(A61K31/496)

2-aminopyrasine derivatives as csf-1r kinase inhibitors // 2642777
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group; R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl; n is 1; X is NH; V is -N=, W is -C(Z)=; Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl; ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group; [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3; x is 0 or 1; Alk1 is an unsubstituted C1-3 alkylene group; X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3; R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring; and R17 represents a hydrogen atom; where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring; R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group; ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or prevention of diseases or disorders mediated by CSF-1R kinase, as well as application of the said compounds for preparation of a medicament useful for treatment of such diseases.EFFECT: increased application efficiency.18 cl, 59 ex
ultifunctional quinoline derivatives as antineurodegenerative agents // 2642466
FIELD: chemistry.SUBSTANCE: invention relates to a hydroxy-derived quinoline of the formula (I) or to a pharmaceutically acceptable salt thereof, (I) wherein R1 is hydrogen, (C1-C3)alkyl, (C1)alkylene(C3)cycloalkyl, (C1)haloalkyl or (C1)alkylene(C6)aryl; R2 is hydrogen or halogen; R3 is hydrogen, halogen, (C1)alkyl or (C1)alkoxy; R4 is hydrogen, halogen, (C1)alkyl, (C1)alkoxy or (C1)haloalkyl; R5 and R6 are hydrogen; and R7 is (C9-C15)alkanol, (C1)alkylenepiperazinyl(C1-C2)alkanol, (C1-C8)alkylenepiperazinyl (C1-C2)alkyl, (C10-C13)alkylene OCOCH3, (C1)alkylene(C1)alkylamino(C3)alkynyl, (C1)alkyleneamino(C8)alkanol or (C1)alkyleneamino(C6)alkanol(C1)alkylene(8-methoxyquinolin-2-yl); or (II), where R1, R2, R3, R4 and R6 each is as described in (I) above; R5 is (C11-C12)alkanol, and R7 is hydrogen. The invention also relates to a pharmaceutical composition based on the formula (I) compounds, a method for treatment of Alzheimer's disease, traumatic brain injury and/or damage to the spinal cord and a method for improvement of the ability of learning and/or memory in a patient suffering from Alzheimer's disease, based on the formula (I) compound.EFFECT: new hydroxy derivatives of quinoline have been obtained that have useful biological properties.13 cl, 13 dwg, 9 ex
Injectable veterinary composition // 2641962
FIELD: veterinary medicine.SUBSTANCE: to treat bacterial infection, an injectable veterinary composition containing quinolone and cephalosporin or their pharmaceutically acceptable salts with propylene glycol with dicaprilocaprate and/or glycerylcaprilocaprate in an oil suspension is administered to the animal. An injectable veterinary composition for bacterial infection treatment in an animal, comprising at least one other therapeutic agent in an oil suspension, is also provided.EFFECT: group of inventions allows treatment of bacterial infection in pigs or cattle.13 cl, 3 tbl, 3 dwg, 3 ex
Partly saturated nitrogen-containing heterocyclic compound // 2641291
FIELD: chemistry.SUBSTANCE: invention relates to a compound of the formula (I'), (wherein W represents the formula -CR11R12CR13R14-; R11 represents a hydrogen atom, a fluorine atom, C1-4 alkyl or phenyl; R12 represents a hydrogen atom, a fluorine atom or C1-4 alkyl; provided that R11 and R12, together with the adjacent carbon atom, optionally form C3-8 cycloalkane or tetrahydropyran; R13 represents a hydrogen atom, a carbamoyl, C1-4 alkyl (C1-4 alkyl is optionally substituted by one group selected from the group consisting of hydroxy, C1-3 alkoxy and di-C1-3 alkylamino), halo-C1-4 alkyl, phenyl, pyridyl, benzyl or phenethyl; R14 represents a hydrogen atom, C1-4 alkyl or halogen-C1-4 alkyl; Y represents a single bond or C1-6 alkanediyl (C1-6 alkanediyl is optionally substituted by one hydroxy group and one of the carbon atoms in C1-6 alkanediyl is optionally substituted by cycloalkpropane-1,1-diyl); R2 represents a hydrogen atom, C1-6 alkyl, C3-8 cycloalkyl {C3-8 cycloalkyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl (C1-6 alkyl is optionally substituted by one phenyl group), phenyl (phenyl is optionally substituted by one halogen atom), C1-6 alkoxy [C1-6 alkoxy is optionally substituted by one group selected from the group consisting of C3-8 cycloalkyl, phenyl (phenyl is optionally substituted by one group selected from the group consisting of a halogen atom and C1-6 alkyl) and pyridyl (pyridyl is optionally substituted by one halogen atom)], C3-8 cycloalkoxy, phenoxy (phenoxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl, C3-8 cycloalkyl and halogen-C1-6 alkyl) and pyridyloxy (pyridyloxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl, C3-8 cycloalkyl and halogen-C1-6 alkyl)}, phenyl (phenyl is optionally substituted by one to three groups that are the same or different and which are selected from the group of α3 substituents), naphthyl, indanyl, tetrahydronaphthyl, pyrazolyl [pyrazolyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl and phenyl (phenyl optionally substituted by one C1-6 alkyl)], imidazolyl [imidazolyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl and phenyl], isoxazolyl [isoxazolyl is optionally substituted by one phenyl group (phenyl is optionally substituted by one halogen atom)], oxazolyl [oxazolyl is optionally substituted by one or two groups that are the same or different and which are selected from the group consisting of C1-6 alkyl and phenyl], thiazolyl [thiazolyl is optionally substituted by one or two groups that are the same or different and which are selected from the group consisting of C1-6 alkyl, phenyl and morpholino], pyridyl (pyridyl is optionally substituted by one or two groups that are are the same or different and are selected from the group of α5 substituents), pyridazinyl [pyridazinyl is optionally substituted by one C1-6 alkoxy (C1-6 alkoxy is optionally substituted by one C3-8 cycloalkyl group)], pyrimidinyl [pyrimidinyl is optionally substituted by one group selected from the group consisting of halogen-C1-6 alkyl, C3-8 cycloalkyl, phenyl and phenoxy (phenoxy is optionally substituted by one C1-6 alkyl)], pyrazinyl [pyrazinyl is optionally substituted by one group selected from the group consisting of C1-6 alkoxy (C1-6 alkoxy is optionally substituted by one C3-8 cycloalkyl), and phenoxy (phenoxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl and C3-8 cycloalkyl)], benzothiophenyl, quinolyl, methylenedioxyphenyl (methylenedioxyphenyl is optionally substituted by one or two fluorine atoms), azetidinyl (azetidinyl is optionally substituted with one pyrimidinyl group), piperidinyl (piperidinyl is optionally substituted by one group selected from the group consisting of pyrimidinyl, phenyl-C1-3 alkyl, C3-8 cycloalkyl-C1-3 alkylcarbonyl and phenyl-C1-3 alkoxycarbonyl) or the following formula (I") -CONR5CH2-R6 (I") [wherein in formula (I") R5 represents a hydrogen atom or C1-3 alkyl and R 6 is phenyl (phenyl is optionally substituted by one group selected from the group consisting of a halogen atom, halogen-C1-6 alkyl and phenyl)], Y4 represents C1-4 alkanediyl; R3 represents a hydrogen atom or methyl; R4 represents -COOH or -CONHOH).EFFECT: compound has a superior PHD2 inhibitory effect.16 cl, 28 tbl, 11 ex

