RussianPatents.com

N-(4-acetoxybenzoyl)glycine lithium salt possessing tranquilising and nootropic action. RU patent 2505294.

N-(4-acetoxybenzoyl)glycine lithium salt possessing tranquilising and nootropic action. RU patent 2505294.
IPC classes for russian patent N-(4-acetoxybenzoyl)glycine lithium salt possessing tranquilising and nootropic action. RU patent 2505294. (RU 2505294):

C07C233/00 - Carboxylic acid amides
A61P25/28 - for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P25/22 - Anxiolytics
A61K31/223 -
Another patents in same IPC classes:
Crystalline form and tosylate of tetracycline compound, crystalline form of said tosylate and polymorph thereof, method of producing tosylate of tetracycline compound, polymorph obtained using said method, and pharmaceutical compositions based on said crystalline form and polymorph Crystalline form and tosylate of tetracycline compound, crystalline form of said tosylate and polymorph thereof, method of producing tosylate of tetracycline compound, polymorph obtained using said method, and pharmaceutical compositions based on said crystalline form and polymorph / 2500665
Invention relates to a tosylate of a tetracycline compound of formula 1, polymorphous forms thereof, a method for production thereof and pharmaceutical compositions based thereon.
Agrochemical composition, aqueous azole composition, method of preventing crystallisation and mycosis control method Agrochemical composition, aqueous azole composition, method of preventing crystallisation and mycosis control method / 2484626
Invention relates to agriculture. The agrochemical composition contains a long-chain N,N-dialkyl alkylamide of formula , where: (a) each of R1 and R2 is independently a linear alkyl radical having 4 to 20 carbon atoms, and R is an alkyl group having 6 to 30 carbon atoms, the total number of carbon atoms in R, R1 and R2 is greater than 40; and at least one azole active ingredient of formula and in which R1 is phenyl, 4-chlorophenyl, 4-chlorophenylethyl, 4-chlorophenyl, 2,4-dichlorophenyl, or 4-chlorophenyloxy; R2 is n-butyl, tert-butyl, phenyl, 2-fluorophenyl or a group of general formula : R3 is hydroxyl, oxygen or cyano. The composition additionally contains at least one member selected from a group consisting of a surfactant, an organic solvent and a low-temperature stabiliser. An aqueous aerosol composition contains said composition and water. Lon-chain N,N-dialkyl alkylamide is used to inhibit and/or prevent growth of crystals of pesticide-active azole derivatives. The long-chain N,N-dialkyl alkylamide is added to a pesticide composition in an amount which is sufficient to reduce crystallisation of the azole derivative. For mycosis control, said composition is applied in the focus.
2-alkyl-cycloalk(en)yl-carboxamides 2-alkyl-cycloalk(en)yl-carboxamides / 2419607
Described is 2-alkyl-cycloalk(en)yl-carboxamides of formula
Amide compound synthesis method and acrylamide polymer / 2402527
Invention can be used as a coagulant and a thickener in paper production. The method involves production of an amide compound from a nitrile compound using a bacterial catalyst. A solution which contains the bacterial catalyst and an amide compound is pumped by a volumetric pump from the reaction vessel into a reservoir or into a filter. Use of the volumetric pump prevents formation of impurities derived from the bacterial catalyst. The monomer produced using this method of producing an amide compound and which contains (meth)acrylamide is polymerised to produce an acrylamide polymer.
Method of treating disturbed neuropsychic development of childhood / 2505293
Preparation of carnitine is administered in the following doses: in the children aged 1-6 months old - 100 mg/day, 6-12 months old - 150 mg/day, 1-3 years old - 200 mg/day, 3-7 years old - 500 mg/day, 7-10 years old - 1000 mg/day, 10 years old and more - 1500 mg/day for more than 3-6 months, and the therapy of right hemisphere dysfunction requires high doses, namely: in the children aged 1-6 months old 150 mg/day, 6-12 months old - 225 mg/day, 1-3 years old - 300 mg/day, 3-7 years old - 1000 mg/day, 7-10 years old - 1500 mg/day, 10 years old and more - 2000 mg/day for 2-3 weeks; thereafter minimum age doses are prescribed in the therapeutic course of 3 weeks every 3 weeks. The length of the treatment makes from 3 months to 3 years depending on the patient's state.
Method of correcting psychic condition of patients and antioxidant status in case of organic personality disorder / 2504367
Invention relates to field of medicine, namely to psychiatry and deals with correction of psychic condition of patients and antioxidant system in case of organic personality disorder.
