Nitrogen atoms (C07D241/20)

C   Chemistry; metallurgy(318327)
C07   Organic chemistry(61593)
C07D241/20                     Nitrogen atoms (nitro radicals c07d0241160000)(25)
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
Piperazine derivatives, their preparation and application for insulin resistance treatment // 2626965
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (1), as well as to methods for its preparation, and pharmaceutical compositions based thereon.EFFECT: new compounds have been obtained that can be used for treatment of pathologies associated with insulin resistance syndrome, for example, type 2 diabetes.8 cl, 1 tbl, 2 ex
Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use // 2611437
FIELD: chemistry; pharmaceutics.SUBSTANCE: invention relates to novel compounds of formula (I) or its pharmaceutically acceptable salt or solvate, which have inhibiting activity lysine specific demethylase-1 (LSD1). In compounds of formula (I) (A) means phenyl or pyridyl, where said phenyl or pyridyl comprises n substitutes (R3); (B) means -O-CH2-phenyl or phenyl, where said phenyl or phenyl fragment, contained in the above -O-CH2-phenyl, comprises n substitutes (R2); (D) means a monocyclic heteroaryl group containing 5 or 6 ring members, where one to three said ring members are heteroatoms, selected from O, S and N, where said heteroaryl group contains one substitute (R1) and, besides, where said heteroaryl group is covalently bonded to molecules through circular carbon atom; (R1) means -NH2; each (R2) is independently selected from a group comprising C1-C6alkyl, hydroxy group, halogen, C1-C6haloalkyl, C1-C6haloalkyl oxy group or C1-C6alkoxy group; each (R3) is independently selected from a group comprising C1-C6alkyl, a hydroxy group, halogen, C1-C6haloalkyl, C1-C6haloalkyl oxy group or C1-C6alkoxy group; and n independently equal to 0, 1, 2 or 3.EFFECT: compounds can be used for treatment or preventing cancer, selected from a prostate cancer, breast cancer, lung cancer, colorectal cancer, cerebral cancer, blood cancer or leukemia; neurological diseases, including depression, Alzheimer's disease, Huntington's disease, Parkinson's Disease, amyotrophic lateral sclerosis, frontal-temporal dementia or dementia with Lewy bodies; or viral infection caused by herpes virus, or selected from a group of HSV-1, HSV-2, and Epstein-Barr virus.66 cl, 2 tbl, 38 ex

Cyclopentylacrylamide derivative // 2565070
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound, represented by general formula or its pharmaceutically acceptable salt, in which R1 and R2 independently represent hydrogen atom, C1-C6alkylsulphonyl group, which includes cyclopropylsulphonyl group, or C1-C6alkoxy- C1-C6alkylsulphonyl group, and A is selected from group which includes: thiazolyl group, 1,2,4-thiadiazolyl group, pyrazolyl group, pyridyl group, pyrazinyl group, isooxazolyl group, benzothiazolyl group and thiazolo[5,4-b]pyridyl group, and A can be mono-substituted by substituent, selected from group, which includes halogen atom; C1-C6alkyl groups, optionally substituted with halogen atom or hydroxyl group; C1-C6alkoxyl groups, optionally substituted with halogen atom or hydroxyl group; C1-C3alkoxy-C1-C2alkoxyl groups; C1-C3alkoxycarbonyl-C1-C2alkoxyl groups; C1-C6alkylsulphanyl groups; C1-C6amino-alkylsulphanyl group, optionally substituted with C1-C3alkyl group; C1-C6alkylsulphanyl-C1-C6alcoxyl groups; phenyl group; 1,3-dipxolane, substituted with two C1-C6alkyl groups; piperazinesulphonyl is substituted with methyl group; 1,3-dioxolanemethyl, substituted with two methyl groups; piperazinemethyl, substituted with methyl group; tetrahydropyranyloxy-C1-C3alkoxy group; aminosulphonyl groups, optionally substituted with C1-C3alkyl group; C1-C6 hydroxyalkylsulphanyl groups; -(O)(CH2)C(O)O-C1-C6alkyl group; -C(O)O-C1-C6 alkyl group; as well as groups, represented by general formula -(CH2)mP(O)R4R5 (where R4 and R5 independently represent C1-C3alkoxyl group; m is integer number from 0 to 1). Compound of formula (1) is intended, as active ingredient, for production of pharmaceutical composition, which has effect for activation of glucokinase (GK) or hypoglycaemic action. Invention also relates to intermediate compounds, represented by formula in which R1 and R2 independently represent hydrogen atom, C1-C6alkylsulphonyl group, which includes cyclopropylsulphonyl group, or C1-C6alkoxy-C1-C6alkylsulphonyl group.EFFECT: acrylamide compounds as glucokinase activator for treatment of diabetes.21 cl, 38 tbl, 55 ex

