Forzicyaside sulfate and its derivatives, method for its production and its application

FIELD: pharmacology.

SUBSTANCE: invention relates to forzicyaside sulfate and its derivative represented by the following formula , wherein R is Na+, K+ or NH+, and a method for their preparation, as well as an antiviral drug based on them and its use.

EFFECT: increased efficiency of agents.

10 cl, 9 tbl, 2 dwg

 



 

Same patents:

FIELD: biotechnology.

SUBSTANCE: invention relates to a low-toxic (E)-2-(4-{[3-(2,4-dimethoxyphenyl)acrylamido]methyl}-1H-1,2,3-triazole-1-yl)-2-isopropyl-9-(4-methyl piperazine-1-yl)-3,7-dioxo-3,7-dihydro-2H-furo[3,2-g]chromen of formula (I) , having the analgesic activity in the test "acetic acid-induced writhing". The said property enables to use this compound in medicine.

EFFECT: compound of formula I is prepared from furocoumarin peucedanine contained in the plant Peucedanum morisonii.

1 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new chromone derivatives of general formula

,

wherein: R1 represents one or more identical or different substitutes on a benzene ring, each of which independently represents a hydrogen atom, or a halogen atom, or C1-4 alkoxy group, or OH group. or group -O(CH2)nO-, wherein n=1 or 2, R2 represents a hydrogen atom, or C1-4 alkyl group; A and B independently represent either a nitrogen atom, or a carbon atom; R3 represents a hydrogen atom or one or more identical or different substitutes specified in a group consisting of: a halogen atom, C1-4 alkyl group, C1-4 alkoxy group, group -O(CH2)nO-, wherein n=1 or 2, group NO2, group NHSO2R4, group NHR5, OH group, C1-4 halogenoalkyl group, CN group, or R3 makes a ring condensed with a benzene ring bearing it, specified in a group consisting of indole, benzimidazole, carbostyril, benzoxazolone and benzoxazolone and benzimidazolone, R4 represents C1-4 alkyl group, or C1-4 dialkylamino group, or C1-4 alkoxyalkyl group, or C1-4 dialkylaminoalkyl group, R5 represents a hydrogen atom, or C1-4 alkylcarbonyl group, or C1-4 alkoxycarbonyl group, and to its pharmaceutically acceptable salts, as well as to methods for preparing them, and to based pharmaceutical compositions, and to using them as a therapeutic agent for central nervous system disorders, as long as they possess the D3 dopaminergic ligand properties.

EFFECT: preparing the compositions for treating central nervous system disorders, as long as they possess the D3 dopaminergic ligand properties.

17 cl, 1 dwg, 2 tbl, 33 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to new quinolin-4-one derivatives of formula (1) or to its pharmaceutically acceptable salt, wherein R1 represents: (1) hydrogen, (2) C1-C6 alkyl, (35) carbamoyl-C1-C6 alkyl optionally containing morpholinyl-C1-C6 alkyl, or (36) phosphonoxy-C1-C6 alkyl optionally containing one or two C1-C6 alkyl groups on a phosphonoxy group; R2 represents: (1) hydrogen or (2) C1-C6 alkyl; R3 represents phenyl, thienyl or furyl, wherein a phenyl ring presented by R3, can be substituted by one C1-C6 alkoxy group; R4 and R5 are bound to form a group presented by any of the following formulas: , , , , , , or a group presented by the following formula: a group optionally containing one or more substitutes specified in a group consisting of C1-C6 alkyl groups and oxogroups; R6 represents hydrogen; and R7 represents C1-C6 alkoxy group. The invention also refers to a pharmaceutical composition based on the compound of formula , to a preventive and/or therapeutic agent based on the compound of formula (1), using the compound of formula (1), a method for preparing the compound of formula , as well as to specific compounds.

EFFECT: there are prepared new quinolin-4-one derivatives effective in treating neurodegenerative diseases, diseases caused by neurological dysfunction, or diseases caused by mitochondrial dysfunction.

18 cl, 1 tbl, 257 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to micheliolide derivatives of formula , a based pharmaceutical composition and using them for treating cancer. In formula (I) R1 represents H, -C(O)R4, wherein R4 represents C1-8alkyl; R2=R3 represents a double bond, or R3 represents H, and R2 represents substituted alkyl having from 1 to 8 carbon atoms, wherein a substitute represents -NR7R8; or its pharmaceutically acceptable salts; and wherein R7 and R8 can be identical or different, and represent C1-8alkyl; X represents oxygen; Y represents a single bond.