New condensed derivative of aminodihydrothiazine New condensed derivative of aminodihydrothiazine / 2503681
Invention refers to new compounds represented with common formula (I) to its pharmaceutically acceptable salts that have inhibiting activity in relation to products of amyloid β-protein (Aβ42) or decomposition with ferment of beta-site of amyloid-β (BACE1) precursor. In general formula , circle A represents aryl chosen from phenyl, which can be replaced with substitutes with number of 1 to 3, which have been chosen from a group of substitutes α, 5-6-membered heteroalkyl with sulphur atom as heteroatom that can have 1 to 3 substitutes chosen from a group of substitutes α, or 9-10-membered benzo-condensed heterocyclic group having 2 atoms of oxygen in heterocyclic part of the above group, which can be replaced with substitutes with number of 1 to 3, which have been chosen from the group of substitutes α, L means ordinary bond, -NRLCO- (in which RL means hydrogen atom) or -NRLCO-C1-6alkyl (in which RL means hydrogen atom). Circle B represents 5-6-membered heteroaryl or saturated heterocyclic group with 1-3 heteroatoms in a cycle, which have been chosen from a group of hydrogen, oxygen or sulphur atoms, each of which can have 1 to 3 substitutes chosen from the group of substitutes α, or 9-10-membered benzo-condensed group having 2 oxygen atoms in heterocyclic part of the above group, X means methylene that can have 1 to 2 substitutes chosen from the group of substitutes α, Y means methylene that can have 1 to 2 substitutes chosen from the group of substitutes α, and Z means oxygen atom. The rest substitutes are specified in the claim.
Oxazolopyrimidines as agonists of edg-1 receptor Oxazolopyrimidines as agonists of edg-1 receptor / 2503680
Invention refers to derivatives of oxazolopyrimidine in any of their stereoisomeric forms, or in the form of a mixture of stereoisomeric forms specified in Claim 1.
Method of treating vertigo of various origins, kinetosis and vegetative-vascular dystonia (versions) and drug preparation Method of treating vertigo of various origins, kinetosis and vegetative-vascular dystonia (versions) and drug preparation / 2503462
Present group of inventions refers to medicine, namely therapy and neurology, and concerns treating kinetosis. That is ensured by administering a pharmaceutical composition containing an activated potentiated form of the antibodies to brain-specific protein S-100 and an activated potentiated form of the antibodies to endothelial NO-synthase.
Imidazopyridine or imidazopyrimidine derivatives as phosphodiesterase 10a inhibitors Imidazopyridine or imidazopyrimidine derivatives as phosphodiesterase 10a inhibitors / 2502737
Invention relates to organic chemistry and specifically to novel imidazopyridine or imidazopyrimidine derivatives of formula (I) and to pharmaceutically acceptable salts and esters thereof, where A is N or C(R6); R1 is hydrogen, lower alkyl; R2 is halogen, C(O)NR7R8 or C(O)OR9; R3 is hydrogen, NR10R11; R4 is hydrogen, lower alkyl; R5 is phenyl or thiazolyl or pyridine, which can be substituted with one substitute independently selected from a group consisting of halogen; R6 is hydrogen, halogen, CN, C3-C6cycloalkyl; R7 and R8 are independently selected from a group consisting of hydrogen, lower alkyl, lower alkoxy-lower alkyl, fluoro-lower alkyl, C3-C6cycloalkyl, N(H,lower alkyl)-lower alkyl, hydroxy- lower alkyl, hydroxy-lower alkoxy- lower alkyl, N(lower alkyl2)C(O)- lower alkyl, lower alkoxy, hydroxy-lower alkyl-oxetanyl- lower alkyl, oxo-tetrahydrofuranyl, tetrahydrofuranyl-lower alkyl, hydroxy-fluoro-lower alkyl, tetrahydrofuranyl, phenyl and thiazolyl or pyridine, or R7 and R8 together with a nitrogen atom with which they are bonded form a heterocyclyl selected from a group consisting of pyrrolidinyl, azetidinyl, morpholinyl, 5,6-dihydro-8H-[1,2,4]triazolo[4,3-a]pyrazinyl, 3,4-dihydro- 1H-pyrrolo[1,2-a]pyrazinyl, 2-oxa-6-aza-spiro[3.3]heptyl, 5,6-dihydro- 8H-imidazo[1,2-a]pyrazinyl, [1,4]oxazepanyl, piperazinyl, thiomorpholinyl and 2-oxa-5-aza-bicyclo[2.2.1]heptyl, where the heterocyclyl is optionally substituted with 1 or 2 substitutes independently selected from a group consisting of halogen, lower alkyl, lower alkyl-C(O), lower alkoxy-lower alkyl, oxo, hydroxy, hydroxy-lower alkyl, N(lower alkyl2); R9 is lower alkyl; R10 and R11 together with a nitrogen atom with which they are bonded form a heterocyclyl selected from a group consisting of piperidinyl, morpholinyl. The invention also relates to a pharmaceutical composition based on the compound of formula (I), a method of treating said pathological conditions and use of the compound of formula (I).