Crystals // 2556206
FIELD: medicine, pharmaceutics.SUBSTANCE: invention describes crystals of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulphonyl)acetamide ("compound A"), as a form I of the compound A crystal, which shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in its power X-ray diffraction spectrum, as a form II of the compound A crystal, which shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in its power X-ray diffraction spectrum, as a form III of the compound A crystal, which shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in its power X-ray diffraction spectrum. There are also described methods for producing the forms I, II and III of the compound A crystal, based pharmaceutical composition and PGI2 receptor agonist agent, an accelerating agent for angiogenic therapy, gene engineering or autoimmune bone marrow transplantation, and an accelerating agent for angiogenesis for peripheral artery recovery or angiogenic therapy on the basis thereof; there are also described a preventive or therapeutic agent for a wide range of diseases and conditions.EFFECT: preparing the new therapeutic agent for the wide range of diseases and conditions.11 cl, 6 dwg, 6 tbl, 5 ex

New phenol derivatives and their pharmaceutical or cosmetic application // 2540858
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of structural formula (I), which can be used for treating diseases mediated by an androgen receptor. In formula (I), R1 means (C2-6)alkyl, (C1-6)alkyloxy, -S(O)m-(C1-6)alkyl, (C1-6)fluoroalkyl, CN or halogen, R2 and R3 are identical or different and mean a hydrogen atom or (C1-9)alkyl, R4, R5, R6, R7 are identical or different and mean a hydrogen or halogen, X means CH or N, Y means either a nitrogen atom, or a carbon atom substituted by (C1-6)alkyl, (C1-6)alkyloxy, (C1-6)fluoroalkyl, a hydrogen atom or halogen; m is equal to 0, 1 or 2.EFFECT: invention refers to using the compounds for preparing a therapeutic agent for preventing and/or treating hirsutism, androgenetic alopecia, hypertrichosis, atopic dermatitis, disordered sebaceous gland, such as hyperseborrhea, acne, greasy skin or seborrheic dermatitis.8 cl, 2 tbl, 26 ex

Benzene or thiophen derivative and using it as vap-1 inhibitor // 2526256
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound presented by formula , wherein A1 means benzene or heterocycle specified in a group consisting of pyridine, pyrazine, imidazole, thiazole, pyrimidine, thiophen, pyridazine, benzoxazine and oxobenzoxazine; A2 means benzene, if needed substituted by fluorine, or thiophen; B1 means hydrogen, lower alkyl, if needed substituted by piperazinyl or morpholino, halogen-substituted lower alkyl, lower alkoxy substituted by carbamoyl, acylamino, carbamoyl or lower alkylcarbonyloxy (provided A1 means thiazole, B1 does not mean acylamino); B2 means hydrogen or a functional group containing at least one nitrogen atom specified in a group consisting of acylamino, pyrrolidinyl, morpholino, piperidinyl, if needed substituted by acyl, piperazinyl, if needed substituted by lower alkyl or acyl, pyrazolyl, diazabicyclo[2.2.1]heptyl, if needed substituted by acyl, and di-(lower alkyl)amino, if needed substituted by amino or acylamino (provided A1 means thiazole, B2 does not mean acylamino); Y means a group presented by formula , wherein J means ethylene or lower alkynylene; L means a bond; M means a bond; X means -(CH2)m-, -(CH2)m-O- or -(CH2)m-NR2- (wherein m is an integer of 0 to 3, and R2 means hydrogen); D means -NR3-, wherein R3 means hydrogen; and E means amino, or its pharmaceutically acceptable salt. The compounds of formula (I) are used for preparing a pharmaceutical agent or a pharmaceutical composition for treating or preventing the VAP-1 related diseases.EFFECT: benzene or thiophen derivative as a VAP-1 inhibitor.13 cl, 25 tbl, 125 ex

