3-methyl-1,2,4-triazole-5-thioacetate (s) -2,6-diaminohexane acid application as active drug base for prevention and treatment of cns vital functions in case of severe forms of acute ethanol poisoning
SUBSTANCE: 3-methyl-1,2,4-triazole-5-thioacetate (s)-2,6-diaminohexane acid application as active drug base for prevention and treatment of cns vital functions in case of severe forms of acute ethanol poisoning is proposed.
EFFECT: highly effective prevention of central nervous system vital functions in case of preventive administration, adjustment of neurotoxic lesions in case of severe forms of acute ethanol poisoning, which in turn allows earlier restoration of the central nervous system vital functions and mortality reduction in case of acute ethanol poisoning.
SUBSTANCE: method involves a combined administration of the preparations Enterosgel, Kudesan and Pantogam. Enterosgel is administered orally in the form of gel 30 minutes before meals in a dose of 1 teaspoon two times a day for 7 days. Kudesan is also administered orally during meals before noon in an age dose of: 10-16 drops (15-24 mg) in the children aged 5 through 7 years old, 16-20 drops (24-30 mg) in the children aged 8 through 10 years old, pre-dissolved in a small amount of boiled water or other beverage of room temperature, once a day in the course of 30 days. Pantogam is administered orally 15-20 minutes after meals in an age dose of: 500 mg 2 times a day in the children aged 5 through 7 years old, 500 mg 3 times a day in the children aged 8 through 10 years old in the course of 30 days.
EFFECT: complex administration regiment provides the effective correction of cognitive disorders in the given group of children by a synergetic detoxification, antioxidant and neuroprotective action of its components.
3 cl, 4 tbl
SUBSTANCE: application of 5% water solution of sodium and potassium salts of humic acids, obtained from leonardite brown coal, in dose 10.0 mg/kg as membrane-protective preparation.
EFFECT: application of composition described above makes it possible to extend arsenal of membrane-protective preparations from low-toxic, cheap, available natural raw material.
2 dwg, 2 ex
SUBSTANCE: agent possessing detoxification activity, containing succinic acid, 10% ethanol extract of propolis, polyethylene glycol 400, polyethylene glycol 1500, polyethylene glycol 4000, Cremophor CO-40, Tween-80 and purified water in certain proportions.
EFFECT: agent possesses the detoxification action, the uniform release of the active substances and the pronounced prolonged action.
2 cl, 4 dwg, 4 tbl, 8 ex
SUBSTANCE: invention relates to radiation and experimental biology, biotechnology and medicine, namely to means of radiological protection and to stimulators of colony formation of stem cells. Invention can be used in research and clinical practice for protection of living organisms in case of exposure to ionising radiation, in emergency and military medicine, in case of emergency situations as means for protection against radiation injury. Claimed is application of preparation gamma-plant as radioprotector with colony-stimulating properties for increasing survival and improving state of organisms, subjected to irradiation. Gamma-plant is non-toxic polysaccharide of vegetable origin, registered by Ministry of Health of the Russian Federation and allowed for medical application; Gamma-plant is included into Russian Pharmacopoeia in section FG-9 "non-narcotic analgesics".
EFFECT: invention makes it possible to increase efficiency of colony formation of stem cells in spleen 2,0-2,3 times, increases survival of experimental animals to 95% with coefficient of dose reduction factor DRF, equal 2-2,2.
SUBSTANCE: invention refers to veterinary science, namely to clinical pharmacology and veterinary therapy. The method consists in administering the complex iron-dextran preparation Ferranimal-75M intramuscularly on the 5th day of calf's life in a dose of 3 ml in a combination with an intramuscular injection of the preparation Hydropeptone in a dose of 10 ml. Ferranimal-75M is injected 10 days later in a dose of 2 ml in a combination with an injection of Hyropeptone 5 ml intramuscularly in different points.
EFFECT: method provides higher antioxidative activity of calf's blood serum, reduced pro-oxidant action of iron and incorporated radionuclides, as well as higher iron accessibility in treating and preventing iron-deficiency anaemia in calves exposed to the chronic incorporated radiation.
