Containing three or more hetero rings (C07D401/14)

C   Chemistry; metallurgy(315514)
C07   Organic chemistry(61593)
C07D401/14                     Containing three or more hetero rings(572)
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 indolin-2-she as inhibitors of proteinkinas // 2627706
FIELD: pharmacology.SUBSTANCE: invention relates to indoline-2-one derivatives, the formula A, which are protein kinase inhibitors for the treatment of hyperproliferative diseases such as lung cancer, colorectal cancer, liver cancer and acute myelomonocytic leukemia.EFFECT: increased efficiency of treatment.15 cl, 3 dwg, 6 tbl, 1 ex
Compounds of pyridazinamide and their use as synthetic syneckinasis inhibitors (syk) // 2627661
FIELD: chemistry.SUBSTANCE: invention relates to novel pyridazinamides of the formula I , where all variable substituents are defined in the claims, and their pharmaceutically acceptable salts, as well as a pharmaceutical composition based on them.EFFECT: compounds of the formula are SYK inhibitors and are useful for the treatment of autoimmune and inflammatory diseases.10 cl, 1 tbl, 43 ex

1-phenyl-2-pyridinylalkyl alcohols derivatives as phosphodiesterase inhibitors // 2626956
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of general formula , where: R1 is selected from the group consisting of: methyl; trifluoromethyl; R2 is selected from the group consisting of: methyl optionally substituted with cyclopropyl; cyclopentyl; or R1 and R2, together with their interconnecting atoms, form a 2,2-difluoro-1,3-dioxolane ring of formula (q) condensed with a phenyl group that carries -OR1 and -OR2 groups, where the asterisks indicate carbon atoms shared by such phenyl ring: , R19 is hydrogen; R3 is one or more substituents independently selected from halogen atoms; Z represents a -(CH2)n- group, where n is 0 or 1; A is a saturated and monocyclic (C3-C7) heterocycloalkylene group selected from the following list of di-radicals: , , , , , , , , , , where symbols [3] and [4] indicate the points of group A attachment to groups Z and K, respectively; K is selected from the group consisting of: -(CH2)mC(O)R4, where m can be 0 or 1; -C(O)(CH2)jR4, where j can be 1 or 2; -SO2(CH2)pR4, where p can be 0, 1 or 2; -(CH2)ySO2R4, where y can be 1 or 2; -(CH2)zR4, where z can be 1; and -C(O)(CH2)2SO2R4; R4 is a ring system which is a mono- or bicyclic ring which may be saturated, partially unsaturated or fully unsaturated, selected from phenyl, (C3-C8) cycloalkyl, (C3-C7) heterocycloalkyl where at least one ring carbon atom is replaced by a heteroatom selected from N, NH and O or heteroaryl, such ring is optionally substituted with one or more R5, which may be the same or different and which are independently selected from the group consisting of: (C1-C6) alkyl, optionally substituted with one or more groups independently selected from the list consisting of: -OH; (C3-C7) heterocycloalkyl(C1-C4)alkyl where at least one ring carbon atom is replaced by a heteroatom selected from N, NH, O; 5-6 member heteroaryl where at least one ring carbon atom is replaced by a heteroatom selected from N and O; -OR6 group, where R6 is selected from the group consisting of (C1-C6) haloalkyl; -SO2R7 group, where R7 is (C1-C4) alkyl; and methyl optionally substituted with one or more (C3-C7) cycloalkyls; halogen atoms; CN; NR8R9, where R8 and R9 are different or identical and independently selected from the group consisting of: H; (C1-C4) alkylen-NR13 R14, where R13 and R14 are different or identical and independently selected from the group consisting of: a (C1-C6) alkyl, or they form a saturated (C3-C7) heterocyclic ring together with the nitrogen atom to which they are attached; -SO2R15 group, where R15 is selected from the group consisting of: (C1-C4) alkyl; -C(O)OR17 group, where R17 is selected from the group consisting of: (C1-C6) alkyl; or they form, together with the nitrogen atom to which they are attached, a saturated or partially saturated heterocyclic ring which is optionally substituted by one or more (C1-C6) alkyl; (C1-C2) alkylene-NR8R9, as mentioned above; COR10, where R10 is (C1-C6) alkyl; oxo; -SO2R11, where R11 is (C1-C4) alkyl or NR8R9, where R8 and R9 are as above; -COOR12, where R12 is H, (C1-C4) alkyl or (C1-C4) alkylene-NR8R9, where R8 and R9 are as above; and -CONR8R9, where R8 and R9 are as above; where R6, R8, R9, R10, R11, R12, R13, R14, R15, R17 and R19 groups in each case may have the same or different value if more than one group is present; and their N-oxide derivatives on the pyridine ring or their pharmaceutically acceptable salts. The compound is a phosphodiesterase 4 (PDE4) enzyme inhibitors.EFFECT: improved properties.19 cl, 26 tbl, 36 ex
Derivatives of (3-methylpyrrolidin-3-yl)-methyl pyridinyl ether and their use as antagonists of receptor nk-3 // 2625798
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the general formula Wherein A is taken from groups (a), (b) or (c): (a) or (b) or is cycloalkyl possibly substituted with a lower alkyl (c); Ar1 is phenyl or a six-membered heteroaryl containing one or two nitrogen atoms; X1 is N or CH; X2 is N-R1 or O; R1 is S(O)2-lower alkyl, C(O)-cycloalkyl, substituted with a lower alkyl, or is C(O)-lower alkyl, lower alkyl, cyano group, cycloalkyl or a six-membered heteroaryl containing one or two nitrogen atoms substituted with a lower alkyl, cyano group, C(O)-lower alkyl, halogen, lower alkyl substituted with halogen or lower alkoxy group, or is a phenyl substituted with a cyano group or halogen. R2 is a lower alkyl, halogen, pyrazolyl, 3-methyl-[1,2,4]oxazolyl, 5-methyl-[1,2,4]oxadiazol-3-yl, pyridyl substituted with a cyano group or is a phenyl substituted with a halogen or is a cyano group, lower alkoxy group or is piperidine-2-on. The invention may also relate to pharmaceutically active salts of the coumpound of the formula I.EFFECT: compounds are prospective antagonists of the NK-3 receptor for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety syndrome and attention deficit/hyperactivity disorder.12 cl, 1 tbl, 27 ex