Derivatives of azaindasole or diazaindasole type for pain treatment // 2640046
FIELD: pharmacology.SUBSTANCE: invention relates application of a compound of formula for treatment or prevention of pain associated with at least one Trk protein. The radicals and symbols in formula (I) have the definitions indicated in the claims. The invention also relates to a pharmaceutical composition comprising a compound of formula (I) as an active substance.EFFECT: compound application efficiency increase.15 cl, 6 dwg, 1 tbl, 35 ex
Indasole inhibitors of wnt signal path and their therapeutic applications // 2638932
FIELD: medicine.SUBSTANCE: invention relates to a indasole derivative that has the following formula , or its pharmaceutically acceptable salt, as well as a pharmaceutical composition containing it. The invention relates to methods for treatment of disorders characterized by the activation of Wnt-signalling pathways (e.g., cancer, abnormal cell proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), including introduction of a therapeutically effective amount of this compound or pharmaceutically acceptable salt thereof. This compound can also be used in modulation of cellular events, mediated by Wnt-signalling, as well as for treatment of genetic diseases and neurological conditions/disorders/diseases due to mutations or disregulation of the Wnt pathway and/or one or more components of Wnt-signalling.EFFECT: inhibits the Wnt signalling pathway and can be used to treat various diseases and pathologies.28 cl, 8 tbl, 8 ex

Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods for application // 2638552
FIELD: pharmacology.SUBSTANCE: invention relates to pyrazol-4-yl-heterocyclylcarboxamide compounds of Formula I , including their stereoisomers, tautomers and pharmaceutically acceptable salts, wherein X is a thiazolyl, pyrazinyl, pyridinyl or pyrimidinyl group, R1 and R2 have the meanings indicated in the claims. The compounds of formula I are useful for Pim kinase inhibition and for treatment of disorders such as cancer mediated by Pim kinase. Methods for application of formula I compounds for in vitro, in situ and in vivo diagnosis, prevention or treatment of such diseases in mammalian cells or acssociated pathological conditions are disclosed.EFFECT: increased efficiency of treatment.26 cl, 4 tbl, 528 ex

Derivative cyclic amine and its pharmaceutical application // 2638549
FIELD: pharmacology.SUBSTANCE: invention refers to derivatives if cyclic amine of formula (I), where A is a group, represented by the general formula (IIa), (IIb) or (IIc), where A is a group, provided by the general formula (IIa) or (IIb), R1 represents an alkyl group containing 1 or 2 carbon atoms and optionally substituted by a hydroxyl group, amine group or carboxyl group, R2 represents a hydrogen atom, R3 is a hydrigen atom or alkyl group containing 1 or 2 carbon atoms, R4 is a hydrogen atom or an alkylcarbonyl group, containing 2 carbon atoms, or an alkyl group, containing 1 or 2 carbon atoms and optionally substituted by alkylcarbonylamine group, containing 2 carbon atoms, and n is 1 or 2, in which, when R3 and R4, each independently represent an alkyl group, containing 1 or 2 carbon atoms, R1 represents an alkyl group containing 1 or 2 carbon atoms and substituted by a hydroxyl group, amine group or carboxyl group; and when A is a group, represented by the general formula (IIc), R1 represents an alkyl group, containing 1 carbon atom and substituted by a carboxyl group, R2 represents a hydrogen atom and X represents CH2, O or -NR5 and R5 is an alkyl group, containing 1 carbon atom. Also, the invention relates to a prodrug of the compound of formula (I), pharmaceutical, analgetic agent and therapeutic agent based on compounds of formula (I), or its prodrug.EFFECT: new derivatives of imidazol, useful in the treatment of pain, have been obtained.11 cl, 24 dwg, 5 tbl, 73 ex
ethod for treatment of chronic prostatitis in dogs // 2637632
FIELD: veterinary medicine.SUBSTANCE: method for treatment of chronic prostatitis in dogs includes introduction of antibacterial drug with antibacterial drug injected once a day and represented by 10% solution of ciprofloxacin at a rate of 5 mg/kg, introduced in a therapeutic dose intramuscularly to the rear femoral muscle group, while introducing nicotinic acid 15 minutes before the therapeutic concentrations of the antibacterial drug in the animal blood the rear femoral muscle group in a biological dose of 0.15 mg/kg.EFFECT: achievement of therapeutic concentrations of antibacterial drug in the prostate gland tissues, in parallel with the achievement of such in the serum, shortened system effects of antibacterial drugs on dogs' body in complex treatment and reduced probability of relapse.1 tbl, 4 ex
Ointment for skin infections treatment // 2637092
FIELD: medicine.SUBSTANCE: invention can be used to treat a wide range of skin lesions infected: ulcers, eczema, wound infections, bitten wounds, pressure sores, psoriasis, herpes, leprosy. The following active ingredients per 100 g of the base are included in the composition of the ointment for skin infections treatment: rifampicin and doxycycline hyclate antibiotics in equal proportions 1-3 g each, human recombinant interferon alpha-2b 250000 - 500000 ME, the vaseline base is the rest.EFFECT: effectively overcomes the factors of pathogenic microbes resistance and expands the spectrum of action on all types of skin infectious lesions.2 ex
Substituted pyrrolidines as xia factor inhibitors for thromboembolic diseases treatment // 2636050
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the general formula , their pharmaceutically acceptable salts, pharmaceutical compositions containing the said compounds.EFFECT: compounds of general formula I are XIa factor inhibitors and are suitable for thromboembolic diseases prevention or treatment.22 cl, 1 tbl, 115 ex
Fluoroquinolones based on 4-deoxypyridoxine // 2634122
FIELD: pharmacology.SUBSTANCE: invention relates to new fluoroquinolone derivatives of the general formula (I), where R1 = ; R2 = H; R3 = ; or R1 = C2H5; R2 = H; R3 = ; or R1 = C2H5; R2 = F; R3 = ; or R1 = ; R2 = OCH3; R3 = .EFFECT: new fluoroquinolone derivatives with antibacterial activity.2 tbl, 6 ex

