Containing three or more hetero rings (C07D413/14)

C   Chemistry; metallurgy(318327)
C07   Organic chemistry(61593)
C07D413/14                     Containing three or more hetero rings(449)
New benzoazepine derivative and its medical application // 2642783
FIELD: pharmacology.SUBSTANCE: invention relates to a new benzoazepine derivative of formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a hydroxyl group, a lower alkoxy group or , where A is absent or a lower alkylene group which may be substituted by a lower alkyl group; R6 represents a hydrogen atom or a lower alkyl group; R7 represents a hydrogen atom, a hydroxyl group, a five-membered aromatic heterocyclic group containing 3 heteroatoms selected from nitrogen and oxygen which may be substituted by a lower alkyl group, a five-membered non-aromatic heterocyclic group containing one nitrogen atom which may be substituted by an oxo group or a carbamoyl group , which may be substituted by a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 is a lower alkyl group which may be substituted by 1 to 3 fluorine atoms or a halogen atom; R4 represents a lower alkoxy group which may be substituted by 1 to 3 halogen atoms, a five-membered aromatic monocyclic heterocyclic group or a five-membered non-aromatic monocyclic heterocyclic group (provided that each of these heterocyclic groups contains one nitrogen atom, two nitrogen atoms or one nitrogen atom and one oxygen atom in the ring, and may contain a lower alkyl group); and R5 represents a hydrogen atom, a lower alkyl group or a halogen atom. The invention also relates to a pharmaceutical composition based on a compound of the formula and intermediates of the formulas and .EFFECT: new benzoazepine derivatives having V2 receptor agonist activity are obtained.14 cl, 12 tbl, 128 ex
Comt inhibitors // 2642779
FIELD: pharmacology.SUBSTANCE: invention relates to new compounds of the formula (I) and their pharmaceutically acceptable salts which have the properties of a catechol-O-methyltransferase (COMT) inhibitor. In the compound of the formula (I) , where R1 is hydrogen, methyl, Br, F or Cl; R2 is hydrogen, lower alkyl, Br, I, C3-6cycloalkyl, C(O)O-lower alkyl, C(O)NH-lower alkyl substituted by halogen, C(O)(morpholine) or is 3,4-dihydronaphthalen-2-yl optionally substituted by lower alkyl, 1,2,3,4-tetrahydronaphthalen-2-yl, 2,3-dihydrobenzofuran-6-yl, 1-methyl-2,3-dihydro-1H-indolin-5-yl, 1-methylindolin-5-yl, tetrahydropyran-4-yl, 3,6-dihydro-2H-pyran-4-yl, 2-isopropyl-1,2,3-tetrahydroisoquinolin-5-yl, 2,3-dihydro- dimethyl[1,4]dioxin-6-yl, benzo[1,3]-dioxol-5-yl, 1,2,3,4-tetrahydroisoquinolin-7-yl optionally substituted by lower alkyl, cyclohexenyl, morpholinyl, 4-methylpiperazinyl, naphthalen-1-yl, naphtalen-2-yl, or represents (CHR)n-phenyl optionally substituted by one to five substituents R4, where R4 is F, Cl, CN, CH2-CN, lower alkyl, hydroxy, lower alkyl, substituted hydroxy, lower alkoxy, (CH2)1.2-lower alkoxy, S-lower alkyl, (CH2)1.2-S-lower alkyl, -CH2)1.2-S (O)2-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkylamino, -S(O)2-piperidinyl, lower alkyl substituted by halogen, -N=N-phenyl, di-lower alkylamino, (CH2)1.2-di-lower alkylamino, (CH2)2-NH-lower alkyl, NHC(O)-lower alkyl, lower alkoxy substituted by halogen, CH(CH3) C(O)O-lower alkyl, O-phenyl, O-benzyl, phenyl, optionally substituted CF3, SF5, benzyl, C(O)-lower alkyl, C(O)-phenyl, C(O)-morpholinyl, C(O)-4-methylpiperazinyl, C(O)-di-oxothiomorpholinyl, C(O)-piperidinyl, optionally substituted by F, C(O)-NH-(CH2)2-morpholinyl, C(O)-NR-(CH2)2-NR2, C(O)-N-di-lower alkyl, CH2-O-(CH2)2-4-methylpiperazinyl, CH2-O-(CH2)2-di-alkylamino, CH2-O-(CH2)2-pyrrolidinyl, CH2-O-(CH2)2-morpholinyl, CH2-O-(CH2)2-piperidinyl optionally substituted by lower alkyl substituted by halogen or lower alkyl, (CH2)3,4-pyrrolidinyl, (CH2)2,3-di-lower alkylamino, morpholinyl, CH2-morpholinyl, CH2-piperazine substituted by lower alkyl, -S(O)2-piperazine substituted by lower alkyl, CH2-O-C(O)-piperazine substituted by lower alkyl, pyrazolyl or (CH2)1,2-lower alkoxy; R is hydrogen, lower alkyl or hydroxyl; n is 0, 1, 2, or 3; or R2 is C(O)-phenyl optionally substituted by lower alkyl; or is -O-phenyl optionally substituted by F; or is CH=CH-phenyl optionally substituted by lower alkyl; or is C≡C-phenyl; or R2 is a heteroaryl selected from the group consisting of pyrazolyl, thiazolyl, pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl, isothiazolyl, thiophenyl, 1-thia-3,4-diazolyl, imidazo[1,2-a]pyridinyl, indazolyl, quinolinyl or isoquinolinyl, and the said groups are optionally substituted by R5, where R5 is halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, hydroxy, (CH2)1.2-lower alkoxy, CH2-di-lower alkylamino, di-lower alkylamino, morpholinyl, piperazinyl, pyrrolidin-1-yl, C(O)-piperidinyl, C(O)-4-methylpiperazinyl, phenyl optionally substituted by halogen, pyridinyl, S(O)2N(CH3)2, C(O)O-lower alkyl, NHC(O)-lower alkyl, or is C(O)-heteroaryl selected from pyridinyl and thiophenyl, where heteroaryl groups are optionally substituted by lower alkyl, n is 0, 1, 2 or 3; R3 is hydrogen, methyl, Br, F, Cl, CF3, nitro, amino, cyano, NHC(O)-phenyl, or is 1-methyl-1,2,3,6-tetrahydropyridinyl, or is pyridinyl optionally substituted by methyl or morpholinyl, or is phenyl optionally substituted by methyl , SO2CH3, CF3, CN, F or C(O)N (di-lower alkyl).EFFECT: compounds can be used to treat Parkinson's disease, depression, cognitive impairment and motor symptoms, resistant depression, cognitive impairment, mood and negative symptoms of schizophrenia.16 cl, 2 tbl, 256 ex
Heterocyclic compounds, effective for kinase inhibition // 2640862
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I)or a pharmaceutically acceptable salt thereof, wherein Q is O; W is phenyl; X is absent; Y is NH; Z1 and Z2 are N; Z3 is NR5, where R5 is hydrogen; R1 is pyridine or pyrimidine; optionally substituted with C1-C6alkyl, C1-C6alkoxy, -NR10R11 or -SOmR12, where R10 and R11 are hydrogen, R12 is C1-C6alkyl; and m is 0; R3 is C1-C6alkyl; R2 is C1-C6alkyl when p is 1; or one R2 is C1-C6alkyl and one R2 is halogen when p is 2; or one R2 and R3 combined with formation of a five- to seven-membered carbocycle; R4 is hydrogen; p=1 or 2; and n is 1.EFFECT: heterocyclic compounds designed for cancer treatment.12 cl, 1 tbl, 8 ex
Benzisoxazole modulators of neurogenesis // 2640590
FIELD: pharmacology.SUBSTANCE: new compounds are obtained that can be used to treat schizophrenia, obsessive-compulsive personality disorders, major depression, bipolar disorders, anxiety, normal aging, epilepsy, retinal degeneration, traumatic brain damage, spinal cord injuries, posttraumatic stress, panic disorders, Parkinson's disease , dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down's syndrome, diseases from the autism spectrum, and loss of hearing, ringing in the ears, spinal-cerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuroactive substances such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.EFFECT: increased efficiency of treatment.12 cl, 44 ex
