Acylsulfonamides as steroid sulfatase inhibitors

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of formulas (Ip3) or (Ip4) wherein R1P3 means unsubstituted or substituted phenyl or thienyl wherein substitutes represent halogen atom, (C1-C6)-alkyl, (C1-C4)-halogenalkyl, nitro group, (C1-C4)-alkoxy group; R16P3 and R17P3 in common with carbon atom to which they are bound mean a bridge-bound saturated (C5-C12)-ring system that is substituted with (C4-C12)-alkyl, (C1-C6)-alkoxycarbonylamino group, for example, tert.-butoxycarbonylamino group; R18P3 means hydrogen atom; R1P4 means unsubstituted or substituted phenyl or thienyl wherein substitutes represent halogen atom, (C1-C6)-alkyl, (C1-C4)-halogenalkyl, nitro group, (C1-C4)-alkoxy group; R16P4 and R17P4 in common with carbon atom to which they are bound mean a substituted bridge-bound saturated (C5-C12)-cycloalkyl ring system, substituted piperidine or substituted bridge-bound piperidine wherein substitutes mean (C1-C6)-alkoxyoxycarbonyl, (C1-C6)-alkyl, unsubstituted phenyl or phenyl substituted with (C4-C12)-alkyl, (C1-C4)-halogenalkyl, nitro group, aminocarbonyl; R18P4 means hydrogen atom or hydroxyl but hydrogen atom preferably; mP4 means 1. Compounds of formulas (Ip3) and (Ip4) inhibit activity of steroid sulfatase that allows their using as components of pharmaceutical composition.

EFFECT: valuable biochemical and medicinal properties of compounds and pharmaceutical composition.

7 cl, 13 tbl, 386 ex

 

The text descriptions are given in facsimile form.

1. The compound of the formula IP3or IP4

where R1P3represents unsubstituted or substituted phenyl or thienyl, where the substituents are halogen, C1-C6alkyl, C1-C haloalkyl, nitro, C1-C4alkoxy;

R16P3and R17P3together with the carbon atom to which they are bound, denote the associated bridge rich C5-C12ring system which is substituted With4-C12the alkyl, C1-C6alkoxycarbonyl, for example, tert-butoxycarbonylamino;

R18P3denotes hydrogen;

R1P4represents unsubstituted or substituted phenyl or thienyl, where the substituents are halogen, C1-C6alkyl, C1-C4haloalkyl, nitro, C1-C4alkoxy;

R16P4and R17P4together with the carbon atom to which they are bound, denote a substituted connected by a bridge saturated With5-C12cycloalkyl ring system, substituted piperidine or substituted associated bridge piperidine, where the substituents mean C1-C6alkoxycarbonyl, C1-C6alkyl, unsubstituted phenyl or phenyl substituted With4-C12the alkyl, C1-C4haloalkyl, nitro, aminocarbonyl;

R18P4denotes hydrogen or hydroxyl, more preferably hydrogen, mP4denotes 1.

2. The compound according to claim 1, which is a compound of the formula

3. Connection is one which one of claims 1 or 2 in the form of salts.

4. The connection according to one of claims 1 to 3 for use as a pharmaceutical drug that inhibits asteroidsurfaces.

5. The connection according to one of claims 1 to 3 for use for the preparation of drugs that inhibits asteroidsurfaces.

6. The pharmaceutical composition inhibiting asteroidsurfaces, comprising pharmaceutically effective amount of at least one compound according to one of claims 1 to 3 in combination with at least one pharmaceutically acceptable excipient.

7. The connection according to one of claims 1 to 3 for use for preparing a pharmaceutical drug that inhibits asteroidsurfaces.



 

Same patents:

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel pyrrolidine-2-ones of the formula (I): , wherein R1 means group chosen from the following formulae:

wherein each of them comprises optionally additional nitrogen (N) atom as a heteroatom; Z means optional substitute halogen atom, -CH2NH2, -NRaRb or -CN; Z' means optional substitute halogen atom, -CH2NH2 or -CN; alk means alkylene or alkenylene; T means sulfur atom (S), oxygen atom (O); R2 means hydrogen atom (H), -(C1-C3)-alkyl-CONRaRb, -(C1-C3)-alkyl-CO2-(C1-C4)-alkyl, -(C1-C3)-alkylmorpholino-group, -CO2-(C1-C4)-alkyl or -(C1-C3)-alkyl-CO2H; X means phenyl or 5- or 6-membered aromatic or nonaromatic heterocyclic group comprising one or two heteroatoms chosen from O, N or S wherein each of them is substituted optionally with 0-2 groups chosen from halogen atom, -CN, -(C1-C4)-alkyl, -(C2-C4)-alkenyl, -CF3, -NRaRb, -NO2, -N-(C1-C4)-alkyl-(CHO), -NHCO-(C1-C4)-alkyl, -NHSO2Rc, -(C0-C4)-alkyl-ORd, -C(O)Rc, -C(O)NRaRb, -S(O)nRc and -S(O)2NRaRb; Y means: (i) a substitute chosen from H, halogen atom, -CN, -(C1-C4)-alkyl, -(C2-C4)-alkenyl, -CF3, -NRaRb, -NO2, -N-(C1-C4)-alkyl-(CHO), -NHCO-(C1-C4)-alkyl, -NHSO2Rc, -(C0-C4)-alkyl-ORd, -C(O)Rc, -C(O)NRaRb, -S(O)nRc and -S(O)2NRaRb, or (ii) phenyl or 5- or 6-membered aromatic or nonaromatic heterocyclic group comprising one or two heteroatoms, chosen from O, N or S and wherein each of them is substituted optionally with 0-2 groups chosen from halogen atom, -CN, -(C1-C4)-alkyl, -(CH2)nNRaRb, -(CH2)nN+RaRbCH2CONH2, -(C0-C4)-alkyl-ORd, -C(O)Rc, -C(O)NRaRb, -S(O)nRc, -S(O)2NRaRb, =O, oxide at N atom in cycle, -CHO, -NO2 and -N-(Ra)(SO2Rc) wherein Ra and Rb mean independently H, -(C1-C6)-alkyl; Rc means -(C1-C6)-alkyl; Rd means H, -(C1-C6)-alkyl; n means 0-2, and to their pharmaceutically acceptable salts or solvates. Compounds inhibit Xa factor that allows their using as components of pharmaceutical composition.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

10 cl, 144 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to novel compounds of the general formula (I): wherein R1 represents hydrogen atom or linear or branched (C1-C4)-alkyl group; R2 represents hydrogen atom or linear or branched (C1-C4)-alkyl group; R3 represents phenyl, thienyl or furyl group that are substituted optionally with one or more linear or branched (C1-C4)-alkyl group, linear or branched (C1-C4)-alkoxy-group or halogen atom; R4 and R5 represent independently of one another hydrogen atom, (C3-C6)-cycloalkyl group, linear or branched (C1-C4)-alkyl group comprising optionally amino-group or amino-group substituted with one or two linear or branched (C1-C4)-alkyl groups, hydroxy-group, carboxy-group or alkoxy-group substituted with linear or branched (C1-C4)-alkyl group; or R4 represents hydrogen atom or linear or branched (C1-C4)-alkyl group or benzyl group; R5 represents hydrogen atom, group -SO2OH or formyl group, or R4 and R5 in common with nitrogen atom form group of the general formula (a): wherein R7 and R8 represent independently one another hydrogen atom, linear or branched (C1-C4)-alkyl group; R6 represents phenyl, benzyl, thienyl or furyl group that are substituted optionally with methylenedioxy-group or one or more linear or branched (C1-C4)-alkyl group, linear or branched (C1-C4)-alkoxy-group or halogen atom; X represents group -NH or oxygen atom; Z represents oxygen atom, sulfur atom, group -CH2, group -NH or group -NR11 wherein R11 represents hydrogen atom, linear or branched (C1-C4)-alkyl group, group -SO2OH, linear or branched (C1-C4)-acyl group; n = 0, 1 or 2; m = 1, 2 or 3; o = 1, 2 or 3; p = 0 or 1; r = 0 or 1, and their salts and solvates. Also, invention relates to a method for synthesis of compounds of the general formula (I), to a pharmaceutical composition, its using and to compounds of the general formulas (I''), (II''), (III''), (IV''), (V''), (VI''), (VII''), (VIII'') and (XIII'') given in the invention description. Invention provides synthesis of novel biologically active compounds that are ligands of adenosine A3 receptors but as antagonists preferably.

EFFECT: valuable biological properties of compounds.

20 cl, 1 tbl, 40 ex

FIELD: organic chemistry, herbicides.

