Dipeptidyl peptidase-4 inhibitor for treatment of type 2 diabetes

FIELD: pharmacology.

SUBSTANCE: application of (R/S)-3-amino-1-[(S)-5-phenyl-[1,2,4] oxadiazol-3-yl)-pyrrolidin-1-yl]-3-(4-fluorophenyl)-propan-1-one (with molecular mass Mr=380) in the form of hydrochloride (in terms of the salt form Mr=380+36.5 (HCl)=416.5), corresponding to the structural formula (I)

as dipeptidyl peptidase-4 inhibitor for treatment of type 2 diabetes mellitus.

EFFECT: chemical structure of the compound prevents its intramolecular cyclization, which preserves chemical and spatial structure in the natural conditions of the human body.

4 dwg, 1 tbl, 6 ex

 



 

Same patents:

FIELD: veterinary medicine.

SUBSTANCE: treatment is carried out with an aqueous solution of the preparation "Biopag-D" at a concentration of 4-2% by drifting animals through the baths with the solution having the immersion depth up to the carpal joint.

EFFECT: invention enables to treat efficiently and stress-free and prevent treatment of diseases of hooves and dew claws of animals.

3 cl, 5 dwg, 4 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: stimulating the excised liver regeneration is ensured by a 70% hepatectomy into a laboratory animal on the second day of the experiment. A liver regeneration stimulator is presented by L-norvaline administered intragastrically in a daily dose of 10.0 mg/kg every 46 hours for the first 7 days of the experiment.

EFFECT: method provides the effective stimulation of the excised liver regeneration evidenced by reducing the animals' lethality, improved hepatic microcirculation, reduced manifestation of cytolysis and enhanced synthetic function of the liver.

2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to therapeutic dentistry, and can be used for the local treatment of chronic gingivitis caused by tobacco smoking in young individuals. That is ensured by a preparatory procedure of luminal-dependent chemiluminescence of the oral fluid aiming at a maximum burst and a glow light sum. If the maximum burst falls within the range of 3.3 to 18.15 standard units, whereas the glow light sum ranges from 8.2 to 40 standard units, an antioxidant therapy is conducted by using a transverse gingival mucosa electrophoresis on 5% aqueous propolis by means of jaw electrodes in a tray at a current intensity of 0.5-1 mA and an exposure of 8-10 minutes. A polarity is alternated with a positive pole to be taken the first. The therapeutic course makes 4 procedures every second day. Colgate Propolis Toothpase and Mouthwash are used additionally during 30 days. If the maximum burst is from 0.8 to 1.24 standard units, whereas the glow light sum ranges from 3.34 to 7.5 standard units, a pro-oxidant therapy is required by using an exposure to magnetic infrared laser (MIL) light covering a projection of gums and generated by Optodan laser with a periodontal attachment The exposure parameters: 2-2,000 Hz in segments, 2 minutes per each segment, no more than 12 minutes per 1 procedure. The therapeutic course makes 4 procedures every second day. Parodontax Toothpase and Mouthwash are used additionally during 12 days.

EFFECT: method simplifies and reduces the length of the treatment in the given category of patients.

2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to oxazolopyramidine compounds of formula I, where A represents O; R1 is selected from phenyl or pyrimidine, which are optionally substituted with R11; R2 represents phenyl, which is optionally substituted wby 1-3 ring carbon atoms with similar or different substituents R22, R11 represents halogen; R22 is selected from hydroxy group, (C1-C4)-alkyl, which is optionallysubstituted with 1-3 atoms of fluorine, (C1-C4)-alkyloxy, (C1-C4)-alkyl-S(O)m-; m equals 2. Invention also relates to pharmaceutical composition, which contains formula I compounds, and to method of obtaining formula I compounds.

EFFECT: formula I compounds, intended for activation of EDG-1 receptor and applied for wound healing.