SUBSTANCE: first, Fraxiparine is inhaled for 5-10 minutes. A dialysis solution for peritoneal dialysis containing extranyl is administered into the abdominal cavity 1-1.5 hours later through a catheter. The solution additionally contains: albumin in the concentration of 35-40 g/l, heparin in the concentration of 500-750 Unit/l and papaverine in the concentration of 50-100 mg/l. Every 6-8 hours after the beginning of exposure of the dialysis solution in the abdominal cavity, the Fraxiparine inhalations are repeated. The time of a single exposure of the dialysis solution in the abdominal cavity makes 12-18 hours.
EFFECT: method provides effective body detoxification in the given category of patients by providing a high toxin clearance owing to a continuous high osmotic concentration of the solution and the dilatation of pre-capillary peritoneal arterioles, prevented inspissation of the albumin solution to the colloidal state and its inactivation that reduces a rate of the dialysis solution exchanges.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, namely to an immunomodulatory composition for injection into a mammal. The immunomodulatory composition for injection into a mammal containing a hydrolysate prepared by acid and/or enzymatic hydrolysis of one or more bioresources specified in a group consisting of bivalve molluscs, annelids, leeches, and water taken in certain proportions. A method for preparing the immunomodulatory composition for injection into a mammal. A method of treating a pathological condition in a mammal in need thereof involving the injections of the immunomodulatory composition into the above mammal. Using the composition for normalising metabolism into the mammal in need thereof.
EFFECT: composition enables extending the range of products with immunomodulatory activity for injections.
19 cl, 7 tbl, 7 ex
FIELD: veterinary medicine.
SUBSTANCE: method of treatment of calves with Simuliidotoxicosis is that 40% solution of urotropine is administered intravenously to calves at a dose of 1.5 ml per 10 kg of animal body weight.
EFFECT: improvement of efficiency of the method.
SUBSTANCE: group of inventions relates to veterinary and medicine, in particular to obtaining and application of biopreparations for immunotherapy of ecopathologies. The group of inventions includes obtaining a protein antigen from a mixture of anatoxins from three enteropathogenic virulent strains of a pathogen of escherichiosis of calves E.coli No. 378, 379, 380 by their growing on Hottinger medium with further addition of 0.4-0.5% formalin, following thermostating for 10-12 days and cooling the mixture of anatoxins with a sterile solution of aluminium hydroxide, after that obtaining radioantigen from E.coli "PL-6" by growing cultures on a meat infusion agar with further washing away a biomass by a physiological solution and irradiation of the obtained suspension with a concentration of 1.2·1010 m.c./cm3 on a gamma-installation in a dose of 140-150 Gr with following thermostating and extraction of radiotoxin with 70% acidified with 0.05% hydrochloric acid to pH 5.5 ethanol, following evaporation of the exractant to the initial volume, after that, obtaining protein-cadmium radioantigen first by preliminary dechlorination of cadmium chloride, obtaining cadmium hydroxide, addition into the obtained 2.7% solution of the antigen of 0.77% solution of cadmium hydroxide in a ratio of 1:1 with following thermostating at a temperature of 37°C for 30 minutes, evaporation and dissolution of the residue to 12.8% concentration, further obtaining protein-cadmium radioantigen by an addition of 1.2% solution of a mixture of three anatoxins of E.coli and 12.8% solution of cadmium radioantigen in a ratio of 1:9, conjugation of components at room temperature for 8-10 hours, standardisation by a dry substance to 10% concentration and pouring into vials, and storage at a temperature of 4-6°C. The group of inventions also relates to a method of treating radiation, chemical and/or bacteriological damage to an organism by introduction of 10% solution of complex protein-cadmium radioantigen.
EFFECT: application of the group of inventions is effective in treatment of radiation, chemical and/or biological damage.
4 cl, 6 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to medicine and particularly to preparations for a therapy of oncological diseases, treatment of allergy, prevention and health improvement. The invention represents a method for preparing fraction 4 (ADP-f4) and fraction (ADP-f5) adaptogenic Dorogov's preparations, characterised by the fact that a primary product is a fraction 2 antiseptic Dorogov's stimulator (ADP-f2) to be thermally treated.
EFFECT: implementing the given invention provides the more effective prevention and eliciting anti-stress reactions for the purpose of improving the functional state of organism and increasing a resistance in an activation therapy.