SUBSTANCE: invention relates to substituted thene-3-ylsulfonylamino(thio)carbonyltriazolinones of the formula (I) and their salts wherein Q means oxygen or sulfur atom; R1 and R2 mean alkyl with 1-6 carbon atoms; R3 means hydrogen atom, halogen atom, alkyl with 1-6 carbon atoms substituted if necessary with alkoxy-group with 1-4 carbon atoms, alkoxy-group with 1-6 carbon atoms substituted if necessary with halogen atom or alkoxy-group with 1-4 carbon atoms, alkylthio-group with 1-6 carbon atoms, cycloalkyl with 3-6 carbon atoms, or aryl, aryloxy- or arylalkoxy-group, respectively, with 6 or 10 carbon atoms in aryl moiety and, in case of arylalkoxy-group, with 1-4 carbon atoms in alkyl moiety; R4 means alkyl with 1-6 carbon atoms, alkoxy-group with 1-6 carbon atoms, dialkylamino-group, respectively, with 1-4 carbon atoms in alkyl moieties, cycloalkyl with 3-6 carbon atoms, or in common with R3 it means if necessary, branched or substituted with alkyl with 1-4 carbon atoms oxaalkanediyl, thiaalkanediyl or azaalkanediyl with 3-6 carbon atoms and wherein oxa-, thia- or aza-groups can be at the beginning, at the terminal part or inside of alkanediyl group. Proposed compounds elicit the herbicide activity. Also, invention describes herbicide agent based on compounds of the formula (I).

EFFECT: valuable property of compounds, and agent.

10 cl, 23 tbl, 3 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to synthesis of thiophene of the general formula (I): wherein R1 and R2 mean independently of one another, H, F, Cl, Br, J or -(X)n-CqH2q-Z; n = 0; R3 means hydrogen atom, methyl, F, Cl, Br or J; R4 means hydrogen atom or -CrH2r-Y wherein Y means hydrogen atom or trifluoromethyl; R5 and R6 mean hydrogen atom or in common they mean a bond; R7 and R8 mean in common alkylene chain; or R7 and R8 mean in common residue of the formula: ; R10 and R11 mean independently of one another hydrogen atom, fluorine atom, chlorine atom, bromine atom, methyl, -OH, -O-CH3 or -CF3; R9 and R12 mean hydrogen atom or F; or one of substitutes in R9 and R12 mean hydrogen atom and another means F, Cl, Br, J, -COOH, -CO-NR13R14 or -(X)n-CqH2q-Z; R13 and R14 in common with nitrogen atoms to which they are bound form saturated 5-, 6- or 7-membered cycle, and their pharmaceutically acceptable salts also. Compounds of the formula (I) possess inhibitory effect on NHE and can be used in treatment of respiration disorders, diseases caused by ischemic and/or reperfusion symptoms and diseases of the central nervous system. Also, invention describes a medicinal agent based on compound of the formula (I) and its using.

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

10 cl, 66 ex

FIELD: organic chemistry, herbicides.

SUBSTANCE: invention describes novel 2-amino-4-bicycloamino-1,3,5-triazines of the general formula (I): wherein R1 and R2 mean independently hydrogen atom, amino-group, (C1-C6)-alkyl, (C1-C4)-alkanoyl, phenylalkyl c 1-6 carbon atoms in alkyl moiety and possibly substituted with halogen atom; or R1 and R2 in common with nitrogen atom to which they are bound form morpholino-group; R3 means hydrogen atom, (C1-C6)-alkyl possibly substituted with halogen atom, hydroxy-, amino-, di-(C1-C4-alkyl)amino-, cyano-group, phenyl, (C1-C4)-alkoxy-, carboxy-group or (C3-C9)-cycloalkyl that can be substituted with halogen atom, phenyl possibly substituted with halogen atom, (C1-C6)-alkyl, hydroxy-group or phenyl, amino-, di-(C1-C4-alkyl)amino-, (C1-C6)-alkoxy-, (C1-C6)-alkylthio-group, or (C2-C6)-alkenyl; R4 and R5 mean independently hydrogen atom, (C1-C4)-alkyl or (C1-C4)-alkanoyl; R6 means independently (C1-C6)-alkyl, (C1-C6)-alkoxy-group or halogen atom; Y1 means a direct bond or -CH2-; Y2 means group -CRaRb wherein Ra and Rb mean independently hydrogen atom or (C1-C6)-alkyl; Y3 means a direct bond, Y2-independent group -CRaRb wherein Ra and Rb mean independently hydrogen atom or (C1-C6)-alkyl, or bivalent group of the formula -O-, -S-; m means 1, 2 or 3; n means 0, 1, 2, 3 or 4, or their salts. Novel compounds possess herbicide activity with the effectiveness 60-100%, for example, in rice plantings and wherein damages of cultivate plants do not exceed 10%.

