Antibacterial piperidine derivatives

FIELD: chemistry.

SUBSTANCE: formula (I) compound has antibacterial activity and can be used as a medicinal agent. In formula ,

R1 is hydrogen, halogen, C1-4alkyl; R2 is selected from hydrogen, halogen, C1-4alkyl; R3 is selected from hydrogen, halogen, cyano, C1-4alkyl; W is -N(R6)-; X is a single bond; ring A is an unsaturated or partially saturated ring containing 5-6 atoms, one or two of which are independently selected from nitrogen and sulphur; or an unsaturated or partially saturated bicyclic ring containing 9-10 atoms, one, two or three of which are selected from nitrogen and sulphur; R4 and R5 are substitutes on a carbon atom and are independently selected from a halogen, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, formyl, hydroxy iminomethyl, C1-4alkoxyminomethyl, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, C1-4alkoxy)carbamoyl, N-(C1-4alkyl)-N-(C1-4alkoxy)carbamoyl, C1-4alkylS(O)a, where a equals 0-2, C1-4alkoxycarbonyl, C1-4alkoxycarbonylamino, C1-4alkylsulphonylamino, (saturated or unsaturated carbocycle containing 3-7 atoms)-R10- or (saturated, partially saturated or unsaturated ring containing 5-6 atoms, one or two of which are selected from nitrogen, oxygen and sulphur)-R11-; where R4 and R5 can independently and optionally substituted at the carbon atom with one or more R12; R6 is hydrogen; n equals 1-4; where values of R4 can be identical or different; m equals 0-4; where values of R5 can be identical or different; R12 is selected from azido, halogen, cyano, hydroxy, amino, carboxy, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C1-4alkanoyl, N-(C1-4alkyl)amino, N,N-(C1-4alkyl)2amino, C1-4alkylS(O)a, where a equals 0-2, (saturated or unsaturated cabocycle containing 3-7 atoms)-R14- or (saturated, partially saturated or unsaturated ring containing 5 or 6 atoms, one or two of which are selected from nitrogen, oxygen and sulphur)-R15-; where R12 can independently and optionally be substituted at the carbon atom with one or more R9; R10, R11, R14 and R15 are independently selected from a single bond, -C(O)-, -N(R19)C(O)- or -C(O)N(R20)-; where R19 and R20 are independently selected from hydrogen or C1-4alkyl; R16 is selected from halogen, cyano, hydroxy, carboxy, methyl and methoxy. The invention also relates to a pharmaceutical composition, having antibacterial activity, containing the disclosed compound as an active ingredient, use of the disclosed compound to prepare a medicinal agent and a method of producing the compound of formula (I).

EFFECT: high activity of the compounds.

22 cl, 52 tbl, 721 ex

 

The text descriptions are given in facsimile form.

1. The compound of formula (I):

in which R1selected from hydrogen, halogen, C1-4of alkyl;
R2selected from hydrogen, halogen, C1-4of alkyl;
R3selected from hydrogen, halogen, cyano, C1-4of alkyl;
W represents-N(R6)-;
X represents a simple bond;
ring a is an unsaturated or partially saturated ring containing 5 to 6 atoms, of which one or two atoms independently selected from nitrogen and sulfur; or an unsaturated or partially saturated bicyclic ring containing 9-10 atoms, of which one, two or three atoms selected from nitrogen and sulfur;
R4and R5are substituents on carbon atom and is independently selected from halogen, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, formyl, gidroxiizomera,1-4alkoxymethyl,1-4of alkyl, C1-4alkoxy, C1-4alkanoyl,1-4alkanolamine, N-(C1-4alkyl)carbamoyl, N,N-(C1-4alkyl)2carbamoyl, N-(C1-4alkoxy)carbamoyl, N-(C1-4alkyl)-N-(C1-4alkoxy)carbamoyl, C1-4S(O)awhere a is 0-2, With1-4alkoxycarbonyl,1-4alkoxycarbonyl,1-4alkylsulfonyl, (saturated or unsaturated carbon ring containing 3-7 atoms)-R10or (saturated, partially saturated or unsaturated ring containing 5 to 6 atoms, of which one or two atoms selected from nitrogen, oxygen and sulfur)-R11-; where R4and R5independently of each other optionally may be substituted at carbon atoms by one or more R12;
R6represents hydrogen;
n is 1-4; where the values of R4may be the same or different;
m is 0-4; where the values of R5can be dinasovymi or different;
R12selected from azido, halogen, cyano, hydroxy, amino, carboxy, C1-4of alkyl, C2-4alkenyl,2-4the quinil,1-4alkoxy, C1-4alkanoyl, N-(C1-4alkyl)amino, N,N-(C1-4alkyl)2amino, C1-4S(O)andwhere a is 0-2, (saturated or unsaturated carbon ring containing 3-7 atoms)-R14or (saturated, partially saturated or unsaturated ring containing 5 or 6 atoms, of which one or two atoms selected from nitrogen, oxygen and sulfur)-R15-; where R12independently of each other optionally may be substituted at carbon atoms by one or more R16;
R10, R11, R14and R15independently selected from a simple link, -C(O)-, -N(R19)C(O)- or-C(O)N(R20)-; where R19and R20independently selected from hydrogen or C1-4of alkyl;
R16selected from halogen, cyano, hydroxy, carboxy, methyl and methoxy;
or its pharmaceutically acceptable salt.

