Containing three or more hetero rings (C07D401/14)

C   Chemistry; metallurgy(312744)
C07   Organic chemistry(60703)
C07D401/14                     Containing three or more hetero rings(550)
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

N-hydroxy-benzamides for treating cancer // 2577861
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula wherein X represents -CH2-, an oxygen atom or -NR4; R1 represents a hydrogen atom or halogen atom; R2 represents a hydrogen atom or C1-C6-alkyl provided X represents -CH2- or an oxygen atom; R3 represents phenyl substituted once or twice by a halogen atom, nitro, cyano; pyridin-2-yl unsubstituted or substituted once by nitro; pyrimidin-2-yl unsubstituted or substituted once or twice by C1-C6-alkyl, trifluoromethyl, C1-C6-alkoxy, phenoxy, pyridinyl, C1-C6-alkylpyridinyl, C1-C6-alkoxypyridinyl, halogenopyridinyl, morpholinylpyridinyl, naphthyl, quinolinyl, phenyl or substituted phenyl, wherein the substituted phenyl represents phenyl substituted once or twice by C1-C6-alkyl, a halogen atom, C1-C6-dialkylamino, C1-C6-alkoxy, trifluoromethyl or phenoxy; quinazolin-2-yl substituted once by a halogen atom; phenylcarbonyl substituted once or twice by a halogen atom, trifluoromethyl, C1-C6-alkoxy or phenyl; pyridinyl alkenyl carbonyl, wherein alkenyl contains from 1 to 6 carbon atoms; pyridinyl alkoxycarbonyl, wherein alkoxy contains from 1 to 6 carbon atoms; phenylsulphonyl, wherein phenyl is substituted once or twice by a halogen atom, trifluoromethyl, trifluormethoxy, C1-C6-alkoxy; or pyridinyl sulphonyl; R4 represents a hydrogen atom or C1-C6-alkyl; or their pharmaceutically acceptable salts. The invention also refers to a pharmaceutical compositions containing the above compounds, and using the compounds of formula (I) for producing a medicinal product and for treating cancer.EFFECT: compounds of formula (I) possessing HDAC6 or HDAC8 inhibitory activity.19 cl, 2 dwg, 3 tbl, 69 ex

Novel nicotinamide derivative or its salt // 2576623
FIELD: chemistry.SUBSTANCE: invention relates to nicotinamide derivative, represented by the following formula wherein R1 represents substituent, represented by the following formula R3 represents hydrogen atom or C1-6 alkyl, C3-8 cycloalkyl, phenyl, pyridyl or thienyl groups, each of which optionally contains substituent, selected from the group of substituents α1-1; group of substituents α1-1: halogen atom and C1-6 alkyl, C3-8 cycloalkyl, C1-6 alkoxy, C1-6 alkylthio, phenyl and pyrazolyl groups, each of which optionally contains halogen atom. R4 represents hydrogen atom, C1-6 alkyl group or C3-8 cycloalkyl group, R5 represents hydroxygroup, halogen atom or C1-6 alkyl or C1-6 alkoxy group, each of which optionally contains phenyl group, n represents integer number from 0 to 2, when n has value 2, R5 can be similar or different from each other and two R5, together with carbon atom, which they are bound to, can form C3-8 cycloalkane ring, X1 represents oxygen atom or -N(R6)- (wherein R6 represents hydrogen atom or acyl group), "*" represents binding site and R2 represents pyridyl, indazolyl, phenyl, pyrazole pyridyl, benzisoxazolyl, pyrimidinyl or quinolyl group, each of which optionally contains substituent, selected from the group of substituents α2-1;group of substituentsα2-1: halogen atom and C1-6 alkyl, C3-8 cycloalkyl, C1-6 alkoxy, (di) C1-6 alkylamino, acyl, pyrazolyl, triazolyl, morpholinyl and pyrrolizyl groups, each of which optionally contains substituent, selected from the group of substituents β2-1;group of substituents β2-1: halogen atom, oxo and C1-6 alkyl and C1-6 alkoxy groups.EFFECT: compounds possess excellent Syk-inhibiting activity.19 cl, 8 tbl

