Linked by a chain containing hetero atoms as chain links (C07D403/12)

C   Chemistry; metallurgy(318327)
C07   Organic chemistry(61593)
C07D403/12                     Linked by a chain containing hetero atoms as chain links(474)
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
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
Heterocyclic pyrimidine analogues as tyk2 inhibitors // 2641895
FIELD: pharmacology.SUBSTANCE: compounds possess the properties of the inhibitor of the non-responsive tyrosine Tyk2 kinase and selective inhibitory action against JAK1, JAK2, JAK3 Janus kinases. The compounds can be used in a method for treatment or prevention of immunological, inflammatory, autoimmune, allergic disorder or graft rejection or graft-versus-host diseases. In the formula (I) , R1 is H; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R3, which are the same or different. At that, C 1-6 alkyl containing a hydroxy group may be deuterated; R3 represents halogen; CN; C(O)OR4; OR4; C(O)R4; (O)N(R4R4a); S(O)2R4; S(O)R4; or T1; R4, R4a, R4b are independently selected from the group consisting of H; T1; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R5, which are the same or different; R5 represents halogen; CN; OR6; or T1; R6 is H; T1 is C3-7 cycloalkyl; 4-7 membered heterocyclyl with 1 to 2 heteroatoms in the ring selected from nitrogen, oxygen or sulfur; or a 7-8 membered heterobicyclyl, optionally spyrocondensed, with two heteroatoms in the cycle, selected from nitrogen or nitrogen and oxygen, where T1 is optionally substituted by one or more R7 , which are the same or different; R7 is halogen; CN; C(O)OR8 ; oxo (= O), wherein the ring is at least partially saturated; C 1-6 alkyl; R 8 are independently selected from the group consisting of H; C1-6 alkyl; X1 is C(R11a) or N; X2 is C(R11b) or N; X3 is C(R11c) or N; X4 is C(R11d) or N; X5 is C(R11e) or N, provided that no more than two of X1, X2, X3, X4, X5 are N; R11a, R11c, R11e are independently selected from the group consisting of H; halogen; CN; OR12; C(O)N(R12 R12a); S(O)2N (R12R12a); S(O)2R12; T2; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R13, which are the same or different; R11b, R11d are independently selected from the group consisting of H; halogen; CN; OR12; S(O)2N (R12R12a); S(O)R12; C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R13, which are the same or different; R12, R12a are independently selected from the group consisting of H and C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R13, which are the same or different; T2 is a 5-membered heterocycle with two nitrogen atoms in the ring; R13 is halogen; CN; OR14; C(O)N (R14R14a); S(O)2N(R14R14a); S(O)2R14; S(O) R14; N(R14) S(O)2N(R14aR14b); N(R14)S(O)N(R14aR14b); SR14; N(R14R14a); NO2; OC(O)R14; N(R14)S(O)2R14a; R14, R14a, R14b are independently selected from the group consisting of H or C1-6 alkyl, where C1-6 alkyl is optionally substituted by one or more R15, which are the same or different; R15 is halogen.EFFECT: increased efficiency.18 cl, 13 tbl, 480 ex
New anti-invasive compounds // 2641650
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula or pharmaceutically acceptable salts thereof, which can be used to prevent, and/or inhibit, and/or treat cancer. In formula (I) A and A' independently represent phenyl or pyridylene group; R2 represents a hydrogen or alkyl group (C1-C4); R3 represents a 2-pyridyl group, 3-pyridyl group, 4-pyridyl group, 2-pyrimidinyl group, 4-pyrimidinyl group or 5-pyrimidinyl group; R4 represents a carbonyl group or sulfonyl group; R5 is a -NH-(CH2)(a)-NR6R7 group or a 4-methylpiperazinyl group and a is an integer from 1 to 4, R6 and R7 independently represent a nalkyl group (C1-C4) or R6 R7 together with nitrogen atom they are bounded to form a heterocyclic group selected from 4-methylpiperazinyl group, morpholine group, pyrrolidinyl group and piperidine group. The invention also relates to a method for preparation of compounds of formula (I) and a pharmaceutical composition containing them.EFFECT: improved compounds properties.16 cl, 6 tbl, 17 ex
Heterocyclic compounds, effective for kinase inhibition // 2640862
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I)or a pharmaceutically acceptable salt thereof, wherein Q is O; W is phenyl; X is absent; Y is NH; Z1 and Z2 are N; Z3 is NR5, where R5 is hydrogen; R1 is pyridine or pyrimidine; optionally substituted with C1-C6alkyl, C1-C6alkoxy, -NR10R11 or -SOmR12, where R10 and R11 are hydrogen, R12 is C1-C6alkyl; and m is 0; R3 is C1-C6alkyl; R2 is C1-C6alkyl when p is 1; or one R2 is C1-C6alkyl and one R2 is halogen when p is 2; or one R2 and R3 combined with formation of a five- to seven-membered carbocycle; R4 is hydrogen; p=1 or 2; and n is 1.EFFECT: heterocyclic compounds designed for cancer treatment.12 cl, 1 tbl, 8 ex
Oxothioimidazoline derivatives, methods for their production and application in medicine as androgen receptor inhibitors // 2639145
FIELD: pharmacology.SUBSTANCE: invention relates to an oxothioimidazoline derivative of the formula or to its mesomer, racemate, enantiomer, diastereomer, or a mixture thereof, wherein A is -CR' or N; R' is hydrogen or halogen; Z1 and Z2 each independently represents methyl; R1 and R2 each is independently selected from the group consisting of S or O; R3 is selected from the group consisting of C1-C3-alkyl, heterocyclyl selected from tetrahydrofuran, tetrahydropyran, piperidine, dioxo-tetrahydrothiopyran, azetidine, pyrrolidine, oxetane; C6-aryl and -S(O)mR6; when R3 is selected from heterocyclyl selected from tetrahydrofuran, tetrahydropyran, piperidine, dioxo-tetrahydrothiopyran, azetidine, pyrrolidine, oxetane; or C6-aryl, each of the heterocyclyl and aryl is optionally substituted by one or more groups selected from the group consisting of C1-alkyl, -OR6, -C(O)NR7R8, -S (O)mR6 and -C(O)R6; when R3 is C1-C3alkyl, alkyl is substituted by one or more groups selected from the group consisting of halogen, cyano, amino, C3-cycloalkyl, tetrahydrofuran, -OR6, -C(O)NR7R8, -S(O)mR6 and -C(O)OR6, wherein the cycloalkyl is optionally substituted by one group selected from cyano, amino, -OR6, -C(O)NR7R8 and -C(O)OR6; R4 and R5 are each independently selected from the group consisting of cyano, C1-alkyl, halogen and -CF3; R6 is hydrogen, C1-alkyl or -CF3; R7 and R8 are each independently selected from the group consisting of hydrogen and C1-alkyl, and m is 2. The invention also relates to intermediates, a process for preparation of a compound of formula (I), a pharmaceutical composition based on the compound of formula (I) and its application.EFFECT: new oxothiohydantoin derivatives, useful for treatment of androgen receptor mediated diseases.18 cl, 51 ex
Pyrazolaminopirimidine derivatives as modulators of leucine-repeating kinase 2 // 2637947
FIELD: pharmacology.SUBSTANCE: invention relates to pyrazolaminopyrimidine derivatives listed in claim 1 which are modulators of leucine-repeating kinase 2 (LRRK2), a pharmaceutical composition containing them, application of these compounds for treatment of diseases associated with the LRRK2 receptor such as Parkinson's disease, and to a method for Parkinson's disease treatment.EFFECT: higher efficacy of compound application.6 cl, 4 tbl, 52 ex
Triazolcarboxamide derivatives // 2637938
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula I. In formula IR1 is phenyl or pyridinyl optionally substituted by halogen, lower alkyl, lower alkoxy, lower alkyl, substituted halogen, and lower alkoxy substituted by halogen; X1 is -N = or CH; X2 is a CR2 or =N-; X3 is -N= or CH; provided that only two of X1, X2 or X3 are nitrogen; where is a triazole group selected from , or ; R2 is hydrogen or lower alkyl; Z is a bond, -O- or -CH2-. The compounds of the invention possess affinity for the receptors associated with trace amines (TAAR). The invention also relates to pharmaceutical compositions and to application of a compound for drug manufacture.EFFECT: new compounds of formula I are obtained that have a high affinity for the receptors associated with trace amines, especially TAAR1.12 cl, 1 tbl, 36 ex

