Linked by a carbon chain containing aromatic rings (C07D403/10)

C   Chemistry; metallurgy(318327)
C07   Organic chemistry(61593)
C07D403/10                     Linked by a carbon chain containing aromatic rings(109)
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
2-aminopyrasine derivatives as csf-1r kinase inhibitors // 2642777
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group; R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl; n is 1; X is NH; V is -N=, W is -C(Z)=; Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl; ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group; [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3; x is 0 or 1; Alk1 is an unsubstituted C1-3 alkylene group; X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3; R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring; and R17 represents a hydrogen atom; where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring; R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group; ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or prevention of diseases or disorders mediated by CSF-1R kinase, as well as application of the said compounds for preparation of a medicament useful for treatment of such diseases.EFFECT: increased application efficiency.18 cl, 59 ex

Diaryl hydantoins // 2638833
FIELD: biotechnology.SUBSTANCE: invention relates to organic chemistry, namely to a new heterocyclic compound [RD93], which may be useful for treatment of hormone-refractory prostate cancer, benign prostatic hyperplasia, breast cancer and ovarian cancer.EFFECT: new heterocyclic compound with useful biological properties is obtained.6 cl, 41 dwg, 11 tbl, 61 ex
Inhibitors of lrrk2 kinases activity // 2637936
FIELD: pharmacology.SUBSTANCE: R1, R2, R3 and R4 values are defined in the claims of this invention. Compounds of the formula (I) inhibit the LRRK2 activity. In addition, the invention relates to particular compounds as defined in claim 14. The invention also relates to a pharmaceutical composition comprising the compounds of the invention and to a method for neurodegenerative diseases treatment, for example those in which the disease is represented by α-synucleinopathy and in particular to a method for treatment of various diseases of the Parkinson's disease type, as well as a method for treatment of autoimmune diseases, such as Crohn's disease or ulcerative colitis.EFFECT: new method for neurodegenerative diseases treatment.22 cl, 10 tbl, 15 ex
New phthalazine derivatives and its production process // 2636585
FIELD: pharmacology.SUBSTANCE: invention relates to the phthalazine derivatives that are represented by the formula I ,where the radicals and symbols have the definitions indicated in the formula of the invention. The compounds of the formula I are activity inhibitors of the poly(ADP-ribose) polymerase ferment. The invention also relates to the pharmaceutical composition for cancer treatment, which comprises the compound of the formula I, to the method of cancer treatment and to the compound application for the medicinal agent for cancer treatment production.EFFECT: compound application efficiency upgrading.16 cl, 8 tbl, 176 ex

Carboxylic acids compounds // 2636146
FIELD: pharmacology.SUBSTANCE: compounds may find use in the treatment of a disease mediated by TLR7. This disease can be a cancer selected from bladder cancer, head and neck cancers, prostate cancer, breast cancer, lung cancer, uterine cancer, pancreatic cancer, liver cancer, kidney cancer, ovarian cancer, colon cancer, stomach cancer, skin cancer, brain tumour, myeloma and lymphoproliferative tumours, such a disease or condition can also be represented by asthma, COPD (chronic obstructive pulmonary disease), allergic rhinitis, allergic conjunctivitis, allergic dermatitis, hepatitis B, hepatitis C, HIV, HPV (human papillomavirus), bacterial infection, or dermatosis. In the formula ,n is equal to 0, 1 or 2; m is 1 or 2; p is 1, 2 or 3, provided that when X is oxygen, p is 2 or 3, and when X is a single bond, p is 1; X is oxygen or a single bond; R1 is chosen from C1-4 alkyl group, C1-3alkyl-(CH2)group, in which C1-3 alkyl functional group is substituted by 1, 2 or 3 fluorine atoms, and C1-4 an alkylcarbonyl group; R2 is hydrogen; or R1 and R2 together with the nitrogen and carbon atoms to which they are attached form a saturated or unsaturated 5-membered heterocyclic ring optionally containing an additional heteroatom selected from N; R3 is selected from hydrogen, hydroxymethyl and 2-hydroxyethyl. The invention also relates to a method for preparation of a compound of formula (I) and to an intermediate of formula wherein n, p, X, R1, R2 have the above values, Y is a hydroxy or substituted group selected from mesitylenesulfonyloxy, or tri(isopropyl)phenylsulfonyloxy; and PG1 is a carboxylic acid protecting group selected from C1-4 alkyl; or a salt thereof.EFFECT: compound application efficiency increase.37 cl, 13 dwg, 7 tbl, 30 ex
Aminopyridine derivatives as modulators of leucine-rich repeated kinase 2 (lrrk2) // 2634716
FIELD: pharmacology.SUBSTANCE: compounds are designed to treat a disease such as Parkinson's disease, in particular hereditary Parkinson's disease. In formula I, m is from 0 to 1; -NRa-; -O-; or -S(O)r- where r is from 0 to 2 and RA is hydrogen; R1 is C1-6-alkyl; R2 is halogen; cyano; or halo-C1-6-alkyl; R3 and R4 are independently halogen; C1-6-alkyl; C1-6-alkoxy; halo-C1-6-alkyl; or halo-C1-6-alkoxy; or R3 and R4 together with the atoms to which they are attached, can form a five- or six-membered ring which optionally includes one or two heteroatoms independently selected from O; and R5 is C1-6-alkylsulfonyl; or cyano.EFFECT: increased efficiency of treatment.17 cl, 3 tbl, 32 ex
Pyridinone and pyridazinone derivatives // 2632915
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I) or its pharmaceutically acceptable salts: , wherein J is a group of formula IIa, R1a is C1-C3alkyl; Y1a is N or CRxa, where Rxa is H, X2a is selected from the group consisting of: H, C1-C4alkyl; X1a is selected from the group consisting of: hydrogen, halogen, C1-C6alkyl, C1-C4haloalkyl,-O-C1-C4alkyl, -O-C1-C3alkylene-C3-C7cycloalkyl, -O-C1-C4haloalkyl, -O-C1-C3alkylene(5-membered heterocycloalkyl having 1 heteroatom selected from O), -O-C1-C6alkylene-N(R10)2, -O-C1-C3alkylene-C(O)OC1-C4alkyl, -C2-C4alkenylene-C(O)-O-C1-C4alkyl, -C(O)-C1-C4alkyl, C(O)O-C1-C4alkyl, C(O)NR10R12, -NR10-C1-C3alkylene-C(O)-C1-C4alkyl, -SO2NR10R12 and any of the groups: ii) 6-membered heterocycloalkenyl, which may be substituted with 1 R2; iii) 5-6 membered heterocycloalkyl with 1 to 2 heteroatoms selected from N, which may be substituted with 1-2 R3; iv) 5-6 membered heteroaryl with 1-3 heteroatoms independently selected from N, O, 9-10 membered bicyclic heteroaryl with 1 to 3 heteroatoms independently selected from N, S, which may be substituted with 1-2 R4; v) phenyl which may be substituted with 1-2 R6; X3 is LG where L is absent or is selected from the group consisting of: -O-, -O-C1-C3alkylene; and G is selected from the group consisting of: phenyl, 6-membered heteroaryl with 1 heteroatom selected from N, 9-membered bicyclic heteroaryl with 2 heteroatoms, selected from N, C3-C7cycloalkyl, 6-membered heterocycloalkyl with 1 heteroatom selected from N, O, where G may be substituted with 1-2 groups, A2 is CR18, and A1, A3 and A4 are CR19, values of the remaining substituents are indicated in the claims. The invention also relates to individual compounds, to a pharmaceutical composition and to a method for cancer treatment.EFFECT: new compounds with proliferative activity are obtained.20 cl, 6 tbl, 293 ex
Azole derivatives // 2622639
FIELD: pharmacology.SUBSTANCE: invention relates to azole derivative of formula (I) or its pharmaceutically acceptable salt, wherein R1 is hydrogen atom or C1-5alkyl; R2 is hydrogen atom or C1-5alkyl; R3 is phenyl or pyridyl (where phenyl or pyridyl is optionally substituted with one or two fragments selected from the group consisting of C1-5alkoxy, halogen and trifluoromethyl atoms); each of R4 and R5, which can be the same or different, represent hydrogen atom or C1-5alkyl (where C1-5alkyl is optionally substituted with one fragment selected from the group consisting of hydroxy and C1-5alkoxy), or R4 and R5 together with nitrogen atom joining them form 4-7-membered saturated or unsaturated heterocycle, optionally compirsing one cyclic nitrogen, oxygen or sulfur atom, aside from the mentioned above joining nitrogen atom (where 4-7-membered saturated and unsaturated heterocycle is optionally substituted with one or two fragments, selected from the group consisting of hydroxy C1-5alkyl (where C1-5 alkyl is optionally substitued with one or two hydroxyl group), C1-5alkoxy, halogen atoms, cyano, C2-5alkanoyl, aminocarbonyl, mono-C1-5alkylaminocarbonyl, di-C1-5 alkylaminocarbonyl, trifluoromethyl, amino, mono-C1-5alkylamino, di-C1-5alkylamino and C2-5alkylamino, wherein the mentioned 4-7-membered saturated or unsaturated heterocycle optionally has C1-5alkylene fragment, joining two different cyclic carbon atoms), or form 2-oxa-6-azaspiro[3.3]hept-6-yl or 7-oxa-2-azaspiro[3.5]non-2-yl; azole cycle represented by formula (α) has any structure of group (II) formula, contained in invention formula, and wherein Ry is hydrogen atom or C1-5alkyl; X1 and X2 are such that: (i) if X1 means an ordinary link or fragment -CO-, X2 means -C1-5alkylene- or -O-C1-5alkylene-; and (ii) if X1 means a fragment -CONRx1-, X2means an ordinary link; Rx1 is hydrogen atom or C1-5alkyl; and cycle A is benzol cycle, pyridine cycle (where benzol cycle is optionally substituted with one or two fragments, selected from the group consisting of halogen atoms and C1-5alkoxy), 5-6-membered saturated or partly unsaturated heterocycle, containing one or two nitrogen atoms (where 5-6-membered saturated or unsaturated heterocycle is optionally substituted with one oxo group) or C3-7cycloalkane. The invention also relates to a pharmaceutical composition having antagonistic effect against V1b arginine-vasopressin receptor, and to agent for treating or preventing mood disorders, anxiety disorders or drug addiction, comprising azole derivative of formula (I) or its pharmaceutically acceptable salt as an active agent.EFFECT: azole derivative having antagonistic effect against V1b arginine-vasopressin receptor.12 cl, 22 tbl, 361 ex

