Drugs for skeletal disorders (A61P19)

A   Human necessities(312083)
A61P19                 Drugs for skeletal disorders(1030)
ethod of conservative treatment of osteochondrosis // 2642253
FIELD: medicine.SUBSTANCE: method includes introducing vitamin B12. According to the invention, vitamin B12 is administered with 0.5% novocaine in the interstitial spaces to a depth up to the yellow ligament at a dose of 500 μg/ml.EFFECT: use of the invention makes it possible to accelerate and prolong analgesia by introducing into the depth to the yellow ligament.1 ex

ethod for degenerative-dystrophic spine diseases (dorsopathies) treatment // 2640001
FIELD: medicine.SUBSTANCE: method includes three main steps. The first is the compensatory stage, which uses known methods of combined drug treatment, aimed at a transfer to a subacute or compensated stage of the disease. At the recovery stage, chondroptic peptide bioregulators VitOrgan are introduced according to a certain scheme. The bioregulators are injected slowly by jets based on 0.5% novocaine solution or saline solution mixed with 10 ml of 30% sodium thiosulfate solution up to 20 ml. Or dropwise introduction is performed, while the drug is dissolved in 100 or 200 ml of saline solution, or 200 ml of Reamberin, introduction rate is 50-60 drops per minute. Intravenous drugs administration is combined with subcutaneous or intramuscular administration of peptide bioregulators, including in combination with vascular and vasoactive agents. The rehabilitation phase involves the use of techniques such as massage, manual and osteopathic treatment techniques, physical therapy, therapeutic exercises, as well as methodologies aimed at body purification. Peptide bioregulators, vasoactive drugs and chondroprotectors are also used.EFFECT: method allows to significantly accelerate the process of patient recovery and achieve a lasting result.23 cl, 2 ex, 4 dwg

Application of growth hormone fragments // 2639474
FIELD: medicine.SUBSTANCE: subject receives an effective amount of peptide with a length from 8 to 50 amino acid residues containing amino acid residues of 182-189 human growth hormone, or growth hormone of another kind of animal, or a site of any of SEQ ID NO:1-41. This peptide does not contain the growth hormone domain responsible for IGF-1 production. A method for stimulation of chondrocytes or cartilaginous tissue formation or recovery is also provided.EFFECT: treatment of a state associated with chondrocytes of cartilage function failure by stimulating the production of collagen and proteoglycan in cartilage tissue.22 cl, 16 dwg, 9 ex

Sterilized composition containing at least one hyaluronic acid and magnesium ascorbyl phosphate // 2639136
FIELD: pharmacology.SUBSTANCE: invention is a sterilized composition used in the cosmetic or pharmaceutical field containing at least one crosslinked hyaluronic acid having a crosslinking ratio of X of 0.1 to 0.2 or one of its biologically acceptable salts individually or in a mixture and magnesium ascorbyl phosphate with mass ratio between the content of hyaluronic acid or one of its salts [HA] and magnesium ascorbyl phosphate [MAP], [HA]/[MAP] content exceeding or equal to 1, the magnesium ascorbyl phosphate content being in the range m 0.03 to 1 wt % based on the total weight of the composition, the elasticity G' of which is maintained or increased after sterilisation and is in the range of 5 to 400 Pa.EFFECT: improvement or preservation of the rheological characteristics of the elasticity index after sterilisation.22 cl, 2 dwg, 12 tbl, 17 ex
Indasole inhibitors of wnt signal path and their therapeutic applications // 2638932
FIELD: medicine.SUBSTANCE: invention relates to a indasole derivative that has the following formula , or its pharmaceutically acceptable salt, as well as a pharmaceutical composition containing it. The invention relates to methods for treatment of disorders characterized by the activation of Wnt-signalling pathways (e.g., cancer, abnormal cell proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), including introduction of a therapeutically effective amount of this compound or pharmaceutically acceptable salt thereof. This compound can also be used in modulation of cellular events, mediated by Wnt-signalling, as well as for treatment of genetic diseases and neurological conditions/disorders/diseases due to mutations or disregulation of the Wnt pathway and/or one or more components of Wnt-signalling.EFFECT: inhibits the Wnt signalling pathway and can be used to treat various diseases and pathologies.28 cl, 8 tbl, 8 ex

ethod for obtaining of two-component preparation for treatment of joints damage by low-invasive introduction into joint bag and preparation obtained by this method // 2638796
FIELD: medicine.SUBSTANCE: method for obtaining of a two-component preparation for treatment of joint damage by low-invasive insertion of the said preparation into the joint bag, in the form of two components, the main and initiating, consisting in the fact that, in order to obtain the main component of the preparation, the blood plasma is transferred with a syringe and a transient filter with a pore size sufficient to ensure sterility, to one of the departments of the cryopack and kept until complete freezing, then the frozen blood plasma is partly defrosted, the first thawed plasma fraction is transferred to the empty compartment of the cryopack and removed from the cryopack by a syringe connected to the pack port, and the cryoprecipitate of the blood plasma remaining in the cryopack is thawed, then the cells which are chondrocyte precursors, are resuspended in the cryoprecipitate of the blood plasma in an amount sufficient to provide a therapeutic effect, and to make the initiating component of the preparation, solution of calcium chloride and thrombin is mixed in a balanced saline solution with addition of aminocaproic acid in an amount not exceeding the maximum recommended dose for a single administration in the joint bag, under certain conditions. A two-component preparation for treatment of joint damage.EFFECT: method allows for cells localization at the site of administration, allowing the cells to migrate from the glue to the damage site and maintain functional activity.8 cl, 5 dwg
Compounds of thienopyrimidine // 2637925
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula I: , where group A is independently monocyclic or bicyclic aryl or heteroaryl optionally substituted by one or more A'; each group A' is independently C1-6 alkyl, halogen, cyano or heteroaryl; group R1 is tetrahydropyranyl substituted with an amino group; or pharmaceutically acceptable salts thereof, which are SYK inhibitors and are useful for treatment of autoimmune and inflammatory diseases.EFFECT: increased efficiency of treatment.10 cl, 2 tbl, 25 ex