Heteroaryl compounds and their application // 2636584
FIELD: medicine, pharmacy.SUBSTANCE: present invention relates to new compounds selected from the group of compounds shown below, or pharmaceutically acceptable salts thereof, which have properties of kinase activity inhibitor selected from BTK, ErbB1, ErbB2, ErbB3, ErbB4, TEC, ITK, BMX and JAC3, or the said kinase mutant. At that, one or more kinases may be inhibited irreversibly by covalent cysteine (Cys) modification. The compounds may be used for treatment of rheumatoid arthritis, multiple sclerosis, diabetes, B-cell chronic or acute lymphocytic leukemia, hairy cell leukemia, non-Hodgkin's lymphoma, Hodgkin's lymphoma, multiple myeloma, colorectal cancer, pancreatic cancer, bone cancer, metastasis in the bone, osteoporosis, diabetes, irritable bowel syndrome, Crohn's disease, systemic lupus erythematosus or disorders associated with renal carcinoma transplant selected from breast cancer, glioblastoma, lung cancer, head and neck cancer, colorectal cancer, bladder cancer, non-small cell lung cancer, squamous cell carcinoma, salivary gland carcinoma, ovarian carcinoma, colorectal cancer or pancreatic cancer. Compounds are selected from the group of compounds , , , , , , , and compounds (I-382) - (I-393) specified in the invention formula.EFFECT: invention can be used to treat many diseases.16 cl, 25 dwg, 20 tbl, 302 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

Cycloalkane derivative // 2635354
FIELD: pharmacology.SUBSTANCE: invention provides a compound represented by the formula , or a pharmacologically acceptable salt thereof, where Ar1 and Ar2: a heteroaryl group or an aryl group; R1, R2 and R3: a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group or a cyano group; R4 and R5: a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a hydroxyl group or a C1-C6 alkoxy group; N: an integer between 1 and 3; and the heteroaryl group or aryl group optionally contains one or two groups, independently selected from a halogen atom, a C1-C6 alkyl group, an amino group, and when a heteroaryl group or aryl group contains two such groups, the two groups are the same or different.EFFECT: increased efficiency of treatment.33 cl, 5 dwg, 8 tbl, 179 ex