onohydrate crystal of fimasartan potassium salt, method for preparing same, and pharmacological composition comprising same // 2613555
FIELD: chemistry.SUBSTANCE: invention relates to a crystalline form a fimasartan potassium salt monohydrate, where crystalline form of a fimasartan potassium salt monohydrate is characterised by X-ray powder diffraction spectrum peaks using Cu-Kα radiation in diffraction angles with value 2θ, reduced at 6.67±0.2, 7.62±0.2, 11.03±0.2, 15.32±0.2, 16.49±0.2, 20.12±0.2, 25.65±0.2 and 27.28±0.2. Invention also relates to methods of producing a fimasartan potassium salt monohydrate and to a pharmaceutical composition.EFFECT: technical result is a novel crystalline form of a fimasartan potassium salt monohydrate, which is resistant to moisture and temperature and has same particle size of crystal.23 cl, 6 dwg, 6 tbl, 18 ex

Uracil or thymine derivatives for treating hepatitis c // 2599635
FIELD: chemistry.SUBSTANCE: invention relates to a compound of N-(6-(3-tert-butyl-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methoxyphenyl)naphthalene-2-yl)methanesulfonamide or its pharmaceutically acceptable salt for use as a medicinal agent for inhibiting replication of hepatitis C virus (HCV), as well as to a medicinal agent containing a therapeutically effective amount of the said compound or its pharmaceutically acceptable salt.EFFECT: technical result is stable indices of efficiency of treating, relieving symptoms of hepatitis C, providing partial or complete reduction of symptoms.5 cl, 46 dwg, 40 tbl, 140 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

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 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

Novel 4-amino-n-hydroxybenzamides as hdac inhibitors for treating cancer // 2591190
FIELD: pharmaceutics.SUBSTANCE: invention relates to the HDAC inhibitors of formula (I) or pharmaceutically acceptable salts, esters or stereoisomers, where R1 represents hydrogen or halogen; R2 represents hydrogen, C1-4-alkyl; R3 is phenyl, unsubstituted or substituted with one or two or three times a halogen, C1-4-alkyl, C1-4-alkoxy, C1-4-alkylsulfonyl, cyano, trifluoromethyl, phenyl, phenoxy, pirrolyl, imidazonyl, oxazolyl or di C1-4-alkylamino-C1-4-alkoxy; naphthalenyl; quinolinyl; C3-7-cycloalkyl; phenylalkyl, where phenyl may not be substituted by or once or twice substituted by halogen, C1-4-alkoxy, phenyl; naftalinilalkyl; phenylcycloalkyl; pyrimidinyl; phenylsulfonyl, where phenyl may not be substituted by or once or twice substituted by halogen, phenyl; or phenylcarbonyl, where phenyl may not be substituted by or once or twice substituted by halogen, C1-4-alkoxy; R4 is hydrogen or C1-4-alkyl; Y represents -CH2- or -C=O; or R4 and Y together with carbon atom to which R4 is connected, can form a phenyl ring or a pyridine ring, which may not be substituted with or substituted with halogen; provided that R2 is C1-4alkyl; A represents -C=O, -CH2- or -CH-alkyl, provided that a and Y simultaneously does not represent -C=O.EFFECT: presented are pharmaceutical compositions of these compounds and use thereof as drug for treating cancer.14 cl, 3 tbl, 101 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

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

Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{ 6-[4-(4-ethylpiperazin-1-yl)-phenylamino]-pyrimidin-4-yl} -1-methylurea and its fractions // 2572848
FIELD: chemistry.SUBSTANCE: invention relates to novel hydrated and anhydrous crystalline forms, as well as to amorphous form of 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{6-[4-(4-ethylpiperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methylurea of formula (I) and its monophosphoric and hydrochloride salt. Compounds possess properties of inhibitors of activity of kinase, selected from the group, including FGFR1, FGFR2, FGFR3, FGFR4, KDR, HER1, HER2, Bcr-Abl, Tie2 and Ret, and can be used in treatment of diseases, mediated by activity of said kinases. Diseases are selected from the group, including carcinoma of kidneys, liver, adrenal glands, urinary bladder, mammary gland, stomach, ovaries, large intestine, rectum, prostate, pancreas, lungs, vagina or thyroid gland; sarcoma, glioblastoma, leukaemia; tumours of head or neck; psoriasis; prostate gland hyperplasia or neoplasia In particular invention relates to anhydrous crystalline form of formula (I) compound and its monohydrate; to salt of phosphoric acid of formula (I) compound, its anhydrous crystalline forms A and B and its amorphous form; crystalline hydrochloride dehydrate. Crystalline form s are characterised by respective data of powder radiograph, indices of thermogram of differential scanning calorimetry, characteristic peaks of Raman scattering Invention also relates to method for obtaining anhydrous crystalline form A of monophosphoric acid salt.EFFECT: amorphous form of monophosphoric acid salt does not contain characteristic peaks on powder radiogram, does not demonstrate vitrification in DSC determination and has decomposition temperature 115°C, determined by TGA.34 cl, 9 dwg, 10 tbl, 21 ex

Derivatives of (4-methylsulphonylaminophenyl)-quinoline, useful in treatment of hepatitis c // 2572835
FIELD: chemistry.SUBSTANCE: invention relates to field of organic chemistry, namely to compound, selected from the group of N-{4-[7-tert-butyl-8-methoxy-5-(2-oxo-1,2-dihydro-pyridin-3-yl)-quinolin-2-yl]phenyl}-methanesulphonamide; N-{4-[7-tert-butyl-8-methoxy-5-(6-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-quinolin-2-yl]-phenyl}- methanesulphonamide; and N-{4-[7-tert-butyl-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-8-methoxy-quinolin-2-yl]-phenyl}- methanesulphonamide; or to its pharmaceutically acceptable salt. The invention also relates to application of said compound for treatment or prevention of infection with hepatitis C virus (HCV) and for manufacturing thereof based medication.EFFECT: novel compounds, possessing useful biological activity have been obtained.5 cl, 2 tbl, 6 ex

