Isoflavon derivatives of tectorigenine, their production and virus inactivating agent containing these derivatives as an active ingredient
SUBSTANCE: invention relates to the new isoflavon derivative of tectorigenine compound of formula (II) , where R1 represents H, NH2 or SO3M; R2 represents OR'; R3 represents H or -CH2NR"; wherein R' represents H, -CH2COONa or -CH2CH2NMe2; NR" represents or -NMe2; M represents H, Na, K or N+H(CH2CH2OH)3, it also relates to virus inactivating agent having this derivative as an active ingredient and to the method for preparation of the injections on its basis.
EFFECT: developing of production method for the injections on basis of tectorigenine.
20 cl, 10 tbl, 2 dwg,10 ex
The text descriptions are given in facsimile form.
1. Derived lektoriranje, having the chemical name 5,7,4′-trihydroxy-6-methoxy-isoflavone of the formula (II)
where R1represents N, NH2or SO3M;
R3represents H or-CH2NR′′;
where R′ represents H, -CH2COONa or-CH2CH2NMe2; provided that R1, R3and R′ are not both hydrogen;
NR′′ is aor-NMe2;
M represents H, Na, K or N+H(CH2CH2OH3).
2. Derived lektoriranje according to claim 1, wherein R1represents the SO3M′′where M′′ represents H, Na, K or N+H(CH2CH2OH)3having the formula (III)
3. Derived lektoriranje according to claim 2, characterized in that M′′ represents Na, having the formula (IV)
4. Derived lektoriranje according to claim 2, wherein R1represents-SO3 -N+H(CH2CH2OH)3having the formula (V)
5. Derived lektoriranje according to claim 1, wherein R1represents NH2, R2HE is a, R3represents H, having the formula (VI)
6. Derived lektoriranje according to claim 1, wherein R1represents H, R2represents-och2COONa and R3represents H, having the formula (VII)
7. Derived lektoriranje according to claim 1, wherein R1and R3represent H, R2is a co2CH2NMe2having the formula (VIII)
8. Derived lektoriranje according to claim 1, wherein R1represents H, R2HE is a, R3represents-CH2NR′′where NR′′ is ahaving the formula (IX)
9. Derived lektoriranje according to claim 1, wherein R1represents H, R2HE is a, R3represents-CH2NMe2having the formula (X)
10. Derived lektoriranje according to claim 5, characterized in that it is the Oh pharmaceutically acceptable salt.
11. Derived lektoriranje of claim 10, characterized in that the salt is a hydrochloride.
12. Derived lektoriranje according to claim 7, characterized in that a represents a pharmaceutically acceptable salt.
13. Derived lektoriranje indicated in paragraph 12, characterized in that the salt is a hydrochloride.
14. Derived lektoriranje of claim 8, wherein a is a pharmaceutically acceptable salt.
15. Derived lektoriranje through 14, characterized in that the salt is a hydrochloride.
16. Derived lektoriranje according to claim 9, characterized in that a represents a pharmaceutically acceptable salt.
17. Derived lektoriranje on item 16, characterized in that the salt is a hydrochloride.
18. Antiviral medication that contains an effective dose derived lektoriranje formula (II) as the active pharmaceutical component and a pharmaceutically acceptable auxiliary components.
19. Antiviral medication to claim 19, characterized in that the said drug is a drug for injection.
20. The method of producing drug for injection containing derived lektoriranje formula (II) as the active pharmaceutical component, in which 5-80 wt. including derivative is aktiivinen formula (II) and 20-150 wt. including glucose for injection is dissolved in 700-800 wt. including water for injection, after complete dissolution add water for injection to a total volume equivalent to 1000 wt. o'clock, and after filtration through a glass sinter funnel with a G4, conventional packaging and sterilization obtain a pale yellow transparent liquid preparation for injection, the glucose which is 2-15%, and the content of the active pharmaceutical component is 5-80 mg/ml
FIELD: organic chemistry, medicine, gynecology.