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

New compounds for selective histone deacetylase inhibitors and pharmaceutical composition including such compounds // 2634694
FIELD: pharmacology.SUBSTANCE: invention relates to new compounds of formula I, their optical isomers or pharmaceutically acceptable salts that can be used for treatment of diseases mediated by histone deacetylase. In formula I, A is , Xa and Xb are CH, L1 and L2 independently hydrogen, -F, -Cl, -Br or -I, Q is C(=O), Y is selected from the group consisting of , and , M is C, O or N, l and m are independently 0 or 1, each of Ra1 and Ra2 is independently hydrogen; hydroxy; linear or branched -C1-4-alkyl, etc., n is 0, 1 or 2, Rb is hydrogen; hydroxy; linear or branched -C1-6-alkyl, etc., Z is selected from the group consisting of , etc., where each of Pa and Pb is independently ; hydrogen; hydroxy; linear or branched -C1-4-alkyl, etc., where is selected from phenyl, pyridine, pyrimidine, thiazole, indole, indazole, etc., each of x, y and z is independently 0 or 1, and each of Rg1, Rg2 and Rg3 is selected independently from hydrogen; hydroxy; -C1-3-alkyl, etc. The invention also relates to a pharmaceutical composition comprising compounds of formula I, a method for treatment of diseases mediated by histone deacetylase and application of said compounds for drugs preparation.EFFECT: increased effeciency of compound application.9 cl, 7 dwg, 16 tbl, 173 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
Heterocyclic derivative and pharmaceutical means // 2632908
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic derivative or a pharmaceutically acceptable salt thereof, of the general formula , wherein ring A is a group represented by the general formulas , or , where X1 is NH, NC1-6alkyl or O; A1 is hydrogen; A2 is i) hydrogen; ii) halogen; iii) C1-6alkyl optionally substituted by one to three groups selected from a group consisting of halogen, amino, mono(C1-6alkyl)amino, di(C1-6alkyl)amino, carbamoyl, mono(C1-6alkyl)aminocarbonyl, di(C1-6alkyl)aminocarbonyl, saturated cyclic aminocarbonyl, wherein the "saturated cyclic amino group" of the "saturated cyclic aminocarbonyl" part is 1-pyrrolidinyl, C1-6alkoxy and C1-6alkoxy-C1-6alkoxy; iv) C3-6cycloalkyl, optionally substituted by C1-6alkyl optionally substituted by one to three halogens; vi) a 4 to 5-membered saturated heterocyclic group containing one nitrogen or oxygen atom in the ring, optionally substituted by C1-6alkyl, (C1-6alkyloxy)carbonyl, (C1-6alkyl)carbonyl or hydroxy; (vii) C1-6alkylthio; (viii) C1-6alkylsulfonyl; ix) C1-6alkylsulfinyl; x) -NR3R4, where R3 and R4 are the same or different groups selected from a) hydrogen, b) optionally substituted C1-6alkyl, or c) C3-6cycloalkyl; or xi) saturated cyclic amino, wherein the "saturated cyclic amino" is piperidino, 1-piperazinyl or 4-morpholino, optionally substituted by C1-6alkyl, amino, mono(C1-6alkyl)amino, di(C1-6alkyl)amino, C1-6alkoxy or hydroxyl; R1 is phenyl, benzyl, naphthyl, C3-6cycloalkyl, C3-6cycloalkylmethyl, heteroaryl wherein heteroaryl is benzothiadiazolyl, benzothiazolyl, indolyl, 1,1-dioxobenzothiophenyl, quinolyl or 1,3-benzoxazol-2-yl, 1,2,3,4-tetrahydronaphthalen-5-yl, 1,2, 3,4-tetrahydronaphthalen-6-yl, 2,3-dihydro-1H-inden-4-yl, 2,3-dihydro-1H-inden-5-yl or C1-6alkyl, wherein the said phenyl, benzyl, cycloalkyl, cycloalkylmethyl and heteroaryl are optionally substituted; R2 is phenyl or pyridyl, wherein the said phenyl and pyridyl are optionally substituted. The invention also relates to a pharmaceutical composition and to an agent having the ability to inhibit mPGES-1 comprising a compound selected from the group consisting of a heterocyclic derivative of formula 1 and a pharmaceutically acceptable salt thereof as an active ingredient.EFFECT: heterocyclic derivatives possessing the inhibitory activity of mPGES-1.10 cl, 18 tbl, 257 ex
Nitrogen-containing heterocyclic compound or its salt // 2632253
FIELD: chemistry.SUBSTANCE: invention relates to compound of the general formula [1]-(1): , where R2ais a hydrogen atom or a C1-6alkyl group, which may be substituted by one or more substituents selected from a halogen atom; an amino-group; a C1-6alkylamino-group, which may be substituted by one or more halogen atoms, di(C1-6alkyl) amino-group, which may be substituted by one or more hydroxy-group, a C1-6alkylaminocarbonyl and di(C1-6alkyl) amino-group, or morpholinyl or piperazinyl group, which may be substituted by one or more substituents selected from hydroxy-group, a C1-6alkyl group and a hydroxy-C1-6alkyl group, R4a is a hydrogen atom or a C1-6alkyl group, which may be substituted by one or more phenyl groups, R17a is a hydrogen atom or a C1-6alkyl group, which may be substituted by one or more substituents selected from a halogen atom, the hydroxyl group, and a C1-6alkoxygroup, provided that R17a together with R4a, the nitrogen atom, to which R4a is attached, and the carbon atom, to which R17a is attached, may form a nitrogen-containing divalent azetidinyl, pyrrolidinyl, piperidinyl, or azepanyl group, which may be substituted by one or more substituents selected from the atom of the halogen atom, a hydroxyl group, a C1-3alkyl group or a C1-6alkoxy group; R17b and R18b are the same or different and are a hydrogen atom or a C1-6alkyl group, which may be substituted by one or more substituents selected from the atom of the halogen atom, a hydroxyl group and a C1-6alkoxy group, provided that R17b and R18b together with the carbon atom, to which they are attached, can form C(=O), or R17b and R18b together with the carbon atom, to which they are attached, may form a tetrahydropyrandyl group; R9a is a C1-6alkoxy group, pyrrolidinyl, piperidinyl, piperazinyl, pyrazolidine, triazoline, or morpholinyl group, which may be substituted by one or more substituents selected from the atom of the halogen atom and a C1-3alkyl group, or N(R15)(R16), where R15 is a hydrogen atom or a C1-6alkyl group, and R16 is a C1-6alkyl group, which may be substituted by one or more groups selected from a halogen atom, a cyano group, a C3-6cycloalkyl group, a phenyl group, which may be substituted by one or more halogen atoms, a C1-6alkoxy group, di(C1-6alkyl) amino-group, and a morpholinyl, a tetrahydropyranyl, or a thiophenol group, a C3-8cycloalkyl group, a phenyl group, which may be substituted by one or more groups selected from a halogen atom, a cyano group, a C1-6alkyl group, a C1-6alkoxy group, or a pyridinyl or chinolyl group, which may be substituted by one or more C1-6alkoxy group, or R15 and R16 may form a cyclic amino-group, which may be substituted by one or more groups selected from halogen and a C1-3alkyl group, and R12a is a C1-6alkyl group, which may be substituted by one or more groups selected from the hydroxy groups, di(C1-6alkyl) amino-group or a pyridinyl, a morpholinyl, or a pyrrolidinyl group, a phenyl group, which may be substituted by one or more groups selected from the halogen atom; a cyano group; an amino-group, which may be protected by the acyl group; a carbamoyl group, which may be substituted by one or more groups selected from the C1-6alkyl groups and the C3-8cycloalkyl group; a C1-6alkyl group, which may be substituted by one or more groups selected from halogen and the triazoline group; a C1-6alkoxy group, which may be substituted with halogen; or pyrazolidine, triazoline, or thiazolidine group which may be substituted by one or more groups selected from C1-6alkyl group and ceanography, or pyridyloxy, izohinolinove, talinolol, isoxazolidine, isothiazolinone, thiadiazolidine, indazolinone, benzothiazolyl, chinolyl, benzoxazolyl, or pyrazolopyrimidinyl group, which may be substituted by one or more groups selected from halogen, a C1-6alkyl group, which may be substituted by one or more C1-6alkoxy group, a C1-6alkoxy group, a C1-6alkyl amino-group, a C1-6alkoxy carbonyl group, or a morpholinyl group; X2a is a C1-6alkylene group, which may be substituted by one or more substituents selected from exography and the C1-6alkyl group, a divalent C2-6alicyclic hydrocarbon group, or a divalent aromatic hydrocarbon group, which may be substituted by one or more groups selected from halogen, a C1-6alkyl group, which may be substituted by halogen and the C1-6alkoxy group, and X3a is a C2-6alkynyl amino-group, or N(R22)-C(=O), where R22 is a hydrogen atom.EFFECT: compounds are an inhibitor of Fms-like tyrosine kinase 3, which can be used as a therapeutic agent for acute myelogenous leukemia.21 cl, 261 tbl, 70 ex