Substituted 6-(1-piperazinyl)-pyridazines as 5-ht6 receptor antagonists Substituted 6-(1-piperazinyl)-pyridazines as 5-ht6 receptor antagonists / 2502734
Invention relates to novel substituted 6-(1-piperazinyl)-pyridazines of formula , where R1 is chlorine, trifluoromethyl or cyano; R2 is phenyl or phenyl substituted with a halogen; R*1 is hydrogen, C1-4-alkyl or pyridinylmethyl; X is -O-, -NH-, -CH2-, -CH(OH)-, -SO2-, -CO-, -NH-CH2-, -O-CH2-, 1,2-ethendiyl or ethyndiyl; or a pharmaceutically acceptable addition salt or solvate thereof as well as pharmaceutical compositions containing said novel compound as an active ingredient.
Method of treating spasticity accompanied by improved consciousness in patients in vegetative state Method of treating spasticity accompanied by improved consciousness in patients in vegetative state / 2502503
Invention refers to medicine, namely to neurology, and may be used for treating spasticity accompanied by improved consciousness in the patients in the vegetative state. That is ensured by administering Xeomin (botulinumtoxinA free from complexing proteins) into the spastic muscles of all the extremities and related body segments regardless of the contractions in total dose of 400-1300 units. The dose shall not exceed 24 unit/kg of body weight in 1-3 stages. The stages follow at least every 3 days. Every 1-day stage involves administering 5-50 units in each accessible muscle or muscle group with the maximum tone in max. total dose 500 units dissolved in 12.5 unit/ml. The injections are distributed uniformly along the area without electromyography. The following courses are similar if observing spasticity and/or if clinically reasonable. The length of one course is up to 3 weeks.
Composition for improvement of brain function and method for improvement of brain function Composition for improvement of brain function and method for improvement of brain function / 2501808
Composition for improvement of brain function as active ingredient includes peptide X-Pro-Pro-Leu-Thr-Gln-Thr-Pro-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu-Y (where X is absent or represents He or Asn-Ile; and Y is absent or represents Val-Met), peptide X-Val-Val-Val-Pro-Pro-Phe-Leu-Gln-Pro-Glu-Y (where X is absent or represents Thr-Gln-Thr-Pro, Pro-Leu-Thr-Gln-Thr-Pro, Leu-Thr-Gln-Thr-Pro or Pro; and Y is absent or represents Val-Met) or their salts. Method for improvement of brain function involves introduction of the above peptide or its salt.
Compounds, compositions and methods for treating beta-amyloid diseases and synucleinopathies Compounds, compositions and methods for treating beta-amyloid diseases and synucleinopathies / 2501792
Invention relates to a compound of formula or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition for treating β-amyloid diseases and synucleinopathies, based on said compound.
(3-arylsulphonyl quinolin-8-yl-dialkyl-amines - selective serotonin 5-ht<sub>6</sub> receptor antagonists, methods for production and use thereof (3-arylsulphonyl quinolin-8-yl-dialkyl-amines - selective serotonin 5-ht6 receptor antagonists, methods for production and use thereof / 2500672
Invention relates to novel (3-arylsulphonyl quinolin-8-yl-dialkyl-amines of general formula 1 and pharmaceutically acceptable salts thereof, which are selective antagonists of serotonin 5-HT6 receptors. The compounds can be used as an active ingredient in pharmaceutical compositions and medicinal agents for treating diseases of the central nervous system, pathogenesis of which is associated with 5-HT6 receptors. In particular, the compounds can be used in case of neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, Huntington's disease, in anxiety or cognitive disorders and for enhancing mental capabilities. In general formula 1 , Ar is phenyl, optionally substituted in position 3 with a halogen atom, or naphthyl, R1 and R2 are an unsubstituted methyl or ethyl.
Agent of hindu lotos seed (nelumbo nucifera) extract possessing anxiolytic and antidepressive action Agent of hindu lotos seed (nelumbo nucifera) extract possessing anxiolytic and antidepressive action / 2497538
Invention refers to pharmaceutical industry, namely preparing an agent of hindu lotus seed extract (Nelumbo nucifera) possessing anxiolytic and antidepressive action. The agent possessing anxiolytic and antidepressive action prepared by extraction of hindu lotus seed extract (Nelumbo nucifera) in 50% ethanol in a Soxhlet extraction apparatus in the specific proportions.