System for dosed distribution // 2637420
FIELD: medicine.SUBSTANCE: systems and methods for controlled dosage of a composition comprising sodium diclofenac contained in a dispensing distribution system are provided. The method includes pressing of a manual pump to dispense a dose of a topical anaesthetic in a viscous solution where the manual pump is configured to dispense a dose within the tolerance indicated by the appropriate instruction approved by the government regulatory authority and topical solution distribution over the skin.EFFECT: systems and method allow to treat the signs and symptoms of osteoarthritis.12 cl, 5 dwg, 6 tbl, 4 ex
ethod for prevention of remote postoperative complications in patients with connective tissue dysplasia // 2637401
FIELD: medicine.SUBSTANCE: method according to the invention includes conducting a short-wave physiotherapy on the surgery area, 10 minutes for 22 days from surgery, with 1 day interruptions. As a medicamentous effect, application of Chondroxide ointmentand oral administration of Nycomed in average age dosages are used, while the duration of the combined physiotherapeutic and medicamentous effects should not exceed 12 days, and the repeated course of treatment is carried out no earlier than 3 months after the end of the previous exposure.EFFECT: improved prevention of distant postoperative complications in patients with connective tissue dysplasia.2 ex
Pharmaceutical composition for thermal injuries and wounds treatment in combination with bone damage // 2636227
FIELD: pharmacology.SUBSTANCE: pharmaceutical composition for treatment of wounds complicated by bone damage, which consists of 4 wt % to 12 wt % of beeswax and 88 wt % to 96 wt % of an extract obtained with sesame oil from initial ingredients including Radix Scutellariae, Coptis Chinensis, Cortex Phellodendri, Pericarpium Papaveris and Lumbricus, based on the total weight of the composition. Individual content of each of Radix Scutellariae, Coptis Chinensis, Cortex Phellodendri, Pericarpium Papaveris and Lumbricus, based on their dry weight, ranges from 1% to 6% of the total weight of sesame oil, respectively. Application of the pharmaceutical composition for manufacture of a drug for treatment of a thermal injury complicated by bone damage. A pharmaceutical composition for treatment of a thermal injury complicated by bone damage. A method for treatment of open injuries complicated by a fracture, a deep thermal injury with bone damage or bone necrosis.EFFECT: composition has increased effectiveness for treatment of wounds and thermal injuries complicated by bone damage.9 cl, 31 dwg, 8 ex
Probiotic strains for application in osteoporosis treatment or prevention // 2636027
FIELD: biotechnology.SUBSTANCE: application of the probiotic strain Lactobacillus paracasei 8700:2, DSM 13434 and the use of the strain Lactobacillus paracasei 8700:2, DSM 13434 in combination with at least one of Lactobacillus plantarum strains for osteoporosis treatment or prevention, bone tissue treatment or prevention, for Ca2+ ions absorption increase in a mammal. Application of the probiotic strain Lactobacillus paracasei 8700:2, DSM 13434 in combination with Lactobacillus plantarum HEAL 9, DSM 15312 and Lactobacillus plantarum HEAL 19, DSM 15313 for osteoporosis treatment or prevention, bone tissue treatment or prevention, for Ca2+ ions absorption increase in a mammal is proposed.EFFECT: reduced cortical bone loss in treatment of postmenopausal osteoporosis.24 cl, 6 dwg, 3 tbl, 4 ex
ethod for treating inflammatory and exchange-dystrophic diseases of musculoskeletal system by optimal combination of cryotherapy, physiotherapy and medical exposure methods (versions) // 2633493
FIELD: medicine.SUBSTANCE: two method versions of optimal combination of cryotherapy, physiotherapy and medical exposure methods are proposed. In order to implement the first version of the method, at first the total cryotherapy is carried with ultralow temperatures from minus 120 to minus 170 degrees Celsius by subtotal immersion of the patient in an open-circuit chamber (cryosauna). 5-10 minutes after the patient leaves the cryosauna, local cryotherapy is carried out at minus 170 degrees Celsius. 10-15 minutes after the local cryotherapy, ultraphonophoresis is performed on the affected joints with ointment, which contains proteolytic enzymes of papaya - Papain or Karipazim. In order to carry out the second version of the method, a complex treatment is also carried out, including 24 procedures for joint diseases and 30 procedures for spine diseases. At first the total cryotherapy is carried out with ultralow temperatures from minus 120°C to minus 170°C by subtotal immersion of the patient in an open-circuit chamber (cryosauna). Then, 5-10 minutes after the patient leaves the cryosauna, local cryotherapy is carried out at minus 170°C. Then, 10-15 minutes after the local cryotherapy, ultraphonophoresis is performed on the affected joints with ointment, which contains Papain or Karipazim. Starting from the sixth procedure of ultraphonophoresis, an additional electrophoresis is performed with Papain or Karipazim from the positive electrode and euphyllin or potassium iodiom from the negative electrode.EFFECT: achievement of pronounced analgesic and anti-inflammatory effects, a decrease in the activity of the inflammatory process and the achievement of disease remission, an effect on the immunological status.6 cl, 9 ex
Pyrazole derivative // 2632884
FIELD: pharmacology.SUBSTANCE: in the above formula , A represents a phenyl group which may be unsubstituted or substituted by 1 to 3 Q groups which are identical or different and are selected from the group consisting of a halogen atom, C1-6alkyl, C3-7cycloalkyl, C1-6haloalkyl, phenyl, -O-R2 and -O-C1-6haloalkyl; X and Z are CH and Y is a nitrogen atom; R is a hydrogen atom; R1 is a hydrogen atom and R2 is a hydrogen atom or C1-6alkyl group.EFFECT: compound has an inhibitory effect on xanthine oxidase, is well suited for treatment or prevention of diseases associated with xanthine oxidase such as gout, hyperuricemia, tumor lysis syndrome, stones in the urinary tract, hypertension, dyslipidemia, diabetes, cardiovascular disease, kidney disease, respiratory tract disease, autoimmune diseases, inflammatory bowel disease.10 cl, 7 tbl, 112 ex
Tricyclic heterocyclic compounds and jak inhibitors // 2632870
FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the formula : , where the Aa ring is represented by the following formula , where T1a is a nitrogen atom, U1a is a nitrogen atom, Xa is CR9a (where R9a represents a hydrogen atom), Ya a is CR10a (where R10a is a hydrogen atom), R1a is a hydrogen atom, ring Ba is C4-7cycloalkane, benzene or a 4 to 6-membered non-aromatic heterocycle containing 1 heteroatom selected from a nitrogen atom, L1a is a single bond, L2a is a single bond, C1-3 is an alkylene group (C1-3 alkylene group is unsubstituted or substituted by a cyano group) or C1-3 halogenoalkylene group, L3a is a single bond or is represented by any of the following formulas: na is 0 or 1, R3a is a hydroxy group, a halogen atom, a cyano group or a methyl group, the remaining radicals are as defined in the claims. The invention also relates to a compound represented by the formula (Ib), to a JAK inhibitor containing the compound of the invention, to a preventive, therapeutic or improving agent for diseases in which JAK inhibition is effective, to a drug.EFFECT: new compounds with inhibitory activity against JAK are obtained.36 cl, 236 tbl, 611 ex
ethod for rehabilitation of patients with combined lesion of spine and large joins as due to production injury at early stage // 2632807
FIELD: medicine.SUBSTANCE: in the patient's abdominal position, the points of greatest pain are detected along the spine in the area of the affected segments by palpation. Up to 2 ml of ozone is injected subcutaneously into the points with a needle. The patient is transferred to a position on the back. By palpation, the points of greatest pain in the affected joints are found. Up to 2 ml of ozone is injected subcutaneously into the points with a needle. No more than two joints are involved in the procedure. After 40-60 minutes, ultraphonophoresis (UPP) of NEOPANT-forte pantogel is performed, for which a layer of pantogel is first applied to the exposure area, and a contact gel or lanolin layer is applied from above. Labile ultrasound exposure is provided in the patient's position on the back on the surface of the affected joint, moving the emitter at a speed of 1-2 cm/s in contact, with intensity of 0.7-0.8 W/cm2, in a continuous mode, 5 minutes per surface. In the position on the abdomen, in the region of the affected vertebral column segments, paravertebrally from CIII to DIII and/or from L1 to L5, depending on the level of lesion, 2 cm to the right and left of the spinous vertebrae protuberances, exposure is provided by moving the ultrasound emitter at a spped of 1-2 cm/s in contact, labile, with an intensity of 0.2 W/cm2, pulse mode: 2-4 ms, 3 minutes per field. After 2-4 hours, a general radon bath procedure is performed, or, in case of concomitant heart pathology, a four-chamber radon bath for the limbs. Radon concentration is 40 nCu/l, water temperature is 36°C, bath time is 10 minutes, for a course of 8 daily procedures.EFFECT: increased effectiveness and quality of treatment, increased remission period for early rehabilitation.4 tbl, 2 ex
ethod for treating knee osteoarthrosis deformans // 2632621
FIELD: medicine.SUBSTANCE: at the first treatment session, a mixture containing 1 ml of diprospan suspension and 2 ml of a 2% lidocaine solution is injected into the tender points in the projection of the medial meniscus of knee joint which are determined by palpation. 3 ml of the mixture is divided into the identified tender points and injected into the points in equal amounts. After the mixture is injected, acupuncture is performed at points Rp 9, Rp 10, E 36 with steel needles for 20 minutes. At the second session, 2.2 ml of Traumeel C preparation is injected into the tender points in the projection of the medial meniscus of knee joint, which are divided in equal amounts into the number of detected tender points, and then this acupuncture is performed.EFFECT: reduction of treatment time due to rapid relief of pain syndrome, inflammatory phenomena, improvement of trophism of tissues and normalization of blood circulation in the area of the affected limb and increase in functional activity in the affected joints.5 cl, 2 ex
Oxy133 oxysterol analogue inducts osteogenesis and signal way hedgehog and inhibited lipogenesis // 2632191
FIELD: chemistry.SUBSTANCE: invention relates to an Oxy133 compound having the formula I . The invention also relates to a bioactive composition, to methods of treatment and to a method for inducing osteoblastic differentiation and/or inhibiting the differentiation of adipocytes of mesenchymal stem cells of mammals.EFFECT: new compound has been obtained that is useful for the treatment of bone disease, for increasing osteoporrelation and/or osteoproliferation, to stimulate bone formation, to induce osteoblastic differentiation, or to inhibit the differentiation of adipocytes of mesenchymal stem cells.8 cl, 15 dwg, 2 tbl, 4 ex
Application of avocado peel for receiving unsaponifiable avocado product enriched with saturated aliphatic hydrocarbons and sterols // 2632111
FIELD: pharmacology.SUBSTANCE: method for producing an unsaponifiable product from an avocado, enriched with saturated aliphatic hydrocarbons and sterols, at least from the avocado peel, wherein said avocado peel is 5 to 50 wt % of the total weight of the avocado used, which includes the following consecutive steps: (1) cutting or grinding avocados. This avocado contains from 5 to 50 wt % of peel, (2) high-temperature drying at a temperature of 60 to 150°C to obtain residual moisture, (3) adding water to the dried avocado by adding 1 to 5% water or steam to the weight of the dried avocado, (4) extracting the oil by mechanical pressing, and then (5) alternatively: - a. Heat treatment of extracted oil at a temperature of 80 to 150°C and then enrich the oil with its unsaponifiable fraction, or - b. Enrichment of oil with its unsaponifiable fraction and then heat treatment at a temperature of 80 to 150°C, (6) followed by a saponification and extraction step of the unsaponifiable product, (7) at least a purification and/or fractionation step, and (8) recovering the unsaponifiable product, wherein the unsaponifiable avocado product contains at least 0.2 wt % of saturated aliphatic hydrocarbons and at least 1 wt % of sterols from the total mass of unsaponifiable product. A non-saponifiable product of avocado enriched with saturated aliphatic hydrocarbons and sterols for use as a medicament for the prevention and/or treatment of connective tissue diseases, arthrosis, joint pathologies, rheumatism or periodontal disease, gingivitis or periodontitis. The above unsaponifiable avocado product contains at least 0.2 wt % of saturated aliphatic hydrocarbons and at least 1 wt % of sterols from the total mass of unsaponifiable product.EFFECT: increased application efficiency.10 cl, 2 tbl, 8 ex
ethod for hydroxyapatite-collagene composite production // 2631594
FIELD: medicine.SUBSTANCE: hydroxyapatite obtained by the condensation method using a hydroacoustic transducer is mixed with collagen, the resulting hydroxyapatite-collagen mixture is homogenized in an ultrasonic field at a frequency of (22÷44) kHz, power density of (1÷10) W/m3 within (10÷400) s.EFFECT: hydroxyapatite-collagen composite is suitable for filling bone defects and forming bone implants with predetermined dimensions and shape.2 ex

