Method of treating baker's cyst
SUBSTANCE: invention refers to orthopaedics, namely rheumatology, and concerns treating Baker's cyst. That is ensured by cyst puncture, aspiration of its content, and introduction of the non-steroid anti-inflammatory preparation xefocam in its cavity; and then the enzymatic preparation longidaza is introduced in a paraarticular space.
EFFECT: method provides effective conservative treatment of Baker's cyst with no recurrences and side effects.
11 cl, 2 dwg, 3 ex
The invention relates to orthopedics, namely, rheumatology, and can be used in medical practice for the treatment of cysts Baker when synovitis.
The knee joint is the largest synovial joint. The synovial membrane covering the inside of the joint capsule forms numerous folds, which juts into the joint cavity. A Baker cyst is a hollow saccular education that develops from the tissues lining the bag knee joint. The typical localization of the cyst Baker - rear surface of the joint. For Baker cyst is characteristically affected or aseptic fluid accumulation in the popliteal fossa of the knee joint, it is often accompanied by synovitis in patients with osteoarthritis, rheumatoid arthritis [lugoves YEAR Popliteal cysts in rheumatic diseases. Discard. the honey. Sciences. - M., 1998. - 95 S.]. In the treatment of synovial cysts are used for both surgical and conservative methods.
Surgical treatment of cysts Baker are surgical excision its walls. The procedure can be performed under local anesthesia and does not require a hospital stay longer than a day. After removal of the cyst in the region of the knee imposed a special adhesive bandage or a plaster bandage for a few days, usually up to a week, limited to the load on operirovanne the leg.
Conservative treatment cyst Baker is to puncture the cavity of the cyst, removal of contents and the introduction of anti-inflammatory drugs (predominantly use steroid hormones). Unfortunately, the frequency of relapse (re-education of cysts) after treatment is quite high, which is one of the main reasons is much more frequent use of surgical methods.
Conservative therapy includes the following methods: unloading joints, physiotherapy, puncture of cysts by aspiration and the subsequent introduction (or not) of drugs.
As a Baker cyst in the knee joint, usually associated with synovitis, then it is logical treatment involving the use of one or another anti-inflammatory drug.
There is a method of treatment of a cyst Baker by intraarticular injection of corticosteroids persons with rheumatoid arthritis, accompanied by Baker cyst, which as a result of treatment is reduced in size [Danilov IM Ultrasonographic diagnosis of cyst Baker in gonarthrosis: Dis...Kida. the honey. Sciences. - Barrow, 2000. - 115 C.]. However, corticosteroids are not only not always have a positive effect, but in some cases, their introduction may lead to loss of proteoglycan of cartilage [Zagorodniy, NV Within the statutory and periarticular therapy of diseases of the musculoskeletal system. - M.: Publishing house of the Russian peoples friendship University, 2001. - 48 S.].
There is a method of treatment of a Baker cyst, which after makuchi the contents of the cyst into it enter the cytostatic drug cyclophosphamide [Babich I.I. non-indigenous GI, I.V. Babich Treatment of Wagram in children // Surgery. - 1989. No. 11. - S-82]. This method is the closest analogue of the method proposed and adopted for the prototype of the invention. However, the drug cyclophosphamide [Cyclophosphamide // Vidal-99: Handbook of drugs in Russia. - 5th ed. - M., 1999. - SE.] - alkylating cytostatic, has a number of undesirable side effects. Thus, it can cause nausea, vomiting, alopecia, aseptic hemorrhagic cystitis, sometimes toxic hepatitis, headache and pain in the muscles and bones; has myelotoxicity, i.e. it can lead to leukopenia and thrombocytopenia. Given the development of possible side effects, the use of such drug in the treatment of cyst Baker's insecure and has a lot of contraindications. For example, it is contraindicated in persons with anemia, leukopenia and thrombocytopenia.
The invention solves the problem of creating an effective treatment for cyst Baker, do not produce any side negative effects, therefore, it is safe for the health of patients.
The problem is solved in that a method for the treatment of cyst Baker, including PU is the Ktsia cysts, the aspiration of its contents and introduction in its cavity therapeutic drug xefocam, then in juxta-articular space of the injected drug logidata.
