3-methyl-8-piperazine-7-(thiethanyl-3)-1-ethylxanthine hydrochloride, exhibiting antiaggregant and disaggregation activity

FIELD: chemistry.

SUBSTANCE: invention relates to 3-methyl-8-piperazino-7-(thiethanyl-3)-1-ethylxanthine hydrochloride of formula .

EFFECT: novel compound which can be used in medicine as an antiaggregation and disaggregation agent is obtained and described.

3 cl, 2 tbl, 1 ex


The invention relates to medicine, namely to pharmaceutical chemistry and pharmacology, and can be used to create new drugs with antiaggregatory and disaggregating activity.

Prototype and product comparison is pentoxifylline (3,7-dimethyl-1-(5-oxohexyl)xanthine), which is used in the clinic as a corrector of rheological disorders, causing a decrease in blood viscosity and disaggregation of platelets (State register of medicines. / The official publication.- M.: Medicine, 2004. - Vol.2. - S. 1791).

The objective of the invention is to expand the Arsenal of biologically active substances exhibiting antiaggregatory and disaggregating activity.

The technical result - obtaining substances exhibiting antiaggregatory and disaggregating activity.

The inventive 3-methyl-8-piperazine derivatives-7-(titanyl-3)-1-metilksantina hydrochloride (Ia) of the formula

showing antiaggregatory and disaggregating activity.

The proposed connection is synthesized as follows.

Compound Ia was synthesized from 8-bromo-3-methyl-7-(titanyl-3)-1-metilksantina (alkylation Reaction of 8-bromo-3-methyl-7-(titanyl-3)xanthine N-1 position. / Uwhealth, Paholyothin // Honey. journal of Bashkortostan. - 2006. - V.4, No. 1. - S-211) in the 2 study is. When boiling 8-bromo-3-methyl-7-(titanyl-3)-1-metilksantina with 3-fold molar excess of the piperazine of uranyl in ethanol is produced 3-methyl-8-piperazine derivatives-7-(titanyl-3)-1-Edilkamin, whose interaction in the environment of dioxane with 5% solution of hydrogen chloride in ethanol leads to 3-methyl-8-piperazine derivatives-7-(titanyl-3)-1-metilksantina hydrochloride.

Example 1. The synthesis of compounds Ia

A solution of 1.38 g (4 mmol) of 8-bromo-3-methyl-7-(titanyl-3)-1-metilksantina and of 2.33 g (12 mmol) of piperazine of uranyl in 50 ml of ethanol is boiled for 5 hours. Cool, filter. The filtrate is evaporated in vacuo, to the residue was added water, the precipitate filtered off, washed with water, dried. Get 1,11 g (79%) of 3-methyl-8-piperazine derivatives-7-(titanyl-3)-1-metilksantina. Tpl.210-213°C (from ethanol).

Elemental analysis.

Found, %: 51.5 N 6,4 N 23,8 - C15H22N6O2S

Calculated, %: C 51,4 H 6,3 N 24,0

An NMR spectrum1H (CDC13), δ, ppm: of 1.27 (3H, t, J 7.0 Hz, CH3), 3,02-3,10 (4H, m, N(CH2)2), 3,11-3,19 (4H, m, N(CH2)2), 3,21-3,30 (2H, m, S(CH)2), 3,52 (3H, s, 3-NCH3), 4,14 (2H, q, J 7.0 Hz, 1-NCH2), 4,32-4,43 (2H, m, S(CH)2), 5,43-5,59 (1H, m, NCH).

To a solution of 0.53 g (1.5 mmol) of 3-methyl-8-piperazine derivatives-7-(titanyl-3)-1-metilksantina in 15 ml of dioxane is added a 5% solution of hydrogen chloride in ethanol to pH 1-2. Cool, the precipitation is filtered off, washed with dioxane and dried. P is to obtain 0.55 g (95%) of compound Ia. Tpl.247°C decomp. (from ethanol).