Crystalline forms of [(s)-1-carbamoyl-2-(phenylpyrimidin-2-ylamino)ethyl]amide 2-(2-methylaminopyrimidin-4-yl)-1h-indole-5-carbonic acid // 2631320
FIELD: chemistry.SUBSTANCE: invention relates to the novel polymorph 1 ((S)-1-carbamoyl-2-(phenylpyrimidin-2-ylamino)ethyl]amide 2-(2-methylaminopyrimidin-4-yl)-1H-indole-5-carboxylic acid and method for its preparation. Polymorph 1 of the compound has the properties of IkB kinase inhibitors and can be used for the treatment of inflammatory, immunologically or metabolically mediated acute and chronic arthritis, arthropathies, rheumatoid arthritis, degenerative joint diseases, spondylosis, diabetes II type, inflammatory bowel disease, loss of cartilage following joint trauma or a relatively long period of joint immobilization after meniscus or patella injuries or torn ligaments, or diseases of the connective tissue, m algy or disorders of bone metabolism, and also for the treatment of pain, including acute pain and chronic pain. Polymorph 1 has characteristic reflections in a powder X-ray diffraction pattern using CuK-alpha1 radiation in the reflection mode at 2 theta angles (in degrees) of 14.9±0.2, 19.4±0.2, 19.7±0.2, 20.0±0.2, 22.3±0.2, 25.0±0.2. The method of producing polymorph 1 involves heating the polymorph 2 of mentioned compound in a mixture of acetone and water to a temperature of 50 to 60°C, cooling the mixture to a temperature of 20 to 25°C and precipitate precipitation. In this case polymorph 2 has a characteristic x-ray powder reflection using CuK-Alpha1 radiation reflection mode with 2 Theta angles (degrees): 5.8±0.2, 6.7±0.2, 9.3±0.2, 11.2±0.2, 16.5±0.2, 18.1±0.2, 19.4±0.2, 22.1±0.2, as well as indicators of DSC peaks 222.1±1; 248.1±1; 251±1 at heating rate 10°C/minute.EFFECT: polymorphic form 1 is thermodynamically stable, has low hygroscopicity and stability.8 cl, 2 tbl, 5 dwg
Applying avocado pit for obtaining avocado oil enriched with aliphatic polyhydric alcohols and/or acetylated derivatives thereof // 2630981
FIELD: food industry.SUBSTANCE: applying avocado seeds to obtain avocado oil enriched with aliphatic polyhydric alcohols and/or acetylated derivatives thereof by mechanical pressing, said seeds being 10 to 50 wt % of the total weight of the avocado used, said aliphatic polyhydric alcohols are saturated, monounsaturated or polyunsaturated trihydric alcohols C17-C21 of the aliphatic linear 1,2,4-trihydroxyl type, where the avocados are ground or cut into slices, and then dried at a high temperature to obtain the residual humidity of less than or equal to 5%, after which 1 to 5% of water or water vapour with respect to the weight of dried avocado are added before obtaining oil by mechanical pressing, and where the avocado oil contains at least 0.5 wt % of aliphatic polyhydric alcohols and/or acetylated derivatives thereof from the total oil weight. Method for obtaining avocado oil enriched with aliphatic polyhydric alcohols and/or acetylated derivatives thereof. Avocado oil enriched with aliphatic polyhydric alcohols and/or acetylated derivatives thereof. Applying avocado oil for preparing avocado oil concentrate. Applying avocado oil to obtain an unsaponifiable avocado product enriched with aliphatic polyhydric alcohols. Unsaponifiable avocado product.EFFECT: products are characterized by an increased content of aliphatic polyhydric alcohols or acetylated derivatives thereof.17 cl, 3 tbl, 9 ex
Nitrogen-containing spirocyclic compound and its application in medicine // 2630694
FIELD: pharmacology.SUBSTANCE: compounds can be used to prepare a medicament for treatment or prevention of a disease selected from the group consisting of organ transplant rejection, graft versus host transplantation, autoimmune disease, allergic diseases and chronic myeloproliferative disease. The disease can be selected from rheumatoid arthritis, psoriasis, atopic dermatitis or a disease caused by dry eyes. In the general formula Ra is the same or different and each represents (1) C1-6 alkyl or (2) a halogen atom, n1 is an integer selected from the integers from 0 to 2, Rb are the same or different and each represents (1) C1-6 alkyl or (2) halogen atom, n2 is an integer selected from the integers from 0 to 2, m1 is an integer selected from the integers from 0 to 3, m2 is an integer selected from the integers from 1 to 4, Xa=Xb is (1) CH=CH, (2) N=CH or (3) CH=N, X is (1) a nitrogen atom or (2) C-Rd, where Rd is a hydrogen atom or halogen atom, Rc is a group selected from the following groups (1)-(6): (1) a hydrogen atom, (2) C1-6 alkyl, optionally substituted with 1-5 same or different substituents selected from the following group A, (3) -C(=O)-Rc1, (4) -C(=O)-O-Rc2, (5) -C(=O)-NRc3Rc4, where Rc1, Rc2, Rc3, Rc4 are the same or different and each represents (i) a hydrogen atom or (ii) C1-6 alkyl, optionally substituted with 1-5 same or different substituents selected from the following group A, or (6) a group of the following formula in which Ya is a group selected from the following groups (i) to(iii) (i) C1-6 alkylene, (ii) -C(=O)- or (iii) -S(=O)-O-, ring T is (i) a phenyl, (ii) C3-10 cycloalkyl or (iii) a saturated monoheterocyclyl, which contains 1 nitrogen atom and carbon atoms, and the number of atoms, constituting the ring, is 3-7, Rc5 is the same or different and each represents (i) cyano, or (ii) a nitro group, p is an integer selected from the integers from 0 to 1, group A is a group, consisting of (a) a hydroxyl, (b) C1-6 alkoxy, (c) a cyano, (d) C1-6 alkoxycarbonyl, (e) C1-6 alkylcarboxylic and (f) C2-6 alkenylacyl.EFFECT: increased efficiency of treatment.60 cl, 33 tbl, 8 ex