Hetero-aromatic methylic derivative of cyclic amine // 2639869
FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the formula (IA), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; Y is any structure from the following group of formulas (a); n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group; R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 an alkyl group; or a pharmaceutically acceptable salt thereof. The invention also relates to a compound represented by the formula (I), where X1 and X2 are the same or different and are a nitrogen atom or a CH group; any one of Y1 and Y2 is a nitrogen atom, and the other is CH; n is 1 or 2; R1 is a hydrogen atom, a halogen atom or a C1-6 alkyl group;R2 is a triazolyl group or a pyrimidinyl group; R3 is a hydrogen atom or a halogen atom; and R4 is a hydrogen atom or a C1-6 alkyl group; or a pharmaceutically acceptable salt thereof. The compounds of the invention are intended for the production of a pharmaceutical composition having antagonistic activity against OX1 and OX2 orexin receptors.EFFECT: hetero-aromatic methyl derivative of cyclic amine, which has antagonistic activity against OX1 and OX2 orexin receptors.9 cl, 6 tbl, 85 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
Dna-pk inhibitors // 2638540
FIELD: biotechnology.SUBSTANCE: invention relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, inhibiting DNA-dependent protein kinase (DNA-PK). The compounds can be used in the treatment of cancer. The compounds have a radiosensitizing effect on the line of cancer cells sensitive to radiation and can be used to enhance the effect of the therapeutic regimen for the treatment of cancer. In general formula (I), X is N or CRA5; RA1is F, C1-4-alkyl, C3-5cycloalkyl, OC1-4-alkyl, OC1-4-alkyl-C3-5cycloalkyl, NH2, NHC1-4-alkyl, NHC1-4-alkyl-C3-5cycloalkyl or C0-4-alkylheterocyclyl, the said heterocyclic ring system being selected from oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, or morpholinyl, and each of the said alkyl, cycloalkyl or heterocyclyl is optionally substituted with a maximum of three F atoms, a maximum of three 2H atoms, a maximum of two non-hemin OH groups, or a maximum of two OC1-2-alkyl; each RA4 is independently H or 2H; RA5 is hydrogen, F, C1-4-alkyl or OC1-4-alkyl, each of the said alkyls being optionally substituted with a maximum of three F atoms or a maximum of three 2H atoms; RB3 is C (O) NHC1-4-alkyl. The said alkyl is optionally substituted with a maximum of three F atoms, a maximum of three 2H atoms, a maximum of two non-hemin OH groups, or a maximum of two OC1-2-alkyl; and each RB4 is independently hydrogen, deuterium, F, or C1-4-alkyl.EFFECT: improved compound properties.18 cl, 3 tbl, 14 ex
Benzo[d]isoxazole derivatives and their application // 2638155
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of the formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, wherein the linker L1 is selected independently and represents -CH2-, -NH-, -O- or -S-; R1 is selected independently and is hydrogen, halogen, -C1-3-alkyl, partially or fully halogenated -C1-3-alkyl, -CN, -OH, -O-C1-3-alkyl, -NH2, -NHC1-3-alkyl, -N (C1-3-alkyl) C1-3-alkyl, -C1-3-alkyl-NH2, -C1-3-alkyl-NH-C1-3-alkyl, -C1-3-alkyl-N(C1-3-alkyl)C1-3-alkyl or a 5-membered heteroaryl ring containing 1 to 4 N atoms and 0 to 1 S atom; R1 group contains 0-2 R4 substituents; R2 is selected independently and is halogen, partially or fully halogenated -CH3 or -OCH3; R3 is selected independently and is hydrogen or halogen; R4 is selected independently and is halogen or C1-3-alkyl; A cycle is selected independently and represents phenyl, a 5-6 membered heteroaryl ring containing 1 to 2 N atoms; A cycle contains 0-1 R5 substituent and 0-2 R6substituent; R5 is selected independently and is phenyl; 5-9 membered heteroaryl containing 1 to 2 N atoms and 0 to 1 S or O atom, 5-6 membered cycloalkyl or 5-6 membered heterocycle containing 1 to 2 N atoms, 0 to 1 S or O atoms; R5 contains 0-2 R'6substituents; R6 and R'6 are selected independently and represent -OH, -C1-3-alkyl, -C(O)OH, -C(O)NH2, -NHC(O)H, -NHC(O)C1-3-alkyl, -C1-3-alkyl-NHC(O)H, -C1-3-alkyl-NHC(O)C1-3-alkyl, -NHC(O)OH, -C1-3-alkyl-NHC(O)OH, -NH2, -NHC1-3-alkyl, -N(C1-3-alkyl)C1-3-alkyl, -C1-3-alkyl-NH2, -C1-3-alkyl-NHC1-3-alkyl, -C1-3-alkyl-N(C1-3-alkyl)C1-3-alkyl, -CN, halogen, -S(O)2NH2, a 5-6 membered saturated, unsaturated or partially saturated heterocycle containing 1 to 4 N atoms, 0 to 1 atom S; R6 and R'6 contain 0-2 R7 substituents; R7 is selected independently and is = O, -C1-3-alkyl, -NH2, -NHC1-3-alkyl, -N (C1-3-alkyl) C1-3-alkyl, -C1-3-alkyl-NH2, -C1-3-alkyl-NHC1-3-alkyl, -C1-3-alkyl-N(C1-3-alkyl)C1-3-alkyl, -OH, -OC1-3-alkyl, -C1-3-alkyl-OH, -C1-3-alkyl-O-C1-3-alkyl or halogen. The compounds of the invention are intended to be used as inhibitors of the coagulation factor XIa in blood or plasma, as well as for preparation of a pharmaceutical composition for treatment and/or prevention of a condition of a mammal characterized by undesirable thrombosis. A pharmaceutical composition for treatment and/or prevention of a condition of a mammal characterized by undesired thrombosis comprises an effective amount of a compound of the invention and at least one pharmaceutically acceptable excipient.EFFECT: increased efficiency of derivatives.9 cl, 5 ex
Pyrazolaminopirimidine derivatives as modulators of leucine-repeating kinase 2 // 2637947
FIELD: pharmacology.SUBSTANCE: invention relates to pyrazolaminopyrimidine derivatives listed in claim 1 which are modulators of leucine-repeating kinase 2 (LRRK2), a pharmaceutical composition containing them, application of these compounds for treatment of diseases associated with the LRRK2 receptor such as Parkinson's disease, and to a method for Parkinson's disease treatment.EFFECT: higher efficacy of compound application.6 cl, 4 tbl, 52 ex
Triazolcarboxamide derivatives // 2637938
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula I. In formula IR1 is phenyl or pyridinyl optionally substituted by halogen, lower alkyl, lower alkoxy, lower alkyl, substituted halogen, and lower alkoxy substituted by halogen; X1 is -N = or CH; X2 is a CR2 or =N-; X3 is -N= or CH; provided that only two of X1, X2 or X3 are nitrogen; where is a triazole group selected from , or ; R2 is hydrogen or lower alkyl; Z is a bond, -O- or -CH2-. The compounds of the invention possess affinity for the receptors associated with trace amines (TAAR). The invention also relates to pharmaceutical compositions and to application of a compound for drug manufacture.EFFECT: new compounds of formula I are obtained that have a high affinity for the receptors associated with trace amines, especially TAAR1.12 cl, 1 tbl, 36 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

