Use of 2-amino-7-bromo-4-acetylazo[5,4-b]indol to protect organism against hyperbaric and hematic hypoxia and/or liver against carbon tetrachloride poisoning
FIELD: pharmaceutical industry.
SUBSTANCE: invention proposes use of 2-amino-7-bromo-4-acetylazo[5,4-b]indol depicted by formula: against hyperbaric and hematic hypoxia and protection of liver against carbon tetrachloride poisoning. Use of this compound reduces concentration of AlAT by a factor of 2.6 and that of AcAT by a factor of 1.67.
EFFECT: increased therapeutic activity.
The invention relates to the use of 2-amino-7-bromo-4-acetylthiazole[5,4-b]indole of formula 1
to protect the body from exposure to hypobaric and himicheskoi hypoxia and liver from poisoning by carbon tetrachloride.
This property suggests the possibility of using this compound for prevention and treatment in humans acute inhalation poisoning pairs of carbon tetrachloride. Widespread use of carbon tetrachloride in industry, agriculture and military Affairs that makes urgent the search for pharmacological agents that protect the body from exposure to this toxicant. To restore liver function used Essentiale, but its activity is insufficient.
Previously installed hepatoprotective activity of the hydrobromide of 2-amino-4-acetylthiazole[5,4-b]indole (Patent 2076867 RF, MKI36 07D 478/04, AK 31/40. The hydrobromide of 2-amino-4-acetylthiazole[5,4-b]indole protecting the liver from carbon tetrachloride poisoning and how to obtain it / Velieva B.C., Melman A... Tomchin A.B., Smirnov A.V., acavity SV, Gaivoronsky V.V. (Russia). - 5042409/04; Claimed 19.05.92.), formula 2.
Analog antihypoxic action is reference antihypoxic drug antizol formula 3 (Methodological recommendations what about the experimental study of drugs, the proposed clinical study as a antihypoxic funds./Edited Ludlowkoeni. - M: BI, 1990. - 18 C.). Hypobaric hypoxia occurs when the lack of oxygen due to reduced atmospheric pressure. These phenomena are common when we are forced to find people in the highlands or in the depressurization of the aircraft.
Himicheskaya hypoxia develops when injected into the blood of toxins, blocking the work of hemoglobin, resulting in impeded the transport of oxygen in the body and death. Poisoning of this kind is not uncommon in case of emergency chemical industries, military conflicts.
The aim of the invention is the use of compounds of indole fused with thiazole, effectively protect the body from hypoxic and hypercapnic hypoxia and liver from poisoning by carbon tetrachloride.
The inventive compound is a white crystalline substance, it is difficult soluble in water, alcohol, acetone and slightly soluble in dimethylformamide and dimethylsulfoxide. The inventive compound is produced by the action of an alkaline agent to the hydrobromide of 2-amino-7-bromo-4-acetylthiazole[5,4-b]indole.
Example. 3.0 g (to 7.67 mmol) to the hydrobromide of 2-amino-7-bromo-4-acetylthiazole[5,4-b]indole suspension in 19 ml of the odes and add 30% aqueous sodium acetate solution to pH 5-6 by the universal indicator, mix and after 30 minutes, filtered. The precipitate was washed with water (5×10 ml), dried in air and 30 min at 105°C. Obtain white crystals, the weight of 2.08 g (87,5%). For analytical purposes the substance periostat of DMF (activated carbon) in a five-fold volume of ether. The next day filtered off the precipitated crystals, washed with acetone and dried. Get shiny white crystals. Sample of Beilstein negative. The melting temperature depends on the temperature entered into the device. In the case of application at 230°With the substance melts at 250-252°C (decomposition).
The substance is homogeneous according to TLC. The adsorbent - Silufol UV-254, the solvent for application - dimethylformamide, eluent is acetone:hexane = 1:1; Rf0,64.
Range of PMR in DMSO d6. 300 MHz, ppm: 2.70 (INSN3), 6.80 (2H, NH2), 7.32 (1H, H6), 7.72 (1H, H8), 8.06 (1H, H5).
