Containing three or more hetero rings (C07D401/14)

C   Chemistry; metallurgy(318327)
C07   Organic chemistry(61593)
C07D401/14                     Containing three or more hetero rings(572)
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
Amide derivatives as grp119 agonists // 2642429
FIELD: pharmacology.SUBSTANCE: invention relates to an amide derivative of the following formula 1, its stereoisomers or its pharmaceutically acceptable salts of formula 1, wherein X1, X2, X3, X4, X5, X6, X7 and X8 each independently is C or N; R1 is -F or -C1-3-perfluorinated alkyl; R2 and R3 each is independently selected from the group consisting of halogen, -C1-5-alkyl and C3-6-cycloalkyl, wherein -C1-5-alkyl and C3-6cycloalkyl independently of one another may be unsubstituted or substituted by halogen, -CN, -OC1-5-alkyl or-C1-5-alkyl, or R2 and R3 together with the carbon atom to which they are attached, can form C3-6-cycloalkyl, where C3-6cycloalkyl may be unsubstituted or substituted by halogen, -OC1-5-alkyl or -C1-5-alkyl; R4 and R5 each independently is H, halogen or -C1-5-alkyl; R6 and R7 each independently is H, halogen, -C1-5-alkyl or -CN; R8 means methyl; R9 means H, halogen or OH; and m is 1 or 2. The invention also relates to individual compounds and to a pharmaceutical composition.EFFECT: new compounds of formula 1 are obtained that have the properties of GPR119 agonists, which can be used in diabetes mellitus treatment.7 cl, 15 tbl
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
5-(pyridine-2-ylamino)-pyrasin-2-carbonitrile compounds and their therapeutic application // 2641693
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the formula , as well as to pharmaceutical compositions based thereon for use in the treatment of a disease or condition mediated by SNK1.EFFECT: new compounds are obtained that inhibit the kinase function of kinase 1 of the control point.37 cl, 2 dwg
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
Partly saturated nitrogen-containing heterocyclic compound // 2641291
FIELD: chemistry.SUBSTANCE: invention relates to a compound of the formula (I'), (wherein W represents the formula -CR11R12CR13R14-; R11 represents a hydrogen atom, a fluorine atom, C1-4 alkyl or phenyl; R12 represents a hydrogen atom, a fluorine atom or C1-4 alkyl; provided that R11 and R12, together with the adjacent carbon atom, optionally form C3-8 cycloalkane or tetrahydropyran; R13 represents a hydrogen atom, a carbamoyl, C1-4 alkyl (C1-4 alkyl is optionally substituted by one group selected from the group consisting of hydroxy, C1-3 alkoxy and di-C1-3 alkylamino), halo-C1-4 alkyl, phenyl, pyridyl, benzyl or phenethyl; R14 represents a hydrogen atom, C1-4 alkyl or halogen-C1-4 alkyl; Y represents a single bond or C1-6 alkanediyl (C1-6 alkanediyl is optionally substituted by one hydroxy group and one of the carbon atoms in C1-6 alkanediyl is optionally substituted by cycloalkpropane-1,1-diyl); R2 represents a hydrogen atom, C1-6 alkyl, C3-8 cycloalkyl {C3-8 cycloalkyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl (C1-6 alkyl is optionally substituted by one phenyl group), phenyl (phenyl is optionally substituted by one halogen atom), C1-6 alkoxy [C1-6 alkoxy is optionally substituted by one group selected from the group consisting of C3-8 cycloalkyl, phenyl (phenyl is optionally substituted by one group selected from the group consisting of a halogen atom and C1-6 alkyl) and pyridyl (pyridyl is optionally substituted by one halogen atom)], C3-8 cycloalkoxy, phenoxy (phenoxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl, C3-8 cycloalkyl and halogen-C1-6 alkyl) and pyridyloxy (pyridyloxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl, C3-8 cycloalkyl and halogen-C1-6 alkyl)}, phenyl (phenyl is optionally substituted by one to three groups that are the same or different and which are selected from the group of α3 substituents), naphthyl, indanyl, tetrahydronaphthyl, pyrazolyl [pyrazolyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl and phenyl (phenyl optionally substituted by one C1-6 alkyl)], imidazolyl [imidazolyl is optionally substituted by one or two groups that are the same or different and are selected from the group consisting of C1-6 alkyl and phenyl], isoxazolyl [isoxazolyl is optionally substituted by one phenyl group (phenyl is optionally substituted by one halogen atom)], oxazolyl [oxazolyl is optionally substituted by one or two groups that are the same or different and which are selected from the group consisting of C1-6 alkyl and phenyl], thiazolyl [thiazolyl is optionally substituted by one or two groups that are the same or different and which are selected from the group consisting of C1-6 alkyl, phenyl and morpholino], pyridyl (pyridyl is optionally substituted by one or two groups that are are the same or different and are selected from the group of α5 substituents), pyridazinyl [pyridazinyl is optionally substituted by one C1-6 alkoxy (C1-6 alkoxy is optionally substituted by one C3-8 cycloalkyl group)], pyrimidinyl [pyrimidinyl is optionally substituted by one group selected from the group consisting of halogen-C1-6 alkyl, C3-8 cycloalkyl, phenyl and phenoxy (phenoxy is optionally substituted by one C1-6 alkyl)], pyrazinyl [pyrazinyl is optionally substituted by one group selected from the group consisting of C1-6 alkoxy (C1-6 alkoxy is optionally substituted by one C3-8 cycloalkyl), and phenoxy (phenoxy is optionally substituted by one group selected from the group consisting of a halogen atom, C1-6 alkyl and C3-8 cycloalkyl)], benzothiophenyl, quinolyl, methylenedioxyphenyl (methylenedioxyphenyl is optionally substituted by one or two fluorine atoms), azetidinyl (azetidinyl is optionally substituted with one pyrimidinyl group), piperidinyl (piperidinyl is optionally substituted by one group selected from the group consisting of pyrimidinyl, phenyl-C1-3 alkyl, C3-8 cycloalkyl-C1-3 alkylcarbonyl and phenyl-C1-3 alkoxycarbonyl) or the following formula (I") -CONR5CH2-R6 (I") [wherein in formula (I") R5 represents a hydrogen atom or C1-3 alkyl and R 6 is phenyl (phenyl is optionally substituted by one group selected from the group consisting of a halogen atom, halogen-C1-6 alkyl and phenyl)], Y4 represents C1-4 alkanediyl; R3 represents a hydrogen atom or methyl; R4 represents -COOH or -CONHOH).EFFECT: compound has a superior PHD2 inhibitory effect.16 cl, 28 tbl, 11 ex
Pyridine derivative // 2640588
FIELD: pharmacology.SUBSTANCE: invention relates to a pyridine derivative of formula (I) , a prodrug thereof, wherein A is a single bond or an oxygen atom; R1 represents a nitrogen atom or CH; one of X1-X5 is a nitrogen atom, and the remaining four are CR2; R2 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, an alkynyl group having 2 to 6 carbon atoms, a halogen atom, a trifluoromethyl group, a difluoromethyl group, a cyano group, an alkylcarbonyl group having 2 to 7 carbon atoms, an alkylsulfonyl group having 1 to 6 carbon atoms, a nitro group, an amino group, a dialkylamino group having 1 to 6 carbon atoms which optionally can form a ring, a formyl group, an alkoxy group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group, a phenyl group, a cyclohexyl group and a halogen atom), an alkylthio group having 1 to 6 carbon atoms, a phenyl a group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom) or a phenoxy group (which may optionally have one or more substituents selected from an alkyl group having 1-6 carbon atoms, an alkoxy group having 1-6 carbon atoms, and a halogen atom), provided that when two CR2 are located side by side, two R2 substituents can be optionally combined with cycle formation; R3 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group, an amino group, a dialkylamino group having 1 to 6 carbon atoms which can optionally form a ring, an imidazole ring, a pyrazole ring, a pyrrolidine ring, a piperidine ring, a morpholine ring and a piperazine ring (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms and alkylsulfonyl group containing from 1 to 6 carbon atoms), an alkenyl group having 2 to 6 carbon atoms, an alkynyl group having 2 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms (which may optionally have one or more substituents selected from a hydroxyl group and a halogen atom), an alkylcarbonyl group having 2-7 carbon atoms, an alkylthio group having 1-6 carbon atoms, an alkylsulfinyl group having 1-6 carbon atoms, a halogen atom, a trifluoromethyl group, a difluoromethyl group, a cyano group, a phenyl group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a pyridyl group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a phenoxy group (which may optionally have one or more substituents selected from an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms and a halogen atom), a carboxyl group, or -CO2 R5; R4 represents a carboxyl group, a tetrazolyl group, -CONHSO2R5, -CO2R5 or any of the following substituents: , provided that when R3 represents an alkyl group having 1 to 6 carbon atoms substituted by a hydroxyl group, and when R4 represents a carboxyl group, then R3 and R4 can optionally be combined to form a lactone cycle; R5 in R3 and R4 each independently represents an alkyl group having 1 to 6 carbon atoms; Z is any of the following substituents, designated as Z1-Z7 (their meanings are defined in claim 1) that can be used to treat or prevent diseases associated with URAT1 such as gout, hyperuricemia, hypertension, kidney diseases such as interstitial nephritis, diabetes, arteriosclerosis and Lesch-Nyhan syndrome.EFFECT: compound application efficiency increase.23 cl, 55 tbl, 303 ex