Imidazo[1,2-b]pyridazine compounds (versions), method for preparing imidazo[1,2-b]pyridazine compounds (versions), pharmaceutical composition and drug preparation for treating and/or preventing diseases related to gaba receptor inhibition Imidazo[1,2-b]pyridazine compounds (versions), method for preparing imidazo[1,2-b]pyridazine compounds (versions), pharmaceutical composition and drug preparation for treating and/or preventing diseases related to gaba receptor inhibition / 2486188
Present invention provides new imidazo[1,2-b]pyridazine compounds covered by general structural formula (I) wherein the radicals and symbols have the values presented in the patent claim, and pharmaceutically acceptable salts thereof. The compounds of structural formula (I) are effective both for treating or preventing the diseases related to GABA receptor inhibition, anxiety, epilepsy, sleep disorders, including insomnia, and for inducing a sedative-hypnotic, anaesthetic effect, sleep and muscle relaxation.
3-phenylpyrazolo[5,1-b]thiazole derivative 3-phenylpyrazolo[5,1-b]thiazole derivative / 2482120
Invention refers to compounds of formula (I) and salts thereof wherein R1 represents -A11-A12-; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 3,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl containing methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine. Also, the invention also refers to a pharmaceutical composition possessing corticotrophin-releasing factor (CRF) receptor antagonist activity, containing a compound of formula (I), to a therapeutic/preventive agent, and a method of treating the diseases specified in the patent claim.
Amide derivative and pharmaceutical composition containing said derivative Amide derivative and pharmaceutical composition containing said derivative / 2481343
Invention relates to a compound of formula (1), in which Ar is a group of formula (Ar-1) or (Ar-2), in which R1 is a halogen, R2 is hydrogen, R3 is hydrogen, R4 is hydrogen, alkyl or alkenyl, X is a nitrogen atom or CH, R5 and R6 are each hydrogen and h equals 1; 1 equals 1 or 2; m equals 1 or 2; n equals 0, 1 or 2; o equals an integer from 0 to 3, under the condition that n and o are equal to 0 at the same time. Values of group A are as given in claim 1 of the invention. Described also is a pharmaceutical composition having agonistic activity with respect to 7 serotonin (5-HT4-receptors), which contains a compound of formula (1) and an agent which stimulates enterokinesis or improves functioning of the alimentary canal, which contains a compound of formula (1) as an active ingredient.
Halogenised pyrazolo[1,5-a]pyrimidines (versions), methods for preparing them, based pharmaceutical composition, intermediate compounds and method for preparing them (versions) Halogenised pyrazolo[1,5-a]pyrimidines (versions), methods for preparing them, based pharmaceutical composition, intermediate compounds and method for preparing them (versions) / 2478101
Invention refers to new halogenised pyrazolo[1,5-a]-pyrimidines of general formula (I) and their pharmaceutically acceptable salts possessing affinity with respect to α1-,α2 subunits of a GABAA receptor. In formula R represents alkyl(C1-C6); R1 is specified in a group consisting of alkyl(C1-C6) and alkinyl(C1-C6); X represents a halogen atom, and Y is specified in a group consisting of -CO- and -SO2. The invention refers to intermediate enamine compounds and methods for preparing them.
Solid forms containing (-)-o-desmethylvenlafaxine and use thereof Solid forms containing (-)-o-desmethylvenlafaxine and use thereof / 2477269
Invention relates to a novel crystalline form of desmethylvenlafaxine of formula in form of a hydrochloride salt of a stereomerically pure compound which is suitable for treating, preventing or managing a disease selected from depression, pain, anxiety, incontinence or vasomotor symptoms caused by menopause. The crystalline form contains water in amount of about 4% to about 8% of the total weight of the sample, and molar ratio of the water to the hydrochloride salt is about 1:1, and the crystalline form has X-ray powder diffraction peaks at positions of about 12.7, 14.5, 19.1, 21.4, 23.0, 25.5 and 27.3°2θ, and is characterised by the following corresponding unit cell parameters measured at 150 K: a=6.78 A; b=9.29 A; c=27.65 A; α=90°; β=90°; γ=90°. The crystalline form is characterised by weight loss during thermal gravimetric analysis of about 4% to about 8%, primarily about 5.6% of the total weight of the sample when heated from about 25°C to about 110°C and endothermic effect during differential scanning calorimetry with onset temperature of the effect of about 50°C to about 125°C, primarily about 93°C. The crystalline form is non-hygroscopic at relative humidity from about 5% to about 85% and absolute form.