Study of biological activity of the claimed compounds. Acute toxicity was determined on outbred mice-males weighing 18-22 g by well-known methods (Prozorovsky V.B. have been and others, "rapid method for determining the average effective dose and its errors, Pharmacology and toxicology, 1978, No. 4, s-502). The target compound was administered intraperitoneally once in suspension in water with the addition of tween-80. LD503890±370 mg/kg, which can be attributed to the claimed little connection to execmem substances.
Study of the protective effect of compound 1 when exposed to hypobaric hypoxic hypoxia. Experiments were performed on outbred mice weighing 18-20 g of the Inventive compound was administered intraperitoneally in the form of a thin slurry with divinam-20 dose of 67.1 mg/kg 30 minutes prior to the hypoxic episode. The optimal dose was chosen based on preliminary experiments. The effect of the drug was compared with known antihypoxic drug-antisolar in equimolar dose of 25 mg/kg to Mice in the control were treated with equivalent volumes of saline. In each group of 6 animals.
Hypoxia was simulated in the chamber "lifting" of the animals at the altitude of 10,000 m with a speed of 50 m/s and an exposure time within 90 minutes assessment of the protective effect was studied by life expectancy and survival of animals after a hypoxic episode. The activity of the claimed compounds 1 in comparison with the known analogue presented in table 1.
|Antihypoxic activity of the claimed compounds|
|Connection||The average life expectancy min||Increase survival of animals %|
|Note. The difference is significant in comparison to the control animals *-R≤0,01.|
According to table 1 it is seen that the inventive compound 1 increases survival of animals in 3.16 times compared to control (antizol in 4.15 times), but the number of surviving individuals at him more than the benchmark (83% and 75% respectively). Therefore, we can conclude that the connection exceeds 1 for this type of activity reference drug.
Gemicescuu hypoxia (Manual on experimental (preclinical) study of new pharmacological substances. Moscow (2000), 153-158) was studied on mice-males weighing 18-20, study drug in equimolar dose in relation to antipolo was injected intraperitoneally in the form of a thin slurry with tween-20 for 30 minutes before hypoxia, which was modeled by the introduction of intraperitoneally 2% solution of sodium nitrite at a dose of 200 mg/kg the Effect of the drug was compared with known antihypoxic drug-antisolar at a dose of 25 mg/kg to Mice in the control were treated with equivalent volumes of saline. Register the lifetime of animals and the number of surviving individuals. The activity of the claimed compounds 1 in comparison with the known analogue presented in table 2.
|Antihypoxic activity of the claimed compounds on the model himicheskoi hypoxia|
|Medication||Dose, mg/kg||Qty animals||Lifetime min||Life expectancy % compared to the control||The increase in survival rate, %|
|Phys. solution||-||7||29,83±to 10.09||-||-|
|Note. The difference is significant in comparison to the control animals *-R≤0,05, **-R≤0,01|
The results of the experiments are given in table 2, show life expectancy of animals are almost two times (the standard one and a half times), but the connection 1 helps to survive half of the individuals, and the standard does not give survival. The claimed connection far exceeds antizol on antihypoxic activity on the model himicheskoi hypoxia.
Hepatotropic action was studied on rats male weight 140-170, carbon Tetrachloride was injected PADCO is but daily in 50% solution in liquid paraffin for 4 days in a row in an amount of 0.4 ml/100 g mass. Simultaneously with CCl4introduced compound 1 at a dose of 67.1 mg/kg intraperitoneally. It was compared with the known hepatoprotector Essentiale and compound 2, which was investigated in equimolar dose of 67.6 mg/kg
The clinical picture of poisoning CCl4develops slowly. The main symptoms of severe intoxication is manifested only at the end of 2 days, and in 4 to 7 days lead to a lethal outcome. All the patients had severe liver damage up to fatty degeneration of the body. Evaluation of the protective effect of compounds 1 and analogues was performed by examining the activity specific for liver alanine transferase (Alt) and aspartate aminotransferase (AST) in the serum. The change in the activity of Alt and AST in the serum indicates deleterious effects CCl4on the cell membrane and organelles of the cell. The results of the experiments are shown in table 3.
|The change in the activity of Alt and AST in the serum on the seventh day of the experiment|
|Groups of animals||B %||AST, %|
The data obtained indicate that the use of compound 1 in 2.6 times reduces the concentration of Alt and 1.67 times the concentration of AST. Thus, the ability to protect the liver from poisoning by carbon tetrachloride connection exceeds 1 connection 2 and table.