Crystalline polymorphyl of 4-[5-(pyridine-4-yl)-1h-1,2,4-triazol-3-yl]-pyridine-2-carbonitrile and method of its obtaining // 2639149
FIELD: chemistry.SUBSTANCE: invention relates to type I crystals of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile showing characteristic peaks in X-ray powder diffractometry at diffraction angles 2θ of about 10.1°, 16.0°, 20.4°, 25.7° and 26.7°. The invention also relates to a method of obtaining type I crystals.EFFECT: new crystals with higher solubility and higher thermal stability are obtained, compared to its hydrate and type II crystals.2 cl, 8 dwg, 4 ex

Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods for application // 2638552
FIELD: pharmacology.SUBSTANCE: invention relates to pyrazol-4-yl-heterocyclylcarboxamide compounds of Formula I , including their stereoisomers, tautomers and pharmaceutically acceptable salts, wherein X is a thiazolyl, pyrazinyl, pyridinyl or pyrimidinyl group, R1 and R2 have the meanings indicated in the claims. The compounds of formula I are useful for Pim kinase inhibition and for treatment of disorders such as cancer mediated by Pim kinase. Methods for application of formula I compounds for in vitro, in situ and in vivo diagnosis, prevention or treatment of such diseases in mammalian cells or acssociated pathological conditions are disclosed.EFFECT: increased efficiency of treatment.26 cl, 4 tbl, 528 ex