SUBSTANCE: invention relates to novel tetracyclic heterocompounds of the formula (I): wherein X, Y, Z, R1 - R4, n and m has values given in the invention description and used as selective modulating agents for estrogen receptors. Also, invention relates to a method for synthesis of these compounds and pharmaceutical compositions comprising thereof, and their using in treatment and/or prophylaxis of disorders mediated by one or more estrogen receptors. Proposed compounds are useful in treatment and/or prophylaxis of disorders associated with depleting estrogen and comprising such disorders as rush of blood, vaginal dryness, osteopenia and osteoporosis, hormone-dependent cancer and hyperplasia of breast, endometrium, uterus cervix and prostate, endometriosis, uterus fibroma, osteoarthritis that can be used as contraceptive agents both separately and in combination with progestogen or progestogenous antagonist.
EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.
25 cl, 7 tbl, 171 ex
FIELD: medicine; veterinary.
SUBSTANCE: medicine for bird influenza treatment includes activated-potentiated form of antibodies to bird alpha, beta and gamma interferon obtained by multiple sequential cultivation and external affection by homeopathic technology.
EFFECT: improved efficiency of treatment.
4 cl, 3 ex
FIELD: medicine; pediatrics.
SUBSTANCE: by the first vaccination of 3-18 months old children vaccination is performed at least over 60 days after their arrival to Far North regions from other climatic zones.
EFFECT: high vaccination efficiency due to taking in consideration processes of child organism adaptation to a change of climatic zones.
FIELD: medicine; pharmacology.
SUBSTANCE: invention claims application of starches substituted by quarterly ammonium groups with substitution degree of 0.4 to 3.0 with the help of a linker, in infection diseases treatment. Suppression of 1 type herpes virus replication by the claimed starches is demonstrated, in comparison to zero antivirus effect of non-modified starches. Minimal inhibiting concentration for staphylococci and mycobacteria is 5-60 g/l.
EFFECT: efficient infection disease treatment by the claimed starches.
5 cl, 7 tbl
FIELD: chemistry, pharmaceuticals.
SUBSTANCE: invention pertains to compounds with formula (I), their pharmaceutical salts or N-oxide used as an inhibitor to replication and/or proliferation of HCV, to the method of inhibiting replication or proliferation of hepatitis C virion using formula (I) compounds, as well as to pharmaceutical compositions based on them. The compounds can be used for treating or preventing infections, caused by hepatitis C virus. In general formula (I) cycle B is an aromatic or non-aromatic ring, which contains two heteroatoms, where X and Y, each is independently chosen from C, CH, N or O, under the condition that, both X and Y are not O and that, both X and Y are not N; U and T represent C; Z represents -CH-; A represents N or -CR2-; B represents -CR3-; D represents N or -CR4-; E represents N or -CR5-; G represents N or -CR6-; J represents N or -CR14-; K represents -CR8-; L represents N or -CR9-; M represents N or -CR10-; R2 and R6, each is independently chosen from a group, consisting of hydrogen, halogen, C1-C6alkyl, substituted C1-C6alkyl, C1-C6alkoxy, C1-C6substituted alkoxy, C1-C6alkoxycarbonyl, cycloheteroalkyl, substituted cycloheteroalkyl, -O-carbamoil, substituted -O-carbamoil, halogen C1-C6alkyl, diC1-C6alkylamino, substituted diC1-C6alkylamino and sylye ethers, where cycloheteroalkyl is a 3-7-member ring, containing 1-2 heteroatoms, chosen from N and O, under the condition that, one of R2 and R6 is not hydrogen; R3 and R5, each is independently chosen from a group, consisting of hydrogen, halogen; R4 represents hydrogen; R7 represents - NR11C(O)R12; R8, R9, R10 and R14, each is independently represents hydrogen; R11 represents hydrogen, C1-C6alkyl; and R12 is chosen from a group, consisting of halogen C1-C6alkyl; where each substituted group is substituted with one or more groups, chosen from -Q, -R40, -OR40, -C(O)R40, -C(O)OR40, where each Q independently represents halogen, R40 and R41 are independently chosen from a group consisting of hydrogen, C1-C6alkyl, C1-C6alkoxy, under the condition that: (i) at least one of A, D, E, G, J, L or M represents N; (ii) not more than one of A, D, E or G represents N; and (iii) not more than one of J, L or M represents N.