Novel compounds, use and production thereof // 2493152
FIELD: chemistry.SUBSTANCE: invention relates to a compound, which is N3-1H-indol-5-yl-5-pyridin-4-ylpyrazine-2,3-diamine, or a pharmaceutically acceptable salt thereof, which can act as inhibitors of protein kinase, especially FLT3 tyrosine kinase. The invention also relates to a pharmaceutical composition which contains said compound in combination with another molecularly directed (target) agent, which is a traditional cytotoxic agent or a compound used after chemotherapy, supporting therapy targeted on stem cells and in case of MLL rearrangement acute lymphoblastic leukaemia in children.EFFECT: obtaining a novel compound which can be used in medicine for preventing or treating haematological malignant growths such as AML, MLL, T-ALL, B-ALL and CMML, myeloproliferative diseases, autoimmune diseases and skin diseases, such as psoriasis and atopic dermatitis.16 cl, 2 tbl, 26 ex

Pyrazinone derivatives and use thereof in treatment of lung diseases // 2479580
FIELD: chemistry.SUBSTANCE: invention relates to pyrazinone derivatives of formula (I): , where R1, R2, R3, R4, R5, R and R7 are as defined in claim 1 of the invention. The invention also describes a crystalline form, compounds of formula I, use of the compound of formula I in producing a medicinal agent for treating chronic obstructive pulmonary disease. A pharmaceutical composition and a pharmaceutical product are also described. Methods of obtaining compounds of formula I are also described.EFFECT: novel compounds which can be used in therapy are obtained and described.20 cl, 334 ex, 15 tbl, 12 dwg

Derivatives with nitrogen-containing six-member aromatic ring and pharmaceutical products containing said derivatives // 2470927
FIELD: chemistry.SUBSTANCE: invention relates to novel pyrimidine derivatives of general formula (I-a), having the capacity to simulate axonal growth coupled with the capacity to stimulate angiogenesis and can be used in treating spinal chord damage, damage to the central nervous system as a result of head injuries, ischaemic stroke, ischemic heart disease, peripheral arterial occlusive disease, vascular dementia, cerebrovascular dementia or senile dementia. In the compound of formula (I-a): R0 is a group where R3 and R4 denote a hydrogen atom; R1 is a methyl group; R2 is a methyl group; R5 is a hydrogen atom; R6 is a hydrogen atom; R7 is a methyl group; E is an oxygen atom; is a benzyl group, a cyclohexyl methyl group, an isobutyl group, a cyclohexane carbonyl group, an acetyl group, a phenylsulphonyl group, a cyclohexyl group, a piperidine-1-carbonyl group, a methylbenzyl group, a phenyl group, a fluorobenzyl group, a methoxybenzyl group or a trifluorobenzyl group; or a pharmaceutically acceptable salt thereof.EFFECT: high efficiency of using the compounds.4 cl, 16 dwg, 27 tbl, 148 ex

3-cyclyl-2-(4-sulphamoylphenyl)-n-cyclylpropionamide derivatives applicable for treating impaired glucose tolerance and diabetes // 2435757
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula in which Q together with carbon and nitrogen atoms whereto attached forms a 9-10-member bicyclic heterocycle, and R1 and R2, R3, R4, R5 and R6 are as specified in cl.1 of the patent claim, or to its enantiomers, or a mixture of its enantiomers, or to its pharmaceutically acceptable salt. Also, an invention refers to a method for activation of glucokinase activity in mammals, by introduction of the compound described above, to a method of treating the pathological conditions associated with glucokinase activity and impaired glucose tolerance by means of introduction of the compound of formula I, to a pharmaceutical composition on the basis of the presented compounds, and also to application of the compounds of formula I for preparing the pharmaceutical composition.EFFECT: there are produced and described new compounds which are activators of glucokinase activity and can be used as therapeutic agents for preventing and treating impaired glucose tolerance, insulin-independent diabetes and obesity.14 cl, 4 ex