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
8-carbamoyl-2-(2,3-di-substituted pyrid-6-yl)-1,2,3,4-tetrahydroisoquinoline derivatives as apoptosis-inducing agents for cancer treatment // 2625315
FIELD: pharmacology.SUBSTANCE: invention relates to organic chemistry, namely a heterocyclic compound of formula (I) or to a therapeutically acceptable salt thereof, where X is benzo[d]thiazolyl, thiazolo[5,4-b]pyridinyl, thiazolo[4,5-c]pyridinyl, imidazo[1,2-a]pyridinyl, thiazolo[5,4-c]pyridinyl, thiazolo[4,5-b]pyridinyl, imidazo[1,2-a]pyrazinyl or imidazo[ 1,2-b]pyridazinyl; Y1 means pyrrolyl, pyrazolyl, triazolyl or pyridinyl; where Y1 is optionally substituted with 1 or 2 substituents independently selected from R5, CN and Cl; L1 is selected from (CR6R7)q, (CR6R7)s-O-(CR6R7)r, (CR6R7)s-S-(CR6R7)r, (CR6R7)s-S(O)2-(CR6R7)r and (CR6R7)s-NR6A-(CR6R7)r; Y2 means mono- or tricyclic C8-C10-cycloalkyl, spiro[2.5]octyl, spiro[3.5]nonyl, oxatricyclo[3.3.1.13,7]decyl or azabicyclo[3.2.1]octyl; where Y2 is optionally substituted with 1, 2 or 3 substituents independently selected from R8, OR8, SO2R8, CO(O)R8, OH and Br; Z1 is selected from , R1 and R3 are absent; R2 is deuterium or C1-C6-alkyl; R5 is C1-C6-alkyl; R6A is selected from hydrogen and C1-C6-alkyl; each R6 and R7 are hydrogen; R8 is selected from the group consisting of C1-C3-alkyl, morpholinyl and dioxydothiomorpholinyl; where R8, meaning C1-C6-alkyl, is optionally substituted with a substituent selected from R16, OR16, SO2R16 and NHR16; Rk is selected from C1-C6-alkyl, morpholinyl, cyclopropyl and C1-haloalkyl; R16 Is selected from C1-C4-alkyl, phenyl, morpholinyl and tetrahydropyranyl; where R16, meaning C1-C4-alkyl, is optionally substituted with 1 substituent selected from OCH3, OCH2CH2OCH3 and OCH2CH2NHCH3; q is 1 or 2; s, m and p is 0; r is 0 or 1; N is 0, 1, or 2. The invention also relates to specific compounds, pharmaceutical compositions based on these compounds and a method for treatment of these diseases.EFFECT: new heterocyclic compounds are obtained, that are useful for treatment of some cancers.16 cl, 3 tbl, 86 ex
Quinolines as fgfr kinase modulators // 2625303
FIELD: pharmacology.SUBSTANCE: invention related to a new quinoline derivative of formula (I), where W us -N(R3)- or -C(R3aR3b)-; each R2 is independently selected from halogen, C1-4alkoxy, Y is -E-D; D is phenyl or 5-6-membered monocyclic heterocyclyl, containing one or two heteroatoms selected from N or O, wherein the mentioned heterocyclyl can be optionally substituted with one group of R1; E is a link; R1 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyl which is substituted with -S(=O)2-C1-6alkyl, R6; R3a is hydroxyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, C1-6alkyl which is substituted with -NR10R11, C1-6alkyl which is substituted with -C(=O)-NR10R11; R3b is hydrogen; or R3a and R3b are combined to obtain =O or to obtain =CH-C0-4alkyl which is substituted with R3c; R3c is cyano; R3 is C2-6alkynyl, hydroxyC1-6alkyl, hydroxyhaloC1-6alkyl, C1-6alkyl which is substituted with R9, C2-6alkynyl which is substituted with R9, C1-6alkyl which is substituted with -NR10R11; R6 is 6-membered monocyclic heterocyclyl, containing one O atom; R9 is 5- or 6-membered monocyclic heterocyclyl, containing one or two heteroatoms, seleceted from N or O, each is optionally and each is independently substituted with substitute selected from =O, C1-4alkyl, C1-4alkoxy, S(=O)2-NR14R15, C1-4alkyl which is substituted with -NH-S(=O)2-haloC1-4alkyl, 6-membered aromatic monocyclic heterocyclyl, containing two N atoms, wherein the mentioned heterocyclyl is optionally substituted with R16; each R10 and R11 independently represent hydrogen, C1-6alkyl, haloC1-6alkyl; each R14 and R15 independently represent C1-4alkyl; R16 is C1-4alkoxy; n independently represent a whole number equal to 2, 3 or 4; as well as to its pharmaceutically acceptable salt and to any tautomeric or stereochemically isomeric form thereof. The invention also relates to pharmaceutical compositions based on compound of formula (I), application of the compound of formula (I), method for the prevention or treatment of a disease and product based on the compound of formula (I).EFFECT: new quinoline derivatives are obtained, useful in the treatment of diseases mediated by FGFR kinase.30 cl, 2 tbl, 35 ex
Heterocyclic compounds and their application as glycogen synthase kinase-3 inhibitors // 2623427
FIELD: chemistry.SUBSTANCE: invention relates to a heterocyclic compound of formula , where A represents NRB, where RB represents hydrogen; X1 and X2 represent CR2 and X3, X4, X5 and X6 represent CR3 or CR4, or X1 and X2 represent CR2, X3 represent N, and X4, X5 and X6 represent CR3; Y1, Y2, Y3 and Y4 represent CR4 or CR5 or Y2 represents N, and Y1, Y3 and Y4 represent CR5; provided that no more than one of Y1, Y2, Y3 and Y4 represents CR4; and provided that one of Y1, Y2, Y3 and Y4 represents CR4 or C-CF3, if none of X3, X4, X5 and X6 represents CR4; R1 represents hydrogen; each R2 represents hydrogen; each R3 is independently selected from the group consisting of hydrogen, CN, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy and C1-C6-haloalkoxy; R4 represents a C-linked saturated or partially unsaturated monocyclic 5- or 6-member heterocyclic ring containing one heteroatom selected from O and N, as ring members, wherein the heterocyclic ring optionally has one N-linked substituent R8; R5 is selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-haloalkyl and C3-C7-cycloalkyl; and R8 is selected independently on the case from the group consisting of C1-C6-alkyl, C1-C6-haloalkyl and C1-C6-alkoxycarbonyl. The invention also relates to pharmaceutical compositions based on a formula (I) compound, formula (I) compound application, a method of treatment of diseases susceptible to treatment by a compound that modulates the activity of 3β glycogen synthase kinase.EFFECT: new heterocyclic compounds useful for treatment of neurodegenerative disorders or inflammatory diseases are obtained.25 cl, 2 tbl, 70 ex

Compound 8-fluorophthalazine-1(2h)-one as inhibitors of bruton tyrosine kinase // 2622391
FIELD: pharmacology.SUBSTANCE: compounds of 8-fluorophthalazine-1(2H)-ones of formula II are proposed, wherein one of X1, X2 and X3 represent N, and the other symbols have meanings defined in claim 1 of the invention formula, or stereoisomers, gautomers and pharmaceutically acceptable salts thereof. The compounds proposed inhibit the kinase Btk (Bruton tyrosine kinase) and can be used to treat immune disorders, such as inflammation, mediated by kinase Btk.EFFECT: increased efficiency while using the compounds of formula II for the diagnosis and treatment in vitro, in situ and in vivo such disorders in mammalian cells, or associated pathological conditions.25 cl, 8 dwg, 2 tbl, 69 ex
Heterobicyclic derivatives as hcv inhibitors // 2621734
FIELD: chemistry.SUBSTANCE: invention relates to heterocyclic compound of formula (I) or to pharmaceutically acceptable salt thereof, wherein Y is CH, N or CR4; W is carbonyl, sulfonyl or CR5R6; is or is independently selected from the group containing R and R' independently selected from -CR1R2R3, where R1 is selected from C1-4alkyl; R2 is C1-4alkyloxycarbonylamino; R3 is hydrogen; R4 is hydrogen or fluorine; CR5R6 together form oxetane. The invention also relates to pharmaceutical composition based on compound of formula (I), its use and product on its base.EFFECT: obtaining novel heterocyclic compounds, useful in the treatment of HCV infections.14 cl, 2 tbl