EFFECT: preparing the pharmaceutical composition for treating cancer.

6 cl, 1 tbl, 8 ex

FIELD: chemistry.

SUBSTANCE: invention provides benzylidene furanone derivatives of (+)-usnic acid of formula 6-13 as anti-tumour agents. The compounds exhibit cytotoxic activity with respect to tumour cell lines CEM-13, U-937, MT-4.

EFFECT: high activity.

2 dwg, 3 tbl, 8 ex

FIELD: medicine.

SUBSTANCE: invention concerns Mycobacterium tuberculosis growth inhibitors representing (+) and (-)-enantiomers of derivatives of usnic acid containing a furilidene furanone fragment, namely (10R,4Z)-8,13-dihydroxy-7,10-dimethyl-4-(2-furanylmethylidene)-5,16-dioxatetracyclo[7.7.0.02.6.010.15]hexadeca-1,6,8,12,14-pentaen-3,11-dione 4a and (10S,4Z)-8,13-dihydroxy-7,10-dimethyl-4-(2-furanylmethylidene)-5,16-dioxatetracyclo[7.7.0.02.6.010.15]hexadeca-1,6,8,12,14-pentaen-3,11-dione 4b

EFFECT: inhibitors possess the high antimicrobial activity.

2 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining pyripyropene derivatives, namely a compound of formula C: , where R represents a linear chain, a branched chain or cyclic C2-6alkylcarbonyl, on condition that, when an alkyl fragment in an alkylcarbonyl group represents a branched chain or a cyclic group, R represents C3-6alkylcarbonyl, including: selective acylation of hydroxyl groups in 1-position and 11-position of a compound B1, represented by formula B1: with an acylating agent in one-three stages in the presence or absence of a base. (i) compound C is obtained by acylation of hydroxyl groups in 1-position and 11-position of the compound B1 in one stage; (ii) method, including obtaining the compound C by acylation in two stages, consisting of stages: acylation of the hydroxyl group in 11-position of the compound B1 with the acylating agent with obtaining the compound B2, represented by formula B2: , where R is determined in formula C; and additional acylation of the hydroxyl group in 1-position of the compound B2; or (iii) method, including obtaining the compound C by acylation in three stages, consisting of stages: acylation of the hydroxyl group in 11-position of the compound B1 with obtaining the compound B2, represented by formula B2: , where R is determined in the formula C; transfer of acyl in 11-position of the compound B2 to hydroxyl in 1-position with obtaining the compound B3, represented by formula B3: , where R is such as determined in the formula C; and acylation of hydroxyl group in 11-position of the compound B3.

EFFECT: increased output.

16 cl, 1 dwg, 3 tbl, 22 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel derivatives of epipodophyllotoxin, substituted in position 4 with possibly substituted chain of (poly)aminoalkylaminoalkylamide, or alkyl-urea, or alkyl-sulphonamide, of formula 1 where R represents hydrogen or C1-4alkyl, A represents CO(CH2)n or CONH(CH2)n, where n equals 2, 3, 4 or 5, R1 represents H or C1-4alkyl, R2 represents (CH2)m-NR3R4, where m equals 2, 3, 4 or 5, R3 represents H or C1-4alkyl, R4 represents H, C1-4alkyl or (CH2)p-NR5R6, where p equals 2, 3, 4 or 5, R5 represents H or C1-4alkyl and R6 represents H, C1-C4alkyl or (CH2)q-NH2, where q equals 2, 3, 4 or 5 or their pharmaceutically acceptable salts, as well as to methods of their obtaining and to their application as anti-cancer medication.

EFFECT: obtaining novel derivatives of epipodophyllotoxin.

