Pharmaceutical composition based on ladasten

FIELD: medicine.

SUBSTANCE: invention relates to field of medicine, in particular to pharmaceutics, and concerns pharmaceutical compositions, which contain as active substance therapeutically effective quantity of ladasten, and as target additives - starch, stearic acid and/or its salt or ludipress and stearic acid and/or its salt with definite ratio of said components. Composition is made in form of pills, contains optimal quantity of target additives, which allows to obtain easy swallowed pills. Pills meet all requirements of State Pharmacopoeia XI edition.

EFFECT: medication form easily releases active substance, which provides its high bioaccessibility.

13 cl, 1 tbl, 5 ex

 

The invention relates to medicine, in particular to the pharmaceutical industry, specifically to drug Ladasten (N-(adamant-2-yl)-N-(para-bromophenyl)amine), another name - bromantan. Ladasten - the original drug, showing anxiolytic activity (patent RF 2175229, "Anxiolytic agent", Seredenin S.B., Yarkova M.A., Modestov B.A., Pyatin BM, Avdonina NI and others, Bulletin of inventions No. 30, 2001). Anxiolytic effect of ladasten is clearly seen in the spectrum of its psychotropic activity, which distinguishes this drug is known as psychostimulants (amphetamine, sidnokarb), and from the typical tranquilizers (diazepam, phenazepam, alprazolam), and allows to characterize it as a psychotropic drug new type that combines the stimulating and anxiolytic effects.

Along with this ladasten has a psychoactive effect, which increases the body's resistance to the effects of adverse environmental factors and activities (USSR author's certificate No. 860446, "Substituted N-adamantylamine manifesting stimulating activity", Valdman A.V., Zaitsev NM, Klimova N.V., Ivanov L.N., Morozov I.S. and others, Bulletin of inventions No. 43-44, 1993 // frost I.S., Whitecrow, Chassereau in the book. "Pharmacology of adamantanes", Volgograd, 2001, s FF.). Unlike psychostimulant the Directors fenomenologia type, ladasten does not cause euphoria and disorders playback fine motor skills of operators, accelerate recovery after exercise. Ladasten exhibit low toxicity, is of great therapeutic breadth.

Previously it was found that this drug has immunostimulatory effects (patent USSR No. 1826906, "Immunostimulatory agent bromantan", Morozov I.S., Artsimovich N.G., Fadeyeva T.A., Klimova N.V., Galushin FORCE and others, Bulletin of inventions No. 25, 1993). Were marked its pharmacological properties, leading to the restoration of the functional activity of the nervous, hormonal and immune systems of the body, and an obstacle to the development of secondary immunodeficiency States of various etiologies (Artsimovich N.G., Galushin T.S., Fadeyeva T.A. "Adamantanes - medicine of the XXI century". International Journal on Immunorehabilitation, 2000, V.2, No. 1, R).

The positive results of the use of this drug in the treatment of chronic fatigue syndrome (Artsimovich N.G., Galushin FORCE, in kN. "Chronic fatigue syndrome", Moscow, Scientific world, 2002, p.172, s).

For the study of the specific pharmacological activity of this drug was formerly created tableted dosage form comprising 50 mg of active substance, and the target additives, starch, sugar, stearic acid, washes the VA to cover core ascensional shell - sugar, gelatin, polyvinylpyrrolidone, glycerin, calcium carbonate precipitated, tartrazine (Kislyak N.A. dissertation, "Creating solid dosage forms derivatives of adamantane", Moscow, 1989).

The disadvantages of the proposed dosage form was the use of the suspension membrane, which reduces the bioavailability of the active substance and complicated technological process of manufacture, in addition, the use of sugar in the core tablet and the shell has created an obstacle to the appointment of the drug to patients with diabetes mellitus.

The essence of the present invention is to provide pharmaceutical compositions on the basis of ladasten, not containing sugar, for the manufacture of dosage forms without a shell having a high biological availability that meets all the requirements of the State Pharmacopoeia XI edition. Two options were developed composition.