N-piperidin-3-yl-benzamide derivatives for cardiovascular diseases treatment // 2618628
FIELD: pharmacology.SUBSTANCE: invention relates to substituted amide compounds of formula pharmaceutical compositions containing such compounds and application of such compounds for lowering plasma lipid levels, such as low density lipoprotein cholesterol (LDL-cholesterol) and triglycerides, and thus, for treatment of diseases exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in mammals, including humans.EFFECT: increased efficiency of compounds application.42 cl, 10 dwg, 55 ex
Bruton's tyrosine kinase inhibitors // 2618529
FIELD: pharmacy.SUBSTANCE: invention relates to a compound of general formula I, below, or a pharmaceutically acceptable salt thereof. In the formula I compound, X is halogen; Y is H or lower alkyl; R is -R1-R2-R3; R1; R1 is pyridyl; R2 is -C (= O) or is absent; R3 is morpholinyl or pyrrolidinyl, optionally substituted by a lower alkyl. The above compounds are used to modulate OMB activity and treat diseases associated with excessive OMB activity. Furthermore, these compounds are used for treatment of inflammatory and autoimmune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. The invention also relates to the pharmaceutical composition comprising a compound of formula I and at least one carrier, diluent or excipient.EFFECT: increased efficiency of compounds application.20 cl, 2 tbl, 7 ex
Acrylic and methacrylic acid amides with oligopiperidines and method for their preparation // 2617694
FIELD: chemistry.SUBSTANCE: invention relates to new compounds of formula where R1 represents H or CH3; R2, R3, R4 represent 4-R3piperazine- or R4R5N; R3, R4, R5 - same or different C1-C4 alkyl groups with straight or branched chain; n=2, 3, …, 20, and to a method for their preparation. Compounds of formula I contain easily polymerizable (meth)acryloyl group and a number of ionic groups and therefore can be used as monomers for the preparation of polyelectrolytes.EFFECT: increased exchange capacity.9 cl, 1 tbl, 15 ex
Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as inhibitors // 2617401
FIELD: chemistry.SUBSTANCE: invention relates to compounds of general formula (I) (I), where: R1 and R2, which can be identical or different, independently selected from a group consisting of: - (C1-C6)alkyl, optionally substituted (C3-C7)cycloalkyl; - (C1-C6)halogenalkyl; - (C3-C7)cycloalkyl and - (C3-C7)heterocycloalkyl, containing heteroatom O; R3 represents hydrogen, (C1-C6)alkyl or (C1-C3)alkylthio(C1-C6)alkyl; A is a partially unsaturated or unsaturated bicyclic ring system consisting of two condensed monocyclic ring systems B and C, presented in cl. 1 of formula, where ring C is a monocyclic aryl or monocyclic heteroaryl ring system, ring B is a 5- or 6-member heterocycloalkyl group, zero of Y groups is bonded to ring C, n of groups Y is bonded to ring B, and n is an integer from 1 to 3; and where ring B and C optionally contains additional heteroatoms in amount of 1 to 4, selected from N, O or S; p is an integer from 0 to 3; Y denotes oxo group; K is selected from a group consisting of: - (C1-C6)alkyl, optionally substituted with one (C3-C7)cycloalkyl group; - (C3-C6)heterocycloalkyl(C1-C4)alkyl containing 1 or 2 heteroatoms selected from N or O; - (C3-C6)heterocycloalkyl containing 1 or 2 heteroatoms selected from N or O, optionally substituted with one or more (C1-C6)alkyl group; - (C1-C4)halogenalkyl; - OR4, where R4 selected from a group consisting of: - H; - (C1-C6)alkyl, optionally substituted (C3-C7)cycloalkyl or heteroaryl; - halogen atoms; - CN; - NO2; - NR5R6, where R5 and R6, which can be identical or different, independently selected from a group consisting of: - H; - OH; - (C1-C4)alkyl-NR7R8, where R7 and R8, which can be identical or different, independently selected from a group consisting of: H; (C1-C6)alkyl, possibly substituted (C1-C6)alkoxyl; and (C1-C6)alkyl-NR9R10, where R9 and R10, which can be identical or different, represent H or (C1-C6)alkyl; or they form together with a nitrogen atom to which they are bonded, (C3-C6)heterocycloalkyl ring containing 1 or 2 heteroatoms, selected from N, O or S, optionally substituted (C1-C6)alkyl or (C1-C6)alkylcarbonyl group; -(C1-C6)alkyl, optionally substituted with (C1-C6)alkoxyl or heteroaryl, (C3-C6)heterocycloalkylcarbonyl containing 1 or 2 heteroatoms selected from N or O, heteroarylcarbonyl, wherein all of them may further be substituted with one or more (C1-C6)alkyl, (C1-C6)halogenalkyl or (C1-C6)alkoxyl groups, which are identical or different and are selected independently; - SO2R11, where R11 represents (C1-C6)alkyl; - C(O)R12, where R12 is (C1-C6)alkyl, optionally substituted with (C1-C6)alkoxyl; - (C1-C4)alkyl-NR13R14, where R13 and R14, which can be identical or different, are independently selected from a group consisting of groups: - SO2(C1-C6)alkyl, H, (C1-C6)alkyl and (C3-C7)heterocycloalkyl(C1-C4)alkyl containing 1 or 2 heteroatoms selected from N or O; and - SO2NR15R16, where R15 and R16, which can be identical or different, independently represent H or (C1-C6)alkyl; where groups with R4 at R16 have similar or different values in each case, if they are present in more than one group; and where heteroaryl is a mono- or bicyclic ring system with 5–10 ring atoms, containing 1 or 2 heteroatoms selected from N, O or S; or its pyridine-N-oxides, pharmaceutically acceptable salts or solvates. As well as to methods of producing such compounds, compositions containing them and their therapeutic application as inhibitors of phosphodiesterase 4 (PDE4) enzyme.EFFECT: disclosed are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as inhibitors.16 cl, 16 tbl, 52 ex

Heterocyclic compounds useful as pdk1 inhibitors // 2615130
FIELD: chemistry.SUBSTANCE: present invention relates to novel compounds of general formulae II, III, IV and V, where values of radicals are given in description, or pharmaceutically acceptable salts thereof, which can be used as PDK1 inhibitors.EFFECT: present invention also relates to pharmaceutical compositions based thereon and to methods of treating cancer, mediated by protein kinase PDK1.32 cl, 2 tbl, 445 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
Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2 negative allosteric modulators, compositions and use thereof // 2610262
FIELD: pharmaceutics.SUBSTANCE: invention relates to organic chemistry, namely, to quinoline carboxamide derivatives of following structures. Invention also relates to pharmaceutical composition based on one of said compounds, use of said compounds for treating diseases or disorders mediated by mGluR2, such as Alzheimer's disease, cognitive disorder, schizophrenia, mood disorders, painful disorders, and sleep disorders.EFFECT: novel quinoline carboxamide derivatives with useful biological properties.25 cl, 8 tbl, 310 ex
(alpha-substituted aralkylamino- and heteroarylalkylamino)pyrimidinyl- and 1,3,5-triazinylbenzimidazoles, pharmaceutical compositions thereof and use thereof in treating proliferative diseases // 2608742
FIELD: chemistry.SUBSTANCE: present invention relates to novel compounds of formula I, , having PI3K enzymatic activity.EFFECT: novel compounds of formula I are obtained, which can be used for regulation of PI3K enzymatic activity, as well as pharmaceutical compositions based thereon.33 cl, 2 tbl, 63 ex, 3 sch
Novel pyrrole compounds, synthesis method thereof and pharmaceutical compositions containing same // 2607788
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I) possessing inhibitory activity on Bcl-2 family proteins. In formula (I) (I) A1 is hydrogen, (C1-C6)polyhaloalkyl group or (C1-C6)alkyl group, A2 is hydrogen, (C1-C6)polyhaloalkyl group, (C1-C6)alkyl group or cycloalkyl group, T denotes a hydrogen atom, (C1-C6)alkyl group, optionally substituted with one-three halogen atoms, group (C1-C4)alkyl-NR1R2 or group (C1-C4)alkyl-OR6, R1 and R2 each independently from each other is a hydrogen atom or (C1-C6)alkyl group, or R1 and R2 form with a nitrogen atom bearing them, heterocycloalkyl, R3 is (C1-C6)alkyl group, cycloalkyl group, heterocycloalkyl group, aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R4 is an aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R5 is hydrogen or halogen atom, R6 is a hydrogen atom or a linear or branched (C1-C6)alkyl group, Ra, Rb, Rc and Rd each independently from other represents hydrogen, linear or branched (C1-C6)alkyl, halogen atom, a linear or branched (C1-C6)alkoxy group, hydroxy group, R7-CO-NH-(C0-C6)alkyl-, R7-SO2-NH-(C0-C6)alkyl-, R7-NH-CO-NH-(C0-C6)alkyl-, R7-O-CO-NH-(C0-C6)alkyl-, or substitutes of pair (Rb, Rc) form together with carbon atoms carrying them, a ring consisting of 5–6 ring members, which may contain 1–2 oxygen atoms, R7 is hydrogen, linear or branched (C1-C6)alkyl, aryl or heteroaryl. Invention also relates to methods of producing compounds of formula (I), to a pharmaceutical composition, use of a pharmaceutical composition for preparing a drug, use of compound of formula (I) for preparing a drug.EFFECT: obtaining novel compounds of formula (I) possessing inhibitory activity on Bcl-2 family proteins.37 cl, 2 tbl, 473 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