2. The compound according to claim 1 or its pharmaceutically acceptable salt, which is a compound of formula (IA)

3. The compound according to claim 2 or its pharmaceutically acceptable salt, which is a compound of formula (IB)

4. The compound according to claim 3 or its pharmaceutically acceptable salt that p is ecstasy a compound of formula (IC)

5. The compound according to claim 4 or pharmaceutically acceptable salt, which is a compound of formula (IE)

in which Y represents NH, N(C1-4alkyl) or S;
where R5aand R5brepresent substituents as defined for R5or together with the carbon atoms to which they are attached, form a 6-membered carbocycle ring, substituted with one or two groups which may be the same or different and are selected from R5.

6. The compound according to claim 5 or its pharmaceutically acceptable salt, which is a compound of formula (IF)

7. The connection according to claim 6 or its pharmaceutically acceptable salt, in which R1represents methyl.

8. The connection according to claim 7 or its pharmaceutically acceptable salt, in which R2represents chlorine.

9. The compound of claim 8 or its pharmaceutically acceptable salt, in which R3represents chlorine.

10. The connection according to claim 9 or its pharmaceutically acceptable salt, in which R4is Deputy on the carbon atom and is selected from methoxy, hydroxy, methoxycarbonyl, fluorine, allyloxy, propoxy, N,N-dimethylcarbamoyl, morpholinomethyl, N-ethylcarbazole, N-(2-hydroxyethyl)carbamoyl, dimethylamino the sludge, N-methyl-N-methoxycarbonyl, methoxymethyl, methylaminomethyl and carboxy.

11. The compound of claim 10 or its pharmaceutically acceptable salt, in which R5is Deputy on the carbon atom and selected from halogen, carboxy, carbamoyl,1-4of alkyl, C1-4alkoxy, N-(C1-4alkyl)carbamoyl, N-(C1-4alkoxy)carbamoyl or1-4alkoxycarbonyl; where R5optionally may be substituted at carbon atoms by one or more R12; R12selected from C1-4alkoxy or carbocyclic-R14-; and R14is a simple link.