The pharmaceutical composition is made in a solid form, in the form of a granular mass containing 0.05-0.20 g ladasten. Mass for solid dosage forms may be obtained from the compositions of this invention in any suitable way. The pharmaceutical composition of the present invention are obtained by wet granulation and direct compression of the various components.

First, anxio itihasa, psychostimulant and immunotropic pharmaceutical composition based ladasten contains a therapeutically effective amount of the active substance and additives target, in which the use of starch, stearic acid and/or its salts in the following ratio, wt.%:

Ladasten33,3-50,0
Stearic acid and/or its salts1-1,3
Starchrest

The starch is preferably used potato and/or corn, as well as salts of stearic acid is predominantly magnesium stearate.

The pharmaceutical composition is made in a solid form, mostly in the form of tablets containing 0,050-0,200 g ladasten.

Tablets produced by wet granulation.

The following examples illustrate a first variant of the pharmaceutical composition.

Example 1. Mix pre-sifted powders ladasten 50.0 g (to 50.0 wt.%), dry potato starch 45,5 g and mix thoroughly, then moisten the mixture with a 7.5%aqueous starch paste (3.5 g starch), then the wetted mass granularit and dried to a residual authority the activity of 2.5-3.5%. The dried granules are milled in a ball mill. Dry granules optivault 1.0 g (1.0 wt.%) magnesium stearate. Get tablets containing ladasten of 0.05, Raspadaemost - 6-7 minutes. The obtained tablets meet the requirements of the State Pharmacopoeia (see table).

Example 2. Obtaining tablets ladasten carried out as in example 1 on the basis of 50.0 g (33.3 wt.%) ladasten, 91,0 g of dry potato starch, 7.5 per cent starch paste (7.0 g starch) and 2.0 g (1.3 wt.%) magnesium stearate. Get tablets containing ladasten 0.05 g and raspadaemost 6-8 min, meets all regulatory requirements (see table).

Example 3. Obtaining tablets ladasten carried out as in example 1 on the basis of 100.0 g of ladasten, 91,0 g of dry potato starch, 7.5 per cent starch paste (7.0 g starch) and 2.0 g of magnesium stearate. Get tablets containing ladasten 0.1 g and raspadaemost 6-8 min, meets all regulatory requirements (see table).

Example 4. Obtaining tablets ladasten carried out as in example 1 on the basis of 100.0 g of ladasten, 182,0 g of dry potato starch, 7.5 per cent starch paste (14.0 g of starch) and 4.0 g of magnesium stearate. Get tablets containing ladasten 0.1 g and raspadaemost 6-8 min, meets all regulatory requirements (see table).

Example 5. Obtaining tablets ladasten carried out as in example 1 based on the C 200,0 g ladasten, 182,0 g of dry potato starch, 7.5 per cent starch paste (14.0 g of starch) and 4.0 g of magnesium stearate. Get tablets containing ladasten 0.2 g and raspadaemost 6-7 min, meets all regulatory requirements (see table).

The second option, the pharmaceutical compositions on the basis of ladasten containing a therapeutically effective amount of the active substance and the target additives, which are used ludipress, stearic acid and/or its salts in the following ratio, wt.%:

Ladasten20,0-28,6
Stearic acid and/or its salts1,0
Ludipressrest

The pharmaceutical composition is made in a solid form, mainly in the form of tablets containing 0.05-0.10 g ladasten.

Tablets produced by direct pressing, mixing all the ingredients in a suitable mixer.

Example 1. In a clean, dry mixer sequentially load pre-sifted powder 50.0 g (of 28.6 wt.%) ladasten, 123,25 g ludipress and 1.75 g (1.0 wt.%) the stearate. The mass is stirred and pressed into tablets containing ladasten of 0.05, Raspadaemost obtained tablets 3-4 minutes, that meets regulatory requirements (see table).

Example 2. Obtaining tablets ladasten carried out as in example 1 on the basis of 50.0 g (25,0 wt.%) ladasten, 148,0 g ludipress and 2.0 (1.0 wt.%) the stearate. Get ladasten pills with a content of 0.05 g of the active substance, raspadaemost 4-5 minutes, meet regulatory requirements (see table).