SUBSTANCE: invention relates to novel compounds of formula
possessing properties of binding with delta opioid receptors. In formula I R1 is selected from the group, consisting of phenyl, pyridinyl and thiazolyl, with R1 being optionally substituted with one or two substituents, independently selected from the group, consisting of C1-4alkoxy, fluorine atom, chlorine atom, bromine atom and cyanogroup; in addition, R1 is optionally substituted with di(C1-4alkyl)aminocarbonyl; Y represents O, S, H3, vinyl, ethinyl or S(O); R2 represents a substituent, selected from the group, consisting of hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, fluorine atom, chlorine atom, bromine atom and hydroxy; Ra represents hydrogen or methyl; R3 is selected from the group, consisting of pyrrolidin-2-ylmethyl; pyrrolidin-3-ylmethyl; piperidin-2-ylmethyl, piperidin-3-ylmethyl, piperidin-4-ylmethyl, piperidin-2-ylethyl, piperidin-3-ylethyl, piperidin-4-ylethyl, pyridine-4-yl-(C1-2)alkyl, azetidin-3-ylmethyl; morpholin-2-ylmethyl, morpholin-3-ylmethyl, imidazolylmethyl, thiazolylmethyl, (amino)-C3-6cycloalkyl, 3-hydroxy-2-aminopropyl, 8-azabicyclo[3.2.1]octanyl, 1-azabicyclo[2.2.2]octanyl, guanidinylethyl, 4-(imidazol-1-yl)phenylmethyl, 2-(methylamino)ethyl, 2-diethylaminoethyl, 4-diethylaminobut-2-yl, piperidin-3-yl, piperidin-4-yl and pyrrolidin-3-yl; with piperidin-3-yl being optionally substituted on a carbon atom with phenyl; with pyrrolidin-2-yl in pyrrolidin-2-yl-methyl, pyrrolidin-3-yl, piperidin-3-yl and piperidin-4-yl being optionally substituted on a nitrogen atom with methyl, phenylmethyl, phenethyl or methylcarbonyl.
EFFECT: compounds can be used in the treatment of pain, induced by diseases or conditions, such as osteoarthritis, rheumatoid arthritis, migraine, burn, fibromyalgia, cystitis, rhinitis, neuropathic pain, idiopathic neuralgia, toothache, etc.
24 cl, 3 tbl, 19 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to novel compounds of formula I, possessing ability of binding with delta-opioid receptors. In formula R1 is selected from the group, consisting of i) phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxyl, di(C1-4alkyl), aminocarbonyl, chlorine and fluorine, in such a way that only one di(C1-4alkyl)aminocarbonyl is present; ii) naphthyl; iii) pyridinyl, optionally substituted with one substituent, selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxy, fluorine, chlorine and cyano; iv) pyrimidin-5-yl; v) furanyl; vi) thienyl; vii) 5-oxo-4,5-dihydro-[1,2,4]oxodiazol-3-yl; and viii) di(C1-2alkyl)aminocarbonyl; Y represents ethyl, vinyl or bond; or Y represents O, when R1 represents optionally substituted phenyl, where substituent represents C1-4alcoxy; R2 represents phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, fluorine, chlorine and cyano, trifluoromethoxy and hydroxy; or R2 represents phenyl, substituted with one aminocarbonyl, di(C1-4alkyl)aminocarbonyl, C1-4alcoxycarbonyl or carboxysubstituent; R3 is selected from the group, consisting of i) 3-aminocyclohexyl; ii) 4-aminocyclohexyl; iii) piperidin-3-yl; iv) piperidin-4-yl; v) pyrrolodin-2-yl-methyl, in which pyrrolodin-2-yl is optionally substituted by 3-rd or 4-th position with one or two fluorine-substituents; vi) azetidin-3-yl; vii) 2-(N-methylamino)ethyl; viii) 3-hydroxy-2-aminopropyl; ix) piperidin-3-yl-methyl; x) 1-azabicyclo[2.2.2]octan-3-yl; and xi) 8-azabicyclo[3.2.1]octan-3-yl; or R3 together with Ra and nitrogen atom, which they both are bound to, form piperazinyl, optionally substituted with 4-C1-4alkyl; Ra represents hydrogen, 2-(N-methylamino)ethyl or C1-2alkyl, optionally substituted with azetidin-3-yl.
EFFECT: compounds can be used in treatment of pain in the range from medium to strong, caused by diseases or conditions, such as osteoarthritis, migraine, burn, fibromyalgia, cystitis, rhenite, neuropathic pain, idiopathic neuralgia, toothache, etc.