Elemental analysis.

Found, %: From 46.4 N 6,2 N a 21.5 - C15H23ClN6O2S

Calculated, %: 46.6 N 6,0 N 21,7

IR Spectrum (tablets with KBr), ν, cm-1: 1659,4; 1672,0; 1706,7 (C=NVal.C=OVal.), 2430-2500, 2570-2720 (N+H2 shaft.).

The proposed connection is a white crystalline substance, soluble in water, dimethylformamide, when heated in ethanol, chloroform.

Antiaggregatory and disaggregating activity.

Antiaggregatory and disaggregating activity proposed compounds were studied in vitro by the method of Born (Born G.V.R. Aggregation of blood platelets by adenosine diphosphate and its reversal. / G.V.R.Born // Nature. - 1962. - Vol.194, No. 4832. - P.924-929) aggregometry "Thromlite-1006A using donated human blood. The method is based on registration of the change of optical density platelet-rich plasma before and after the introduction of the inducer of platelet aggregation. As inducer of aggregation used adenosine diphosphate (ADP) at a concentration of 20 μg/ml as the reference product used "Trental", produced by Aventis Pharma Ltd., Mumbai, India, in equimolar concentrations.

Antiaggregatory activity of compound Ia.

The effect of compound Ia on ADP-induced platelet aggregation was assessed by the degree of reduction of aggregation in the prior 5-minute Incubus and substances in platelet-rich plasma (table 1). The results of the study found that the introduction of 10-3mol/l of the claimed compounds in the cell of aggregometry 5 minutes before ADP leads to a complete suppression of platelet aggregation relative to the control. Pentoxifylline in this concentration inhibits platelet aggregation by 13.9%. When studying the dependence of the effect on the concentration determined that the effective concentration (EC50) compounds Ia, causing inhibition of platelet aggregation by 50%, equal to 5·10-4mol/L. Effective concentration (EC50) pentoxifylline equal to 2·10-3mol/L. Introduction to 2.5·10-4mol/l proposed connection in the cell of aggregometry inhibited platelet aggregation in an average of 24.3%. In this concentration pentoxifylline is inactive.

Disaggregating the potency of the compound Ia.

Disaggregating activity was calculated in percent of the collapsed platelet aggregates after entering the claimed connection after 5 minutes of ADP (table 2). The introduction of compound Ia in a concentration of 10-3mol/l at a height of ADP-induced aggregation within 5 minutes leads to disaggregation average of 52.9% of the originally existing units of platelets, which is higher than the comparison drug (pentoxifylline in this concentration causes a breakdown in the middle 37,4% platelet aggregates). BB is Denia compound Ia in a concentration of 5·10 -4mol/l at a height of ADP-induced aggregation leads to decay on average 37.4% of units of platelets. Pentoxifylline in this concentration is inactive.

Accordingly, the chemical compound (Ia) is very antiaggregatory and disaggregating activity than pentoxifylline.


Table 1
The effect of the claimed compounds and drug comparisons on ADP-induced platelet aggregation
ConnectionConcentration, mol/lInhibition of ADP-induced platelet aggregation, % of control
10-3 13,9±2,6*
Note: * - the difference from the control was significantly (p<0,05).

Table 2
The effect of the claimed compounds and drug comparisons on the disaggregation of platelets
ConnectionConcentration, mol/l% broken platelet aggregates
Note: * - the difference from the control was significantly (p<0,05).

1. 3-Methyl-8-piperazine derivatives-7-(titanyl-3)-1-metilksantina hydrochloride formula

2. The compound according to claim 1, exhibiting antiaggregatory activity.

3. The compound according to claim 1, times the total disaggregating activity.


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38 cl, 1 tbl, 1 ex

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2 cl, 3 tbl, 8 ex

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2 tbl, 4 ex

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6 cl, 3 tbl, 87 ex

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12 cl, 2 dwg, 6 ex

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1 ex

Anticoagulant // 2399377

FIELD: medicine, pharmaceutics.