Derivative cyclic amine and its pharmaceutical application // 2638549
FIELD: pharmacology.SUBSTANCE: invention refers to derivatives if cyclic amine of formula (I), where A is a group, represented by the general formula (IIa), (IIb) or (IIc), where A is a group, provided by the general formula (IIa) or (IIb), R1 represents an alkyl group containing 1 or 2 carbon atoms and optionally substituted by a hydroxyl group, amine group or carboxyl group, R2 represents a hydrogen atom, R3 is a hydrigen atom or alkyl group containing 1 or 2 carbon atoms, R4 is a hydrogen atom or an alkylcarbonyl group, containing 2 carbon atoms, or an alkyl group, containing 1 or 2 carbon atoms and optionally substituted by alkylcarbonylamine group, containing 2 carbon atoms, and n is 1 or 2, in which, when R3 and R4, each independently represent an alkyl group, containing 1 or 2 carbon atoms, R1 represents an alkyl group containing 1 or 2 carbon atoms and substituted by a hydroxyl group, amine group or carboxyl group; and when A is a group, represented by the general formula (IIc), R1 represents an alkyl group, containing 1 carbon atom and substituted by a carboxyl group, R2 represents a hydrogen atom and X represents CH2, O or -NR5 and R5 is an alkyl group, containing 1 carbon atom. Also, the invention relates to a prodrug of the compound of formula (I), pharmaceutical, analgetic agent and therapeutic agent based on compounds of formula (I), or its prodrug.EFFECT: new derivatives of imidazol, useful in the treatment of pain, have been obtained.11 cl, 24 dwg, 5 tbl, 73 ex
Dna-pk inhibitors // 2638540
FIELD: biotechnology.SUBSTANCE: invention relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, inhibiting DNA-dependent protein kinase (DNA-PK). The compounds can be used in the treatment of cancer. The compounds have a radiosensitizing effect on the line of cancer cells sensitive to radiation and can be used to enhance the effect of the therapeutic regimen for the treatment of cancer. In general formula (I), X is N or CRA5; RA1is F, C1-4-alkyl, C3-5cycloalkyl, OC1-4-alkyl, OC1-4-alkyl-C3-5cycloalkyl, NH2, NHC1-4-alkyl, NHC1-4-alkyl-C3-5cycloalkyl or C0-4-alkylheterocyclyl, the said heterocyclic ring system being selected from oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, or morpholinyl, and each of the said alkyl, cycloalkyl or heterocyclyl is optionally substituted with a maximum of three F atoms, a maximum of three 2H atoms, a maximum of two non-hemin OH groups, or a maximum of two OC1-2-alkyl; each RA4 is independently H or 2H; RA5 is hydrogen, F, C1-4-alkyl or OC1-4-alkyl, each of the said alkyls being optionally substituted with a maximum of three F atoms or a maximum of three 2H atoms; RB3 is C (O) NHC1-4-alkyl. The said alkyl is optionally substituted with a maximum of three F atoms, a maximum of three 2H atoms, a maximum of two non-hemin OH groups, or a maximum of two OC1-2-alkyl; and each RB4 is independently hydrogen, deuterium, F, or C1-4-alkyl.EFFECT: improved compound properties.18 cl, 3 tbl, 14 ex
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
Substituted pyrrolidines as xia factor inhibitors for thromboembolic diseases treatment // 2636050
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the general formula , their pharmaceutically acceptable salts, pharmaceutical compositions containing the said compounds.EFFECT: compounds of general formula I are XIa factor inhibitors and are suitable for thromboembolic diseases prevention or treatment.22 cl, 1 tbl, 115 ex
Fluoroquinolones based on 4-deoxypyridoxine // 2634122
FIELD: pharmacology.SUBSTANCE: invention relates to new fluoroquinolone derivatives of the general formula (I), where R1 = ; R2 = H; R3 = ; or R1 = C2H5; R2 = H; R3 = ; or R1 = C2H5; R2 = F; R3 = ; or R1 = ; R2 = OCH3; R3 = .EFFECT: new fluoroquinolone derivatives with antibacterial activity.2 tbl, 6 ex
New inhibitors of serine-threonine kinases, including for treatment of oncological diseases and tuberculosis // 2633032
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the general formula or n=0-2; A is independently selected and is a 5-7-membered aromatic heterocycle containing 1-2 N atoms and 0-1 S atom; A contains 0-2 R substituents; R is independently selected and represents methyl or ethyl; B is independently selected and represents phenyl, 5-6-membered heteroaryl cycle containing 0-2 N atoms and 0-1 S atom, or 5-6-membered cycloalkyl containing 0-2 N atoms and 0-1 S atom; B contains 0-3 R1 substituents; C is independently selected and represents phenyl, -NH2, -NH-C1-3-alkyl, -NH (C1-3-alkyl) C1-3-alkyl, a 5-6-membered heteroaryl cycle containing 0-2 N atoms and 0-1 S atom, or a 5-6-membered cycloalkyl containing 0-2 N atoms and 0-1 S atom; C contains 0-3 R1 substituents; R1 is independently selected and represents -C1-6-alkyl, halogen, phenyl, -C5-7-heteroaryl containing 1-2 N atoms and 0-1 S atom, -COOH, -CONH2, -NH2 or -NHR2; R2 is independently selected and represents -C1-6-alkyl, -C (O) -C1-8-alkyl; the linker X is independently selected and is -CH2-, -C(=O)-CH2- or -CH2-O-group; the linker Q is independently selected and represents -NH- or -NH-C(O) -group; the Y linker is independently selected and represents -O-(CH2) m or -C(O)-NH-(CH2)m, where m=1-3; Z is independently selected and represents -CH2- group or an oxygen atom.EFFECT: compounds are prospective for use in the therapy of diseases associated with the activity of serine-threonine kinases.13 cl, 2 tbl, 16 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
Pyrazole derivative // 2632884
FIELD: pharmacology.SUBSTANCE: in the above formula , A represents a phenyl group which may be unsubstituted or substituted by 1 to 3 Q groups which are identical or different and are selected from the group consisting of a halogen atom, C1-6alkyl, C3-7cycloalkyl, C1-6haloalkyl, phenyl, -O-R2 and -O-C1-6haloalkyl; X and Z are CH and Y is a nitrogen atom; R is a hydrogen atom; R1 is a hydrogen atom and R2 is a hydrogen atom or C1-6alkyl group.EFFECT: compound has an inhibitory effect on xanthine oxidase, is well suited for treatment or prevention of diseases associated with xanthine oxidase such as gout, hyperuricemia, tumor lysis syndrome, stones in the urinary tract, hypertension, dyslipidemia, diabetes, cardiovascular disease, kidney disease, respiratory tract disease, autoimmune diseases, inflammatory bowel disease.10 cl, 7 tbl, 112 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