Compounds, compositions and methods suitable for cholesterol mobilisation // 2576402
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to a novel heterocyclic compound of general formula (II) or to a pharmaceutically acceptable salt, where each R9 is -H; each R10 is independently -H, -OH, NH(methyl), -N(methyl)(methyl) or -O-methyl; each of Q1, Q2 and Q3 is independently CR10 or N; X is CHR10 or O; and each m is 1. The invention also relates to a pharmaceutical composition based on a compound of formula (II), a treatment method based on the use of a compound of formula (II), and a method of determining the level of activity of P2Y13 in a subject, based on the use of a compound of formula (II).EFFECT: obtaining novel compounds having agonistic activity with respect to the P2Y13 receptor.18 cl, 28 dwg, 4 tbl, 20 ex

Compounds for treating clostridium difficile associated diseases // 2575477
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to organic chemistry, namely to a bibenzoimidazol derivative of general formula wherein R1 is pyridyl; R2 represents an aromatic 9-merous bicyclic ring system, wherein one or two carbon atoms can be substituted by N, O, or S; or to its pharmaceutically acceptable salt, hydrate or solvate. The invention also refers to a combination based on the compound of formula (I) and an additional specified agent, a pharmaceutical composition based on the compound of formula (I), a method of treating Clostridium difficile infection and a method of eliminating Clostridium difficile bacterium.EFFECT: produced are new bibenzoimidazol derivatives possessing effective biological properties.14 cl, 2 tbl, 2 ex

Aryl-substituted carboxamide derivatives as calcium or sodium channel blockers // 2575168
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to aryl-substituted carboxamide derivatives of formula (I)or their pharmaceutically acceptable salts, wherein in formula (I) R represents hydrogen; R1 is independently specified in a group consisting of: (1) hydrogen, (2) halogen, (3) hydroxyl, (4) -On-C1-6 alkyl, wherein alkyl is unsubstituted or substituted by one or more substitutes optionally specified in R7, (5) -On-heterocylic group specified in piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl and oxetanyl; n has the value of 0 or 1; when n has the value of 0, a chemical bond is present instead of On; p has the value of 1 or 2; when p is equal to two, R1 can be identical or different from each other; R2 represents C1-6 alkyl, which is unsubstituted or substituted by one or more substitutes, independently specified in R7; or R2 together with R1 forms C3-C6 cycloalkyl; X represents 1,2-C3 cycloalkylene; W, Y and Z are independently specified in nitrogen atom or carbon atom; at least one of W, Y and Z represents nitrogen, and simultaneously W, Y and Z are other than carbon; R3, R4, R5 and R6 are such as presented in the patent claim; Ar means aryl, which represents mono- or bi-carbocyclic or mono or bi-heterocyclic ring containing 0-3 heteroatoms specified in O, N and S, including phenyl, furyl, oxazolyl, thiazolyl, imidazolyl, pyridyl, piperidinyl, pyrimidinyl, isooxazolyl, triazolyl, tetrahydronaphthyl, benzofuranyl, benzothiophenyl, indolyl, benzoimidazolyl, quinolyl, isoquinolyl, quinoxalinyl, pyrazolo [1,5-a] pyridyl, thieno [3,2-b] pyrrolyl, wherein aryl is optionally substituted by 1-3 substitutes specified in the patent claim. Also the invention refers to compounds of formula (II)and their aryl-substituted carboxamide derivatives specified in cl. 3 of the patent claim, a pharmaceutical composition, a method of treating and using.EFFECT: aryl-substituted carboxamide derivatives exhibiting blocking activity on T-type calcium channels or voltage-dependent channels.10 cl, 6 tbl, 464 ex

New amide derivatives and using them as medicinal product // 2574409
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to an amide derivative of formula (I)exhibiting the property of inhibiting proMMP-9 production, as well as to a based pharmaceutical composition and medicinal product on it's base and an agent for inhibiting MMP-9 production. In general formula (I), A represents phenylene or 6-merous heteroarylene presented by the following formula R1 represents C1-C6alkyl or C3-C6cycloalkyl; R2 represents aC1-C6alkyl optionally substituted by a halogen atom, or C3-C6cycloalkyl; R3 represents a hydrogen atom or C1-C6alkyl; each R4a, R4b and R4c represents a hydrogen atom; W represents a bond, C1-C6alkylene or C3-C6cycloalkyldiene; X represents a nitrogen atom (if Y represents a bond, The nitrogen atom can be oxidised to form N-oxide); Y represents a bond; m is equal to 1 or 2; Z1 represents a carbon atom or a nitrogen atom, each Z2 and Z3 represents a carbon atom; Ra and Rb together with an adjacent atom form a nitrogen-containing cyclic group presented below: , or , which is optionally substituted by C1-C6alkyl optionally substituted by a hydroxyl group or C1-C6alkoxy or oxo.EFFECT: producing new amide derivatives.12 cl, 5 tbl, 843 ex

