Halides of 1-(4-tert-butylphenyl)-2-{3-[2-(4-fluoro-phenoxy)ethyl]-2-methyl-3h-benzimidazole-1-yl}ethanone with property of rupture cross-linkers of glycated proteins

FIELD: chemistry.

SUBSTANCE: halides of the formula 1

are described, possessing the property of rupture cross-linkers of glycated proteins.

EFFECT: new halides that have beneficial biological properties.

4 cl, 2 dwg, 1 tbl

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining compound, described by formula (I) or its salt, where X stands for halogen residue, and R1 and R2 together stand for residue, described by formula (II), where R4 and R5 independently on each other represent alkyl residue and n represents number in the range 0-12. In accordance with claimed method compound of formula (III) is introduced into reaction with mixture, containing compound (i), selected from group, consisting of compound of formula (IV), where R6 represents H or alkyl residue, and R7 and R8 independently on each other represent alkyl residue, and compound of formula (V) where R9 and R10 independently on each other represent alkyl residue, and compound (ii), which is described by formula (VI). R1 and R2 in compound of formula (III) and X in compound of formula (VI) are determined above for compound of formula (I). Invention also relates to method of obtaining respective acids by hydrolysis of ester group in compound of formula (I).

EFFECT: claimed methods make it possible to obtain desired compounds with reproducible high outputs and can be applied in synthesis of bendamustine derivatives, used in chemical therapy of various cancer diseases.

14 cl, 3 ex

FIELD: organic chemistry, medicine, hormones.

SUBSTANCE: invention describes imidazole derivatives of the formula (I) , racemic-diastereomeric mixtures and optical isomers, pharmaceutical salts wherein ---- represents an optional bond; R1 represents hydrogen atom (H), -(CH2)m-C(O)-(CH2)m-Z1, -(CH2)m-Z1; R2 represents hydrogen atom (H), or R1 and R2 are joined with nitrogen atoms to which they are bound forming compounds represented by formulae (Ia), (Ib) or (Ic) wherein R3 represents -(CH2)m-E-(CH2)m-Z2; R4 represents hydrogen atom (H) or -(CH2)m-A1; R5 represents (C1-C12)-alkyl, (C0-C6)-alkyl-C(O)-NH-(CH2)m-Z3 and optionally substituted phenyl; R6 represents hydrogen atom (H); R7 represents (C1-C12)-alkyl or -(CH2)m-Z4; m = 0 or a whole number from 1 to 6; n is a whole number from 1 to 5. Proposed compounds bind with subtypes of somatostatin receptors selectively.

EFFECT: valuable properties of compounds.

20 cl, 13776 ex

)-cis-3-(2'-benzimidazolyl)-1,2,2 - trimethylcyclopentanone acid exhibiting hypoglycemic and antidiabetes action" target="_blank">

The invention relates to medicine, specifically to a new biologically active compound () -CIS-3-(2'-benzimidazolyl)-1,2,2-trimethylcyclopentanone acid exhibiting hypoglycemic and antidiabetes action

The invention relates to new heterocyclic compounds of the formula (I), where R1represents a group of formula (II), R is 2,4-dioxothiazolidine-5-ylmethylene group and others, And represents C1-6alkylenes group, A represents an oxygen atom, R4represents a substituted phenyl or pyridyl which may have a Deputy, R6represents a hydrogen atom or a C1-6alkyl group, D represents an oxygen atom or sulfur, E is a CH group or a nitrogen atom, or their pharmacologically acceptable salts

The invention relates to medicine, for new DiagramItem 1,2,3-substituted benzimidazole and their water-soluble compositions of formula I, where R1, R3- Alk; ArAlk; CH2COOAlk; R2- H, Alk; ArAlk

The invention relates to the creation of new chemical compounds with anticonvulsant, antihypoxic and antioxidant activity and belonging to a new class of anticonvulsants