Crystalline form i of tyrosine kinase inhibitor dicaletat and method for its preparation // 2631321
FIELD: pharmacology.SUBSTANCE: invention relates to the crystalline form I of (R,E)-N-(4-(3-chloro-4-(pyridin-2-yl-methoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide dimaleate, a method for its preparation, a pharmaceutical composition based thereon, and its use.EFFECT: resulting crystalline form I of dimaleate has good crystal stability and chemical stability and can be used to prepare drugs for treatment of diseases associated with EGFR tyrosine protein kinase or HER-2 receptor tyrosine protein kinase.7 cl, 4 dwg, 2 tbl, 7 ex
Compounds // 2630677
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of the general formula ,where Cyc1 is imidazolyl or triazolyl; Cyc2 is phenyl; Cyc3 is phenyl or 5-10 membered heteroaryl containing 1 heteroatom selected from S and N; R1 is halogen; s is equal to 0 or 1, R2 is hydrogen; R3 is hydrogen, C1-8 alkyl or C1-8 alkyl which is substituted by a group selected from pyridyl or -OC1-8 alkyl; Y is N or C (R5); R4 is hydrogen or C1-4 alkyl; R5 is hydrogen or halogen; or R3 and R4 can be taken together to form C2 alkylene; where one carbon of the alkylene chain can be replaced by sulfur; R6 is C1-8 alkyl, Cyc10, halogen or Cyc10 substituted by halogen or cyano, wherein Cyc10 is a 5-membered heteroaryl containing 3-4 nitrogen atoms; m is equal to 2, where each R6 can be the same or different; R7 is halogen, -NH2, -COOR48, -NHC (O) O-C1-8 alkyl, -NHC (O) O-C1-4 alkylene-OC1-8 alkyl; R48 is hydrogen or C1-8 alkyl; n is equal to 1 or 2, where n is an integer 2, each R7 can be the same or different; and R62 is hydrogen, their pharmaceutically acceptable salts or solvates thereof.EFFECT: compounds are factor XIa inhibitors, so they can be used to prevent or treat thromboembolic diseases.15 cl, 3 tbl, 927 ex

