Derived pyridinesulfonamide with herbicide activity

 

(57) Abstract:

Usage: agriculture as a herbicide. The inventive product is n- [4,6-dimethoxypyrimidine-2-yl (aminocarbonyl)] 1-3-dimethyl - aminocarbonyl - 2 - pyridinesulfonamide f-ly 1. BF C13H18N6O6S; so pl. 169-173°C. Reagent 1: compound f-crystals 2. Reagent 2: compound f-crystals 3, where Z1- NH2group, -NCO, NHCOCI or NHCOOR5, Z2- NH2, NCO, NHCOCI, NHCOOR5R is alkyl or aryl. Reaction conditions: in a medium of an organic solvent at room temperature. 5 table. The connection structure of f-crystals 1, 2, 3:

The invention relates to a new compound derived pyridinesulfonamide with herbicide activity, the method of its production and use in suppressing the growth of unwanted plants.

The aim of the invention is the creation of new compounds with a broad spectrum herbicide action and gentle action on the corn. Specifically, the invention relates to a derivative of pyridinesulfonamide formula

(I)

Substituted pyridinesulfonamide connection that meets the General formula (I) can be obtained in the following way.

Conduct the reaction between pyridone group -HCOCl-group, or-HCCOR5group (in which R5represents an alkyl or aryl group), and pyrimidinium compound conforming to the following formula

(III) in which Z2represents NH2group-NCO-group-NHCOCl-group, or-HCOOR5group (in which R5has the same values as described above), provided that, when Z1represents NH2group, Z2is an-NCO, -NHCOCl or HCOOR5group, and if Z2represents NH2group, Z1is an-NCO-, -NHCOCl or-NHCOOR5-group. If you want, then spend processing with the aim of obtaining salt.

The purpose of the invention is achieved in that the herbicide composition comprises pyridinesulfonamide derivative as active substance:

(A)

This compound can be used alone or in a composition, which can be used as a carrier - kaolin, finely dispersed silicon dioxide or a mixture, as the surfactant is a mixture of compounds selected from the group comprising vinylsulfonate sodium, polycarboxylic sodium, alkylarylsulfonate sodium, polyoxyethyleneglycol and p: Active substances 10-80 Media 7-83,7

Surfactant 6,3-13.

The specified composition is produced by mixing the above components with subsequent grinding for forming a wettable powder. For biological testing were obtained the following compounds.

P R I m e R 1. Composition, wt.%: Connection And 10 Kaolin 70,2

The reaction product con-

densely naphthalenol-

fonate sodium form aldehyde 1,8

Polyoxyethylenated - unilaterality 4,5 Microdispersed di - oxide silicon 13,5

P R I m m e R 2. Composition, wt.%: Vinylsulfonate sodium 6 Polycarboxylic sodium 5 Alkylarylsulfonate sodium 2

Microporosities hydrated silica 7 Connection AND 80

P R I m e R 3. Composition, wt.%: Vinylsulfonate sodium 4 Polycarboxylic sodium 3 Alkylarylsulfonate 1 Kaolin 42 Connection AND 50

The connection is As shown in example 4.

P R I m e R 4. To a suspension obtained by adding 0,229 g 2-aminosulfonyl-N, N-diethylnicotinamide and 0,275 g 2 phenoxycarbonylamino-4,6-dimethoxyphenyl-Medina in 5 ml of anhydrous acetonitrile add 0.152 g of 1,8-diazabicyclo (5,4,0)-undecene and the resulting mixture is left for 1 h at room temperature. Upon termination of the reaction mixture added to the water to filter nerastvorim in a weak acid solution and extracted with methylene chloride. Then the solution is dried with anhydrous sodium sulfate, the solvent is distilled off, and get 0,330 g of target compound is N-[(4,6-dimethoxypyrimidine-2-yl(aminocarbonyl)]-3 - dimethylaminoethyl-2-pyridinol - Namida with so pl. 169-173aboutC.

The compounds listed in examples 1-3 were subjected to biological tests. The test results presented in examples 5-7 and table.1-3.

P R I m e R 5. For testing we used the composition of example 1.