New glp-1 receptor modulators // 2634896
FIELD: pharmacology.SUBSTANCE: compounds can be used in combination to reduce glucose with exenatide. In the formula IR or IS , A is a heteroaryl selected from imidazole, oxadiazole, thiadiazole, thiazole, oxazole, pyridine, pyrimidine, pyridazine, triazine; B is a heterocyclyl selected from isoxazole, oxazole, pyrimidine, pyrazole, thiazole, thiophenyl, thiadiazole, azepine, optionally fused to another nitrogen-containing 6-membered heterocyclic ring; C is an aryl selected from phenyl and naphthyl, benzyl; Y1 and Y2 are absent; Z is -C(O)-; each R1 is independently H or C1-4 alkyl; R2 is -O-R8, -N(R1)-SO2-R8, -NR41R42, -N(R1)-(CRaRb)m-COOH, -N(R1)-(CRaRb)m-CO-N(R1)-heterocyclyl, -N(R1)-(CRaRb)m-CO-N(R1)(R7) or -N(R1)-heterocyclyl, wherein R2 is not -OH or -NH2, and heterocyclyl is a 5-6 membered heterocyclyl containing 1 to 3 heteroatoms selected from N and S; each R3 and R4 is independently halogen, C1-C4alkyl, C1-C4alkyl substituted with R31, C1-C4alkoxy, halogenC1-C4alkyl, perhalogenC1-C4alkyl, halogenC1-C4alkoxy, -OH, -NR1R8, -C(O)R8, -C(O)NR1R8, -S(O)2R8, -OS(O)2R8, -(CRaRb)mNR1R8, -(CRaRb)mO(CRaRb)mR8; or any two R3 or R4 groups on the same carbon atom, taken together, form oxo, values of R31, R40, R41, R42 are indicated in the claims; W1 is absent; each Ra and Rb have values indicated in the claims; R5 is R7, -(CH2)m-L2-(CH2)m-R7 or -(-L3-(CRaRb)r-)s-L3-R7; R7, R8 have values indicated in the claims; L2 is independently, from the near to the far end of the structure of the formula I-R or I-S, absent or -O-; each L3 is independently absent, -O- or -N(R1)-, each m is independently 0, 1, 2, 3, 4, 5 or 6; each n is independently 0, or 1, or 2; P is 0, 1, 2, or 3; Q is 0, 1, 2, or 3.EFFECT: compounds have activity for glucagon-like peptide 1 and can be used to treat diseases for which modulation or potentiation of GLP-1R is prescribed, particularly for the treatment of diabetes.8 cl, 2 tbl, 381 ex

