Means for correction of psychoemotical status of organism based on astragalus herbs extract

FIELD: pharmacology.

SUBSTANCE: means for correction of the psychoemotional status of the organism, with antistress, antidepressant, anxiolytic and nootropic action, which is an aqueous or hydroalcoholic extract of Astragalus vulpinus Willd., containing flavonoids, ascorbic acid, saponins and tannins in a certain quantity.

EFFECT: drug has a pronounced anti-stress, antidepressant, anxiolytic and nootropic effect, restores psychoemotional state of the organism.

5 ex

 



 

Same patents:

FIELD: biotechnology.

SUBSTANCE: biologically active peptide is obtained, which has curative effect against Alzheimer disease, and consisting of the amino acid sequence Ala-Trp-Lys-Val-Leu-Ser-Pro-Gln-Gly-Gly-Gly-Pro-Trp-Asp-Ser-Val-Ala.

EFFECT: invention enables to use the resulting peptide to create a drug effective in the therapy of Alzheimer disease.

1 dwg, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a hexapeptide of formula Thr-Gly-Glu-Asn-His-Arg-NH2, having neuroprotective and nootropic activity. Disclosed novel pharmaceutical composition based on a peptide, which is highly effective in low doses and is used as nasal drops.

EFFECT: high efficiency in preventing and treating neurodegenerative and cerebrovascular diseases.

2 cl, 3 dwg, 6 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel water-soluble potassium salt of N-(4-acetoxybenzoyl)glycine of formula

given below, which possesses cerebroprotective activity.

EFFECT: invention can be used in chemical-pharmaceutical industry for obtaining effective cerebroprotective medications.

2 dwg, 3 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of structural formula

,

having Aβ42 secretion inhibiting activity. In formula I , hetaryl I is a five- or six-member heteroaryl group containing 1-3 heteroatoms selected from O, S or N, hetaryl II is a five- or six-member heteroaryl group containing 1-3 heteroatoms as defined above for hetaryl I, or is a bicyclic ring system containing 1-4 heteroatoms selected from S, O or N, where at least one ring is aromatic by nature, R1 is C1-7-alkyl, C1-7-alkoxy, C1-7-alkyl substituted with a halogen, or a halogen; R2 is a halogen, C1-7-alkyl, C1-7-alkoxy, hydroxy, C1-7-alkyl substituted with a halogen, C1-7-alkyl substituted with a hydroxy, or benzo[1,3]dioxolyl or is -(CHR)p-phenyl, optionally substituted with a halogen, C1-7-alkyl, C1-7-alkoxy, S(O)2-C1-7-alkyl, cyano, nitro, C1-7-alkoxy substituted with a halogen, dimethylamino, -(CH2)p-NHC(O)O-C1-7-alkyl or C1-7-alkyl, substituted with a halogen. The values of radicals R, R3, R4,p, n, m, o are given in the claim.

EFFECT: invention relates to a method of producing said compounds, a medicinal agent containing said compounds and a method of treating Alzheimer's disease, cerebral amyloid angiopathy, Hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), vascular dementia, dementia pugilistica or Down syndrome, associated with β amyloid activity.

21 cl, 283 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine and deals with the application of at least one peptide, selected from the group, including SEFKHG(C), TLHEFRH(C), ILFRHG(C), TSVFRH(C), SQFRHY(C), LMFRHN(C), SPNQFRH(C), ELFKHHL(C), THTDFRH(C), DEHPFRH(C), QSEFKHW(C), ADHDFRH(C), YEFRHAQ(C) and TEFRHKA(C), for the production of a medication for the prevention and/or treating Alzheimer's disease. The group of inventions relates a vaccine, containing at least one said peptide, intended for the induction of immune response aimed against Aβ.

EFFECT: group of invention provides the favourable effect of vaccination with vaccines with mimotopes in the treatment of Alzheimer's disease.

24 cl, 3 ex, 10 dwg, 5 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to biotechnology and immunology. What is presented is a hybridoma cell line FP12H3-C2 deposited under No. DSM ACC2750 producing the anti-beta-amyloid antibody. Presented are methods for preparing an antibody, including a humanised antibody with using a hybridoma line according to the invention, as well as diagnostic techniques for a beta-amyloid associated disease or condition in a patient or a liability to such disease or condition, a method for determining a degree of the tissue involvement into amyloidogenic plaques, a method for monitoring minimal residual signs of the disease into a patient following treating with the antibody or its active fragment, a method for prediction of sensitivity in the patient treated with the antibody or its active fragment.