The use of 2-amino-7-bromo-4-acetylthiazole[5,4-b]indole of the formula
to protect the body from hypobaric and himicheskoi hypoxia and/or liver from poisoning by carbon tetrachloride.
FIELD: organic chemistry, medicine, biochemistry, pharmacy.
SUBSTANCE: invention relates to novel azaheterocycles of the general formula (I): possessing inhibitory effect on activity of tyrosine kinase and can be used in treatment of different diseases mediated by these receptors. In compound of the general formula (1) W represents azaheterocycle comprising 6-13 atoms that can be optionally annelated with at least one (C5-C7)-carbocycle and/or possibly annelated with heterocycle comprising 4-10 atoms in ring and comprising at least one heteroatom chosen from oxygen (O), sulfur (S) or nitrogen (N) atom; Ra 1 represents a substitute of amino group but not hydrogen atom, such as substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-10-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; Rb represents carbamoyl group -C(O)NHRa wherein Ra represents a substitute of amino group but not hydrogen atom, such as possibly substituted alkyl, possibly substituted aryl, possibly substituted 5-10-membered heterocyclyc comprising at least one heteroatom chosen from O, S or N; Rc represents a substitute of cyclic system, such as possibly substituted (C1-C6)-alkyl, possibly substituted aryl and possibly substituted 5-6-membered heterocyclyl comprising at least one heteroatom chosen from O, S or N; or Rb and Rc form in common aminocyanomethylene group [(=C(NH2)CN], or their pharmaceutically acceptable salts. Also, invention relates to methods for synthesis of these compounds (variants), a pharmaceutical composition, combinatory and focused libraries.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved methods for synthesis and preparing.
35 cl, 16 sch, 13 tbl, 43 ex
FIELD: organic chemistry, medicine.
SUBSTANCE: invention relates to compounds of the formula (I): and their salts, to methods for their preparing, compositions containing thereof and their using in medicine, in particular, for prophylaxis or treatment of clinical state wherein a selective agonist of β2-adrenoceptors is prescribed.
EFFECT: valuable medicinal properties of compound and compositions.
32 cl, 4 dwg, 82 ex
FIELD: organic chemistry, pharmaceuticals.
SUBSTANCE: invention relates to new compounds of formula I , or stereoisomers, or pharmaceutically acceptable salts thereof, wherein Q is SO2; n = 2 or 3; each R1 and R2 is independently H, halogen, OR22 or C1-C6-alkyl; each R3 and R4 is H; each R5 and R6 is independently H or C1-C6-alkyl optionally substituted with phenyl or R5 and R6 together with together with atom to which they are attached may form 5-7-membered ring optionally containing N as the second heteroatom optionally substituted with COOH or C1-C6-alkyl; R7 is H; R7 is optionally substituted 8013-membered bicyclic or tricyclic ring system, containing N in bridge bond and optionally 1, 2 additional heteroatoms selected from N, S wherein substituent represent 1 or 2 halogen atoms; R22 is H or C1-C6-phenyl optionally substituted with C1-C6-alkyl. Compounds of present invention specifically bond to 5-HT6 receptor and are useful in pharmaceutical compositions.
EFFECT: compounds with specific bonding to 5-HT6 receptor.
10 cl, 3 tbl, 45 ex
FIELD: organic chemistry, pharmaceuticals.