11 cl, 19 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing a compound C of formula: [1] where R' is a linear, branched or cyclic C2-6 alkyl carbonyl group. In this method, the protective group for the hydroxy group in position 7 used is R1b; where R1b is a formyl group, optionally substituted with a linear C1-4 alkyl carbonyl group, optionally substituted benzyl group, a -SiR3R4R5 group, where R3, R4 and R5 are independently a linear or branched C1-4 alkyl group or a phenyl group, which can be substituted with a halogen atom, a C1-6alkyloxy-C1-6alkyl group, which can be substituted with a halogen atom, C1-6alkylthio-C1-6alkyl group, which can be substituted with a halogen atom, a linear, branched or cyclic C1-6alkyl group, which can be substituted with a halogen atom (in case of branched or cyclic, denotes a C3-4alkyl group), C2-6alkenyl group, which can be substituted with a halogen atom, C2-6alkynyl group, which can be substituted with a halogen atom, or an optionally substituted saturated or unsaturated 5-member or 6-member heterocyclic group. The invention also includes methods of producing intermediate compounds B2a and B2b and the compound of formula 2Bb itself.

EFFECT: method enables to obtain a pyripyropene derivative with high output, which contains an acyloxy group in position 1 and in position 11 and a hydroxy group in position 7; such a pyripyropene derivative can be used as a pest control agent.

15 cl, 26 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compound with spirochiral carbon base, or its pharmaceutically acceptable salt of general formula 1 , where W represents CO or CHO(C=O)CH3; X represents N3 or OR2; R2 represents hydrogen, linear or branched alkyl C1~C8 or Y represents O; Z represents simple bond or O; R3 represents linear or branched alkyl C1~C8 or alkenyl C2~C8, and M and N represent, each independently, hydrogen, OH or are absent; carbon atom, bound with M or N forms simple bond or double bond with other carbon atoms, and number of double bonds constitutes one or less for each of carbon atoms. Invention relates to method of obtaining and pharmaceutical compositions.

EFFECT: compound with spirochiral carbon base possesses excellent activity of osteoblast differentiation, activity of inhibiting mast cells and activity of inhibiting synthesis of fatty acids in liver that is why compound will play leading role in treatment of steoporosis, fatty liver dystrophy and obesity.

13 cl, 6 ex, 5 tbl, 17 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to benzimidazole-4-carboxamide derivatives of formula , wherein X means an alkenyl group C2-C7 substituted by two methyls, nitro-radical mono-substituted thienyl, unsubstituted quinolinyl, unsubstituted indolyl, unsubstituted pyridazinyl, unsubstituted piperazinyl, C1-C6-alkyl disubstituted piperazinyl, unsubstituted piperidinyl, unsubstituted pyrazinyl, unsubstituted imidazolyl, unsubstituted pyrimidinyl, phenyl monosubstituted pyrimidinyl, pyrimidinyl disubstituted by an amine radical and a radical specified in a group containing -F, -Cl, -Br or -I, hydroxyl trisubstituted phenyl, methoxy-radical trisubstituted phenyl, hydroxyl and methoxy-radical disubstituted phenyl, pyrazolyl disubstituted by a radical specified in a group containing a C1-C6-alkyl, and by a radical specified in a group containing -F, -C1, -Br or -I; Y means aminophenyl monosubstituted by a radical of -F, -O, -Br or -I phenyl, hydroxyethyl disubstituted by hydroxymethyl or C1-C6-alkyl and phenyl monosubstituted by a nitro group, an amino group or a halogen atom; Y also means unsubstituted piperazinyl, unsubstituted pyridyl, unsubstituted pyrazinyl, C1-C6-alkyl monosubstituted thiazol, unsubstituted pyrimidinyl, unsubstituted purinyl. The invention also refers to a pharmaceutical composition based on the compound of formula (I), using the compound of formula (I), a method for producing the compound of formula (I).

EFFECT: there are prepared new benzimidazol-4-carboxamide derivatives possessing antiviral activity.

5 cl, 6 dwg, 4 tbl, 688 ex

FIELD: chemistry.

SUBSTANCE: method includes reacting 2,4-difluoro-5-nitro-1-chlorobenzene (2) with a compound of formula (3) to obtain a compound of formula (4) , reducing the compound of formula (4) with sodium dithionite in a suitable solvent to obtain a compound of formula (5) , ring closure of the compound of formula (5) to form a compound of formula (6) , crystallising a compound of formula (7) from the compound of formula (6), reacting said compound of formula (7) with an amino derivative of a compound of formula (9)

EFFECT: high degree of purity.