Oxime derivatives and preparation thereof // 2420525
FIELD: medicine.SUBSTANCE: in formula (I) , the ring A represents 6-members aryl or 5-6-members heteroaryl containing 1-2 heteroatoms selected from nitrogen and sulphur; Q means C3-8 cycloalkyl, 5-6-members heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulphur, C1-6 alkyl or C2-6 alkenyl; the ring T represents 5, 6, 9 or 10-members heteroaryl or 9-members heterocycle optionally additionally substituted by 1-3 heteroatoms independently selected from nitrogen or sulphur. The values of other substitutes are specified in the patent claim. Also, the invention refers to methods for preparing oxime derivatives of general formula (I), to pharmaceutical compositions containing the compound of the invention as an active ingredient and to applications of the compounds of the invention in preparing a drug.EFFECT: compounds of the invention exhibit properties of a glucokinase activator.33 cl, 1499 ex

Sulfonamide derivatives as glycokinase activators applicable for treating insulin-dependent diabetes // 2419624
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to compounds of formula wherein Q together with carbon and nitrogen atoms whereto attached forms a 5-6-members monocyclic heteroaromatic ring; or Q together with carbon and nitrogen atoms whereto attached forms a 9-10-members bicyclic heterocycle; R1 and R2 independently mean hydrogen, halogen, alkyl, alkyl substituted by one or more halogen, alkoxygroup, alkoxygroup substituted by alkoxygroup, alkylthiogroup, sulphonyl, free or etherified carboxygroup, carbamoyl, sulohamoyl, morpholinyl or pyridinyl; or R2 is absent; R3 means (C3-C6)cycloalkyl; R4 means hydrogen, halogen, lower alkyl or lowest alkyl substituted by one or more halogen; R5 means (C3-C6cycloalkyl, (C6-C10) aryl, (C3-C10)heterocyclyl or (C1-C6)alkyl optionally substituted by (C1-C6)alkoxygroup, (C3-C7)cycloalkyl, (C6-C10)aryl or (C3-C10)heterocyclyl; R6 means free or etherified carboxygroup; and n is an integer equal to 1-6; or to its enanthiomer, or a mixture of its enanthiomers, or its pharmaceutically acceptable salt. Besides, the invention refers to a method of glucokinase activation in mammals, to a method of treating pathological conditions associated with glucokinase activation in mammals and impaired glucose tolerance, as well as to a pharmaceutical composition based on these compounds and to application of said compositions for preparing a drug.EFFECT: there are produced and described new compounds which are activators and can be used as therapeutic agents for treating the glucokinase mediated pathological conditions.31 cl, 4 ex

Some substituted amides, method of their obtaining and method of their application // 2418788
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound of formula 2: and to its pharmaceutically acceptable salts and their mixtures, where values of R, M, Q, Z, W, D radicals are described in i.1 of the invention formula. Invention also relates to pharmaceutical compositions, which possess inhibiting activity with respect to Btk, based on formula 2 compounds.EFFECT: obtained are novel compounds and based on them pharmaceutical compositions which can be applied in medicine for treatment of patients with diseases associated with inhibiting Btk activity and/or B-cell activity.55 cl, 19 ex

Aromatic compound // 2416608
FIELD: chemistry.SUBSTANCE: invention describes a novel compound of general formula (1), where radicals R1, R2, X1, Y and A are as described in claim 1 of the invention. The invention also describes a method of obtaining compounds of formula (1), as well as a pharmaceutical composition based on said compounds, for treating fibrosis.EFFECT: novel compounds with excellent collagen formation suppression, cause fewer side-effects and which are safer are obtained.62 cl, 2717 ex, 432 tbl