FIELD: medicine.

SUBSTANCE: what is described is N-(4-acetoxybenzoyl)glycine lithium salt of formula I: .

EFFECT: higher tranquilising and nootropic action.

4 tbl, 5 ex

 

The invention relates to new water-soluble lithium salts derived glycine (aminoacetic acid) with 4-hydroxybenzoic acid and its application as trankviliziruyuschego and nootropic drugs.

Reference that is used to recover violations of intellectual functions in patients with disorders of cerebral circulation, is pyracetam (2-oxo-1-, CAS 932-17-2). The disadvantage of pyracetam as a reference preparation is its low activity: the level of effective doses of the action is 200-500 mg/kg, the effect of pyracetam often poorly reproducible. Another drug, "Mexidol" (etilmetilgidroksipiridina succinate) shows , , anxiolytic, , , alcohol, and anticonvulsant activity etc. However, lethal dose of Mexidol, causes the death of 50% of the animals (LD 50 ) in rats is 820 (625 to 1025) mg/kg for mice 475 (365 to 617) mg/kg, while the inside is more than 3000 mg/kg in rats and 2010 (1608 to 2513) mg/kg in mice. Therapeutic index, calculated by the ratio LD 50 /ED 50 is 16,4 [Voronin, T.A. Domestic preparation of a new generation of Mexidol: the main effects mechanism of action, application. - M: 2004. - 248 S.].