12. The compound according to claim 1, which is a
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-foreperiod-1-yl)-1,3-thiazole-5-carboxylic acid;
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-{[(2-methoxyethyl)amino]carbonyl}-1,3-thiazole-5-carboxylic acid;
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-({[(1S)-2-methoxy-1-methylethyl]amino}carbonyl)-1,3-thiazole-5-carboxylic acid;
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-[(methylamino)carbonyl]-1,3-thiazole-5-carboxylic acid;
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-methyl-1,3-thiazole-5-carboxylic acid;
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-the l)carbonyl]amino}-3-methoxypiperidine-1-yl)-1,3-thiazole-5-carboxylic acid;
4-acetyl-2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-1,3-thiazole-5-carboxylic acid;
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-({[(1R)-2-methoxy-1-methylethyl]amino}carbonyl)-1,3-thiazole-5-carboxylic acid;
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-({[(2S)-2-methoxypropyl]amino}carbonyl)-1,3-thiazole-5-carboxylic acid;
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-({[(2R)-2-methoxypropyl]amino}carbonyl)-1,3-thiazole-5-carboxylic acid;
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-({[(1R,2S)-2-forciblepoppy]amino}carbonyl)-1,3-thiazole-5-carboxylic acid;
CIS()2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-1,3-benzothiazole-7-carboxylic acid;
CIS()2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-(methoxymethyl)-1,3-thiazole-5-carboxylic acid;
CIS()2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)isonicotinate acid;
2-((3S,4R)-4-{[(4-chloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-1,3-benzothiazole-7-carboxylic acid;
CIS()-2-(3-chloro-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidine-1-yl)-4-(methoxymethyl)-1,3-thiazole-5-carboxylic acid;
2-((3S,4's)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-foreperiod-1-yl)-4-methyl-1,3-thiazole-5-carboxylic acid;
CIS()-2-[4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-(prop-2-in-1 yloxy)piperidine-1-yl]-1,3-thiazole-5-carboxylic acid;
CIS()2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-foreperiod-1-yl)-1,3-thiazole-4-carboxylic acid; or
2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-({[2-methoxy-1-(methoxymethyl)ethyl]amino}carbonyl)-1,3-thiazole-5-carboxylic acid;
or its pharmaceutically acceptable salt.

13. The compound according to claim 1, which is a
ethyl 2-((3S,4R)-4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-yl)-4-({[2-methoxy-1-(methoxymethyl)ethyl]amino}carbonyl)-1,3-thiazole-5-carboxylate;
or its pharmaceutically acceptable salt.

14. Pharmaceutical composition having antibacterial activity, containing as active ingredient a compound according to any one of claims 1 to 13 or its pharmaceutically acceptable salt and a pharmaceutically acceptable diluent or carrier.

15. The compound according to any one of claims 1 to 13 or its pharmaceutically acceptable salts, which have antibacterial activity intended for use as a medicine.

16. The use of the compounds of formula (I) or its pharmaceutically acceptable salt according to any one of claims 1 to 13 for the preparation of medicinal products that have antibacterial and the efficiency.

17. The method of obtaining compounds of formula (I) or their pharmaceutically acceptable salts according to claim 1, including the interaction of the compounds of formula (V):

with the compound of the formula (IV) or its activated derivative of the acid

and then, if necessary:
i) the conversion of compounds of formula (I) into another compound of formula (I);
ii) removing any protective groups;
iii) formation of pharmaceutically acceptable salts.

18. The compound which is 2-[(3S,4R)-4-[(3,4-dichloro-5-methyl-1H-pyrrole-2-carbonyl)amino]-3-methoxy-1-piperidyl]-4-[[(1S)-2-methoxy-1-methylethyl]carbarnoyl]thiazole-5-carboxylic acid or its pharmaceutically acceptable salt.

19. The connection, which is 4-acetyl-2-[(3S,4R)-4-[(3,4-dichloro-5-methyl-1H-pyrrole-2-carbonyl)amino]-3-methoxy-1-piperidyl]thiazole-5-carboxylic acid or its pharmaceutically acceptable salt.

20. The compound which is 2-[(2S,4R)-4-[(3,4-dichloro-5-methyl-1H-pyrrole-2-carbonyl)amino]-3-methoxy-1-piperidyl]-4-(2-methoxyethanol)thiazole-5-carboxylic acid or its pharmaceutically acceptable salt.

21. The compound according to any one of p-9,
where R5arepresents carboxy;
R5bis a N-(C1-4alkyl)carbarnoyl or1-4alkanoyl, where each R5optionally can be substituted one is m or more R 12;
R12represents a C1-4alkoxy.

22. Connection item 21, where R4represents methoxy.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention describes compounds of formula I: formula I or its pharmaceutically acceptable salt, where the radical values R3, R4, R2, X1, X2, R1 are such as presented in claim 1. Also, the invention describes a pharmaceutical composition exhibiting a Tec-family kinase inhibitor activity and based on the compounds of formula I, a method of Tec-family kinase activity inhibition, and a method of producing the compound of formula I.

