECT: invention provides reducing of collateral toxic damage.1cl, 1 tbl

Pi3-kinase inhibitors and use thereof // 2595718
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds which are irreversible PI3-kinase inhibitors, and conjugates containing one or more PI3-kinases, containing cysteine residue, which is covalently and irreversibly boned with PI3-kinase inhibitor. Invention also discloses pharmaceutical compositions containing said compounds.EFFECT: compounds are intended for treating disorders and diseases associated with PI3-kinase.19 cl, 16 dwg, 26 tbl, 52 ex

Nitrogen-containing saturated heterocyclic compounds // 2595136
FIELD: pharmaceutics.SUBSTANCE: invention relates to a compound of formula [I] and its pharmaceutically acceptable salts thereof. Compound of formula [I] possesses renin-inhibitory activity. In formula [I] R1 is C3-6-cycloalkyl group; R denotes lower alkyl group or makes 5-6-member ring by binding with R22 at each end; T is a carbonyl group; Z is -O-, -NH- or single bond; and R3, R4, R5 and R6 are a hydrogen atom. Invention also relates to a pharmaceutical composition containing a compound of the invention, and to a compound of formula [II].EFFECT: obtaining novel compounds of formula [I], having renin inhibitory activity.11 cl, 93 tbl, 422 ex

ethods for treatment using selective bcl-2 inhibitors // 2593231
FIELD: medicine; pharmaceuticals. SUBSTANCE: group of inventions concerns using 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazine-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulphonyl)-2-(1H-pyrrolo[2,3-b]pyridine-5-yloxy)benzamide, or 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-ene-1-yl]methyl}piperazine-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulphonyl]-2-(1H-pyrrolo[2,3-b]pyridine-5-yloxy)benzamide, or their pharmaceutically acceptable salts for preparing drug. This device can be used for treating autoimmune diseases-systemic lupus erythematosus, lupous nephritis or Sjogren's syndrome in patient administered with therapeutically effective amount of this agent, for example, in range from 0.001 mg/kg to 1,000 mg/kg. Drug can be used in combination with binding protein for additional increase of efficiency of compound in desired place action. EFFECT: inventions provide most selective inhibition of activity antiapoptotic Bcl-2 proteins with most low affinity than inhibition of activity of other proteins of family Bcl-2, including Bcl-xL, that require smaller doses of used compounds. 12 cl, 9 ex, 12 dwg, 4 tbl

ethod of producing phenoxypyridine derivative // 2590158
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing a compound or salt thereof of formula (I), which involves reaction of compound or salt thereof of formula (II), and aniline derivative of formula (III), in water or a mixed solvent of water and organic solvent in presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide and substantially in absence of a base:.EFFECT: technical outcome is a novel improved method of producing a compound or salt thereof of formula (I).3 cl, 1 tbl, 5 ex

Aripiprazole compositions and methods for transdermal delivery // 2589689
FIELD: medicine.SUBSTANCE: invention refers to medicine. Described is a composition of liquid or gel-like composition contains aripiprazole in the form of plaster for transdermal delivery. EFFECT: composition has acceptable in vitro characteristics and good bioavailability.4 cl, 3 dwg, 2 tbl

ethod of producing chiral hydrazides // 2588570
FIELD: chemistry.SUBSTANCE: invention relates to methods of producing chiral compounds, particularly to method of producing chiral compound of formula (II). Method involves reaction of chiral compound of formula (I) with H2N-NH-CHO in solvent to obtain compound of formula (II). In formulae (I) and (II) Y denotes substituted or unsubstituted aryl fragment, wherein substituted aryl fragment contains 1, 2 or 3 substitutes, which are selected from group comprising halogen, alkyl and C1-C6alkoxy group. Invention also relates to methods of producing chiral compounds of formulae (III)-(V) using method of producing chiral compound of formula (II), chiral compounds of formulae (II)-(V) and use thereof to obtain fungicidal agent, preferably of posaconazole.EFFECT: in formulae (III)-(V) Y has value specified for compounds of formulae (I) and (II); Raa, Rbb and Rcc can be identical or different and denote alkyl or aryl residue; R1 denotes an alkyl residue.31 cl, 2 dwg, 3 ex

ethod of producing chiral triazolones // 2585760
FIELD: chemistry.SUBSTANCE: invention relates to method of producing compound of formula (IVb), involving (1.1) using compound of formula (Ia) or salts thereof (Ia) (1.2) using phosgene derivative of formula (IIb) (IIb), wherein Y1N-and Y2N-denote identical or different optionally substituted nitrogen-containing heterocyclic fragments, preferably selected from group comprising imidazolyl and benzimidazolyl; (1.3) using compound of formula (III) or salts thereof (III), in which R1 denotes ethyl, and in which R denotes h; (2) mixing and introduction into reaction of compounds of formulae (Ia), (IIb) and (III) in solvent in any order to obtain reaction mixture containing Chiral compound of formula (IVb) (IVb). Invention also relates to chiral compound of formula (IVb), to optionally crystalline chiral compound of formula (IVb) and to compound of formula (IIc) (IIc) to obtain compound of formula (IVb) or formula (IVd). EFFECT: technical result is new non-toxic method of producing compound of formula (IVb).29 cl, 5 dwg, 6 ex
Pyrazole compounds as sigma receptor inhibitors // 2582338
FIELD: medicine.SUBSTANCE: invention refers to compounds of general formula (1) shown below, or their pharmaceutically acceptable salts having pharmacological activity towards sigma receptor, to methods for producing these compounds and to pharmaceutical compositions containing them, and to using them for treating and/or preventing sigma receptor-related diseases. In the compounds of formula (I), R1 represents phenyl substituted by halogen atoms; naphthyl; C5-6 cycloalkyl; or quinolyl; R2 and R3 are independently specified in H and C1-6 alkyl group; R4 and R5 together with the nitrogen atom to which they are attached, form a substituted or unsubstituted 5-6-merous heterocyclyl group with one or two heteroatoms specified in O or N, wherein the substitute is specified in C1-6alkyl and C1-6alkanoyl; X represents an oxygen atom or a CH2 group; m is specified in 1, 2, 3 and 4; and n is specified in 1, 2, 3 and 4.EFFECT: higher efficacy.13 cl, 2 tbl, 50 ex
 
2550934.
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