Each pot is filled with soil and seeded with a certain number of seeds of different test plants. When the test plants have reached a certain stage (i.e. stage 2.2 sheet for corn, 2.0 sheet for cocklebur, 0.5 sheet ipomea, 0.5 sheet for the Highlander pepper, 0.1 sheet for breast barbed), the plants are sprayed with an aqueous solution prepared from the composition of example 1.

The leaves of plants sprayed with a small sprayer. 30 days to visually determine the degree of development of plants. Suppression of weeds assessed on a 10-point scale, where 10 means that the plant is killed, and 1 shows what the raw plant, as shown in the table.1.

Test connection A. Connected)

The results are given in table.1.

P R I m e R 6. The test composition of example 3.

Corn (varieties Golden cross vantum (1), Royal Dent 105 (2)), weed blood, spickle green, oats, black nightshade and Highlander pepper were sown in pots with an area of 1/10000 ar (a) each and were grown in the greenhouse. After the experimental plants were reached, respectively, defined growth stages, i.e. stage 4-th sheet for Golden cross vantum, stage 4.3 sheet for Royal Dent 105T, 3,3 sheet Rosicky blood, 3,3 sheet for spickle green, 2,3 sheet for wild oats, stage 2-th sheet of black nightshade and stage 3-th sheet for the Highlander pepper, they were sprayed with an aqueous solution prepared from the composition of example 2. After 27 days after spraying visually determined the degree of growth of the treated plants. The degree of effectiveness of weed control was evaluated on a 10-point scale, where a value of 10 meant completely destroyed the plant, and a value of 1 was defined as plants that looked similar to the control, untreated, as indicated in the table.3.

P R I m e R 7. The test composition of example 2.

Corn (varieties Golden cross vantum and Royal Dent 105T) and weed blood was inoculated in a pot with an area of 1/10000 ar (a) each and expressed the o stages (i.e., stage 3.5 sheet for Golden cross vantum, stage 4-th sheet for Royal Dent 105T and stage 2.5 sheet Rosicky blood), they were sprayed with an aqueous solution prepared from the composition of example 2.

After 27 days after spraying visually determined the degree of growth of the treated plants. The effectiveness of weed control was evaluated on a 10-point scale, where a value of 10 meant completely destroyed the plant, and the value of 1 was used to refer to plants that looked similar to the control, untreated, as indicated in the table.2.

As can be seen from the results of the tests are presented in table.1-3, the composition with the connection And completely inhibit the growth of barnyard millet, which is a weed, and does not exert any influence on corn. In addition, sufficiently suppressed the growth of broadleaf weeds such as cocklebur, morning glory, brisket prickly, Highlander pepper and amaranth. On the other hand, a well-known composition affect the growth of corn. Therefore, a well-known composition is impractical to use for processing corn fields.

In examples 8 and 9 and table.4 and 5 presents comparative data on herbicide activity of the new compounds and linali mountain soil and a certain number of grains of maize (variety: Royal Dent, Zea Mays). Typical herbaceous weeds, i.e., Johnson grass (Sorghum halepense), green Alopecurus (Setaria viridis) and wild oats ('avene fatua), were sown separately.

The aqueous dispersion was obtained by dissolving a certain amount of each test compound in 500 l/ha of water, and thereto was added 0.2% of the agricultural sprayer.

When the test plants respectively were reached certain stages of growth (i.e., 3,3-leaf stage for corn, 4,0-leaf stage, and herb Johnson, 2,6-leaf stage for green Alopecurus and 1.6-leaf stage of wild oats) aqueous dispersion was applied on the leaves of plants.

After twenty-one days after the application of the net weight of the plants was measured from ground level.

The degree of damage to corn (%) and degree of suppression of weeds (%) was determined using the following equations:

damage = 100 - 100

suppression = 100 - 100

Comparative test 2.

Each pot was filled mountain soil and sown certain number of seeds of different test plants. When the test plants respectively were reached certain stages of growth (i.e., 3,8-leaf stage for corn (Zea mays), a 3.0-leaf stage green is uranium wettable powder, containing a certain amount of each of the test compounds in 500 l/ha of water, and 0.2% of the agricultural sprayer was added to aqueous solution. The resulting solution was applied on the leaves of plants by spray small size. Twenty days after the application is visually observed degree of suppression of plant growth in %.

Test connection:

Connection: the proposed connection

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B-J: known compounds.

Test results

The results of the test plants I shown in the table.4, below.

