R (+)-n-propargyl-1-aminoindan and its pharmaceutically suitable acid additive salts and a pharmaceutical composition having inhibitory b-form of the enzyme monoamine oxidase activity

 

(57) Abstract:

Usage: in acheave inhibitors of b-form of the enzyme monoamine oxidase Product - P{+)-S-propargyl-1-aminoindan its pharmaceutically suitable acid additive salt, hydrochloride. TT 184 - 185°C. (a)+30.90 Reagent 1:R-{-)-1-aminoindan Reagent 2: propargylic reaction Conditions: environment acetonitrile in the presence of FROM impasse containing R(+LM-themetal-Ü-aid in the amount of 1 - 20 mg per dose and a pharmaceutically acceptable carrier in a form for oral administration of injection solution, emulsion candles. 16 silt, 7 PL.

 

Same patents:

FIELD: medicine, anesthesiology, resuscitation.

SUBSTANCE: one should perform puncturing of epidural space at Th12-L1 level. Through the lumen of puncture needle one should introduce catheter to move it cranially at the depth of 3 cm. After that one should inject 10 ml 05%-marcaine solution to perform repeated injections per 5.0 ml every 4 h during 1-8 d. The effect is achieved due to unloading minor cycle of circulation.

EFFECT: higher efficiency of therapy.

2 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention proposes new tablets with size less 3 mm with sustained-releasing the opioid analgesic drug for 30 min in the amount above 75%. Invention provides opioid for oral intake with taking into account individual necessity of patient due to selection of required amount of mictotablets by dispenser.

EFFECT: valuable properties of tablet, expanded assortment of medicinal formulations of opioid analgesics.

19 cl, 4 tbl, 4 ex

FIELD: medicine, endocrinology.

SUBSTANCE: the present innovation deals with preventing diabetes mellitus and its aftereffects. It is suggested to apply sibutramin and its analogs to decrease non-susceptibility to insulin in diabetes-free patients, prevent decreased tolerance to glucose and decrease the quantity of introduced insulin in diabetes-suffering patients and normalize body weight, as well.

EFFECT: higher efficiency of application.

28 cl, 3 dwg, 1 tbl

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of benzene of the formula (I): wherein A represents a group taking among the following groups: -C≡C-, -CH=CH-, -CH2-CH2; n = 1 or 2; X represents hydrogen, chlorine or fluorine atom or methyl or methoxy-group; Y represents hydrogen, chlorine or fluorine atom; R1 represents cyclohexyl group monosubstituted, disubstituted, trisubstituted or tetrasubstituted with methyl group, phenyl group monosubstituted or disubstituted with fluorine or chlorine atom or methoxy-group, cycloheptyl, tert.-butyl, dicyclopropylmethyl, 4-tetrahydropyranyl or 1- or 2-adamantyl, or adamantine-2-ol group; or R1 represents phenyl group and in this case X and Y both represents chlorine atom; R2 represents hydrogen atom or (C1-C4)-alkyl group; R3 represents (C5-C7)-cycloalkyl, and salts of these compounds formed by addition of pharmaceutically acceptable acids, and their solvates and hydrates also. Also, invention relates to methods for preparing compounds of the formula (I) and to pharmaceutical composition able to interact with receptors sigma-2 based on these compounds. Invention provides preparing new compounds and medicinal agents based on thereof for treatment of autoimmune states, disturbance on heart contraction frequency and control against proliferation of tumor cells.

EFFECT: improved preparing methods, valuable medicinal properties of compositions.

18 cl, 14 tbl, 78 ex

FIELD: medicine.

SUBSTANCE: method involves administering typical tricyclic antidepressants combined with selective reverse serotonin capture inhibitors. Anxious version of subpsychotic level depressive syndrome of endogenous genesis being treated, intravenous drop-by-drop infusion of 2.-4.0 ml of 1% amitriptiline solution per 200 ml of physiologic saline is applied in 12-14 procedures combined with selective reverse serotonin capture inhibitor given per os, Zoloft is per os administered as the inhibitor at a dose of 50-100 mg. Then, supporting Zoloft therapy is applied at a dose of 100 mg during 3 months. Atypic version of depressive syndrome of subpsychotic level and endogenous genesis is treated with intravenous drop-by-drop infusion of 1.25% Melipramine solution at a dose of 2.0-4.0 ml per 200 ml of power supply source in 12-14 infusions combined with a reverse serotonin capture inhibitor. Paxyl is taken at a peroral dose of 40-60 mg as the inhibitor. Then, supporting Paxyl therapy is applied at a dose of 40-60 mg during 3 months.