Amide compounds, methods for production, application as means for treatment and prevention of diseases caused by rna-containing viruses // 2628800
FIELD: pharmacology.SUBSTANCE: compounds of the invention are intended for manufacture of a pharmaceutical composition, kit or drug. The invention also relates to a process for preparation of compounds of the invention (versions). Compounds of the invention are intended for use in the prevention or treatment of diseases caused by RNA-containing viruses belonging to enteroviruses, metapneumoviruses or pneumoviruses.EFFECT: amide compounds for treatment or prevention of diseases caused by RNA-containing viruses.26 cl, 8 tbl, 5 ex
Compounds of pyridazinamide and their use as synthetic syneckinasis inhibitors (syk) // 2627661
FIELD: chemistry.SUBSTANCE: invention relates to novel pyridazinamides of the formula I , where all variable substituents are defined in the claims, and their pharmaceutically acceptable salts, as well as a pharmaceutical composition based on them.EFFECT: compounds of the formula are SYK inhibitors and are useful for the treatment of autoimmune and inflammatory diseases.10 cl, 1 tbl, 43 ex
ethod of producing n,n-bis(4,6-diazido-1,3,5-triazine-2-yl) amine // 2627357
FIELD: chemistry.SUBSTANCE: invention relates to the method of producing N,N-bis(4,6-diazido-1,3,5-triazine-2-yl) amine (I) by reacting N, N-bis (4,6-dichloro-1, 3,5-triazine-2-yl) amine with an azidating agent, in which sodium azide is used, in an aqueous acetone medium at room temperature, followed by isolation of the desired product by precipitation from water (I).EFFECT: method of producing a compound of formula I is developed with high yield and purity.3 ex

New pyrazole derivative // 2625790
FIELD: pharmacology.SUBSTANCE: in particular, invention relates to a compound represented by the following general formula (I): [wherein Ar1 is 2-methoxy-4-(2-pyridylmethoxy)phenyl, etc. and Ar2 is 1H-indole-6-yl group, etc.] or to salt thereof.EFFECT: increased efficiency of treatment.19 cl, 4 dwg, 1 tbl, 112 ex

Conjugates for integrin antagonist targeted delivery to cells, expressing lfa-1 // 2624732
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula wherein R1 is selected from compounds (1) (2) (3), which are used for the manufacture and delivery of conjugated groups, such as small molecules, peptides, nucleic acids, fluorescent groups and polymers crosslinked with antagonists of integrin LFA-1 for targeted delivery to cells expressing LFA-1.EFFECT: improved properties.21 cl, 6 dwg, 1 tbl, 10 ex

Conjugates for integrin antagonist targeted delivery to cells, expressing lfa-1 // 2624731
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula I wherein R1 is selected from the group consisting of formula (1), formula (2), formula (3), for the manufacture and delivery of conjugated molecules, such as small molecules, peptides, nucleic acids, fluorescent molecules and polymers that are associated with the integrin antagonists of VLA-4, target cells expressing VLA-4.EFFECT: improved properties of compounds.16 cl, 6 dwg, 5 tbl, 14 ex
Oxazethydine derivatives, method for their production and their use in medicine and cosmetics // 2624011
FIELD: chemistry.SUBSTANCE: invention relates to a heterocyclic compound of formula (I) and its enantiomer where R1 is a cyclopropylmethyl group, and R2 represents a methyl group; or R1 represents a 4-hydroxybutyl group, and R2 represents a hydrogen atom. The invention also relates to use of a formula compound (I) or compositions on the basis thereof, pharmaceutical compositions and cosmetic compositions based on compounds of formula (I).EFFECT: obtained new compound is useful in the treatment of pigmentation disorders and inflammatory or immune disorders.12 cl, 2 tbl, 3 ex
Inhibitors of nonprilyzine // 2622288
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula , wherein R1 is selected from -OR7 and -NR8R9; R2 is H; X is -C1-9heteroaryl, selected from pyrazole, imidazole, triazole, benzotriazole, furan, tetrazole, pyrazine, thiophene, oxazole, isoxazole, thiazole, oxadiazole, pyridazine, pyridine, pyrimidine, benzoxazole, pyridylimidazole and pyridyltriazole; R3 is absent or is selected from H; Halogen; -C0-5alkylene-OH; -NH2; -C1-6alkyl; -CF3; -C3-7cycloalkyl; -C0-2alkylene-O-C1-6alkyl; -C(O)R20; -C0-1alkylene-COOR21; -C (O) NR22R23; -NHC(O)R24; =O; -NO2; -C(CH3) =N(OH); Phenyl optionally substituted with one or two groups independently selected from halogen, -OH, -CF3, -OCH3, -NHC(O)CH3 and phenyl; Naphthalenyl; Pyridinyl; Pyrazinyl; Pyrazolyl optionally substituted with methyl; Thiophenyl, optionally substituted by methyl or halogen; Furanyl; and -CH2-morpholinyl; and R3, when present, is attached to a carbon atom; R4 is absent or is selected from H; -HE; -C1-6alkyl; -C1-2alkylene-COOR35; -OCH2 O(O)CH (R36)NH2; -OCH2O(O)CH3; -CH2CH(OH)CH2OH; and phenyl or benzyl optionally substituted with 1 to 3 groups selected from halogen, -COOR35, -OCH3, -OCF3 and -SCF3; and R4, when present, is attached to a carbon or nitrogen atom; or R3 and R4 are taken together to form -phenylene-O- (CH2) 1-3- or -phenylene-O-CH2-CHOH-CH2-; A is 0 or 1; R5 is halogen; B is 0 or an integer of 1 to 3; Each R6 is independently selected from halogen, -OH, -CH3 and -OCH3; R7 is selected from H, -C1-8alkyl, -[(CH2)2O]1-3CH3, -C1-6alkylene-OC(O)R10, -C0-6alkylenemorpholinyl, -C1-6alkylene-SO2-C1-6alkyl and the structure of formula (a); R10 is -O-C3-7cycloalkyl; and R32 is -C1-6alkyl; R8 and R9 are H; R20, R21 and R35 are independently selected from H and -C1-6alkyl; R22 and R23 are independently selected from H, -C1-6alkyl, -CH2COOH, -(CH2)2OH, -(CH2)2OCH3, - (CH2)2SO2NH2, -(CH2)2N(CH3)2, -C0-1alkylene-C3-7-cycloalkyl and -(CH2)2-imidazolyl; or R22 and R23 are taken together to form a ring; R24 is selected from -C1-6alkyl; -C0-1alkylene-O-C1-6alkyl; Phenyl optionally substituted by halogen or -OCH3; and pyridinyl; and R36 is -CH (CH3) 2; and wherein the methylene linker on the biphenyl is optionally substituted with one or two -C1-6 alkyl groups; or a pharmaceutically acceptable salt thereof. Compounds of formula (I) are prepared by combining a compound of formula with a compound of formula 2 to provide a compound of formula I; Where P1 is also H. Also, the invention relates to an intermediate of formula 1, wherein P1 is H. The compounds of formula (I) are intended for the preparation of a medicament or pharmaceutical composition having inhibitory activity against non-prolamin (NEP). (a).EFFECT: compounds that have a non-lysine inhibitory enzyme activity.28 cl, 61 tbl, 25 ex
Optical bleaching agents for high-quality jet printing // 2620812
FIELD: printing industry.SUBSTANCE: invention relates to an optical bleaching agent comprising of a mixture of compounds of the formulas and wherein R is hydrogen or methyl; Y is an amino acid that is derived from aspartic acid, glutamic acid or iminodiacetic acid and from which the hydrogen atom of the amino group is removed; and M is an alkali metal cation. The invention also relates to an optical bleaching agent comprising a compound of formula (4), to a process for preparing an optical bleaching agent, to a compound of formula (4), to a composition for bleaching paper surface, and to paper optically bleached with an optical bleaching agent.EFFECT: new optical bleaching agents are obtained, providing a bleaching effect when applied to the paper surface.14 cl, 1 tbl, 9 ex
4-aminoquinoline-3-carboxylic acid derivatives and compositions containing them for enhancing sweet taste // 2617700
FIELD: chemistry.SUBSTANCE: invention relates to a new derivative of quinoline of formula (I) (I)or its salt suitable for internal use, where R1 and R2 represents hydrogen; L represents a C1-C7 alkylene, C3-C6 cycloalkylene or -(CH2)1-3-(C3-C6) cycloalkylene; M represents -NR4-C(O)- or -C(O)-NR4-; when M represents -NR4-C(O)-, R4 represents hydrogen; or alternatively R4 represents a C1-C3 alkilinity linker, where the specified alkilinity linker and from 2 to 5 atoms of L, together with the nitrogen to which they are attached, form a 5-8-membered monocyclic, bicyclic or bridged heterocyclic ring that is optionally substituted and contains one hetero-atom representing a nitrogen atom; and R3 represents a C1-C6 alkyl, a substituted C1-C3 alkyl, a C3-C6 cycloalkyl, a substituted C3-C6 cycloalkyl, a 6-membered heterocyclyl containing one oxygen atom, or a substituted 6-membered heterocyclyl containing one nitrogen atom; when M represents -C(O)-NR4-, R4 represents hydrogen; or alternatively R4 and R3 together with the nitrogen to which they are attached form a 5-6-membered monocyclic heterocyclic ring which contains one nitrogen atom; where in the group indicated as substituted, one substituent is selected from the group consisting of the following substituents: -NH2, a hydroxyl, a C1-6 alkoxy, a C1-6 alkyl, a 6-membered heterocyclyl containing one or two atoms selected from N and O, a C3-4 cycloalkyl, and C(=O)NRaRa, where each Ra independently means hydrogen or a C3-6 cycloalkyl; provided that the compounds of the formula (I) cannot represent compounds mentioned in claim 1. The invention also relates to a composition based on a compound of the formula (I) and methods for enhancing the sweet taste.EFFECT: new quinoline derivatives useful as sweet taste modifiers are obtained.31 cl, 24 tbl, 24 ex