The claimed compound (compound A) shows the best herbicide effect when applied to a corn field, which is important for crop, where unwanted plants are almost completely suppressed, while corn can grow without damage.

On the other hand, the compounds of the prior art (compounds B, C and D) show much less activity against undesirable plants, while completely inhibit the growth of corn.

The results of the test plants 2 are shown in table.5, below.

The proposed connection And shows the best herbicide effect when the pump is EMA, as corn can grow without damage.

On the other hand, the compounds of the prior art (compounds E, F, G, H, I and J) do not show such significant selectivity.

Structural formulas of compounds analogues tested on herbicide activity:

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< / BR>
< / BR>

DERIVED PYRIDINESULFONAMIDE WITH HERBICIDE ACTIVITY.

Derived pyridinesulfonamide formula

< / BR>
have a weed-killing activity.

 

Same patents:

The invention relates to tetrahydropyrimidine derivative of formula (1) or their pharmaceutically acceptable salts, suitable as 3-HT3-capetronic antagonists:

(1) where Неt is a heterocyclic group, possibly substituted by 1-3 substituents selected from lower alkyl, lower alkenyl, lower quinil, group cycloalkyl-lower alkyl, arylalkyl, lower alkoxycarbonyl, halogen atom;

X represents a single bond attached to the carbon atom of the heterocyclic group

The invention relates to a method for obtaining new pyrimidine derivatives possessing valuable fungicidal properties, which can find application in agriculture

The invention relates to pyrimidine derivative of the General formula I:

where R1- alkyl-(C1-C4), O-alkyl-(C1-C4), halogen;

R2- alkyl-(C1-C4), O-alkyl-(C1-C4);

n = 3-5;

Z = COOH, COO-alkyl-(C1-C4), CONHSO2C6H5with herbicide activity, and to a method of controlling undesirable vegetation by processing them in the locus, namely, that the treatment is carried out pyrimidine derivatives of General formula I:

where R1- alkyl-(C1-C4), O-alkyl-(C1-C4), halogen;

R2- alkyl-(C1-C4), O-alkyl(C1-C4);

n = 3-5;

Z = COOH, COO-alkyl-(C1-C4), CONHSO2C6H5in the amount of 1-10 kg/ha

The invention relates to methods of producing derivatives of 2-anilinopyrimidines or acid additive salts of novel biologically active compounds, which can find application in agriculture

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new sulfur-containing compounds of the formula (I):

their pharmaceutically acceptable salts or solvates, or salt solvates wherein R1 represents (C1-C6)-alkyl, cycloalkyl, aryl, aliphatic or aromatic heterocyclyl substituted with one more basic group, such as amino-, amidino- and/or guanidine-group; R2 represents hydrogen atom (H), alkyl, alkylthio-, alkoxy- or cycloalkyl group; R3 represents COOR5, SO(OR5), SOR5 and others; R4 represents hydrogen atom (H) or (C1-C6)-alkyl; R6 represents hydrogen atom (H); X represents C(Z)2 or NR6CO; Y represents C(Z)2; Z represents hydrogen atom (H), (C1-C6)-alkyl, aryl or cycloalkyl. Indicated compounds inhibit activity of carboxypeptidase U and can be used for prophylaxis and treatment of diseases associated with carboxypeptidase U.

EFFECT: improved preparing method, valuable biochemical and medicinal properties of compounds.

14 cl, 36 ex

FIELD: organic chemistry, chemical technology, fungicides.

SUBSTANCE: invention describes derivative of benzoylpyridine of the formula (I) or its salt:

wherein X represents halogen atom, (C1-C6)-alkoxy-group optionally substituted with a substitute taken among halogen atom, phenyl, methoxy-, methylthio-, dimethylamino-group, vinyl or ethynyl; phenoxy-group, (C3-C6)-cycloalkoxy-group, hydroxyl group, (C1-C6)-alkyl group, (C2-C6)-alkenyl group, CF3, (C1-C6)-alkylthio-group, (C1-C6)-alkoxycarbonyl group, (C1-C6)-dialkylaminocarbonyl group, (C1-C6)-alkylcarbonyloxy-group, (C1-C6)-alkylcarbonyl group, amino-group, (C1-C4)-alkylamino-group or di-(C1-C4)-alkylamino-group; n represents 1, 2, 3 or 4; R1 represents (C1-C6)-alkyl group; R2 represents (C1-C6)-alkyl group, (C1-C6)-alkoxy-group optionally substituted with phenyl, phenoxy-group, (C3-C10)-cycloalkyloxy-group or hydroxyl group; m = 1, 2 or 3 under condition that if m = 2 then R2 can form ring -OCH2O- (with exception when pyridine ring is substituted with benzoyl group at 2-position; pyridine ring is substituted with (C1-C6)-alkoxy-group, hydroxyl group or benzyloxy-group; n = 1; m = 1 or 2). Also, invention describes fungicide comprising compound of the formula (I) or it salt as an active component, methods for preparing derivatives of benzoylpyridine, phenylpyridylmethanol that is an intermediate compounds used for synthesis of compound of the formula (I). Invention provides fungicide properties of compound of the formula (I) or its salt.

EFFECT: improved method for preparing, valuable properties of compounds.

17 cl, 36 tbl, 4 ex

FIELD: organic chemistry, herbicides, agriculture.

SUBSTANCE: invention elates to novel derivatives of uracil of the formula [I] possessing herbicide activity, a herbicide composition based on thereof and to a method for control of weeds. In derivatives of uracil of the formula [I] the group Q-R3 represents a substituted group taken among:

wherein a heterocyclic ring can be substituted with at least a substitute of a single species taken among the group involving halogen atom, (C1-C6)-alkyl-(C1-C6)-alkoxy; Y represents oxygen, sulfur atom, imino-group or (C1-C3)-alkylimino-group; R1 represents (C1-C3)-halogenalkyl; R2 represents (C1-C3)-alkyl; R3 represents OR7, SR8 or N(R9)R10; X1 represents halogen atom, cyano-group, thiocarbamoyl or nitro-group; X2 represents hydrogen or halogen atom wherein each among R7, R8 and R10 represents independently carboxy-(C1-C6)-alkyl and other substitutes given in the invention claim; R9 represents hydrogen atom or (C1-C6)-alkyl. Also, invention relates to intermediate compounds used in preparing uracil derivatives.

EFFECT: improved preparing method, valuable properties of compounds.

40 cl, 16 sch, 12 tbl, 65 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to anthranilic acid amides of the formula (I): wherein R1 means hydrogen atom or (lower)-alkyl; R2 means hydrogen atom or (lower)-alkyl; R3 means perfluoro-(lower)-alkyl; X means oxygen atom or sulfur atom, or to its N-oxide or tautomer, to salts of such anthranilic acid amides, their N-oxides or their tautomers. Compounds of the formula (I) possess inhibitory activity with respect to tyrosine kinase VEGF receptors and can be used in treatment of neoplasm, retinopathy or age degeneration resulting to appearance of spots in retina in humans or mammals. Also, invention relates to using anthranilic acid amide of the formula (I) for preparing a pharmaceutical drug possessing above said activity, to a method for treatment of neoplasm disease, a pharmaceutical drug and a method for synthesis of anthranilic acid amide of the formula (I).

EFFECT: improved method of synthesis, valuable medicinal properties of compounds and pharmaceutical drug.

9 cl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention describes novel 2-pyridinylethylbenzamide compounds of general formula (I) , in which: n is equal 1, 2 or 3; X is similar or different and represents hydrogen atom, halogen atom, C1-C8alkyl; R1 represents hydrogen atom, halogen atom, pentafluorine- λ 6-sulphanyl group, C1-C8alkyl; on condition that X and R1 both are not hydrogen atom; R2 and R3 are similar or different and represent hydrogen atom, C1-C6alkyl; or R2 and R3 together can form 3-, 4-, 5- or 6-member carbocycle; R4 and R5 are similar or different and represent hydrogen atom; R6 represents hydrogen atom, C1-C6alkyl, p equals 1, 2, 3 or 4; Y is similar or different and represents hydrogen atom, halogen atom; and R7 represents halogen atom, C1-C8alkyl, containing 1-5 halogen atoms C1-C8halogenalkyl, as well as its salts, N-oxides, metal-containing and metalloid-containing complexes. As well as method of obtaining said compound and fungicidal composition, containing compound of general formula (I), method of processing plants by applying compound of general formula (I) or composition containing it.