15 cl, 2 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to oxazolopyramidine compounds of formula (I), where A represents O; X represents (C1-C6)-alkanediyl or (C1-C6)-alkanediyloxy, where oxygen atom of (C1-C6)-alkanediyloxy is bound to group R2; Y represents pyrrolidinyl; R1 represents (C1-C4)-alkyl; R2 represents phenylene, optionally substituted by one or two carbon atoms in ring with similar or different substituent R22; R3 is selected from group, which consists of cycloalkyl-CuH2u-, where u equals 1; radical of saturated 3-10-member monocyclic ring, phenyl or pyridyl, where ring radical is optionally substituted by one or two carbon atoms of ring with substituent R31; R4 represents hydrogen; R22 represents (C1-C4)-alkyl; R31 is selected from group, which consists of halogen and (C1-C4)-alkyl. Invention also relates to (S)-l-[2-(2,6-dimethyl-4-{5-[methyl-(3,3,3-trifluoropropyl)amino]-7-propoxyoxazolo[5,4-d]pyrimidine-2-yl}phenoxy)acetyl]pyrrolidine-2-carboxylic acid, pharmaceutical composition and to method of obtaining compounds of formula (I) .

EFFECT: compounds of formula (I), intended for activation of EDG-1 receptor and applied for wound healing.

16 cl, 2 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention relates to veterinary and can be applied in animal-breeding for stimulation of metabolic processes, and growth activity of calves. Medication for stimulation of metabolic processes and growth activity of calves includes succinic acid as energetic stimulator, with application of citric acid as activator of succinic acid, beetroot molasses as carbon component, and methionine and sodium chloride as stimulators of digestion system.

EFFECT: application of invention makes it possible to ensure expressed acceleration of growth energy in early postnatal period.

3 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: cytoflavin is administered into laboratory animals (rats) daily immediately before overheating in an air laboratory thermostat at +40±1-2°C for 45 minutes. The preparation is administered intraperitoneally in a dose of 100 mg/kg of body weight for 14 days.

EFFECT: higher body adaptability by increasing antioxidant activity and reducing a rate of lipid peroxidation products accumulation with underlying thermal exposure.

4 tbl

FIELD: medicine.

SUBSTANCE: minor amputation of the foot with the further necrectomy is performed. After the application of an antimicrobial bandage and drainage, the wound is hermetised from the environment by the creation of a negative pressure above the wound in a combination with drug treatment. The reatment is performed in two steps. At the first step the wound with the antimicrobial bandage and drainage is first hermetised from above with an adhesive film, with the creation and support of the negative pressure not lower than 80 mm Hg. Urokinase 500000 U is additionally introduced daily intravenously by drop infusion per 100 ml of physiological solution, Vessel-Due-F in a dose of 600 LU per 100 ml of physiological solution and VAP 20 - alprostadil in a dose of 40 mcg per 100 ml of physiological solution. In addition Antistax in capsules is introduced to the patient. At the second stage active 24-hour vacuum aspiration with the change of the negative pressure from 10 to 80 mm Hg within a day is carried out. Additionally introduced is Vessel-Due-F in a dose of 1 capsule with 250 LU 2 times per day between meals and Antistax. At the first and second stages Antistax is introduced in a dose of 2 capsules in the morning 30-40 minutes before meal, daily. Duration of each stage constitutes not less than 7 days.

EFFECT: increase of the treatment efficiency due to the complete and timely purification of the wound from pathological exudates, elimination of the progression of the purulent-necrotic process, increase of the regenerative activity of tissues, activation of local immunity, recovery of microcirculation and oxygenation of the affected tissues.

2 cl, 2 ex

FIELD: medicine.

SUBSTANCE: method involves professional oral hygiene is carried out consisting in ultrasonic removal of supra- and subgingival dental deposits and polishing of supragingival teeth. Bite splinting and recovery of dentition integrity may be required. After dissecting a mucoperiosteal flap according to the known technique, an incision area is sanitated by means of a photodynamic therapy (PDT). The PDT is conducted with the use of a diode laser at wave length 660±5 nm and emitting power 0.5-1.0 Wt. The photosensitiser "Photoditasin" in the form of 0.5% gel is introduced by means of a cannula into dental gaps, under the dissected segments of the flap and onto the mucosal tissue for 5 minutes. The photosensitiser is washed out, and the gingival pockets are repeatedly exposed to laser light for 2-3 min in the same environment. Sterile osteoplastic material is introduced into bone defects, and the flap is sutured together.

EFFECT: effective cleansing of the surgical area, eliminating the periodontal inflammation, stimulating tissue osteogenesis and regeneration, stabilising the processes of bone tissue absorption of alveolar interdental septa and preserving the tissues.

2 cl, 1 ex

FIELD: medicine.