Example 3. Obtaining tablets ladasten carried out as in example 1 on the basis of 100.0 g (20.0 wt.%) ladasten, 395,0 g ludipress and 5 g (1.0 wt.%) the stearate. Get tablets ladasten content 0,100 g of the active substance, raspadaemost 4-3 minutes, meet regulatory requirements (see table)

Table
The TECHNOLOGICAL characteristics of the SUBSTANCE LADASTEN
IndexThe value of the index
Flowability, g/s0
Bulk density, g/cm30,465±0,025
The compressibility, N.67,03±5,34
Density, g/cm31,26±0,4

IndexThe value of the index
Flowability, g/s10,0±0,5
Bulk density, g/cm30,468±0,032
The compressibility, N.83,5±10,5

TECHNOLOGICAL characteristics of PHARMACEUTICAL COMPOSITIONS CONTAINING LADASTEN, USING as a "CARRIER" - LUDIPRESS
IndexThe value of the index
Flowability, g/s9,8±0,4
Bulk density, g/cm30,47±0,05
The compressibility, N.of 84.8±to 9.32

Characteristics of the FINISHED TABLETS LADASTEN OBTAINED by WET GRANULATION
IndexThe value of the index
Raspadaemost, minnot more than 15
Compressive strength, N63,77±1,9
Abrasion, %the 96.3±0,8

Characteristics of the FINISHED TABLETS LADASTEN, OBTAINED by DIRECT PRESSING
IndexThe value of the index
Raspadaemost, minnot more than 15
Compressive strength, N47,81±1,5
Abrasion, %of 99.7±0,6

1. Pharmaceutical composition with anxiolytic, stimulating and immunotropic effect, on the basis of ladasten, comprising as active ingredient a therapeutically effective amount of ladasten, and as an excipient is starch, stearic acid and/or its salt in the following ratio, wt.%:

Ladasten33,3-50,0
Stearic acid and/or its saltStarchRest

2. The pharmaceutical composition according to claim 1, characterized in that the starch it contains potato starch.

3. The pharmaceutical composition according to claim 1, characterized in that as the salt of stearic acid is used primarily magnesium salt.

4. The pharmaceutical composition according to claim 1, characterized in that it is made mostly in the form of solid dosage forms.

5. Tablets with anxiolytic, stimulating and immunotropic activity that contains, wt%:

Ladasten33,3-50,0
Stearic acid and/or its salt1,0-1,3
StarchRest

6. Tablets according to claim 5 with a content of active substance from 0.05 to 0.2,

7. Tablets according to claim 5 or 6 with an average weight of 0.1 to 0.4,

8. Pharmaceutical composition with anxiolytic, stimulating and immunotropic action on the basis of ladasten, comprising as active ingredient a therapeutically effective amount of ladasten, and as excipients - ludipress, stearic acid and/or with the ü in the following ratio of components, wt.%:

Ladasten20,0-28,6
Stearic acid and/or its salt1,0
LudipressRest

9. The pharmaceutical composition of claim 8, characterized in that as the salt of stearic acid is used primarily magnesium salt.

10. The pharmaceutical composition of claim 8, characterized in that it is made mostly in the form of solid dosage forms.

11. Tablets with anxiolytic, stimulating and immunotropic activity that contains, wt%:

Ladasten20,0-28,6
Stearic acid and/or its salt1,0
LudipressRest

12. Pills to claim 11 with a content of active substance from 0.05 to 0.1,

13. Pills to claim 11 or 12 with an average weight from 0,175 0.500,



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention relates to virology, immunology and medicine. The composition contains antigen bound or fused with virus-like particle (VLP), completed with immunostimulating nucleic acid containing at least one unmathylated CpG-sequence and ligand of toll-like receptor (TLR). There are also disclosed vaccine composition and method for potentiating immune response in an animal.

EFFECT: invention can be used for inducing strong antibody and T-cell response and, particularly it is effective in treatment of allergy, tumours and virus chronic diseases, and also other chronic diseases.

25 cl, 12 dwg, 1 tbl, 11 ex

FIELD: medicine.

SUBSTANCE: invention refers to medical products and concerns an ellagic acid composition for immune system enhancement, differing that additionally is contains chitosan beta-1.3/1.6-glucans or oligosaccharides.