Quinoline and quinoxaline derivatives effective as cysteinyl-leukotriene antagonists // 2605929
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to a heterocyclic compound of formula (IA) or to a pharmaceutically acceptable salt thereof, where in each case R1 and R3 are independently selected from a group comprising hydrogen, halogen, -OH, -C1-2alkyl, -O-C1-2alkyl, -O-C1halogenalkoxy, -N(C1alkyl)2; R2 represents hydrogen; W represents a group selected from -CH= or -N=; X represents a group selected from -CH=CH- or -N=CH-, where nitrogen from -N=CH- is directly bonded with ring 'a'; Y represents a group selected from -CH=CH- or -C≡C-; Z denotes a bond or group selected from -(CH2)n- and -CH=CH-; A is a group selected from -OR, -O(CH2)nphenyl, -O(CH2)nthiophene; P is selected from a group comprising -O-; Q is a group selected from -COOH; where R is selected from a group comprising hydrogen, -C1-6alkyl, -C3-6cycloalkyl, -C1alkyl (C3-6cycloalkyl), -C3-6alkenyl and -C3-6alkynyl; 'n' in each case represents an integer, selected from 1, 2 or 3; 'm' in each case represents an integer, selected from 0-3, inclusive. Invention also relates to a compound of formula (Id), where radicals are described in patent claim.EFFECT: obtaining novel heterocyclic compounds effective as antagonists of cysteinyl-leukotriene.9 cl, 1 dwg, 2 tbl, 67 ex

Salts of 4-methyl-n-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-ylpyrimidine-2-ylamino)benzamide // 2605551
FIELD: chemistry.SUBSTANCE: invention relates to novel salts of 4-methyl-N-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-yl-pyrimidine-2-ylamino)benzamide (nilotinib), which have protein kinase inhibitor properties and can be used for treating diseases responding to protein kinase activity inhibition. Salts are selected from hydrochloride, diphosphate, sulphate, methanesulphonate, ethanesulphonate, benzolesulphonate and n-toluene sulphonate. Method involves the stage for reacting 4-methyl-N-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-yl-pyrimidine-2-ylamino)benzamide in the form of a free base with the corresponding acid of formula HB selected from the said acids in a solvent medium. Invention also relates to a pharmaceutical composition containing: (a) a therapeutically effective amount of the salt and (b) at least one pharmaceutically acceptable carrier, a diluent, an adjuvant or an excipient.EFFECT: method of treating involves introducing a patient requiring such treatment a therapeutically effective amount of the said salt, or monohydrate of monohydrochloride, or a monophosphate salt of 4-methyl-N-[3-(4-methylimidazole-1-yl)-5-trifluoromethylphenyl]-3-(4-pyridine-3-yl-pyrimidine-2-ylamino)benzamide.13 cl, 8 dwg, 17 tbl, 11 ex

Piperidine derivatives as gpr119 agonists // 2603346
FIELD: chemistry.SUBSTANCE: invention relates to a piperidine derivative of formula 1, stereoisomers or pharmaceutically acceptable salts thereof. Compounds of formula 1 have GPR119 agonist properties. In formula 1 [formula 1] W is O or N-Rh group; Ra, Rb and Rh each independently is H or C1-3 alkyl group; Rc is -F or -C1-3 hyperfluoride alkyl group; Rd and Re are each independently selected from a group consisting of H, halogen, -C1-5 alkyl group; or Rd and Re are combined to form a -C3-7 cycloalkyl group; selected from a group consisting of: , where Rf1 and Rf2 are each independently H, halogen or -CN group; selected from a group consisting of: , where Rk1 and Rk2 are each independently H, -CN Group, halogen or -C1-5 alkyl(OH) group; is ; Q is H, -S(O)R1 group, -S(O)2R1 group, -C(O)R1 group, -C(O)OR1 group, -C(O)NHR1 group, -C(O)NR2R3 group, -S(O)2NHR1 group, -S(O)2NR2R3 group or . Invention also relates to a pharmaceutical composition.EFFECT: novel piperidine derivatives of formula 1, which control GPR119 activity, are obtained.8 cl, 183 tbl, 131 ex

New compounds for treating diseases, associated with amyloid or amyloid-like proteins // 2603008
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula (I) possessing properties of aggregation of Aβ1-42, pharmaceutical composition, based thereon, use thereof, method of treating using them, kit for detecting or diagnosing diseases, method of reducing deposits of β-amyloid plaques and method of maintaining or improving cognitive abilities. In general formula (I) A there are selected from group, consisting of (i), (ii), (iii), (iv), (v), (vi) and (viii), L1 is selected from group, consisting of (a), B is selected from group, consisting of (ix), (x), (xi), (xii), (xiii), where R1, R2 and R3 are selected from group of hydrogen, halogen, CN, -CONR30R31, -N(R30)-C(O)-R31, alkyl, -O-alkyl, -C(O)O-alkyl, 6-membered heterocycle with 1-2 heteroatoms, selected from N and O, fluoroalkyl, where the heterocycloalkyl can be optionally substituted with acetyl or methyl group, or, if any of these groups R1/R2/R3 are adjacent, they can be taken together and form 5-8-member ring, containing carbon atoms and optionally one or two heteroatoms, selected from O, S or N, and where 5-8-member ring can be substituted with NR20R21 or -O-alkyl, where alkyl can be substituted with F, methoxy or SO2Me; Ra is selected from hydrogen, alkyl; Rb is selected from hydrogen, halogen, CONR30R31; R30, R31, R20 and R21 are selected from hydrogen, alkyl; X and Y are selected from CRb and N; p equals to 0, 1 or 2.EFFECT: compounds can be used for treating of group of violations and disorders, associated with amyloid protein, such as Alzheimer's disease, and diseases or conditions, associated with amyloid-like proteins, as well as for treating eye diseases, associated with pathological abnormalities/changes in visual system tissues.36 cl, 12 dwg, 10 tbl, 219 ex A-L1-B (I), , , , , , and ,, , , and ,

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

Cyanoquinoline derivatives // 2600928
FIELD: chemistry.SUBSTANCE: invention relates to novel cyanoquinoline derivatives of general formula I, as well as to stereoisomers, cis-trans-isomers or pharmaceutically acceptable salts thereof, where R1 is selected from a group consisting of 4-bromobut-2-enamide, 4-(dimethylamino)but-2-enamide, acrylamido, but-2-enamide, 3-methylbut-2-enamide, 2-(1-tert-butoxycarbonylpiperidin-4-ylidene) acetamide, 2-(piperidin-4-ylidene)acetamide, 2-(1-methylpiperidin-4-ylidene) acetamide, 2-(1-ethylpiperidin-4-ylidene) acetamide, 2-(1-benzylpiperidin-4-ylidene) acetamide, 2-(1-(2-methoxyethyl) piperidin-4-ylidene)acetamide, 2-(1-(2-methoxycarbonylmethylene)piperidin-4-ylidene)acetamide, 2-(1-isopropylpiperidin-4-ylidene) acetamide, 2-(1-(2-hydroxyethyl)piperidine-4-ylidene)acetamide, 2-(pyrrolidin-3-ylidene)-acetamide, N-(N-(2-(2-(dimethylamino)ethoxy)ethyl)amino)fumaramide, 2-(1-(2-(2-(2-hydroxyethoxy)ethylamino)acetyl) piperidin-4-ylidene)acetamide, 2-((1-methylsulphonyl)piperidin-4-ylidene) acetamide, 4-(piperidin-1-yl)but-2-enamide, 4-(morpholin-4-yl)but-2-enamide, 4-(tert-butylamino)but-2-enamide, 4-(benzylamino)but-2-enamide, 4-(6-hydroxyhexylamino)but-2-enamide, 4-(N-methylbenzylamino)but-2-enamide, 4-(diethylamino)but-2-enamide, 4-(2-methoxyethylamino)but-2-enamide, 4-(diethanolamino)but-2-enamide, 4-(N-methylmethoxyethylamino) but-2-enamide, 4-(N-methyl-ethanolamino)but-2-enamide, 4-(dimethoxyethylamino)but-2-enamide, 4-(N-methyl-6-amino-1-hexanolyl)but-2-enamide and propylamide; one of R2 and R3 is H, while other is selected from unsubstituted C6-aryl-C1-2-alkyl, substituted with 1-2 substitutes or unsubstituted C6-aryl and substituted with 1 substitute or unsubstituted 6-9-member heteroaryl, where, when R2 or R3 is selected from a substituted C6-aryl, substitute is selected from C2-C6-alkynyl, halogen, C6-aryl-C1-alkyloxy (where said C6-aryl can be substituted with 1 substitute selected from halogen, cyano, C1-C6 alkyl, C1-C-6 alkoxy), and 6-member heteroaryl-C-1-alkyloxy, and when R2 or R3 are selected from a substituted heteroaryl, substitute is selected from a group comprising C6-aryl-C1-alkyl (where said C6-aryl is optionally substituted with 1 substitute selected from halogen and cyano, methoxy group), C6-arylamido (where the said C6-aryl can be unsubstituted or substituted with 1 dimethylamino group), C6-arylsulphonylamino, C5-heteroarylamido, C6-cycloalkylamido, C6-arylaminocarbonyl (where said C6-aryl is substituted with 1 methoxy group), C6-aryl-C1-alkyloxy and C6-aryloxy; or R2 and R3, together with a nitrogen atom to which they are bonded, form a substituted or unsubstituted 9-10-member heterocyclyl, where heterocycyl substitutes are selected from halogen, C1-C-6 alkyl, CF3, C6-aryl-C1-alkoxy, -COOMe, -CH2OH and pyrrolyl; and R4 is substituted with 1 methyl or unsubstituted 5-6-member heterocyclyl or unsubstituted 6-member heteroaryl. Invention also relates to specific compounds, pharmaceutical composition based on compound of formula I and use of formula I.EFFECT: technical result is obtaining novel cyanoquinoline derivatives which are useful in treating tumours.33 cl, 20 tbl, 228 ex