EFFECT: produced and described new compounds which are effective as Tec-family (eg, Tec, Btk, Itk/Emt/Tsk, Bmx, Txk/Rlk) protein kinase inhibitors, and acceptable compositions are applicable for treatment or prevention of some diseases, disorders or conditions including but not limited, autoimmune, inflammatory, proliferative or hyperproliferative, or immunologically mediated diseases.

50 cl, 18 ex, 3 tbl

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

FIELD: medicine.

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

EFFECT: increased antiamyloidogenic action.

20 cl, 20 tbl, 6 dwg, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I): where: A is a monocyclic or polycyclic aryl or heteroaryl group, where the heteroaryl radical denotes a 5-10-member cyclic system containing at least one heteroaromatic ring and containing at least one heteroatom selected from O, S and N; optionally substituted with one or more substitutes independently selected from a group comprising halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, C1-4alkoxy and a hydroxyl group; B is a monocyclic nitrogen-containing heteroaryl group, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from S and N; optionally substituted with one or more substitutes selected from a group consisting of halogen atoms, C1-4alkyl, C3-8cycloalkyl, C3-8cycloalkyl-C1-4alkyl, aryl and C1-8alkylthio; either a) R1 is a group of formula: -L-(CR'R")n-G, where L is a binding group selected from a group consisting of a direct bond, -(CO)-, -(CO)NR'- and -SO2-; R' and R" is independently selected from hydrogen atoms; n assumes values from 0 to 1; and G is selected from a group consisting of a hydrogen atom and C1-4alkyl, aryl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O, S and N; C3-8cycloalkyl and saturated heterocyclic groups, where heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one or two carbon atoms are substituted with a N heteroatom; where alkyl, C3-8cycloalkyl, aryl or heteroaryl groups are unsubstituted or substituted with one or more substitutes selected from halogen atoms; and R2 is a group selected from hydrogen atoms, halogen atoms and C1-4alkyl, C2-5alkynyl, C1-4alkoxy, -NH2 and cyano groups, where alkyl and alkynyl groups may be unsubstituted or substituted with one aryl group; or b) R2, R1 and -NH- group to which R1 is bonded form a group selected from groups of formulae and , where: Ra is selected from a hydrogen atom or groups selected from C1-4alkyl, C3-8cycloalkyl, aryl, aryl-C1-4alkyl, heteroaryl, where the heteroaryl radical denotes a 5-6-member heteroaromatic ring containing at least one heteroatom selected from O and N; saturated heterocyclic rings, where the heterocyclic group denotes a non-aromatic saturated 6-member carbocyclic ring in which one carbon atom is substituted with a heteroatom selected from O and N; and C1-4alkylthio; where the aryl or heteroaryl groups are unsubstituted or substituted with one or more groups selected from halogen atoms, cyano group, trifluoromethoxy and carbamoyl; Rb denotes hydrogen; and pharmaceutically acceptable salts thereof and N-oxides; provided that the compound is not selected from N-[6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]benzamide, and N-[3-ethoxycarbonyl-6-(1-methyl-1H-indol-3-yl)-5-pyridin-2-ylpyrazin-2-yl]formamide. The invention also relates to a pharmaceutical composition, use of compounds in any of claims 1-20, a method of treating a subject, as well as a composite product.

EFFECT: obtaining novel biologically active compounds having adenosine A2B receptor antagonist activity.

27 cl, 160 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted 2-quinolyloxazoles of formula (I) or pharmaceutically acceptable salts thereof, having PDE4 inhibiting properties, a pharmaceutical composition based on said compounds and use thereof to prepare a medicinal agent which inhibits inflammatory cell recruitment in respiratory tracts. , where is , X is O, R1 is alkyl, R3 and R4 are independently selected from H, R5 and R6 are independently selected from a group comprising H, alkyl, hydroxyalkyl, t equals 1 or 2. Values of substitutes R7-R11, R13 are given in the formula of invention.

EFFECT: high efficiency of using the composition.