The treatment can be supplemented by the fact that within two to three weeks spend 2-5 injections xefocam in the joint and 2-5 injections longitute intramuscularly, alternating them every other day.
It is advisable to perform diagnostic ultrasound of the knee joint, verification of diagnosis, clarification of the size, shape and position of the cyst
Diagnostic ultrasound of the knee joint can be performed biopsy probe with standard sterile disposable nozzle for holding the punctures.
Puncture of the cyst can be performed with the patient lying on his stomach.
After puncture of the cyst, aspiration of its contents and the introduction of the skin it is advisable to treat with antiseptic and apply aseptic adhesive bandage.
The aspiration of cyst it is advisable to carry out under ultrasound control.
Longido you can enter with the patient lying on his back.
Longido can be used to position the patient lying on his stomach.
The most effective type longido at the position in the periarticular area to the side.
After drug treatment, it is advisable to carry out sclerotiniaceae cysts 96% of what percom.
The inventive method of treatment of a cyst Baker is as follows.
First perform a diagnostic ultrasound examination of the knee joint, verification of diagnosis, clarification of the size, shape, position of the cyst. After that start the treatment, which is carried out in three stages.
Manipulation of the punctured cysts is performed from the position of the patient lying on his stomach. Ultrasonic navigation performed using a biopsy probe with standard sterile disposable nozzle for holding punctures. For this process antiseptic skin, be intra-articular manipulation, and cause them sterile gel for the ultrasound.
At the first stage of treatment the cyst puncture and aspiration. To do this, select the optimal route of a needle into the cyst cavity, evacuating the contents, controlling for ultrasound completeness of extraction.
In the second stage of treatment, leaving the needle in the cavity of the cyst, replace the syringe with the remote content on the syringe with the drug xefocam and implement its introduction into the cavity of the cyst. After removing the contents of the cyst and the introduction in its cavity preparation xefocam treat the skin with antiseptic and put aseptic adhesive bandage. The process of drug xefocam after aspiration of the cyst shown in figure 1. Drug xefocam OK which shows a pronounced analgesic and anti-inflammatory effect.
At the third stage of treatment carry out the introduction side in the juxta-articular space of the drug logidata, which increases the bioavailability of anti-inflammatory drug xefocam. Preparation logidata can be entered either from the position of the patient lying on his back, and the position of the patient lying on his stomach.
Within two to three weeks, depending on the initial condition of the patient, to consolidate anti-inflammatory treatment, alternating every other day, 2-5 injection drug xefocam in the joint and 2-5 injection drug logidata intramuscularly.
Control over the joint state after aspiration of the cyst and the treatment is carried out by ultrasound in a week. If the cyst is not filled with liquid content, conduct fine-needle sclerosing therapy 96%ethyl alcohol.
In case of recurrence of the cyst and filling her cavity content, although this usually does not happen in full, aspiration of the cyst with the introduction of drug xefocam repeat. Exercise and injections longitute, and then sclerosing therapy.
The inventive method of treatment is illustrated by the following examples.
Example 1. Patient B., aged 47. Diagnosis: gonarthrosis stage I, the pain syndrome. When U3-study diagnosed with synovitis, defined by the presence of cysts Baker, located in Duramed the real part of the right knee joint. When ultrasound determined the contents of the cyst - anechoic mass with the cyst oval, without partitions and inclusions. Despite the small volume (~ 6 ml) Baker cyst caused pain when bending the leg at the knee. Held aspiration of the cyst under U3-control with the introduction of the cavity 8 mg xefocam in 2 ml of water for injection and the introduction of longitute 3000 ME in 2 ml of 2% lidocaine in the periarticular area to the side. Additionally, within two weeks, through day three injections xefocam in the joint and longitute intramuscularly. Pain in the joint stopped. After treatment couch cysts sklerozirovana the introduction of 1 ml of ethanol under ULTRASOUND control. Monitoring the state of the joint is carried out by ultrasound in a month. The dynamics of the treatment under ULTRASOUND control shown in Fig.2, where: a) the cyst Baker oval shape of the right knee joint;
b) Baker cyst after aspiration of the content and the introduction of xefocam;) cyst Baker after sclerotherapy, ultrasound in a month after treatment.