New substituted quinoline compounds as inhibitors of s-nitrozoglutation-reductase inhibitors // 2599144
FIELD: chemistry.SUBSTANCE: invention is related to organic chemistry and specifically to novel quinoline derivatives of general formula I or pharmaceutically acceptable salts, stereoisomers or N-oxides, where m = 0 and 1; R1 is independently selected from a group consisting of chlorine, fluorine and bromine; R2b and R2 c are independently selected from a group, consisting of hydrogen, halogen, C1-C3 alkyl, fluorinated C1-C3alkyl, cyano and N (CH3)2; X is selected from a group consisting of n is selected from a group consisting of 0 and 1; R3 is independently selected from a group consisting of halogen, C1-C3 alkyl, fluorinated with1-C3 alkyl, cyano, C1-C3alkoxy and NR4R4′, where R4 and R4′ are independently selected from a group consisting of C1-C3 alkyl; and a is selected from a group consisting of .Invention is also related to the use of formula I, pharmaceutical composition based on the compound of formula I, method of treating pulmonary disorders and inflammatory diseases based on use of the compound of formula I, and a method of producing a pharmaceutical composition based on the compound of formula I.EFFECT: technical result is obtaining novel quinoline derivatives, useful as inhibitors of S-nitrozoglutation reductase (GSNOR).17 cl, 64 ex

Thiohydantoin derivatives useful as androgen receptor antagonists // 2598854
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, in particular to novel thiohydantoin derivatives of general formula (I) or pharmaceutically acceptable salts thereof, where Z is selected from CF3, C1-C3 alkoxy and halogen; Y is selected from halogen; W denotes oxygen; R3 and R4 are independently selected from C1-C4 alkyl, or R3 and R4 and a carbon atom, to which they are bonded, form a 3-6-member cycloalkyl ring; A1 denotes phenyl or pyridyl optionally substituted with one halogen; A2 is (CH2)mY1(CH2)nQ, where m and n are integers independently selected from 0-2, and where at least one of m or n is not equal to zero; Q is selected from C(O)NHR″, C(RxRy)C(O)NR″R1″, cyano, C(O)OR″, C(O)NR″R1″ and 5-member heteroaryl containing 2 heteroatoms selected from nitrogen, oxygen and sulphur; and Y1 is selected from a direct bond and -O-; R″ and R1″ are independently selected from hydrogen, C1-C6 alkyl, or NR″R1″ together form a 4-6-member heterocyclic ring additionally containing 0-1 oxygen atoms, where one carbon atom can be optionally substituted with one hydroxyl group; Rx and Ry are independently selected from hydrogen or methyl; or C(RxRy) together form a 3-5-member cyclic alkyl ring. Invention also relates to a pharmaceutical composition and a local pharmaceutical composition based on the thiohydantoin derivative of formula (I).EFFECT: technical result is obtaining novel thiohydantoin derivatives useful for antagonizing androgen receptor activity.17 cl, 1 tbl, 69 ex

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

Pyrrolidine derivatives as nk-3 antagonists // 2598604
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula I, where R1 is or phenyl, pyridinyl or pyridazinyl, where phenyl, pyridinyl, pyridazinyl can be substituted with cyano, lower alkyl, halogen-substituted phenyl, lower alkyl-substituted [1,2,4]oxadiazol-3-yl or 2-oxo-piperidin-1-yl, X is NR or O, R is -C(O)-lower alkyl, -C(O)-cycloalkyl substituted with lower alkyl, cycloalkyl or phenyl, pyridinyl or pyridazinyl, where phenyl, pyridinyl, pyridazinyl can be substituted with lower alkyl, lower alkoxy, cyano, -C(O)-lower alkyl, halogen or lower alkyl, substituted with halogen, R2 represents hydrogen or lower alkyl, R3 represents hydrogen, halogen, R4 is hydrogen or lower alkyl, where R2 and R4 simultaneously are not hydrogen or lower alkyl, R5 denotes lower alkyl, R6 - halogen, or their pharmaceutically acceptable acid-additive salts.EFFECT: it has been found that present compounds are high potential NK-3 receptor antagonists for treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).18 cl, 36 ex

Compounds for binding to platelet specific glycoprotein iib/iiia and their use for imaging thrombi // 2597425
FIELD: chemistry.SUBSTANCE: invention relates to fluorine containing compounds of formula III:, where R3 is selected from group comprising H, F, CN and NO2; R7 is selected from group comprising Y, -O(CH2)n-Y, -(OCH2CH2)m-Y, Z, -OCH2-Z; -CH2-CH2-Z, -CH=CH-Z and -C≡C-Z; X is selected from CH or N; Y is selected from 18F or F; Z is a group , where * indicates the atom of connection of Z; R5 is selected from group comprising H, CN and NO2; R8 is selected from group comprising Y and -O(CH2)n-Y; n is a 1-3; and m is a 2-3; including E-and Z-isomers and diastereomers, mixtures thereof, and any pharmaceutically acceptable salt or their complex, as well as methods for production thereof, intermediate synthesis compounds.EFFECT: use of salts as diagnostic agents, especially for imaging thrombi.14 cl, 6 tbl, 55 ex

Primary amine diazeniumdiolate heterocyclic derivatives // 2596867
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, which have antihypertensive action. In formula I X represents O or NR7; group is bonded to any carbon ring atom, different from carbon atom to which are bonded R1 and R2; R1 represents hydrogen or together with R2 forms =O; R2 represents hydrogen or together with R1 forms =O; R4 is -C1-6alkyl; R5 and R6, which are bonded to any available carbon ring atom, independently represent hydrogen or R5 and R6 in cases when they are bonded to same carbon atom, form =O; R7 is -C1-6alkyl, -C(O)O-C-1-6alkyl, -C(O)O-C-1-6alkylene-CR8R9R10, -C(O)C1-6alkyl, -C(O)OC3-6carbocycle, -C(O)aryl, -C(O)heteroaryl, where heteroaryl is unsaturated 5- or 6-member ring containing 1-4 heteroatoms selected from N, -C(O)NHC1-6alkyl, -C(O)NH-adamantyl, -SO2C1-6alkyl, aryl or unsaturated 5- or 6-Member heteroaryl ring containing 1-4 heteroatoms selected from N, where aryl, alkyl, alkylene, carbocycle and heteroaryl are unsubstituted or substituted with 1-4 groups independently selected from -CN, halogen, -CF3, -OCF3, -C(O)NH2, -C-1-6alkyl, aryl, unsaturated 5-member heteroaryl ring with 1-3 nitrogen atoms, where R8 and R9 together with carbon atom to which they are bonded form C3-6carbocycle or 4-8-member heterocycle containing an oxygen atom, and where R10 is C1-6alkyl.EFFECT: invention also relates to pharmaceutical compositions containing said compounds, and a method of treating hypertension.29 cl, 43 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