Pharmaceutical composition // 2630617
FIELD: pharmacology.SUBSTANCE: pharmaceutical composition for treatment of cyclooxygenase-2 mediated diseases is described. The said composition includes, (2S)-7-tret-butyl-6-chloro-2- (trifluoromethyl)-2H-chromene-3-carboxylic acid as the active substance and a filler selected from tromethamine or meglumine. The filler is used in an amount of 0.5 wt % to 70 wt %. Two versions of the method for preparation of this composition and its application are also described.EFFECT: increased dissolution rate and oral bioavailability of the said composition, including the free form of the said compound.9 cl, 5 dwg, 16 tbl, 6 ex
Pharmaceutical composition forlocomotor disorders treatment // 2630064
FIELD: medicine.SUBSTANCE: invention is a pharmaceutical composition of active substances for an oral dosage form, in the form of a solid dosage form. The invention consists in being a bifunctional drug containing chondroitin sulfate, celecoxib as the biologically active substances and auxiliary substances as the rest, at a certain ratio of components.EFFECT: creation of a drug for oral administration in the form of capsules, which has reparative, anti-inflammatory and analgesic effects and can be used as an independent or auxiliary drug for conditions associated with reduced functions of the musculoskeletal system.3 cl, 1 tbl, 1 ex

ethod for tendon or ligament reconstruction // 2629809
FIELD: medicine.SUBSTANCE: flap is applied to the ligament or tendon, which is flexible and biocompatible, and contains a support layer consisting of collagen sheet that is permeable to the cells, as well as a matrix cell-permeable layer located on the support layer, which is a collagen liner with collagen fibers distributed therein and natural hyaluronic acid dispersed in the free spaces of collagen fibers.EFFECT: restoration of the functional activity of ligament or tendon tissue by maintaining the growth of cells and new tissue formation.18 cl, 12 dwg