SUBSTANCE: invention relates to compounds of general formula I and pharmaceutically acceptable salt thereof, wherein R1, R3, R4, R5, and R10 are independently H, halogen, C1-C4-alkyl, etc.; R2 is H, halogen, NO2, etc.; R6 is H, C1-C6-alkyl, C1-C6-alkoxy-substituted C1-C4-alkyl, etc.; R7 is H, C1-C4-alkyl or C2-C4-alkenyl, optionally substituted with halogen; R8 and R9 are H, R11 and R12; meanings of the rest substituents are as define in specification.
EFFECT: new compounds with value biological properties and useful as drug having activity in relates to progesterone receptor.
15 cl, 3 tbl, 80 ex
FIELD: organic chemistry.
SUBSTANCE: invention relates to bicyclic 1,4-piridotiazine-1,1-dioxides of general formula I wherein R1 is chlorine or fluorine; R2 is linear or branched alkyl, cycloalkyl, optionally reduced aryl or heteroaryl, etc. Method for production of said compounds includes reaction of acyclic sulfones with primary alcohols, preferably in presence of inorganic or organic such as carbonates or alkali metal hydroxides tertiary organic amines or base mixtures, preferably in aprotic bipolar media without solvents, or mixture thereof with water.
EFFECT: safe method for production of new compounds useful as drugs.
2 cl, 2 ex
SUBSTANCE: compound is represented by structural formula
or its pharmaceutically permissible salts, where R1 is the hydrogen atom (1), C1-8acyl(2), hydroxyl (3), halogen atom (5), C2-8acyl (3), C1-8-alcocsy (4), substituted with phenyl or C2-8acyl, substituted with NR2R3; R2R3 independently represent hydrogen atom (1) or C1-8acyl(2), X and Y each independently representing C (1), CH (2) or N (3). is (1) single or (2) double bond. is 5-7-member carbocyclic group or 5-7-member partially or fully saturated heterocyclic group defined in claim 1 of invention. A is one of A1 to A5 groups defined by claim 1 of the invention. The compounds show inhibiting properties relative to poly(ADP-ribose)polymerase are usable as prophylactic and/or curative drugs for treating ischemic diseases (in brain, spinal cord, heart, digestive tract, skeletal muscle, eye retina, e.t.c.), inflammatory diseases (intestinal inflammation, disseminated sclerosis, arthritis, e.t.c.), neurodegenerative disorders (extrapyramidal disorder, Alzheimer disease, muscle dystrophy, cerebrospinal canal stenosis in lumbar segment of the vertebral column, e.t.c.), diabetes, stroke, cerebral injury, hepatic insufficiency, hyperalgesia, e.t.c. The compounds are also of use in struggling against retroviruses (HIV and others), as sensitizing agents for treating cancer cases and immunodepressant agents.
EFFECT: enhanced effectiveness of treatment.
19 cl, 90 tbl
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel lactam compounds of the formula (I) or their pharmaceutically acceptable salts wherein A means phenyl, thienyl, pyridyl, pyrimidinyl, pyrazinyl; R2, R3 and R4 can be similar or different and mean independently of one another hydrogen atom (H), halogen atom, -OH, (C1-C6)-alkyl, (C1-C6)-alkoxy-group, -NH2, -NO2, -CF3, phenyl that can comprise substitute(s), benzyloxy-group that can comprise substitute(s), pnehylvinyl, and one among R2, R3 and R4 means -CF3-O- and others mean H; B means phenyl that can comprises substitute(s), monocyclic aliphatic (C3-C8)-ring, dihydropyrane ring; -X- and -Y- xan be similar or different and they mean independently -O-, -NH-, -NR5-, -S-; Z means -CH2-, -NH-; W means -NR1-, -CR8R9- wherein R1 means H; R8 and R9 are similar or different and mean H; wherein R5 represents a linear alkyl group that can comprise substitute(s), (C1-C8)-linear or branched alkoxycarbonyl group, acyl group chosen from formyl group, acyl group comprising (C1-C6)-alkyl, (C1-C6)-alkenyl or (C1-C6)-alkynyl group that can comprise substitute(s), carbamoyl group comprising (C1-C6)-alkyl group at nitrogen atom that can comprise substitutes, sulfonyl group comprising (C1-C6)-alkyl group at sulfur atom that can comprise substitute(s); each among a, b and c represents position of carbon atom under condition that: (i) substitute(s) is chosen from the group comprising halogen atom, -OH, (C1-C6)-alkyl, mercapto-group, (C1-C6)-alkoxy-group, -NO2, -COOH, -CF3, phenyl, -NH2, (C1-C8)-linear or branched alkoxycarbonyl group, (C1-C8)-linear or branched acyl group, (C1-C8)-linear or branched acyloxy-group; (ii) when B represents benzene ring, each among -X- and -Y- represents -NH-, -Z- represents -CH2- and -W- represents -NH- then R2, R3 and R4 can not mean phenyl group, 4-bromophenyl group, 4-hydroxyphenyl group, 4-methoxyphenyl group, 2-hydroxyphenyl group, 3,4-dimethoxyphenyl group or 3-methoxy-4-hydroxyphenyl group. Compounds of the formula (I) show the enhanced capacity for transport of sugar and can be used in pharmaceutical compositions for prophylaxis and/or treatment of diabetes mellitus and diabetic nephropathy.
EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.
19 cl, 21 tbl, 54 ex
FIELD: organic chemistry, herbicides.
SUBSTANCE: invention relates to a compound of the general formula [I]: wherein R1 and R2 can be similar or different and each represents (C1-C10)-alkyl group; each among R3 and R4 represents hydrogen atom; R5 and R6 can be similar or different and each represents hydrogen atom or (C1-C10)-alkyl group; Y represents 5-6-membered aromatic heterocyclic group or condensed aromatic heterocyclic group comprising one or some heteroatoms chosen from nitrogen atom, oxygen atom and sulfur atom wherein heterocyclic group can be substituted with 0-6 of similar or different groups chosen from the following group of substitutes α, and so on; n means whole values from 0 to 2; [Group of substitutes α]: hydroxyl group, halogen atoms, (C1-C10)-alkyl groups, (C1-C10)-alkyl groups wherein each group is monosubstituted with group chosen from the following group of substitutes β, (C1-C4)-halogenalkyl groups, (C3-C8)-cycloalkyl groups, (C1-C10)-alkoxy-groups, (C1-C10)-alkoxy-groups wherein each group is monosubstituted with group chosen from the following group of substitutes and so on; [Group of substitutes β]: hydroxyl group, (C3-C8)-cycloalkyl groups that can be substituted with halogen atom or alkyl group, (C1-C10)-alkoxy-group, (C1-C10)-alkylthio-groups, (C1-C10)-alkylsulfonyl groups, (C1-C10)-alkoxycarbonyl groups, amino-group, carbamoyl group (wherein its nitrogen atom can be substituted with similar or different (C1-C10)-alkyl groups), (C1-C6)-acyl groups, (C1-C10)-alkoxyimino-groups, cyano-group, optionally substituted phenyl group; [Group of substitutes γ]: optionally substituted phenyl group, optionally substituted aromatic heterocyclic groups, cyano-group. Also, invention relates to herbicide comprising derivative of isoxazoline of the formula [I] as an active component or its pharmaceutically acceptable salt. Invention provides the development of isoxazoline derivative possessing the herbicide activity with respect to resistant weeds, selectivity for cultural crop and weed.
EFFECT: valuable herbicide properties of substances.
18 cl, 24 tbl, 106 ex
FIELD: organic chemistry.
SUBSTANCE: invention relates to new 2-amino-4-acetyl-7-bromo-8b-hydroxy-3a,8b-dihydroxytiazolo[5,4-b]indole of formula useful in liver protection from poisoning with carbon tetrachloride. Said compound has boiling point of 174-175°C (decomposition) and LD50 of 1950±180 mg/kg. Method for production of claimed compound also is disclosed.
EFFECT: new compound for liver protection from poisoning with carbon tetrachloride.
2 ex, 1 tbl
FIELD: organic chemistry, medicine, pulmonology.
