Method for obtaining of 1-r-indole-3-ylsulfanylacetates of (2-hydroxyethyl)ammonium

FIELD: pharmacology.

SUBSTANCE: invention relates to a method for the preparation of indole-1-H-, 1-methyl-, 1-benzylindole-3-ylsulfanylacetate of (2-hydroxyethyl)ammonium heterocyclic compounds that have a broad spectrum of action, for example, selective erythropoiesis and immunomodulators with a minimum potential for undesirable effects on various body systems, and can be used to prevent and treat immune-dependent lesions that occur with anaemia, cancer and inflammatory diseases, complications with organs and bone marrow transplantation, protection against cardiogenic shock, stresses, etc. The method consists in the reaction of 1-R-indole-3-ylsulfanyl acetic acids with (2-hydroxyethyl)amines - triethanolamine, methyldiethanolamine, dimethylethanolamine without solvent upon heating to 60-65°C for 0.5-1 hour, with washing of the resulting salt with ether. The yield is 92-99%. The initial 1-R-indole-3-ylsulfanyl acetic acids (compounds 2) are obtained for this reaction from 1-H- or 1-methyl-or 1-benzylindole with thiourea, bromine, potassium bromide, taken in the molar ratios of 1:2:1:1, respectively, in a water medium at a temperature of 30-40°C for 3 h in inert gas, with subsequent processing of the reaction mass by an aqueous solution of sodium hydroxide, then an aqueous solution of monochloroacetic acid taken in the molar ratios of indole, sodium hydroxide, acid 1:(4-5):(1-1.2), heating of the reaction mixture at 90-100°C for 3 h at a pH of 9-10 with subsequent acidification with hydrochloric acid until pH=1 with a yield of 92-95%. Purity is 98.7-99.7. Replacement of scarce and expensive iodine and potassium iodide in alcohol solution with a more accessible aqueous solution of bromine and sodium bromide, excluding toxic hydrazine hydrate and toxic solvent (alcohol) from the process leads to a decrease in product cost and an increase in environmental fire safety, since the reaction is carried out in an aquatic environment. , R=H, CH3, CH2C6H5; R1, R2=H, CH3, CH2CH2OH; n=1-3.

EFFECT: increased efficiency of compounds application.

2 cl, 2 dwg, 8 ex

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds of formula (X) and their salts and to their application as intermediate compounds in method of obtaining pharmaceutically active compound of formula (I), where X represents =O or =N-OH; Y represents hydrogen or para-chlorophenylsulphanyl; Z represents hydrogen or -CH2COOR1, where R1 is selected from hydrogen and alkyl.

EFFECT: obtaining novel compounds.

9 cl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to (hetero)arylcyclohexane derivatives of formula , where values of Y1, Y1', Y2, Y2', Y3, Y3', Y4, Y4', R1-R3 are given in the first claim, having affinity for the µ- opioid receptor and ORL 1-receptor.

EFFECT: enabling use of the derivatives in drugs for treating pain.

10 cl, 2 tbl, 40 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to 7-substituted indoles of formula I:

or their pharmaceutically acceptable salts wherein the values A1, B1, C1, D1, E1, F1, G1, L are presented in cl. 1 of the patent claim.

EFFECT: compounds inhibit activity of anti-apoptotic protein Mc1-1 that enables using them in pharmaceutical compositions.

5 cl, 7 dwg, 2 tbl, 609 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or pharmaceutically acceptable salts thereof: where: each of R1, R2, R3, R4 is independently selected from a group consisting of a hydrogen atom, a halogen atom, an aryl, a C5-6 heteroaryl having 1-3 heteroatoms in the ring which are selected from O, S and N, -OR5, -NR5R6, and -NR5COR6, where said aryl or C5-6 heteroaryl, having 1-3 heteroatoms in the ring selected from O, S and N, is unsubstituted or additionally substituted with one or more groups selected from a group consisting of alkyl, alkoxyl and halogen, each of R5 and R6 is independently selected from a group consisting of a hydrogen atom or an alkyl, where said alkyl is unsubstituted or additionally substituted with one or more groups selected from a group consisting of an aryl, haloaryl, hydroxyl and alkoxyl. The invention also relates to a pharmaceutical composition which inhibits protein kinase and contains a compound of formula I, a method of producing the compound of formula I, use of said compounds to produce a medicinal agent for treating disorders associated with protein kinase, and a method of modulating catalytic activity of protein kinase.

