Immunomodulatory steroids

FIELD: medicine.

SUBSTANCE: claimed invention relates to application of steroid compounds, preferably 17 α-ethinyl derivatives of androstane.

EFFECT: insuring treatment of inflammatory or autoimmune disease in subject and/or infection prevention.

7 cl, 12 ex, 18 dwg

 

The text descriptions are given in facsimile form.

1. The use of compounds for the treatment of the subject of inflammation or autoimmune diseases, with the specified connection has

where R represents CRAand CRA=H or possibly containing substituents With1-20alkyl;
R1is a HE or esters;
R2is a HE, ester or halogen,
R3represents H, HE, complex EF the p or halogen,
R5and R6independently represents-H, -CH3, -CH2ORPRand
RPRrepresents-H or a protective group;
R7, R8and R9independently represent-CHR10-where R10represents-H, -HE or ester.

2. The use according to claim 1, wherein R1is a HE or SLA; R2represents-OH, -SLA or Br, and R3represents-H, -OH, -SLA or-Br.

3. The use according to claim 2, wherein R5and R6located in the β-configuration and represents a-CH3.

4. The use according to claim 3, wherein R7, R8and R9represent-CH2-.

5. The use according to claim 4, wherein RAis a-H.

6. The use according to claim 5, characterized in that the inflammation or autoimmune disease associated with multiple sclerosis, inflammatory bowel disease, trauma, bleeding, arthritis, or diabetes.

7. The use according to claim 5, characterized in that the inflammation associated with infection.



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention provides administration of triterpene glycosides of holothurian Cucumaria okhotensis chosen from a group consisting of Frondoside A1, Ochotoside B1, Ochotoside A1-1, Ochotoside A2-1 or Cucumarioside A2-5 or their mixtures, as an agent stimulating cell-mediated immunity in mammals, as well as for preparing a pharmaceutical composition stimulating cell-mediated immunity in mammals.

EFFECT: extended range of the agents stimulating cell-mediated immune reaction in mammals.

4 dwg, 1 tbl, 2 cl

FIELD: medicine.

SUBSTANCE: invention refers to a method of Δ4-3-ketosteroids 11 β-hydroxylation by a biomass Curvularia lunata strain mycelium, RNCIM No. F-988. For the transformation, Curvularia lunata strain mycelium, RNCIM No. F-988 not older than 30 h and washed of nutrient medium is used. Mycelium is taken in such amount that the relation of the biomass to the transformed steroid makes 1.5-2.5:1. The transformation is performed in a buffer solution, and a steroid substratum is added as a microcrystal suspension, or as a water-soluble methyl - β-cyclodextrine complex with steroid related thereto as 1:1-0.6:1 (mol/mol). The yield of 11β-hydroxyderivatives is 50-80 %.

EFFECT: offered invention allows for higher selectivity of 11β-hydroxylation process, concentration of the transformed steroid substratum up to 20 g/l and reduced reaction period to 24-50 h.

1 tbl, 10 ex, 2 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described compounds of the following structure or their salts: where A, B, R2, R4, R6, R7, R10, R16, R17α, R17β, Z, Y, X have the values specified in the description. Some of these compounds exhibiting tissue-specific antiandrogen activity and tissue-specific androgen activity can be applied for treating or reducing risk of the diseases associated with androgen stimulation loss.

EFFECT: preparation of the compounds which reducing probability of the androgen-dependent diseases, such as prostate cancer, benign prostate hyperplasia, polycystic ovary syndrome, acne, hirsutism, seborrhoea, etc.

41 cl, 176 ex, 4 tbl

Organic compounds // 2387664

FIELD: medicine.

SUBSTANCE: there are described compounds of formula in a free form or in the form of salt where R1 and R2 have values specified in the description of the application which are used for treating inflammatory conditions, first of all inflammatory or obstructive respiratory tract diseases. Besides the application describes the pharmaceutical compositions containing said compounds, and methods for preparing said compounds.

EFFECT: compounds exhibits improved efficiency.

5 cl, 8 ex

FIELD: chemistry.

SUBSTANCE: described is a 15β-substituted oestradio derivative having selective oestrogenic activity. The preferred compound is 7α-ethyl-15β-methyl-19-nor-17α-pregna-1,3,5(10)-trien-20-yne-3,17β-diol.

EFFECT: obtaining compounds which can be used in treating or preventing diseases or physiological conditions related to oestrogen receptors.

11 cl, 4 ex, 2 tbl

FIELD: medicine.