Solid dispersions produced by melt extrusion and containing apoptosis-inducing agent // 2633353
FIELD: pharmacology.SUBSTANCE: dispersion includes a compound of Formula I , where the value of R0, R1, R2, R3, R4, A, B, R5, X, Y and R6 groups is determined in the claims, or a pharmaceutically acceptable salt thereof. The compound of Formula I or its pharmaceutically acceptable salt are dispersed in a solid matrix which contains (a) at least one pharmaceutically acceptable water-soluble polymer carrier, and (b) at least one pharmaceutically acceptable surfactant. At least 5% of the compound of Formula I or its pharmaceutically acceptable salt is presented in the crystalline form, as studied by X-ray diffractometry. The compound or its pharmaceutically acceptable salt is presented in an amount equal to an amount of the parent compound from approximately 5% to approximately 40% by weight; at least one pharmaceutically acceptable water-soluble polymer carrier is presented in an amount from approximately 40% to approximately 85% by weight, and at least one pharmaceutically acceptable surfactant is presented in an amount from approximately 5% to approximately 20% by weight. A compound of Formula I in which R0 is chlorine, R1 and R2 are H, R3 and R4 are methyl, A is N, B is CH, R5 is nitro, X is -NH-, Y is - (CH2)n-, where n=1 , and R6 is selected from the group consisting of tetrahydropyranyl and 4-hydroxy-4-methylcyclohexyl, is excluded from the scope of the compound of Formula I. Methods for preparation of a solid dispersion suitable for oral delivery, a pharmaceutical dosage form and a solid dispersion for use as a medicament are also proposed.EFFECT: solid dispersion is applicable for oral administration to the patient in need of treatment of a disease characterised by overexpression of one or more Bcl-2 family antiapoptotic proteins.51 cl, 1 dwg, 17 tbl, 19 ex
Heterocyclic amines and their application // 2632900
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (III) or a pharmaceutically acceptable salt thereof, wherein W is S; Y is N; X is N; R1 is selected from (a) C1-C6 alkyl optionally substituted with amino, methylamino, dimethylamino, C1-C6 alkoxy or isoindolyl; (B) -NR8R7, -CH2NR7R8, where R7 and R8 are joined to form optionally substituted C3-C7 non-aromatic ring which is pyrrolidine, morpholine, piperazine, piperidine, 1,4-diazepane, azepane, azetidine, 2-azabicyclo[2.2.1]heptane or 2,5-diazabicyclo[2.2.1]heptane and optionally substituted by one or more C1-C6alkyl, C1-C6alkoxy, methoxyethyl, 1-methoxypropane, isopropyloxymethyl, isopropyloxyethyl, -C(O(CH2)-methyl, -C(O)(CH2)-O-isopropyl, C1-C6haloalkyl, -S(O)2-methyl, -S(O)2-isopropyl, oxo, -C(O)(C1-C2)alkyl-N(methyl)2, -C(O)(C2)alkyl-(pyrrolidine), t-butyl-C(O)- or phenyl; or (c) -O-(tetrahydro-2H-pyran); each of R2, R3 and R5 are hydrogen; R4 is selected from C3-C6cycloalkyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl and optionally substituted heteroaryl selected from pyridine, pyrazole, pyridazine, pyrimidine. The said heteroaryl is optionally substituted with 1 to 2 substituents selected from C1-C6 alkyl and CN. The invention also relates to specific compounds as defined in the claims. The compounds of the invention are intended for the manufacture of a pharmaceutical composition having an inhibitory activity against an interleukin 1 receptor associated kinase 1 (IRAK-1) and an interleukin 1 receptor associated kinase 4 (IRAK-4). The compounds of the invention are also useful in a method for treatment of a disorder sensitive to inhibition of IRAK-1-mediated signalling.EFFECT: heterocyclic amines having inhibitory activity against an interleukin 1 receptor associated kinase 1 and interleukin 1 receptor associated kinase 4.24 cl, 4 tbl, 431 ex