EFFECT: valuable herbicide properties of compounds.

7 cl, 1 tbl, 4 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to N-pyrazinylphenylsulfonamides of the general formula (I) or their pharmaceutically acceptable salts or solvates wherein each R1, R2 and R3 represents independently hydrogen atom, halogen atom, cyano-group, -CF3, -OCF3, -O-(C1-C6)-alkyl or (C1-C6)-alkyl; R4 represents halogen atom, -CO2R12, (C1-C6)-alkoxy-, (C3-C6)-alkenyloxy- or (C3-C6)-alkynyloxy-group, -O-(C1-C6)-alkyl-X-(C1-C6)-alkyl, -O-(C1-C6)-alkyl-R11, -O-(C2-C6)-alkyl-X-R11 or -O-(C1-C6)-alkyl-R16; each R5 and R6 represents independently hydrogen atom, halogen atom, -CO2R12, -CONR14R15, (C1-C6)-alkyl substituted possibly with hydroxy-group, -NR14R15 or 1-3 fluorine atoms; (C1-C6)-alkyl-R11, -XCH(R11)-(C1-C6)-alkyl or -XCH(R16)-(C1-C6)-alkyl, -NR14R15, -N(R11)R11, X-(CH2)qNR14R15, (CH2)nNR14R15, -NHC(O)-(C1-C6)-alkyl substituted possibly with one or more hydroxy-group, (C3-C6)-alkynyl or (C3-C6)-alkenyl possibly branched and, possibly, substituted with 1-3 groups chosen from hydroxy-, cyano-group, halogen atom and =O. Proposed compounds can be used in treatment of chemokine-mediates diseases, for example, inflammatory diseases, such as asthma. Also, invention describes methods for synthesis of compounds of the formula (I), pharmaceutical composition based on thereof, method for preparing pharmaceutical composition and using compounds in producing a medicinal agent.

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

17 cl, 212 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel imidazoline-2-yl-aminophenylamides of the formula (I): wherein R1 means phenyl optionally substituted with one, two or three substitutes chosen independently from group comprising alkyl, alkenyl, alkoxy-group, optionally substituted aryl, optionally substituted aryloxy-, aralkyloxy-group, halogen atom, halogenalkyl, halogenalkoxy-, hydroxy-group, hydroxyalkyl, alkylsulfonyl, alkoxyalkyloxy-, hydroxyalkyloxy-, cyano-, hydroxy-group, cycloalkyl, cycloalkyloxy-, cycloalkylalkoxy-, amino-, alkylamino-, dialkylamino-group, optionally substituted heterocyclyl, optionally substituted heterocyclyloxy-group, optionally substituted heterocyclylsulfonyl, optionally substituted heterocyclylalkyloxy-group, sulfamoyl, alkylsulfamoyl, dialkylsulfamoyl; R2 means hydrogen atom; A means -C(O)-NRa-(CRbRc)n- or -NRa-C(O)-(CRbRc)n-; n = 1-6; each among Ra, Rb and Rc means independently hydrogen atom or alkyl, or their pharmaceutically acceptable salt or solvates, and to compounds of the formula (II): wherein R1, R2, Rb, Rc and A have above given values; each R3 and R4 means independently hydrogen atom or alkoxycarbonyl; Ra means hydrogen atom, alkyl or cycloalkyl. These compounds are effective modulators of IP receptors and firstly antagonists of IP receptors. Except for, invention involves pharmaceutical compositions containing indicated compounds.

EFFECT: valuable biological and medicinal properties of compounds and pharmaceutical composition.

11 cl, 1 tbl, 10 ex

FIELD: organic chemistry, medicine.