SUBSTANCE: invention relates to a new chemical compound, namely, 7-bromo-4-acetylthiazolo[5,4-b]indol-2-succinimide of the formula: that is able to protect body against hypoxia and possesses the curative effect in lung toxic edema. The melting point of this compound is 267-269°.
EFFECT: valuable medicinal properties of compound.
2 tbl, 1 ex
SUBSTANCE: method involves administering pharmaceutical composition for restoring liver functions, cholesterol metabolism and intestinal biocenosis.
EFFECT: enhanced effectiveness of treatment.
13 cl, 1 tbl
SUBSTANCE: method involves introducing human fetus liver cells suspension containing stem cells, into patient liver and/or in pareneteral way. The suspension is introduced under ultrasonic control in the amount of 200-300 millions of cells under hepatic capsule at a depth of 0.5-1.0 cm. Being intravenously introduced, the dose is equal to 1.0-1.5 billions of cells. When combining both introduction methods, the total dose does not exceed 1.5 billions of cells.
EFFECT: stable restoration of kidney functions.
SUBSTANCE: method involves introducing Detralex at a dose of 500 mg twice a day. No hemorrhages threatening, the grug is introduced in interrupted mode like 30 days receiving the drug and 1 month log pause. Marked gastroenteropathy being the case with hemorrhages threatening, the drug is administered in continuous mode within 2-6 months. Control esopahagoduodenoscopy and endoscopically sclerosing varicose veins of cardia is carried out when indicated. Next, the treatment is continued in interrupted mode. General therapy period is equal to 2-4 years in both groups.
EFFECT: enhanced effectiveness of treatment; no adverse side effects observed; reduced risk of gastrointestinal hemorrhages.
FIELD: chemical-pharmaceutical industry, medicine, pharmacy.
SUBSTANCE: invention relates to a solid medicinal formulation of hepatoprotective effect that comprises combination of flavanolignan with phopholipids as active components and special additive - colloidal silicon dioxide, polyvinylpyrrolidone, trehalose, sodium stearylfumarate, calcium phosphate and/or mannitol. Method for preparing this medicinal formulation involves a wetting step of mixture of phospholipid with colloidal silicon dioxide with small amount of water in the mass ratio about 2:1, respectively, addition of flavanolignan, calcium phosphate and/or mannitol, trehalose followed by wetting the mixture with 15% polyvinylpyrrolidone aqueous solution, wet and dry granulation and powdering dry granulate with sodium stearylfumarate. Agent is prepared in form of capsule preferably. Invention provides simplifying technology and enhancing stability of agent and expands assortment of agents of hepatoprotective effect.
EFFECT: improved and valuable medicinal properties of formulation.
4 cl, 1 tbl
FIELD: medicine, hepatology.
SUBSTANCE: invention proposes a drug for treatment of chronic hepatitis B in the exacerbation stage based on using fumaric acid (tris-2-oxyethylammionium fumarate) triethylamine salt. This salt possesses antioxidant and immunomodulating properties, allows decreasing the level of autoimmune damage of liver cells. Effect of this drug has been studied by indices of intoxication syndrome in patients, decreasing bilirubin content and cytolysis enzymes.
EFFECT: valuable medicinal properties of drug.
FIELD: medicine, pharmaceutical industry, phytotherapy, pharmacy.
SUBSTANCE: invention proposes a hepatoprotective agent showing antioxidant activity, in particular, to using a plant dropwort (Filipendula ulmaria (L.) Maxim.) above-ground part as a hepatoprotective agent possessing the antioxidant activity. Method for preparing a hepatoprotective agent possessing the antioxidant activity involves extraction of vegetable raw with ethanol in percolator devices battery wherein dropwort (Filipendula ulmaria (L.) Maxim.) above-ground part is subjected for extraction under definite conditions. Extract possessing the hepatoprotective effect prepared by above describes method possesses the enhanced antioxidant activity.
EFFECT: valuable medicinal property of agent, improved prepared method.
3 cl, 5 tbl, 4 ex
FIELD: medicine, hepatology.