EFFECT: present invention can find further application in diagnosing and therapy of beta-amyloid related diseases, such as Alzheimer disease.

9 cl, 4 dwg, 5 tbl, 17 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to a pharmaceutical composition based on a compound of formula (I) or its pharmaceutically acceptable salt or solvate. wherein X is S or O, and provided X is S, R1 is OH or NH2; and provided X is O, R1 is OH, NH2 or NHMe. The invention also refers to a compound of formula (I) and a based kit.

EFFECT: there are prepared new imidazolidine derivatives effective in treating prostate cancer.

28 cl, 14 tbl, 14 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical composition for treating insomnia. Said composition includes root of Polygonum multiflorum and/or its extracts, seeds of Ziziphus spinosa and/or its extracts, mulberry fruit and/or its extracts, Ganoderma and/or its extracts, lily bulb and/or its extracts, Anemarrhena rhizome and/or its extracts, root of Salvia miltiorrhiza and/or its extracts, chrysanthemum flower and/or its extracts, Poria and/or its extracts and Albizia flower and/or its extracts. Invention also relates to application of said composition.

EFFECT: claimed invention provides sedative and soporific effect, contributes to memory stimulation.

17 cl, 6 tbl, 14 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of organic chemistry, namely to novel derivatives of pyrazole pyridine of formula , as well as to its tautomers, geometrical isomers, enantiomers, diastereomers, racemates and pharmaceutically acceptable salts, where G1 represents H; G2 represents -CHR1R2; R1 and R2 independently on each other are selected from H; C1C6-alkoxy-C1C6-alkyl; C1-C6-alkyl; optionally substituted phenyl; optionally substituted phenyl-C1-C6-alkyl; optionally substituted morpholine-C1-C6-alkyl; or -CHR1R2 together form a ring, selected from an optionally substituted C3-C8-cycloalkyl and substituted piperidine; G3 is selected from an optionally substituted C1C6-alkoxy -C1-C6-alkyl; C1-C6-alkyl; substituted phenyl; substituted phenyl-C1C6-alkyl; G4 is selected from a substituted acyl-C1C6-alkyl, where acyl represents a group -CO-R and R stands for H or morpholine; optionally substituted C1-C6-alkyl; optionally substituted phenyl or indene; substituted phenyl-C1-C6-alkyl; optionally substituted pyridine- or furanyl-C1C6-alkyl; morpholine- or piperidine-C1-C6-alkyl; G5 represents H; where the term "substituted" stands for the groups, substituted with 1 to 5 substituents, selected from the group, which includes a "C1-C6-alkyl," "morpholine", "C1-C6-alkylphenyl", "di-C1-C6-alkylamino", "acylamino", which stands for the group NRCOR", where R represents H and R" represents a C1-C6-alkyl, "phenyl", "fluorine-substituted phenyl", "C1-C6-alkoxy", "C1-C6-alkoxycarbonyl", "halogen". The invention also relates to a pharmaceutical composition based on the formula (I) compound and particular compounds.

EFFECT: obtained are the novel derivatives of pyrasole pyridine, useful for the treatment and/or prevention of disorders or states, associated with NADPH-oxidase.

12 cl, 3 tbl, 21 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of biochemistry, in particular to cyclic peptide, capable of inducing antibody response. Peptide consists of formula X2X3VGSNK-Z or X3VGSNKG-Z, where X2 represents E, G, Q or K, X3 represents D or N and Z represents agent, stabilising bent, present inside peptide sequence, with peptide being cyclised by covalent bonding of N-end amino acid with Z, where Z represents peptide fragment YNGK. Conjugate, containing said cyclic peptide, conjugated with immunogenic carrier molecule is also claimed. peptide and conjugate, which contains it, can be applied for production of medication or as vaccine against Alzheimer's disease. Methods of obtaining cyclic peptide and conjugate are also claimed.

EFFECT: invention makes it possible to obtain improved, less toxic vaccine against Alzheimer's disease.

8 cl, 11 dwg, 1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine and aims at treating fibromyalgia syndrome. The method of treating fibromyalgia syndrome involves administering a therapeutically effective amount of a substance having structural formula , or its pharmaceutically acceptable salt into a mammal in need thereof, wherein Rx, R1 and R2 represent hydrogen and x is equal to 1. What is also provided is a pharmaceutical composition containing the substance having structural formula (1), or its pharmaceutically acceptable salt.