Pyrazole compound and its pharmaceutical use // 2617678
FIELD: medicine, pharmacy.SUBSTANCE: invention refers to a compound of general formula or pharmaceutically acceptable salt thereof. In formula (I) Cy represents phenyl, C3-8 cycloalkyl or C3-8 cycloalkenyl , Cya is a heterocyclic group with the structure given in the invention formula, R1a and R2b are groups defined in the formula. The objects of invention are also the pharmaceutical composition and the agent based on formula (I) compound, the method of diabetes treatment and prevention and compound application.EFFECT: invention is SGLT1 inhibitor and can be used to treat or prevent diabetes.24 cl, 4 tbl, 605 ex
Process for preparation of 1-acyl-4-phenylsulfonylprolinamide derivatives and new intermediates // 2615997
FIELD: chemistry.SUBSTANCE: invention relates to a method of producing proline of formula 1, where R1 is selected from C1-7-alkyl or a radical of formula II, where R4 is selected from a group, containing C1-7-alkyl, halogen-C1-7-alkyl and phenyl, optionally substituted by halogen; R2 is selected from a group, containing halogen or halogen-C1-7-alkyl; and R3 is selected from a group, containing hydrogen, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy or 5-or 6-member heterocycle, containing one or two nitrogen atoms, wherein cycle is optionally substituted with C1-7-alkyl or halogen, and a novel intermediate compound used in method.EFFECT: proline derivatives of formula 1 are preferable inhibitors of cysteic cathepsin protease S and are therefore useful in treating metabolic diseases, such as diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral artery disease and diabetic neuropathy.29 cl, 1 ex

Use of sigma ligands in diabetes type-2 associated pain // 2608943
FIELD: chemistry.SUBSTANCE: invention relates to use of a sigma ligand, which is a 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine or a pharmaceutically acceptable salt thereof.EFFECT: prevention and/or treatment of pain associated with type 2 diabetes and related symptoms.6 cl, 9 dwg, 4 ex
Spiro-condensed cyclohexane derivatives as inhibitors of hsl, effective for diabetes treatment // 2607080
FIELD: pharmaceutics.SUBSTANCE: present invention relates to novel compounds of formula (I), as well as to their pharmaceutically acceptable salts possessing activity of HSL inhibitors, to pharmaceutical composition, method of inhibiting of enzyme HSL lipase, as well as to use of disclosed compounds for preparing a drug. Values R1, R2, R3, Ca and Cb are given in the claim.EFFECT: invention discloses spiro-condensed cyclohexane derivatives as inhibitors of HSL, effective for diabetes treatment.24 cl, 377 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

3-carboxy-4-aminoquinoline derivates, useful as sweet taste modifiers // 2605549
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry and specifically to novel quinoline derivatives of general formula (IIIb) or ingestible salt thereof, where A is NH2; B is C1-C4 alkyl; C is -CO2R7; R7 is hydrogen; L1 is C1-C8 alkylene, C6-cycloalkylene or -CH2-C6-cycloalkylene; L2 is -O-, NR34-C(O)-, -C(O)-NR34-, -(3-6-member heterocyclylene-C(O))-group, where heterocyclylene contains one nitrogen atom; R33 is C1-C6 alkyl, optionally substituted C1-C6 alkoxy or hydroxy, C3-C10 carbocyclyl, optionally substituted with one C1-C6 alkoxy, C6-C10 aryl, optionally substituted with one or two substitutes, selected from -OH, halogen, -C(=O)NH2, -C(=O)NHC1-6 alkyl, C1-C6 alkoxy, C1-C6 alkyl-OH and O-C1-C6 alkyl-OH, C6-C10 aryl C1-C4 alkyl, optionally substituted C1-C6 alkoxy, 5-10-member heterocyclyl containing 1 or 2 oxygen atoms, pyridine or pyridine-C1-C4 alkyl; and R34 is hydrogen. Invention also relates to quinoline derivatives of formula (IIIc) and (IIIc'), specific quinoline derivatives, ingestible composition based on compounds of formula (IIIb), (IIIc) and (IIIc'), method of enhancing sweet taste of ingestible composition, method of producing intermediate compounds of formulae (IV) and (IVc).EFFECT: novel quinoline derivatives, useful as sweet taste modifiers.23 cl, 23 tbl, 133 ex, , ,