SUBSTANCE: anticoagulant exhibiting a thrombin and factor Xa inhibiting activity represents a solution of biologically active birch bark complex prepared by water extraction of ground birch bark on boiling, concentration of aqueous extract and sodium chloride saturation, sediment discharge, ethyl acetate extraction of filtrate, concentration of filtrate, dilution with chloroform, sediment filtration and dissolution to ensure final concentration of 1.0-251.2 mcg/ml, effective for thrombin activity inhibition, and final concentration of 0.1-851.0 mcg/ml, effective for blood coagulation factor Xa activity inhibition.

EFFECT: invention allows implementing thrombin activity inhibition.

3 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula I , where: R1, R2, R3 and R4 independently from each other mean hydrogen, F, CI, Br, I; R5 designates hydrogen, alkyl with 1, 2, 3, 4, 5 or 6 C atoms, or cycloalkyl with 3, 4, 5 or 6 C atoms; R6 designates hydrogen; R7 and R8 independently from each other mean hydrogen, W means CrH2r or CsH2S-2; and one or more CH2-groups in C2H2r and CsH2s-2 can be substituted with NR17, oxygen or S; R17 means hydrogen, alkyl with 1, 2, 3 or 4 C atoms; r means 1, 2, 3, 4, 5 or 6; s means 2, 3 or 4; X designates-with C(O)- or -S(O)2-; Z means -C(O)- or a bond; and also to their pharmaceutically acceptable salts and trifluoroacetates. The invention also concerns application of the compounds of formula I, and also to a pharmaceutical composition.

EFFECT: preparation of new biologically active compounds exhibiting NHE3 inhibiting activity.

16 cl, 64 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: there is offered a method for preparing low-molecular heparins by enzymatic degradation. For enzymatic depolymerisation, immobilised lysozyme is used.

EFFECT: prepared low-molecular heparin shows higher inhibitor activity with respect to blood coagulation factor Xa and lower inhibitor activity with respect to thrombin in comparison with initial heparin.

2 tbl, 3 ex

Rgd-like peptides // 2396271

FIELD: chemistry.

SUBSTANCE: invention discloses novel synthetic RGD-like peptides capable of dose-dependant inhibition of thrombocyte aggregation.

EFFECT: obtaining novel compounds capable of dose-dependant inhibition of thrombocyte aggregation.

2 tbl, 1 ex

Novel compounds // 2395511

FIELD: chemistry.

SUBSTANCE: present invention relates to novel xanthine derivatives of general formula (I) and their pharmaceutically acceptable salts which have HM74A receptor activity, which can be used in therapy for treating diabetic dyslipidemia, combined dyslipidemia, heart failure, hypercholesteremia, atherosclerosis, arteriosclerosis, hypertriglyceridemia, type II sugar diabetes, type I diabetes, insulin resistance, hyperlipidemia, anorexia nervosa, obesity, coronary artery disease, thrombosis, stenocardia, chronic kidney disease, peripherical vascular disease or stroke. In compounds of formula (I) , R1 is hydrogen or methyl; R2 is unsubstituted H-C4-6 alkyl; and R3 is chlorine.

EFFECT: obtaining novel compounds and a pharmaceutical composition based on the said novel xanthine derivatives.

15 cl, 54 ex

FIELD: medicine.

SUBSTANCE: pellet-form pharmaceutical composition for treating vertigo containing cinnarizine and dimenhydrinate wherein the release of active ingredients is slowed down, and the composition also contains a binding agent, a slow-release agent, an excipient and a pharmaceutical aid taken in a certain ratio. The application of the pharmaceutical composition for treating vertigo of any genesis.

EFFECT: slow-release composition is effective in treating vertigo.

6 cl, 4 dwg, 3 tbl, 6 ex