EFFECT: obtaining pyridyl-substituted heterocycles for treating and preventing infections, caused by hepatitis C virus.
33 cl, 85 dwg, 101 ex
SUBSTANCE: invention refers to veterinary science. Medicinal agent applied for prevention and treatment of bird viral influenza is represented with polystibuim. Polystibium inhibits infectious activity of influenza virus.
EFFECT: development of effective method applied for treatment and prevention of bird influenza.
6 tbl, 6 ex
SUBSTANCE: invention refers to medical products and concerns combination for HIV-infection treatment, containing (a) therapeutically effective amount of HIV-protease inhibitor by formula or its pharmaceutically accepted salt or ester and (b) effective amount of rhytonavir or its pharmaceutically accepted salt or ester. Besides, method of improved pharmacokinetics of HIV-protease inhibitor by formula (4) or its pharmaceutically accepted salt or ester, including introduction to an individual requiring such treatment, therapeutically effective amount of rhytonavir or its pharmaceutically accepted salt or ester with therapeutically effective amount of specified HIV-protease inhibitor by formula (4) is described.
EFFECT: offered combination has synergetic action if taken in any molar ratios.
33 cl, 6 dwg, 9 tbl, 4 ex
SUBSTANCE: novel polynucleotide is invented which is produced from the nucleotide sequence of the IFNα-17 gene, containing the single nucleotide polymorphism SNP g771c. Also, the novel polynucleotide is invented which is derived from the natural protein IFNα-17 of the wild type containing SNP G45R.
EFFECT: can be used for producing effective therapeutic agent with antiviral, antiproliferative and/or immunomodulating activity.
13 cl, 5 dwg, 6 ex
FIELD: medicine; pharmacology.
SUBSTANCE: invention refers to creation and application of aerosol spray compositions for treatment of diseases or disorders requiring lowering of cell proliferation and/or induction of cell apoptosis, such as neoplastic, autoimmune, viral diseases. Agent contains as active substance vitamin E based composition of structural formula , where R1 is carboxylic acid; R2 and R3 are hydrogen or R4; R4 is methyl, and R5 is alkyl; or where R1 is hydrogen or carboxylic acid; R2 and R3 are hydrogen or R4; R4 is methyl, and R5 is alkenyl.
EFFECT: improved delivery of specified composition by inhalation with intensified antiproliferation activity.
59 cl, 17 dwg, 6 tbl, 35 ex
SUBSTANCE: method of production of dry polyvalent virus-vaccine includes separate infection of cell culture with strain PC-126 of turkey herpesvirus (virus of Marek's disease 3rd serotype) and one-day chicken infected with chicken herpesvirus (virus of Marek's disease 2nd serotype), incubation, turkey herpesvirus harvest, and sampling of double flag follicles of chicken herpesvirus infected chicken, protective medium addition, separate ultrasonic processing of virus cell mass and flag follicle mass, freezing and drying of end product followed with their mixing. At that chicken herpesvirus strain are sampled for (VMD 2nd serotype) strains "42", "50", "SB-1", inoculated in dosage 10000-50000 functional residual capacity (FRC) for chicken and grown in body within 12-25 days. Follicles processed with ultrasonic is removes, and protective medium processed with ultrasonic and containing released chicken herpesvirus is added equal proportion of processed with ultrasonic clean cell cultures of bird embryos grown within 24-72 hours. Dry polyvalent virus-vaccine contains cell-free lyophilized strain FC-126 of turkey herpesvirus - 3rd serotype of Marek's disease virus in protective medium. In addition virus-vaccine includes cell-free lyophilised strains of chicken herpesvirus - 2nd serotype of Marek's disease virus, produced by any cl.1-5, in protective medium at ratio 2000 FRC /units: 100-5 00 FRC /units, respectively.