Heteroaromatic derivatives of urea and use thereof as glucokinase activators // 2386622
FIELD: chemistry.SUBSTANCE: invention relates to compounds of general formula (I) and to their pharmaceutically acceptable salts, optical isomers or their mixture as glucokinase activators. In general formula (I) where R1 is C3-8-cycloalkyl, C3-8-cycloalkenyl, a 6-member heterocyclyl with 1 nitrogen atom, condensed phenyl-C3-8-cycloalkyl, each of which is possibly substituted with one or two substitutes R3, R4, R5 and R6; R2 is C3-8-cycloalkyl, a 5-6-member heterocyclyl with 1-2 heteroatoms selected from N, O, or S, each of which can be substituted with one or two substitutes R30, R31, R32 and R33, and R3, R4, R5, R6, R30, R31, R32 and R33 are independently selected from a group consisting of halogen, hydroxy, oxo, -CF3; or -NR10R12; or C1-6-alkyl, phenyl, C1-6-alkoxy, C1-6-alkyl-C(O)-O-C1-6-alkyl, each of which is possibly substituted with one substitute independently selected from R12; or -C(O)-R27, -S(O)2-R27; or two substitutes selected from R3, R4, R5 and R6 or R30, R31, R32 and R33, bonded to the same atom or to neighbouring atoms, together form a -O-(CH2)2-O- radical; R10 and R11 independently represent hydrogen, C1-6-alkyl, -C(O)-C1-6-alkyl, -C(O)-O- C1-6-alkyl, -S(O)2- C1-6-alkyl; R27 is C1-6-alkyl, C1-6-alkoxy, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, phenyl, phenyl-C1-6-alkyl, a 5-6-member heteroaryl with 1-2 heteroatoms selected from N or S, a 6-member heteroaryl-C1-6-alkyl with 1 nitrogen atom, a 6-member heterocyclyl-C1-6-alkyl with 1-2 heteroatoms selected from N or O, R10R11-N- C1-6-alkyl, each of which is possibly substituted with one substitute independently selected from R12; R12 is a halogen, CF3, C1-6-alkoxy, -NR10R11; A is a 5-9-member heteroaryl with 1-3 heteroatoms selected from N, O or S, which is possibly substituted with one or two substitutes independently selected from R7, R8 and R9; R7, R8 and R9 are independently selected from halogen, cyano, -CF3; or C1-6-alkyl, C2-6-alkenyl, C1-6-alkoxy, C1-6-alkylthio, -C(O)-O-C1-6-alkyl, formyl, - C1-6-alkyl-C(O)-O-C1-6-alkyl, -C1-6-alkyl-O-C(O)-C1-6-alkyl or hydroxy-C1-6-alkyl, each of which is possibly substituted with a substitute independently selected from R16; or phenyl, 5-member heteroaryl-C1-6-alkylthio with 2-4 nitrogen atoms, phenylthio, 5-6-member heteroarylthio with 1-2 nitrogen atoms, each of which is possibly substituted on the aryl or heteroaryl part with one or two substitutes independently selected from R17; or C3-8-cycloalkyl; or a 6-member heterocyclyl with 2 nitrogen atoms, 5-7-member heterocyclyl-C1-6-alkylthio with 1-2 heteroatoms selected from N or O, each of which is possibly substituted with one substitute independently selected from R16; or C1-6-alkyl-NR19R20, -S(O)2-R21 or -S(O)2-NR19R20; or -C(O)NR22R23; R16, R17 and R18 independently represent C1-6-alkyl, carboxy, -C(O)-O-C1-6-alkyl, -NR19R20, -C(O)NR19R20; R19 and R20 independently represent hydrogen, C1-6-alkyl, phenyl, 5-member heteroaryl with 2 heteroatoms selected from N or S, 6-member heterocyclyl with 1 nitrogen atom, -C(O)-O-C1-6-alkyl or -S(O)2-C1-6-alkyl, each of which is possibly substituted with one substitute independently selected from R24; or R19 and R20 together with a nitrogen atom to which they are bonded form a 5-7-member heterocyclic ring with the said nitrogen atom, where this heterocyclic ring possibly contains one additional heteroatom selected from nitrogen, oxygen and sulphur, where this heterocyclic ring is possibly substituted with one substitute independently selected from R24; R21 is selected from C2-6-alkenyl; or R22 and R23 are independently selected from hydrogen, -C1-6-alkyl-C(O)-O-C1-6-alkyl, -C1-6-alkyl-S(O)2-C1-6-alkyl, C3-8-cycloalkyl; or R22 and R23 together with a nitrogen atom to which they are bonded form a 6-member heterocyclic ring with the said nitrogen atom, where this heterocyclic ring is possibly substituted with one substitute independently selected from R24; R24 is oxo, C1-6-alkyl, carboxy- C1-6-alkyl, a 6-member heterocyclyl with 1 nitrogen atom, -NH-S(O)2R28 or -S(O)2R28, where each cyclic group is possibly substituted with one substitute independently selected from R29; R28 is C1-6-alkyl, -C1-6-alkyl-C(O)-O- C1-6-alkyl or -N(CH3)2; R29 is C1-6-alkyl.EFFECT: obtaining compounds which can be used for treating and preventing diseases mediated by low glucokinase activity.21 cl, 1 dwg, 608 ex, 1 tbl