Aminomethyl quinolones useful ifor treatment of jnk-mediated disorder // 2629111
FIELD: chemistry.SUBSTANCE: invention relates to new aminomethyl quinolone derivative of formula (I) or its pharmaceutically acceptable salt, where R is -C(=O)A, -C(=O)OA, -C(=O)NHA, -C(=N-C≡N)A, -C(=N-C≡N)NHA or A; A is C1-6-alkyl, phenyl, lower cycloalkyl, adamantyl, heterocycloalkyl selected from benzodioxin, pyrrolidine, piperidine, morpholine or piperazine, heteroaryl selected from pyridine, pyrazole, thiazole, triazole or pyrimidine or bicyclic heteroaryl selected from quinoline, quinazoline, indole, benzothiazole, benzoimidazole or imidazopyridine optionally substituted with one or two A1; each A1 independently represents A2 or A3; each A2 is independently halo or oxo; each A3 is independently C1-6-alkyl, C1-6-alkoxy, phenyl, benzyl, heterocycloalkyl selected from morpholine, piperidine, diazepane, pyrrolidine, azepane or piperazine, bicyclic heterocycloalkyl selected from benzodioxole or diazobicycloheptane, heteroaryl selected from oxazole, triazole, pyrazole, imidazole, thiadiazole, oxadiazole, thiazole or tetrazole, amino, C1-6-alkylamino, C1-6-dialkylamino, amido, C1-6-alkyl ester group, sulfonyl, sulfonamido, -C(=O) or -C(═O)O, optionally substituted by one, two or three groups, selected from halo, hydroxy, C1-6-alkylamino, C1-6-alkyloxy, C1-6-alkyl, C1-6-alkoxy, phenyl, hydroxycycloalkyl wherein cycloalkyl is adamantyl, amino, C1-6-alkylamino, C1-6-dialkylamino, t-butyl complex of carbamic acid ester, (C1-6-alkyl) sulfonyl-piperidinyl or hydroxy- (C1-6-alkyl); R' is H or methyl; X is CX'; X' is H or halo; X1 is H, 2-oxazolyl, dimethylamido or C1-6-alkyl ester group; Y is CH or N; and Y1 is H, halo, C1-6- alkoxy or halo (C1-6alkyl). The invention also relates to particular aminomethyl quinolone derivatives and to the use of said aminomethyl quinolone derivatives.EFFECT: obtained new aminomethyl quinolone derivatives, useful in the treatment of JNK-mediated disorder.15 cl, 2 tbl, 211 ex
Compound as wnt signal inhibitor, its compositions and application // 2627712
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic compound of the general formula (I) or an N-oxide thereof, wherein X1, X2, X3 and X4 independently represent CR4 or N, where 0 or 1 of X1-X4 can be N; Y1, Y2 and Y3 are hydrogen; R1 is selected from hydrogen, , C6 aryl, 6-member heterocycloalkyl containing 2 heteroatoms selected from N and O, and 5- or 6-member heteroaryl containing 1-4 heteroatoms selected from N, O and S, wherein each of C6 aryl, 6-member heterocycloalkyl and 5- or 6-member heteroaryl may be optionally substituted with one R4; R2 is selected from hydrogen, halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl and 6-member heteroaryl may be optionally substituted with one R4. If X5 is N, R2 is selected from halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where each of C6 aryl, and 6-member heteroaryl may be optionally substituted with one R4; each R4 Is independently selected from hydrogen, halogen, cyano, oxo, C1-6 alkoxy, -C(O)OR5, -C(O)R5, C1-6 alkyl. Moreover , C1-6 alkyl may be optionally substituted with 1 to 3 substituents selected from halogen and cyano; R5 is C1-6 alkyl; and where the central structure of Formula I, limited by X5, X6, X7 and X8, is: or The invention also relates to particular compounds, a method for inhibiting the secretion of WNT signalling in a cell, use of a compound of formula (I), a method for treatment of a disorder mediated by WNT. .EFFECT: new heterocyclic compounds have been obtained that are useful for treatment of cancer, fibrosis and osteoarthritis.22 cl
Sulfonamide compounds and their use as tnap inhibitors // 2627701
FIELD: chemistry.SUBSTANCE: invention relates to compounds of Formula I: wherein: Y1 is a bond and Y2 is -N(R6)-; L1 and L2 are each a bond; X1 is =N- or =C(R2)-; X2 is =N- or =C(R3)-; R1 and R4 are independently selected from the group consisting of -F, -Cl, -Br, -CN, -C(O)N(R7)-R8, -C(O)-O-R9, methyl, -OMe, -OCF3, optionally substituted phenyl and optionally substituted 5- or 6-membered heteroaryl; R2, R3 and R5 are hydrogen; R6 is hydrogen; R7 is hydrogen and R8 is selected from hydrogen, optionally substituted C1-C4 alkyl, optionally substituted C3-C6 cycloalkyl or optionally substituted phenyl; either R7 and R8 together with the nitrogen atom to which they are attached form an optionally substituted heterocycloamino which is an optionally substituted pyrrolidine, an optionally substituted piperidine, an optionally substituted morpholine or an optionally substituted piperazine; R9 is selected from hydrogen, optionally substituted C1-C4 alkyl, optionally substituted C3-C6 cycloalkyl or optionally substituted phenyl; A is selected from the group consisting of -C(O)-N(R7)-R8 or -C(O)-O-R9, or A is , R12 and R13 are independently selected from the group consisting of hydrogen, halogen, -CN, -OH, -C(O)-O-R19, optionally substituted C1-C4 alkyl, optionally substituted C3-C6 cycloalkyl optionally substituted with C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, optionally substituted phenyl and optionally substituted 5- or 6-membered heteroaryl, R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4 lkila, C1-C4 haloalkyl, optionally substituted C3-C6 cycloalkyl and optionally substituted phenyl; and R15 represents hydrogen or C1-C4 alkyl; Wherein the substituted group is substituted by -CO2H, nitrile, hydroxyl, C1-C4 alkyl, C1-C4 alkoxy, phenyl, C3-C6 cycloalkyl or diC1-C4 alkylamine, which modulate TNAP activity.EFFECT: improved properties of compounds.14 cl, 1 tbl, 12 ex
Pharmaceutical preparation for rheumatological diseases treatment // 2627424
FIELD: pharmacology.SUBSTANCE: pharmaceutical preparation in the form of a solution for use in rheumatological diseases treatment contains a combination comprising sodium diclofenac or naproxen sodium, betamethasone sodium phosphate and hydroxy-cobalamin sulfate as active substances and benzyl alcohol, propylene glycol, sodium metabisulphite and water for injection as auxiliary components. A method for production of the preparation is described as well.EFFECT: stable, effective formulation with analgesic, anti-inflammatory and antineurotic effects.4 cl, 1 tbl, 4 ex
Aza-aryl-1-h-pyrazol-1-yl-sulphonamides // 2627268
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I) ,in which radicals and characters have values specified in the claims and their versions. The proposed compounds act as potent antagonists of CCR (9) receptor. Animal testing has shown that these compounds are useful for treatment of inflammation, disease with a hallmark for CCR (9). The compounds as a whole are arylsulfamide derivatives and are used in pharmaceutical compositions, methods for treatment of CCR (9) mediated diseases and as a control in assays for identification of CCR (9) antagonists.EFFECT: increased efficiency of compounds application.26 cl, 2 tbl, 33 ex