SUBSTANCE: invention describes derivatives of aminotetraline of the formula (I) wherein R1 means (C1-C6)-alkyl; R2 means halogen atom or -OR'; R3 means hydrogen atom (H) or -OR' wherein R' means (C1-C6)-alkyl or -SO2R'' wherein R'' means phenyl, thienyl, isoxazolyl; R4 means (C1-C6)-alkyl, phenyl, piperidinyl, pyrrolidinyl, morpholinyl, piperazinyl, diazepinyl, furanyl, isoxazolyl, imidazolyl and pyrazolyl that can be substituted optionally, and pharmaceutical compositions containing derivatives of aminotetraline. Proposed compounds are selective antagonists of M2/M3 muscarinic receptors and designated for treatment and prophylaxis of diseases associated with smooth muscle disorder.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

23 cl, 1 tbl, 16 ex

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to novel derivatives of nicotinamide of the general formula (I): wherein R1 is chosen from hydrogen atom, unsubstituted or substituted (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C7)-cycloalkyl, phenyl or heteroaryl; R2 is chosen from hydrogen atom, (C1-C6)-alkyl and group -(CH2)q-(C3-C7)-cycloalkyl, or -(CH2)mR1 and R2 in common with nitrogen atom to which they are bound form (four-six)-membered heterocyclic ring; R3 represents chlorine atom or methyl group; R4 represents group -NH-CO-R7 or -CO-NH-(CH2)q-R8; R7 is chosen from hydrogen atom, (C1-C6)-alkyl, group -(CH2)q-(C3-C7)-cycloalkyl and others; R8 is chosen from hydrogen atom, (C1-C6)-alkyl, (C3-C7)-cycloalkyl and others; each X and Y is chosen independently from hydrogen atom, methyl group and halogen atom; Z represents halogen atom; m is chosen from 0,1, 2, 3 and 4; n and q are chosen from 0, 1 and 2, and to pharmaceutically acceptable salts or their solvates. Indicated compounds possess inhibitory activity with respect to p38 kinase and can be used in medicine.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

15 cl, 127 ex

FIELD: organic chemistry, agriculture.

SUBSTANCE: invention relates to 5-substituted alkylaminopyrazole derivatives of formula I , wherein R1 is CN; W is C-halogen; R1 is halogen; R3 is C1-C3-haloalkyl, C1-C3-haloalkoxy; R4 is hydrogen, C1-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, COR8; A is C1-C12-alkylene; R5 is hydrogen, C3-C6-alkenyl, -(CH )qR7 or NR10R11; R5 is C1-C6-haloalkyl; as well as method for animal exogenous and endogenous pest controlling; pesticide composition and application of said compounds for production of veterinary drug. 5-Substituted alkylaminopyrazole derivatives are useful in pest controlling, including insects, arachnids and helminthes, such as nematodes.

EFFECT: new pesticide derivatives.

9 cl, 12 tbl, 20 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel anthranilic acid amides with a by-side heteroarylsulfonyl chain. Invention describes compounds of the formula (I): wherein R1 means compounds of formulae: or wherein A means -CnH2n- wherein n = 0, 1, 2, 3, 4 or 5; D means a bond or -O-; E means -CmH2m- wherein m = 0, 1, 2, 3, 4 or 5; R8 means hydrogen atom, alkyl with 1, 2, 3 or 4 carbon atoms or -CpH2p-R14 wherein p = 1, 2, 3, 4 or 5; R14 means phenyl or heteroaryl wherein phenyl and heteroaryl are unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting fluorine (F), chlorine (Cl), bromine (Br) and iodine (J) atom, alkyl with 1, 2, 3 or 4 carbon atoms; R9 means hydrogen atom or alkyl with 1, 2, 3, 4, 5 or 6 carbon atoms; R10 means hydrogen atom, alkyl with 1, 2, 3 or 4 carbon toms, phenyl, naphthyl or heteroaryl wherein phenyl, naphthyl and heteroaryl are unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting of F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms; R11 means cycloalkyl with 3, 4, 5 or 6 carbon atoms, phenyl, furyl, pyridyl, pyrazinyl wherein phenyl, furyl, pyridyl, pyrazinyl are unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting of F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms, alkoxy-group with 1, 2, 3 or 4 carbon atoms; R12 means alkyl with 1, 2, 3 or 4 carbon atoms, alkynyl with 1, 2, 3 or 4 carbon atoms, cycloalkyl with 3, 4, 5 or 6 carbon atoms, phenyl or heteroaryl; R13 means -CpH2p-R14 wherein p = 0, 1, 2, 3, 4 or 5; R15 means cycloalkyl with 3, 4, 5, 6, 7 or 8 carbon atoms; R2 means hydrogen atom; R3 means heteroaryl wherein heteroaryl is unsubstituted or substituted with 1, 2 or 3 substitutes chosen from group consisting of F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms; R4, R5, R6 and R7 mean independently of one another hydrogen atom, F, Cl, Br, J, alkyl with 1, 2, 3 or 4 carbon atoms, alkoxy-group with 1, 2, 3 or 4 carbon atoms, and their pharmaceutically acceptable salts also. Also, invention describes pharmaceutical composition containing compounds of the formula (I) possessing the effect blocking Kv1.5-channel. Proposed compounds can be used in treatment and prophylaxis of diseases mediated by K+-channel.