EFFECT: improved method.

10 cl, 24 ex

FIELD: chemistry.

SUBSTANCE: invention relates to use of at least one compound of formula (I): (I), which is capable of being in form of salts of physiologically acceptable acids such as hydrochlorides, where: the values of R, R1, R2, R3, R4, R5, R6, R7 and B are given in claim 1, for producing a medicinal agent possessing either antibacterial activity or efflux pump inhibiting activity. Methods of producing certain compounds are described.

EFFECT: high activity of derivatives.

24 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel substituted pyrimidine derivatives, possessing properties of inhibiting activity of receptor of kinase insertion domain (KDR), or their pharmaceutically acceptable salts. In formula (1): each of X and Y independently represent O, NR, where R represents H; Z represents CR', where R' represents H or halogen; V, U and T together represent or each of R1, R2, R3, R4 and R6 independently represent H, halogen, cyano, C1-10alkyl; R5 values are given in the invention formula; R7 represents C1-10alkyl.

EFFECT: invention also relates to method of treating angiogenesis-associated disorder such as cancer or age-related macular degeneration.

16 cl, 318 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described novel acylsulfonamide peri-substituted condensed bicyclic compounds of general formula (I), values of radicals are given in invention formula. Also described is pharmaceutical composition based on formula (I) compound.

EFFECT: compounds can be used for inhibition of prostaglandin E2 binding with receptor EP3.

30 cl, 371 ex, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: there is described a compound of formula I: or its pharmaceutically acceptable salt, where R2 represents (CR3R4)n-NR5R6 and m, p, q, Ar, R1, R3, R4, R5 and R6 are those as specified in the patent claim and defined as selective 5-NT6 and/or 5-NT2A antagonists. There is also described a pharmaceutical composition containing this compound, and application thereof in preparing drugs for treating diseased conditions of central nervous system chosen from psychoses, schizophrenia, manic depressions, neural disorders, memory impairment, attention deficient syndrome, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, malnutrition and Huntington's disease.

EFFECT: preparation of the compounds which can find application in treatment of a diseased condition of central nervous system.

27 cl, 1 tbl, 29 ex

FIELD: medicine.