EFFECT: using the group of inventions provide the effective treatment of fibromyalgia syndrome.

13 cl, 1 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: correcting cognitive disorders in the patients suffering arterial hypertension accompanying type 2 diabetes mellitus is ensured by combining a standard drug therapy with administering the preparation Kudesan 60 mg a day throughout two months.

EFFECT: administering Kudesan in the above dose and regimen provides the effective correction of cognitive disorders in the above group of patients in a combination with improving the cardiovascular function and metabolic processes.

2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: correcting increased levels of anxiety and depression in the patients with arterial hypertension accompanying type 2 diabetes mellitus is ensured by combining a standard drug treatment and administering Kudesan 60 mg a day for two months.

EFFECT: method provides the effective correction of anxiodepressive conditions in the given category of patients that in turn enables normalising blood pressure more effectively by reducing the negative psychosomatic effect.

1 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula I, possessing ability of binding with delta-opioid receptors. In formula R1 is selected from the group, consisting of i) phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxyl, di(C1-4alkyl), aminocarbonyl, chlorine and fluorine, in such a way that only one di(C1-4alkyl)aminocarbonyl is present; ii) naphthyl; iii) pyridinyl, optionally substituted with one substituent, selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxy, fluorine, chlorine and cyano; iv) pyrimidin-5-yl; v) furanyl; vi) thienyl; vii) 5-oxo-4,5-dihydro-[1,2,4]oxodiazol-3-yl; and viii) di(C1-2alkyl)aminocarbonyl; Y represents ethyl, vinyl or bond; or Y represents O, when R1 represents optionally substituted phenyl, where substituent represents C1-4alcoxy; R2 represents phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, fluorine, chlorine and cyano, trifluoromethoxy and hydroxy; or R2 represents phenyl, substituted with one aminocarbonyl, di(C1-4alkyl)aminocarbonyl, C1-4alcoxycarbonyl or carboxysubstituent; R3 is selected from the group, consisting of i) 3-aminocyclohexyl; ii) 4-aminocyclohexyl; iii) piperidin-3-yl; iv) piperidin-4-yl; v) pyrrolodin-2-yl-methyl, in which pyrrolodin-2-yl is optionally substituted by 3-rd or 4-th position with one or two fluorine-substituents; vi) azetidin-3-yl; vii) 2-(N-methylamino)ethyl; viii) 3-hydroxy-2-aminopropyl; ix) piperidin-3-yl-methyl; x) 1-azabicyclo[2.2.2]octan-3-yl; and xi) 8-azabicyclo[3.2.1]octan-3-yl; or R3 together with Ra and nitrogen atom, which they both are bound to, form piperazinyl, optionally substituted with 4-C1-4alkyl; Ra represents hydrogen, 2-(N-methylamino)ethyl or C1-2alkyl, optionally substituted with azetidin-3-yl.

EFFECT: compounds can be used in treatment of pain in the range from medium to strong, caused by diseases or conditions, such as osteoarthritis, migraine, burn, fibromyalgia, cystitis, rhenite, neuropathic pain, idiopathic neuralgia, toothache, etc.

21 cl, 4 tbl, 26 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is a group of inventions concerning a new application of bicyclo[2,2,2]octane-2-carboxylic acid salt. What is presented is using it for treating dysphoria in a person suffering epilepsy for treating alcohol addiction, for reducing the level of hepatic function marker specified in AST (aspartate aminotransferase), ALT (alanine aminotransferase) or bilirubin in the person for reducing an erythrocyte sedimentation rate, as well as for reducing a number or an intensity of epileptic attacks in a daily dose of min 400 mg.

EFFECT: implementing the above applications with no negative effect on patient's behaviour and the functions of the main organs and systems.