Pyridodiazins as fungicides for plants // 2352570
FIELD: chemistry.SUBSTANCE: described is compound of general formula , in which W and Z represent N, and X and Y represent CH; R represents halogen; R1 represents phenyl, substituted with 1-3 substituents, selected from halogen; R2 represents NR3R4; R3 and R4 independently represent H, C1-C8alkyl, C2-C8alkenyl, halogen(C1-C8)alkyl, C1-C4alkoxy(C1-C8)alkyl, C3-C8cycloalkyl, optionally substituted with methyl, or R3 and R4 together form C3-C7alkylene chain, optionally containing as substituent C1-C4alkyl group, or together with nitrogen atom, to which they are bound, R3 and R4 form morpholine or pyperazine-N-(C1-C4)alkyl (more preferably N-methyl) ring. Described is method of obtaining compound of general formula (I), intermediate chemical products, as well as fungicidal composition for plants and method to combat phytopathogenic fungi or their elimination, using compound of formula (I).EFFECT: increase of compound fungicidal activity.10 cl, 133 tbl, 6 ex

Derivatives of heteroarylcarbamoylbenzene // 2330030
FIELD: chemistry.SUBSTANCE: present invention relates to the obtaining of the new derivatives of benzamide of the formulas (I), which possess the activating influence on glucokinase, which can be used for treating of diabetes and obesity: where X1 and X2 represent oxygen, R1 represents alkylsufonyl, alkaneyl, halogen or hydroxyl; R2 represents alkyl or alkenyl, R3 represents alkyl or hydroxyalkyl, ring A represents phenyl or pyridyl, the ring B represents thiazolyl, thiadiazolil, isoxazoleyl, pyridothiazolyl or pyrazolyl, in which the atom of carbon of ring B, which is connected with the atom of nitrogen of the amide group of the formula(I), forms C=N bond with ring B.EFFECT: obtaining new bioactive benzamides.12 cl, 166 ex, 4 tbl

Derivatives of propionic acids and their using as hppars activators // 2316539
FIELD: organic chemistry, medicine, pharmacy.SUBSTANCE: invention relates to compound of the formula (I): or its pharmaceutically acceptable salt, solvate or hydrolyzed ester wherein R1 and R2 represent independently hydrogen atom or (C1-C3)-alkyl; X represents oxygen atom (O); one of radicals R3 and R4 represents independently hydrogen atom and another represents (C1-C3)-alkyl; X1 represents -CH2 or -SO2; R5 represents (C1-C6)-alkyl (possibly substituted with (C1-C6)-alkoxy- or (C1-C6)-alkylthio-group), (C2-C6)-alkenyl, (C0-C6)-alkylphenyl (wherein phenyl is substituted possibly with one or more -CF3 group, halogen atom, (C1-C3)-alkyl, (C1-C3)-alkoxy-group), -CO-(C1-C6)-alkyl, -SO2-(C1-C6)-alkyl; R6 represents phenyl or 6-membered heteroaryl group comprising 1 or 2 nitrogen atom (N) and wherein phenyl or heteroaryl group are substituted possibly with 1, 2 or 3 groups chosen from group consisting of (C1-C6)-alkyl, phenyl (possibly substituted with one or more group chosen from halogen atom, -CF3, (C1-C3)-alkyl, O-(C1-C3)-alkyl, -CN). Compound of the formula (I) is designated for using as activator of human receptors activated by peroxisomal proliferators (hPPAR). Invention provides derivatives of propionic acids activating human receptors activated by peroxisomal proliferators (hPPAR).EFFECT: valuable medicinal properties of derivatives.14 cl, 58 ex