SUBSTANCE: to correct pathologic changes in the condition of viable offspring under a cytostatic impact the medication glutoxim is introduced to female rats in a dose of 50 mcg/kg 5 days before and 5 days after the introduction of the cytostatic medication vepesid. The latter is introduced once intravenously in a maximal tolerable dose, equal to 30 mg/kg. It has been established that glutoxim can be applied as means for the correction of pathologic changes in the viable offspring of rats, obtained from coupling 3 months after the cytostatic impact.

EFFECT: application of glutoxim as the means of corrective therapy makes it possible to increase efficiency and reduce its side effects.

6 dwg

FIELD: medicine.

SUBSTANCE: integrated resort treatment is conducted. A patient takes carbonic sodium chloride mineral water. The mineral water is heated to a temperature of 37°C before use and taken at 3 ml per 1 kg of body weight 3 times a day 40 minutes before meals. The therapeutic course makes 18 days. The patient also takes "dry" carbon dioxide baths with the CO2 concentration of 1.2-1.4 g/l at the water temperature of 35°C. The water temperature is reduced to 32°C by the end of the course. The procedure length is 15-20 minutes. CO2 is supplied from a balloon into a special box compartment at a rate of 15-20 l/min. The gas mix temperature ranges from 28°C to 38°C. The procedures are performed every second day. The course of 8-10 procedures is required.

EFFECT: method provides normalising the complete blood count, blood sugar, common urine analysis, improving the visual analysis health, renal blood flow, ophthalmic parameters by the integrated intake of mineral water and dry carbon dioxide baths, optimum regimen and length of the therapeutic course.

1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to biotechnology, specifically to novel analogues of a glucagon-like peptide, and can be used in medicine to activate insulin expression in mammals and to treat sugar diabetes.

EFFECT: obtained peptide derivatives have a peptide imitating linker and provide prolonged action when treating diabetes and other diseases associated with insulinotropic peptides, gastrointestinal functions and glucagon levels.

25 cl, 23 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to pharmaceutical composition, which contains compound of insulin in concentration, sufficient for supplying therapeutically effective level of insulin compound in blood plasma for at least 3 days. Insulin compound relates to pro-medical compound, which represents insulin conjugate with linker, bound with hydrogel carrier. Also described is suspension, containing pharmaceutical composition of insulin conjugate, method of suspension obtaining, set, including pharmaceutical composition of insulin conjugate and container for introduction of composition.

EFFECT: pharmaceutical composition of insulin conjugate by invention is characterised by the fact that it has pharmacokinetic profile in vivo in fact without release of insulin compound.

26 cl, 9 dwg, 21 ex

FIELD: medicine.

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

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

2 tbl, 1 ex

FIELD: medicine.

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

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

1 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to methods of treating type 2 diabetes, insulin resistance, insulin hyposecretion, obesity, hyperglycaemia and hyperinsulinemia, involving administering an effective amount of an anti-IL-1β antibody or its fragment into an individual, as well as to using the anti-IL-1β antibody or its fragment in preparing a composition applicable for treating the above diseases or conditions.

EFFECT: group of inventions is effective in treating type 2 diabetes mellitus, insulin resistance, insulin hyposecretion, obesity, hyperglycaemia and hyperinsulinemia.