SUBSTANCE: invention is related to new compounds of common formula IC1: , where A represents cyano; B represents hydrogen; R1, R2, R3 and R4 independently represent hydrogen; alkyl; halogen or nitro; R5 and R6 independently represent hydrogen; alkyl; cycloalkyl; cycloalkylalkyl; heteroaryl; heteroarylalkyl; alkenyl; carboxyalkyl; cyanoalkyl; diphenylalkyl; aryl, arylalkoxyaryl, arylalkyl, arylalkylaryl, arylcarbonylaryl or aryloxyaryl, or R5 and R6, together with atom of nitrogen, to which they are connected, create heterocyclic ring system; or to salts of such compound; at the same time "heteroaryl" used separately or in combination, is related to mono-, bi- or tricyclic aromatic ring system, which contains up to 14 atoms included in ring, in which at least one ring contains at least one heteroatom, independently chosen from nitrogen, oxygen or sulfur, besides specified heteroaryl group may be unsubstituted or substituted with one to three substituents, independently selected from alkyl and alkoxy; "diphenylalkyl" is related to alkyl group, where each of two atoms of hydrogen is substituted with unsubstituted phenyl group; "aryl" is related to carbocyclic group, selected from group, which consists of phenyl, biphenyl, 1,2,3,4-tetrahydronaphthyl, naphthyl, antryl, phenantryl, fluorenyl, indanyl, 2,3-dihydrobenzo[1,4]dioxynyl and benzo[1,3]dioxolyl group, besides specified aryl group may be unnecessarily substituted with functional groups in number from one to three, which are separately and independently selected from alkoxy, alkoxycarbonyl, alkyl, alkylcarbonyl, cyano, halogen, halogenlkoxy, halogenalkyl and nitro groups, where in certain specific cases, if aryl group represents condensed system from several rings, in which not all the rings are aromatic, one of carbon atoms of which is not included into aromatic ring may be in oxidised condition, and according fragment of ring -CH2- will be substituted by fragment-C(O); "arylalkoxy", used separately or in combination, is related to aryl group, which is connected to initial molecular fragment via alkoxygroup, where aryl group is unsubstituted; "arylalkyl", used separately or in combination, is related to aryl group, which is connected to initial molecular fragment via alkyl group, where aryl group may be unsubstituted or substituted with 1-3 substituents, independently selected from group, which consists of halogen; "aryloxy", used separately or in combination, is related to aryl group, which is connected to initial molecular fragment via oxygen bridge, where aryl group may be unsubstituted or substituted with 1-3 substituents, independently selected from group, which consists of halogen; "arylcarbonyl", used separately or in combination, is related to aryl group, which is connected to initial molecular fragment via carbonyl group, where aryl group is unsubstituted; "heterocyclic ring system", used separately or in combination, is related to monocyclic, bicyclic or polycyclic ring system, which contains up to 15 atoms included into ring, at least one of which represents heteroatom, independently selected from nitrogen, oxygen or sulfur, besides specified ring system may be saturated, partially unsaturated, unsaturated or aromatic, where specified heterocyclic fragment may be unnecessarily substituted with one or more substituents, every of which separately and independently is selected from group made of halogen and halogenalkyl, excluding the following compounds: {3-[(E)-2-cyano-2-(4-fluorophenylcarbamoyl)vinyl]indole-1-yl}acetic acid; [3-((E)-2-cyano-2-m-tolylcarbamoylvinyl)indole-1-yl]acetic acid; (3-[(E)-2-(3-bromophenylcarbamoyl)-2-cyanovinyl]indole-1-yl}acetic acid; [3-((E)-2-cyano-2-phenylcarbamoylvinyl)indole-1-yl]acetic acid; [3-((E)-2-benzylcarbamoyl-2-cyanovinyl)indole-1-yl]acetic acid; [3-((E)-2-cyano-2-o-tolylcarbamoylvinyl)indole-1-yl]acetic acid; [3-((E)-2-cyano-2-t-tolylcarbamoylvinyl)indole-1-yl]acetic acid; (3-[(E)-2-(4-bromophenylcarbamoyl)-2-cyanovinyl]indole-1-yl}acetic acid; {3-[(E)-2-cyano-2-(4-ethylphenylcarbamoyl)vinyl]indole-1-yl}acetic acid; {3-[(E)-2-cyano-2-(4-methoxyphenylcarbamoyl)vinyl]indole-1-yl}acetic acid; {3-[(E)-2~cyano-2-(4- ethoxyphenylcarbamoyl)vinyl]indole-1-yl}acetic acid; [3-((E)-2-cyano-2-isopropylcarbamoylvinyl)indole-1-yl]acetic acid; {3-[(E)-2-cyano-2-(3-etoxyphenylcarbamoyl)vinyl]indole-1-yl}acetic acid; {3-[(E)-2-cyano-3-[[2-(1H-indole-3-yl)ethyl]amino]-3-oxo-1-propenyl]indole-1-yl}acetic acid; {3-[(E)-2-cyano-2-(4-chlorophenylcarbamoyl)vinyl]indole-1-yl}acetic acid; {3-[(E)-2-cyano-3-(4-methyl-piperidine-1-yl)-3-oxopropenyl]indole-1-yl}acetic acid; {3-[(E)-2-(3-chloro-4-methylphenylcarbamoyl)-2-cyanovinyl]indole-1-yl}acetic acid; {3-[(E)-2-cyano-2-(3-phenylpropylcarbamoyl)vinyl]indole-1-yl}acetic acid; {3-[(E)-2-cyano-2-(2,3-dichlorophenylcarbamoyl)vinyl]indole-1-yl}acetic acid; {3-[(E)-2-(5-chloro-2-methylphenylcarbamoyl)-2-cyanovinyl]indole-1-yl}acetic acid; {3-[(E)-2-cyano-2-(4-methoxybenzylcarbamoyl)vinyl]indole-1-yl}acetic acid; {3-[(E)-2-cyano-2-(2-fluorophenylcarbamoyl)vinyl]indole-1-yl}acetic acid; and {3-[(E)-2-cyano-3-oxo-3-(4-phenyl-piperazine-1-yl)propenyl]indole-1-yl}acetic acid. Invention is also related to pharmaceutical composition, and also to application of compounds of clause 1.

EFFECT: production of biologically active compounds, which have activity of antagonist coupled with G-protein of chemoattractant receptor of molecules homologue released by Th2-cells.