Derivatives of 4- acid (parabens) used in industry as preservatives (, E-214, CAS 120-47-8, propylparaben, E-216, CAS 94-13-3), (2-()ether ethyl 3-amino-4- acid CAS 499-67-2) mestnoanesteziruyuschee [Register of medicines in Russia RLS drug encyclopedia. - 18-th vol./CH. amended .. vyshkovsky. - M: radar-MEDIA, 2009. - .681], nifuroxazide (hydrazide [(5-nitro-2-)methylene]-4-hydroxybenzoic acid) - antibacterial - blocks dehydrogenase and depresses the respiratory chain, the tricarboxylic acid cycle and a number of other biochemical processes in the microbial cell, destroys microbial wall or cytoplasmic membrane, reduces production of toxins microorganisms [Mashkovsky, PPM Medicines: manual for physicians. - T.1. - M: a New wave. - 2002. - .167]. Glycine (aminoacetic acid CAS 56-40-6) as a tool that improves mental performance and reduces emotional stress [Mashkovsky, PPM Medicines: manual for physicians. - Vol.2. - M: a New wave. - 2002. - P.124]. Lithium carbonate () used in manic phase and for the prevention of exacerbations of bipolar affective disorder, disorder, manic States of various origins, affective disorders in chronic alcoholism, drug addiction, sexual deviations, Meniere's syndrome, migraine [Mashkovsky, PPM Medicinal products: a manual for physicians. - T.1. - M: a New wave. - 2002. - .108].

The purpose of the invention consists in obtaining of highly water-soluble derivative of glycine and 4-hydroxybenzoic acid, which combines the main effects inherent in tranquilizing and neuroprotective means and is characterized by low toxicity and acting in small doses.

Summary of the invention consists in the synthesis of N-(4-) lithium formula

and use it as trankviliziruyuschego and nootropic drugs.

In studies trankviliziruyuschego and nootropic effect compounds were used doses of 10 and 50 mg/kg dissolved in izotonicescom 0.9% NaCl at room temperature. Substance is introduced once for 60 minutes before the start of the experiment. Research results subjected to statistical analysis, the significance of differences was estimated with the help of student's criterion adjusted Б.

Example 1. Lithium salt N-(4-)glycine. In the reactor, supplied with a mixer, put glycine and 50 ml DMF. Dropwise poured acid chloride 4-acetoxybenzoic acid within 1.5 hours. The reaction is carried out at cooling 1.5 hours. Then the reaction mixture was stirred for another 2.5 hours (refrigeration), controlling the pH of the medium (pH>7). To maintain protection type 6 n solution of potassium hydroxide. The resulting mixture was poured into ice and acidified with hydrochloric acid to pH=5, loose crystals of N-(4-)glycine filtered and dried. Exit 73%. T p =194-197°C, Rf 0,569 (butanol-1). M+ 237 (mass-spectrometer «Saturn-2100», Varian). Then the resulting N-(4-)glycine mixed with lithium (molar ratio 1:1) in the environment of benzene and toluene or at hashing is heated at a temperature of 100 C for 60 minutes. After cooling, the product separate filtering, washed with a small amount of solvent and dry. Get a white crystalline solid (22,2 g 97%), with a melting point above 270 degrees C, Rf 0,654 (n-propanol: water in a ratio of 7:3). M+ 243. Found: C (54,39%), H (4,09%), Li (2.85 percent), N (Of 5.79%), O (32,88%), calculated: C (54,34%), H (4,15%), Li (2.85 percent), N (USD 5.76%), O (32,90%).

Example 2. Method of the study of spontaneous motor activity to the «open field» (table 1).

This method allows to study the spontaneous locomotor activity, approximately-exploratory behavior and the level of emotional response animals. Within three minutes of observing the animals recorded the following indicators: the number of crossing squares (vertical activity), the number of on his hind legs and in the hole (approximately research activity), a number of outputs in the Central zone, the number of acts of grooming and the number of fecal bolus (emotional factor).