ethods of production isoquinolinones and solid forms isoquinolinones // 2626883
FIELD: chemistry.SUBSTANCE: invention relates to new polymorphic forms of the compounds of formula (I), having inhibitory action against phosphoinositide 3-kinase (PI3K). The compounds may be used to treat cancer, such as leukemia, lymphoma, inflammatory disease and autoimmune disease. The polymorphic forms of the compound of formula (I) is the polymorphic form C of the hydrate of the compound of formula (I), which has characteristic peaks in the x-ray powder diffraction pattern (XRPD) 2θ=10.4°(±0.2°), 13.3°(±0.2°) and 24.3°(±0.2°); Polymorph A, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.6°(±0.2°), 12.2°(±0.2°), and 18.3°(±0.2°); Polymorph B, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=7.9°(±0.2°), 13.4°(±0.2°), and 23.4°(±0.2°); polymorphic form D, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=11.4°(±0.2°), 17.4°(±0.2°), and 22.9°(±0.2°); polymorphic form E, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=6.7°(±0.2°), 9.3°(±0.2°) and 24.4°(±0.2°); Polymorphic form F, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.6°(±0.2°), 17.3°(±0.2°), and 24.6°(±0.2°); Polymorphic form G which is the solvate of the tert-butyl methyl ether of the compound of formula (I) and has characteristic peaks in the powder XRPD pattern 2θ=6.7°(±0.2°), 9.5°(±0.2°) and 19.0°(±0.2°); Polymorphic form H, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=8.9°(±0.2°), 9.2°(±0.2°) and 14.1°(±0.2°); Polymorphic Form I, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.7°(±0.2°), 19.3°(±0.2°), and 24.5°(±0.2°), and the polymorphic form J, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.1°(±0.2°), 17.3°(±0.2°) and 18.3°(±0.2°). The invention also relates to a process of preparing form C. For example, mentioned process comprising (i) exposure of the medium containing water, a composition comprising at least one polymorphic form, not a form of a compound of formula (I), for a period time sufficient for the transformation, preferably for 18-24 hours, at least 50% of the total amount of the polymorphic form (s) a non-form C; and (ii) recovering mentioned polymorph form C.EFFECT: high effectiveness of compounds.84 cl, 31 dwg, 16 tbl, 42 ex
Preparation for treatment of bony lumps, headaches and heartaches // 2626844
FIELD: pharmacology.SUBSTANCE: invention is a preparation for application to the skin surface for bony lumps, headaches and heartaches treatment, consisting of 5 ml of turpentine, 50 ml of 40% formalin, characterized by additional content of 96% ethyl alcohol solution in an amount of 45 ml. The proportions of constituents are given for 100 ml of the preparation.EFFECT: invention provides resorption of bony lumps, disappearance of pain in the heart and head areas, and also allows to do without surgical installation of plates for vertebrae fixation while infringing the nerve fibers as a result of their squeezing.5 ex
ethod of treatment of posttraummatic fibrosive ankiloses of small juices of brush // 2626591
FIELD: medicine.SUBSTANCE: method includes the installation of an external fixation device (EFD) and the implementation of a stage distraction of the joint area up to 9 mm by 3 mm per day. In the formed cavity on the 3rd and 6th day after the AVF installation, 1.5-2 ml of plasma enriched with platelets (PRP) is injected, which amounts to 1,000,000-1200,000 cells. After the second injection, the EFD is dismantled and active rehabilitation treatment is carried out. The third injection of PRP is performed pararticularly on the 9th day.EFFECT: reducing the time to restore or improve the function of the fingers.1 ex, 5 dwg

Bromelain extract with proteolytic activity to treat connective tissue diseases // 2625726
FIELD: medicine.SUBSTANCE: pharmaceutical composition comprising a proteolytic extract obtained from bromelain is used for treatment of connective tissue diseases. Thus, bromelain is obtained from pineapple stem. Proteolytic extract contains stem bromelain, ananain and jacalin-like lectin. The connective tissue disease is associated with excessive deposition of collagen, such as Dupuytren's disease and Peyronie's disease.EFFECT: efficiency and selectivity of action against type III collagen degradation in Dupuytren's chords; no damage for healthy connective tissue.16 cl, 13 dwg, 2 ex
ethod for spinal osteomyelitis treatment // 2625596
FIELD: medicine.SUBSTANCE: puncture needle is introduced under ultrasound supervision in the abscess cavity, the contents is taken for the study, a drainage system is installed, which is used for abscess cavity sanitation and drainage. Laboratory research of the abscess cavity content is performed dynamically. At that, the necessary amount of antiseptic solution is determined for introduction into the abscess cavity in liters/min based on: abscess cavity volume ratio Vcavity/l multiplied by a factor of 0.7. Sanitation is carried out to achieve abscess cavity abacillation by supplying of an antiseptic solution combined with active aspiration of an antiseptic solution and dispersive suspended necrotic masses from the abscess cavity. A sodium chloride solution saturated with ozone-oxygen mixture with a level of oxidation-reduction potential of not lower than 600 mVA is used as the antiseptic solution, which is maintained during the entire sanitation by providing continuous readjustment of sodium chloride solution saturation with ozone-oxygen mixture until the end of the procedure.EFFECT: method allows to increase the efficiency of pathological focus antiseptic treatmen, provide a reliable bactericidal effect.1 ex
ethod for adhesiogenesis stimulation in pleural cavity in case of polytraumas with predominant thoracic involvement // 2625002
FIELD: medicine.SUBSTANCE: invention concerns adhesionogenesis stimulation in the pleural cavity in case of polytraumas with predominant thoracic involvement. To do this, a 10% homogenized suspension of autologous adipose tissue in a physiological solution is injected pointwise into the pleural cavity into the ribs fracture region subpleurally, under the parietal pleura.EFFECT: method ensures pulmonary framework stabilisation and early fusion of ribs due to adhesiogenesis stimulation and adhesions formation in the pleural cavity.2 cl, 1 ex
ethod for obtaining of composite scaffold for bone tissue defects restoration // 2624854
FIELD: medicine.SUBSTANCE: method for composite scaffold obtaining for bone defects reconstruction is described, which includs synthesis of a polymer solution with a concentration of 9 wt % by polycaprolactone granular powder dilution in chloroform. Siliceous hydroxyapatite Ca10(PO4)6-x(SiO4)x(OH)2-x powder is added to the obtained polymer solution in the substitution x = 0.5 at a concentration of 5-15 wt % in the solution. The mixture is homogenized for at least 2 h, then a scaffold is formed by electric formation at a voltage of not less than 7 kV and a minimum distance of 50 mm between a die electrode in the form of a needle with an internal diameter of 0.55 mm and a deposition electrode in the form of a spinning shaft 60 mm in diameter.EFFECT: method allows to improve the scaffolds surface wettability parameter.3 dwg, 3 tbl
ethod for combined medical and balneological treatment of joint diseases // 2624362
FIELD: medicine.SUBSTANCE: for combined medical and balneological treatment of joint diseases, the patient is treated with medication, including administration of a non-steroidal anti-inflammatory drug and a chondroprotector. At the stage of exacerbation, starting from day 1-3 of medical treatment, the patient is additionally treated with foam and licorice liquor baths with a temperature of 35°C, containing a thick extract of licorice root (LRTE) from 50 to 150 ml. If the patient enters the stage of fading exacerbation, he/she additionally receives foam and vortex baths with a temperature of 36-38°C, containing from 50 to 70 ml of LRTE, starting from day 3-5 of medical treatment. In case if the patient enters the stage of incomplete remission, he/she additionally receives foam-mineral-vortex baths with a temperature of 36-38°C, containing "Dzhemukhskaya Tselebnaya" mineral water instead of fresh water, and LRTE in an amount of 50 to 70 ml, starting from day 5-7 of medical treatment. Bath duration is 10-15 minutes. Baths are performed daily or once in two days, 8-10 per a course of treatment.EFFECT: increased efficiency while reducing the duration of disease treatment.2 tbl, 3 ex
Radio pharmaceutical composition for radiosynovectomy and method for its production // 2624237
FIELD: pharmacology.SUBSTANCE: set of reagents and a solution of sodium perrhenate, 188Re obtained from 188W/188Re generator is prepared. First, a set of lyophilized reagents is prepared, consisting of two vials of lyophilized reagents. Vial 1 contains lyophilized tin dichloride, dihydrate and stabiliser. Vial 2 contains a lyophilized neutralizing agent to adjust acidity. Radio pharmaceutical composition for radiosynovectomy is synthesized. First, a sodium perrhenate solution, 188Re, from 188W/188Re generator is obtained. For elution, an 0.9% isotonic sodium chloride solution for injection is used. Then 1.0 ml of sodium perrhenate solution 188Re, with a volume activity of 37 to 1850 MBq/ml is introduced into vial 1. The resulting suspension is stirred. Kept at the room temperature for 1 hour. Then 2.5 ml of 0.9% isotonic sodium chloride solution for injection is injected into vial 2 and stirred. After complete dissolution of the lyophilized agent, a syringe is used to remove all content from vial 2 and inject it into vial 1, the formed suspension is stirred, obtaining a radio pharmaceutical composition for radiosynovectomy ready for application, the pH value of the finished composition is 3.2-5.9, radiochemical purity exceeds 90%, output of labelled particles with dimensions of 2-10 µm is more than 80%. A radio pharmaceutical composition for radiosynovectomy is proposed as well.EFFECT: homogeneous distribution of the radio pharmaceutical composition in the intra-articular space for 72 hours without causing an inflammatory reaction.6 cl, 8 tbl, 3 ex
ethod for treatment of patients with acute stage of diabetic neurosteoartropathy of charcot foot type // 2624230
FIELD: medicine.SUBSTANCE: invention relates to treatment of the acute stage of diabetic neuro-osteoarthropathy ("Charcot foot"). To do this, the affected limb is unloaded and 2.0 to 4.0 ml of platelet-enriched autoplasma is injected into the area of aseptic inflammation and osteodestruction. The number of procedures is from 1 to 3 per a course of treatment of up to 2-3 weeks.EFFECT: method prevents the development of destruction of the foot osteoarticular apparatus, deformation and plantar ulcer defects formation.1 ex
Chondroitin sulfate solution for intramuscular administration and method for its preparation // 2623050
FIELD: pharmacology.SUBSTANCE: pharmaceutical preparation in the form of solution for intramuscular administration contains chondroitin sodium sulfate and auxiliary substances: sodium metabisulphite, methylparaben and water for injection at a certain component ratio. A method for obtaining a stable solution with reduced side effects is also proposed.EFFECT: maintaining stability and reduced amount of impurities during storage.3 cl, 1 tbl, 3 ex