Antiretroviral compounds and use thereof // 2571662
FIELD: medicine.SUBSTANCE: invention refers to new compounds of formula (I) and their pharmaceutically acceptable salts, which inter alia inhibit hepatotropic hepatitis C virus and are applicable in treating hepatitis C virus. In formula (I) R1 is specified in a group consisting of is specified in a group consisting of a carbon-carbon single bond and carbon-carbon double bond; R5, R6, R11, R12, R13 and R14 are independently specified in a group consisting of a hydrogen atom, methyl and a protective group for nitrogen specified in C1-6alkylsulphonyl; R7 represents a hydrogen atom; R2 is specified in a group consisting of a halogen atom, C1-6alkyl and heterocyclyl specified in 5-merous heteroaryl with 1-2 heteroatoms specified in nitrogen, oxygen and sulphur, wherein alkyl is optionally substituted by one or more substitute optionally specified in a group consisting of a halogen atom; and heterocyclyl is optionally substituted by C1-3alkyl; R3 is specified in a group consisting of C1-6alkyl, C2-4alkenyl, C1-6alkyloxy and a halogen atom; L means a bond, and R4 is specified in a group consisting of C5-C6-carbocyclyl, or R4 means carbocyclyl with 2 condensed cycles specified in a group consisting of naphthalinyl, indenyl and dihydroindenyl, hexahydroindenyl, octahydroindenyl, wherein each can be substituted by a substitute specified in a group consisting of RE, RF and RJ, and RE means hydroxy, oxo; RF means C1-3alkyl substituted by C1-4alkylsulphonylamino, imino, wherein imino is substituted by a C1-4alkylsulphonylamino group; and RJ means an alkylsulphonylamino group; or L is specified in a group consisting of C(RA) = C(RB), wherein RA and RB mean a hydrogen atom, and R4 is specified in a group consisting of C6carbocyclyl specified in phenyl substituted by RJ having the above value.EFFECT: higher efficacy of the compound.16 cl, 2 tbl, 52 ex

1,2,4-triazolone derivative // 2566754
FIELD: chemistry.SUBSTANCE: invention relates to 1,2,4-triazolone derivatives and pharmaceutically acceptable salts thereof. The disclosed compounds have antagonistic activity with respect to the arginine vasopressin V1b receptor. In formula (IA): R1 is C1-5 alkyl (the C1-5 alkyl is optionally substituted with 1-3 groups selected from a group consisting of hydroxy, halogen atoms, and C3-7 cycloalkyl), C3-7 cycloalkyl or a 4-8-member saturated heterocycle, containing one heteroatom selected from an oxygen atom; R2 is a hydrogen atom; R3 is a phenyl or pyridyl (the phenyl or pyridyl is optionally substituted with 1 or 2 groups selected from a group consisting of C1-5 alkoxy, halogen atoms, cyano and C1-5 alkylsulphonyl); R4 and R5 can be identical or different, and each is a hydrogen atom or C1-5 alkyl (the C1-5 alkyl is optionally substituted with one hydroxy), or R4 and R5 optionally, together with a nitrogen atom with which they are bonded, form a 4-8-member saturated or unsaturated heterocycle, optionally containing one nitrogen, oxygen or sulphur atom, in addition to the nitrogen atom with which they are bonded, in a ring (the 4-8-member saturated or unsaturated heterocycle is optionally substituted with one or two groups selected from a group consisting of hydroxy, C1-5 alkyl ( the C1-5 alkyl is optionally substituted with one hydroxy), C1-5 alkoxy, halogen atoms, cyano, C2-5 alkanoyl, aminocarbonyl, trifluoromethyl and amino (the amino is optionally substituted with one or two groups selected from a group consisting of C1-5 alkyl and C2-5 alkanoyl), and the 4-8-member saturated heterocycle optionally has a C1-5 alkylene group which crosslinks two different carbon atoms in the ring, or form 2-oxa-6-azaspiro[3.3]hept-6-yl or 7-oxa-2-azaspiro[3.5]non-2-yl; A is phenylene, pyridinediyl or pyrimidinediyl (the phenylene, pyridinediyl and pyrimidinediyl are optionally substituted with one group selected from halogen atoms and C1-5 alkoxy); X is a single bond or -O-; Ra is a hydrogen atom or a C1-5 alkyl and n equals 0 or 1. The invention also relates to 1,2,4-triazolone derivatives, the structural formulae and values of radicals of which are given in the claim, to a pharmaceutical composition and to a therapeutic or preventive agent containing a 1,2,4-triazolone derivative or a pharmaceutically acceptable salt thereof.EFFECT: improved properties.12 cl, 16 tbl, 250 ex

ethods of producing oxazolidinones and compositions containing same // 2556234
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing compounds of formula where R1a and R1b are selected from H and F and one of R1a and R1b is F, Het is tetrazolyl, optionally substituted with methyl, R2 is selected from benzyl and C1-C6 alkyl, optionally substituted with a halogen or C1-C4 alkyloxy. The present method includes combining compounds and where X is selected from Cl, Br, I and trifluoromethanesulphonate, Y is selected from BF3 and BR3R4, R3 and R4 are selected from OH, C1-C6monoalcohols and C1-C6diatomic alcohols, or where R3 and R4 together with B, to which they are attached, form a cyclic boronate optionally substituted with methyl.EFFECT: obtaining oxazolidinones.22 cl, 10 ex, 1 tbl

Uracyl and thymine derivatives for treating hepatitis c // 2543620
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of structural formula (I), which possess the properties of HCV polymerase inhibitors. In formula , is specified in a group consisting of a single carbon-carbon bond and a double carbon-carbon bond; R1 and R3 are specified in hydrogen and methyl; R2 represents hydrogen; R5 is specified in a group consisting of hydrogen, hydroxy, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkoxy, C2-C6alkenyloxy, C3-C6alkynyloxy and halo; L represents a bond, and R6 represents a condensed 2-ring carbocyclyl, wherein each substitute is optionally substituted by one or more substitutes independently specified in a group consisting of RE, RF, RG, RH, RI, RJ and RK; or L is specified in a group consisting of a bond, C≡C, C(O)N(RC), N(RD)C(O), C1-C2-alkylene, C(H)2O, OC(H)2, cyclopropyl-1,2-ene, C(H)2N(RL), N(RM)C(H)2, C(O)CH2 and CH2C(O), and R6 is specified in a group consisting of C5-C6-carbocyclyk and 5-6-merous heterocyclyl, wherein each substitute is optionally substituted by one or more substitutes independently specified in a group consisting of RE, RF, RG, RH, RI, RJ, RK, RL and RM; the R4, RE, RF, RG, RH, RI, RJ, RK, RL and RM values are presented in the patent claim.EFFECT: invention refers to a pharmaceutical composition containing the above compounds, to using the compounds for producing a drug preparation for HCV RNA polymerase inhibition and hepatitis C treatment, and to a method for preparing the above compounds.21 cl, 46 dwg, 42 tbl, 140 ex

N-phenyl-dioxox-hydropyrimidine used as hepatitis c virus inhibitor (hcv) // 2542099
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of structural formula I, their pharmaceutically acceptable salts and crystalline forms, which possess the properties of HCV polymerase inhibitor. In formula I is specified in a group consisting of a single carbon-carbon bond and a double carbon-carbon bond; R1 represents hydrogen; R2 is specified in a group consisting of hydrogen and halo; R3 represents hydrogen; R4 is specified in a group consisting of halo, C1-C6alkyl, C1-C6alkylsulphonyl and 5-6-merous heteroaryl containing heteroatom specified in N, O and S, wherein alkyl is optionally substituted by one or more hydroxy; R5 is specified in a group consisting of hygrogen, hydroxy, C1-C6alkyloxy and halo; L is specified in a group consisting of C(RA)=C(RB), ethylene and cyclopropyl-1,2-ene; RA and RB are independently specified in a group consisting of hydrogen, C1-C6alkyl, C1-C6alkyloxy and halo; R6 represents C6aryl optionally substituted by one or more substitutes independently specified in a group consisting of RE, RF, RG, RH, RI and RJ; the substitutes RE, RF, RG, RH, RI and RJ are presented in the patent claim.EFFECT: invention refers to the pharmaceutical composition containing the above compounds, to using the compounds for inhibiting HCV RNA-polymerase and treating hepatitis C and to a method of preparing the above compounds.40 cl, 23 dwg, 7 tbl, 40 ex