EFFECT: novel compounds can find application in agriculture.

21 cl, 70 ex

FIELD: chemistry, medicine.

SUBSTANCE: invention refers to the method for modulation of the CRTh2-receptor activity with usage of the compounds of formula (I) or their pharmaceutically acceptable salts where: W is O, S(O)n (where n is equal 0, 1 or 2), NR15, CR1OR2 or CR1R2; X is hydrogen, halogen or C1-6 alkyl which can be substituted with one or more halogen atom; Y is hydrogen, halogen; Z is phenyl, pyridyl, pyrimidyl or quinolyl possibly substituted with one or more substituting group independently selected from following groups: halogen, CN, nitro, SO2R9, SO2NR10R11, CONR10R11, NHSO2R9 or C1-3 alkyl substituted with one or more halogen atom; R1 and R2 are independently hydrogen atom or C1-6 alkyl; R9 is C1-6 alkyl; R10 and R11 are independently hydrogen atom or C1-6 alkyl; R15 is hydrogen atom or C1-6 alkyl.

EFFECT: improvement of the method.

19 cl, 68 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula IV: , where: R1 represents Cl or F; R3 represents H, Me, Et, OH, MeO-, EtO-, HOCH2CH2O-, HOCH2C(Me)2O-, (S)-MeCH(OH)CH2O-, (R)-HOCH2CH(OH)CH2O-, cyclopropyl-CH2O-, HOCH2CH2-, , , , , or , R7 represents methyl or ethyl which are optionally substituted with one or more F; R8 represents Br, I or SMe; and R9 represents H, C1-C4alkyl, Cl or CN where said alkyl it optionally substituted with one or more groups independently chosen from F or CN provided when a) R1 represents F, R8 represents Br, R9 represents H, and R7 represents either Me, or Et, then R3 cannot represent HOCH2CH2O; b) R1 represents F, R8 represents I, R9 represents H, and R3 represents MeO then R7 cannot represent Me; c) R1 represents F, R8 represents Me, R9 represents H, and R3 represents HOCH2CH2O then R7 cannot represent Me; and d) R1 represents F, R8 represents Br, R9 represents H, and R3 represents cyclopropyl-CH2O then R7 cannot represent Me, as well as to the use of said compound in preparing a drug for treating hyperproliferative disorder or an inflammatory state and to a pharmaceutical composition which inhibits MEK.

EFFECT: there are prepared and described new compounds effective in treating hyperproliferative diseases, such as cancer and inflammation.

17 cl, 25 ex, 8 tbl, 15 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (II-A) or pharmaceutically acceptable salt thereof: [in which symbols denote the following: R10-R12: are identical or different and each denotes halogen, lower alkyl, halogen-lower alkyl, -OR0, -O-halogen-lower alkyl or -CN, R13: R0, halogen, halogen-lower alkyl, -OR0, -O-halogen-lower alkyl or -CN, ring B: benzene ring or a 5-6-member heteroaromatic ring containing 1-2 heteroatoms selected from O, S and N, R14: R0, halogen or -OR0, R0: are identical or different and each denotes H or lower alkyl, Y1: a single bond, lower alkylene, lower alkenylene or O-lower alkylene-, and Z1: -CO2R0 or -C0-NH-SO2-lower alkyl]. The invention also relates to a pharmaceutical composition based on the said compound, having antagonistic effect on the EP1 receptor.

EFFECT: obtaining novel compounds and a pharmaceutical composition based on said compounds, which can be used in a medicinal agent for treating lower urinary tract symptoms.

6 cl, 56 tbl, 231 ex

FIELD: chemistry.

SUBSTANCE: compound, represented by formula

,

or its pharmaceutically acceptable salt, where Y1 represents nitrogen atom or group, represented by CRA, Y2 represents nitrogen atom or group, represented by CRB, Y3 represents nitrogen atom or group, represented by CRC, RA, RB and RC, which can be similar or different, each represents hydrogen atom, etc. (except in the case, when Y1 is CRA, Y2 is CRB and Y3 is CRC), X represents oxygen atom, etc., R1 represents C1-C6alkyl group, etc., R3 represents optionally substituted phenyl group, etc., R4 represents hydrogen atom, etc., and R5 represents optionally substituted phenyl group, etc.), possesses inhibiting action with respect to S1P binding with its receptor Edg-1(SlP1).