19 cl, 6 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts, wherein A is thiazolyl, oxazolyl, thienyl, furyl, imidazolyl, pyrazolyl or oxadiazolyl (structures of which are presented in cl.1 of the patent claim), R1 represents C1-6alkyl; R2 represents (i) phenyl substituted by halogen; C1-6alkyl optionally substituted by morpholine or C1-6dialkylamino; C1-6alkoxy optionally substituted by halogen; or heterocyclyl, wherein a heterocyclyl substitute is specified in morpholine; pyrazolyl optionally substituted by C1-6alkyl; piperidinyl; pyrrolidinyl; oxadiazolyl substituted by C1-6alkyl; furyl substituted by C1-6alkyl; dioxydoisothiazolidinyl; triazolyl; tetrazolyl substituted by C1-6alkyl, tridiazolyl substituted by C1-6alkyl; thiazolyl substituted by C1-6alkyl; pyridyl; or pyrazinyl; (ii) substituted or unsubstituted heterocyclyl specified in quinolinyl; pyridyl substituted by C1-6alkoxy or morpholinyl; or benzo [d] [1, 2, 3] triazolyl substituted by C1-6alkyl; R3 represents phenyl substituted by 2 or 3 substitutes specified in halogen; C1-6alkyl; C1-6alkoxy optionally substituted by halogen; hydroxy group; cyano; or -C(=O)ORa, wherein Ra represents phenyl; R4 represents hydrogen, C1-6alkyl or C1-6halogenalkyl. The invention also refers to a pharmaceutical composition containing the compounds of formula (I), a method for PDE10 inhibition, a method of treating neurological disorders, and to intermediate compounds: 2-(4-chlor-3,5-dimethoxyphenyl)furan and 4-(5-methyl-1,3,4-thiadiazol-2-yl)benzaldehyde.

EFFECT: compounds of formula (I) as PDE10 inhibitors.

39 cl, 13 ex, 2 tbl, 77 dwg

FIELD: medicine.

SUBSTANCE: correcting night eating syndrome in the patients with anxiety and depressive disorders is ensured by prescribing agomelatine 25mg a day for the night. The therapeutic course is continued until a long-lasting remission is observed for 6 months and more.

EFFECT: method enables reducing the intensity of night eating syndrome in the patients with an affective pathology by levelling the anxiety and depressive manifestations with improving the sleep quality and minimum side effects.

2 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to 2-bromo-1-(thietanyl-3)imidazole-4,5-dicarboxylic acid derivatives of formula Ia, b where R is COOK (Ia) or (Ib)

EFFECT: obtaining novel heterocyclic compounds having antidepressant activity.

4 cl, 1 tbl, 5 ex

Antidepressant // 2535027

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine, namely to pharmacology, and deals with a synthetic biologically active compound - hydrochloride of 2-(diethylamino)ethyl ether of 9-hydroxy-9H-fluorene carboxylic acid, representing an amyzilum M-cholinoblocker derivative. The said amyzilum derivative has not been described before. The claimed compound possesses low toxicity, its synthesis is simple and available. It is demonstrated that hydrochloride of 2-(diethylamino)ethyl ether of 9-hydroxy-9H-fluorene carboxylic acid, representing the amyzilum M-cholinoblocker derivative demonstrates an expressed antidepressant activity and an anxiolytic action, possesses a sedative, and in high doses a soporific effect, it also positively influences an exploratory ability and memory. In addition, it has been stated that the claimed pharmacological substance in expressiveness of the antidepressant properties surpasses the widely applied tricyclic antidepressant amitriptylinum. The obtained data make it possible to recommend the claimed amyzilum derivative as the antidepressant for the treatment of depression and anxiety disorders.

EFFECT: invention extends an arsenal of pharmacological means, used as depression therapy.

4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new crystalline forms of acid addition salts of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, wherein the acid is specified in methanesulphonic, maleic, fumaric, citric, orotic, 10-camphor sulphonic acids and fencifose. The salts possess the agonist properties of neuronal nicotine receptor (NNR) and can be used for managing or preventing pain, an inflammation or a CNS disorder. Each of the crystalline salts is characterised by an X-ray powder diffraction diagram. The invention also involves an amorphous form of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine monocitrate and polymorphic forms of the above crystalline salts.

EFFECT: invention refers to a pharmaceutical composition containing an effective amount of the presented salts.