N,n-substituted 3-aminopyrrolidine compounds effective as monoamine reuptake inhibitors // 2574406
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to versions of a serotonin and/or norepinephrine and/or dopamine reuptake inhibitor applicable for treating disorders caused by reduced serotonin, norepinephrine, or dopamine neurotransmission and containing as an active ingredient a pyrrolidine derivative of general formula (1) or its pharmaceutically acceptable salt, wherein R101 and R102 have the values specified in the patent claim.EFFECT: invention refers to methods of treating various disorders and disturbances involving the declared inhibitors administered.8 cl, 162 tbl, 1478 ex

Pharmaceutically active compounds as axl inhibitors // 2573834
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound of structural formula (I) possessing inhibitory activity on the TAM family of receptor tyrosine kinases (RTKs). In formula (I) A represents C-R10; B represents C-R11, N; R1, R4 are independently specified in -H, -F, -Cl, -Br, -I, -OH, -NH2, -OCH3, -OC2H5, -OC3H7, -OCH(CH3)2, -NO2, -CHO, -COCH3, -COC2H5, -COC3H7, -O-cyclo-C3H5, -OCH2-cyclo-C3H5, -O-C2H4-cyclo-C3H5, -OCF3, -OC2F5, -CH2F, -CHF2, -CF3, -CH2Cl, -CH2Br, -CH2I, -CH2-CH2F, -CH2-CHF2, -CH2-CF3, -CH2-CH2Cl, -CH2-CH2Br, -CH2-CH2I, cyclo-C3H5, -CH2-cyclo-C3H5, -CH3, -C2H5, -C3H7, -CH(CH3)2, -C4H9, -CH2-CH(CH3)2, -CH(CH3)-C2H5, -C(CH3)3, -CH=CH2, -CH2-CH=CH2, -C(CH3)=CH2, -CH=CH-CH3; R2 are R3 are independently specified in -O-R18, -O-CR73R74-R18, -O-CR73R74-CR75R76-R18, -O-CR73R74-CR75R76-CR77R78-R18, -O-CR73R74-CR75R76-CR77R78-CR79R80-R18; R5 and R6 represent -H; R7, R8, which can be identical or different from each other, represent -H, -F, -Cl, -Br, -I, -CN, -NO2, -CH3, -C2H5, -C3H7, -CH(CH3)2, cyclo-C3H5, -CH2-cyclo-C3H5, -OCH3; R9 represents -H. The radical values D, R10, R11, R18, R73-R80 are presented in the patent claim. The invention also refers to a pharmaceutical composition containing the above compound.EFFECT: producing the compounds possessing the inhibitory activity on the TAM family of receptor tyrosine kinases (RTKs).14 cl, 3 tbl, 106 ex