Example 2. Patient P., 66 years. Diagnosis: metabolic-dystrophic gonarthrosis stage II. Turned with severe pain in left knee joint, the knee is swollen, has come to accept, using a cane. When U3-examination of the left knee diagnosed with synovitis, defined by the presence of cysts Baker, located in dorsomedial of the left knee the Charter at the level of the joint space, the sizes of a cyst 21×22×22. Held aspiration of the cyst under U3-control with the introduction of the cavity 8 mg xefocam in 2 ml of water for injection and the introduction of longitute 3000 ME in 2 ml of 2% lidocaine. Additionally, through day two injections xefocam in the joint and longitute in juxta-articular space. After treatment there was a partial filling of the cyst liquid. Was repeated aspiration of the cyst with the introduction of xefocam on the above scheme and the introduction of longitute. After re-treatment cyst Baker declined. Conducted cyst sclerotherapy with alcohol under ULTRASOUND control. Additional control condition of the knee joint after 1, 3, 6 months. Recurrence of the cyst Baker was not observed and one year after treatment.
Example 3. Patient D., 52 years old. Diagnosis: Rheumatoid arthritis, gonarthrosis II-III century left knee. Pain syndrome. Cyst Baker's boat-shaped without inclusions. Using the proposed method treatment: puncturing the cyst, aspiration under U3 control, the introduction of xefocam in the cavity of the cyst and longitute in juxta-articular space. Achieved complete reduction of cysts. Then, as described above, had a course of injections of xefocam periartikulyarno (8 mg xefocam, No. 5) and the injection of longitute intramuscularly (Logidata 3000 ME in 2 ml of 2% lidocaine, No. 5). Under U3-what stralem cyst Baker sclerotic (fibrous) 96% alcohol. The patient has a drug Arcoxia at a dose of 60 mg twice a day. Additional control condition of the knee joint after 1, 3, 6, 12 months. Recurrence of the cyst Baker was not observed.
In the treatment of synovitis of the knee in 42 patients with rheumatoid arthritis cyst Baker diagnosed by ultrasound in 43% of cases; in 36 patients with gonarthrosis in 33% of cases.
The rate of cyst Baker claimed method in rheumatoid arthritis - 78%, and in gonarthrosis - 97%. All patients, in addition to treatment cyst Baker was conducted therapy of the underlying disease in accordance with the diagnosis. Side effects in the form of ill health patients was not observed.
Thus, the proposed method of treatment cyst Baker gives no negative side effects, and therefore safe for the health of patients, this effectively makes it possible to treat these disease without surgical intervention.
1. The way to treat a cyst Baker, involving puncture of the cyst, aspiration of its contents and introduction in its oral drug treatment, characterized in that the cavity of the cyst impose drug xefocam, then in juxta-articular space of the injected drug logidata.
2. The method of treatment according to claim 1, characterized in that it further in the next two or three weeks spend 2-5 injection drug xefocam in the joint and 2-5 injection is Reparata logidata intramuscularly, alternating every other day.
3. The method of treatment according to claim 1, wherein the pre-perform diagnostic ultrasound of the knee joint, verification of diagnosis, clarification of the size, shape and position of the cyst.
4. The method of treatment according to claim 3, characterized in that the diagnostic ultrasound examination of the knee joint perform a biopsy probe with standard sterile disposable nozzle for holding the punctures.
5. The method of treatment according to claim 1, characterized in that the puncture of the cyst was performed at the position of the patient lying on his stomach.
6. The method of treatment according to claim 1, characterized in that after the puncture of the cyst, aspiration of its contents and the introduction of the drug xefocam the skin is treated with antiseptic and put aseptic adhesive bandage.
7. The method of treatment according to claim 1, characterized in that the aspiration of cyst performed under ultrasound control.
8. The method of treatment according to claim 1, characterized in that longido administered during the patient lying on his back.