Example 3. A method of studying nootropic activity elaboration of the conditional reaction of passive avoidance (passive avoidance reaction).

For the study of nootropic activity compounds have used the methodology of elaboration of passive avoidance reaction. In this work, we used a modification of this technique, which was specially developed for the rats. Production of conditional reaction of avoidance of darkened compartment produced in the experimental chamber, which consisted of two adjoining compartments, large illuminated (60 x 40 cm) and a small dark (15 x 15 cm), with electrode floors. Rat was considered as trained if within 30 seconds after the training session, she had not walked in the dark compartment of the experimental chamber. Test playback memorial trail was carried out 24 hours after the study. The animal is placed in a compartment light camera and within 3 minutes to register 3 indicators: the latent period of the first entry in the dark compartment, the number of calls and total time spent in a dark cell. effect of the analyte of interest was expressed in increase of latency period of the first approach, the animal in the dark compartment, reducing the number of calls into the Bay and time of stay in it in comparison with the animals of the control group (table 3).

Example 4. The method of determining the anxiolytic effect plus - maze.

The method allows to estimate anxiolytic (, antifobicescoe) effect of psychotropic agents. Labyrinth lifted over level of the floor to a height of 70 cm and is a square pad (10 x 10 cm) with four crosswise located sleeves length of 50 cm and a width of 10 see Two sleeves are opaque fence height 40 cm, two arms are open. A rat is placed on the Central site of the maze tail to the experimenter. Within 2 minutes of observation recorded the number of visits to the open arms and the time spent in them. Increase in the number of outputs in the open arms and time of stays there, as compared to those values in the control group was assessed as a manifestation of anxiolytic () actions substances (table 2).

Example 5. Determination of acute toxicity. Acute daily toxicity after acute administration was studied in mice-female weight 25-30 Connection, in izotonicescom solution of sodium chloride animals were injected intraperitoneally in a variety of increasing doses once. Observation of animals was performed during the day, noting the number of stranded animals. Calculation LD 50 carried out by the method of Litchfield and Wilcoxon signed. Studies of acute toxicity of the proposed derivative showed that the hazard classification (harm) substances N-(4-) lithium at intraperitoneal mice belong to the class of low-toxic compounds [, I.V. Criterion of harmfulness in hygiene and toxicology when assessing the danger of chemical compounds / IV , I.P. Ulanova. - M: Medicine, 1975 - 328 S.] (table 4).

Thus, production of N-(4-) lithium dose of 10 mg/kg resulted in the manifestation expressed antiamnestic activity in the test passive avoidance reaction, which was accompanied by the increase of the latent period of the call in the dark compartment and the reduction of residence time in the dark compartment and effect ó in increasing the time of stay in the open sleeves in the test elevated plus-maze». These effects were accompanied by a reduction in acts of grooming in the «open field»test that confirms the anti-anxiety effect of N-(4-) lithium. Increasing doses up to 50 mg/kg resulted in the elimination of antiamnestic activity of this compound, while maintaining a clear trend to the manifestation of antiamnesic effect, strengthen the research and motor activity of the animals in the open field test» and the emergence of weak activity in the test «+labyrinth».

From a comparison of doses, in which the N-(4-) lithium (lithium salt N-(4-)glycine) shows and nootropic properties (10 mg/kg) with LD 50 (3751,11 mg/kg), one can conclude that the drug has a wide range of therapeutic action and low toxicity.

Table 4

Comparative characteristics of effective N-(4-) lithium with Mexidol

LD 50 , mg/kg

Therapeutic index

N-(4-) lithium (intraperitoneally)

3751,11,400* (3638,84 to 3866,85)

375,1 475

Mexidol (intraperitoneally)

(365 to 617)

16,4 Attitude 14,42

* - the data are statistically valid, student's criterion adjusted Б, p<0.05

Water soluble lithium salt N-(4-)glycine formula

with tranquilizing and nootropic effects.

 

© 2013-2014 Russian business network RussianPatents.com - Special Russian commercial information project for world wide. Foreign filing in English.