ethod and agent for chlamydial etiology reactive arthritis treatment // 2622747
FIELD: pharmacology.SUBSTANCE: method of invention comprises intra-articular introduction of agent containing pharmaceutically acceptable nafamostat salt, (2-hydroxypropyl)-β-cyclodextrin and chondroitin sulphate. The agent of the invention comprises nafamostat dimesylate, cyclodextrin enhancing solubility of nafamostat, as well as chondroprotective component - chondroitin sulphate.EFFECT: use of the invention enables to achieve complete elimination of pathogen from the infected joint while reducing the total dose of nafamostat and injection frequency.11 cl, 6 tbl, 3 dwg, 8 ex

Selective and reversible ubiquitin-specific protease 7 inhibitor // 2622640
FIELD: pharmacology.SUBSTANCE: viral infections and diseases are selected from viral infections of Herpes simplex-1 or -2, hepatitis A, hepatitis C, SARS of coronavirus infection and disease, Epstein-Barr virus, rhinovirus infections and diseases, adenovirus infections and diseases, poliomyelitis. In the formula each identical or different R1 is selected from the group consisting of halogen, linear or branched (C1-C6)alkyl, OR; L1 is a linear or branched (C1-C6)alkylene; Q is 0, 1, 2, 3 or 4; X' is CR7; R7 is OR; N is 0, 1 or 2; P is 1, 2 or 3; R3, R4, R8' and R8 each represents H; A is -C (O)-; L2 is linear or branched (C1-C6) alkylene, optionally interrupted by at least one O; R6 is selected from the group consisting of aryl, heteroaryl, cycloalkyl, H, wherein aryl, heteroaryl, cycloalkyl is mono- or polycyclic and is optionally substituted by halogen, OR; each R, identical or different, is independently selected from H, linear or branched (C1-C6)alkyl. At that, "aryl" means an aromatic monocyclic hydrocarbon ring system of 6 carbon atoms, "cycloalkyl" means a non-aromatic, monocyclic, hydrocarbon ring of 3-10 carbon atoms; "heteroaryl" means a 5-membered aromatic mono-heterocyclic ring. The invention also relates to versions of the for preparation of compounds.EFFECT: compounds can be used to prepare a drug for treatment or prevention of cancer and metastases, viral infections and diseases, or viral infectivity, or latency mediated by ubiquitin-specific proteases activity.19 cl, 6 dwg, 4 tbl, 14 ex
Furo[3,2-b]- and thieno[3,2-b]pyridine derivatives as tbk1 and ikkε inhibitors // 2622034
FIELD: pharmacology.SUBSTANCE: invention relates to a novel compound of formula I , wherein X means O or S, R1 means O(CYY)nHet1 or O(CYY)nCyc, R2 means Ar or Het2, Het1 means pyrrolidinyl, tetrahydro imidazolyl, dihydropyrazolyl, tetrahydropyrazolyl, tetrahydropyranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, morpholinyl, hexahydropyrimidinyl, azepanyl, tetrahydrofuranyl, furyl, thienyl, pyrazolyl, pyridyl, chromanyl or piperazinyl, each of which is unsubstituted or monosubstituted by A, COOA, OY and/or =O (carbonyl oxygen), Het2 means mono- or bicyclic saturated, unsaturated or aromatic heterocycle which contains from 1 to 2 N, O and/or S atoms, which may be unsubstituted or monosubstituted by A, (CYY)p-OY, (CYY)p-Het1, -CO-Het1 and/or =O, Ar means phenyl, which is unsubstituted or monosubstituted by Hal, A, (CYY)p-OY, (CYY)p-Het1, (CYY)p-COOY, CO(CYY)pNH2, CO-NYA, CONY(CYY)mNYCOOA, CO-Het1, O(CYY)p-NYY, CONY(CYY)pHet1 and/or CONH(CYY)pNHCOA, Y means H or an alkyl, which contains 1, 2, 3 or 4 C-atom, A is an unbranched or branched alkyl that contains from 1 to 10 C-atoms, Cyc means a cycloalkyl, which contains from 3 to 7 C-atoms, which is unsubstituted or monosubstituted by A, Hal means F, Cl, Br or I, n means 0, 1 or 2, m means 1, 2 or 3, p means 0, 1, 2, 3, or 4 and pharmaceutically applicable salts and stereoisomers thereof, including mixtures thereof in all ratios.EFFECT: compounds are inhibitors of TVK1 and ε IKK, and can be used in particular for the treatment of malignant neoplasms and inflammatory diseases.6 cl, 3 tbl, 120 ex