Substituted benzene compounds // 2629118
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (Ie) or pharmaceutically acceptable salts thereof: where Z is NR7R8 or S(O)aR7, where a is 0; R1 is H or C1-C6 alkyl optionally substituted with one or more substituents selected from hydroxyl, C1-C6 alkoxy; Each of R2 and R4 is independently -Q1-T1, wherein Q1 is a bond or a C1-C3 alkyl linker optionally substituted with one or more substituents selected from halogen and hydroxyl, and T1 is H, C1-C3 alkyl; R3 is H or halogen; R5 is H or C1-C6 alkyl; R6 is H, halogen, -C(O)NRaRb or RS2, where RS2 is C1-C6 alkyl or 4-12 membered heterocycloalkyl containing from 0 to 3 heteroatoms in the ring selected from O, N or S, and Wherein each of Ra and Rb is independently H, C1-C6 alkyl or Ra and Rb together with the N atom to which they are attached form a 4-12 membered heterocycloalkyl ring containing 0 or 1 additional heteroatom selected from O, N or S; R7 is -Q4-T4, wherein Q4 is a bond or a C1-C4 alkyl linker and T4 is H, C1-C6 alkyl, C3-C8 cycloalkyl, C(O)-C1-C6 alkyl or 4-14 membered heterocycloalkyl, Containing 1 to 3 ring heteroatoms selected from O, N or S, each of which is optionally substituted with one or more -Q5-T5, wherein Q5 is a bond, C(O), C(O) NRk, NRkC(O) or a C1-C3 alkyl linker, wherein Rk is H or C1-C6 alkyl, and T5 is H, C1-C6 alkyl; R8 is H, C1-C6 alkyl optionally substituted with halogen or C1-C6 alkoxy, C2-C6 alkenyl, C3-C8 cycloalkyl or 4- to 7-membered heterocycloalkyl containing 1-3 heteroatoms in the ring selected from O, N or S; or R7 and R8 together with the N atom to which they are attached form a 4-12 membered heterocycloalkyl ring containing 0-2 additional heteroatoms selected from O, S or N and a 4-12 membered heterocycloalkyl ring that forms R7 and R8 is optionally substituted with one or more -Q6-T6, wherein Q6 is a bond or a C1-C3 alkyl linker and T6 is H, halogen, C1-C6 alkyl; and R12 is halogen, C1-C6 alkoxyl, C2-C6 alkenyl or C1-C6 alkyl optionally substituted with halogen.EFFECT: compounds are used to treat cancer.24 cl, 4 tbl, 47 ex
New azetidine derivatives // 2629114
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula , where one of A1 and A2 is -NR9-, and the other is -CH2-; R1 is halogen; R2 is hydrogen; R3 is hydrogen, halogen; R4 and R5 together with the carbon atom to which they are attached form C3-C6-cycloalkyl; R6 is halogen; R7 is hydrogen; R8 is hydrogen, halogen, C1-C6-alkoxy, halo-C1-C6-alkoxy or substituted heterocyclyl, wherein the heterocyclyl is pyridinyl, pyrazolyl, wherein the substituted heterocyclyl is heterocyclyl substituted with one to three substituents independently selected from C1-C6-alkyl; and R9 is hydrogen, C1-C6-alkyl, halo-C1-C6-alkyl, formyl or C1-C6-alkoxycarbonyl.EFFECT: compounds have cathepsin S or L cysteine protease inhibitor activity and can be used to treat or prevent diseases associated with cathepsin S or L cysteine protease.15 cl, 1 tbl, 53 ex
Compound as wnt signal inhibitor, its compositions and application // 2627712
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic compound of the general formula (I) or an N-oxide thereof, wherein X1, X2, X3 and X4 independently represent CR4 or N, where 0 or 1 of X1-X4 can be N; Y1, Y2 and Y3 are hydrogen; R1 is selected from hydrogen, , C6 aryl, 6-member heterocycloalkyl containing 2 heteroatoms selected from N and O, and 5- or 6-member heteroaryl containing 1-4 heteroatoms selected from N, O and S, wherein each of C6 aryl, 6-member heterocycloalkyl and 5- or 6-member heteroaryl may be optionally substituted with one R4; R2 is selected from hydrogen, halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl and 6-member heteroaryl may be optionally substituted with one R4. If X5 is N, R2 is selected from halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl, and 6-member heteroaryl may be optionally substituted with one R4; each R4 Is independently selected from hydrogen, halogen, cyano, oxo, C1-6 alkoxy, -C(O)OR5, -C(O)R5, C1-6 alkyl. Moreover , C1-6 alkyl may be optionally substituted with 1 to 3 substituents selected from halogen and cyano; R5 is C1-6 alkyl; and where the central structure of Formula I, limited by X5, X6, X7 and X8, is: or The invention also relates to particular compounds, a method for inhibiting the secretion of WNT signalling in a cell, use of a compound of formula (I), a method for treatment of a disorder mediated by WNT. .EFFECT: new heterocyclic compounds have been obtained that are useful for treatment of cancer, fibrosis and osteoarthritis.22 cl
Derivatives of indolin-2-she as inhibitors of proteinkinas // 2627706
FIELD: pharmacology.SUBSTANCE: invention relates to indoline-2-one derivatives, the formula A, which are protein kinase inhibitors for the treatment of hyperproliferative diseases such as lung cancer, colorectal cancer, liver cancer and acute myelomonocytic leukemia.EFFECT: increased efficiency of treatment.15 cl, 3 dwg, 6 tbl, 1 ex
Compounds of pyridazinamide and their use as synthetic syneckinasis inhibitors (syk) // 2627661
FIELD: chemistry.SUBSTANCE: invention relates to novel pyridazinamides of the formula I , where all variable substituents are defined in the claims, and their pharmaceutically acceptable salts, as well as a pharmaceutical composition based on them.EFFECT: compounds of the formula are SYK inhibitors and are useful for the treatment of autoimmune and inflammatory diseases.10 cl, 1 tbl, 43 ex