24 cl, 1 dwg, 64 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to oxazolidinone derivatives covered by general graphic formula (I) and to their pharmaceutically acceptable salts. In formula (I) R1, R2, R3 and R4 are independently chosen from a group including -H and halogen; A is chosen from a group including R5 and R6 are independently chosen from a group including -H, -F, -CI, -Br, -OH, alkyl(C1-C6), haloalkyl(C1-C6), alkoxygroup(C1-C6); R7 is chosen from a group including -H, alkyl(C1-C6); either R7 and R5 or R6 taken together form a cycle of 2 carbon atoms and include 1 group chosen from O which in turn can be substituted by one substitute chosen from alkyl(C1-C6); R12 is chosen from a group including -H, -COR14, -CSR14, -COOR14; R14 is chosen from a group including alkyl (C1-C6), cycloalkyl(C3-C6), alkenyl(C2-C6), R16, R17 and R18 represent -H; R21 is chosen from a group including -H, alkyl(C1-C6); X is chosen from a group including O, S, and Y is chosen from a group including O, S, SO, SO2, and NR12; and optional substitutes of alkyl(C1-C6) groups can represent one or two groups chosen from the following: -OR21, -CN.

EFFECT: invention refers to methods for preparing the compounds of the invention, to application of oxazolidinone derivatives for preparing a drug for treating bacterial infections and to a pharmaceutical composition for treating bacterial infections, including a therapeutically effective amount of the compound of the invention.

36 cl, 10 tbl, 44 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates or tautomers thereof, where substitute M is selected from groups D1 and D2, having structural formulae given below, and R1, E, A and X are as described in the formula of invention. Disclosed also are pharmaceutical compositions which contain these compounds, methods for synthesis of these compounds, intermediate compounds and synthesis methods thereof, as well as use of compounds of formula (I) in preventing or treating diseases mediated by CDK kinases, GSK-3 kinases or Aurora kinases.

EFFECT: high effectiveness of the compounds.

40 cl, 8 dwg, 18 tbl, 84 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

FIELD: medicine, pharmaceutics.

SUBSTANCE: compound of formula pharmaceutically acceptable salt or solvate of a compound or salt (I), ring Q represents optionally substituted monocyclic or condensed (C6-C12)aryl or optionally substituted monocyclic or condensed heteroaryl where said substitutes are chosen from: halogen; (C1-C6)alkyl optionally substituted by 1-3 halogen atoms; (C1-C6)alkylsulphonyl; phenyl optionally substituted by 1 or 2 substitutes chosen from halogen, (C1-C6)alkyl which can be substituted by 1-3 halogen atoms, groups (C1-C6)alkylamino, di(C1-C6)alkylamino, (C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkyl and (C1-C6)alkylthio; monocyclic or condensed heteroaryl optionally substituted by halogen; or oxo; Y1 represents a bond or -NR6-CO-, where R6 represents hydrogen, ring A represents optionally substituted a nonaromatic heterocyclyldiyl where said substitutes are chosen from (C1-C6)alkyl optionally substituted by groups hydroxy, (C1-C6)alkylamino, di(C1-C6)alkylamino, morpholino, (C1-C6)alkylaminocarbonyl, di(C1-C6)alkylaminocarbonyl; cyano; (C3-C6)cycloalkyl; (C1-C6)alkoxy; (C1-C6)alkoxy(C1-C6)alkyl; phenyl; benzyl; benzyloxymethyl; thienyl; 4-8-members monocyclic nonaromatic heterocycle having 1 or 2 heteroatoms chosen from N or O, and optionally substituted by 1 or 2 substitutes chosen from (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkoxy(C1-C6)alkyl and oxo; (C1-C6)alkylamino; di(C1-C6)alkylamino; a group of formula: -Y2Z'- represents a group of formula: [Formula 2] each R7 independently represents hydrogen, (C1-C6)alkyl or (C3-C6)cycloalkyl, each of R8 and R9 independently represents hydrogen or (C1-C6)alkyl, n is equal to an integer 0 to 3, Z1 represents a bond, -O-, -S- or-NR9 - where R9 represents hydrogen, (C1-C6)alkyl, acyl or (C1-C6)alkylsulphonyl, ring B represents optionally substituted aromatic carbocyclediyl or optionally substituted aromatic heterocyclediyl where said substitutes are chosen from (C1-C6)alkyl, halogen, (C1-C6)alkoxy and oxo; Y3 represents a bond optionally substituted (C1-C6)alkylene or (C3-C6)cycloalylene, optionally interrupted -O- or optionally substituted (C2-C6)alkenylene where said substitutes are chosen from (C1-C6)alkyl, (C3-C6)cycloalkyl, halogen and (C1-C6)alkoxycarbonyl; Z2 represents COOR3; R3 represents hydrogen or (C1-C6)alkyl.