21 cl, 4 tbl, 26 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, namely to using medicinal plant Gelsemium elegans Benth. and Datura metel L. blossom in preparing a therapeutic agent for eliminating or relieving acute and persistent withdrawal symptoms caused by taking a dependence-producing substance. The invention refers to pharmaceutical compositions (versions) for eliminating or relieving acute or persistent withdrawal symptoms caused by taking the dependence-producing substance, and containing Gelsemium elegans Benth. and Datura metel L. blossom in certain relations.
EFFECT: pharmaceutical compositions containing Gelsemium elegans Benth and Datura metel L. blossom are effective for the individuals suffering drug dependence.
15 cl, 12 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, namely to a composition for treating nicotine addiction by means of an electronic device intended to simulate tobacco smoking. A pharmaceutical composition for treating nicotine addiction by means of the electronic device comprising a cartridge simulating tobacco smoking with the use of vapour or fog generating compound containing water, glycerol, propylene glycol, contains citric acid additionally, as well as varenicline, or anabasin hydrochloride, or cytisin taken in certain relations. A method for preparing the pharmaceutical composition by mixing water, glycerol, propylene glycol and citric acid, as well as varenicline, or anabasin hydrochloride, or cytisin. The cartridge of the electronic device for simulating tobacco smoking. A method of treating nicotine addiction by means of simulating tobacco smoking by means of the electronic device.
EFFECT: pharmaceutical composition described above enables treating nicotine addiction effectively.
4 cl, 2 dwg, 5 tbl, 15 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: group of inventions relates to methods of obtaining a lyophilised preparation of tetrodotoxin and to a tetrodotoxin preparation for relief of the drug withdrawal in case of addiction to opiates. The method of obtaining the lyophilised preparation of tetrodoxin includes the following stages: 0.1-20 mcg/dose of tetrodotoxin is dissolved with 0.1% solution of citric acid to regulate pH within the range of 3.5-4.5 in injection water and filtered to remove pyrogen; separately dissolved are: a stabiliser - dextran or trehalose - and a filling agent, representing an isotonic solution of sodium chloride or mannit in injection water. After that, 0.1% solution of citric acid is added to regulate pH within 3.5-4.5, then, activated carbon is added with keeping at a temperature of 60°C and mixing for more than 30 minutes, filtering to remove pyrogen and cooling to room temperature. After homogeneous mixing of the obtained solutions and realisation of ultrafiltration, lyophilic drying is carried out. Lyophilic drying consists in preliminary freezing, drying under vacuum at reduced temperature, drying under vacuum at increased temperature, with each drying being performed at a certain temperature for the specified time period. After that, filling with inert gas is performed with control of water content at 3% level, with further sealing. Another version includes addition of additional solution of lidocaine chloride to the solution of tetrodotoxin and citric acid at the first stage. Also disclosed is the tetrodotoxin preparation for relief of the drug withdrawal in case of addiction to opiates, obtained by the said method, which is characterised by the weight ratio tetrodotoxin:filling agent:stabiliser, equal to 1:(150-3000):(50-6000).
EFFECT: claimed group of inventions ensures obtaining the stable tetrodotoxin solution with accurate dosage, which is used for introduction into the human organism.
25 cl, 9 tbl, 14 dwg
FIELD: medicine, pharmaceutics.
SUBSTANCE: there are presented: a combination possessing analgesic action of at least one sigma ligand and at least one opioid or opiate compound specified in morphine and its structural derivatives, phentanyl and tramadol for simultaneous, separate or sequential administration; the sigma ligand has the general formula ;
using it for preparing a therapeutic agent potentiating analgesic action of morphine or its structural derivatives, phentanyl and tramadol and/or relieving addiction thereto. What is also presented is using the combination of at least one sigma ligand and at least one opioid or opiate compound for preparing the therapeutic agent for potentiating analgesic action of opioids or opiates and for relieving addiction thereto; the opiate is specified in a group of: hydromorphone, oxymorphone, desomorphine, diacetylmorphine, nicomorphine, dipropanoylmorphine, benzylmorphine and ethylmorphine.
EFFECT: what is shown is the synergetic analgesic action of the morphine and compound 63 combination; the compound appeared to relieve the effects of positive stimulation caused by morphine with establishment of behaviour reflex.