Bicyclic nitrogen-containing heterocyclic compounds, useful in treatment of hepatitis c // 2540332
FIELD: chemistry.SUBSTANCE: invention relates to field of organic chemistry, namely to novel heterocyclic compounds of general formula (I) or to their pharmaceutically acceptable salts, where X1 stands for N and X2, X3 and X4 stand for CR5; or X1 and X2 stand for N and X3 and X4 stand for CR5; or X1, X2 and X4 stand for CR5, and X3 stands for N; or X1, X2, X3 and X4 stand for CR5; R1 stands for (a) heteroaryl radical, selected from the group, including pyridinyl, 2-oxo-1,2-dihydropyridin-3-yl, 2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl, said heteroaryl optionally contains as substituents halogen, C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C3-alkoxy-C1-C3-alkyl, C1-C6-alkoxygroup, or (b) heterocyclic radical, selected from the group, including 2-oxotetrahydropyrimidin-1-yl, 2,6-dioxotetrahydropyrimidin-1-yl, 2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl and 2,4-dioxotetrahydropyrimidin-1-yl; R2 stands for hydrogen or C1-C6-alkoxygroup; R3 stands for (a) phenyl, (b) pyridine, where said phenyl or said pyridine independently optionally contain 1-3 substituents, selected from the group, including halogen, (CH2)nNRcRd, or (c) NRaRb, (d) hydrogen, (e) halogen; Ra and Rb together with nitrogen atom, which they are bound to, form cyclic amine, containing from 3 to 5 carbon atoms, independently substituted with group (CH2)nNReRf; Rc and Rd independently stand for hydrogen, SO2R8, where R8 stands for C1-C6-alkyl; Re and Rf independently stand for hydrogen, SO2R8, where R8 stands for C1-C6-alkyl; R4 stands for CF3, CH2CF3 or CR4aR4bR4c, where (i) R4a, R4b and R4c are independently selected from the group, including C1-C3-alkyl, CD3; or (ii) taken together R4a and R4b form C2-C4-alkylene and R4c stands for cyanogroup or C1-C2-fluoroalkyl; R5 in each case independently stands for hydrogen, halogen, C1-C6-alkoxygroup or C1-C6-alkyl; n in each case independently equals 0-3. Invention also related to method of treating infection with hepatitis C virus, method of inhibiting HCV replication, application of formula (I) compound and based on it pharmaceutical composition.EFFECT: novel heterocyclic compounds of formula (I), possessing useful biological activity are obtained.24 cl, 3 tbl, 43 ex

Pyrimidines applicable as anti-infectious agents, and applications thereof // 2539570
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to pyrimidine derivatives of structural formula (I-L0) and their crystalline forms possessing the inhibitory activity on the hepatitis C virus (HCV) polymerase. In formula is specified in a single or double carbon-carbon bond; R1, R2 and R3 represent hydrogen; R4 is specified in halo, C1-C6alkyl, C2-C6alkinyl, amino, C1-C6alkylsulphonyl, C3-C10carbocyclyl and 5-6-merous heterocyclyl having a heteroatom specified in a group consisting of O and S, wherein amino is optionally substituted by one or two C1-C6alkylsulphonyls, and C1-C6alkyl and C2-C6alkynyl are optionally substituted by one or more substitutes optionally specified in a group consisting of halo, oxo, hydroxy, C1-C6alkyloxy and trimethylsilyl, and C3-C10carbocyclyl and 5-6-merous heterocyclyl are optionally substituted by substitutes specified in C1-C6alkyl, halo and amino, wherein amino is optionally substituted by one or two C1-C6alkylsulphonyls; R5 is specified in a group consisting of hydrogen, hydroxy, C1-C6alkyloxy and halo; R6 represents a condensed 2-ring C3-C10carbocyclyl optionally substituted by substitutes specified in RE, RF, RG, RH, RI, RJ and RK, the values of which are specified in the patent claim.EFFECT: invention refers to a pharmaceutical composition containing the above compounds, to using the compounds for producing a therapeutic agent for hepatitis C, to an intermediate compound for producing the compound of structural formula (I-L0) and to a method for preparing the above compounds and their crystalline forms.70 cl, 23 dwg, 9 tbl, 83 ex

Compound with successive aricyclic structure, possessing activity of inhibiting acycloenzyme a diacylglycerolacyltransferase (dgat1) // 2538964
FIELD: chemistry.SUBSTANCE: invention relates to heterocyclic compound of formula or to its pharmaceutically acceptable salt, where Alk represents linear C1-6 alkylene group, branched C1-6 alkylene group or C1-6 alkylene group, which has ring structure, where part of carbon atoms, constituting ring structure can be optionally substituted with oxygen atom, in ring X, X1 represents N or CRX1, X2 represents N or CRX2, X3 represents CRX3, X4 represents N or CRX4, where RX1, RX2, RX3 and RX4 each independently represents hydrogen atom; linear or branched C1-6alkyl group; linear or branched C1-6alcoxygroup; or halogen atom, in ring Y, Y1 represents CRY1, Y2 represents N or CRY2, Y3 represents N or CRY3, Y4 represents N or CRY4, RY1, RY2, RY3 and RY4 each independently represents hydrogen atom; linear or branched C1-6alkyl group, which can be substituted with halogen atom(s); C3-7alkyl group, which has ring structure; linear or branched C1-6alkoxygroup; halogen atom or cyanogroup, in ring Z, RZ represents linear or branched C1-6alkyl group, which can be substituted with halogen atom(s), or C3-7alkyl group, which has ring structure, which can be substituted with halogen atom(s). Invention also relates to particular compounds, DGAT1 inhibitor based on formula (I) compound, application of formula (I) compound, method of prevention or treatment of diseases, mediated by DGAT1 inhibition.EFFECT: obtained are novel compounds, possessing useful biological activity.19 cl, 19 tbl, 149 ex

Phenylpyrimidone derivatives, pharmaceutical compositions, methods for preparing and using them // 2522578
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to new phenylpyrimidone derivatives of formula I possessing the properties of a phosphodiesterase type 5 (PDE5) inhibitor. The compounds of formula I can be used for treating various vascular disorders, such as erectile dysfunction, pulmonary arterial hypertension, etc. In formula each R1 and R2 independently means H; C1-C10alkyl; halogen; CF3; CN; OR5; NR6R7; NHCOR8; aryl; or C1-C4alkyl optionally substituted by OR5; Z means OR3; R3 means C1-C6alkyl or C1-C3alkyl, substituted by C1-C3alkoxy group; R4 means SO2NR6R7; NR9R10, providing NR9R10 is other than NH2; COR11; OR12; or R4 means 5-6-merous heterocyclyl optionally substituted by one or more substitutes specified in a group consisting of OH and C1-C6 alkyl; or R4 means 5- or 6-merous cyclic monosaccharide group; R5 means C1-C6alkyl; C1-C4alkyl optionally substituted by C1-C4alkoxy group; each R6 and R7 independently means H, OH, C1-C6alkyl, C1-C6alkoxy group, C3-C6alkenyl, C3-C6cycloalkyl, adamantyl, C3-C8lactamyl, aryl, Het or (CH2CH2O)jH, wherein j is 1-3; or each R6 and R7 independently means C1-C6alkyl, optionally substituted by OH, C1-C4alkoxy group, SO3H, SO2NR13R14, SO2R16, NR13R14, aryl, Het or 5-6-merous heterocyclyl; or each R6 and R7 independently means 5-6-merous heterocyclyl optionally substituted by one or more substitutes specified in a group consisting of C1-C6 alkyl and C1-C6alkyl substituted by hydroxyl; or R6 and R7 together with a nitrogen atom attached whereto form 5-7-merous heterocyclyl optionally substituted by one or more substitutes specified in a group consisting of OH, COOR8, (CH2CH2O)jH, wherein j is 1-3, C1-C4alkoxy group, Het and C1-C6alkyl substituted by aryl; or R6 and R7 together with a nitrogen atom attached whereto form a glucosyl amino group, an amino acid residue, a residue of an amino acid ester or an amino amide residue. The other radical values are specified in the patent claim.EFFECT: invention refers to pharmaceutical compositions based on the above compounds, using them, methods for preparing the compounds, and intermediate products.18 cl, 2 tbl, 224 ex

ethod of producing salts of tetrazole methanesulphonic acid and novel compound used therein // 2509769
FIELD: chemistry.SUBSTANCE: present invention relates to a method of producing a salt of tetrazole methanesulphonic acid of formula (I) , which involves acylating a compound (II) with a compound (III) and then adding methanesulphonic acid. The invention also relates to an intermediate compound of formula (II) and a method for production thereof.EFFECT: method according to the present invention can cut reaction time, improve safety and enables to obtain salts of tetrazole methanesulphonic acid of high purity with high output without using a column chromatography technique.22 cl, 2 tbl, 3 ex