2-hetaryl-substituted of 1,3-tropolone, method for their preparing (variants) and pharmaceutical composition with antibacterial effect // 2314295
FIELD: organic chemistry, medicine, pharmacy.SUBSTANCE: invention relates to 2-hetaryl-substituted derivatives of 1,2-tropolones of the general formula (Ia): wherein R1 and R2 mean (C1-C6)-alkyl; R3 means hydrogen atom, (C1-C6)-alkyl, nitro-group; Het means six-membered nitrogen heterocycle condensed with one or two benzyl rings that can be substituted with substitutes chosen from group comprising halogen atom, nitro-group, (C1-C6)-alkyl, oxy-(C1-C6)-alkyl, secondary amino-group chosen from anilino-, substituted anilino-, hydroxyethylamino-group, or tertiary amino-group chosen from morpholino-, piperidino-, piperazino-group, 1H-1-imidazolyl. Also, invention relates to a method for synthesis of 2-hetaryl-substituted derivatives of 1,3-tropolone. Method involves condensation of benzoquinones-1,2 with 2-methylheterocycles at heating in the presence of acetic acid taken in the amount providing its role as both a catalyst and a solvent. Also, invention relates to a pharmaceutical composition with antibacterial effect based on 2-hetaryl-substituted derivatives of 1,3-tropolone.EFFECT: improved method of synthesis, valuable medicinal properties of compounds and pharmaceutical composition.9 cl, 5 tbl, 3 ex

Heterocyclic compound derivatives and pharmaceutical agents // 2283835
FIELD: organic chemistry, pharmaceuticals.SUBSTANCE: invention relates to heterocyclic compounds of general formula I with PGl2 receptor agonist activity. In formula R1 and R2 represent independently optionally substituted phenyl; Y represents N, N-O or CR5; Z represents N or CR6; A represents NR7; D represents alkylene or alkenylene; or A and D may together form divalent group; E represents phenylene or direct bond, or D and E may together form divalent group; G represents O, S, SO, SO2; R3 and R4 represent hydrogen atom or alkyl; Q represents carboxyl, alkoxycarboxyl, tetrazolyl, carbamoyl or -CONH-SO-R10 group. Prostaglandin I2(PGl2) is potent inhibitor of platelet aggregation and may be effectively used in treatment of vascular diseases, arteriosclerosis, hypertension, etc.EFFECT: new compounds and drugs for platelet aggregation inhibition and treatment of vascular and other diseases.15 cl, 3 tbl, 109 ex

Isoindoline-1-on-glucokinase activators // 2249590
FIELD: organic chemistry, pharmaceutical composition.SUBSTANCE: new isoindoline-1-on-glucokinase activators of general formula I , as well as pharmaceutically acceptable salts or N-oxide thereof are disclosed. In formula A is phenyl optionally substituted with one or two halogen or one (law alkyl)sulfonyl group, or nitro group; R1 is C3-C9cycloalkyl; R2 is optionally monosubstituted five- or six-membered heterocyclic ring bonded via carbon atom in cycle to amino group, wherein five- or six-membered heteroaromatic ring contains one or two heteroatoms selected form sulfur, oxygen or nitrogen, one of which is nitrogen atom adjacent to carbon atom bonded to said amino group; said cycle is monocyclic or condensed with phenyl via two carbon atoms in cycle; said monosubstituted with halogen or law alkyl heteroaromatic ring has monosubstituted carbon atom in cycle which in not adjacent to carbon atom bonded to amino group; * is asymmetric carbon atom. Claimed compounds have glucokinase inhibitor activity and useful in pharmaceutical composition for treatment of type II diabetes.EFFECT: new isoindoline-1-on-glucokinase activators useful in treatment of type II diabetes.23 cl, 3 dwg, 43 ex

New derivatives of ndimethylacetamide, the method of production thereof, pharmaceutical composition and protease inhibitors based on them // 2181360
The invention relates to new compounds of the formula (I), where R0- phenyl, R1- phenyl, heteroaryl, lower alkyl which may be substituted or unsubstituted, R2substituted or unsubstituted phenyl, lower alkyl, R3is hydrogen, acyl group, sulfonylurea group, X and Y independently represent a nitrogen atom or a carbon atom, Z is methylene group
 
2550994.
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