EFFECT: obtaining composition, which can be used as therapeutic medication in case of autoimmune diseases, rheumatoid arthritis, asthma, atopic dermatitis, rejection after organ transplantation, cancer, retinopathy, psoriasis, osteoarthritis or age-related macula lutea degeneration, etc.

13 cl, 9 ex, 1 tbl, 4 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to substituted compounds of general formula I , in which n equals 1; R1 denotes H; F; Cl; Br or I; R2 denotes H; F; Cl; Br; I; -CF3; -CN; -NH2; -OH or -OR16; R3 denotes H; F; Cl; Br; I; -NH2; -NO2; -OH; -C(=O)-NH2; -C(=NH)-NH2; -NH-C(=O)-R13; -OR16; -C(=O)-NHR18; -C(=O)-R25 or a linear or branched, saturated of unsaturated, unsubstituted or at least mono-substituted aliphatic C1-10 radical, where said substitutes are independently selected from a group which includes F; -OH; -NH2; -NH(C1-5-alkyl) and -N(C1-5-alkyl)(C1-5-alkyl); R4 denotes H; F; Cl; Br, I or a linear or branched, saturated or unsaturated, unsubstituted aliphatic C1-10 radical; R5 denotes H; F; Cl; Br or I; R6 denotes H or a linear or branched, saturated or unsaturated, unsubstituted aliphatic C1-10 radical; R7 denotes hydrogen; R8 denotes -CF3; -O-CFH2; -O-CF2H; -CFH2; -CF2H or an unsubstituted or at least mono-substituted tert-butyl radical; T denotes C-R35; U denotes C-R36; V denotes N or C-R37; W denotes C-R38 and where values of R13, R16, R18, R25, R35, R36, R37 and R38 are as given in claim 1 of the invention. The invention also relates to methods of producing the compounds described above, a medicinal compound based on said compounds for treating vanilloid receptor mediated disorders or diseases, as well as use of compounds of formula I to produce a medicinal agent.

EFFECT: novel compounds used as vanilloid receptor ligands are obtained and described.

25 cl, 34 ex, 1 tbl

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compounds of the formula (I):

wherein X means group of the formula (X-1) wherein R15 means halogen atom, (lower)-alkyl and perfluoro-(lower)-alkyl; R16 means hydrogen, halogen atom and (lower)-alkyl; or X means group of the formula (X-2) wherein Het means 5- or 6-membered heteroaromatic ring comprising 1 or 2 heteroatoms as nitrogen (N) atom; R15 and R16 have values indicated above for (X-1); R30 means hydrogen atom or (lower)-alkyl; p means a whole number from 0 to 1; or X means group of the formula (X-3) wherein R18 means aryl; R19 means unsubstituted arylalkyl or heteroarylalkyl representing 6-membered heteroaromatic ring comprising nitrogen (N) atom as a heteroatom; R20 means unsubstituted (lower)-alkanoyl; Y means group of the formula (Y-1) wherein R22 and R23 mean independently from one another hydrogen atom, (lower)-alkyl, halogen atom or perfluoro-(lower)-alkyl and at least one of radicals R22 and R23 doesn't mean hydrogen atom; R24 means hydrogen atom; or Y means group of the (Y-3) wherein R25 means group of the formula: R26-(CH2)e- wherein R26 means (lower)-alkoxy-group, (lower)-alkylthio-group, (lower)-alkylsulfonyl; or R26 means group of the formula: -NR28R29 wherein R28 means hydrogen atom; R29 means (lower)-alkanoyl or (lower)-alkylaminocarbonyl; Q means -(CH2)f- wherein e means a whole number from 0 to 4; f means a whole number from 1 to 3; a bond denoted as a dotted line can be hydrogenated optionally; and to its pharmaceutically acceptable salts and esters. Also, invention proposes a pharmaceutical composition designated for treatment or prophylaxis of rheumatic arthritis, cerebrospinal sclerosis, intestine inflammatory disease and asthma and containing compound of the formula (I) or its pharmaceutically acceptable salt or ester in combination with a compatible pharmaceutical carrier. Invention proposes derivatives of thioamide inhibiting interaction between α4-comprising integrins and VCAM-1.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