11 cl, 156 ex, 8 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to formula (I) compounds and to their use in treating diseases related to lipid storage disorders, such as atherosclerosis and diabetes. In R1 represents hydrogen, alkyl, halogen, formyl, hydroxyalkyl or trifluoromethyl, R2 represents hydrogen, alkyl or halogen, R3 represents hydrogen or alkyl, R4 represents hydrogen, alkyl, hydroxy or alkoxy, R5 and R6 are chosen from hydrogen, alkyl, phenylalkyl, hydroxyalkyl, alkoxycarbonyl and phenyl, A represents aryl or heterocyclyl, m equals 0-3, n equals 0-1, p equals 0-3, sum of m, n and p equals 1-4, the bond between carbon atoms Ca and Cb is a single or double carbon-carbon bond.

EFFECT: obtaining new biologically active compounds.

27 cl, 147 ex

Substituted indoles // 2255087

FIELD: organic chemistry, biochemistry.

SUBSTANCE: invention relates to new substituted indoles of the formula (I): and/or stereoisometic form of compound of the formula (I) and/or physiologically acceptable salt of compound of the formula (I) wherein R3 means residue of the formula (II): wherein D means -C(O)-; R7 means hydrogen atom (H) or -(C1-C4)-alkyl; R8 means (a) typical residue of amino acid among the group: phenylalanine or homophenylalanine wherein phenyl residue is unsubstituted or substituted with halogen atom; or (b) -(C1-C4)-alkyl wherein alkyl is a linear or branched and (b) 1) mono- or multi-substituted independently of one another with pyrrole residue wherein this residue is unsubstituted or substituted with halogen atom; (b) 2) mono- or bi-substituted independently with residue -S(O)x-R10 wherein x = 0, 1 or 2, or (b) 3) mono- or bi-substituted independently of one another -N(R10)2 wherein R10 means (a) hydrogen atom (H); (b) means -(C1-C6)-alkyl wherein alkyl is unsubstituted or substituted with halogen atom from 1 to 3 times; (c) phenyl wherein phenyl is substituted or substituted with halogen atom from 1 to 3 times; in the case (R10)2 residues R10 have values independently of one another (a), (b), (c); Z means (a) residue of heterocycles group comprising benzothiadizine, pyrrole, pyridine, pyrimidine, pyrazine, imidazole, pyrazole, oxazole, isoxazole, thiazole, isothiazole, tetrazole, oxadiazolone, triazole being heterocycles are unsubstituted or substituted with -NH2=, =O, alkoxycarbonyl or aminocarbonyl from 1 to 3 times, or (b) means -C(O)-R11 wherein R11 means 1. -O-R10 or 2. -N(R10)2; R9 means (a) hydrogen atom (H); (b) means (C1-C6)-alkyl wherein alkyl is unbranched or branched and substituted with phenyl or =O independently of one another from 1 to 3 times; (c) phenyl wherein phenyl is unsubstituted or substituted with halogen atom; R1, R2 and R4 mean hydrogen atom (H); R5 means hydrogen atom (H); R6 means (a) phenyl wherein phenyl is unsubstituted or substituted with -NH2; (b) pyridine, or (c) pyrimidine being pyridine or pyrimidine is unsubstituted or substituted with groups -NH2, -NH-CH3. Compounds of the formula (I) are specific inhibitors of IkB kinase.

EFFECT: valuable biochemical properties of compounds.

3 cl, 3 tbl, 29 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

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new substituted indole compounds of Mannich bases of the formula (I):