9. The method of treatment according to claim 1, characterized in that longido being in the position of a patient lying on his stomach.
10. The method of treatment according to claim 1, characterized in that longido injected into the periarticular area to the side.
11. The method of treatment according to claim 1, characterized in that it further out sclerotiniaceae cysts 96%alcohol.
FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed invention relates to compounds of formula (I) where values of substituents are given in description, possessing inhibiting activity with respect to cathepsin K as well as to pharmaceutical compositions for treating diseases, associated with cysteine protease activity and to methods of inhibiting cathepsin K in mammals, requiring such treatment by introduction of efficient amount of compound to mammal.
EFFECT: claimed is application of formula (I) compound or its pharmaceutically acceptable salt in manufacturing medication for application in cathepsin K inhibition in a warm-blooded animal.
10 cl, 45 ex, 5 dwg
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to new compounds of formula (I) and its pharmaceutically acceptable salts possessing dihydroorotate dehydrogenase inhibitory ability, to a based pharmaceutical composition, to application thereof in preparing a drug compound and to a combined preparation containing the presented compounds and the other active compound (I) in effective amounts wherein both groups G1 mean CRC, G2 mean a nitrogen atom or group CRd, of the groups G3 and G4 mean a nitrogen atom and the other one means group CH, M means a hydrogen atom or a pharmaceutically acceptable cation, while R1, R2, Ra, Rb, Rc and Rd have the values specified in the patent claim.
EFFECT: preparing pharmaceutically acceptable salts possessing dihydroorotate dehydrogenase inhibitory ability.
25 cl, 115 ex, 2 tbl
SUBSTANCE: invention refers to medicine, namely traumatology, orthopaedics and rehabilitation, and may be used for treating inflammatory-degenerative arthropathies. The therapy is three-staged. The first stage involves at least one course of the integrated therapy aiming at inflammatory response suppression and pain syndrome arrest. The second stage involves at least one session of focused extracorporeal shock wave therapy to create microcavities buried in a interarticular cartilage. At the third stage, the created microcavities buried in the interarticular cartilage are filled with a modelling compound by interarticular electrophoresis followed by stabilising the modelling compound. The modelling compound is represented by a mixture of 15 portions of fine biopolymer gel, 65 portions of hyaluronic acid, 15 portions of animal's articular cartilage extracts and 5 portions of Dimexidum solution. The modelling compound is stabilised by non-invasive exposure to pulse high-power IR laser at wave length 785 nm and heated to 44 Celsius degree.
EFFECT: method provides high clinical effectiveness to be implemented in outpatient care that enables avoiding a surgical intervention, including joint replacement, and ensuring complete removal ensured by possibility of recovery of shape, volume and normal consistence of the interarticular cartilage.
SUBSTANCE: presented group of inventions refers to medicine. What is presented is application of IL-1β binding antigen for producing a drug preparation for treating juvenile rheumatoid arthritis in a patient, containing at least one antigen-binding centre which involves a first domain having an amino acid sequence specified in SEQ ID NO:1, and a second domain having an amino acid sequence specified in SEQ ID NO:2. What is presented is a pharmaceutical composition containing said antibody in a combination with pharmaceutically acceptable excipients, solvents or carriers introduced parenterally.
EFFECT: presented group of inventions provides new application of IL-1β binding antibody for treating juvenile rheumatoid arthritis, particularly systemic idiopathtic juvenile rheumatoid arthritis in mammals, particularly in a human.
10 cl, 3 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed invention relates to pharmaceutical industry, in particular to composition for prevention or therapeutic treatment of inflammatory and/or degenerative condition. Composition for local application for prevention or therapeutic treatment of inflammatory and/or degenerative condition, including (i) woundwort or obtained from woundwort compound or its analogue or derivative, and (ii) tannic acid or its analogue or derivative. Method of prevention or therapeutic treatment of inflammatory and/or degenerative condition (versions). Application of composition for local application for production of medication for prevention or therapeutic treatment of inflammatory and/or degenerative condition. Set, including in two or more containers (i) tannic acid or its analogue or derivative and (ii) woundwort or obtained from woundwort compound or its analogue or derivative or any their combination. Set, including container, which includes composition for local application.