EFFECT: enhanced effectiveness of treatment; reduced risk of complications; accelerated depressive syndrome relief.

FIELD: medicine.

SUBSTANCE: the suggested transdermal therapeutic system (TTS) is indicated for percutaneous injection of tolterodin for several days. It is, also, described the method for its manufacturing. The suggested TTS is being a self-gluing lamellar matrix structure that contains methacrylate copolymer including ammonium groups, at least, one plastifier and up to 25 weight% tolterodin. TTS is of good tolerance by skin and is of good physical and chemical stability at prolonged storage and application, it, also, has got good adhesive properties and can provide the penetration of maximal quantity of active substance through skin.

EFFECT: higher efficiency of application.

8 cl, 2 dwg, 3 ex, 3 tbl

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to new acid-additive nitrate salts of compounds taken among salbutamol, cetirizine, loratidine, terfenadine, emedastine, ketotifen, nedocromil, ambroxol, dextrometorphan, dextrorphan, isoniazide, erythromycin and pyrazinamide. Indicated salts can be used for treatment of pathology of respiratory system and elicit an anti-allergic, anti-asthmatic effect and can be used in ophthalmology also. Indicated salts have less adverse effect on cardiovascular and/or gastroenteric systems as compared with their non-salt analogues. Also, invention proposes pharmaceutical compositions for preparing medicinal agents for treatment of pathology of respiratory system and comprising above indicated salts or nitrate salts of metronidazol or aciclovir.

EFFECT: improved and valuable properties of compounds.

6 cl, 5 tbl, 19 ex

FIELD: medicine.

SUBSTANCE: method involves applying fractal introduction of 0.2 mg/kg MT calypsol and 0.4 mcg/kg MT fentanyl every 10 min during operation. Additional local spinal cord root irrigation with 2% lidocaine solution at maximum traumatic operation moment.

EFFECT: enhanced effectiveness of treatment; preserved spontaneous patient respiration.

1 tbl

FIELD: organic chemistry, medicine.

SUBSTANCE: invention reports about preparing new substituted derivatives of 2-dialkylaminoalkylbiphenyl of the general formula (I):

wherein n = 1 or 2; R1 means cyano-group (CN), nitro-group (NO2), SO2CH3, SO2CF3, NR6aR7a, acetyl or acetamidyl; R2 means hydrogen atom (H), fluorine atom (F), chlorine atom (Cl), bromine atom (Br), cyano-group (CN), nitro-group (NO2), CHO, SO2CH3, SO2CF3, OR6, NR6R7, (C1-C6)-alkyl, acetyl or acetamidyl being alkyl can comprise one or more similar or different substitutes taken among halogen atom or hydroxy-group; or R1 and R mean in common group -OCH2O, -OCH2CH2O, CH=CHO, CH=C(CH3)O or CH=CHNH; R3 means H, F, Cl, Br, CN, NO2, CHO, SO2CH3, SO2CF3, OR6, NR6R7, (C1-C6)-alkyl, acetyl or acetamidyl being alkyl can comprise one or more similar or different substitutes taken among halogen atom or hydroxy-group; R4 and R5 have similar or different values and mean hydrogen atom (H) or unsubstituted (C1-C6)-alkyl; R6 and R7 have similar or different values and mean hydrogen atom (H) or unsubstituted (C1-C6)-alkyl; R6a means hydrogen atom (H) or unsubstituted (C1-C6)-alkyl; R7a means unsubstituted (C1-C6)-alkyl as their bases and/or salts of physiologically acceptable acids, with exception of compound representing 4-chloro-2'-dimethylaminomethylbiphenyl-2-carbonitrile and to a method for their preparing. Derivatives of 2-dialkylaminoalkylbiphenyl can be used in medicine for treatment or prophylaxis of pains, inflammatory and allergic responses, depressions, narcomania, alcoholism, gastritis, diarrhea, enuresis, cardiovascular diseases, respiratory ways diseases, cough, psychiatry disorders and/or epilepsy.

EFFECT: valuable medicinal properties of compounds.

13 cl, 2 tbl, 43 ex

FIELD: obstetrics and gynecology.

SUBSTANCE: over a 2-5 day period, 2.0 ml of Ginipral is administered once a day intravenously in a drop-by-drop manner followed by intravenously drop-by-drop administered 30-40 min later 2.0 ml of Instenone and, in the evening, 1 dragee Instenone orally. Afterwards, Instenone and Ginipral are administered orally: the former in dose of 1 dragee thrice a day with meal and the latter in dose of 1 pellet four times a day after meal until symptoms of the risk of prevention of pregnancy disappear.