wherein R1 means hydrogen atom (H), (C1-C10)-alkyl, unsubstituted phenyl or naphthyl bound through (C1-C2)-alkylene group or that monosubstituted at least with hydroxy group (-OH), halogen atom, -CF3, -CN, (C1-C6)-alkyl, (C1-C6)-alkoxy group; R2 means atoms H, F, Cl, Br, groups -CF3, -CN, -OR10, -CO(OR11), -CH2CO(OR12), -COR19, (C1-C10)-alkyl, unsubstituted phenyl or naphthyl, or that monosubstituted at least with -OH, halogen atom, -CF3, -CN, (C1-C6)-alkyl and (C1-C6)-alkoxy group; R3 means -CH(R13)N(R14)(R15); R4, R5, R6 and R7 can have similar or different values and mean atoms H, F, Cl, Br and groups -CF3, -CN, -NO2, -OR10 and others; R10 means H, -COR17, (C1-C6)-alkyl and others; R13 means unsubstituted phenyl or phenyl monosubstituted with at least (C1-C4)-alkyl, halogen atom, -CF3, -CN and -OH; R14 and R15 can have similar or different values and mean unbranched or branched (C1-C6)-alkyl, or R14 and R15 represent in common (CH2)n wherein n means a whole number from 3 to 6, or (CH2)O(CH2)2; R17 means (C1-C6)-alkyl; R19 means -NHR20, (C1-C6)-alkyl and others; R20 means H, (C1-C6)-alkyl and others, and/or their racemates, enantiomers, diastereomers and/or corresponding bases, and/or corresponding salts of physiologically acceptable acids with exception of racemates of some compounds given in claim 1. Also, invention describes method for their preparing and using as a medicinal agent possessing analgesic effect.

EFFECT: valuable medicinal properties of compounds.

42 cl, 2 dwg, 3 tbl, 103 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel substituted indoles or its pharmaceutically acceptable salts of the formula (I): , wherein R1 means hydrogen (H) atom, halogen atom, -CN, nitro-group, -SO2R4, -OH, -OR4, -SO2NR5R6, -CONR5R6, -COOH, -COOCH3, -NR5R6, phenyl, naphthyl or (C1-C6)-alkyl wherein the latter group is possibly substituted with one or more substitutes chosen independently from halogen atom, -OR8 and -NR5R6 wherein x = 2; R2 means (C1-C7)-alkyl; R3 means phenyl, naphthyl or heteroaryl and each of them is possibly substituted with one or more substitutes chosen independently from H, halogen atom, -CN, -OH, -SO2R4, -OR4, -SO2NR5R6, -CONR5R6, phenyl, naphthyl, (C1-C6)-alkyl wherein the latter group is possibly substituted with one or more substitutes chosen independently from halogen atoms, -OR8 and -NR5R6, -S(O)xR7 wherein x = 2; R4 means (C1-C6)-alkyl; R5 and R6 mean independently H, (C1-C6)-alkyl, or R5 and R6 in common with nitrogen atom to which they are bound can form 6-membered saturated heterocyclic ring comprising one atom chosen from -NR16; R7 means (C1-C6)-alkyl; R8 means H, (C1-C6)-alkyl; R16 means H, -COY-(C1-C4)-alkyl wherein Y means oxygen atom (O) and wherein alkyl group in the substitute group can be direct, branched or cyclic, and wherein heteroaryl means 5-6-membered heteroaromatic ring comprising from 1 to 3 heteroatoms chosen from nitrogen (N), oxygen (O) and sulfur (S) atoms, or means 6,6-condensed bicyclic aromatic ring system comprising one nitrogen atom. Compounds of the formula (I) can be used in production of a medicinal agent used in treatment of asthma and chronic obstructive disease.

EFFECT: valuable medicinal properties of compounds.

7 cl, 2 tbl, 59 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for synthesis of a novel (3-cyano-1H-indole-7-yl)-[4-(4-fluorophenethyl)-piperazine-1-yl]methanone of the formula (I): or its physiologically acceptable salts. Method involves (1) the formylation reaction of indole ester of the formula (II): wherein R means (C1-C6)-alkyl, and (2) ester formyl of the formula (III): wherein R mean as given above and synthesized at stage (1) is interacted with hydroxylamine to yield an oxime derivative of the formula (IV): wherein R means as given above; (3) oxime of the formula (IV) is converted to cyanoindole ester of the formula (V): wherein R is given above; (4) ester of the formula (V) is saponified to yield 3-cyano-1H-indole-7-carboxylic acid; (5) 3-cyano-1H-indole-7-carboxylic acid is interacted with 1-[2-(4-fluorophenyl)ethyl]-piperazine or its salts to yield compound of the formula (I), and (6) synthesized base of the formula (I) is converted to one of its physiologically acceptable salts by treatment with acid.

EFFECT: improved method of synthesis.