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

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

Inhibitors of hepatitis c virus having rodlike chain and comprising {2-[4-(biphenyl-4-yl)-1h-imidazo-2-yl]pyrrolidin-1-carbonylmethyl}amine fragment // 2625787
FIELD: pharmacology.SUBSTANCE: invention relates to compound of formula (IV) or to pharmaceutically acceptable salt thereof, wherein R1 is selected from C1-6alkyl, optionally substituted with hydroxy or methoxy, and tetrahydropyran; R2 is a hydrogen atom; R3 is -C(O) OC1-6alkyl; R4 is methyl, methoxy or -CH2OCH3; R7 is selected from atom of fluoro, chloro, -CF3 and -OCF3; R8 independently represents methyl or hydroxymethyl; R9 is selected from -NHCH3, cyclopropyl, 2.2-dimethylcyclopropyl, tert-butyl, C1-6alkyl substituted with -OH, and imidazolyl; R10 is hydrogen atom or hydroxymethyl; a takes on a value of 1 or 2; and b takes on a value of 1 or 2. The invention also relates to heterocyclic compound of formula (V), specific compound, pharmaceutical composition based on compound of formulas (IV) or (V), method for preparing a target compound, intermediate compound, as well as to application of the produced compounds and method for inhibiting hepatitis C virus replication.EFFECT: new heterocyclic compounds are obtained, useful in the treatment of a viral infection of hepatitis C virus.15 cl, 1 dwg, 29 tbl, 24 ex
8-carbamoyl-2-(2,3-di-substituted pyrid-6-yl)-1,2,3,4-tetrahydroisoquinoline derivatives as apoptosis-inducing agents for cancer treatment // 2625315
FIELD: pharmacology.SUBSTANCE: invention relates to organic chemistry, namely a heterocyclic compound of formula (I) or to a therapeutically acceptable salt thereof, where X is benzo[d]thiazolyl, thiazolo[5,4-b]pyridinyl, thiazolo[4,5-c]pyridinyl, imidazo[1,2-a]pyridinyl, thiazolo[5,4-c]pyridinyl, thiazolo[4,5-b]pyridinyl, imidazo[1,2-a]pyrazinyl or imidazo[ 1,2-b]pyridazinyl; Y1 means pyrrolyl, pyrazolyl, triazolyl or pyridinyl; where Y1 is optionally substituted with 1 or 2 substituents independently selected from R5, CN and Cl; L1 is selected from (CR6R7)q, (CR6R7)s-O-(CR6R7)r, (CR6R7)s-S-(CR6R7)r, (CR6R7)s-S(O)2-(CR6R7)r and (CR6R7)s-NR6A-(CR6R7)r; Y2 means mono- or tricyclic C8-C10-cycloalkyl, spiro[2.5]octyl, spiro[3.5]nonyl, oxatricyclo[3.3.1.13,7]decyl or azabicyclo[3.2.1]octyl; where Y2 is optionally substituted with 1, 2 or 3 substituents independently selected from R8, OR8, SO2R8, CO(O)R8, OH and Br; Z1 is selected from , R1 and R3 are absent; R2 is deuterium or C1-C6-alkyl; R5 is C1-C6-alkyl; R6A is selected from hydrogen and C1-C6-alkyl; each R6 and R7 are hydrogen; R8 is selected from the group consisting of C1-C3-alkyl, morpholinyl and dioxydothiomorpholinyl; where R8, meaning C1-C6-alkyl, is optionally substituted with a substituent selected from R16, OR16, SO2R16 and NHR16; Rk is selected from C1-C6-alkyl, morpholinyl, cyclopropyl and C1-haloalkyl; R16 Is selected from C1-C4-alkyl, phenyl, morpholinyl and tetrahydropyranyl; where R16, meaning C1-C4-alkyl, is optionally substituted with 1 substituent selected from OCH3, OCH2CH2OCH3 and OCH2CH2NHCH3; q is 1 or 2; s, m and p is 0; r is 0 or 1; N is 0, 1, or 2. The invention also relates to specific compounds, pharmaceutical compositions based on these compounds and a method for treatment of these diseases.EFFECT: new heterocyclic compounds are obtained, that are useful for treatment of some cancers.16 cl, 3 tbl, 86 ex
Quinolines as fgfr kinase modulators // 2625303
FIELD: pharmacology.SUBSTANCE: invention related to a new quinoline derivative of formula (I), where W us -N(R3)- or -C(R3aR3b)-; each R2 is independently selected from halogen, C1-4alkoxy, Y is -E-D; D is phenyl or 5-6-membered monocyclic heterocyclyl, containing one or two heteroatoms selected from N or O, wherein the mentioned heterocyclyl can be optionally substituted with one group of R1; E is a link; R1 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyl which is substituted with -S(=O)2-C1-6alkyl, R6; R3a is hydroxyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, C1-6alkyl which is substituted with -NR10R11, C1-6alkyl which is substituted with -C(=O)-NR10R11; R3b is hydrogen; or R3a and R3b are combined to obtain =O or to obtain =CH-C0-4alkyl which is substituted with R3c; R3c is cyano; R3 is C2-6alkynyl, hydroxyC1-6alkyl, hydroxyhaloC1-6alkyl, C1-6alkyl which is substituted with R9, C2-6alkynyl which is substituted with R9, C1-6alkyl which is substituted with -NR10R11; R6 is 6-membered monocyclic heterocyclyl, containing one O atom; R9 is 5- or 6-membered monocyclic heterocyclyl, containing one or two heteroatoms, seleceted from N or O, each is optionally and each is independently substituted with substitute selected from =O, C1-4alkyl, C1-4alkoxy, S(=O)2-NR14R15, C1-4alkyl which is substituted with -NH-S(=O)2-haloC1-4alkyl, 6-membered aromatic monocyclic heterocyclyl, containing two N atoms, wherein the mentioned heterocyclyl is optionally substituted with R16; each R10 and R11 independently represent hydrogen, C1-6alkyl, haloC1-6alkyl; each R14 and R15 independently represent C1-4alkyl; R16 is C1-4alkoxy; n independently represent a whole number equal to 2, 3 or 4; as well as to its pharmaceutically acceptable salt and to any tautomeric or stereochemically isomeric form thereof. The invention also relates to pharmaceutical compositions based on compound of formula (I), application of the compound of formula (I), method for the prevention or treatment of a disease and product based on the compound of formula (I).EFFECT: new quinoline derivatives are obtained, useful in the treatment of diseases mediated by FGFR kinase.30 cl, 2 tbl, 35 ex
Heterocyclic compounds and their application as glycogen synthase kinase-3 inhibitors // 2623427
FIELD: chemistry.SUBSTANCE: invention relates to a heterocyclic compound of formula , where A represents NRB, where RB represents hydrogen; X1 and X2 represent CR2 and X3, X4, X5 and X6 represent CR3 or CR4, or X1 and X2 represent CR2, X3 represent N, and X4, X5 and X6 represent CR3; Y1, Y2, Y3 and Y4 represent CR4 or CR5 or Y2 represents N, and Y1, Y3 and Y4 represent CR5; provided that no more than one of Y1, Y2, Y3 and Y4 represents CR4; and provided that one of Y1, Y2, Y3 and Y4 represents CR4 or C-CF3, if none of X3, X4, X5 and X6 represents CR4; R1 represents hydrogen; each R2 represents hydrogen; each R3 is independently selected from the group consisting of hydrogen, CN, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy and C1-C6-haloalkoxy; R4 represents a C-linked saturated or partially unsaturated monocyclic 5- or 6-member heterocyclic ring containing one heteroatom selected from O and N, as ring members, wherein the heterocyclic ring optionally has one N-linked substituent R8; R5 is selected from the group consisting of hydrogen, C1-C6-alkyl, C1-C6-haloalkyl and C3-C7-cycloalkyl; and R8 is selected independently on the case from the group consisting of C1-C6-alkyl, C1-C6-haloalkyl and C1-C6-alkoxycarbonyl. The invention also relates to pharmaceutical compositions based on a formula (I) compound, formula (I) compound application, a method of treatment of diseases susceptible to treatment by a compound that modulates the activity of 3β glycogen synthase kinase.EFFECT: new heterocyclic compounds useful for treatment of neurodegenerative disorders or inflammatory diseases are obtained.25 cl, 2 tbl, 70 ex