EFFECT: preparation of new compounds.

30 cl, 9 tbl, 944 ex

FIELD: medicine.

SUBSTANCE: invention refers to the compound 3-{[5-(azetidine-1-ylcarbonyl)pyrazine-2-yl] oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazine-5-yl)benzamide or to its pharmaceutically acceptable salt. Also, it refers to a pharmaceutical composition for treating insulin-independent diabetes or obesity containing said compound.

EFFECT: there is produced and described a new compound which can be effective in treating insulin-independent diabetes and obesity.

5 cl, 64 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new benzimidazole derivatives of general formula I and to their pharmacologically acceptable salts, where lb R = CI, R1 = H, R2 = 3,4-Cl2-C6H3; Ic R = H, R1 = CH3, R2 = 3,4-C12-C6H3; Id R = H, R1 = CI, R2 = CONH2; X = Cl-, Br-, showing antibacterial action.

EFFECT: new benzimidazole derivatives exhibiting high antibacterial activity are produced.

1 cl, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medication for treatment of infectious disease, cancer treatment, wound healing and/or detoxification of subject, which contains nanoparticles of heterocrystalline mineral selected from group of heterocrystalline minerals SiO2, quartzite, grothite, leucoxene and rutilated quartz. Nanoparticles of said minerals have sizes from 0.5 to 200 nm, have ability to desorption in water, can be transported into cell by DNA molecule and can be applied together with anti-metabolic anti-tumour medication.

EFFECT: nanoparticles of heterocrystalline minerals demonstrate high chemical and biological activity.

13 cl, 3 ex, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of biotechnoloy and deals with compositions for production of vaccine against Neisseria meningitidis, which represent conjugates of different serogroups of N. meningitides with protein-carrier, selected from bacterial toxins or anatoxins, with specified size, in determination by gel-penetrating chromatography (GPC) and/or definite molecular weight in determination by exclusion chromatography with detecting by photometry of multi-angle light diffusion (SEC-MALS).

EFFECT: conjugates of claimed sizes, representing saccharide fragments, are applied in combination into polyvalent vaccine.

6 cl, 11 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to biotechnologies and represents immunogenic composition - emulsion of type "oil-in-water", which contains water solution, containing antigen or immunogen, nonionogenic lipophilic ethoxylated C9-C22 alcohol of fatty series, ethoxylated 1-4 EO, mineral oil, which contains linear or branched carbon chain, which contains from 15 to 32 atoms of carbon, nonionic hydrophilic surface-active substance, which represents ethoxylated C9-C22 alcohol from fatty series, ethoxylated 5-21 EO. Total concentration of surface-active substances (by weight per volume of emulsion) constitutes from 0.2% to 6.5%, concentration of oil phase, which includes oil(s) and surface-active substances constitutes from 2% to 50% and temperature of phase inversion (PIT) constitutes from 25C to 65C.

EFFECT: invention can be applied as adjuvant.

19 cl, 5 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine, namely to infectious diseases, and can be used for treating whooping cough and/or for Bordetella infection protection. Polypeptide under the invention represents a fragment of adenylate cyclase Bordetella containing CD11b/CD18 interaction domain from an amino acid sequence extended from position 1166 to position 1281 SEQ ID NO:1. Said invention also concerns the specific fragments of adenylate cyclase Bordetella containing CD11b/CD18 interaction domain, and to their application, particularly for targeting of molecules of interest to CD11b expressing cells.

EFFECT: use of the inventions allows extending the range of products for treatment and prevention of the Bordetella infection.