EFFECT: offered composition possesses enhanced immunostimulating effect.

3 ex

FIELD: medicine.

SUBSTANCE: invention refers to pharmacology and can be used in veterinary science and medicine for chemotherapy. There is disclosed immunostimulating and antioxidant lithium composition containing lithium ascorbate and lithium aspartate in percentage ratio 50:50.

EFFECT: expansion of the list of low-toxicity immunomodulators applicable for manufacture of drugs.

1 dwg, 2 tbl

FIELD: medicine.

SUBSTANCE: invention concerns medicine, particularly therapy, and can be applied in chronic disease treatment. Method involves causative agent extraction or determination of antibodies to causative agents or extraction of genetic components from blood, body fluid or smear. Treatment is performed by vaccine drugs specific to one or several identified causative agents, additionally immunomodulators are administered.

EFFECT: activated repair processes, arrested development of disease state of organs and systems due to elimination of identified pathogen from organism and to immune correction.

3 cl, 8 ex

FIELD: medicine.

SUBSTANCE: invention concerns medicine, particularly granulocytopoiesis stimulants, radioprotectors and immune stimulants. Under cytostatics effect Cyclophilin A amplifies granulocyte precursor removal from marrowbone and stimulates granulocytopoiesis.

EFFECT: in case of sublethal radiation, cyclophilin A stimulates migration of marrowbone stem elements and participates in recovery of blood cells and immune system, and shows redioprotection properties.

4 dwg, 2 tbl

FIELD: medicine.

SUBSTANCE: medicinal agent contains alpha and/or beta and/or gamma human recombinant interferon, tocopherol acetate or other tocopherol derivatives, ascorbic acid and/or its salts, pantothenic acid or calcium pantothenate, or dexapanthenol, riboflavin or levocarnitine, and orotic acid and/or ornithine or its derivative - citrulline malate, or Glutoxim, antibacterial, antimycotic agents, additives: emulsifiers, stabilisers, preservatives, antioxidants and base. The formulation is suppositories in certain component ratio.

EFFECT: efficiency for severe infectious diseases and mixed infections.

9 cl, 18 ex

FIELD: medicine.

SUBSTANCE: invention concerns medicine, be more specific to oncology, and concerns the substances stimulating maturing of dendritic cells (DC). Application of fucoidan from Fucus evanescens or polysaccharide composition from Fucus evanescens consisting of fucoidan in amount of 60-80% and poly-mannuronic acid in amount of 20-40%, as an agent possessing ability to induce maturing of dendritic cells is offered. The declared fucoidan preparations have a standardised composition and, hence, possess direct biological effect. They keep the properties for long time (3 years).

EFFECT: increase of DC functional activity under the influence of the declared substances.

8 dwg

FIELD: medicine, veterinary science.

SUBSTANCE: invention concerns veterinary science, in particular, to ways of reception of immunomodulatory and antiseptic compounds for prevention and treatment of infectious diseases of animals. The way of reception of a complex immunotropic antiseptic preparation for prevention and treatment of infectious diseases of animals includes mixing of an amber acid, novocaine, Dorogov's antiseptic-stimulator of the second fraction and formalin in water at a following parity of components, wt %: amber acid 1; DAS №2 4; novocaine 0.25; formalin 0.4; the distilled water - the rest, and sterilisation using autoclave treatment which is performed in a 1 atm regimen. Within 20 minutes. The received compound possesses antiseptic, immunomodulatory and trophicostimulating activity at a parenteral way of introduction.

EFFECT: rising of efficiency of the received preparation at treatment and prevention of infectious diseases of animals.

2 tbl

FIELD: medicine.

SUBSTANCE: invention concerns medicine, namely to creation of immunogene compositions and vaccines for prevention or treatment of the infections caused by Gram-negative bacteria. The immunogene compositions containing a transferrin-binding fiber and Hsf, and a way of their reception are offered. It is shown, that the combination of these two antigens synergically influences on production of antibodies with high activity in the analysis of bactericidal Serum. The composition can be used in vaccines against Gram-negative bacteria, including Neisseria meningitides, Neisseria gonorrhoeae.