20 cl, 1 tbl, 86 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to new 2-aminopyridine derivatives of formula I , wherein R1 is cyano, carboxyl or carbamoyl; R2 is hydrogen, hydroxyl, C1-C6-alkoxy or phenyl; R3 and R4 are aromatic hydrocarbon such as phenyl or naphthyl, 5-14-membered 5-14-membered optionally substituted aromatic group, excepted cases, when (1) R1 is cyano, R2 is hydrogen, and R3 and R4 are simultaneously phenyl;(2) R1 is cyano, R2 is hydrogen, R3 is 4-pyridyl, and R4 is 1-pyridyl; (3) R1 is cyano, R2 is 4-methylphenyl, and R3 and R4 are simultaneously phenyl;(4) R1 is cyano, R2, R3 and R4 are simultaneously phenyl, or salts thereof. Derivatives of present invention have adenosine receptor antagonist activity and are useful in medicine for treatment of irritable bowel syndrome, constipation, and defecation stimulation.

EFFECT: 2-aminopyridine derivatives as adenosine receptor antagonists useful in medicine.

34 cl, 2 tbl, 179 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention describes derivatives of 4-phenylpyridine N-oxides of the general formula (I) and their pharmaceutically acceptable acid-additive salts wherein R means hydrogen atom, lower alkyl or halogen atom; R1 means hydrogen atom; R2 and R2' mean independently of one another hydrogen, halogen atom, trifluoromethyl group, (lower)-alkoxy-group; or R2 and R2' can mean in common the group -CH=CH-CH=CH- optionally substituted with one or two substitutes taken among lower alkyl or (lower)-alkoxy-group; R3 and R3' mean independently of one another hydrogen atom, lower alkyl; R4 and R4' mean independently of one another -(CH2)mOR6 or lower alkyl; or R4 and R4' form in common with N-atom to which they are bound substituted R5-cyclic tertiary amine representing pyrrolidine-1-yl, piperidine-1-yl, piperazine-1-yl, morpholine-4-yl or 1,1-dioxomorpholine-4-yl; R5 means hydrogen atom, hydroxyl, -COOR3, -N(R3)CO-lower alkyl or -C(O)R3; R6 means hydrogen atom, lower alkyl; X means -C(O)N(R6)-, -N(R6)C(O)-; n = 0, 1, 2, 3 or 4; m = 1, 2 or 3. Also, invention describes a medicinal agent comprising these compounds. Compounds can be used as drugs in treatment or prophylaxis of diseases associated with antagonists of NK-1 receptor.

EFFECT: valuable medicinal properties of agent.

6 cl, 32 ex

FIELD: organic chemistry, agriculture, insecticides.

SUBSTANCE: invention relates to a substituted anilide derivative of the formula (I): wherein R1 represents hydrogen atom, (C1-C6)-alkyl group; R2 represents hydrogen atom, halogen atom or halogen-(C1-C6)-alkyl group; R3 represents hydrogen atom, halogen atom, (C1-C6)-alkyl group, hydroxyl group or (C1-C6)-alkoxy-group; t = 1; m = 0; each among X that can be similar or different represents (C2-C8)-alkyl group, hydroxy-(C1-C6)-alkyl group or (C3-C6)-cycloalkyl-(C1-C6)-alkyl group; n = 1 or 2; Z represents oxygen atom; Q means a substitute represented by any of the following formulae: Q1-Q3, Q6, Q8-Q12, Q14-Q19, Q21 and Q23 (wherein each among Y1 that can be similar or different represents halogen atom, (C1-C6)-alkyl group, and so on); Y2 represents (C1-C6)-alkyl group or halogen-(C1-C6)-alkyl group; Y3 represents (C1-C6)-alkyl group, halogen-(C1-C6)-alkyl group or substituted phenyl group; p represents a whole number from 1 to 2; q represents a whole number from 0 or 2; r represents a whole number from 0 to 2. Also, invention proposes a chemical for control of pests of agricultural and fruit crops. The chemical comprises substituted anilide derivative of the formula (I) as an active component and represents insecticide, fungicide or acaricide. Also, invention proposes a method for addition of the chemical for control of pests of agricultural and fruits crops. Also, invention proposes aniline derivative represented by the general formula (II): wherein R1 represents hydrogen atom, (C1-C6)-alkyl group; R2 represents hydrogen atom, halogen atom or halogen-(C1-C6)-alkyl group; R3 represents hydrogen atom, halogen atom, (C1-C6)-alkyl group, hydroxyl group or (C1-C6)-alkoxy-group; t = 1; m = 0; each among X that can be similar or different represents (C2-C8)-alkyl group, hydroxy-(C1-C6)-alkyl group or (C3-C6)-cycloalkyl-(C1-C6)-alkyl group; n = 1 or 2. Invention provides the development of anilide derivative as insecticide, fungicide and acaricide against pests of agricultural and fruit crops.