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

3-aminopyridines as gpbar1 agonists // 2594886
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula , where B1 represents CR7 or N; B2 is CR8 or N; R1 is selected from group consisting of phenyl, which is unsubstituted or substituted by one, two or three groups; heteroaryl, which is 5-6-member ring, which may include one or two nitrogen atoms, which is unsubstituted or substituted; 3,6-dihydro-2H-pyran-4-yl, and piperidinyl substituted with C1-7-alkyl groups in amount of one to four; R2 is selected from group consisting of hydrogen atom, C1-7-alkyl, halogen atoms, cyano, C1-7-alkoxy, amino, C1-7-alkylamino, C1-7-alkoxy-C1-7-alkyl-(C1-7-alkyl)amino, and heteroaryl; R2a is selected from group consisting of hydrogen atom, methyl and halogen atom; R3 is selected from group consisting of C1-7-alkyl, halogen-C-1-7-alkyl, hydroxy-C-1-7-alkyl, C1-7-alkoxy-C1-7-alkyl, C1-7-alkylcarbonyl-C1-7-alkyl, carboxyl-C-1-7-alkyl, C1-7-alkoxycarbonyl-C-1-7-alkyl, cyano-C-1-7-alkyl, aminocarbonyl-C-1-7 _alkyl, C1-7-alkylaminokarbonyl-C-1-7-alkyl, di-C1-7-alkylaminokarbonyl-C-1-7-alkyl, C1-7-alkylsulphonyl-C-1-7-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C-1-7-alkyl, unsubstituted heterocyclyl, heterocyclyl-C-1-7-alkyl, where heterocyclyl is unsubstituted or substituted with one or two groups, selected from C1-7-alkyl, and represents 4-6-member ring which can contain one oxygen atom, heteroaryl-C-1-7-alkyl, where heteroaryl is unsubstituted or substituted with one or two groups, selected from C1-7-alkyl, and phenyl-C-1-7-alkoxycarbonylamino-C-1-7-alkyl; R4 is selected from group consisting of hydrogen atom and halogen atom; R5 and R6 are selected independently from each other from group consisting of hydrogen atom, C1-7-alkyl, C1-7-cycloalkyl, halogen atom, halogen-C-1-7-alkyl, halogen-C-1-7-alkoxy, hydroxy, hydroxy-C-1-7-alkyl, C1-7-alkoxy, cyano, carboxyl, C1-7-alkoxycarbonyl, C1-7-alkoxycarbonyl-C-1-7-alkyl, hydroxy-C-1-7-alkoxy, C1-7-alkoxy-C1-7-alkoxy, C1-7-alkylsulfonyl, hydroxy-C-1-7-alkylsulfonyl, C1-7-alkoxy-C1-7-alkylsulfonyl, C1-7-alkylsulfonyl, hydroxy-C-1-7-alkylsulfonyl, C1-7-alkoxy-C1-7-alkylsulfonyl, carboxyl-C-1-7-alkylsulfonyl, carboxyl-C-1-7-alkylsulfonyl, C1-7-alkoxycarbonyl-C-1-7-alkylsulfonyl, C1-7-alkoxycarbonyl-C-1-7-alkylsulfonyl, C1-7-alkoxykarbonylamino-C-1-7-alkylsulfonyl, carboxyl-C-1-7-alkyl-aminocarbonyl-C-1-7-alkylsulfonyl, carboxyl-C-1-7-alkyl-aminocarbonyl-C-1-7alkylsulfonyl, heterocyclilsulfonyl, where it is unsubstituted or substituted by C1-7-alkoxycarbonyl, heterocyclilsulfonyl, besides R8 is selected from group consisting of hydrogen atom, C1-7-alkyl, halogen atom, halogen-C-1-7-alkyl and C1-7-alkoxy; as well as to their pharmaceutically acceptable salts.EFFECT: said compounds are agonists of 1 bile acid receptor interfaced with G protein (GPBAR1; G protein coupled bile acid receptor), and can be used as medicinal agents for treating diabetes, in particular diabetes type 2.22 cl, 5 tbl, 323 ex

3,3-disubstituted-(8-azabicyclo[3.2.1]octa-8-yl)-[5-(1h-pyrasol-4-yl)-thiophen-3-yl]- methanone and related compounds and their use // 2593753
FIELD: chemistry. SUBSTANCE: invention relates to compounds of formula or its pharmaceutically acceptable salts thereof: wherein: -J1 and -J3, taken together, form -CH2CH2-; -Q independently represents pyrid-2-yl and has n substitutes -RF; or -Q independently represents pyrimidin-2-yl and has n substitutes -RF; -n independently equal to 0, 1, 2 or 3; each -RF independently represents -RZ, -F, -Cl, -CF3, -OH, -ORZ, -OCF3, -NH2, -NHRZ or -NRZ 2; each -RZ, if present, independently represents an unsubstituted aliphatic saturated C1-4alkyl; -Y independently represents -OH, -ORYA, -F, -Cl or -CN; -RYA independently represents saturated aliphatic C1-6alkyl; -RA1 independently represents -H or -RAA; -RA2 independently represents H or -RAA; each -RAA independently represents -RAA1, -F, -Cl or -CN; each -RAA1 represents saturated aliphatic C1-4alkyl and possibly substituted with one or more groups -F; -RB1 independently represents -H or -RBB; -RB2 independently represents H or -RBB; each -RBB independently represents -RBB1, -F, -Cl or -CN; each -RBB1 represents saturated aliphatic C1-4 alkyl and possibly substituted with one or more groups -F; -RN independently represents -H or -RNN; and -RNN is a saturated aliphatic C1-4alkyl, which are inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). EFFECT: novel compounds. 63 cl, 4 tbl, 47 ex

Substituted benzoazepines as modulators of toll-like receptors // 2593261
FIELD: chemistry. SUBSTANCE: invention relates to a compound of formula I or tautomer, enantiomer or pharmaceutically acceptable salt thereof, where said formula Y represents -(O)x(CH2)yR11; x is selected from 0 and 1; y is selected from 0, 1, 2, and 3; R11 is selected from phenyl, pyridyl, morpholinyl, 1-oxo-1,3-dihydroisobenzofuranyl and 2-oxo-tetrahydrofuranyl, when x equals 0, said phenyl or pyridinyl substituted -C(O)NR1R2 or T; R1 and R2 is selected independently from hydrogen and C1-6alkyl, wherein said alkyl is optionally substituted -C(O)O(CH2)tR12, or R1 and R2 together with a nitrogen atom to which they are bonded, form a saturated 5-member heterocycle containing 1-4 heteroatoms selected from nitrogen, oxygen and sulphur; t is selected from 0, 1, 2, and 3; R12 is selected from C3-6cycloalkyl and phenyl; T is selected from 2-oxo-1,3-dioxolane, 2-oxotetrahydrofuran -(CHR7)zOR9, -(O)u(CH2)sC(O)R8, -OSO2R13 and -CH(OH)CH2OH; R7 represents H; R8 is -OR10; R9 represents H; R10 is selected from C1-6alkyl, -(CH(2)R12 and hydrogen, wherein said alkyl is optionally substituted with halogen or diC1-6alkylamine; R13 represents CF3; u is selected from 0 and 1; z is selected from 1, 2, and 3; s is selected from 1 and 2; R5 is selected from -NR3R4 and -OR10; R3 and R4 independently selected from H, C1-12alkyl, -(O)q(CH2)rP; said alkyl is optionally substituted with -OH; q is selected from 0 and 1; r is selected from 0, 1, 2, and 3; P is selected from phenyl, -SO2R6, piperidinyl and pirrolidinyl; and R6 is -NH2, provided that when R11 is a phenyl or pyridyl, then a) x+y ≥ 1; or b) R11 is substituted with T; or c) R5 is NR3R4, and at least one of R3 or R4 is -(O)q(CH2)rP-, and q+r ≥ 1; or d) at least one of R1 or R2 represents alkyl, substituted with -C(O)O(CH2)R12. Invention also relates to a pharmaceutical composition exhibiting TLR7- and/or TLR8 agonist activity, comprising an effective amount of a compound of formula I together with a pharmaceutically acceptable diluent or carrier. EFFECT: substituted benzoazepine exhibiting TLR7- and/or TLR8 agonist activity. 17 cl, 3 tbl, 47 ex