67 cl, 13 dwg, 5 tbl, 14 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel N-containing heteroaryl derivatives of formula I or II or their pharmaceutically acceptable salts, which possess properties of JAK kinase, in particular JAK3, and can be applied for treating such diseases as asthma and chronic obstructive pulmonary disease (COPD). In formulae A represents carbon and B represents nitrogen or A represents nitrogen and B represents carbon; W represents CH or N; R1 and R2, independently represent hydrogen, C1-4alkyl, halogenC1-4alkyl, -CN; R3 represents C1-4alkyl, R9-C1-4alkyl, Cy1, where Cy1 is optionally substituted with one or several substituents R10; R4 represents hydrogen, C1-4alkyl, R12R7N-C0alkyl, where one of R7 and R12 represents hydrogen, and the other represents C1-4alkyl or group R13, which is selected from C1-5alkyl, Cy2-C0alkyl; R5 represents hydrogen; R6 represents hydrogen, C1-4alkyl, C1-4alkoxyC1-4alkyl, hydroxyC1-4alkyl, R12R7N-C1-4alkyl, R16CO-C0alkyl, Cy1; R7 represents hydrogen or C1-4alkyl; R9 represents halogen, -CN, -CONR7R12, -COR13, CO2R12, -OR12, -SO2R13, -SO2NR7R12, -NR7R12, -NR7COR12; R10 represents C1-4alkyl or R9-C0-4alkyl; R11 represents C1-4alkyl, halogen, -CN, -NR7R14; R12 represents hydrogen or R13; R13 represents C1-5alkyl, hydroxyC1-4alkyl, cyanoC1-4alkyl, Cy2-C0alkyl or R14R7N-C1-4alkyl; where Cy2 is optionally substituted with one or several constituents R11; R14 represents hydrogen or C1-4alkyl; R16 represents C1-4alkyl, halogenC1-4alkyl, C1-4alkoxyC1-4alkyl, hydroxyC1-4alkyl or cyanoC1-4alkyl; Cy1 represents monocyclic carbocyclic unsaturated or saturated ring, selected from C3-C6cycloalkyl, phenyl, or saturated monocyclic 4-6-membered heterocyclic ring, containing from 1 to 2 heteroatoms, selected from N and S, or partially unsaturated 10-membered bicyclic heterocyclic ring, containing oxygen atom as heteroatom, which can be substituted with group R11, where said ring is bound with the remaining part of molecule via any available C atom, and where one or several ring C or S atoms are optionally oxidised with formation of CO or SO2; and Cy2 represents monocyclic carbocyclic unsaturated ring, selected from C3-C6cycloalkyl, or aromatic monocyclic 4-6-membered heterocyclic ring, containing from 1 to 2 heteroatoms, selected from N and S, or unsaturated 10-membered bicyclic heterocyclic ring, containing oxygen atom as heteroatom, which can be substituted with group R11, where said ring is bound with the remaining part of molecule via any available atom C or N.

EFFECT: obtaining novel heteroaryl derivatives.

27 cl, 41 ex

Transdermal plaster // 2553350

FIELD: medicine.

SUBSTANCE: group of inventions relates to medicine. Described is matrix layer, suitable for application in plaster for transdermal delivery, aimed at introduction of biologically active compounds, which includes phosphate compound of tocopherol and polymer carrier. Also described is transdermal plaster and method of its production.

EFFECT: plaster makes it possible to efficiency introduce biologically active compounds.

48 cl, 15 tbl, 13 dwg, 12 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry and represents clinical nutrition for prevention, treatment or relief of one or several symptoms, associated with impairment of metabolism or its disorder, which contains composition of polysaccharide high-viscosity dietary fibre, including viscous fibre mixture or its complex, consisting of from 48% to 90% in wt % of glucomannan, from 5 to 20 % in wt % of xanthan gum and from 5% to 30% in wt % of alginate, as well as, at least, one macroelement, selected from the group, consisting of protein carbohydrate and fat, where clinical nutrition is composed in order to provide dose of composition of polysaccharide high-viscosity dietary fibre from 20 g/day to 35 g/day for time period, effective for prevention, treatment and relief of one or several symptoms, associated with impairment of metabolism or its disorder.

EFFECT: invention ensures extension of arsenal of means, preventing, relieving or treating one or several symptoms, associated with impairment of metabolism or metabolic disease.

14 cl, 6 ex, 20 tbl, 48 dwg

FIELD: medicine.

SUBSTANCE: patients with diabetic microangiopathy are subjected to an examination which includes: general blood test, blood sugar, general urine analysis, ultrasonic examination of kidneys with the determination of indices of the kidney blood flow (Vmax, Vmin, S/D, PI, RI), basic ophthalmological parameters (vision acuity, examination of eye fundus vessels). Then, the intake of mildly-mineralised hydrocarbonate-chloride-sodium mineral water "Obyhovskaya" directly from the spring under sanatorium conditions is administered. Water is taken in heated to a temperature of 37°C in a dose of 3 ml per 1 kg of body weight 3 times per day 40 minutes before meal, the course constitutes 18 days.

EFFECT: application of the invention makes it possible to normalise the general blood test, blood sugar, general urine analysis, improve the condition of the visual analyser and indices of the kidney blood flow.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to chemical-pharmaceutical industry and represents application of substituted nitrocatechols of formula for prevention or treatment of disorders, associated with central and peripheral nervous system, which obtain use from inhibition of catechol-O-methyltransferase (COMT), in accordance with schedule of dosing in the range from one time per three days to one time per week.

EFFECT: obtaining composition for prevention or treatment of disorders, associated with central and peripheral nervous system.

45 cl, 1 dwg, 3 ex

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