Substituted benzene compounds // 2629118
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (Ie) or pharmaceutically acceptable salts thereof: where Z is NR7R8 or S(O)aR7, where a is 0; R1 is H or C1-C6 alkyl optionally substituted with one or more substituents selected from hydroxyl, C1-C6 alkoxy; Each of R2 and R4 is independently -Q1-T1, wherein Q1 is a bond or a C1-C3 alkyl linker optionally substituted with one or more substituents selected from halogen and hydroxyl, and T1 is H, C1-C3 alkyl; R3 is H or halogen; R5 is H or C1-C6 alkyl; R6 is H, halogen, -C(O)NRaRb or RS2, where RS2 is C1-C6 alkyl or 4-12 membered heterocycloalkyl containing from 0 to 3 heteroatoms in the ring selected from O, N or S, and Wherein each of Ra and Rb is independently H, C1-C6 alkyl or Ra and Rb together with the N atom to which they are attached form a 4-12 membered heterocycloalkyl ring containing 0 or 1 additional heteroatom selected from O, N or S; R7 is -Q4-T4, wherein Q4 is a bond or a C1-C4 alkyl linker and T4 is H, C1-C6 alkyl, C3-C8 cycloalkyl, C(O)-C1-C6 alkyl or 4-14 membered heterocycloalkyl, Containing 1 to 3 ring heteroatoms selected from O, N or S, each of which is optionally substituted with one or more -Q5-T5, wherein Q5 is a bond, C(O), C(O) NRk, NRkC(O) or a C1-C3 alkyl linker, wherein Rk is H or C1-C6 alkyl, and T5 is H, C1-C6 alkyl; R8 is H, C1-C6 alkyl optionally substituted with halogen or C1-C6 alkoxy, C2-C6 alkenyl, C3-C8 cycloalkyl or 4- to 7-membered heterocycloalkyl containing 1-3 heteroatoms in the ring selected from O, N or S; or R7 and R8 together with the N atom to which they are attached form a 4-12 membered heterocycloalkyl ring containing 0-2 additional heteroatoms selected from O, S or N and a 4-12 membered heterocycloalkyl ring that forms R7 and R8 is optionally substituted with one or more -Q6-T6, wherein Q6 is a bond or a C1-C3 alkyl linker and T6 is H, halogen, C1-C6 alkyl; and R12 is halogen, C1-C6 alkoxyl, C2-C6 alkenyl or C1-C6 alkyl optionally substituted with halogen.EFFECT: compounds are used to treat cancer.24 cl, 4 tbl, 47 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
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

Solid forms of gyrase inhibitor (r)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl) pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1h-benzimidazol-2-yl] urea // 2625305
FIELD: chemistry.SUBSTANCE: compounds can be used for controlling, treating or reducing the progression, severity or effects of nosocomial or non-nosocomial bacterial infection. Compound solid forms of formula (I), represent a crystalline Form I or amorphous Form III. Crystalline Form I is characterized by X-ray powder diffractogram (XRPD), comprising at least three positions of closely located peaks (2θ±0.2 in degrees) when measured using Cu Kα radiation, selected from the group consisting of 9.3, 11.7, 12.1, 12.4, 14.5, 15.9, 16.3, 16.6, 18.5, 19.4, 21.5 22.3, 22.8, 23.8, 24.5, 25.7, 28.1, 28.4, 30.3 and 33.4 in the case when XRPD is collected in the angular range of two-theta (2θ) from about 5 to about 38 degrees. The amorphous form III is characterized by X-ray powder diffraction (XRPD), obtained using Cu Kα radiation, which has a diffuse halogen peak in the absence of a clearly distinguishable diffraction peak. A method for producing crystalline Form I comprises suspending of the free base solid material in a solvent system containing alcohol and ether, and extraction of the solid material. A process for producing amorphous Form III comprises lyophilization, spray drying, drum drying or impulse conversion drying of the compound 6-fluoro-benzimidazolyl-urea solution.EFFECT: improved properties of compounds.13 cl, 10 dwg, 9 tbl, 2 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