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

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

Heterocyclic compounds useful as pdk1 inhibitors // 2615130
FIELD: chemistry.SUBSTANCE: present invention relates to novel compounds of general formulae II, III, IV and V, where values of radicals are given in description, or pharmaceutically acceptable salts thereof, which can be used as PDK1 inhibitors.EFFECT: present invention also relates to pharmaceutical compositions based thereon and to methods of treating cancer, mediated by protein kinase PDK1.32 cl, 2 tbl, 445 ex
Substituted dihydropyrazolones for treating cardiovascular and hematologic diseases, use thereof, drug and method of treating and/or preventing // 2611012
FIELD: chemistry; pharmaceutics.SUBSTANCE: present invention relates to use of dihydropyrazolone derivatives of formula (I), in which radicals and symbols are defined in p. 1 of patent claim.EFFECT: making drug for treating and/or preventing cardiac diseases of blood circulation, cardiac failure, anemia, chronic diseases of kidneys and renal failure, as well as medicinal agent containing said dihydropyrazolone derivatives, and method of treating and/or preventing said diseases in human and animals.4 cl, 10 tbl, 180 ex
Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2 negative allosteric modulators, compositions and use thereof // 2610262
FIELD: pharmaceutics.SUBSTANCE: invention relates to organic chemistry, namely, to quinoline carboxamide derivatives of following structures. Invention also relates to pharmaceutical composition based on one of said compounds, use of said compounds for treating diseases or disorders mediated by mGluR2, such as Alzheimer's disease, cognitive disorder, schizophrenia, mood disorders, painful disorders, and sleep disorders.EFFECT: novel quinoline carboxamide derivatives with useful biological properties.25 cl, 8 tbl, 310 ex
(alpha-substituted aralkylamino- and heteroarylalkylamino)pyrimidinyl- and 1,3,5-triazinylbenzimidazoles, pharmaceutical compositions thereof and use thereof in treating proliferative diseases // 2608742
FIELD: chemistry.SUBSTANCE: present invention relates to novel compounds of formula I, , having PI3K enzymatic activity.EFFECT: novel compounds of formula I are obtained, which can be used for regulation of PI3K enzymatic activity, as well as pharmaceutical compositions based thereon.33 cl, 2 tbl, 63 ex, 3 sch
Novel pyrrole compounds, synthesis method thereof and pharmaceutical compositions containing same // 2607788
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I) possessing inhibitory activity on Bcl-2 family proteins. In formula (I) (I) A1 is hydrogen, (C1-C6)polyhaloalkyl group or (C1-C6)alkyl group, A2 is hydrogen, (C1-C6)polyhaloalkyl group, (C1-C6)alkyl group or cycloalkyl group, T denotes a hydrogen atom, (C1-C6)alkyl group, optionally substituted with one-three halogen atoms, group (C1-C4)alkyl-NR1R2 or group (C1-C4)alkyl-OR6, R1 and R2 each independently from each other is a hydrogen atom or (C1-C6)alkyl group, or R1 and R2 form with a nitrogen atom bearing them, heterocycloalkyl, R3 is (C1-C6)alkyl group, cycloalkyl group, heterocycloalkyl group, aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R4 is an aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R5 is hydrogen or halogen atom, R6 is a hydrogen atom or a linear or branched (C1-C6)alkyl group, Ra, Rb, Rc and Rd each independently from other represents hydrogen, linear or branched (C1-C6)alkyl, halogen atom, a linear or branched (C1-C6)alkoxy group, hydroxy group, R7-CO-NH-(C0-C6)alkyl-, R7-SO2-NH-(C0-C6)alkyl-, R7-NH-CO-NH-(C0-C6)alkyl-, R7-O-CO-NH-(C0-C6)alkyl-, or substitutes of pair (Rb, Rc) form together with carbon atoms carrying them, a ring consisting of 5–6 ring members, which may contain 1–2 oxygen atoms, R7 is hydrogen, linear or branched (C1-C6)alkyl, aryl or heteroaryl. Invention also relates to methods of producing compounds of formula (I), to a pharmaceutical composition, use of a pharmaceutical composition for preparing a drug, use of compound of formula (I) for preparing a drug.EFFECT: obtaining novel compounds of formula (I) possessing inhibitory activity on Bcl-2 family proteins.37 cl, 2 tbl, 473 ex
Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors // 2606131
FIELD: pharmaceutics.SUBSTANCE: invention relates to compounds of formula I given below, or to their stereoisomers, tautomers or pharmaceutically acceptable salts thereof. R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and ring C are as defined by the invention formula. Wherein the Y-B moiety and the NH-C(=X)-NH moiety are in the trans configuration.EFFECT: compounds of formula I are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.56 cl, 31 tbl, 649 ex