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

Novel triazole compounds // 2588137
FIELD: pharmaceuticals.SUBSTANCE: invention relates to compounds of formula (I), pharmaceutically acceptable salts and esters. Compounds of formula (I) have affinity and selectivity for GABA A α5 receptor. In formula X is N or CH; R1, R2 - C1-C7-alkyl, phenyl substituted by 1 halogen, wherein one of substituents R1 and R2 is an alkyl group; R3 - haloC1-C7-alkyl, nitro, -C(O) R4, -C(O) NR5R6; R4 - C1-C7-alkyl, hydroxy, C1-C7-alkoxy; R5 - hydrogen, C1-C7-alkyl, haloC1-C7 alkyl hydroxyC1-C7-alkyl, -(CH2)n-C3-C8 cycloalkyl, - (CH2)n- (4-6 membered heterocycloalkyl with 1 heteroatom selected from O), wherein heterocycloalkyl is optionally substituted with one C1-C7-alkyl group; n is an integer ranging from 0 to 1; R6 - hydrogen, C1-C7-alkyl; or R5 and R6 together with nitrogen to which they are attached form a bicyclic 7-membered heterocycloalkyl with additional heteroatom selected from O, 6-membered heterocycloalkyl with additional heteroatom selected from O, S, wherein heterocycloalkyl is optionally substituted by one or more oxo groups. Invention also relates to a pharmaceutical composition comprising a compound of invention in an effective amount, to a method for treating or preventing diseases associated with GABA A α5 receptor, use of compounds for preparation of medicaments and use of compounds for treating or preventing diseases associated with GABA A α5 receptor.EFFECT: technical result is obtaining novel compounds having affinity and selectivity for GABA A α5 receptor.23 cl, 1 tbl, 53 ex

Catechol-o-methyl transferase inhibitors and use thereof in treating psychotic disorders // 2586974
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, namely to derivatives of 4-pyridinone formula I or pharmaceutically acceptable salts thereof, where A is hydrogen, B(OH)2, halogen, C(O)NH(CH2)nC(O)N(R3)2; X is hydrogen or halogen; Y denotes phenyl, benzimidazolil, benztiazolil, benzoksazolil, benzpiperidinil, quinolyl, indolyl, indazolyl or pyridyl, each optionally substituted with 1-3 groups Ra, provided that Y denotes phenyl, then at least one of said Ra selected from OCF3, O(CH2)nC3-6cycloalkyl, NR2C(O)R2, C(O)R2, N(R2)2, (CH2)nC(O)OR2, OR2, (CH2)nheterocyclyl, NH(CH2)nheterocyclyl, (CH2)n(C)6-10aryl, O(CH2)nC6-10aryl or O(CH2)nheterocyclyl, where said heterocyclic ring and aryl optionally substituted with 1-3 groups Rb; R1 represents hydrogen, NR2R3, Si(CH3)3, (CH2)nC6-10aryl, C2alkenyl or C1-4alkyl, said alkyl and alkenyl optionally substituted with 1-3 groups of halogen, OH, C1-6alkyl, O-C1-6alkyl, NR2R3, SOR2, NHSO2R2, CF3, C6-10aryl, heterocyclyl, -C≡C-C6-10aryl, C(O)NR2R3, wherein said aryl and heterocyclyl optionally substituted with 1-2 groups Ra; R2 and R3 independently denote H, C1-6alkyl, (CH2)nheterocyclyl, (CH2)nC6-10aryl, wherein said aryl optionally substituted by group Ra or R2 and R3 together with nitrogen atom to which they are bonded, form a 6-member ring, which contains oxygen; Ra is C1-6alkyl, halogen, CF3, OCF3, C3-6cycloalkyl, O(CH2)nC3-6cycloalkyl, NR2C(O)R2, C(O)R2, CN, N(R2)2, (CH2)nC(O)OR2, OR2, (CH2)nheterocyclyl, NH(CH2)nheterocyclyl, (CH2)nC6-10aryl, O(CH2)nC6-10aryl or O(CH2)nheterocyclyl, wherein said heterocyclyl and aryl optionally substituted with 1-3 groups Rb; Rb is C1-6alkyl, halogen, CHF2, oxo (=O), N(R2)2, CH2OH, S(O)2NR2R3, (CH2)nC6-10aryl, (CH2)nheterocyclyl, NH(CH2)nheterocyclyl, OR2, C3-6cycloalkyl, CF3 or CN; and n equals 0-3; and where heterocycle is aromatic or saturated or partially saturated monocyclic or bicyclic ring containing 5-10 atoms, among which 1-4 atoms are heteroatoms selected from nitrogen, oxygen and sulphur. Invention also relates to pharmaceutical composition based on compound of formula I, method of treating and/or preventing neurological and psychiatric disorders and method of intensifying action of antipsychotic agent based on use of compound of formula I.EFFECT: new compounds are prepared effective in treating diseases associated with catechol-O-methyltransferase (COMT).52 cl, 1 tbl, 17 ex

Pharmaceutically acceptable salt (e)-n-[4-[[3-chloro-4-(2-pyridylmethoxy) phenyl] amino] -3-cyano-7-ethoxy-6-quinolyl] -3-[(2r)- 1- methylpyrrolidin-2-yl] prop-2-enamide, method for production and use thereof in treating cancer // 2583056
FIELD: pharmaceutics.SUBSTANCE: invention relates to a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide (formula (I)), where n equals 1, 2 or 3; and M is a molecule of acid, where said salt is selected from group consisting of hydrochloride, para-toluene sulphonate, methanesulphonate, maleate, succinate and L-malate. Invention also relates to method of producing salt of formula (I), pharmaceutical composition based on salt compound of formula (I) and use of salt compound of formula (I).EFFECT: novel salt of compound of formula (I) effective in treating cancer.10 cl, 7 tbl, 13 ex
Sgc stimulators // 2582679
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula IA or IB or their pharmaceutically acceptable salts. The compounds of formula IA or IB possess sGC-stimulating activity. In formulas IA and IB , a circled B symbol means B ring, and B ring represents phenyl; n is equal to an integer specified in 0 to 1; each JB is independently specified in halogen; X is specified in N or C-H; D ring represents a 6-merous ring having X in formula IA, or a 5-merous ring having Y in formula IB; each Y is independently specified in C-H, C, N, O or S and independently substituted by JD when Y represents C or N; each of bonds between the two neighbouring atoms Y or between neighbouring Y and N in formula IB independently represents a single or double bond depending on whether Y is C, N, O or S, and D ring is aromatic; m is equal to an integer specified in 0 to 3; each JD is a substituted on a halogen or nitrogen atom of the ring and independently specified in halogen, -C(O)N(RD)2, -N(RD)2, -N(Rd)C(O)RD, -N(Rd)C(O)ORD, a 4-8-merous heterocyclic ring, wherein each specified 4-8-merous heterocyclic ring contains 1 to 2 heteroatoms independently specified in O, N or S; RC is specified in halogen, -CN, C1-6alkyl or C ring. The invention also refers to individual compounds and a pharmaceutical composition containing the compound of the invention or its pharmaceutically acceptable salt in an effective amount.EFFECT: produced are the new compounds of formula IA or IB possessing sGC-stimulating activity.58 cl, 6 tbl, 12 ex
Quinoline derivatives and melk inhibitors containing same // 2582610
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, namely to a heterocyclic compound of general formula (I) or its pharmaceutically acceptable salt thereof, where: R1 is C1-C6 alkyl sulphonyl or -CO-R5, where R5 is C1-C-6 alkyl or C3-C5 cycloalkyl; R2 represents phenyl which can contain group substitute selected from group of substitutes C, or -NR6AR7A, where R6A is hydrogen atom and R7A is -(CH2)n-R10A (where n equals whole number from 0 to 2 and R10A represents mono- or tricyclic C3-C10 cycloalkyl, which can contain group substitute selected from group of substitutes D, phenyl, which can contain group substitute selected from a group of substitutes E, aliphatic heterocyclic group which is selected from piperidinil, piperazinil and azabicyclooctanil and can be substituted C1-C-6 alkyl, aromatic heterocyclic group which is selected from a pyridinyl, pyrimidinyl and pirazolil and can contain group substitute selected from a group of substitutes I), or R6A and R7A is formed with adjacent nitrogen atom aliphatic heterocyclic group that is selected from piperidinil and piperazinil and may contain group substitute selected from a group of substitutes F; R3 is C6-C10 aryl, which can contain group substitute selected from a group of substitutes G, or aromatic heterocyclic group which is selected from a pyridinyl, pyrimidinyl, tiofenil, isoxazolyl, pyrrolyl and pirazolil and can contain group substitute selected from a group of substitutes H; R4 is hydrogen atom or halogen; R is hydrogen atom or halogen; and R101 is hydrogen atom; where said substitutes C - I are one-three substitutes are given in claim. Invention also relates to pharmaceutical composition, an inhibitor of MELK, agent, which simulates the expression MELK, anticancer agent based on compounds of formula (I), method of treating and/or preventing diseases, which includes MELK overexpression, using compound of formula (I).EFFECT: obtained are novel heterocyclic compounds effective as anti-tumour agent.19 cl, 4 tbl, 1200 ex