EFFECT: prolonged pregnancy and prevented premature birth, which favors reduced irritation, normalized tonus, contractive activity of uterus, and improved psychic and emotional state of women.

2 ex

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to novel derivatives of fullerenes comprising organic amines and hydrogen atoms bound to fullerene-C60 molecule by 6,6-double bonds of the general formula: C60Hn(R1R2N)n wherein R1 means -C6H5CH2; R2 means -C6H5CH2; n = 4 (tetra-(dibenzylaminohydro)[60]fullerene); R1 means -C5H9; R2 means hydrogen atom (H); n = 3 (tri-(cyclopentylaminohydro)[60]fullerene). Also, invention relates to using derivatives of fullerenes, in particular, (tetra-(benzylaminohydro)[60]fullerene, (tetra-(dibenzylaminohydro)[60]fullerene, tri-(cyclopentylaminohydro)[60]fullerene, 2-(azahomo[60]fullereno)-5-nitropyrimidine, 1,3-dipropyl-5-[5'-(azahomo[60]fullereno)pentyl]-1,3,5-triazin-2,4,6(1H,3H,5H)-trione, O,O-dibutyl-(azahomo[60]fullereno)phosphate as acceptors of electrons in composites polymer/fullerene designated for photovoltaic cells. Also, invention relates to photovoltaic device comprising mixture of poly-conjugated polymer and abovementioned fullerene derivative or their mixture as an active layer. Also, invention relates to a method for synthesis of derivatives of fullerenes comprising aromatic amines and hydrogen atoms bound to fullerene-C60 molecule by 6,6-double bonds. Method involves interaction of C60 with the corresponding organic amine in solution, and this reaction is carried out in aromatic solvent medium in amine excess at temperature 25-70°C for 2-5 days followed by evaporation of solution and precipitation of the end product by addition of alcohol.

EFFECT: improved method of synthesis.

6 cl, 1 tbl, 2 dwg, 6 ex

FIELD: chemical technology, pharmacy.

SUBSTANCE: invention relates to an improved method for preparing sertraline hydrochloride form V that possesses the antidepressant effect. Method involves the following steps: (a) dissolving or suspending sertraline mandelate in a protonic solvent or a mixture of protonic solvents; (b) decreasing pH value of solution or suspension by addition of HCl aqueous solution of HCl solution in protonic solvent with addition of water to form a clear solution, and (c) isolation of the sertraline hydrochloride form V. At step (a) solvents from group comprising alcohol, water or their mixtures are chosen as solvents. For example, an alcoholic solvent used in step (a) can be chosen from group comprising methanol, ethanol, n-propyl alcohol, isopropyl alcohol, n-butyl alcohol, tert.-butyl alcohol and isobutyl alcohol or their mixtures but isopropyl alcohol is preferable. The dissolving or suspending step (a) is carried out at heating and/or stirring in solvent at temperature in the range 20-90oC usually. Decreasing the pH value in step (b) is carried out usually up to the range 1-3 preferably. Sertraline hydrochloride form V obtained at step (c) is isolated by cooling the mixture obtained at step (b). Cooling is carried out under natural conditions to room temperature or using mild cooling agents, such as cold water, water, alcohol or their mixtures wherein indicated alcohol is chosen from group comprising monohydric alcohol, dihydric alcohol or their mixtures. Also, invention relates to a method for preparing a pharmaceutical composition with immediate releasing the sertraline hydrochloride form V that involves mixing sertraline hydrochloride form V prepared by cl. 1 having particles size less 20 mcm and in the amount 90% of the total amount of particles, not less, with a pharmaceutically acceptable diluting agent, carrier or carrier. Proposed method provides simplifying the process for preparing the preparation based on decreasing the total amount of steps.

EFFECT: improved preparing method.

14 cl, 4 sch, 2 dwg, 1 tbl

FIELD: chemistry.

SUBSTANCE: described is a compound of formula

or its pharmaceutically acceptable salt, where m, p, q, Ar, R1 and R2 are as given in the description, as well as a pharmaceutical composition with selective affinity to 5-HT receptors which contains a formula (I) compound.

EFFECT: obtained compounds have selective affinity to 5-HT receptors and can be used, as expected, in treating certain central nervous system disorders.