11 cl

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for synthesis of hydroxyindolylglyoxylamides of the formula (1) wherein R means linear or branched (C1-C6)-alkyl that can be if necessary substituted once with monocyclic saturated or polyunsaturated carbocycle comprising 3-14 members in cycle wherein carbocyclic substitute, in turn, can be substituted once or more times with the following groups: -OH, -NO2, -F, -Cl, -Br, -J, -O-(C1-C6)-alkyl; R2 and R3 mean hydrogen atom or -OH and it is necessary that one of two substitutes has to mean -OH; R4 means monocyclic aromatic carbocycle comprising 6-14 members in cycle or pyridyl and if necessary substituted once or more times with the following groups: -F, -Cl, -Br, -J, -O-(C1-C6)-alkyl or -(C1-C6)-alkyl wherein each (C1-C6)- alkyl radical can be substituted once or more times with the following groups: -F, -Cl, -Br, -J. Proposed method involves the following steps: (a) interaction of the parent compound of the formula (1a) wherein R2 and R3 mean hydrogen atom or benzyl-protected -OH and it is necessary that at least one of two substitutes has to mean benzyl-protected -OH with compound of the formula: R1-X wherein R1 means above given values, and X means halogen atom resulting to formation of compound of the formula (1b) ; (b) interaction of compound of the formula (1b) with compound of the formula: (COX)2 wherein X means halogen atom resulting to formation of compound of the formula (1c) ; (c) interaction of compound of the formula (1c) with compound of the formula: H2NR wherein R has values as given for R4 and resulting to formation of compound of the formula (1d) , and (d) interaction of compound of the formula (1d) involving splitting off benzyl from R2 and/or R3 and resulting to formation of the end compound of the formula (1). Also, invention relates to intermediate compounds of formulae (1c) and (1d) and using compounds of formulae (b), (1c) and (1d) for synthesis of the end compounds of the formula (1). Proposed invention provides synthesis of the end compounds of the formula (1) with the high yield and in high pure form.

EFFECT: improved method of synthesis.

25 cl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention pertains to new 2,4-substituted indole with formula: I, its pharmaceutically accepted salt, where R1 represents phenyl, optionally substituted with one or two substitutes, chosen from a group, consisting of a halogen, C1-12alkyl, halogen C1-12alkyl, or represents thienyl; R2 represents residue of a saturated ring, consisting of six ring atoms, one or two of which are nitrogen atoms, and the others are carbon atoms, optionally substituted with one or two C1-12alkyls; R represents H, C1-12alkyl; R4 represents H; p represents 1 or 2; n represents 0,1 or 2. The compounds have antagonistic activity to the "5-ГТ6" receptor, which allows to use in pharmaceutical mixtures.

EFFECT: use in pharmaceutical mixtures.

10 cl, 7 dwg, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention pertains to new 2,7-substituted indoles of formula: its pharmaceutical salts, where n represents 0, 1 or 2; p represents 1 or 2; R1 represents phenyl, optionally substituted with one or two substitutes, chosen from a group, including halogen, C1-C12alkyl, halogenC1-C12alkyl; R2 represents a mono-valent saturated residue, consisting of one ring, containing six ring atoms, one or two of which are nitrogen atoms, and the others are carbon atoms, optionally substituted with one or two C1-C12alkyls; R3 represents H, C1-C12alkyl. The compounds have antagonist action to the "5-ГТ6" receptor.

EFFECT: possibility of using these compounds in pharmaceutical compositions in an effective quantity.