EFFECT: composition possesses synergetic pharmacological effect.
41 cl, 17 ex
SUBSTANCE: invention refers to a compound of formula (I) or to its pharmaceutically acceptable salt: formula (I) wherein; R1 represents hydrogen; R2 represents phenyl, benzothienyl, benzofuranyl or the group -CH2CH2-phenyl; wherein R2 is optionally substituted by 1 or 2 substitutes optionally specified in F, O, Br, I, -CN, -NO2, -OR8, C1-C6alkyl and -N(R9)2; R4 represents phenyl substituted by 1 or 2 substitutes optionally specified in F, CI, Br, I, -CP3, -OH, -OR8 and C1-C6alkyl; each R8 is optionally specified in C1-C6alkyl; and each R9 is optionally specified in H and C1-C6alkyl. The invention also refers to a pharmaceutical composition for activity modulation of depot-controlled calcium channels (SOC-channels) containing such compounds.
EFFECT: there are produced new compounds and based pharmaceutical compositions which can find application in medicine for treating the diseases or conditions, such as rheumatoid arthritis, psoriasis, inflammatory intestinal disease, asthma and multiple sclerosis.
12 cl, 21 dwg, 1 tbl, 14 ex
SUBSTANCE: invention relates to medicine, namely to diseases of locomotive apparatus and can be applied for treatment of acute or chronic tendovaginitis. Ultrasonic scanning (US) of inflamed synovial bursas is performed to patient. During examination under local anesthesia with solution of 2% lidocaine puncture of bursa and suction of content with the following inoculation on medium for verification of causative agent and sensitivity to antibiotics are performed. Synovial bursa is washed with solutions of antiseptics with following introduction into its cavity of target antibiotics, dissolved in 1% solution of novocaine. Then, after thirty minutes after achiving anesthetic effect of novocaine absorption, patient performs flexion-extention movements. Procedure is carried out two times per day with interval in twenty hours.
EFFECT: claimed method of tendovaginitis treatment is simple in application, reduces temporary disability, has strongly pronounced cosmetic effect and can be recommend to wide range of practicing doctors of hospital or clinic.
SUBSTANCE: invention relates to medicine, in particular to traumatology, and deals with elaboration of problems of treating traumatic affection of joints. Results, carried out in experiment, make it possible to suggest the following method of treating intraarticular fractures. Immobilisation of joint with recovery of anatomically correct interrelationship, stabilisation and further training movements in joint by means of apparatus of external fixation are performed. After recovery of anatomically correct interrelationship, not later than 3 days after trauma, joint surfaces are brought apart for the width which up to 50% exceeds the width of joint space of unaffected joint. During 4-5 days 24-hour drop-by-drop introduction of 0.9% sodium chloride solution into joint cavity is performed. Simultaneously one time per day freshly prepared solution consisting of 40% glucose solution, 5% ascorbic acid solution and autologic blood plasma, taken in volume ratio 1:2:7.
EFFECT: method ensures considerable reduction of fracture treatment terms in comparison with such treated by method of tranosseous osteosynthesis with application of apparatuses of external fixation due to enhancement of reparative regeneration processes.
SUBSTANCE: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts possessing the properties of a MMP12 inhibitor, a method for preparing them, an intermediate compound of formula (III), a pharmaceutical composition, a method for preparing it, using the compounds of formula (I) and versions of methods of treating with the use of the compounds of formula (I). The compounds may be used for treating the MMP12-mediated diseases, such as chronic obstructive pulmonary disease. In formula (I) and (III) R1 represents H, CH3, CH3CH2, CF3 or cyclopropyl; and R2 represents H or CH3.
EFFECT: higher clinical effectiveness.