Pesticide compositions and related methods // 2597421
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula one, two or three: Formula 1 Formula 2 Formula 3, where Ar1 is a substituted phenyl, containing one substitute independently selected from C1-C6 halogenalkyl with C1-C6 halogenalkoxy; Het denotes a 5-member unsaturated heterocyclic ring containing two or three heteroatoms selected from nitrogen; Ar2 is phenyl. Invention also relates to a method of pest control.EFFECT: obtaining novel compounds which can be used in agriculture against pests.8 cl, 5 tbl, 22 ex

Bi-aryl-meta-pyrimidine kinase inhibitors // 2597364
FIELD: chemistry.SUBSTANCE: present invention relates to a novel compound of formula 33 and a method of producing a compound of formula LVII using compound of formula 33 as a starting compound. Compound of formula LVII possesses ability to inhibit JAK-kinase family, in particular JAK2 kinase. Compound LVII can be used for treating myeloproliferative disease, in treating idiopathic polycytemia, primary thrombocytopenia, myeloid fibrosis, proliferative diabetic retinopathy, cancer or eye disease. Compound of formula 33 corresponds to structural formula given below. Method of producing a compound of formula LVII involves reaction of 4-(2-pyrrolidin-1-yl-ethoxy)phenylamine with compound of formula 33. Method involves cleaning reaction mixture obtained at step of reacting a compound of formula 33 with 4-(2-pyrrolidin-1-yl-ethoxy)phenylamine, for separation of compound of formula XLV.EFFECT: obtaining a compound of formula LVII using compound of formula 33 as a starting compound.3 cl, 2 dwg, 3 tbl, 246 ex

Substituted benzamide derivatives // 2595902
FIELD: chemistry.SUBSTANCE: invention relates to compound of formula (I), where R is hydrogen or C1-7alkyl; R1 represents -(CH2)n-(O)o-5-7-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, except for piperazine, where said heterocycloalkyl group optionally substituted with C1-7alkyl, hydroxy or halogen; n equals to 0, 1 or 2; o equals to 0 or 1; R2 represents CF3, C3-6-cycloalkyl, possibly substituted C1-7alkoxy or halogen, or represents indane-2-yl, or is 6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, optionally substituted with pyrimidinyl, or is 5-6 mono- or 9-10-member bicyclic heteroaryl containing 1-2 heteroatoms selected from N, O and S, where the heteroaryl is not thiazol and where said aromatic ring, is possibly substituted with one or two substitutes selected from C1-7alkyl, halogen, 5-6-member heteroaryl containing 1-2 heteroatoms selected from N and O, hydroxy, CF3, OCF3, OCH2CF3, OCH2-cycloalkyl, OCH2C(CH2OH)(CH2Cl)(CH3), S-C-1-7alkyl, C1-7alkoxy, CH2-C-1-7alkoxy, C2-7alkynyl or cyano, or substituted with -C(O)-phenyl, -O-phenyl, -O-CH2-phenyl, phenyl, and where said phenyl ring may be substituted with halogen, -C(O)OH or -C(O)O-C-1-7alkyl, or said aromatic ring, is possibly substituted with 5-6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, OCH2-oxetane-3-yl or O-tetrahydropyran-4-yl, possibly substituted C1-7alkyl; X is bond, -CH2NH-, -CHR″-, -(CHR″)q-O-, -O-(CHR″)q- or -(CH2)2-; Y is bond; R″ is hydrogen, C1-7alkyl, CF3, C1-7alkoxy; q is equal to 0, 1, 2 or 3; or pharmaceutically acceptable acid addition salt thereof, except for compounds specified in patent claim. Invention also relates to specific compounds specified in patent claim. Compounds are intended for producing medicinal agents, showing affinity to TAAR1.EFFECT: technical result: benzamide derivatives having high affinity to receptors associated with TAAR1 trace amines.9 cl, 1 tbl, 323 ex

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

ethod of producing 1-(2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl)benzylcarbamoyl)-l-proline-n,n-dimethylamide // 2594164
FIELD: chemistry. SUBSTANCE: invention relates to a method of producing crystalline polymorph of 1-(2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl)benzylcarbamoyl)-1-proline-N,N-dimethylamide, comprising steps of: i) adding 1-(2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl)benzylcarbamoyl)-1-proline-N,N-dimethylamide to an organic solvent, where organic solvent is an aqueous organic solvent; ii) heating mixture to temperature of 40-60 °C until an emulsion is formed; iii) cooling emulsion to temperature of 20-35 °C until a clear solution is obtained; iv) stirring clear solution until a suspension is obtained; and v) isolating resulting crystalline form of 1-(2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl)benzylcarbamoyl)-1-proline-N,N-dimethylamide. Method is suitable for implementation on an industrial scale. EFFECT: method provides good reproducibility and stable production of product which can be used for preparing a drug. 6 cl, 3 dwg, 1 tbl, 1 ex

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

Substituted phenyl-containing compounds // 2592696
FIELD: chemistry. SUBSTANCE: invention relates to novel substituted phenyl-containing compounds of formula (VI), which are used as intermediate products for producing 6-substituted derivatives of 1-(2H)-isoquinolinone derivatives. EFFECT: production of 6-substituted derivatives of 1-(2H)-isoquinolinone derivatives. 20 cl, 3 tbl, 1 ex

Bi-aryl-meta-pyrimidine kinase inhibitors // 2589878
FIELD: chemistry.SUBSTANCE: invention relates to a novel compound of formula 32 and to a method of producing a compound of formula XLV using a compound of formula 32 as a starting compound. Compounds of formula XLV can inhibit kinase family of JAK-kinase, in particular JAK2 kinase. Compounds XLV can be used for treating myeloproliferative disease, in treating idiopathic polycytemia, primary thrombocytopenia, myeloid fibrosis, proliferative diabetic retinopathy, cancer or eye disease. Compound of formula 32 corresponds to structural formula given below. Method of producing a compound of formula XLV involves reaction of 3-bromo-N-tert-butylbenzosulphonamide with a compound of formula 32. Method involves cleaning reaction mixture obtained at step of reacting a compound of formula 32 with 3-bromo-N-tert-butylbenzosulphonamide for extraction of compound of formula XLV.EFFECT: obtaining a compound of formula XLV using compound of formula 32 as a starting compound.3 cl, 2 dwg, 3 tbl, 246 ex