8 cl, 2 tbl, 8 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the novel indole derivatives with the common formula I: or its pharmaceutically acceptable salt, where R1 is (a) -X-aryl-Y-Z and (b) -X-heteroaryl-Y-Z, where aryl and heteroaryl are unsubstituted or substituted with 1-3 groups, chosen independently from A; aryl means phenyl or naphthyl; heteroaryl means the monocyclic or condensed bicyclic aromatic ring structure containing one heteroatom chosen independently from N or O, where the monocyclic ring or each ring of the bicyclic ring structure means the penta- or hexamerous ring; X means the bond CH2, CH(CH3) and C(CH3)2; Y means -CH=CH-, -CH(OH)CH(OH)-, -OCR7R8-, -SCR7R8- and -CH2CR5R6-; Z means -CO2H, tetrazole; A means C1-4alkyl, -OC1-4alkyl and halogen, where alkyl, and -Oalkyl, each not necessarily substituted with 1-5 halogens; R5, R6, R7 and R8 , each independently means H, C1-C5alkyl, -OC1-C5alkyl, C3-6cycloalkyl and phenyl, where C1-C5alkyl, -OC1-C5alkyl, C3-6cycloalkyl and phenyl are not necessarily substituted with 1-5 halogens; and C3-6cycloalkyl and phenyl are additionally not necessarily substituted with 1-3 groups, independently chosen from C1-C3alkyl and -OC1-C3alkyl, at that, the said C1-C3alkyl and -OC1-C3alkyl are not necessarily substituted with 1-3 halogens; or alternatively, R7 and R8 together can form the C3-C6cycloalkyl group; or alternatively, when R1 means -X-phenyl-Y-Z, Y means -OCR7R8 and R7 are chosen from group containing H, C1-C5alkyl, -OC1-C5alkyl, then R8 can, not necessarily , mean the 1-2-hydrocarbon bridge, bound to the phenylic ring by the orthoposition relative to Y, and generating in this way the 5- or 6-membered heterocyclic ring, condensated with the phenylic ring; R2 means C1-C4alkyl, which is not necessarily substituted with 1-5 halogens; R3 means (a) bensoxazolil, (d) aryl, (e) -C(=O)aryl, (f) -C(=O)heteroaryl, (g) -Oaryl, (i) -S(O)naryl and where R3 is not necessarily substituted with 1-3 substituting groups, independently chosen from halogen, C1-3alkyl, -OC1-3alkyl and -SC1-3alkyl, where C1-3alkyl, -OC1-3alkyl and -SC1-3alkyl are not necessarily substituted with 1-5 halogens; each R4 means from H, halogen, C1-C5alkyl and -OC1-C5alkyl, where C1-C5alkyl and -OC1-C5alkyl are not necessarily substituted with 1-5 halogens; n is the even number 0-2 and p is the even number 1-3.

EFFECT: composition I reveals agonistic activity considering PPAR, that allows to use them in pharmaceutical composition, in means to fix PPAR and production of medication to fix PPAR.

33 cl, 8 tbl, 32 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the novel indole derivatives with the formula , where X means S, SO, SO2; R1 means 6-membered mono-homocyclic saturated or unsaturated ring structure or 5-, 6-membered monohetercyclic saturated or unsaturated ring structure with one or two heteratoms, chosen from N, O, S, and each of the said structures is not necessarily substituted with one or more substituters, chosen from the group, consisting of halogen, CN, (1C-4C)fluoroalkyl, NO2, (1C-4C)alkyl, (1C-4C)alkoxi or (1C-4C)fluoroalkoxi; R2 means 2-nitorphenyl, 2-cyanophenyl, 2-hydroxymethylphenyl, pyridine-2-il, pyridine-2-il-N-oxide, 2-benzamide, methylic ether of the 2-benzoic acid or 2-methoxyphenyl; R3 means H, halogen or (1C-4C)alkyl; R4 means H, OH, (1C-4C) alkoxy or halogen; R5 means H, OH, (1C-4C) alkoxy, NH2 CN, halogen, (1C-4C)fluoroalkyl, NO2, hydroxy(1C-4C)alkyl, CO2H, CO2(1C-6C)alkyl, or R5 means NHR6, where R6 means (1C-6C)acyl, not necessarily substituted with one or more halogens, S(O)2(1C-4C)alkyl or S(O)2heteroaryl, not necessarily substituted with (1C-4C)alkyl or one or more halogens, where heteroaryl is the 5-membered mono-heterocyclic unsaturated ring structure with one S atom or two N atoms, or R5 means C(O)N(R8,R9), where R8 and R9 , each independently, mean H, (3C-6C)cycloalkyl or CH2R10, where R10 means H, (1C-5C)alkyl, hydroxy(1C-3C)alkyl, complex (1C-4C)alkyl ether of the carboxy(1C-4C)alkyl, (1C-3C)alkoxy(1C-3C)alkyl, (mono- or di(1C-4C)alkyl)aminomethyl, (mono- or di1C-4C)alkyl)aminocarbonyl or pyhenyl, where R8 and R9 together with N form 5- or 6-membered saturated aor unsaturated heterocyclic ring, not necessarily containing N or O as the second heteroatom, not necessarily substituted with (1C-4C)alkyl; or its saline or hydrated form.

EFFECT: allows using indoles for producing pharmaceutical agent and in method for inhibiting 5α-dihydrosterone activity.

17 cl, 7 dwg, 5 tbl, 25 ex

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