15 cl, 1 tbl, 6 ex
SUBSTANCE: invention relates to composition for pain treatment, as well as for treatment of osteoarthritis in patient with joint pain. Claimed composition includes 0.1-10 wt % of non-steroid anti-inflammatory compound - sodium diclofenac or sodium diclofenac solution, 25-60% wt dimethylsulfoxide, ethanol, propylene glycol, thickening agent, selected from hydroxypropylcellulose and polymers-carbomers and glycerol in case of thickening agent is carbomer, water and has viscosity equal to 500-5000 centipoise. Invention also relates to medication for treatment pain, as well as treatment of osteoarthritis in patient, with joint pain, which contains said composition.
EFFECT: invention ensures excellent means of sodium diclofenac delivery through skin, which demonstrates better duration of drying, greater viscosity, greater pharmacokinetic absorption in vivo and which can be applied for topic pain treatment.
13 cl, 12 dwg, 17 tbl, 8 ex
SUBSTANCE: invention refers to medicine, namely traumatology and orthopaedics, and is applicable for the purpose of the integrated treatment of posttraumatic knee arthritis. For this purpose, the final stage of the operation involves knee sanation with ozonised physiologic saline in the concentration of 2 mg/l, from the following postoperative day five intra-articular injections of the ozone-oxygen mixture 5 mg/l every second day are prescribed. The ozone therapy is combined with three intra-articular injections 8 mg, once every 4 days.
EFFECT: invention enables higher joint resistance to regional tissue hypoxia, reduced inflammation, prevented developing destructive dystrophic changes and stimulated reparative processes in the involved joint tissues.
SUBSTANCE: invention relates to a novel heteroaryl-substituted derivative of benzothiazole - 2-[6-(methylamino)pyridin-3-yl]-1,3-benzothiazol-6-ol where one or more atoms may be a detectable isotope, in form of a free base or pharmaceutically acceptable salt thereof, capable of binding with amyloid deposits, to pharmaceutical compositions based on the radioactive-labelled disclosed compound, to use of the detectable isotope-labelled disclosed compound for determining amyloid deposits, as well as use of the disclosed compound in producing a medicinal agent for preventing and/or treating Alzheimer's disease and familial Alzheimer's disease. The present invention also relates to a novel intermediate compound for producing the disclosed heteroaryl-substituted benzothiazole derivative
EFFECT: high efficiency of using the compounds during treatment.
15 cl, 1 tbl, 15 dwg, 82 ex
SUBSTANCE: invention relates to a compound of formula in which: X denotes S, N-R5 or O; R denotes H; alkyl; heteroaryl, which is a thienyl optionally substituted with alkyl; R1 denotes alkyl; aryl, optionally substituted with a halogen; heteroaryl which is a thienyl optionally substituted with an alkyl, a a halogen, a methoxy group; R2 denotes heteroaryl which is 2-, 3- or 4-pyridyl; R3 denotes H; aryl, optionally substituted with a halogen, a methoxy group; heteroaryl, which is a thienyl optionally substituted with a halogen; alkyl, optionally substituted with oxytetrahydropyranyl; R4 denotes H; R5 denotes H; alkyl; or salt thereof.
EFFECT: invention also relates to a method of producing said compounds, which can be used as antifungal agents for crops, as well as agents against other pests, such as insects or mites and weeds which can harm crops.
10 cl, 7 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: present inventions refers to a new crystalline form of tetomilast hydrate of the X-ray powder diffraction spectrum having characteristic peaks at the angle 20=10.6°, 12.9°, 21.1°, 22.3° and 25.0°, to a new crystalline form of anhydrous tetomilast type C of the X-ray powder diffraction spectrum having characteristic peaks at the angle 2θ=4.2°, 8.2°, 12.0°, 16.4°, 24.7° and 25.9°, to a new crystalline form of acetonitrile tetomilast solvate of the X-ray powder diffraction spectrum having characteristic peaks at the angle 2θ=3.6°, 7.1°, 10.6°, 14.2° and 24.8°, to based pharmaceutical compositions and to methods for preparing.
EFFECT: new crystalline forms shows useful processing characteristics with relation to preparing pharmaceutical drugs of them.