16 cl, 10 dwg
SUBSTANCE: conjugate represents benzoate-hydrocodone that has the following structure: benzoate-hydrocodone (Bz-HC). Invention also pertains to the application of pharmaceutical compound for obtaining the drug for curing the patient with illness, disease or condition mediated by opioid binding to the opioid receptors of the patient.
EFFECT: improvement of medical treatment efficiency or prevention of drug abuse, drug withdrawal symptoms or pain relief.
10 cl, 11 ex, 4 tbl, 20 dwg
SUBSTANCE: invention refers to medicine, namely to psychiatry and drug addiction, and may be used for detoxification-infusion therapy of the patients used psychotropic cannabis products. That is ensured by the infusion intravenous drop-by-drop sequential administration of drugs. A mixture containing 5% glucose 200 ml, 25% magnesium sulphate 10 ml and 4% potassium chloride 10 ml are administered. That is combined with the additional bolus administration of 5% vitamin B1 2 ml. That is followed by introducing a mixture containing 0.9% normal saline 200 ml and 20% piracetam 10 ml. That is added with the bolus administration of 5% vitamin B6 10 ml. Then, a mixture containing rheopolyglucin 200 ml, 5% ascorbic acid 5 ml and 1% nicotinic acid 1 ml is administered. Then, a mixture containing 0.9% normal saline 200 ml and 2.4% aminophylline 5 ml is administered. The procedure is performed twice a day for 10 days.
EFFECT: method provides the higher therapeutic effectiveness and reduced length of the therapy, as well as the presented method is reproducible easily.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to medicine and describes a disulphiram implant for treating the alcohol or opiate addictive patients. The implant contains disulphiram 95.0-59.0 wt %, nitrogen polymer composition 4.8-40.5 wt % and stearic acid or magnesium stearate 0.2-0.5 wt %. The nitrogen polymer composition contains N-vinylpyrrolidone and 2-methyl-5-vinylpyridine copolymer or salts of branched oligomers hexamethylene diamine and guanidine, and polyvinylpyrrolidone.
EFFECT: implant may be used in addictology and provides a prolonged and uniform release of disulphiram with improving incisional wound healing.
5 ex, 2 tbl
FIELD: medicine, pharmaceutics.
SUBSTANCE: there are presented methods of treating or preventing an addiction or recurrent addictive behaviour, including: alcohol, nicotine, marijuana, marijuana derivative, opioid receptor antagonist, benzodiazepine, barbiturate and psychostimulant by administering the peroxisome proliferator-activated receptor gamma (PPARγ) agonist thiazolidinedione, alone or in a combination with another therapeutic agent - an opioid receptor agonist, a mixed partial opioid receptor agonist/antagonist, an anti-depressant, an antiepileptic agent, an antiemetic agent, a corticotrophin releasing factor 1 (CRF-1) receptor antagonist, a selective serotonin 5-HT3 receptor antagonist, a 5-HT2A/2C antagonist or a cannabinoid 1 (CB1) receptor antagonist (versions), related pharmaceutical compositions with the above combinations (versions), a standard dosage form (versions) and kits (versions).
EFFECT: it is shown that the PPARγ agonist pioglitazone had no effect on amphetamine sensitisation, however it reduced opiate consumption and opiate addiction, also reduced nicotine self-administration in rats, and reduced alcohol consumption if synergistically combined with topiramate Pioglitazone reduced ethanol self-administration in rats.