Novel phenylpyrazinones as kinase inhibitors // 2507202
FIELD: chemistry.SUBSTANCE: present invention relates to organic chemistry and specifically to 5-phenyl-1H-pyrazin-2-one derivatives of general formula II or pharmaceutically acceptable salts thereof, where R denotes -R1 or - R1-R2-R3; R1 denotes aryl or heteroaryl, and is optionally substituted with one or two R1'; where each R1' independently denotes C1-6alkyl, halogen or C1-6halogenalkyl; R2 denotes -C(=O), -CH2-; R3 denotes R4; where R4 denotes an amino group or heterocycloalkyl, and is optionally substituted with one or two substitutes selected from C1-6alkyl, hydroxy group, oxo group, C1-6hydroxyalkyl, C1-6alkoxy group; Q denotes CH2; Y1 denotes C1-6alkyl; Y2 denotes Y2b; where Y2b denotes C1-6alkyl, optionally substituted with one Y2b'; where Y2b' denotes a hydroxy group, n and m are equal to 0; Y4 denotes Y4c or Y4d; where Y4c denotes lower cycloalkyl, optionally substituted with halogen; and Y4d denotes an amino group, optionally substituted with one or more C1-6alkyl; where "aryl" denotes phenyl or naphthyl, "heteroaryl" denotes a monocyclic or bicyclic radical containing 5 to 9 atoms in the ring, which contains at least one aromatic ring containing 5 to 6 atoms in the ring, with one or two N or O heteroatoms, wherein the remaining atoms in the ring are carbon atoms, under the condition that the binding point of the heteroaryl radical is in the aromatic ring, "heterocycloalkyl" denotes a monovalent saturated cyclic radical consisting of one ring containing 5 to 6 atoms in the ring, with one or two ring heteroatoms selected from N, O or SO2. The invention also relates to use of the compound of formula II or a pharmaceutical composition based on the compound of formula II.EFFECT: obtaining novel compounds that are useful for modulating Btk activity and treating diseases associated with excessive activity of Btk.7 cl, 2 tbl, 53 ex

Histone deacetylase inhibitors // 2501787
FIELD: chemistry.SUBSTANCE: invention relates to compounds of general formula (I) , where is a substituted 5-member heteroaryl ring selected from thienyl, thiazolyl, oxazolyl, pyrrolyl, imidazolyl or pyrazolyl, W is selected from a group comprising N and -C=; M is selected from a group comprising -C(O)N(R1)OR2, -CXCONR1R2 and -C(O)OR1, or M is -C1-C2alkyl-C(O)N(R1)OR2, wherein is , R1 and R2 are independently selected from a group comprising -H, C1-C3-alkyl, C6-aryl, and C1-C3-alkyl-C6-aryl; R is selected from a group comprising H, C1-C3alkyl, halogen, NR1R2, -OR1 and C6aryl; n is an integer from 0 to 1; L and Y are as indicated in the claim; and to compounds of formula (II) , where L2 is selected from a group comprising H, - C0-C3alkyl- C6aryl, -C0-C3alkyl-heteroaryl, where the heteroaryl is pyridyl; -C1-C6alkyl, Y and M are the same as for compounds of formula (I). The invention also relates to a pharmaceutical composition based on compounds (I) and (II), having inhibiting action on histone deacetylase (HDAC), a method of inhibiting and a method of treating a disease which is sensitive to the HDAC inhibitor.EFFECT: compounds of formula I and II as histone deacetylase inhibitors.18 cl, 18 dwg, 10 tbl, 19 ex

Novel pyrrole inhibitors of s-nitrosoglutathione reductase as therapeutic agents // 2500668
FIELD: chemistry.SUBSTANCE: invention relates to novel pyrrole compounds of formula I or pharmaceutically acceptable salts thereof: I, where: Ar denotes phenyl, thiophenyl; R1 denotes imidazolyl, imidazolyl substituted with C1-C6alkyl, chlorine, bromine, fluorine, hydroxy group, methoxy group; R2 denotes H, CH3, Cl, F, OH, OCH3, OC2H5, propoxy group, carbamoyl, dimethylamino group, NH2, formamide group, CF3; X denotes CO and SO2. The compounds inhibit S-nitrosoglutathione reductase (GSNOR).EFFECT: using the compound to produce a pharmaceutical composition and for treating asthma.17 cl, 1 tbl, 14 dwg, 4 ex

Pyridazinone derivatives as parp inhibitors // 2490265
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula (I): . Therein the values A, R1, R2, R6, r, Rc are presented in cl.1 of the patent claim, as well as to pharmaceutically acceptable salts or tautomers of the above compound being poly(ADP-ribose)polymerase (PARP) inhibitors.EFFECT: preparing the pharmaceutically acceptable salts or tautomers of the above compound being poly(ADP-ribose)polymerase (PARP) inhibitors.

Protein kinase inhibitor (versions), use thereof for treating oncological diseases and based pharmaceutical composition // 2477723
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula and possessing the protein kinase inhibitor property, their pharmaceutically acceptable salts, solvates and hydrates, as well as to the use thereof and a based pharmaceutical composition. In general formula (1) X1 represents N, CRt 1; X2 represents N, CRt 2, X3 represents N, CRt 3, X4 represents N, CH and wherein X1, X2, X3 and X4 are independently specified; Rt 1 represents -H, halogen, -COOH, -CH3, -CH2CH3, -OH, -OCH3, -OCH2CH3, -CN, -CH3OH; Rt 2 represents -H, halogen, -CH3, -CH2CH3, -OH, -OCH3, -OCH2CH3, -CN, CH2OH, -NH2; Rt 3 represents -H, -S(O)rR4, halogen, -CN, -COOH, -CONH2, -COOCH3, -COOCH2CH3; the cycle A represents phenyl or a 6-member heteroaryl cycle, wherein heteroaryl contains 1-2 heteroatoms specified in N optionally substituted by 1-4 groups R'; the cycle B represents phenyl or a 5- or 6-member heteroaryl cycle, wherein heteroaryl contains 1-2 heteroatoms specified in N, S optionally substituted by 1-5 groups Rb; Ra and Rb are independently specified and represent -H, halogen, -CN, -R6, -OR4, -NR4R5, -C(O)YR4, -S(O)rR4, -SO2NR4R5, -NR4SO2NR4R5 wherein Y is independently specified and represents a chemical bond, -O-, -S-, -NR3-; L1 represents NR3C(O) or C(O)NR3; R3, R4 and R5 are independently specified and represent H, C1-C6-alkyl, and also the group NR4 R5 may represent a 5- or 6-member saturated or aromatic cycle; in each case R6 is independently specified and represents C1-C6-alkyl optionally substituted by C1-C6- alkyl or 5-6 merous heterocyclyl which may be substituted by C1-C6-alkyl; r is equal to 0; In general formula (II) Z represents CH; X, represents CRt 1; X2 represents CRt 2, X3 represents CRt 3 X4 represents CH and wherein X1, X2, X3 and X4 are independently specified; Rt 1 represents -H; Rt 2 represents -H, -F; Rt 3 represents -H, -F; the cycle A represents phenyl or 6-member heteroaryl cycle wherein heteroaryl contains 1-2 heteroatoms specified in N optionally substituted by 1-4 groups R3; the cycle B represents phenyl or a 5- or 6-member heteroaryl cycle wherein heteroaryl contains 1-2 heteroatoms specified in N, S optionally substituted by 1-5 groups Rb, Ra and Rb are independently specified and represent -H, halogen, -CN, -R6, -OR4, -NR4R5, -C(O)YR4, -S(O)rR4, -SO2NR4R5 wherein Y is independently specified and represents a chemical bond, -NR3-; L represents NR3C(O) or C(O)NR3; R4 and R5 are independently specified and represent H, C1-C6-alkyl, also the group NR4R3 may represent a 6-member saturated cycle; in each case R6 is independently specified and represents, C1-C6-alkyl optionally substituted by C1-C6-alkyl or 5-6 member heterocyclyl which may be substituted by C1-C6-alkyl; r is equal to 0; m is equal to 1; p is equal to 1.2.EFFECT: preparing the compounds possessing the protein kinase inhibitor property.16 cl, 5 ex

Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme // 2474576
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, where Q is phenyl or pyridinyl; A is pyrazolyl or triazolyl, where each A is independently additionally unsubstituted or substituted with 1 or 2 substitutes represented by Ra, or A is formula (a); Va is C(R4), Vb is N or C(R5) and Vc is N; or Va is N, Vb is C(R5) and Vc is N or C(R6); R4 is hydrogen, R5 is hydrogen, C1-6alkyl, -ORb, -SRb, aryl, selected from phenyl, heteroaryl, selected from thienyl, or cycloalkyl, selected from cyclopropyl; R6 is hydrogen or aryl, selected from phenyl; R7 is hydrogen or C1-6alkyl; R3 is hydrogen, C1-3alkyl, -OH, -S(O)2R1, or heteroaryl, selected from tetrazolyl, where the heteroaryl is bonded to a nitrogen atom through a ring carbon atom; Rb, Rx, Ry, Rza, Rzb, Rw, Re, Rk, Rm, Rn, Rq and R1, in each case, are independently hydrogen, C1-3alkyl or C1-3haloalkyl; and Rf, in each case, is independently hydrogen, C1-3alkyl or -OH (the rest of the substitutes assume values given in the claim). The invention also relates to a pharmaceutical composition, having inhibiting action on DGAT-1, which contains a compound of formula (I), and a treatment method.EFFECT: compounds of formula (I) as DGAT-1 inhibitors are provided.16 cl, 9 dwg, 1 tbl, 127 ex

Insecticidal aryl pyrrolidines // 2473541
FIELD: chemistry.SUBSTANCE: invention concerns novel aryl pyrrolidines of formula I: , where X, which can be identical or different, denote halogen, halogen-C1-6alkyl, NO2, C1-6alkyl, C1-6alkoxy, CN, halogen-C1-6alkoxy, C1-6alkylthio, C1-6alkylthionyl, C1-6alkylsulphonyl, halogen- C1-6alkylthio, halogen- C1-6alkylthionyl, halogen- C1-6alkylsulphonyl, OH, mercapto groups, NH2, C1-6alkylcarbonyl amino groups, halogen- C1-6alkylcarbonyl-amino, C1-6alkoxycarbonyl amino groups, halogen-C1-6alkoxycarbonylamino; Y, which can be identical or different, denote halogen, halogen- C1-6alkyl, NO2, C1-6alkyl, C1-6alkoxy, CN, halogen- C1-6alkoxy, C1-6alkylthio, C1-6alkylthionyl, C1-6alkylsulphonyl, halogen- C1-6alkylthio, halogen- C1-6alkylthionyl, halogen- C1-6alkylsulphonyl, hydroxyl groups, mercapto groups, NH2, C1-6alkylcarbonyl amino groups, halogen- C1-6alkylcarbonyl amino, C1-6alkoxycarbonyl amino groups, halogen- C1-6alkoxycarbonyl amino; R denotes halogen- C1-6alkyl; m equals 0, 1, 2, 3, 4, 5; n equals 1, 2, 3, 4; G denotes a group: , where R1 and R2 each independently denotes H, unsubstituted C1-6alkyl, halogen- C1-6alkyl, -CH2R7;R3, R4 each independently denotes H; I equals 1, 2, 3; R5 denotes H; R6 denotes C1-6alkylcarbonyl, a group: G6 - G8: b where k3 equals 0; k4 equals 0; R7 denotes an unsubstituted 6-member heteroaryl with one N; A denotes C, N.EFFECT: compounds exhibit insecticidal activity, which enables use thereof in insect and/or tick control method.7 cl, 13 tbl, 8 ex

Pyridinone pyridazinone derivatives as inhibitors of poly(adp-ribose) polymerase (parp) // 2472782
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (IX) wherein radicals and symbols have values given in the claim, and pharmaceutically acceptable salts or tautomers thereof. Said compounds are inhibitors of poly(ADP-ribose)polymerase (PARP) and can be used to treat cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitisers for cancer treatment. The invention also relates to a pharmaceutical composition containing said compounds, use of said compounds and a method of treating said diseases.EFFECT: high efficiency of using the compounds.10 cl, 18 ex

Poly(adp-riboso)polymerase inhibitors // 2455286
FIELD: medicine, pharmaceutics.SUBSTANCE: invention describes poly(ADP-riboso)polymerase inhibitors of formula (Ik) its pharmaceutically acceptable salt wherein R101, R104 and R105 represent H; R102 represents R11 wherein R11 is specified from pyrrolidinyl, oxazolyl, imidazolidinyl, isothiazolidinyl, piperidinyl, piperazinyl and azepanyl with R102 being substituted by one or two (O) substitutes; R103 represents fluorine, besides, a pharmaceutical composition on the basis of said compounds showing poly(ADP-riboso)polymerase (PARP) inhibitory activity, a method of treating cancer and a method of reducing tumour volume in a mammal.EFFECT: there are produced and described new compounds which show poly(ADP-riboso)polymerase (PARP) inhibitory activity.9 cl, 491 ex, 2 tbl

Novel pyridone derivatives, having mch antagonist activity, and medicinal agent containing said compounds // 2453543
FIELD: chemistry.SUBSTANCE: invention relates to compounds of general formula (I), , where groups and radicals R1, R2 independently denote H, C1-8-alkyl or C3-7-cycloalkyl, where the alkyl or cycloalkyl group can be mono- or poly-substituted with identical or different groups R11; or R2 denotes a -CH2- or -CH2-CH2- bridge which is bonded with a group Y, and R1 is as defined above, or denotes a group selected from C1-4-alkyl-CO-, C1-4-alkyl-O-CO-, (C1-4-alkyl)NH-CO- or (C1-4-alkyl)2N-CO-, where the alkyl groups can be mono- or polyfluorinated; or R1 and R2 form an alkylene bridge such that R1R2N- denotes a group selected from: azetidine, pyrrolidine, piperdine, azepan, 2,5-dihydro-1H-pyrrole, 1,2,3,6-tetrahydropyridine, 2,3,4,7-tetrahydro-1H-azepine, 2,3,6,7-tetrahydro-1H-azepine, piperazine, in which the free amino group is substituted with R13, piperidin-4-one, morpholine, thiomorpholine, 4-C1-4-alkoxy iminopiperidin-1-yl and 4-hydroxy iminopiperidin-1-yl. Wherein, when R1 and R2 form an alkylene bridge, one or more H atoms in the alkylene bridge can be substituted with identical or different groups R14, and X denotes a C1-3-alkylene bridge which can contain one, two or three identical or different C1-3-alkyl substitutes; and Y denotes a group of subformula selected from: and , where the group can be mono-substituted with a substitute R20; Z denotes -CH2-CH2- or -C(=O)-CH2-; U, V both denote CH, one of groups U, V denotes N, and the other of U, V denotes CH, where CH can be substituted with L; and L independently denotes halogen, cyano or C1-3-alkyl; and k equals 0, 1 or 2; W is selected from a group consisting of -CH2-O- and -O-CH2-; B is selected from a group consisting of phenyl, pyridyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, tetrazolyl, furyl, thiophenyl and thiazolyl; each of which can be mono- or poly-substituted with identical or different substitutes R20; radicals R11, R13, R14, R20 assume values given in claim 1. The invention also relates to a pharmaceutical composition containing at least one compound of formula I and having action on MCH receptor.EFFECT: disclosed pharmaceutical compositions are useful in treating metabolic disorders or eating disorders, especially obesity, bulimia, anorexia, hyperphagia and diabetes.