Compositions and methods for therapeutic means delivery // 2632445
FIELD: pharmacology.SUBSTANCE: invention group is a nanoparticle for retroviral infection suppression, comprising at least one therapeutic agent and at least one surfactant, wherein the said nanoparticle is crystalline, wherein the said surfactant covers a crystal of the said therapeutic agent, wherein the said therapeutic agent is selected from the group consisting of atazanavir (ATV), efavirenz (EFV), indinavir (IDV) and ritonavir (RTV), wherein the said surfactant is an amphiphilic block copolymer, wherein the said nanoparticle is obtained by wet grinding or high pressure homogenization, and wherein the said nanoparticle contains at least 95% of a therapeutic agent; composition for retroviral infection suppression; method for HIV infection treatment or suppression.EFFECT: invention provides steady drug delivery to the serum and tissue and improved antiviral efficacy relative to the equivalent dose of the free drug.18 cl, 5 ex, 4 tbl, 25 dwg
Oral pharmaceutical composition for prevention or treatment of "dry eye" syndrome containing rebamipid or its precursor // 2632107
FIELD: pharmacology.SUBSTANCE: oral pharmaceutical composition for "dry eye" syndrome prevention or treatment, comprising a renamipide precursor or a pharmaceutically acceptable salt thereof in an amount of 0.5 to 1 wt % as an active ingredient. The composition is in the form of a suspension. Also an oral pharmaceutical preparation, a method for "dry eye" syndrome prevention or treatment and application of a renimidine precursor for pharmaceutical drug preparation are described. These rebamipide precursors can treat the "dry eye" syndrome with oral route of administration.EFFECT: safety and ease of use compared with conventional eye drops.10 cl, 15 dwg, 1 tbl, 28 ex

Pyperazinyl derivatives for cancer treatment // 2629115
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the general formula (I), where X represents a (C1-C6)alkyl, phenyl, benzyl, C(O)OR5 or C(O)NHR5 group; R1 represents a hydrogen atom or a C(O)R6 or C(O)OR6 group; R2 represents a hydrogen atom or a (C1-C6)alkyl group; or R2 together with R1 or X form a saturated hydrocarbon chain that forms a 5- or 6-member ring; R3 represents a hydrogen atom or a (C1-C6)alkyl group; R4 represents a halogen atom or a (C1-C6)alkyl, (C1-C6)alkoxy or phenyloxy group, the said group being optionally substituted by one or more halogen atoms; Ar represents a thiophenyl or phenyl group optionally substituted by one halogen atom; and R5 and R6 independently of each other represent a (C1-C6)alkyl, phenyl-(C1-C6)alkyl group or phenyl optionally substituted by one halogen atom. The invention also relates to a pharmaceutical composition and to a process for preparation of general formula (I) compounds.EFFECT: new piperazinyl compounds of the general formula are obtained that can be used for breast cancer, leukemia, colon cancer, pancreatic cancer and ovarian cancer treatment or prevention.12 cl, 1 dwg, 6 tbl, 8 ex