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

Derivatives of sitaxenthan // 2622386
FIELD: pharmacology.SUBSTANCE: invention relates to N-(4-chloro-3-methyl-1.2-oxazol-5-yl)-2-[2-(6-methyl-1.3-dihydro-2-benzofuran-5-yl)acetyl]thiophene-3-sulfonamide or a pharmacologically acceptable salt thereof. The compound of the invention is intended as an endothelin receptor antagonist or therapeutic or prophylactic agent for the treatment of pulmonary arterial hypertension.EFFECT: compound that maintains the main therapeutic effect of sitaxentan and has an improved CYP inhibitory effect.3 cl, 4 tbl, 3 dwg, 3 ex
Heterocyclic derivatives as receptors associated with tracer amines (taars) // 2621050
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula and to pharmaceutical compositions based thereof.EFFECT: new compounds are obtained with an affinity for the receptors to TAAR1 and can be used to treat depression, anxiety disorders, bipolar disorder, attention deficit/hyperactivity disorder, disorders caused by stress, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, malnutrition, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, temperature homeostasis disorders, sleep disturbance, circadian dysregulation and cardiovascular disorders.23 cl, 16 dwg, 1 tbl, 55 ex

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
Phenylpyrrole derivative // 2618228
FIELD: pharmacy.SUBSTANCE: invention relates to new derivatives of formula (I) Q: (A) or (B) phenylpyrrole, or pharmaceutically acceptable salts thereof, which are useful for prevention or treatment of diseases such as dementia, Alzheimer's disease, attention deficit, hyperactivity disorder, schizophrenia, epilepsy, "central" cramp, obesity, diabetes, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behavior-induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm, parasomnia, sleep-related traffic violation, insomnia and depression, or allergic rhinitis.EFFECT: increased compound application effeciency.13 cl, 3 tbl, 10 ex
New oxazolidinone derivative and pharmaceutical composition that includes it // 2617408
FIELD: chemistry.SUBSTANCE: invention relates to oxazolidinone derivative represented by the formula (1): wherein R is a heterocyclic group selected from the following groups represented by the formula (1a): (1а), R1 is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl; R2 is hydrogen, C1-C6-alkyl, -CH2-CH = CH2, -CH2-FROMCH,≡ -C(O)CH(OH)CH2OH, -CH2-C(O)OC2H5, -CH2CH2OH, -CH2C(O)OH, -CH2C(O)OC(CH3)3, -C(O)CH2OH, -C(O)CH2OC (O)CH3, or (CH2)mC(=O)R21, where R21 is hydrogen, (CH2)nNHR211, where R211 is hydrogen or C1-C6 alkyl, or CH(OH)CH2OH, and m and n, each independently represent an integer from 0 to 3; and Q is OR3, NHR3 or 1,2,3-triazole, where R3 is hydrogen, C1-C6-alkyl, -C(=O)R31 or a heteroaromatic cyclic group selected from isoxazol-3-yl or isoxazol-5-yl, R31 is hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl or O-(C1-C6) alkyl. The invention also relates to oxazolidinone prodrug represented by a compound selected from compounds of formulas (5)-(7) wherein Q is the same substituents as specified for the compounds of formula (1), and M+ represents an alkali metal ion such as Na or K Or an ammonium ion. Compounds of the invention also relate to specific oxazolidinone derivatives listed in the claims. Compounds of the invention are intended for manufacture of a pharmaceutical composition for antibiotic comprising (a) a therapeutically effective amount of oxazolidinone and (b) a pharmaceutically acceptable carrier, diluent, excipient or combination thereof.EFFECT: oxazolidinone derivatives with antibiotic activity.6 cl, 1 tbl, 113 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