Quinoxalines and azaquinoxalines as crth2 receptor modulators // 2589709
FIELD: chemistry.SUBSTANCE: invention relates to compound of formula (IC) and pharmaceutically acceptable salts thereof. Disclosed compounds have properties of CRTH2 receptor modulators. In formula (IC) R1 represents -C(O)-N(R6a)(R6b); I) R6a is H, and R6b represents a) -Q-RAH, where RAH is phenyl, and where RAH is unsubstituted or substituted with one fragment R8, selected from group consisting of fluorine and -CN; Q is selected from group consisting of (i) link; (ii) , where Re denotes H, and R(f) is H or methyl; b) -Q-RHC, where RHC is C5-C6 cycloalkyl, where said C5-C6 cycloalkyl forms condensed cycle with benzene ring and where RHC is unsubstituted or substituted with 1-2 fragments of R12, independently selected from group consisting of halogen and -CN; II) or R6a and R6b together with N atom to which they are bonded form R6h, where R6h is pyrrolidinyl, piperidinyl or piperazinyl, where R6h is substituted with -Z-RCY, Z is bond and RCY is unsubstituted phenyl or phenyl, substituted with 1-2 fragments of R10, selected from group consisting of halogen and -CN; R6H optionally substituted with 1-2 fragments in R9, where each fragment R9 is independently C1-C3 alkyl, halogen or -CN, and R2 is unsubstituted phenyl. Invention also relates to pharmaceutical composition for treating asthma or allergic rhinitis and method of treating asthma or allergic rhinitis.EFFECT: technical result is obtaining novel compounds which can be used to treat asthma or allergic rhinitis.10 cl, 2 tbl, 44 ex

elanocortin receptor modulators, method for production thereof and use thereof in medicinal and cosmetic preparations for human use // 2589056
FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry, namely to heterocyclic compound of formula (I), as well as to its pharmaceutically acceptable salt and enantiomer, where R1 is a hydrogen atom, phenyl, linear saturated hydrocarbon chain containing 1-5 carbon atoms, cycloalkyl containing 5-6 carbon atoms, or straight saturated hydrocarbon chain containing 1-4 carbon atoms, substituted cycloalkyl containing 3 carbon atoms; R2 is hydrogen atom, hydroxyl, linear saturated hydrocarbon chain containing 1-5 carbon atoms, straight saturated hydrocarbon chain containing 1-4 carbon atoms, substituted cycloalkyl containing 3-7 carbon atoms, oxygen atom, substituted linear saturated hydrocarbon chain containing 1-4 carbon atoms, an oxygen atom, substituted carbonyl, substituted linear saturated hydrocarbon chain containing 1-4 carbon atoms, carbonyl, substituted linear saturated hydrocarbon chain containing 1-4 carbon atoms, or cycloalkyl containing 6 carbon atoms, carbonyl, substituted by oxygen atom, substituted linear saturated hydrocarbon chain containing 1-4 carbon atoms, Carbonyl, substituted monoalcylamino, alkyl which is linear saturated hydrocarbon chain containing 1 carbon atom, carboxyl group, cyano group or amino group, bisubstituted phenyl or linear hydrocarbon chain containing 1-4 carbon atoms; R3 is linear saturated hydrocarbon chain containing 1 carbon atom, substituted phenyl, possibly substituted with one or two groups, selected from halogen and oxygen, substituted linear saturated hydrocarbon chain containing 1 carbon atom; R4 is linear saturated hydrocarbon chain containing 1-4 carbon atoms, substituted imidazole, unsubstituted or substituted linear saturated hydrocarbon chain containing 1 carbon atom; R5 represents hydrogen atom or linear hydrocarbon chain containing 1-4 carbon atoms; X represents oxygen atom or sulphur atom; n, m equals to 1 or 2. Invention also relates to use of formula (I), pharmaceutical and cosmetic compositions based on compound of formula (I).EFFECT: technical result is obtaining novel heterocyclic compounds, useful as modulators of melanocortin receptors.21 cl, 2 dwg, 1 tbl, 26 ex

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

Diaminopyrimidine derivatives and methods for production thereof // 2587493
FIELD: pharmaceutics.SUBSTANCE: present invention relates to a novel diaminopyrimidine derivative formula 1 or pharmaceutically acceptable salts thereof possessing properties of agonist of 5-HT4 receptors. In formula 1 (Formula 1)R1 denotes a phenyl group substituted with one or more substitutes selected from a group consisting of hydroxy, amino, halogen, cyano, nitro, C1-5alkyl (where C1-5alkyl is optionally substituted with halogen), C1-5alkoxy, C1-5alkylthio, C1-5alkoxycarbonyl, aminosulphonyl and benzyloxycarbonylamino; or heteroaryl group selected from a group comprising pyridinyl, quinolinyl, chromenonyl, indolyl, indolinyl and benzimidazolyl, wherein heteroaryl group can be optionally substituted with one or more substitutes selected from a group consisting of C1-5alkyl (where C1-5alkyl is optionally substituted with halogen) and acetyl, R2 denotes hydrogen; C1-5alkyl group, optionally substituted with a substitute selected from a group consisting of hydroxy, C1-5alkoxy, benzylamino (where benzylamino is optionally substituted by halogen), phenylamino, C1-5alkylamino, C3-6cycloalkylamino and hydroxy-C1-5alkylamino; C1-5alkoxycarbonyl group or formyl group, R3 denotes hydrogen, hydroxyl group; C1-5alkyl group, optionally substituted with a substitute selected from a group consisting of C1-5alkoxycarbonylamino and di-C1-5alkylamino, or group selected from a group consisting of following formulae A, B, D and E (where symbol * in formulae A, B, D and E denotes position of attachment of said group of compounds of formula 1),R4 denotes hydrogen, R5 denotes C1-5alkyl group, optionally substituted phenyl or C2-6alkenyl group, optionally substituted phenyl or C3-6cycloalkyl, R6 denotes C1-10alkyl group, optionally substituted with a substitute selected from a group consisting of hydroxy, halogen, C1-5alkoxy, amino, C1-5alkoxycarbonylamino, benzyloxycarbonylamino, di-C1-5alkylamino, C1-5alkoxy-C1-5alkyloxy, phenoxy, benzyloxy, phenyl (where phenyl is optionally substituted with one or more substitutes selected from a group consisting of halogen, amino and C1-5alkoxy), thiophenyl, pyridinyl, piperidinyl, piperazinyl (where piperazinyl is optionally substituted with benzyl) and acetyl; C3-6cycloalkyl group; piperidinyl group; C1-10alkenyl group, optionally substituted phenyl; trifluoromethyl group, trifluoroethyl group or a phenyl group optionally substituted with halogen, R7 denotes hydrogen, R8 and R9 each independently denote hydrogen; C1-10alkyl group, optionally substituted with substitute selected from a group consisting of amino, C1-5alkoxycarbonylamino, hydroxy, C1-5alkylthio, C3-10cycloalkyl, phenyl (where phenyl is optionally substituted with one or more substitutes selected from a group consisting of hydroxy, C1-5alkyl, mono-or di-C1-5alkylamino, trifluoromethyl, halogen, C1-5alkoxy C1-5alkylcarbonyloxy), thiophenyl, pyrrolyl, furanyl (where furanyl is optionally substituted with mono-or di-C1-5alkyl), pyridinyl and benzyloxy; piperidinyl group, optionally substituted benzyl, benzoyl, C1-5alkyl or C1-5alkylcarbonyl; azetidinyl group, optionally substituted C1-5alkoxycarbonyl; C1-5alkylsulphonyl group or C3-10cycloalkyl group.EFFECT: invention relates to use of formula 1 or its pharmaceutically acceptable salt for preparing a drug for preventing or treating gastrointestinal motility dysfunction; gastrointestinal motor dysfunction is gastroesophageal reflux disease (GERD), lock (constipation), irritable bowel syndrome (IBS), dyspepsia, postoperative intestinal obstruction, prolonged gastric emptying, gastroparesis, intestinal pseudo-obstruction,drug-induced delayed transit content over colon or diabetic gastroparesis.9 cl, 54 tbl, 495 ex