SUBSTANCE: invention proposes a preparation containing spotted milk thistle fruits extract and field artichoke leaves extract or pumpkin seeds extract, and normophlora active microorganisms sorbed on a carrier. The preparation comprises lactulose or lactose, or lactite as an agent stimulating multiplication of microorganisms. Components of the preparation are placed into two capsules wherein one capsule comprises plant extracts possessing the hepatoprotective effect, and another capsule comprises intestine normophlora microorganisms and agent stimulating multiplication of microorganisms. Invention provides enhanced effectiveness in treatment of diseases associated with liver damage, accelerating regeneration and recovering functional activity of hepatocytes. Invention can be used in treatment of liver and hepatobiliary system diseases.
EFFECT: valuable properties and enhanced effectiveness of preparation.
6 cl, 4 tbl, 8 ex
SUBSTANCE: it has been suggested the method for introducing a preparation in efficient dosage being either a substance or preparation prepared according to homeopathic technique or biologically active additive that contains a substance isolated out of hepatic cells being slightly hydrophobic, water-soluble, negatively charged at alkaline pH, at molecular weight ranged 500-15000 Da that enables to decrease tissue-specifically the ratio of phosphorylated adenosine diphosphate against the quantity of atomic oxygen spent by highly energized mitochondria in the course of oxidizing phosphorylation. The suggested method and preparation enable to treat efficiently astheno-depressive state and, also, increases the efficiency of complex therapy of pulmonary and intestinal diseases.
EFFECT: higher efficiency of therapy.
16 cl, 21 ex
FIELD: organic chemistry, medicine, hepatology.
SUBSTANCE: invention proposes using 2-amino-4-acetylthiazolo[5,4-b]indole as a substance protecting liver against poisoning with carbon tetrachloride. Invention provides enhancing degree of liver protection against poisoning with carbon tetrachloride.
EFFECT: valuable medicinal property of compound.
FIELD: organic chemistry, medicine, hepatology.
SUBSTANCE: invention proposes using 2-amino-7-bromo-4-acetylthiazolo[5,4-b]indole hydrobromide of the formula (I) as a substance protecting liver against poisoning with carbon tetrachloride and/or possessing prophylactic effect in lung toxic edema. Invention provides enhancing degree of liver protection against poisoning with carbon tetrachloride, decreasing expression of lung edema by the pulmonary coefficient and enhancing viability of animals (with respect to control).
EFFECT: valuable medicinal property of substance.
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to novel derivatives of tetrahydrocarbazole of the formula (I): wherein n = 0, 1 or 2; X represents -NH or oxygen atom (O); each R is a similar or different radical and chosen independently from group consisting of halogen atom, halogenalkyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, -R10-cycloalkyl, -OR2, -R10OR2, -R10C(O)R2, -C(O)R2, -CO2R2, -R10CO2R2, -R10SO2R2, -S(O)mR2, cyano- or nitro-group; each R1 is a similar or different radical and chosen independently from group consisting of halogen, halogenalkyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, -R10-cycloalkyl, -OR2, -R10OR2, -R10C(O)R2, -C(O)R2, -CO2R2, -R10CO2R2, -R10SO2R2, -S(O)mR2, cyano- or nitro-group and wherein each m means 2 independently; each R10 is a similar or different radical and chosen independently from alkylene; each p and q is chosen independently from 0, 1, 2, 3, 4 or 5; each R2 is a similar or different radical and chosen independently from group consisting of hydrogen atom (H), alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, -R10-cycloalkyl and -R10OH; ring A represents phenyl, naphthyl or heteroaryl wherein heteroaryl represents monocyclic 5-7-membered aromatic ring or condensed bicyclic aromatic ring system consisting of two such aromatic rings that comprise one or two nitrogen atoms and/or sulfur atoms, and to their pharmaceutically acceptable salts, solvates, esters and amides. Compounds of the formula (I) possess effect against disorders caused by HPV-infection and useful in treatment of human papilloma. Also, invention relates to a pharmaceutical composition based on compounds of the formula (I) and its using in preparing drugs for their using in treatment and prophylactic of states or disorders caused by HPV-infection.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.