Polymorph form of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2h-pyran-4-carboxylic acid // 2616978
FIELD: chemistry.SUBSTANCE: invention relates to a polymorphic form I 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid, which is characterised by powder diffraction pattern, produced by X-ray phase analysis (XPA) when exposed to radiation of Cu-Kα, comprising following main peaks 2θ(°): 5.9, 9.3, 9.8, 11.9, 13.7, 14.3, 15.0, 17.8, 18.2–19.3, 19.7, 22.6, 23.4–24.5 and 24.9 +/-0.2. Polymorphic form I is obtained by recrystallisation 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid from ethyl acetate for 24 hours at 40 °C and 5 days at room temperature. Polymorphic form I is intended for preparing a pharmaceutical composition or for use as a medicinal agent, having antagonistic activity on 5-HT4 receptor.EFFECT: polymorphic form 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid, having improved characteristics of stability and hygroscopicity.7 cl, 1 tbl, 5 dwg, 6 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
Selective protein kinase inhibitors // 2612972
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, where R1 is hydrogen or (C1-C10)alkyl group; R2 is H, halogen, COOH, (C1-C6)alkyl, optionally substituted with -NR10R11, OH or (C1-C4)alkoxy, optionally substituted OH; (C1-C6)alkoxy, optionally substituted OH, (C1-C4)alkoxy or group -NR12R13; group of -OR14, where R14 denotes a 5- or 6-member heterocycloalkyl, containing 1 or 2 nitrogen atoms; group -CONR15R16, where R15 and R16 each independently denotes H or (C1-C4)alkyl, optionally substituted (C1-C4)alkoxy or 5- or 6-member heterocycloalkyl, containing 1 or 2 heteroatoms selected from O and N; group -NR17R18, where R17 denotes H or (C1-C4)alkyl and R18 denotes H, (C1-C4)alkyl, optionally substituted with (C1-C4)alkoxy, or 5- or 6-member heteroaryl containing 1–3 heteroatoms selected from O, S and N; group -NR19COR20, where R19 denotes H and R20 denotes (C1-C4)alkyl, optionally substituted amino, (C1-C4)alkylamino or di(C1-C4)alkylamino or 5- or 6-member heterocycloalkyl, containing 1 or 2 nitrogen atoms, said heterocycloalkyl is optionally substituted with 1–3 (C1-C4)alkyls; or 5- or 6-member heterocycloalkyl or heteroaryl containing 1 or 2 nitrogen atoms, said heterocycloalkyl or heteroaryl is optionally substituted with oxo groups; R3 is hydrogen, halogen, cyano, (C1-C10)alkyl group or (C1-C10)alkoxy group, CF3; Q denotes O or S; W is N or CR21; X is N or CR25, where R25 is H; CN; (C1-C4)alkyl; or group -COO(C1-C4)alkyl; and A denotes a 5- or 6-member heterocycloalkyl or heteroaryl containing 1–3 nitrogen atoms, said heterocycloalkyl or heteroaryl is optionally substituted with 1–3 substitutes, selected from an oxo group; halogen; (C1-C4)alkyl, optionally substituted amino, (C1-C4)alkylamino, di(C1-C4)alkylamino or 5- or 6-member heterocycloalkyl, containing 1 or 2 nitrogen atoms. Invention also relates to a pharmaceutical composition for treating a disease mediated by inhibition of native and/or mutant c-kit, containing a compound of formula I or its pharmaceutically acceptable salt and at least one pharmaceutically acceptable carrier.EFFECT: selective inhibitors of native and/or mutant protein kinase c-kit.10 cl, 3 tbl, 225 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
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
(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
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

Pyrazine derivatives used as atr kinase inhibitors // 2604066
FIELD: chemistry.SUBSTANCE: present invention relates to pyrazine compounds , used as inhibitors of ATR protein kinase, pharmaceutical compositions containing compounds according to invention, and use of compounds according to present invention to increase cell sensitivity to DNA damaging agents and as a radio-sensitiser and a chemo-sensitiser.EFFECT: high sensitivity of cells to DNA damaging agents, radio-sensitiser and chemo-sensitiser.115 cl, 98 dwg, 18 tbl, 77 ex

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

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

Chromenone compounds as pi3-kinase inhibitors for treating cancer // 2598028
FIELD: pharmaceutics.SUBSTANCE: invention relates to chrome neon compounds with formula I possessing properties of PI3-kinase enzymes inhibitor or its pharmaceutically acceptable salts, pharmaceutical compositions based on them. In general formula I R1 represents C1-4alkyl, possibly substituted hydroxy; R2 represents C1-4alkyl; or R1 and R2 form together 4-6-member nitrogen-containing heterocyclic ring system which optionally contains 1 additional heteroatom selected from oxygen and sulphur, where sulphur ring atom is optionally oxidated with formation of S-oxide(-s), where said ring is possibly substituted with hydroxy; R3 and R5 are independently selected from H, halogen, C1-3alkoxy and cyano; R4 represents H or fluorine; n equals to 0 or 1.EFFECT: prevention and treatment of tumours sensitive to inhibition of PI3-kinase enzymes.15 cl, 4 dwg, 3 ex, 1 tbl

5-ht4 receptor agonist as prokinetic agent // 2597766
FIELD: veterinary science.SUBSTANCE: disclosed group of inventions is intended for stimulating antral (upper portions) and colonic (lower portions) motility of an animal suffering from gastrointestinal diseases. Disclosed is use of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]-oxy}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid or a pharmaceutically acceptable salt thereof for preparing a medicinal agent for stimulating antral (upper portions) and colonic (lower portions) motility of an animal, including a mammal suffering from gastrointestinal diseases. Disclosed is a pharmaceutical composition for stimulating antral (upper portions) and colonic (lower portions) motility of an animal, including a mammal suffering from gastrointestinal diseases, which contains a therapeutically effective amount of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]-oxy}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid or a pharmaceutically acceptable salt thereof. Disclosed is a method for stimulating antral (upper portions) and colonic (lower portions) motility of an animal, including a mammal suffering from gastrointestinal diseases, which comprises administering to an animal, including a mammal, 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]-oxy}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid or a pharmaceutically acceptable salt thereof.EFFECT: use of disclosed group of inventions is highly effective for stimulating antral (upper portions) and colonic (lower portions) motility of an animal, including a mammal suffering from gastrointestinal diseases.12 cl, 5 dwg, 1 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