26 cl, 9 dwg

FIELD: medicine.

SUBSTANCE: invention refers to a compound of formula to its salt or hydrate where R1 represents hydrogen atom, alkyl group containing 1-6 carbon atoms or cycloalkyl group containing 3-6 carbon atoms; and alkyl group is optionally substituted by halogen atom; R2 represents hydrogen atom or alkyl group containing 1-6 carbon atoms; R3 represents alkyl group containing 1-6 carbon atoms or cycloalkyl group containing 3-6 carbon atoms; and alkyl group is optionally substituted by halogen atom; R4 and R5 independently represent hydrogen atom, halogen atom, alkyl group containing 1-6 carbon atoms, alkoxygroup containing 1-6 carbon atoms or alkenyl group containing 2-6 carbon atoms; and alkyl group is optionally substituted by halogen atom; and provided R4 and R5 are not hydrogen atoms simultaneously; or substitutes R4 and R5 together represent (a) 3-6-members cyclic compound including carbon atom, common for R4 and R5, with formation of a spirocyclic compound with a pyrrolidine ring; or (b) exomethylene group bound with the pyrrolidine ring by a double bond; R6 and R7 independently represent hydrogen atom or alkyl group containing 1-6 carbon atoms; R8 represents halogen-substituted alkyl group containing 1-6 carbon atoms or cycloalkyl group containing 3-6 carbon atoms; and cycloalkyl group can be substituted by halogen atom; R9 represents hydrogen atom; X1 represents hydrogen atom or halogen atom; and A represents nitrogen atom or a fragment presented by formula , where X2 represents hydrogen atom, alkyl group containing 1-6 carbon atoms or alkoxygroup containing 1-6 carbon atoms; or X2 together with R8 represents a cyclic compound containing a portion of a nucleus, and the ring formed thereby optionally contains oxygen atom and is substituted by alkyl group containing 1-6 carbon atoms. Besides, the invention refers to an antibacterial agent based on the compound of formula I, to a therapeutic agent for infections, to a method of treating an infectious disease and an application of said compounds for preparing an antibacterial drug.

EFFECT: there are produced and described new compounds showing strong antibacterial activity in relation to gram-positive and gram-negative bacteria.

30 cl, 112 ex, 10 tbl, 4 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds - benzoquinone derivatives of formula (I): , where each of R1 and R2 is O-C(O)phenyl; where the phenyl is substituted with 1 substitute selected from halide, nitro, C1-C6 alkyl or C1-C6 alkoxy, and pharmaceutically acceptable salts thereof.

EFFECT: low activity of pancreatic lipase based on compounds of the said formula.

6 cl, 3 tbl, 23 ex

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine and deals with improvements of meningococcus outer membrane vesicles (OMV), directed against particular epidemic strains, which cam be extremely efficiently used for struggle with local outbreaks of the disease. Essence of method includes mixture of (OMV), from 2 serortypes of meningococci P1.7b,4 and PI.7,16, set for meningitis treatment and method of introduction of OMV-based composition.

EFFECT: elaboration of vaccine for mass immunisation.

12 cl

FIELD: medicine.

SUBSTANCE: claimed is application of: (a) solvating system which contains surface active substance, able to separate, remove or destruct in any other way, at least, part of biofilm, attached or adhered to a part of middle or internal ear, to the surface in nasal cavity or in sinus cavity, or to mouth or gullet tissue, and (b) polymer film-forming medical hermetic, able to form protective layer above the place, on which such biofilm was destroyed, and which possesses adhesion to natural tissues in the processed place and is resistant to separation or other destruction until natural decomposition or resorption of hermetic takes place, for manufacturing therapeutic system for treatment of infectious diseases of ear or throat, corresponding method of treatment and composition of said hermetic and anti-microbial preparation, which includes gallium-containing compound for application in the method. Demonstrated is 5.2-fold logarithmic reduction of the level of microbial contamination in vitro by cultures Staphylococcus aureus, Pseudomonas aeruginosa.

EFFECT: invention suggests efficiency of treatment by the claimed method of chronic otitis media with evaporation (COME), recurrent acute otitis media (RAOM), cholesteatoma, chronic rhinosinusitis.