EFFECT: vaccine has high immunogenic activity and storage stability.
10 cl, 3 tbl, 4 ex
FIELD: medicine; pharmacology.
SUBSTANCE: agent contains oil extract of poplar buds and sprouts and oil extract of aspen buds and sprouts with component ratio as follows, mass.%: oil extract of poplar buds and sprouts 20-90, oil extract of aspen buds and sprouts 10-80, mixed oil extract of poplar buds and sprouts and oil extract of aspen buds and sprouts, with component ratio as follows, mass.%: oil extract of poplar buds and sprouts 20-90, oil extract of aspen buds and sprouts 10-80, as well as fat extract of plant raw with plant component ratio as follows, mass.: marsh tea 3, comfrey 3, blueash 2, silver fir 1, common burdock (root) 2, horseheal (root) 1, deer's-tongue 1, horseradish 1, musquash-poison 2, hog bean (herb) 2, hop (cones) 2, cowberry (root) 2, mountain arnica (blossom) 2, ratio of oil extracts and fat extract of plant raw is 1:3 respectively.
EFFECT: agent allows widening range of preventive and therapeutic herbal medicinal agents of antiviral and anti-inflammatory action.
2 cl, 9 ex
FIELD: medicine; pharmacology.
SUBSTANCE: composition is intended for treatment or prevention of insulin resistance of susceptible warm-blooded animals, including humans, and contains selective modulator of estrogen receptor EM-652-HC1, taken in amount determined by therapeutic efficiency.
EFFECT: effective treatment of prevention of insulin resistance development for warm-blooded mammals.
5 cl, 20 ex, 12 tbl, 8 dwg
FIELD: medicine; pharmacology.
SUBSTANCE: invention refers to medicinal agents, specifically to cold preventive composition, containing vitamin C and ginkgetine, and to method of cold prevention provided preventive intake of specified composition.
EFFECT: cold prevention provided preventive intake of specified composition.
16 cl, 4 ex, 9 tbl
SUBSTANCE: film dosage form sticking to mucous, containing at least on active substance from hemp. The form contains the polymeric matrix, which is used as a reservoir for the active substance and sticking to mucous. The form can have the multilayer structure. It can also contain the non-active ingredients, odorants or aromatisors. The film form is used in treatment of pain in such diseases as carcinomatosis, AIDS, trauma and other disorders.
EFFECT: invention provides better tolerance to administered substances and rapid onset of administered drug, simplifies administration procedures.
SUBSTANCE: the present innovation deals with applying hesperidin compound or one of its derivatives chosen out of the group that consists of hesperidins, α-glycosyl-hesperidin, methyl-hesperidin, hesperetin conjugate and sulfate or glucoronide, as active compound that stimulates osteogenesis and inhibits osseous resorption for obtaining a composition indicated for osteogenesis stimulation and/or inhibiting human or animal osseous resorption. The innovation illustrates the decrease of osseous demineralization and improves biomechanical properties of femur due to hesperidin action.
EFFECT: higher efficiency.
18 cl, 14 dwg, 4 tbl
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to drugs and in particular provides a receptor ligand activated by peroxisome proliferator γ (PPAR γ), and a composition comprising the indicated ligand used for aim in improving insulin-resistance state or for prevention and/or improving the insulin-resistance syndrome state. Invention relates to a receptor ligand activated by peroxisome proliferator that comprises prenylflavonoid, chalcone derivative, flavonol derivative and their salt, glycoside and/or esterified form. Also, invention relates to composition comprising abovementioned ligand, a vegetable extract containing abovementioned ligand, and to a novel compound (dehydroglyasperin D) represented by the following formula: .
EFFECT: improved preparing method, valuable medicinal properties of ligand.
33 cl, 26 tbl, 13 ex