2,3-substituted pyrazine sulphonamides as crth2 inhibitors // 2453540
FIELD: chemistry.SUBSTANCE: invention relates to 2,3-substituted pyrazine sulphonamides of formula (I), use thereof in treating allergic diseases, inflammatory dermatosis, immonological disorders and neurodegenerative disorders, as well as pharmaceutical compositions, having CRTH2 receptor inhibiting action and inhibiting chemoattractant receptor, homologous to the molecule expressed on T-helpers 2. in general formula . A is selected from a group consisting of , n denotes an integer independently selected from 0, 1, 2, 3 or 4; m equals 1 or 2; B is selected from a group consisting of phenyl or piperazinyl; R1 denotes hydrogen; R2 denotes phenyl, where R2 is optionally substituted with one or more substitutes selected from a group consisting of halogen, cyano, (C1-C6)alkyl; R3 is selected from a group consisting of (C1-C6)alkyl, aryl, heteroaryl, (C1-C6)alkylaryl, (C1-C6)alkylheteroaryl, (C3-C8)cycloalkyl and (C3-C8)heterocycloalkyl, where each of said (C1-C6)alkyl, aryl, heteroaryl, (C1-C6)alkylaryl, (C1-C6)alkylheteroaryl, (C3-C8)cycloalkyl and (C3-C8)heterocycloalkyl is optionally substituted with one or more substitutes selected from a group consisting of halogen, cyano, (C1-C6)alkyl, (C1-C6)alkoxy, heteroaryl, aryl, thioalkoxy and thioalkyl, or where said aryl, heteroaryl, (C1-C6)alkylaryl, (C1-C6)alkylheteroaryl, (C3-C8)cycloalkyl or (C3-C8)heterocycloalkyl can be condensed with one or more aryl, heteroaryl, (C3-C8)cycloalkyl or (C3-C8)heterocycloalkyl groups and can be substituted with one or more substitutes selected from a group consisting of (C1-C6)alkyl, alkoxy, aryl, heteroaryl, carboxyl, cyano, halogen, hydroxy, amino, aminocarbonyl, nitro, sulphoxy, sulphonyl, sulphonamide and trihaloalkyl; R7 is selected from a group consisting of hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, aryl, heteroaryl, (C3-C8)cycloalkyl, (C3-C8)heterocycloalkyl, carboxyl, cyano, amino and hydroxy; aryl is selected from phenyl or naphthyl; and heteroaryl is selected from pyridyl, indolyl, 3H-indolyl, benzimidazolyl, quinolizinyl.EFFECT: high efficiency of using the compounds.4 cl, 10 dwg, 46 ex

Cyclopropylamide derivatives as n3-histamine receptor modulators // 2449989
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new cyclopropylamine derivatives of formula: or its pharmaceutically acceptable salt, wherein: one of R1 and R2 means a group of formula -L2-R6a-L3-R6b; the other of R1 and R2 means H, C1-10alkyl, C1-10alkoxy, halogen, CN; each R3, R3a R3b independently means H, C1-6alkyl, trifluoromethyl, C1-10alkoxy, CN; R4 and R5 taken together with a nitrogen atom whereto each attached form a non-aromatic cycle of formula: R7, R8, R9 and R10 each H, C1-10alkyl; R6a means cyanophenyl, phenyl, pyrazolyl, pyridazinyl, pyridinyl, pyrimidinyl, [1,2,3]triazolyl, [1,2,4]triazolyl, azepanyl, azetidinyl, azetidin-2-onyl, pyridazin-3(2H)-onyl, pyridin-2(1H)-onyl, pyrimidin-2(1H)-onyl, pyrrolidin-2-onyl, benzothiazolyl wherein the pyridinyl and pyrimidinyl groups optionally contain 1-3 substitutes specified in a group consisting of C1-10alkyl and C1-10alkoxy; R6b means H; L means - [C(R16)(R17)]k; L2 means a bond, C2-10alkylene, -O-, -C(=O)-, -NH-, -N(R16)C(=O), -C(=O)N(R16) and -N(C1-6alkyl)-;L3 means a bond; R15 means H, C1-6alkyl, C1-6alkoxycarbonyl, amido and formyl R16 , R17 in each specific case means H, C1-6alkyl; Rx and Ry in each specific case independently mean H, C1-6alkyl, C1-6alkoxy, C1-6alkylamino, fluorine, diC1-6alkylamino; k is equal to 1, 2 or 3; m is equal to 2.EFFECT: compounds show H3 receptor inhibitory activity that makes them applicable in a pharmaceutical composition.10 cl, 7 dwg, 44 ex

Substituted isoindoles as bace inhibitors and use thereof // 2446158
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new compounds of formula , wherein: R1 means phenyl, 6-member heteroaryl containing one or two atoms N as heteroatoms and wherein said phenyl, 6-member heteroaryl is optionally substituted by one R7; R2 means phenyl, 6-member heteroaryl containing one or two atoms N as heteroatoms and wherein each of said phenyl or 6-member heteroaryl is optionally substituted by one R7; R3 means halogen R7 independently means halogen, OR8, phenyl, 6-member heteroaryl containing one or two atoms N as heteroatoms wherein any phenyl or heteroaryl can be optionally substituted by one R14; R14 means halogen, OR8; R8 independently means C1-6alkyl; m is equal to 1; in the form of a free base or its pharmaceutically acceptable salt, and to their pharmaceutically acceptable salt.EFFECT: compounds possess BACE inhibitory activity.8 cl, 6 tbl, 136 ex

Substituted phenyl methanone derivatives // 2437872
FIELD: chemistry.SUBSTANCE: invention relates to novel phenyl methanone derivatives of the formula I: where R1 denote -OR1, heterocycle such as morpholinyl, pyrrolidinyl, tetrahydropyranyl, phenyl, heteoaryl such as pyrazolyl, which are not substituted or substituted with C1-6alkyl, halogen; R1 denote C1-6alkyl, C1-6alkyl substituted with halogen, or denotes a -(CH2)0-saturated C3-6cycloalkyl; R2 denotes -S(O)2-C1-6alkyl, -S(O)2NH-C1-6alkyl, NO2 or CN; R3 denotes pyridinyl, substituted with C1-6alkyl, substituted with halogen, or phenyl which is not substituted or substituted with one to three substitutes selected from a group consisting of C1-6alkyl, C1-6alkoxy, CN, NO2, halogen, C1-6alkyl, substituted with halogen, C1-6alkoxy, substituted with halogen, phenyl, sulphonamide; X denotes -CH2-, -NH-, -CH2O- or -OCH2-; n denotes 1, 2; m denotes 1, 2; o denotes 1 or 1; and pharmaceutically acceptable acid addition salt thereof.EFFECT: compounds have glycine reuptake inhibition which enables their use to prepare a pharmaceutical composition.9 cl, 2 tbl, 40 ex

Benzimidazole derivatives and use thereof in modulating gabaa-receptor complex // 2435759
FIELD: chemistry.SUBSTANCE: present invention relates to novel benzimidazole derivatives of formula any isomers thereof or any mixture of isomers thereof or a pharmaceutically acceptable salt, where R is -(CR'R")n-Rc, where Rc is C1-6-alkyl, R' is hydrogen or C1-6-alkyl, and R" is hydroxy; n equals 1; X is N; and Y, Z and W is CRd, where each Rd is hydrogen; Ro is halogen. The invention also relates to a pharmaceutical composition containing a compound of formula I, use of the compound of formula I and a GABAA-receptor complex modulating method.EFFECT: obtaining novel benzimidazole derivatives which are sensitive to GABAA-receptor complex modulation.8 cl, 1 tbl, 9 ex