33 cl, 23 dwg, 27 ex
SUBSTANCE: invention relates to organic chemistry and specifically to novel heterocyclic compounds of general formula (I) or enantiomers, diastereomers or pharmaceutically acceptable salts thereof, where Y is: phenyl or a heteroaryl selected from thiazolyl, pyridyl, pyrimidinyl, 1,3,5-triazinyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl and 1,3,4-thiadiazolyl; wherein the phenyl or heteroaryl is optionally substituted with one substitute selected from fluorine, chlorine, bromine, iodine, C1-4alkyl, trifluoromethyl, C1-4alkoxy, C1-4alkylthio, nitro and cyano; r=1-2; R2 is absent or is an oxo-group; Z is: (a) phenyl substituted with NRaRb; where Ra is: H or C1-4alkyl; where Rb is: C1-4alkyl, cycloalkyl, phenyl, furanylmethyl, or phenyl(C1-2alkyl); and wherein the phenyl or the furanyl are optionally substituted with iodine; alternatively, Ra and Rb are taken together with the nitrogen atom to which they are bonded to form a 5-8 member heterocyclyl, which is optionally condensed to a benzene ring; (b) biphenyl-3-yl or biphenyl-4-yl; where the interior phenyl ring, attached to the carbonyl in formula (I) is optionally substituted with a fluorine atom; and where the terminal phenyl ring is optionally substituted with a substitute selected from trifluoromethyl, C1-4alkoxy, chlorine, dichloro, fluorine, and iodine; (c) phenyl substituted with a substitute selected from C5-8cycloalkyl, -NHC(=O)cyclohexyl, phenyloxy, phenylcarbonyl, phenyl(C1-3)alkyl, phenyl(C1-3)alkoxy, pyrrolyl, pyrazolyl, imidazolyl, isoindol-2-yl-l,3-dione, 2,3-dihydro-isoindol-2-yl; l-(tert- butoxycarbonyl)piperidin-4-yloxy, and 1-(tert-butoxycarbonyl)piperidin-4-yl; (d) phenyl substituted with 1-2 substitutes independently selected from: C1-6alkyl, C1-4alkoxy, iodine, chlorine and nitro; (e) phenyl(C1-2)alkyl; where the phenyl is optionally substituted with 1 or 2 substitutes independently selected from iodine, fluorine, C1-6alkyl, phenyl and NRcRd; where Rc: H or C1-4alkyl; where Rd is: C1-4alkyl or C1-6cycloalkyl(C1-4)alkyl; and where the C1-2alkyl of phenyl(C1-2)alkyl is optionally substituted with phenyl; (f) phenyl(C2-4)alkenyl; where the phenyl is optionally substituted with a substitute selected from C1-4alkyl, C1-4alkoxy, trifluoromethyl, trifluoromethylthio and phenyl; (g) naphthyl; where the naphthyl is optionally substituted with one C1-4alkoxy substitute; (h) fluorenyl or xanthenyl; where the fluorenyl or xanthenyl is optionally substituted with an oxo group; (i) C5-8cycloalkyl; where the C5-8cycloalkyl is optionally substituted with one C1-6alkyl substitute; (j) benzene ring-condensed C5-8cycloalkyl or benzene ring-condensed C5-8cycloalkyl(C1-4)alkyl; where said C5-8cycloalkyl fragment is optionally substituted with 1-4 methyl groups; (k) bicyclo[2.2.2]octyl-1-yl; where the bicyclo[2.2.2]octyl-l-yl is optionally substituted with C1-6alkyl; (1) a heteroaryl or benzene ring-condensed heteroaryl selected from benzooxazolyl, quinolinyl, benzimidazolyl, pyridinyl, indolyl, thienyl, furanyl, pyrazolyl, oxazolyl, benzothienyl and benzofuranyl; where the heteroaryl or benzene ring-condensed heteroaryl is optionally substituted with 1 or 2 substitutes independently selected from C1-4alkyl, trifluoromethyl, C5-8cycloalkyl, phenyl, phenyl(C1-2)alkoxy, phenyl(C2-4)alkynyl and dichlorophenoxy; and where the phenyl substitute in the heteroaryl is further optionally substituted with C1-4alkyl, C1-4alkoxy or trifluoromethyl; (m) l,5-diphenyl-lH-pyrazol-3-yl; where the pyrazol-3-yl is optionally substituted with a methyl group; and where each of the phenyl groups of the 1,5-diphenyl substitutes is also optionally substituted with substitutes selected from chlorine, dichloro or aminosulphonyl; (n) 1,2,3,4-tetrahydroquinolin-6-yl; where the 1,2,3,4-tetrahydroquinolin-6-yl is optionally substituted with phenyl or trifluoromethyl-substituted phenyl; and (o) benzene ring-condensed heterocyclyl(C2-4)alkenyl; where the benzene ring-condensed heterocyclyl is attached to the C2-4alkenyl via the benzene ring; and where benzene ring-condensed heterocyclyl is further optionally substituted with C5-6cycloalkyl; taking into account constraining conditions indicated in claim 1. The invention also relates to a pharmaceutical composition based on the compound of formula (I), a method of producing said pharmaceutical composition, a method of treating said pathological conditions and use of the compound of formula (I).
EFFECT: obtaining novel heterocyclic compounds having MGL inhibiting activity.
21 cl, 5 tbl, 11 ex