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

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

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

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

Pyrazole derivatives // 2600983
FIELD: chemistry.SUBSTANCE: pyrazole derivatives are disclosed, which are encompassed by formula (I), in which radicals and groups are defined in patent claim and which are suitable for treating disorders mediated by peripheral cannabinoid 1 receptor 1.EFFECT: invention also discloses pharmaceutical compositions and methods related to use of said compounds.29 cl, 11 ex

Cyanoquinoline derivatives // 2600928
FIELD: chemistry.SUBSTANCE: invention relates to novel cyanoquinoline derivatives of general formula I, as well as to stereoisomers, cis-trans-isomers or pharmaceutically acceptable salts thereof, where R1 is selected from a group consisting of 4-bromobut-2-enamide, 4-(dimethylamino)but-2-enamide, acrylamido, but-2-enamide, 3-methylbut-2-enamide, 2-(1-tert-butoxycarbonylpiperidin-4-ylidene) acetamide, 2-(piperidin-4-ylidene)acetamide, 2-(1-methylpiperidin-4-ylidene) acetamide, 2-(1-ethylpiperidin-4-ylidene) acetamide, 2-(1-benzylpiperidin-4-ylidene) acetamide, 2-(1-(2-methoxyethyl) piperidin-4-ylidene)acetamide, 2-(1-(2-methoxycarbonylmethylene)piperidin-4-ylidene)acetamide, 2-(1-isopropylpiperidin-4-ylidene) acetamide, 2-(1-(2-hydroxyethyl)piperidine-4-ylidene)acetamide, 2-(pyrrolidin-3-ylidene)-acetamide, N-(N-(2-(2-(dimethylamino)ethoxy)ethyl)amino)fumaramide, 2-(1-(2-(2-(2-hydroxyethoxy)ethylamino)acetyl) piperidin-4-ylidene)acetamide, 2-((1-methylsulphonyl)piperidin-4-ylidene) acetamide, 4-(piperidin-1-yl)but-2-enamide, 4-(morpholin-4-yl)but-2-enamide, 4-(tert-butylamino)but-2-enamide, 4-(benzylamino)but-2-enamide, 4-(6-hydroxyhexylamino)but-2-enamide, 4-(N-methylbenzylamino)but-2-enamide, 4-(diethylamino)but-2-enamide, 4-(2-methoxyethylamino)but-2-enamide, 4-(diethanolamino)but-2-enamide, 4-(N-methylmethoxyethylamino) but-2-enamide, 4-(N-methyl-ethanolamino)but-2-enamide, 4-(dimethoxyethylamino)but-2-enamide, 4-(N-methyl-6-amino-1-hexanolyl)but-2-enamide and propylamide; one of R2 and R3 is H, while other is selected from unsubstituted C6-aryl-C1-2-alkyl, substituted with 1-2 substitutes or unsubstituted C6-aryl and substituted with 1 substitute or unsubstituted 6-9-member heteroaryl, where, when R2 or R3 is selected from a substituted C6-aryl, substitute is selected from C2-C6-alkynyl, halogen, C6-aryl-C1-alkyloxy (where said C6-aryl can be substituted with 1 substitute selected from halogen, cyano, C1-C6 alkyl, C1-C-6 alkoxy), and 6-member heteroaryl-C-1-alkyloxy, and when R2 or R3 are selected from a substituted heteroaryl, substitute is selected from a group comprising C6-aryl-C1-alkyl (where said C6-aryl is optionally substituted with 1 substitute selected from halogen and cyano, methoxy group), C6-arylamido (where the said C6-aryl can be unsubstituted or substituted with 1 dimethylamino group), C6-arylsulphonylamino, C5-heteroarylamido, C6-cycloalkylamido, C6-arylaminocarbonyl (where said C6-aryl is substituted with 1 methoxy group), C6-aryl-C1-alkyloxy and C6-aryloxy; or R2 and R3, together with a nitrogen atom to which they are bonded, form a substituted or unsubstituted 9-10-member heterocyclyl, where heterocycyl substitutes are selected from halogen, C1-C-6 alkyl, CF3, C6-aryl-C1-alkoxy, -COOMe, -CH2OH and pyrrolyl; and R4 is substituted with 1 methyl or unsubstituted 5-6-member heterocyclyl or unsubstituted 6-member heteroaryl. Invention also relates to specific compounds, pharmaceutical composition based on compound of formula I and use of formula I.EFFECT: technical result is obtaining novel cyanoquinoline derivatives which are useful in treating tumours.33 cl, 20 tbl, 228 ex
 
2550985.
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