Benzimidazole derivatives, synthesis methods thereof, use thereof as farnesoid x receptor (fxr) agonist and pharmaceutical preparations containing said derivatives // 2424233
FIELD: chemistry.SUBSTANCE: invention relates to novel benzimidazole derivatives of formula and pharmaceutically acceptable salts and esters thereof, where R1 denotes C1-10alkyl, lower alkoxy group-lower alkyl, lower alkoxy group-carbonyl-lower alkyl, C3-6cycloalkyl, C3-6cycloalkyl-lower alkyl, phenyl, phenyl-lower alkyl, di(phenyl)-lower alkyl, heterocyclyl, such as piperidinyl, tetrahydropyranyl, 2-oxo-pyrrolidinyl-lower alkyl, where the cycloalkyl, phenyl or heterocyclyl group is optionally substituted with 1-2 substitutes independently selected from a group comprising lower alkyl, lower alkoxy group, lower alkoxy group-carbonyl, morpholinyl, formylamino group and halogen; R2 denotes hydrogen or lower alkyl; R3 denotes lower alkyl, C3-6cycloalkyl, partially unsaturated cyclohexyl, phenyl, phenyl-lower alkyl, pyridinyl, benzodioxolyl, tetrahydropyranyl, where the phenyl group is optionally substituted with 1-2 substitutes independently selected from a group comprising a halogen, lower alkyl, lower alkoxy group, fluoro-lower alkyl, fluoro-lower alkoxy group, N(lower alkyl)2; R4 denotes: a) heteroaryl which is an aromatic 5-6-member monocyclic ring or a 9-10-member bicyclic ring containing 1 or 2 heteroatoms selected from nitrogen, oxygen and/or sulphur, which is optionally substituted with 1-2 substitutes independently selected from a group comprising lower alkyl, phenyl, lower alkoxy group, -N(lower alkyl)2, oxo group, NH2, halogen, cyano group and morpholinyl; b) unsubstituted naphthyl, naphthyl or phenyl, which are substituted with 1-3 substitutes independently selected from a group comprising halogen, hydroxy group, NH2, CN, hydroxy-lower alkyl, lower alkoxy group, lower alkyl-carbonyl, lower alkoxy group-carbonyl, sulphamoyl, di-lower alkyl-sulphamoyl, lower alkyl-sulphonyl, thiophenyl, pyrazolyl, thiadiazolyl, imidazolyl, triazolyl, tetrazolyl, 2-oxopyrrolidinyl, lower alkyl, fluoro-lower alkyl, fluoro-lower alkoxy group, N(lower alkyl)2, carbamoyl, lower alkenyl, benzoyl, phenoxy group and phenyl which is optionally substituted with 1-2 substitutes independently selected from halogen and fluoro-lower alkyl; or c) if R3 denotes cycloalkyl and R1 denotes cycloalkyl, then R4 can also denote phenyl; R5, R6, R7 and R8 independently denote H, halogen, lower alkoxy group or lower alkyl, or R6 and R7, which are bonded to each other, form a 6-member aromatic carbocyclic ring together with carbon atoms to which they are bonded; provided that the compound of formula (I) is not selected from a group comprising butylamide 2-[2-(2-chlorophenyl)benzoimidazol-1-yl]-4-methylpentanoic acid and 2-(2-benzo[1,3]dioxol-5-ylbenzoimidazol-1-yl)-N-benzyl-butyric acid amide. The invention also relates to a pharmaceutical composition based on the formula I compound.EFFECT: novel benzimidazole derivatives which are useful as farnesoid X receptor antagonists are obtained.30 cl, 379 ex

Neurologically active compositions // 2420520
FIELD: medicine.SUBSTANCE: compounds can be used for treating neurological conditions, more specifically for treating neurodegenerative conditions, such as Alzheimer's disease. In a compound of formula I R2 represents H or CH2NR1R4 where R1 and R4 are independently selected from H, unsubstituted C1-6alkyl, substituted or unsubstituted C3-6 cycloalkyl, R3 represents H; substituted or unsubstituted C1-4alkyl; substituted or unsubstituted C2-4alkenyl; substituted or unsubstituted 6-members aryl condensed or uncondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl, containing 1-2 nitrogen atoms in a cycle; substituted or unsubstituted saturated or unsaturated 5 or 6-members N-containing heterocycle which can additionally contain nitrogen, oxygen or the sulphur atom condensed or ucondensed with substituted or unsubstituted 6-members aryl or 5-6-members heteroaryl containing nitrogen in a cycle; (CH2)nR6 where n is an integer from 1 to 6, and the values of R6 and the values of other radicals are specified in the patent claim.EFFECT: increased antiamyloidogenic action.20 cl, 20 tbl, 6 dwg, 7 ex

Compound for organic electronic devices // 2419648
FIELD: chemistry.SUBSTANCE: present invention relates to organic electroluminescent devices based on compounds of formula where Y, Z is selected from N, P, P=O, C=O, O, S, S=O and SO2; Ar1, Ar2, Ar3 are selected from benzene, naphthaline, anthracene, phenanthrene, pyridine, pyrene or thiophene, optionally substituted with R1; Ar4, Ar5, Ar6, Ar7 are selected from benzene, naphthaline, anthracene, phenanthrene, pyridine, pyrene, thiophene, triphenylamine, diphenyl-1-naphthylamine, diphenyl-2-naphthylamine, phenyldi(1-naphthyl)amine, phenyldi(2-naphthyl)amine or spirobifluorene, optionally substituted with R1; E is a single bond, N(R1), O, S or C(R1)2; R1 denotes H, F, CN, alkyl, where the CH2 can be substituted with -R2C=CR2 -, -C=C-, -O- or -S-, and H can be substituted with F, optionally substituted aryl or heteroaryl, where R1 can form a ring with each other; R2 denotes H, aliphatic or aromatic hydrocarbon; X1, X4, X2, X3 are selected from C(R1)2, C=O, C=NR1, O, S, S=O, SO2, N(R1), P(R1), P(=O)R1, C(R1)2-C(R1)2, C(R1)2-C(R1)2-C(R1)2, C(R1)2-O and C(R1)2-O-C(R1)2; n, o, p, q, r and t are equal to 0 or 1; s = 1.EFFECT: obtaining novel compounds - emission layer dopants, and novel electroluminescent devices based on said compounds which emit a blue colour.18 cl, 91 ex, 6 tbl

Pyrazole derivatives as protein kinase modulators // 2419612
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula which exhibits an inhibiting action on protein kinases A and B. In the compounds of formula (I), A represents a saturated hydrocarbon binding group containing 1 to 7 carbon atom where the binding group includes a chain of the maximum length 5 atoms located between R1 and NR2R3, and a chain of the maximum length 4 atoms located between E and NR2R3 where one of carbon atoms in the binding group can be optionally substituted by an oxygen or nitrogen atom; and where the carbon atoms of the binding group A can optionally have one or more substitutes selected from oxo, fluorine and hydroxy provided the hydroxy group if any is not located on a carbon α-atom in relation to the NR2R3 group and provided the oxo group if any is located on the carbon α-atom in relation to the NR2R3; E represents a phenyl or pyridine group; R1 represents a C6-10aryl or pyridyl group which is not substituted or substituted with 1 or 2 substitutes specified in the patent claim; and R2, R3, R4 and R5 have the values specified in the points of the patent claim.EFFECT: invention refers to a pharmaceutical composition containing said compounds, to methods of making the compounds and their application as cancer drugs.29 cl, 1 tbl, 108 ex

ethod of producing losartan // 2412940
FIELD: chemistry.SUBSTANCE: described is a method of producing a compound of general formula I where R1 denotes a radical of formula II: where R2 is a protective tetrazole group which is a novel intermediate compound when producing losartan - 2-n-butyl-4-chloro-5-hydroxymethyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4]methyl}-imidazole, and a method of producing losartan based on compound I by reducing the formyl group and then adding a chlorine atom to the imidazole ring and removing the protective R2 group.EFFECT: method ensures high output of the end product from available starting and intermediate compounds on an industrial scale.9 cl
 
2551315.
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