EFFECT: creation of immunogene compositions and vaccines for prevention or treatment of the infections caused by Gram-negative bacteria.

56 cl, 10 ex, 1 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention concerns area of medical products, in particular to application of complex bonds of iron (III) with carbohydrates or their derivatives for reception of a medical product for improvement of immune protection and-or activity of a brain at patients without an anaemia caused by deficiency of iron or deficiency of iron in which complex bond of iron (III) is iron (III)-polymaltose complex bond or complex bond of iron (III) with a product of oxidation one or several maltodextrins.

EFFECT: development of preparations for improvement of immune protection and-or activity of a brain at patients without an anaemia caused by deficiency of iron or deficiency of iron.

7 cl, 1 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: invention is related to antagonists of serotonin 5-HT6 receptors of common formula 1 and their pharmaceutically acceptable salts and/or hydrates, pharmaceutical compositions, dosage forms and methods of production. Invention also includes new compounds of formula 1.1. In formulae 1 and 1.1 , Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur and heteroatom; R1 represents atom of hydrogen, unnecessarily substituted C1-C5 alkyl; Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur as heteroatom; R1 represents atom of hydrogen, which is unnecessarily substituted C1-C5 alkyl; R21,R22, R31, R32 independently from each other represent atom of hydrogen or substituent of aminogroup, selected from unnecessarily substituted C1-C4 alkyl, unnecessarily substituted phenyl, or R31 and R32 together with atom of nitrogen, to which they are bound, create unnecessarily substituted saturated 6-member heterocycle, possibly containing atom of nitrogen in cycle; or R1 together with atom of nitrogen, to which it is bound, and R21 and R22 together with atom of nitrogen, to which they are bound, create substituted pyrimidine cycle. In formula 1.1 R4, R5 and R6 independently from each other represent atom of hydrogen, unnecessarily substituted C1-C3 alkyl or phenyl.

EFFECT: compounds of invention may find application for treatment and prevention of development of conditions and disorders of central nervous system.

13 cl, 11 dwg, 4 tbl, 11 ex

FIELD: medicine.

SUBSTANCE: invention is related to new derivatives of common formula (I) , in which: A, if available, means (C1-C6)-alkyl; R1 means group NR6R7, (C4-C7)-azacycloalkyl, (C5-C9)-azabicycloalkyl, besides, these groups, unnecessarily, are substituted with one or more substituents, selected from (C1-C5)-alkyl or halogen; A-R1 is such that nitrogen of radical R1 and nitrogen in position 1 of pyrazole are necessarily separated at least by two atoms of carbon; R3 means radical H, OH, NH2, ORc, NHC(O)Ra or NHSO2Ra; R4 means phenyl or heteroaryl, unnecessarily, substituted with one or more substituents, selected from halogen, CN, NH2, OH, ORc, C(O)NH2, phenyl, polyfluoroalkyl, linear or ramified (C1-C6)-alkyl, besides these substituents, unnecessarily, are substituted with halogen, and moreover, heteroaryl radicals are 3-10-member, containing one or more heteroatoms, selected from sulphur or nitrogen; R5 means radical H, linear or ramified (C1-C6)-alkyl; Ra means linear or ramified (C1-C6)-alkyl; Rc means linear or ramified (C1-C6)-alkyl, (poly)fluoroalkyl or phenyl; R6 and R7, independently from each other, means hydrogen, (C1-C6)-alkyl; R6 and R7 may create 5-, 6- or 7-member saturated or non-saturated cycle, which includes one heteroatom, such as N, and which, unnecessarily, substituted with one or more atoms of halogen; to its racemates, enantiomers, diastereoisomers and their mixtures, to their tautomers and their pharmaceutically acceptable salts, excluding 3-(3-pyridinyl)-1H-pyrazole-1- butanamine, 4-(3-pyridinyl)-1H-pyrazole-1-butanamine and N-(diethyl)-4-phenyl-1H-pyrazole-1-ethylamine. Invention is also related to methods for production of compounds of formula (I) and to pharmaceutical composition intended for treatment of diseases that appear as a result of disfunction of nicotine receptors α7 or favorably responding to their modulation, on the basis of these compounds.