13 cl, 14 dwg, 8 ex
SUBSTANCE: invention relates to novel compounds of formula
where: X is a nitrogen or carbon atom; Ar is phenyl or a heteroaromatic ring selected from pyrazolyl, furanyl, thiophenyl and isoxazolyl; R1 is hydrogen, halogen, CN or (C1-C4)alkyl; R2 is halogen or (C1-C3)alkoxy optionally fluorinated with 1-3 fluorine atoms; R3 and R5 independently denote hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkenyl or hydroxymethyl; R4 is hydrogen, halogen, optionally fluorinated (C1-C4)alkoxy or aryl(C1-C4)alkoxy; R6 is hydrogen, optionally fluorinated (C1-C4)alkyl; each R7 independenlty denotes hydrogen, halogen, optionally fluorinated (C1-C4)alkyl or (C1-C4)alkoxy optionally fluorinated with 1-3 fluorine atoms; or pharmaceutically acceptable acid addition salts thereof. The invention also relates to use of compounds of formula (I) in a pharmaceutical composition and when preparing a medicinal agent meant for treatment, the aim of which is to change the secondary signal activity level after activation of glucocorticoid receptors.
EFFECT: compounds of formula I for changing the secondary signal activity level after activation of glucocorticoid receptors.
7 cl, 5 dwg, 49 ex
SUBSTANCE: invention relates to a compound of formula
where R1 is a phenyl group (said phenyl group is substituted with one or more C1-6alkyl groups, one C1-3alkyl group (said C1-3alkyl group is substituted with one or more halogen atoms), one C1-3alkoxy group (said C1-3alkoxy group is substituted with one or more halogen atoms) or one or more halogen atoms), R2 is a C1-3alkyl group, R3 is a phenyl group (said phenyl group is substituted with one or more substitutes selected from a group comprising halogen atoms or a (C=O)R5' group (where R5' is NR6'R7', (where R6' is a hydrogen atom, and R7' is a C1-6alkyl group substituted with a hydroxyl group))), a thienyl group (said thienyl group is substituted with one or more substitutes selected from a group comprising hydrogen atoms and a (C=O)R5 group (where R5 is NR6R7 (where R6 is a hydrogen atom or a C1-3alkyl group, and R7 is a C1-6alkyl group (said C1-6alkyl group can be substituted with one or more hydroxyl groups, one C1-3alkoxy group or a 5-6-member aromatic heterocyclic group containing 1-2 heteroatoms selected from oxygen or nitrogen (where the 5-6-member aromatic heterocyclic group can be substituted with one or more C1-3alkyl groups, one or more C1-3alkoxy groups, and in case of a 5-6-member aromatic heterocyclic group containing one nitrogen atom, can be in be in form of N-oxides)), a pyridyl group, or overall NR6R7 is a nitrogen-containing heterocyclic group which is a 5-6-member hetero-monocyclic group which contains one or two nitrogen atoms and can additionally contain on oxygen atom (said nitrogen-containing heterocyclic group can be substituted with one or more hydrogen atoms, one or more C1-6alkyl group, one or more hydroxyl groups)) or C1-6alkyl group (said C1-6alkyl group can be substituted with one or more halogen atoms and is substituted with one cyano group))), and R4 is a hydrogen atom or to a pharmaceutically acceptable salt of said compound. The invention also relates to a medicinal agent for preventing or treating diseases, in which activation of the thrombopoietin receptor is effective, based on said compounds.
EFFECT: obtaining novel compounds and agents based thereon, which can be used in medicine to increase the number of thrombocytes.
33 cl, 7 tbl, 43 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed invention relates to chemical-pharmaceutical industry. Pharmaceutical compositions including, at least, one compound of formula where -X- represents, for instance, group of formula and Y represents, for instance, group of formula or its pharmaceutically acceptable salts, esters or amides, or pro-drugs and pharmaceutically acceptable carrier, which is acceptable in therapy, can be applied for modulation in vitro and in vivo processes of binding, mediated by binding of E-, P- or L- selectin.
EFFECT: obtaining novel floroglucin derivatives.