SUBSTANCE: invention relates to new 3.15-substituted estrone derivatives that are inhibitors of 17β-hydroxysteroid-dehydrogenase type 1 (17β-HSD1), to their salts, pharmaceutical compositions, containing specified compounds and to methods of such compound producing. Besides the invention refers to application in medicine of specified new 3,15-substituted estrone derivatives firstly to their application for treatment or prevention of steroid-dependent diseases or disorder such as steroid-dependent diseases or disorders treatment of which requires inhibition of 17β-hydroxysteroid dehydrogenase type 1 and/or reducing of endogenous 17β-estradiol concentration. The invention also relates to general application of selective inhibitors of 17β-hydroxysteroid-dehydrogenase type 1 that do not bind with estrogen receptor or display antipathic affinity to estrogen receptor.

EFFECT: possibility of application for treatment and prevention of benign gynaecologic diseases.

49 cl, 836 ex, 42 tbl

FIELD: chemistry.

SUBSTANCE: invention refers to synthesis of [18F]fluororganic compounds ensured by reaction of [18F]fluoride and relevant halogenide or sulphonate with alcoholic vehicle of formula 1 where R1, R2 and R3 represent hydrogen atom or C1-C18 alkyl.

EFFECT: possibility for mild process with low reaction time and high yield.

21 cl, 2 tbl, 27 ex

FIELD: technological processes.

SUBSTANCE: invention is related to automation of technological processes and may be used in automation of process of production of loose form of powdery choline chloride from its aqueous solution. In method that provides for use of crushed and fractionated dry sugar beet pulp as active adsorbent, its mixing with previously heated aqueous solution of choline chloride, and then drying in vibration dryer by superheated steam of atmospheric pressure, separation of spent superheated steam flow into the main one, sent to vibration dryer with creation of recirculation circuit, and additional one sent for reheating of choline chloride prior to its supply for mixing, the novelty is the fact that superheating of atmospheric pressure steam is done with heating steam, at that heating steam is produced by means of steam generator with electric heating elements, feed pump and safety valve, heating steam condensate produced in this process after superheating and condensate produced during heating of aqueous solution of choline chloride is taken to condensate collector, and then in mode of closed circuit is supplied in steam generator, at that flow rate of crushed and fractionated dry pulp is measured, as well as aqueous solution of choline chloride coming for mixing, flow rate and temperature of superheated steam upstream vibration dryer, choline chloride temperature before and after its heating, pressure of choline chloride after heating, temperature and humidity of mixture of crushed and fractionated dry pulp and aqueous solution of choline chloride prior to supply for drying, amplitude and frequency of oscillations in gas-distributing grid of vibration dryer, flow rate and humidity of powdery choline chloride after drying, level of condensate in steam generator and pressure of heating steam, at that flow arte of dry sugar beet pulp after fractionation is used to set flow rate of heated choline chloride coming for mixing, and flow rate and humidity of prepared mixture of crushed and fractionated dry pulp and aqueous solution of choline chloride prior to supply for drying, flow rate and humidity of powdery choline chloride after drying are used to determine amount of evaporated moisture in vibration dryer, which is used to establish flow rate of superheated steam in the main circuit of recirculation, and its temperature is established by current value of temperature of mixture of crushed and fractionated dry pulp and aqueous solution of choline chloride by setting of specified capacity of steam generator affecting power of electric heating elements, at that in case condensate level in steam generator falls below specified value, condensate is supplied from condensate collector, and when pressure of steam in steam generator reaches upper limit value, steam pressure is released through safety valve, if flow rate of mixture of crushed and fractionated dry pulp and aqueous solution of choline chloride deviates prior to supply for drying to the side of increase from specified value, at first frequency is increased, and then amplitude of oscillations in gas-distributing grid of vibration dryer, if flow rate of mixture of crushed and fractionated dry pulp and aqueous solution of choline chloride deviates to the side of reduction from specified value, at first frequency is reduced, and then amplitude of oscillations in gas-distributing grid of vibration dryer, current values of temperature and flow rate of choline chloride prior to heating are used to set flow rate of spent superheated steam in additional recirculation circuit, at that temperature of choline chloride after heating is used to set specified pressure of choline chloride at the inlet to mixer.

EFFECT: provides for increased quality of finished product, accuracy and reliability of control, increased yield of finished product, reduced specific heat and power inputs and prime cost of finished product.

1 dwg

FIELD: chemistry.