21 cl, 1 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel aminoindane derivatives of formula (Ia) or pharmaceutically acceptable salts thereof, which have NMDA receptor antagonist effect, and can be used to prepare a medicinal agent for treating dementia. In formula (Ia):

,

R1 is a lower alkyl, C5-C6 cycloalkyl, phenyl which can be substituted with OH, lower alkyl, halogen atom, O-alkyl, C5-C6 heteroaryl containing a S atom as a heteroatom, or lower alkyl substituted with one or more halogen atoms, R2 and R3 are identical or different, each denoting alkyl or phenyl, R4 and R5 are identical or different and each denotes a hydrogen atom, lower alkyl, -O-lower alkyl, -lower alkylene-OH or -lower alkylene-O-lower alkyl, R6-R9 are identical or different and each denotes a hydrogen atom, lower alkyl, -O-lower alkyl, halogen atom, lower alkyl substituted with one or more halogen atoms, OH, CN, lower alkenyl or nitrogen-containing C5-C6 heterocyclic group, R10 and R11 are identical or different and each denotes a hydrogen atom or lower alkyl. The invention also relates to a pharmaceutical composition containing the said compounds.

EFFECT: improved properties of the derivative.

6 cl, 15 tbl, 130 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents a pharmaceutical composition containing transnorsertraline or its pharmaceutically acceptable salt or solvate, and mannitol or xylitol, as well as to a method of treating, preventing or reducing recurrent neurological disturbance, involving administration of the above composition into the patient.

EFFECT: invention provides creating the pharmaceutical composition of transnorsertraline, possessing improved chemical and physical stability.

11 cl, 26 tbl, 10 dwg

FIELD: chemistry.

SUBSTANCE: present invention relates to novel compounds of formula (1) or pharmaceutically acceptable salts thereof having inhibitory effect on LSD1 (lysin-specific demethylase-1 inhibitors). Said activity enables their use for treating or preventing some diseases such as cancer. Above cancer is selected from the group including breast cancer, colorectal cancer, lung cancer, prostate cancer, testicular cancer, cerebral cancer, skin cancer and blood cancer. In compounds of formula 1

,

(A) denotes a pyridyl or phenyl; each (A′), if conained, is independently selected from a group consisting of phenyl, phenyl-C1-C4-alkoxy group, phenyl-C1-C4-alkyl, halogen, C1-C4-alkoxy group and halogen-C1-C4-alkyl, where each (A′) contains 0, 1, 2 or 3 substitutes independently selected from a group comprising halogen, halogen-C1-C4-alkyl, phenyl, C1-C4-alkyl and C1-C4-alkoxy group; X equals to 0, 1 or 2; (B) denotes cyclopropyl ring, where (A) and (Z) covalently connected with different carbon atoms in (B); (Z) denotes -NH-; (L) is selected from rhe group including a single link, -CH2-, -CH2CH2-, -CH2CH2CH2- and -CH2CH2CH2CH2-; and (D) denotes C3-C7-cycloalkyl or benzo-C5-C7-cycloalkyl, where said C3-C7-cycloalkyl or said petrol-C5-C7-cycloalkyl, contains 0, 1, 2 or 3 substitutes independently selected from the group, including -NH2, halogen, amido group, C1-C4-alkoxy group and halogen-C1-C4-alkyl; or its pharmaceutically acceptable salt. Compound, which is substituted with heteroarylcyclopropylamine or substituted arylcyclopropylamine and correponds to formula 2

,

where (R3) is present or is not, if (R3) is present, it is selected from the group consisting of phenyl-C1-C4-alkyl and phenyl-C1-C4-alkoxy group, where the said group (R3) contains 0, 1, 2 or 3 substitutes independently selected from the group including halogen, C1-C4-alkyl, C1-C4-alkoxy group, halogen-C1-C4-alkyl and phenyl; (W) denotes phenyl or pyridyl group, where the said (W) contains 0, 1 or 2 substitutes selected from the group including halogen, C1-C4-alkoxy group, halogen-C1-C4-alkyl and phenyl; (L′) denotes a bridge of formula -(CH2)n-, where n equals 0, 1, 2, 3 or 4; and R4 is C3-C7-cycloalkyl or benzo-C5-C7-cycloalkyl, wherein the above C3-C7-cycloalkyl or said benzo-C5-C7-cycloalkyl contains 0, 1, 2 or 3 substitutes, selected from the group including halogen, C1-C4-alkoxy group, halogen-C1-C4-alkyl, amine group and C-amido group; may be used as LSD1 selective inhibitor for identification method within the group of formula 2 compounds, which inhibits LSD1 in greater degree than MAO-A and/or MAO-B.

EFFECT: said compounds may be used for production of medicinal agent having LSD1 inhibiting activity for in treatment or preventing diseases or pathological condition.

51 cl, 1 tbl, 21 ex

циклопропил - cyclopropyl

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