EFFECT: valuable medicinal property of compounds and pharmaceutical composition.

20 cl, 4 tbl, 70 ex

FIELD: organic chemistry, biochemistry, pharmacy.

SUBSTANCE: invention relates to new heterocyclylsulfonyl alkylcarboxylic acids and their derivatives of the general formula (1): or their pharmaceutically acceptable salts, N-oxides or hydrates possessing the inhibitory effect on kinase activity and to the focused library for search of active leader-compounds comprising at least abovementioned compound. In the general formula 91) W represents optionally substituted heterocyclic radical, among them: pyrrole-3-yl, thiophene-2-yl, isooxazole-4-yl, pyrazole-4-yl, imidazole-4-yl, pyridine-3-yl, 1H-2,4-dioxopyrimidine-5-yl, 2,3-dihydro-1H-indole-5-yl, 2,3-dihydro-1H-indole-7-yl, 1,3-dihydro-2-oxoindole-5-yl, 2,3-dioxo-1H-indole-5-yl, 2-oxo-3H-benzoxazole-6-yl, benzothiazole-6-yl, 1H-benzimidazole-5-yl, benzo[1,2,5]oxadiazole-4-yl, benzo[1,2,5]thiadiazole-4-yl, 1,2,3,4-tetrahydroquinoline-6-yl, 3,4-dihydro-2-oxo-1H-quinoline-6-yl, quinoline-8-yl, 1,4-dihydro-2,3-dioxoquinoxaline-6-yl, 3-oxo-4H-benzo[1,4]oxazine-7-yl, 3-oxo-4H-benzo[1,4]thiazine-7-yl, 2,4-dioxo-1H-quinazoline-6-yl, 2,4-dioxo-1,5-dihydrobenzo[b][1,4]diazepine-7-yl or 2,5-dioxo-3,4-dihydrobenzo[b][1,4]diazepine-7-yl; Y represents optionally substituted methylene group; R1 represents chlorine atom, optionally substituted hydroxyl group, optionally substituted amino-group, optionally substituted azaheterocyclyl; n = 1, 2 or 3; or Yn represents carbon atom of optionally substituted (C3-C7)-cycloalkyl or optionally substituted (C4-C7)-heterocyclyl. Also, invention relates to a pharmaceutical composition in form of tablets, capsules or injections placed into pharmaceutically acceptable package.

EFFECT: valuable properties of compounds.

5 cl, 3 sch, 5 tbl, 6 ex

The invention relates to N-substituted aminotetralin formula 1

< / BR>
where R1independently selected from the group consisting of hydrogen; hydroxy; halogen; C1-8-alkoxy; substituted C1-8-alkoxy, where the Deputy is a halogen; n is 0-2; Y is methylene; m is 0-3;1means hydrogen;2means hydrogen; R2selected from the group consisting of hydrogen; hydroxy; C1-6-alkyl, C1-6-alkenyl; phenyl; substituted phenyl where the Deputy is chosen from halogen, C1-6-alkyl, C1-6-alkoxy, trifter-C1-6-alkyl, nitro; naphthyl and pyridyl; L is chosen from the group consisting of C1-8-alkylene; C1-4-alkylen-C3-7-cycloalkyl-C1-4-alkylene; C1-4-alkylen-aryl-C1-4-alkylene; R3selected from phenyl; substituted phenyl where the Deputy is chosen from halogen, nitro, C1-8-alkoxy, trifloromethyl and amino-C1-8-alkyl; naphthyl; and tanila and their enantiomers, diastereoisomers and pharmaceutically acceptable salts

The invention relates to new derivatives of nitromethylene General formula 1 in which R represents the radical (I), (II) or (III)

The invention relates to a new group of antibiotics, the carbapenems and their non-toxic pharmaceutically acceptable salts, having antimicrobial activity, which can be used both separately and in combination with other antibiotics to treat bacterial infections in humans and animals

The invention relates to new heterocycles compounds, more particularly to a new heterocycles compounds which are inhibitors of the enzyme 5-lipoxygenase (5-LO)
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