71 cl, 4 dwg, 2 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to oxazolidinone derivatives covered by general graphic formula (I) and to their pharmaceutically acceptable salts. In formula (I) R1, R2, R3 and R4 are independently chosen from a group including -H and halogen; A is chosen from a group including R5 and R6 are independently chosen from a group including -H, -F, -CI, -Br, -OH, alkyl(C1-C6), haloalkyl(C1-C6), alkoxygroup(C1-C6); R7 is chosen from a group including -H, alkyl(C1-C6); either R7 and R5 or R6 taken together form a cycle of 2 carbon atoms and include 1 group chosen from O which in turn can be substituted by one substitute chosen from alkyl(C1-C6); R12 is chosen from a group including -H, -COR14, -CSR14, -COOR14; R14 is chosen from a group including alkyl (C1-C6), cycloalkyl(C3-C6), alkenyl(C2-C6), R16, R17 and R18 represent -H; R21 is chosen from a group including -H, alkyl(C1-C6); X is chosen from a group including O, S, and Y is chosen from a group including O, S, SO, SO2, and NR12; and optional substitutes of alkyl(C1-C6) groups can represent one or two groups chosen from the following: -OR21, -CN.

EFFECT: invention refers to methods for preparing the compounds of the invention, to application of oxazolidinone derivatives for preparing a drug for treating bacterial infections and to a pharmaceutical composition for treating bacterial infections, including a therapeutically effective amount of the compound of the invention.

36 cl, 10 tbl, 44 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds selected from a group comprising piperazine compounds of formula I: , where X is -CH2- or a bond; n equals 1; R1 is alkyl; cycloakyl; hydroxyethyl; benzo[1,3]dioxolyl; phenyl, which can be mono-substituted with a halide, alkyl, alkoxy, -CF3 or alkylcarbonyl; or phenyl which is di- or tri-substituted with substitutes independently selected from alkyl and halide; pyridyl which can be mono-substituted with a halide, alkyl or -CF3; furanyl which can be mono-substituted with methyl, hydroxymethyl or bromine, or furanyl which is disubstituted with an alkyl; thienyl which can be mono-substituted with methyl or chromium; pyrimidinyl; isoquinolinyl; benzhydryl; imidazolyl optionally mono-substituted with an alkyl; or thiazolyl; or X is -C(=O)- and R1 is hydrogen; R2 is indolyl, imidazolyl optionally mono-substituted with alkyl; phenyl which can be mono-substituted with a halide, alkyl, hydroxy or cyano, or phenyl which is disubstituted with a halide; pyridyl; benzothienyl; thiazolyl or thienyl; R3 is indolyl, pyridyl which can be mono-substituted with alkoxy, alkoxyalkoxy, NR31R32, morpholine, piperadine, oxopiperidinyl, oxopyrrolidinyl, pyridyl or phenyl; or phenyl which is mono-substituted with phenyl, pyridyl, alkyl, alkoxy, dialkylamino, morpholine, N-benzyl-N-alkylamino, (dialkylamino)alkoxy, phenylalkoxy or tetrahydroisoquinolinyl; or R3 denotes the group: , where Z is phenyl or pyridyl; R31 is 2-C1-C5alkoxyethyl, phenyl, pyridyl, phenylalkyl, hydroxyalkylcarbonyl, alkylcarbonyl, cycloalkylcarbonyl or phenylcarbonyl; R32 is hydrogen or methyl; R35 is alkyl, alkylcarbonyl, phenyl, pyridyl or pyrimidinyl; and R4 is phenyl-CH=CH-, where the phenyl can be mono-, di- or tri-substituted with substitutes independently selected from halide, alkyl, alkoxy and -CF3; or phenyl-CH2-CH2, where the phenyl is disubstituted with -CF3; and to optically pure enantiomers thereof, mixtures of enantiomers, such as, for example, racemates, optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates and mesoforms, such as salts of such compounds. The invention also relates to a pharmaceutical composition, as well as to use of compounds in any of claims 1-4.

EFFECT: obtaining novel biologically active compounds with antimalarial activity.

8 cl, 138 ex, 1 tbl

Up!