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

Inhibitors of type erbb inhibitors // 2592703
FIELD: chemistry. SUBSTANCE: invention relates to novel compounds of formula 10 and method for production thereof. Compounds possess properties of receptor tyrosine kinase type I inhibitors and can be used in treating hyperproliferative disorders. Invention also relates to novel intermediate compounds of formula 8 and 9 and to method of producing compounds 9. Compounds 10 and 8 correspond to common formulas (8) (10), where each R6, R8 and R8a are independently hydrogen or C1-C6alkyl, where said alkyl is optionally substituted OR15; or R8 and R8a together with atom to which they are connected, three-six-Member carbocyclic ring is formed; and R15 is hydrogen or C1-C6alkyl. Connection 9 corresponds to general formula (9), where A represents O; E represents , where X is CH; D1, D2 and D3 independently represent N or CR19; D4 and D5 are independently N or CR19 and D6 represents O, S or NR20, at least one of D4 and D5 is not CR19; D7, D8, D9 and D10 represent independently N or CR19, wherein at least one of D7, D8, D9 and D10 represents N; R1 represents H or C1-C6alkyl; each R2 independently represents halogen, cyano, trifluoromethyl, difluoromethyl, ftormetil or C1-C6alkyl; each R6, R8 and R8a are independently hydrogen or C1-C6alkyl, where said alkyl is optionally substituted by OR15, or R8 and R8a together with atom, to which they are bonded, 3-6-member carbocyclic ring is formed; R15 represents H or C1-C6alkyl; each R19 independently represents H, halogen or C1-C6alkyl; each R20 is independently hydrogen or C1-C4alkyl, j is 0 and n represents 0, 1 or 2. EFFECT: method of preparing compound of formula 10 involves condensation of compound of formula 8 with compound of formula 2 (2) in presence of acid in acceptable solvent, followed by thiourea of formula 9 cyclization, preferably in water solution of NaOH in tetrahydrofuran with addition of thozilchloride TsCl. 9 cl, 1 tbl, 281 ex

Oxazolyl-methylether derivatives as alx receptor agonists // 2588567
FIELD: medicine; pharmaceuticals.SUBSTANCE: invention relates to compound of formula (I) or its pharmaceutically acceptable salt thereof, in which R1 denotes phenyl, which is unsubstituted or mono-substituted halogen, (C1-C4)alkyl, (C1-C4)alkoxy group, (C1-C2)fluoroalkyl or (C1-C2)fluoralkoxygroup; R2 denotes hydrogen, methyl or cyclopropyl; R3 and R4 are identical and mean hydrogen or methyl; and R5 denotes (C1-C2)alkyl. Invention also relates to pharmaceutical composition having ALX receptor agonist activity and containing as active substance compound of formula (I) or its pharmaceutically acceptable salt in pharmaceutically active amount and at least one therapeutically inert filler. Compound of formula (I) or its pharmaceutically acceptable salt thereof are used for preventing or treating disease selected from rheumatoid arthritis, acute pulmonary injury, asthma, cystic fibrosis, inflammatory bowel disease, dry keratoconjunctivitis, sepsis, retroviral infections mediated HIV, cardiovascular disorders, atopic dermatitis, pulmonary fibrosis and Alzheimer's disease.EFFECT: oxasolilmethyl ester derivatives of formula (I) for use as medicinal agent for preventing or treating disease responding to ALX receptor activation.18 cl, 4 tbl, 15 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

Diaminopyrimidine derivatives and methods for production thereof // 2587981
FIELD: pharmaceutics.SUBSTANCE: present invention relates to a novel compound of diaminopirimidine formula 1 or its pharmaceutically acceptable salts possessing the properties of 5-HT4 receptors agonist. In formula 1 (Formula 1)R1 denotes a phenyl group substituted with one or more substitutes selected from a group consisting of hydroxy, amino, halogen, cyano, nitro, C1-2alkyl (where C1-2alkyl optionally substituted with halogen), C1-5alkoxy,C1-5alkylthio, C1-5alkoxycarbonyl and aminokarbonil, or heteroaryl group selected from a group consisting of furanyl, pyrrolyl, tiofenil, hinolinil, hromenonil, indolil, benzimidazole-4-yl, benzimidazole-5-yl, benzimidazole-6-yl, benzimidazole-7-yl and indazolil, herewith the heteroaryl group can be optionally substituted with one or more substitutes selected from a group consisting of C1-5alkyl (where C1-5alkyl optionally substituted with halogen) and C1-5alkoxy, R2 denotes a nitrogen-containing cyclic group selected from a group consisting of the following formulae from A to D (where * symbol in A-D formulae denotes the position of this group attachment to a compound of formula (1))R3 denotes C1-5alkyl group, optionally substituted by phenyl, R4 denotes hydrogen, C1-5alkyl group optionally substituted with a substitute selected from a group consisting of hydroxy, C1-5alkylamino, pyrrolidinyl and hydroxy-C-1-5alkylamino; C1-5alkoxycarbonyl group or amin-carbonyl group, R5 denotes hydrogen, hydroxyl group; C1-5alkoxy group; C1-5alkyl group, optionally substituted with a substitute selected from a group consisting of amino and C1-5alkoksikarbonilamino; or group selected from a group consisting of the following formulae of E to I (where * symbol in E-I formulae is the position of this group attachment to one of the of A-D formula compounds),R6 means hydrogen, hydroxyl group or C1-5alkyl group optionally substituted with hydroxy, X denotes -CH(R7)-, -C(=O)-, -N(R8)- or -O-, R7 means hydrogen; hydroxyl group; amino-carbonyl group; phenyl group or C1-5alkyl group optionally substituted with hydroxy, R4 and R5, R5 and R6, R4 and R6 or R5 and R7 may be interconnected while forming 5- or 6-element ring; the said ring may be carbocyclic or additionally contain an oxygen atom as a heteroatom, R8 denotes hydrogen or C1-5alkyl group. Values of R9-R12 radicals are given in the patent claim.EFFECT: invention relates to the use of formula 1 or its pharmaceutically acceptable salt for preparing a drug in order to prevent or treat gastrointestinal motility dysfunction; Gastrointestinal motor dysfunction is gastroesophageal reflux disease (GERD), a lock (constipation), an irritable bowel syndrome (IBS), dyspepsia, postoperative intestinal obstruction, prolonged gastric emptying, gastroparesis, intestinal pseudo-obstruction, content transit deceleration over the colon induced by medicines or diabetic gastroparesis.8 cl, 38 tbl, 355 ex