10 cl, 4 dwg, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound, represented by the following formula

,

or its pharmaceutically acceptable salt. In claimed formula each symbol has values, determined in formula of invention. Versions of formula [I] compound and particular compounds are also objects of invention. In addition, invention relates to pharmaceutical composition, ITK inhibitor and means for treatment or prevention of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection and other diseases and methods of treating said diseases.

EFFECT: claimed compounds inhibit induced T-cellular kinase (ITK).

32 cl, 86 tbl, 387 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to a novel compound of formula

(I)

or its pharmaceutically acceptable salt, possessing properties of the IKKβ and TNFα inhibitor. The compound can be used with an additional therapeutic agent, selected from vincristine, camptothecin hydrochloride (CPT-11), lefunomid, dexamethasone and TNFα. Preferable are compounds of formula (I), corresponding to 2-{5-chloro-2-[(1R,2R)-2-hydroxycyclopentylamino]pyrimidin-4-yl}-N-cyclopropyl-1H-indole-4-carboxamide and 2-{5-chloro-2-[(1R,2S)-2-hydroxycyclopentylamino]pyrimidin-4-yl}-N-cyclopropyl-1H-indole-4-carboxamide.

EFFECT: compound can be applied in the treatment of inflammatory diseases such as rheumatoid arthritis, chronic obstructive lung disease, bronchial asthma, multiple sclerosis and intestinal inflammatory diseases, or cancer diseases, such as multiple myeloma, colon cancer, pancreas cancer and ovary cancer, by IKKβ inhibition.

30 cl, 4 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I) such as below, or to their pharmaceutically acceptable salts, wherein R1 means H, C1-8alkyl morpholinyl, haloC1-8alkylamino, C1-8alkyloxadiazolyl, hydroxyl, halopyrrolidinyl, azetidinyl, C1-8alkylamino, amino, cyano C1-8alkylamino, halophenylC1-8alkylamino or cyanoC3-8cycloalkylamino; R2, R3, R4, R5 and R6 independently mean H, C1-8alkyl, haloC1-8alkyl, hydroxyC1-8alkyl, C1-8alkoxy, haloC1-8alkyloxy, halogen, hydroxyl, cyanopyrazinyloxy, halogen, hydroxyl, cyanopyrazinyloxy, pyrazolyl, C1-8alkylpyrazolyl, imidazolyl, benzimidazolyl, 6-oxo-6H-piridazinyl, C1-8alkyl-6-oxo-6H-pyridazinyl, piperazinyl, N-C1-8alkylpiperazinyl, piperidinyl, difluoropyrrolidinyl, phenylimidazolyl, oxo-pyrrolidinyl, oxo-oxazolidinyl, morpholinyl, oxo-morpholinyl, oxo-pyridinyl, 2-oxo-2H-pyrazinyl, difluoropiperidinyl, haloC1-8alkylpiperidinyl, piperidinylC1-8alkoxy, oxetanyloxy, C1-8alkylpyrazolyl, halopyridinyl, C1-8alkylpyridinyl, C3-8cycloalkyl, C3-8 cycloalkylC1-8alkyl, halophanyl, C1-8alkylcarbonylamino-C3-8-cycloalkyl-C1-8alkyl, haloC1-8alkylpiperazinyl, C1-8alkylamino, C1-8alkoxy-C1-8alkylpiperazinyl, C3-8cycloalkylpiperazinyl, hexahydropyrrolo[1,2-a]pyrazinyl, 5,6-dihydro-8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl, C1-8alkylimidazolyl, azetidinyl, C3-8cycloalkylpiperazinyl, C1-8alkylimidazolyl, C1-8alkoxy C1-8alkoxy, imidazo[4,5-c]pyridinyl, C1-8alkylpiperazinyl, hexahydro-pyrrolo[1,2-a]pyrazinyl, haloazetidinyl, pyrimidinyl and C2-8alkenyloxy; A1 means -CH2-, carbonyl, -C(O)O- or is absence; A2 means N, CR7; A3 means N, CR8; A4 means N, CR9; R7 means H, C1-8alkyl, haloC1-8alkyl, halogen, hydroxyl, haloC1-8alkylaminocarbonyl; halophenylC1-8alkylaminocarbonyl, phenyl-C3-8-cycloalkylaminocarbonyl, haloC1-8alkylphenylC1-8alkylaminocarbonyl, halophenylC3-8 cycloalkylaminocarbonyl, halophenylC3-8cycloalkylC1-8alkylaminocarbonyl; R8 means H, C1-8alkyl, haloC1-8alkyl, halogen or hydroxyl; or R7 and R8 together with a carbon atom they are attached to, form C3-8cycloalkyl or substituted pyrrolidine, wherein substituted pyrrolidine represents pyrrolidine, N-substituted haloC1-8alkyl or formyl; R9 means H, C1-8alkyl, haloC1-8alkyl, halogen or nitro; or R8 and R9 together with a carbon atom they are attached to, form C3-8cycloalkyl; or its pharmaceutically acceptable salt