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 +401-2C 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 6605 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, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to benzimidazole-4-carboxamide derivatives of formula , wherein X means an alkenyl group C2-C7 substituted by two methyls, nitro-radical mono-substituted thienyl, unsubstituted quinolinyl, unsubstituted indolyl, unsubstituted pyridazinyl, unsubstituted piperazinyl, C1-C6-alkyl disubstituted piperazinyl, unsubstituted piperidinyl, unsubstituted pyrazinyl, unsubstituted imidazolyl, unsubstituted pyrimidinyl, phenyl monosubstituted pyrimidinyl, pyrimidinyl disubstituted by an amine radical and a radical specified in a group containing -F, -Cl, -Br or -I, hydroxyl trisubstituted phenyl, methoxy-radical trisubstituted phenyl, hydroxyl and methoxy-radical disubstituted phenyl, pyrazolyl disubstituted by a radical specified in a group containing a C1-C6-alkyl, and by a radical specified in a group containing -F, -C1, -Br or -I; Y means aminophenyl monosubstituted by a radical of -F, -O, -Br or -I phenyl, hydroxyethyl disubstituted by hydroxymethyl or C1-C6-alkyl and phenyl monosubstituted by a nitro group, an amino group or a halogen atom; Y also means unsubstituted piperazinyl, unsubstituted pyridyl, unsubstituted pyrazinyl, C1-C6-alkyl monosubstituted thiazol, unsubstituted pyrimidinyl, unsubstituted purinyl. The invention also refers to a pharmaceutical composition based on the compound of formula (I), using the compound of formula (I), a method for producing the compound of formula (I).

EFFECT: there are prepared new benzimidazol-4-carboxamide derivatives possessing antiviral activity.

5 cl, 6 dwg, 4 tbl, 688 ex

FIELD: chemistry.

SUBSTANCE: invention relates to encapsulation, particularly to a method of producing albendazole nanocapsules in a sodium alginate envelope. The disclosed method includes adding albendazole to a sodium alginate suspension in hexane in the presence of an E472c preparation while mixing at 1000 rps. The weight ratio of albendazole and sodium alginate is 1:3 or 3:1. Further, 1,2-dichloroethane is added. The obtained suspension of nanocapsules is filtered, washed and dried. The process of producing the nanocapsules is carried out at 25C for 20 minutes.

EFFECT: invention provides a simpler and faster process of producing nanocapsules, reduces losses during production thereof (high mass output).

3 ex, 1 dwg

FIELD: nanotechnology.

SUBSTANCE: according to the invention method, albendazole is added to the suspension of sodium alginate in butanol in the presence of the preparation E472s when stirring at 1000 revolutions per second. The mass ratio of albendazole and sodium alginate is 1:3 or 3:1. Then acetonitrile is added. The resulting suspension of the nanocapsules is filtered, washed, and dried. The process of production of nanocapsules is carried out at 25C for 20 min.

EFFECT: simplification and acceleration of the process of production of nanocapsules, reduction of losses in their production.

1 dwg, 2 ex

FIELD: medicine.

SUBSTANCE: 5-6 days before surgery, 0.15% Tantum Verde mouth wash solution is prescribed daily two times a day in a dose of 15 ml, and postoperatively the patient is supposed to take 2-3-minute oral baths of the same 3-4 times a day for 5-7 days. The postoperative care also implies 5-7 sessions of intraoral anode electrophoresis with 10% Dimexidum on the surgical area.

EFFECT: method enables providing the more effective prevention of inflammatory complications.

3 ex

FIELD: medicine.

SUBSTANCE: phenazepamum 1.0 mg is prescribed per os to patient on the eve of planned operation; then, in pre-narcosis room after catheterisation of peripheral vein suprastinum in dose 0.3 mg/kg of patient's body weight and atropine in dose 0.01 mg/kg of patient's body weight are introduced intramuscularly 30 minutes before operation. After that, solution of dexmedetomidine with concentration 4.0 mkg/ml in dose 1.0 mcg/kg of patient's body weight is introduced by intravenous infusion by syringe-batcher for 10 min.

EFFECT: method ensures optimal level of sedation and stability of haemodynamics indexes at the background of reduction of patient's psycho emotional stress and preservation of their contact with medical staff.

2 ex

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