Aminoalkylpyrimidine derivatives as histamine h4 receptor antagonists // 2573828
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new aminoalkylpyrimidine derivatives of formula (I) or their pharmaceutically acceptable salts exhibiting the properties of histamine H4 receptor antagonists. The compounds are applicable in respiratory diseases, including asthma, allergic rhinitis, chronic obstructive pulmonary disease (COPD); ophthalmic diseases, including conjunctivitis, dry eye syndrome, cataract; dermatological diseases, including eczema, dermatitis (e.g., atopic dermatitis), psoriasis, urticaria, pemphigus, dermatitis herpetiformis, cutaneous vasculitis, itch; inflammatory intestinal diseases, including nonspecific ulcerative colitis, Crohn's disease; and autoimmune diseases, including rheumatoid arthritis, multiple sclerosis, cutaneous lupus, systemic lupus erythematosus, widespread vasculitis and graft rejection. In formula IR1 and R2 form together with N atom to which they are bound, a saturated heterocyclic group containing one nitrogen atom and free frpm any other heteroatoms; the above heterocyclic group is substituted by one -NRaRb group and optionally substituted by one or more C1-4alkyl groups; wherein the heterocyclic group represents a 4-7-merous monocyclic group; Ra represents H or C1-4alkyl; Rb represents H or C1-4alkyl; R3 represents H or C1-8alkyl; R4 represents a) C1-8alkyl optionally substituted by one or more halogens; b) C3-10cycloalkyl-C0-4alkyl; c) aryl-C0-4alkyl or d) 5-6-merous heteroaryl-C0-4alkyl, wherein the radicals b), c) or d) may be substituted as specified in the patent claim; n equals to 1 or 2; each R5 independently represents H or C1-8alkyl.EFFECT: compounds can find application in treating or preventing an allergic, immune system or inflammatory disease, pain or cancer.22 cl, 18 ex

Isoindolinone-based phosphatidylinositol-3-kinase inhibitors // 2573569
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to pharmaceutically acceptable compositions containing the above compounds, and to methods for using the compositions for treating various diseases, conditions or disorders.EFFECT: invention refers to the compounds applicable as PI3K, particularly PI3Kγ inhibitors.18 cl, 2 tbl, 26 ex

Arylethinyl derivatives // 2573560
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a new ethinyl derivative of formula I in the form of a racemic mixture or respective enanthiomer and/or optic isomer and/or stereoisomer or to a pharmaceutically acceptable salt of the above compounds formed by acid addition. The compounds are allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5) and can find application in treating diseases mediated by mGluR5 action, wherein a disease is schizophrenia, cognitive disorders, fragile X syndrome or autism. In formula I , U is N or C(R5); V is CH or N; W is CH or N; provided only one of the groups U, V or W is a nitrogen atom, R5 is hydrogen, methyl or halogen; Y is -N(R6)-, -O-, -C(R7')(R7)-, -CH2O- or -CH2S(O)2-; R6 is hydrogen or lower alkyl, whereas R7/R7' independently represent hydrogen, hydroxy group, lower alkyl or lower alkoxy group; R1 is phenyl or 5-6-merous heteroaryl containing 1-2 heteroatoms specified in nitrogen atoms, which can contain one or two substitutes specified in halogen or lower alkyl; R2/R2' independently represent hydrogen, lower alkyl, hydroxy group, lower alkoxy group, C3-C6-cycloalkyl, CH2-lower alkoxy group, or together with a carbon atom, to which they are attached, can form C3-C6-cycloalkyl, or a ring containing -CH2OCH2-; m is equal to 0, 1 or 2; if m is equal to 1, R3/R3' independently represent hydrogen, lower alkyl, CH2-lower alkoxy group, or together with a carbon atom, to which they are attached, can form C3-C6-cycloalkyl; or R3 and R2 together with a carbon atom, to which they are attached, can form C3-6-cycloalkyl or a ring containing -(CH2)2OCH2-; n is equal to 0 or 1; if n is equal to 1, R4/R4' independently represent hydrogen, lower alkyl, CH2-lower alkoxy group or together with a carbon atom, to which they are attached, can form C3-C6-cycloalkyl; R4 and R2 together with a carbon atom, to which they are attached, can form C3-6-cycloalkyl; or if n is equal to 0, and Y is -N(R6)-, then R6 and R2 together with a carbon atom and a nitrogen atom, to which they are attached, can form C3-6-cycloalkyl; if n and m are equal to 0, then R2 and R7 with a carbon atom, to which they are attached, can form C3-6-cycloalkyl.EFFECT: producing the compounds mediated by mGluR5 action.28 cl, 1 tbl, 174 ex