New piperidine compound or salt thereof // 2581834
FIELD: pharmaceutics.SUBSTANCE: present invention relates to novel piperidine compound of general formula (I) or its pharmaceutically acceptable salt. Besides, present invention relates to novel agent for enhancing anti-tumour effect, agonist, which include taxane anticancer agent for combined therapy. In compounds of formula (I) R1 is carboxyl group of -C(=O)NR5R6 or oxadiazolyl group, optionally containing C1-C6alkyl group or trifluoromethyl group as substitute; R2 is halogen atom or C1-C6alkoxy group; R3 is phenyl group, optionally containing 1-3 identical or different groups selected from halogen atom, C1-C6alkyl group C1-C6alkoxy group and trifluoromethyl group as substitute; R4 is a hydrogen atom or C1-C6alkyl group; and R5 and6 are identical or different, and each denotes a hydrogen atom, C1-C6alkyl group or C3-C6cycloalkyl group, or R5 and R6 optionally form 3-6-member nitrogen containing heterocyclic group saturated together with nitrogen atom to which R5 and R6 are connected.EFFECT: this compound has excellent aurora A selective inhibiting action and is suitable as orally administered anticancer drug.24 cl, 23 tbl, 28 ex

Triazole derivatives and application thereof in neurological diseases // 2581504
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts and esters. The compounds of formula (I) possess GABA A α5 receptor affinity and selectivity. In formula A represents -CH2-O-, -CH=CH- or -C≡C-; X represents N or CH; Y represents N or CR9; Z represents N or CR10; R1, R2 represent C1-7-alkyl, phenyl optionally substituted by one halo, or 6-merous heteroaryl containing one ring N heteroatom optionally substituted by one halo, wherein one of R1, R2 represents C1-7-alkyl; R3 represents halo, -C(O)R4 or -C(O)NR5R6. The invention also refers to a pharmaceutical composition containing the compound of the invention in an effective amount and the use of the compounds to produce medicinal products.EFFECT: new compounds of formula (I) possessing GABA A α5 receptor affinity and selectivity are produced.24 cl, 1 tbl, 84 ex

Prodrug of triazolone compound // 2581369
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a new compound of formula (I) or its pharmaceutically acceptable salt possessing the properties of blood coagulation inhibitor. In the compound of formula (I) , R1 represents 1) phenyl optionally substituted by one to three C1-C6alkyl groups, 2) C1-C6alkoxy or 3) C2-C6alkenyloxy; R2 represents a hydrogen atom, C1-C6alkylcarbonyl or pyridylcarbonyl; each of R3 and R4 independently represents a hydrogen atom or C1-C6alkyl; A represents a single bond, oxygen atom, or a group presented by formula (II) , wherein each of Ra and Rb independently represents a hydrogen atom or C1-C6alkyl, whereas *1 and *2 mean a binding to carbonyl and R5, respectively, in formula (I), or a group presented by formula (III) , wherein each of Rc, Rd, Re and Rf independently represents a hydrogen atom or C1-C6alkyl, whereas *1 and *2 are characterised by the same values described above; and R5 represents C1-C6alkyl or C3-C8cycloalkyl, whereas C1-C6alkyl or C3-C8cycloalkyl in R5 is independently substituted by one to three identical or different substitutes specified in a group of substitutes consisting of a halogen atom, C1-C6akyl and C1-C6alkoxy.EFFECT: compounds can find application in the diseases caused by thrombus formation, such as thrombosis, deep-vein thrombosis, pulmonary embolism, cerebral infarction, myocardial infarction, acute coronary syndrome, vascular restenosis, disseminated intravascular coagulation, or malignant tumour.16 cl, 6 dwg, 5 tbl, 68 ex

Aminopyrazole derivative // 2580543
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound, which has formula presented below, or a pharmaceutically acceptable salt thereof. This compound can inhibit fibroblast growth factor receptor (FGFR) kinases in tumour tissues. In formula (I) A means a heteroaryl specified in indole, azaindole, benzofuran, benzothiophene, benzorhiazole, quinoline and pyrrole, or a benzene ring; R1 particularly means hydrogen, hydroxy, halogen, cyano, C1-4 haloalkyl, C1-6 alkyl, C2-6 alkinyl; R2 particularly means hydrogen, hydroxy, halogen, cyano, C1-4 haloalkyl, C1-6 alkyl, C2-6 alkinyl, C3-7 cycloalkyl, phenylC1-4 alkyl, or R1 and R2 together with a nitrogen atom connected thereto form a 5-6-merous heterocyclyl group containing two oxygen atoms optionally substituted by a halogen; R3 means H, C1-5 alkyl group, phenylC1-5 alkyl group or C1-4 haloalkyl group; and R4 means H or halogen.EFFECT: invention refers to a pharmaceutical composition and an agent for FGFR inhibition, an agent for preventing or treating a malignant new growth, a method for preventing or treating malignant new growths, and the use of the compounds for producing a medicinal agent for preventing or treating malignant new growths.10 cl, 35 tbl, 246 ex

Substituted benzoazepines as toll-like receptor modulators // 2580320
FIELD: chemistry.SUBSTANCE: invention relates to formula compounds, where Y stands for 6-membered heteroaryl, containing 1-2 nitrogen atoms; R2 is selected from OR14 and NR6R7; each of R6 and R7 is independently selected from H, C1-C12 alkyl, C3-C12 cycloalkyl, 6-membered heterocycle, containing 1 nitrogen atom, or benzyl, where said alkyl, cycloalkyl or benzyl are optionally substituted with one or more groups, independently selected from -F, -OR8, -NR12SO2R13, -C(=O)NR12R13, or R6 and R7, together with nitrogen atom, which they are bound to, form 5-6-membered heterocylic ring, containing 1 nitrogen atom, and said 5-6-membered heterocyclic ring is optionally substituted with one or more -OH; R8 is selected from hydrogen and C1-C12 alkyl, and each of R12, R13 and R14 is independently selected from H and C1-C12 alkyl, where said alkyl is optionally substituted with -OH; or their tautomers, enantiomers or pharmaceutically acceptable salts. The invention also relates to particular derivatives of benzo[b]azepine, given on i. 3, to set for treating TLR7- and/or TLR8-mediated condition, pharmaceutical composition and methods for treating TLR7- and/or TLR8-mediated conditions.EFFECT: derivatives, possessing agonistic activity with respect to TLR7 or TLR8 receptor.14 cl, 3 tbl, 222 ex
 
2551206.
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