19 cl, 8 dwg, 33 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel heterocyclic compounds of general formula (I) or enantiomers, diastereomers or pharmaceutically acceptable salts thereof, where Y is: phenyl or a heteroaryl selected from thiazolyl, pyridyl, pyrimidinyl, 1,3,5-triazinyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl and 1,3,4-thiadiazolyl; wherein the phenyl or heteroaryl is optionally substituted with one substitute selected from fluorine, chlorine, bromine, iodine, C1-4alkyl, trifluoromethyl, C1-4alkoxy, C1-4alkylthio, nitro and cyano; r=1-2; R2 is absent or is an oxo-group; Z is: (a) phenyl substituted with NRaRb; where Ra is: H or C1-4alkyl; where Rb is: C1-4alkyl, cycloalkyl, phenyl, furanylmethyl, or phenyl(C1-2alkyl); and wherein the phenyl or the furanyl are optionally substituted with iodine; alternatively, Ra and Rb are taken together with the nitrogen atom to which they are bonded to form a 5-8 member heterocyclyl, which is optionally condensed to a benzene ring; (b) biphenyl-3-yl or biphenyl-4-yl; where the interior phenyl ring, attached to the carbonyl in formula (I) is optionally substituted with a fluorine atom; and where the terminal phenyl ring is optionally substituted with a substitute selected from trifluoromethyl, C1-4alkoxy, chlorine, dichloro, fluorine, and iodine; (c) phenyl substituted with a substitute selected from C5-8cycloalkyl, -NHC(=O)cyclohexyl, phenyloxy, phenylcarbonyl, phenyl(C1-3)alkyl, phenyl(C1-3)alkoxy, pyrrolyl, pyrazolyl, imidazolyl, isoindol-2-yl-l,3-dione, 2,3-dihydro-isoindol-2-yl; l-(tert- butoxycarbonyl)piperidin-4-yloxy, and 1-(tert-butoxycarbonyl)piperidin-4-yl; (d) phenyl substituted with 1-2 substitutes independently selected from: C1-6alkyl, C1-4alkoxy, iodine, chlorine and nitro; (e) phenyl(C1-2)alkyl; where the phenyl is optionally substituted with 1 or 2 substitutes independently selected from iodine, fluorine, C1-6alkyl, phenyl and NRcRd; where Rc: H or C1-4alkyl; where Rd is: C1-4alkyl or C1-6cycloalkyl(C1-4)alkyl; and where the C1-2alkyl of phenyl(C1-2)alkyl is optionally substituted with phenyl; (f) phenyl(C2-4)alkenyl; where the phenyl is optionally substituted with a substitute selected from C1-4alkyl, C1-4alkoxy, trifluoromethyl, trifluoromethylthio and phenyl; (g) naphthyl; where the naphthyl is optionally substituted with one C1-4alkoxy substitute; (h) fluorenyl or xanthenyl; where the fluorenyl or xanthenyl is optionally substituted with an oxo group; (i) C5-8cycloalkyl; where the C5-8cycloalkyl is optionally substituted with one C1-6alkyl substitute; (j) benzene ring-condensed C5-8cycloalkyl or benzene ring-condensed C5-8cycloalkyl(C1-4)alkyl; where said C5-8cycloalkyl fragment is optionally substituted with 1-4 methyl groups; (k) bicyclo[2.2.2]octyl-1-yl; where the bicyclo[2.2.2]octyl-l-yl is optionally substituted with C1-6alkyl; (1) a heteroaryl or benzene ring-condensed heteroaryl selected from benzooxazolyl, quinolinyl, benzimidazolyl, pyridinyl, indolyl, thienyl, furanyl, pyrazolyl, oxazolyl, benzothienyl and benzofuranyl; where the heteroaryl or benzene ring-condensed heteroaryl is optionally substituted with 1 or 2 substitutes independently selected from C1-4alkyl, trifluoromethyl, C5-8cycloalkyl, phenyl, phenyl(C1-2)alkoxy, phenyl(C2-4)alkynyl and dichlorophenoxy; and where the phenyl substitute in the heteroaryl is further optionally substituted with C1-4alkyl, C1-4alkoxy or trifluoromethyl; (m) l,5-diphenyl-lH-pyrazol-3-yl; where the pyrazol-3-yl is optionally substituted with a methyl group; and where each of the phenyl groups of the 1,5-diphenyl substitutes is also optionally substituted with substitutes selected from chlorine, dichloro or aminosulphonyl; (n) 1,2,3,4-tetrahydroquinolin-6-yl; where the 1,2,3,4-tetrahydroquinolin-6-yl is optionally substituted with phenyl or trifluoromethyl-substituted phenyl; and (o) benzene ring-condensed heterocyclyl(C2-4)alkenyl; where the benzene ring-condensed heterocyclyl is attached to the C2-4alkenyl via the benzene ring; and where benzene ring-condensed heterocyclyl is further optionally substituted with C5-6cycloalkyl; taking into account constraining conditions indicated in claim 1. The invention also relates to a pharmaceutical composition based on the compound of formula (I), a method of producing said pharmaceutical composition, a method of treating said pathological conditions and use of the compound of formula (I).

EFFECT: obtaining novel heterocyclic compounds having MGL inhibiting activity.

21 cl, 5 tbl, 11 ex

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