EFFECT: production of new compounds and pharmaceutically acceptable composition on their basis, which may find application in medicine for treatment, prophylaxis, diagnostics and observance over development of psychiatric or neurological disorders or diseases of central nervous system, when cognitive functions deteriorate or quality of sensor information processing drops.

16 cl, 106 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new 2-alkylsufanyl-3-arylsufonyl-cycloalkano[e]pyrazolol[1,5-a]pyrimidines of general formula 1 or 2-alkylsufanyl-3-arylsufonyl-cycloalkano[d]pyrazolo[1,5-a]pyrimidines of general formula 2, which are antagonist of 5-HT6 receptors. In compounds of formula 1

and 2 ,

R1 is a hydrogen atom or C1-C3 alkyl; R2 is C1-C3 alkyl; R3 is a hydrogen atom, one or two optionally identical halogen atoms, C1-C3 alkyl or hydroxyl, optionally substituted with C1-C3 alkyl; n is an integer equal to 1, 2 or 3.

EFFECT: compounds can be used in preventing and treating diseases of the central nervous system, anxiolytics and as compounds with nootropic effect and suitable for enhancing memory.

12 cl, 1 dwg, 4 tbl, 9 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to ligand with a wide range of simultaneous receptor activity towards adrenergic α1A, α1B , α1D, α1A, α2A, β2, dopamine D1, D21, D2S, D3, serotonin 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5- HT7, sigma α1, α2 receptors, to calcium and sodium channels, monoamine transporters [norepinephrine (NET) and dopamine (DAT)], which is 3-methyl-9-benzyl-1,2,3,4-tetrahydrocarbonyl naphthalene-1,5-disulphonate of formula 1:

. The invention also relates to a pharmaceutical composition, which has a medicinal origin, which is a ligand of formula 1 with the given range of simultaneous receptor activity for preventing and/or treating diseases of the central nervous system, pathogenesis of which is related to GPCR receptors, ion channels and monoamine transporters, method of preparing said composition, and to medicinal agents.

EFFECT: range of simultaneous activity towards said receptors increases capacity and effectiveness of using the said ligand.

10 cl, 10 dwg, 7 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I), their R and S isomers; or a mixture of R and S isomers; or pharmaceutically acceptable salts. Disclosed compounds can be used as a medicinal agent with agonist properties towards PPAR. In formula (I) and L represents (II) or (III); R1, R2, R3, Ya, R4a, R", Yb, R4b are hydrogen; R and R' are independently hydrogen, C1-C4alkoxy; n equals 0, 1 or 2; m equals 0, 1 or 2; X1 is a -Z-(CH2)P-Q-W group; X2 is -CH2-, -C(CH3)2-, -O- or -S-.

EFFECT: invention relates to a pharmaceutical composition, which contains the disclosed compound, to use of the pharmaceutical composition as a medicinal agent, to use of the disclosed compound in making the pharmaceutical composition.

13 cl, 35 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to a compound of formula: which is N-{2-tert-butyl-1-[(4,4-diflurocyclohexyl)methyl]-1H-benzimidazol-5-yl}ethanesulfonamide and its pharmaceutically acceptable salt, their diastereomers, enantiomers or their mixture. The invention also relates to use of this compound in making a medicinal agent with modulator activity of CB1 receptors; to a pharmaceutical composition based on this compound; to a method of modulating CB1 receptors, based on use of effective quantities of this compound, as well as to a method of producing the compound described above.

EFFECT: obtaining a new derivative of benzimidazole with useful biological activity.