Dihydrooxazole-2-amine derivatives // 2587512
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I), in which R1 is hydrogen or lower alkyl; R2 represents hydrogen or represents heteroaryl, selected from a pyridinyl, containing as a substitute cyano group; R3 represents hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy group, lower alkoxy group, substituted with halogen, cyano group, S-lower alkyl, S(O)-lower alkyl, S(O)2-lower alkyl, C(O)-lower alkyl or C3-6-cycloalkyl; R4 is hydrogen or lower alkyl; 6-member aromatic ring, possibly containing (N), is a phenyl or pyridinyl, in which N atom can be in different positions; X is a bond or -CH(CF3)-; Ar denotes aryl or heteroaryl, selected from phenyl, naphthyl, quinolinyl, pyridinyl, pyrimidinyl, pyrazinyl, possibly containing one or more as a substitute R3. Invention also relates to a pharmaceutical composition having high affinity for trace amine receptors (TAAR1), containing as an active ingredient a compound of formula (I) and a pharmaceutically acceptable carrier.EFFECT: dihydrooxazole-2-amine derivatives, having high affinity for trace amine receptors (TAAR1), used as therapeutically active substance.14 cl, 1 tbl, 75 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

Synthesis and anticancer activity of derivatives of aryl and heteroaryl quinolines // 2584688
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I and pharmaceutically acceptable salts thereof , where R is hydrogen, RO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2; W represents 2-halogenphenyl, 3-halogenphenyl or 4-halogenphenyl; R5 is (C1-C6)alkoxy, hydroxyl or OR8; R6 is hydroxyl or (C1-C6)alkoxy; R7 represents hydrogen, hydroxyl or O-(C1-C6)alcylenphenyl; R8 represents a RO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2, and m is monovalent metal ion; or where R is hydrogen, RO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2; W represents 2-halogenphenyl, 3-halogenphenyl or 4-halogenphenyl; R5 represents hydrogen, (C1-C6)alkoxy, hydroxyl or OR8; R6 is (C1-C6)alkoxy; R7 is hydroxyl or O-(C1-C6)alcylenphenyl; R8 represents PO(OH)2, P(=O)(O-(C1-C6)alcylenphenyl)2 or P(=O)(OM)2, and m is monovalent metal ion. Disclosed compounds have anti-cancer activity. Invention also relates to compounds of formula I, radicals of which are presented in patent claim and to using pharmaceutical composition containing effective amount of compound of invention for treating cancer.EFFECT: technical outcome is new compounds possessing anticancer activity.17 cl, 23 dwg, 7 tbl, 4 ex
Heteroarylsulphonamide derivatives, production and use thereof for human treatment // 2582995
FIELD: chemistry.SUBSTANCE: invention relates to geteroarilsulfonamide derivatives of formula I, where R1 is a substituent of the phenyl nucleus X selected from the group consisting of: hydrogen, F, Cl, Br, trifluoromethyl, trifluoromethoxy group, a linear or branched C1-C4-alkyl, linear or branched C1-C4 alkoxy group; n is 0, 1 or 2; A is oxygen or sulfur; D is -C (=O)-, -CH2O- or -O-; B is a nitrogen atom if n = 1 or 2, and D is -C(=O) -, or B is CH, if n = 0, and Dis -CH2O-, or if n = 1, D is -O-; R2 is hydrogen, and HetAr is pyridyl or quinolyl, optionally containing a substituent which is a linear or branched C1-C4-alkyl or trifluoromethyl; or pharmaceutically acceptable salts thereof. Invention also relates to the methods for producing compounds of formula I and to the pharmaceutical composition containing a therapeutically effective amount of the compound of formula I. EFFECT: technical result is geteroarilsulfonamide derivatives of formula I, with blocking activity to Kv1,5 potassium channels.12 cl, 1 tbl, 35 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
Triazole derivatives as gaba receptor ligands // 2582337
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts. The compounds of formula (I) possess GABA A α5 receptor affinity and selectivity. In formula A represents -CH2-O- or -CH=CH-; X represents S or CH; Y represents O, NR9 or CR9, provided X represents S, then Y represents CR9, and if X represents CH, then Y represents O or NR9; each of u and v represents a single bond or double bond provided both u and v are other than double bonds, and both are other than single bonds; R1, R2 represent C1-7-alkyl, phenyl, optionally substituted halogeno, or 6-merous heteroaryl containing one ring N heteroatom; one of R1 and R2 represents C1-7-alkyl; R3 represents -C(O)NR5R6. The invention also refers to pharmaceutical compositions containing an effective amount of the compound of the invention and using the compounds for producing medicinal products.EFFECT: new compounds of formula (I) possessing GABA A α5 receptor affinity and selectivity are produced.16 cl, 1 tbl, 11 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

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
 
2550921.
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