EFFECT: valuable properties of compound.

5 cl, 6 tbl, 27 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new biologically active ortho-substituted nitrogen-containing bis-aryl compounds. Invention describes compounds of the formula (I): wherein A1, A2, A3, A4, A5, A6, A7 and A8 mean independently of one another nitrogen atom or -CH and wherein at least one or two (not above) these groups mean nitrogen atom; R(1) means -C(O)OR(9) or -COR(11) wherein R(9) and R(11) mean independently of one another CxH2x-R(14) wherein x has a value 0, 1, 2, 3 or 4 and R(14) means alkyl c 1, 3, 4, 5 or 6 carbon atoms, phenyl or isoxazolyl wherein phenyl and isoxazolyl are not substituted or substituted with 1, 2 or 3 substitutes chosen from the group consisting of F, Cl, Br, J, CF3, OCF3, alkyl with 1, 2, 3 or 4 carbon atoms and alkoxy-group with 1, 2, 3 or 4 carbon atoms; R(2) means hydrogen atom; R(3) means CyH2y-R(16) wherein y has a value 0, 1, 2, 3 or 4but y can't mean 0 if R(16) means -OR(17), and R(16) means alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms, cycloalkyl with 3 carbon atoms, -OR(17), phenyl or pyridyl wherein phenyl and pyridyl are not substituted or substituted with 1, 2 or 3 substitutes chosen from the group consisting of F, Cl, Br, J and alkoxy-group with 1, 2, 3 or 4 carbon atoms; R(17) means hydrogen atom; or R(3) means -CHR(18)R(19) wherein R(18) means alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms and R(19) means -CONH2; R(4) means hydrogen atom; R(30) and R(31) mean hydrogen atom, and their pharmaceutically acceptable salts also. Also, invention describes a pharmaceutical composition showing effect that inhibits K+-channel and comprising the effective amount of at least compound of the formula (I) and using compounds of the formula (I). Invention provides preparing new compounds possessing useful biological properties.

EFFECT: valuable medicinal properties of compounds and composition.

10 cl, 8 tbl, 35 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention describes derivatives of 4-phenylpyridine of the following general formulae: (IA)

and (IB) wherein R1 means and , or -NH(CH2)2OH, -NR3C(O)CH3 or -NR3C(O)-cyclopropyl; R2 means methyl or chlorine atom; R3 means hydrogen atom or methyl; R means hydrogen atom or -(CH2)2OH; n = 1 or 2, and their pharmaceutically acceptable acid-additive salts. Also, invention describes a medicinal agent possessing effect of agonist of NK-1 receptors based on these compounds. Proposed compounds show good affinity degree to NK-1 receptors and can be used in treatment or prophylaxis of diseases associated with these receptors.

EFFECT: valuable medicinal properties of compounds and agent.

10 cl, 1 tbl, 14 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of 4-phenylpyridine of the general formula: (I) wherein R means halogen or halogen atom; R1 means -(C≡C)mR1' or -(CR'=CR'')mR1'; X means -C(O)N(R8)-, -N(R8)C(O)- or -N(R8)-(CH2)p- wherein m = 0-4 and p = 1-2; values of radicals R1', R2, R3', R3, R4, R4', R8, R' and R'' are given above, and to their pharmaceutically acceptable acid-additive salts and a medicinal agent based on thereof. New compounds are neurokinine-1 antagonists and can be used as medicinal agents in treatment of diseases mediated by neurokinine-1 receptors.

EFFECT: valuable medicinal properties of derivatives.

13 cl, 119 ex

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