EFFECT: compounds inhibit the enzyme catepsin that enables using them in pharmaceutical compositions.

27 cl, 8 dwg, 1 tbl, 88 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a chemical compound of formula wherein R=benzyl and to an antituberculous therapeutic agent representing a composition of imidazo[1,2-b][1,2,4,5]tetrazine derivative of formula I, wherein R=benzyl, isopropyl or phenyl and the known antituberculous preparation pyrazinamide with the ingredients in mole ratio 1:1.

EFFECT: there are prepared new antituberculous therapeutic agents.

2 cl, 2 tbl, 6 ex

Antiviral compounds // 2541571

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula I, such as below, or its pharmaceutically acceptable salts. What is described is a method for preparing them.

,

wherein: A independently from B means phenyl,

, or ,

and B independently from A means phenyl,

, or ,

and the values Z, Y, D, L1, L2, L3, Z1, Z2 are presented in the patent claim.

EFFECT: compounds are effective for hepatitis C virus (HCV) replication inhibition.

17 cl, 3 tbl, 8 dwg, 177 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula , wherein A represents CRaRb or -CH2-CH2-; R1 represents hydrogen or alkyl; R2 represents hydrogen or alkyl; R3 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl, substituted aryl, 1H-pyrazolyl or substituted 1H-pyrazolyl, wherein substituted aryl represents aryl substituted by 1-3 substitutes independently specified in alkyl, halogen and halogenalkyl, and wherein substituted 1H-pyrazolyl represents 1H-pyrazolyl substituted by 1-3 substitutes independently specified in alkyl and aryl; Ra represents hydrogen or methyl; Rb represents hydrogen or methyl; or Ra and Rb together with a carbon atom, to which they are attached, form cyclopropyl, cyclobutyl or cyclopentyl; provided Ra and Rb both represent hydrogen, or both represent methyl simultaneously, R3 represents (1-methylcyclopropyl)methyl, which possess the inhibitory action on 11b-HSD1.

EFFECT: preparing the compounds, which possess the inhibitory action on 11b-HSD1.

15 cl, 1 tbl, 32 ex

FIELD: chemistry.

SUBSTANCE: invention relates to application of 2-R1-4-R2-6-polynitromethyl-1,3,5-triazines of general formula: , where n=0, X=NO2, Cl, Br, R1=R2=OR3, OAr (R3=CH3, C2H5, CH2(CH2)6CH3, CH2CH2Cl, Ar=metha-C6H4CH3), R1=OR3, OAr, R2=N(C2H5)2; n=1, X=Cl, R1=OR3, R2=NH(CH2)2NH2, N(CH2CH2)2NCH3 as compounds, which possess antibacterial activity.

EFFECT: identification of compounds based on 1,3,5-triazine derivatives, which possess high antibacterial activity.

3 tbl, 7 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, namely to mixture of E- and Z-isomers of (4-bromophenyl)ethylidene hydrazide of 2-[6-methyl-1-(thiethan-3-yl)uracyl-3-yl]acetic acid in molar ratio 3.5:1 of general formula: .

EFFECT: obtained is novel mixture of isomers, demonstrating hypotensive activity.

2 cl, 4 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry and represents medication, possessing virucidal activity, for preventive and therapeutic treatment of viral infections, caused by virus of herpesviridae family, characterised by the fact that said medication contains pyroxican in carrier substance.

EFFECT: invention provides extension of arsenal of means, possessing virucidal activity.

7 cl

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