esoionic pyrido [1,2-a] pyrimidine pesticides // 2585616
FIELD: chemistry.SUBSTANCE: invention relates to novel compounds which are N-[(5-pyrimidinyl)methyl] -2-pyridinamine and N-(5-pyrimidinylmethylene) -2-pyridinamine. In compounds of formula 1 R1 is phenyl or pyridinyl, each optionally substituted with (Q) and has up to 3 substitutes, and Q is phenyl or pyridinyl, each of which optionally has up to 5 substitutes.EFFECT: compounds can be used as intermediate compounds for producing compounds of formula 1, having activity in invertebrate pests or for growth of cultivated plants.3 cl, 50 tbl, 2 ex
Some chemical compounds, compositions and methods // 2582676
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to new compounds of formula V-A or their pharmaceutically acceptable salts possessing the properties of PI3-kinase (phosphatidylinositol-3-kinase) activity inhibitors. The compounds can find application for treating diseases and conditions associated with PI3-kinase activity, particularly in a T-cell, B-cell, mastocyte, dendritic cell, or neutrophil. This disease represents one or more diseases specified in cancer, a bone disorder, inflammatory disease, immune disease, respiratory disease or thrombosis. Cancer represents leukaemia or lymphoma, or cancer is specified in acute myeloid leukaemia, chronic lymphocytic leukaemia and multiple myeloma, where lymphoma represents non-Hodgkin lymphoma; an inflammatory or immune disorder is asthma, allergy, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, systemic lupus erythematosus, or graft-versus-host disease. The compound of formula V-A, or its pharmaceutically acceptable salt, or a composition can be used in a combination with rapamycin. In formula V-A:B represents a group of formula wherein Wc represents phenyl, 6-merous heterocyclyl with one heteroatom specified in oxygen or nitrogen, or C3-C6cycloalkyl; q is equal to 0 or 1; R1 represents hydrogen, C1-C4alkyl or halogeno; R2 represents halogeno or C1-C4alkyl optionally substituted by halogeno; R3 represents halogeno; R9 represents hydrogen or C1-C4alkyl.EFFECT: producing the new compounds for treating the diseases or conditions associated with PI3-kinase activity.62 cl, 19 dwg, 6 tbl, 55 ex
Pyrazole compounds as sigma receptor inhibitors // 2582338
FIELD: medicine.SUBSTANCE: invention refers to compounds of general formula (1) shown below, or their pharmaceutically acceptable salts having pharmacological activity towards sigma receptor, to methods for producing these compounds and to pharmaceutical compositions containing them, and to using them for treating and/or preventing sigma receptor-related diseases. In the compounds of formula (I), R1 represents phenyl substituted by halogen atoms; naphthyl; C5-6 cycloalkyl; or quinolyl; R2 and R3 are independently specified in H and C1-6 alkyl group; R4 and R5 together with the nitrogen atom to which they are attached, form a substituted or unsubstituted 5-6-merous heterocyclyl group with one or two heteroatoms specified in O or N, wherein the substitute is specified in C1-6alkyl and C1-6alkanoyl; X represents an oxygen atom or a CH2 group; m is specified in 1, 2, 3 and 4; and n is specified in 1, 2, 3 and 4.EFFECT: higher efficacy.13 cl, 2 tbl, 50 ex
Triazole derivatives as gaba receptor ligands // 2582337
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts. The compounds of formula (I) possess GABA A α5 receptor affinity and selectivity. In formula A represents -CH2-O- or -CH=CH-; X represents S or CH; Y represents O, NR9 or CR9, provided X represents S, then Y represents CR9, and if X represents CH, then Y represents O or NR9; each of u and v represents a single bond or double bond provided both u and v are other than double bonds, and both are other than single bonds; R1, R2 represent C1-7-alkyl, phenyl, optionally substituted halogeno, or 6-merous heteroaryl containing one ring N heteroatom; one of R1 and R2 represents C1-7-alkyl; R3 represents -C(O)NR5R6. The invention also refers to pharmaceutical compositions containing an effective amount of the compound of the invention and using the compounds for producing medicinal products.EFFECT: new compounds of formula (I) possessing GABA A α5 receptor affinity and selectivity are produced.16 cl, 1 tbl, 11 ex

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

Fungicidal pyrazoles // 2577247
FIELD: chemistry.SUBSTANCE: invention object is formula compounds and their salts, where Q1 represents phenyl or pyridyl ring, which can contain optional substituents, given in the invention formula, Q2 represents phenyl, pyridyl or pyrimidyl ring, which can contain optional substituents, given in the invention formula; X represents O, NR4, CR15R16 or C(=O); and R1, R1a, R2, R4, R15 and R16 have designations, given in the invention formula.EFFECT: invention relates to fungicidal compositions, containing Formula 1 compounds, and to method for controlling plant diseases, caused by fungal pathogen, and to intermediate compounds of Formula , and their salts, where X represents NH; and Q1, Q2 and R2 are determined for Formula 1.18 cl, 794 tbl, 8 ex
 
2551138.
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