SUBSTANCE: invention concerns novel compounds of formula I: , where M is macrolide subunit of substructure II: , L is chain of substructure III: -X1-(CH2)m-Q-(CH2)n-X2-, D is steroid or non-steroid subunit derived from steroid or non-steroid NSAID medicines (nonsteroid anti-inflammatory drug) with anti-inflammatory effect; pharmaceutically acceptable salts and solvates of claimed compounds; methods and intermediary compounds for obtainment of claimed compounds.

EFFECT: improved therapeutic effect, application in inflammatory disease and state treatment for humans and animals.

37 cl, 18 ex

FIELD: chemistry.

SUBSTANCE: claimed invention relates to novel fusidic acid derivatives of general formula [I], where X represents halogen, trifluoromethyl, C1-C7alkyl, substituted with phenyl, C2-C9alkenyl, optionally substituted with C1-C7alkyl, halogen or phenyl, phenyl, optionally substituted with one or two similar or different substituents, selected from group consisting of halogen, C1-C7alkyl, C2-C9alkenyl, phenyl, C1-C6alkoxy, nitro, C1-C6alkyltio, trifluoromethyl and cyano; or X represents naphtyl; Y and Z both represent hydrogen or together with bond C-17/C-20 form double bond between C-17 and C-20 or together represent methylene and form cyclopropane ring in combination with C-17 and C-20; A represents O, S or S(O); B represents C1-6alkyl, C2-6alkenyl, C1-6acyl, phenyl or benzoyl, where C1-6alkyl is optionally substituted with one or more halogens, hydroxy, C2-6alkenyl, phenyl, C1-4heteroaryl or C1-6alkoxy; Q1 represents -(CHOH)-, or -(CHW)-, where W represents halogen or azido; Q2 represents -(CHOH)-; to their pharmaceutically acceptable salts and easily hydrolysed esters and to pharmaceutical compositions, including said derivatives, as well as to their application in therapy.

EFFECT: application in therapy.

31 cl, 127 ex, 5 tbl

FIELD: medicine.

SUBSTANCE: invention provides administration of triterpene glycosides of holothurian Cucumaria okhotensis chosen from a group consisting of Frondoside A1, Ochotoside B1, Ochotoside A1-1, Ochotoside A2-1 or Cucumarioside A2-5 or their mixtures, as an agent stimulating cell-mediated immunity in mammals, as well as for preparing a pharmaceutical composition stimulating cell-mediated immunity in mammals.

EFFECT: extended range of the agents stimulating cell-mediated immune reaction in mammals.

4 dwg, 1 tbl, 2 cl

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to pediatrics, and concerns treating pneumonia in adolescents. For this purpose, a conventional integrated therapy is added with a non-microbial probiotic Actoflor-C containing synthetic analogues of low-molecular bacteria exometabolites of probiotic strains, which is introduced per os by 20 drops 3 times a day for 10 days.

EFFECT: method provides effective treatment ensured by enhanced immune response with no side dysbiotic effect of antibiotic therapy.

2 ex, 2 tbl

FIELD: medicine, veterinary science.

SUBSTANCE: invention refers to veterinary science, particularly to method for producing drugs. Substance of the method consists in the fact that a preparation is made of drone larvae aged 5 to 14 days which are placed in a freezing chamber at temperature (-4°C-(-5°C)) for 12-14 h. Further, a brood is defrozen to temperature +18°C and homogenised for 3-5 minutes. It is added with diacetophenonylselenide 3.5-4 mg per 100 ml of a homogenate, then added with acetylsalicylic acid in amount 0.2 % to the volume, mixed thoroughly for 2-3 min to produce a homogeneous mass, poured in sterile flasks 100 ml, closed with sterile bulky plugs and placed in a thermostat at temperature +50-(+ 55°C) for 35-40 min, at the end of a preset time, the flasks are moved to another thermostat for incubation at +37°C for 8 h. A cycle is repeated for three times. Then, it is cooled to room temperature. In sterile conditions, mixed homogenate and diacetophenonylselenide is added with a sterile drying medium (saccharose-gelatin mixture containing 10% of saccharose and 5% of gelatin) in the homogenate to drying medium ratio 1:10. The mixture is mixed for 2-3 minutes, and filtered in a sterile box through 4-5 layers of a sterile gauze, frozen at temperature -50°C and sublimated in a vacuum chamber at shelve preheat temperature +30-(+45°C), when achieving preparation temperature +20°C-(+22°C), shelve temperature is decreased to +25°C and dried up for 22-24 h.