8 cl, 1 tbl, 28 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds of formula , where R1 is -O-X, where X is -(CH2)m-(CR9R10)p-(CH2)n-Z-(CH2)q-W, where m, n and q are independently equal to zero or assume values from 1 to 5; p equals 0 or 1; R9 and R10 are independently hydrogen, hydroxy, halogen, lower alkyl, lower alkoxy or cycloalkyl; or R9 and R10 together represent alkylene, which together with the carbon atom to which the are bonded, form an aryl; Z is a bond or O, W is aryl; R2 is hydrogen; L is a bond; R3 is hydrogen; R4 is hydrogen; R5 and R6 are independently hydrogen; R7 is hydrogen, halogen, hydroxy, trifluromethyl, lower alkyl, lower alkoxy, alkanoyl, alkyloxyalkoxy, alkanoyloxy, amino, alkylamino, dialkylamino, acylamino, carbamoyl, carboxy, alkoxycarbonyl; or R5 and R6 together represent -(CH2)1-2-; Y is -(CH2)r-, -O-(CH2)r, -(CH2)r-O-, where r equals zero or assumes values from 1 to 3; Q together with atoms to which it is bonded form an aryl, pyridyl, pyrimidinyl, thienyl, furyl, pyrroliyl or indolyl ring; or to its pharmaceutically acceptable salts. The invention also relates to a method of inhibiting rennin activity in mammals, to a pharmaceutical composition, as well as to application.

EFFECT: obtaining new biologically active compounds with inhibitory activity towards renin.

23 cl, 52 ex

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds of formula (I) and their pharmaceutically acceptable salts with antagonistic properties towards adenosine A2A receptor, which can be used for treating central nervous system diseases such as Parkinson's disease. In general formula (I) , R is ,, R1, R2, R3, R4 and R5 is independently selected from a group which consists of hydrogen; R6 is hydrogen, (C1-C6)alkyl or -CH2F; R7, R8 and R9 are independently selected from a group which consists of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, haloid and -CF3; Z is R10-phenyl, R10-5-6-member heteroaryl, which contains 1 or 2 hetwroatoms, selected from nitrogen or from nitrogen and oxygen, possibly condensed with a benzene ring, or ; R10 represents 1 to 3 substitutes, independently selected from a group which consists of hydrogen, (C1-C6)-alkyl, hydroxy, (C1-C6)-alkoxy, hydroxy-(C1-C6)-alkyl, hydroxy-(C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C1-C6)-alkoxy-(C1-C6)-alkoxy, (C1-C6)-alkoxy-(C1-C6)-alkoxy-(C1-C6)-alkyl, (di-(C1-C6)-alkoxy)-(C1-C6)-alkyl, (hydroxy)-(C1-C6)-alkoxy-(C1-C6)-alkyl, (C3-C6)-cycloalkyloxy, (C3-C6)-cycloalkyl-O-(C3-C6)-alkoxy, (C1-C6)-alkyl-SO2-, (C1-C6)-alkyl-SO-, haloid, -CN, cyano-(C1-C6)-alkyl, -CHF2, -CF3, -C(O)R13, -C(O)O-(C1-C6)-alkyl, -N(R11)(R12), N(R11)(R12)- (C1-C6)-alkyl, - C(O)N(R13)(R16), R11-5-6-member nitrogen-containing heteroaryl, possibly condensed with a benzene ring, R15-5-6-member heterocycoalkyl, with 1 or 2 heteroatoms selected from nitrogen and oxygen, R15-5-6-member heterocycloalkyl-(C1-C6)-alkyl, with 1 or 2 heteroatoms selected from nitrogen and oxygen, R15-5-6-member heterocycloalkyl-(C1-C6)-alkoxy, with 1 or 2 heteroatoms selected from nitrogen and oxygen, R15-5-6-member heterocycloalkyl-oxy, with 1 or 2 heteroatoms in a heterocyclic ring selected from nitrogen and oxygen, CF3-(C1-C4)alkylene-O-(C1-C6)alkyl, CF3-hydroxy(C1-C6)alkyl, cyano-(C1-C6)-alkoxy, (C1-C4)alkylene-C(O)-O-(C1-C6)alkyl, -SO2-N((C1-C4)alkyl)2, ((C3-C4)cycloalkyl)hydroxy(C1-C6)alkyl, (hydroxy(C1-C6)alkyl)-(C1-C4)alkoxy, (dihydroxy)-(C1-C6)-alkyl, (dihydroxy)(C1-C6)alkoxy, -C(=NOR17)- (C1-C6)alkyl and -C(=NOR17)-CF3; or two R10 groups, on neighbouring carbon atoms of the ring, together form -O-CH2-O-, -O-(CH2)2-O-, -CH2-O(CH2)2-O-, -O-(CH2)2-, -(CH2)3-O-, -O-(CH2)3-O, -(CH2)3-, where the ring, formed by two R10 substitutes and ring carbon atoms with which they are bonded, is substituted with R16; or two R10 groups on neighbouring ring carbon atoms, together form -O(CH2)3CH((OR18)-, each R11 is independently selected from a group which consists of hydrogen and (C1-C6)alkyl; each R12 is independently selected from a group which consists of (C1-C6)alkyl, hydroxy(C1-C6)alkyl, -C(O)-(C1-C6)alkyl, -C(O)O-(C1-C6)alkyl, ((C1-C6)alkoxy)hydroxy(C1-C6)alkyl, (C1-C6)alkoxy (C1-C6)alkyl-C(O)-, -SO2(C1-C6)alkyl; R13 is hydrogen, (C1-C6)alkyl or -CF3; R14 is (C1-C6)alkoxy-C(O)-; R15 represents 1 to 3 substitutes, independently selected from a group which consists of (C1-C6)alkoxy, hydroxy-(C1-C6)alkyl; or two R15 substitutes, taken together with the carbon atom with which they are bonded, form a -C(=O)- group; R16 is (C1-C6)alkoxy(C1-C6)alkyl, hydroxy or hydroxy(C1-C6)alkyl; R17 is hydrogen or (C1-C6)alkyl. The invention also relates to a pharmaceutical composition based on said compounds.