9 cl, 10 ex, 3 tbl
SUBSTANCE: invention refers to medicine, namely to therapy and parasitology, and can be used for treating patients with chronic glomerulonephritis (CGN) combined with chronic opisthorchiasis (CO). That is ensured by introducing a cytoprotector and an antiaggregant, namely Chopytol 0.4 g 4 times a day 30 minutes before meals combined with ticlopidine 0.25 g 2 times a day for 3 weeks. If observing the improvement of the haemostatic system and urine analysis values, the therapy is prolonged for 4 weeks in the previous regimen; while the improvement of the haemostatic system and urine analysis values requires prescribing Chopytol 0.4 g 3 times a day for 3 weeks with underlying administration of ticlopidine 0.25 g 2 times a day. If necessary, the therapeutic course is repeated 6 months after.
EFFECT: method allows enabling more evident and permanent therapeutic effect ensured by the correction of endothelial, hemostatic and hepatobiliary dysfunctions in the patients suffering CGN combined with CO with reduced adverse reactions.
2 ex, 2 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to application of thienopyridone derivatives of formula (I), in which B represents CH, represents , or , R represents H, R1 and R2, independently on each other, represent H, linear or branched (C1-C4)alkyl, (C1-C4)cycloalkyl, halogen or together form group -(CH2)n-, where n=1- 4, R3 and R4, independently on each other, represent H, R6 represents H, X represents -O-, or their pharmaceutically acceptable salts for preparation of pharmaceutical composition.
EFFECT: obtaining pharmaceutical composition, suitable for treatment of diabetes, metabolic syndrome and obesity.
8 cl, 1 tbl, 210 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed invention relates to compound of formula I: where: R1 represents R6C(O)-, R6SO2-, (R6)2NC(O)-; R2 represents hydrogen, -CF3 or R8; R3 represents -T-R9; R4 represents -COOH or -COOR8; R5 represents -CH2F or -CH2O-2, 3, 5, 6 - tetrafluorophenyl; R6 represents R6a or R6b; two R6 groups, together with the atom to which they are bound optionally form 3-10-member aromatic or non-aromatic ring; and where each R6 is independently substituted with 6 substituents, independently selected from R; R6a and R6b each independently represents (C1-C3)-aliphatic group, (C6-C10)-aryl-, (C6-C10)-aryl-(C1-C12) aliphatic group; R represents halogen, -OR7, -R7; each R7 is independently selected from: hydrogen, (C1-C12)-aliphatic group, (C6-C10)-aryl; R8 represents (C1-C12)-aliphatic group; T represents direct bond or (C1-C6)-aliphatic group, where to 2 aliphatic carbon atoms in T can be optionally substituted with O; R9 is optionally substituted (C6-C10)-aryl or (C5-C10) - heteroaryl, invention also relates to pharmaceutical composition, to methods of treatment, inhibition of caspase-mediated processes, to method of cell preservation with application of formula I compounds application of such compositions for treatment of caspase-mediated diseases and to methods of obtaining formula I compounds.
EFFECT: obtained and described are novel compounds, which can be useful in treatment of caspase-mediated diseases.
38 cl, 22 ex
FIELD: organic chemistry, medicine.
SUBSTANCE: invention relates to new 2-aminopyridine derivatives of formula I , wherein R1 is cyano, carboxyl or carbamoyl; R2 is hydrogen, hydroxyl, C1-C6-alkoxy or phenyl; R3 and R4 are aromatic hydrocarbon such as phenyl or naphthyl, 5-14-membered 5-14-membered optionally substituted aromatic group, excepted cases, when (1) R1 is cyano, R2 is hydrogen, and R3 and R4 are simultaneously phenyl;(2) R1 is cyano, R2 is hydrogen, R3 is 4-pyridyl, and R4 is 1-pyridyl; (3) R1 is cyano, R2 is 4-methylphenyl, and R3 and R4 are simultaneously phenyl;(4) R1 is cyano, R2, R3 and R4 are simultaneously phenyl, or salts thereof. Derivatives of present invention have adenosine receptor antagonist activity and are useful in medicine for treatment of irritable bowel syndrome, constipation, and defecation stimulation.
EFFECT: 2-aminopyridine derivatives as adenosine receptor antagonists useful in medicine.
34 cl, 2 tbl, 179 ex