Inhibitors of catechol-o-methyltransferase and thereof application in treatment of psychic disorders // 2572624
FIELD: medicine, pharmaceutics.SUBSTANCE: claimed invention relates to novel compounds of 4-pyrimidinone of structural formula I and II, which possess properties of catechol-O-methyltransferase (COMT) inhibitor. Compounds can be applied in treatment and prevention of neurological, psychic disorders and diseases, which COMT fragment is involved in, such as negative and positive symptoms of schizophrenia, depression, depressive phase of bipolar disorder, diseases, associated with DA deficiency, such as ADD/ADHD, and addiction, such as opiate, drug and tobacco-addiction, as well as against growth of weight/sense of hunger, associated with cessation of smoking of use of antipsychotics. In formula and compounds A represents hydrogen or C1-6alkyl; X represents hydrogen or halogen; R1 represents phenyl or heterocyclyl, selected from 6-membered unsaturated heterocyclyl with one nitrogen atom in cycle, where said phenyl and heterocyclyl is substituted with 1-3 groups Ra; R2 represents C1-6alkyl, N(CH3)2, (CH2)nC5-10heterocyclyl, (CH2)nC6-10aryl, where said aryl and heterocyclyl is optionally substituted with 1-2 groups Ra; Ra represents halogen, C2-4alkinyl, (CH2)nCF3, CN, NHSO2R2, OR2, (CH2)nC5-10heterocyclyl, containing 1-2 nitrogen atoms and possibly additionally oxygen or sulphur atom in ring, (CH2)nC6aryl, O(CH2)nC6aryl, where said aryl represents phenyl, where said alkinyl, heterocyclyl and aryl is optionally substituted with 1-3 groups Rb; Rb represents C1-6alkyl, OC1-6alkyl, halogen, CHF2, OCHF2, -O-, (CH2)nC6aryl, (CH2)nC5heterocyclyl, containing 3 heteroatoms in cycle, selected from nitrogen and oxygen, OR2, (CH2)nCF3, where said heterocycle is optionally substituted with 1 or several C1-6alkyls; and n equals 0-1.EFFECT: invention relates to pharmaceutical composition, containing claimed invention compounds and possibly additionally containing monoamine oxidase inhibitor (MAOI), selected from moclobemide.16 cl, 1 tbl, 8 ex

Phenyloxadiazole derivatives as pgds inhibitors // 2572608
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I), where R1 is hydrogen or C1-C6alkyl; R2 is hydrogen and R3 is hydroxy(C1-C6)alkyl; or pharmaceutically acceptable salts thereof. The invention also relates to methods of producing compounds of formula (I), intermediate compounds given in paragraphs 14-19 of the claim, and a method of producing an intermediate compound according to paragraph 17 of the claim.EFFECT: obtaining compounds of formula as PGD2 synthase inhibitors and intermediate compounds for production thereof.20 cl, 3 ex

Substituted pyridine compound // 2572606
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound of general formula possessing CETP-inhibiting activity. In formula (I) R1 represents hydrogen atom, C1-C6 alkyl group, hydroxy(C1-C6alkyl) group, (C1-C6alkoxy)-(C1-C6alkyl) group, (C1-C6alkyl)amino-(C1-C6alkyl) group, [N-(C1-C6alkyl)-N-hydroxy(C1-C6 alkyl)amino]-(C1-C6alkyl) group, [N-(C1-C6alkyl)-N-(C1-C6 alkyl)sulphonylamino]-(C1-C6alkyl) group, carboxy(C1-C6alkyl) group, halogen (C1-C6alkyl) group, C2-C6alkenyl group, C3-C8cycloalkyl group, C3-C8cycloalkenyl group, hydroxyl group, C1-C6alkoxy group, hydroxy(C1-C6alkoxy) group, (C1-C6alkyl)sulphonyl-(C1-C6alkoxy) group, carboxy(C1-C6 alkoxy) group, halogen(C1-C6alkoxy) group, C1-C6 alkylthio group, C1-C6alkylsulphonyl group, N-(C1-C6alkyl)-N-hydroxy(C1-C6alkyl)aminogroup, carboxy group, (C1-C6 alkoxy)carbonyl group, (C1-C6 alkylamino)carbonyl group, di(C1-C6 alkyl)aminocarbonyl group, cyanogroup, halogen group, substituted phenyl group, in which substituent(substituents) represent 1-4 groups, independently selected from substituting group α, substituted with 5-membered aromatic heterocyclic group, containing 3 heteroatoms, selected from N and O, in which substituent (substituents) represent 1-4 groups, independently selected from substituting group α, 6-membered saturated heterocyclic group, containing 1-2 heteroatoms, selected from N, S and O, substituted 5- or 6-membered saturated heterocyclyl group, containing 1-2 heteroatoms, selected from N and S, in which substituent (substituents) represent 1-4 groups, independently selected from substituting group α, substituted 5- or 6-membered saturated heterocyclyloxy group, containing 1 heteroatom, selected from N, in which substituent (substituents) represent 1-4 groups, independently selected from substituting group α, 6-membered saturated heterocyclylcarbonyl group, containing 2 heteroatoms, selected from N and O, and substituting group α represents group, consisting of C1-C6 alkyl group, hydroxyl group, carboxy group, (C1-C6 alkoxy)carbonyl group and oxogroup.EFFECT: invention relates to pharmaceutical composition, containing said compound, to medication for increasing concentration of cholesterol of high-density lipoproteins or for reduction of concentration of cholesterol of low-density lipoproteins and to method of treating or preventing disease, mediated by CETP activity.53 cl, 2 tbl, 58 ex