EFFECT: increased effectiveness of composition and method of treatment.

17 cl, 23 ex

FIELD: medicine.

SUBSTANCE: invention concerns new biologically active compound peptide possessing protective action against Alzheimer's disease of formula Glu-Trp-Asp-Leu-Val-Gly-Ile-Pro-Gly-Lys-Arg-Ser-Glu-Arg-Phe-Tyr-Glu-Cys-Cys-Lys-Glu.

EFFECT: can be used to produce a preparation for immunoprophylaxis of Alzheimer's diseases.

1 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention concerns medicine, particularly therapy and neurology and selection of treatment tactics for chronic cerebral ischemia cases. It involves determination of electrophoretic mobility of erythrocytes. Its rise above 1.26±0.02 indicates preservation of adaptation reserves and suitability of administering adaptogens of herbal origin for activation of stress-realising body systems. Electrophoretic mobility fallen under 1.21±0.012 indicates depletion of body adaptation capacity and suitability of administering neuropeptides of stress-limiting effect.

EFFECT: enhanced treatment efficiency, reduced side effects due to taking individual features of adaptation process into account.

1 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention is related to antagonists of serotonin 5-HT6 receptors of common formula 1 and their pharmaceutically acceptable salts and/or hydrates, pharmaceutical compositions, dosage forms and methods of production. Invention also includes new compounds of formula 1.1. In formulae 1 and 1.1 , Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur and heteroatom; R1 represents atom of hydrogen, unnecessarily substituted C1-C5 alkyl; Ar represents aryl, selected from unnecessarily substituted phenyl or unnecessarily substituted 5-6-member heteroaryl, which contains atom of nitrogen or atom of sulfur as heteroatom; R1 represents atom of hydrogen, which is unnecessarily substituted C1-C5 alkyl; R21,R22, R31, R32 independently from each other represent atom of hydrogen or substituent of aminogroup, selected from unnecessarily substituted C1-C4 alkyl, unnecessarily substituted phenyl, or R31 and R32 together with atom of nitrogen, to which they are bound, create unnecessarily substituted saturated 6-member heterocycle, possibly containing atom of nitrogen in cycle; or R1 together with atom of nitrogen, to which it is bound, and R21 and R22 together with atom of nitrogen, to which they are bound, create substituted pyrimidine cycle. In formula 1.1 R4, R5 and R6 independently from each other represent atom of hydrogen, unnecessarily substituted C1-C3 alkyl or phenyl.

EFFECT: compounds of invention may find application for treatment and prevention of development of conditions and disorders of central nervous system.

13 cl, 11 dwg, 4 tbl, 11 ex

Up!