Antibody agains csf-1r // 2621859
FIELD: biotechnology.SUBSTANCE: proposed allocated recombinant or purified antibody that specifically binds to the receptor of colony stimulating factor-1 (CSF-1R, CSF-1R), characterized by amino acid sequences of the variable domains. Also is provided nucleic acid encoding the antibody of the invention, vector, cell and method of producing the antibody. Furthermore, a pharmaceutical composition and the use of the antibodies and pharmaceutical composition of the invention as a medicament for the treatment of cancer, disease associated with increased osteoclast activity, inflammatory disease and rheumatoid arthritis, are described.EFFECT: invention may find further application in the treatment of diseases associated with the CSF-1R.19 cl, 32 dwg, 4 tbl

Antagonists of trpv1, containing dihydroxy group as substitute, and their use // 2621708
FIELD: pharmacology.SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, in which R1 represents -halo or -CF3; R4 represents -H or -CH3; each of R8 and R9 independently represents -H, -halo, -CH3 or -OCH3, each halo independently represents -F, -Cl, -Br or -I; and m means an integer of 0 or 1; (1) provided that if R4 represents -H, the m means 1; and (2) provided that if R4 represents -H and the carbon atom in the position a of the a-b bond is in (S)-configuration, the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group, a (S)-3-methyl group or a (R)-3-methyl group; (3) provided that if R4 represents -H, the carbon atom in position a of the a-b bond is in (S)-configuration, R8 represents -H and R9 represents -halo, then the methyl group connected to piperazinonyl ring represents a (R)-3-methyl group; (4) provided that if R4 represents -H, the carbon atom in position a of the a-b bond is in (S) configuration, R8 represents -F and R9 represents -F, then the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group or a (S)-3-methyl group; and (5) provided that if R4 represents -CH3, each of the carbon atoms in positions a and c and the a-b bond and the c-d bond is in (S) configuration,R8 represents -H, R9 represents -halo, and m means 1, the methyl group connected to piperazinonyl ring is a (S)-3-methyl group or a (R)-3-methyl group. Invention also relates to a compound of formula (II) or a pharmaceutically acceptable salt thereof, a specific compound of formula (Ia) or a pharmaceutically acceptable salt thereof and / or a co-crystal of fumaric acid. Invention also relates to specific compounds of formula (Ib) or a pharmaceutically acceptable salt thereof. The compounds as per invention are intended to inhibit the function of TRPV1 in a cell and to treat pain, pain associated with osteoarthritis, osteoarthritis, urinary incontinence (UI), ulcer, inflammatory bowel disease (IBD) or irritable bowel syndrome (IBS) in an animal.EFFECT: compounds having an affinity for the receptor TRPV1.38 cl, 11 tbl, 3 dwg, 16 ex
Spirocyclic nitriles as protease inhibitors // 2621695
FIELD: biotechnology.SUBSTANCE: invention relates to formula (I) compounds and physiologically acceptable salts thereof, which provide inhibitory activity against K, B and S cathepsins. In formula (I), partial cycles and , each independently from each other, are selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, dioxolane, 1,3-dioxolane and piperidine, wherein the two partial cycles are unsubstituted; X is a covalent bond; Y is -C(O)-; Z is -N(R26)-(C(R24)(R25))m-CN; R26 represents a hydrogen atom; m is integer 1; R24 and R25, and the carbon atom to which they are attached, form a cycloalkyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, which is unsubstituted; R1 represents a hydrogen atom; R2 and R3 are the same or different and each independently represents a hydrogen atom or -(C0-C3)-alkylene-C-(R27)(R28)(R29); R27 represents a hydrogen atom, -(C1-C9)-alkyl, -(C0-C4)-alkylene-(C3-C6)-cycloalkyl; R28 and R29 are identical or different and independently represent a hydrogen atom, -(C1-C4)-alkyl; or R28 and R29 with the carbon atom to which they are attached, form -(C3-C6)-cycloalkyl; or R2 and R3 with the carbon atom to which they are attached, form a three to six member cycloalkyl, which is unsubstituted. The invention also relates to methods for formula (I) compounds preparation, methods for preparation of physiologically acceptable salts and N-oxides thereof, medicament containing them, and formula (I) compounds application for the manufacture of a medicament for prophylaxis, prevention and treatment of diseases, related to inhibitory activity against K, B and S cathepsins.EFFECT: higher efficiency of compounds application.10 cl, 2 tbl, 105 ex
Application of whole soft avocado for preparing avocado oil with high content of unsaponifiable compounds // 2621631
FIELD: pharmacology.SUBSTANCE: whole soft avocado is crushed, then it is dried at the high temperature, of 60 to 150°C, until the residual moisture content of less than or equal to 5% is received, and then it is hydrated to obtain avocado oil by mechanical pomace. The process for preparing avocado oil from whole soft avocados. Avocado oil. The use of avocado oil for preparing the avocado oil concentrate, rich in unsaponifiable compounds. The application of the avocado oil or the avocado oil concentrate, enriched with unsaponifiable compounds, obtained from this oil, to obtain the avocado unsaponifiable fraction, rich in aliphatic furans.EFFECT: avocado unsaponifiable fraction with the high aliphatic furan content or the avocado oil concentrate, rich in unsaponifiable compounds, for use as a medicament for prophylaxis or treatment of connective tissue disorders such as arthritis, articular pathologies such as rheumatic disease, or periodontal diseases such as gingivitis or periodontitis.18 cl, 3 ex

New crystalline salt form of 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazin-2-yl)amino)-2h-pyrido[3,2-b][1,4]oxazin-3(4h)-one for medical use // 2621187
FIELD: chemistry.SUBSTANCE: invention relates to a salt of 4-methylbenzenesulfonic acid and 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazin-2-yl)amino)-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one base, its hydrate, solvate or polymorph salt, hydrate or solvate modification effective to inhibit Src kinases. The invention also relates salt application for prevention and/or treatment of a disorder associated with aberrant kinase activity, and a pharmaceutical composition.EFFECT: new salt can be used to prevent or treat a disorder associated with aberrant kinase activity.16 cl, 21 dwg, 11 tbl, 1 ex

Composition of bone filler // 2621151
FIELD: pharmacy.SUBSTANCE: bone filler composition is described comprising a mixture of a curable bone filler based on calcium phosphate, which is formed from a liquid component and a powder component based on calcium phosphate, and a composition comprising particulate bisphosphonate. Bisphosphonate particles are introduced into particles of polymeric material, which dissolves after composition implantation.EFFECT: improved mechanical properties of bone filler composition.15 cl, 4 dwg, 2 tbl
 
2551293.
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