Aminomethyl quinolones useful ifor treatment of jnk-mediated disorder // 2629111
FIELD: chemistry.SUBSTANCE: invention relates to new aminomethyl quinolone derivative of formula (I) or its pharmaceutically acceptable salt, where R is -C(=O)A, -C(=O)OA, -C(=O)NHA, -C(=N-C≡N)A, -C(=N-C≡N)NHA or A; A is C1-6-alkyl, phenyl, lower cycloalkyl, adamantyl, heterocycloalkyl selected from benzodioxin, pyrrolidine, piperidine, morpholine or piperazine, heteroaryl selected from pyridine, pyrazole, thiazole, triazole or pyrimidine or bicyclic heteroaryl selected from quinoline, quinazoline, indole, benzothiazole, benzoimidazole or imidazopyridine optionally substituted with one or two A1; each A1 independently represents A2 or A3; each A2 is independently halo or oxo; each A3 is independently C1-6-alkyl, C1-6-alkoxy, phenyl, benzyl, heterocycloalkyl selected from morpholine, piperidine, diazepane, pyrrolidine, azepane or piperazine, bicyclic heterocycloalkyl selected from benzodioxole or diazobicycloheptane, heteroaryl selected from oxazole, triazole, pyrazole, imidazole, thiadiazole, oxadiazole, thiazole or tetrazole, amino, C1-6-alkylamino, C1-6-dialkylamino, amido, C1-6-alkyl ester group, sulfonyl, sulfonamido, -C(=O) or -C(═O)O, optionally substituted by one, two or three groups, selected from halo, hydroxy, C1-6-alkylamino, C1-6-alkyloxy, C1-6-alkyl, C1-6-alkoxy, phenyl, hydroxycycloalkyl wherein cycloalkyl is adamantyl, amino, C1-6-alkylamino, C1-6-dialkylamino, t-butyl complex of carbamic acid ester, (C1-6-alkyl) sulfonyl-piperidinyl or hydroxy- (C1-6-alkyl); R' is H or methyl; X is CX'; X' is H or halo; X1 is H, 2-oxazolyl, dimethylamido or C1-6-alkyl ester group; Y is CH or N; and Y1 is H, halo, C1-6- alkoxy or halo (C1-6alkyl). The invention also relates to particular aminomethyl quinolone derivatives and to the use of said aminomethyl quinolone derivatives.EFFECT: obtained new aminomethyl quinolone derivatives, useful in the treatment of JNK-mediated disorder.15 cl, 2 tbl, 211 ex
Apoptosis-inducing means for treatment of malignant tumour and immune and autoimmune diseases // 2628885
FIELD: pharmacology.SUBSTANCE: invention relates to application of a combination of a formula (III) compound with one or more additional drugs for the manufacture of a drug for use in therapy that inhibits the activity of anti-apoptotic Bcl-2 proteins. The radical values are set forth in claim p.1.EFFECT: increased efficiency of compounds.16 cl, 6 tbl, 19 ex

Amide compounds, methods for production, application as means for treatment and prevention of diseases caused by rna-containing viruses // 2628800
FIELD: pharmacology.SUBSTANCE: compounds of the invention are intended for manufacture of a pharmaceutical composition, kit or drug. The invention also relates to a process for preparation of compounds of the invention (versions). Compounds of the invention are intended for use in the prevention or treatment of diseases caused by RNA-containing viruses belonging to enteroviruses, metapneumoviruses or pneumoviruses.EFFECT: amide compounds for treatment or prevention of diseases caused by RNA-containing viruses.26 cl, 8 tbl, 5 ex

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
 
2551283.
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