EFFECT: method allows producing an effective preparation using which allows higher total and specific resistance of animal organism.

5 ex, 2 tbl, 1 dwg

FIELD: medicine.

SUBSTANCE: invention relates to medicine, can be applied in resuscitation science, surgery, clinical immunology. For correction of immune insufficiency in patients with mechanical jaundice of non-tumour genesis in addition to complex traditional therapy of post-operational period from the first day after operation one time per day intravenously introduced is 1 ml of 1%-solution of glutoxim on autoblood, with its preliminary 30 minute incubation with 20 ml of autoblood. Treatment course is 5 sessions.

EFFECT: method makes it possible to increase treatment efficiency, reduce lethality, reduce duration of patient's presence in hospital.

2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to clinical immunology and aims at patient-specific immunotherapy. That is ensured by the use in a nidus zone of supernatant of stimulated autologous leukocytes with the concentration of neutrophilic antimicrobial peptides in supernatant not less than 2000 pg/ml. Supernatant is administered in applications and/or subcutaneously, or submucosally, or in instillations for 5-10 days.

EFFECT: method provides prevention of secondary immunodeficiency, reduced inflammation, wound decontamination, stimulated repair, allows lower dosages and period of administering antibiotics, due to joint action of a complex of cytokines and antimicrobial neutrophilic peptides produced by autologous leukocytes.

6 cl, 3 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed is application of immobilised oligonucleotides as immunostimulating and hemostimulating medication for peroral introduction. Immobilised on polyethylene oxide oligonucleotides of DNA of salmon soft roes demonstrate immuno- and hemostimulating activity in conditions in vivo in case of peroral introduction in experimental animals and in vitro, which is manifested in stimulation of phagocytic reactions in vivo and in vitro, increase of IFN-γ in vitro, increase of cytotoxic activity of natural killers, increase of spontaneous proliferative activity of lymphoid cells of experimental animals and index of B-lymphocyte stimulation, increase of nitrogen oxide production, as well as in enchancement of hemopoiesis regeneration in early terms after cytostatic impact.

EFFECT: immobilised by physical method oligonucleotides are protected from destruction in gastrointestinal tract, which facilitates their permeability through intestine wall and increases bioavailability.

11 tbl

FIELD: medicine, veterinary science.

SUBSTANCE: method for preparing an immunostimulating drug for animals consists in the fact that stevioside is dissolved in 0.9 % physiologic saline, the prepared solution is added to pre-grinded lecithin, then olive oil heated to 35-40°C is introduced gradually in the prepared composition and mixed; further the prepared solution is filtered and autoclaved at temperature 115-120°C for 15-20 minutes, then the produced sterile drug is bottled and corked up. The immunostimulating drug for animals contains stevioside, 0.9 % physiologic saline, olive oil, lecithin in a certain ratio.

EFFECT: higher viability and productivity of animals by correcting body immune responsiveness.

2 cl, 4 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry, namely to creation of medication, stimulating immunostimulating action, which represents liquid extract of burdock greater and woolly burdock roots, taken in ratio 1:1, obtained by method of repercolation with 40% ethanol.

EFFECT: medication extends arsenal of immunostimulating medications, amplifies humoral immune response, phagocytic activity of peripheral blood neutrophilsand peritoneal macrophages.

3 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry, namely to creation of medication, stimulating immunostimulating action, which represents liquid extract of marsh-mallow roots, obtained by method of repercolation with 40% ethanol.

EFFECT: medication extends arsenal of immunostimulating medications, amplifies humoral immune response, cell immune response and phagocytic activity of peripheral blood neutrophils.

3 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to the development of new drugs for inflammatory diseases, particularly asthma. The pharmaceutical compositions under the invention contain 1-methyl-2-phenylthiomethyl-3-carbethoxy-4-dimethylaminomethyl-5-oxy-6-bromoindole in the effective amount or its pharmaceutically acceptable salts and/or hydrates as an active ingredient. The drug can be presented in the form of tablets, capsules, injections or aerosol.

EFFECT: provided anti-inflammatory and antiasthmatic action, as well as practically absolute absence of by-effects proper for the formerly known drugs administered for the same intended purpose.

10 cl, 4 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to gynaecology, and may be used for treatment of benign diseases of uterine neck. For this purpose after basis therapy with radio wave method of treatment, from the first days the female patients use hormonal therapy with single-phase contraceptives.

EFFECT: invention makes it possible to reduce time of postoperational wound epithelisation and to reduce frequency of uterine neck diseases relapses.

2 ex

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