N-[(1h-pyrazol-1-yl) aryl]-1h-indole or 1h-indazole-3-carboxamide derivatives, producing and using them as p2y12 antagonists // 2572593
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to compounds characterised by general formula (I), wherein A represents an aromatic diradical specified in groups having formulas such as below whereas the other radical and groups have values presented in the patent claim.EFFECT: invention refers to methods for producing the compounds of formula (I) , pharmaceutical composition containing them, and using them as P2Y12 antagonists for treating cardiovascular diseases.14 cl, 16 tbl, 21 ex

3-acylaminopyridin derivatives, applicable as serine-threonine proteinkinase gsk3b inhibitors, as medications for type ii diabetes treatment // 2570907
FIELD: chemistry.SUBSTANCE: invention relates to 3-acylaminopyridin-2(1H)-one and its novel derivatives, which can be potential medications for treatment of type II diabetes. , wherein X - -(CH2)n-n=0-2, -CH(OCH3)-, -CH=CH-; Y - 1-adamantyl, 4-isopropylphenyl,3-(methoxymethyl)-4-methoxyphenyl, 3-(4-methyl-1H-pyrazol-1-yl)methyl-4-methoxyphenyl, 4-(difluoromethoxy)phenyl, 3,5-dimethylisoxazol-4-yl, 3,5-dimethyl-4-nitro-1H-pyrazol-1-yl, 3-trifluoromethyl-1H-pyrazol-1-yl, 1-ethyl-3-trifluoromethyl-1H-pyrazol-5-yl, 1-benzyl-5-methyl-1H-1,2,3-triazol-4-yl; Z - 4 pyridyl, bromine.EFFECT: obtaining medication for treating diabetes.4 cl, 2 dwg, 3 tbl, 21 ex

New antithrombotic agent // 2570426
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula or their pharmaceutically acceptable salts, wherein Xa represents N or CH; R1e represents C1-6-alkyl optionally substituted by aryl specified in phenyl, naphthyl, fenanthryl and anthryl, or by halogen; C1-6-alkoxy optionally substituted by aryl specified in phenyl, naphthyl, fenanthryl and anthryl, by halogen or C3-8-cycloalkyl; C2-6-alkenyl; C3-8-cycloalkyl; or halogen; R1f represents hydrogen, C1-6-alkyl, C1-6-alkoxy, hydroxyl, cyano or halogen; R21 represents 5-10-merous heteroaryl, which has 1-3 heteroatoms specified in nitrogen, oxygen or sulphur, and which can be substituted by identical or different 1-3 groups specified in the patent claim; R31 represents 6-merous heteroaryl, which has 1 or 2 nitrogen atoms, and which can be substituted by identical or different 1-3 groups specified in the patent claim. The invention also refers to an antithrombotic agent and a medicinal product containing the compounds of formula IIa as an active ingredient, to a method for preventing thrombocyte aggregation, and a method for preventing or treating ischemic stroke, acute coronary syndrome, microvascular dysfunction, peripheral arterial disease, arteriosclerosis obliterans, ischemic heart disease, thrombotic microangiopathy, or unstable or stable angina.EFFECT: compounds of formula IIa exhibiting the inhibitory activity on thrombocyte aggregation.18 cl, 34 tbl, 192 ex
 
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