|
|
Technetium and rhenium complexes with bis(heteroaryls) and methods for using them Invention refers to a compound presented by formula OR or its pharmaceutically acceptable salt or solvate. The radical values are as follows: Rt - H, C1-C8 alkyl group, ammonium ion, alkali or alkali-earth ion; R84 - substituted C1-8 alkyl; R - C1-8 hydroxyalkyl, C1-8 alkoxyalkyl, C1-8 aminoalkyl, (CH2)8(NHC(S)NH)Ph(SO2NH2), (CH2)dPh(SO2NH2), (CH2)5C(O)NH-(1-acetylpyrrolidin-2-yl)boric acid, (1-acetylpyrrolidin-2-yl)boric acid, (CH2)4CH(NH2)CO2H, (CH2)3CH(NH2)CO2H, (CH2)2CH(NH2)CO2H, -(CH2)d-R80, -C(O)(CH2)d-R80, or amino acid radical; R80 is carboxylate, C6-10 aryl, 3-6-merous heterocyclyl, amino acid; d represents an integer within 0 to 12 inclusively; and R82, R83, R85 and R86 are hydrogen, substituted or unsubstituted alkyl, ether, ester, CH2CH2OCH2CH3, CH2CH(OCH3)2, -(CH2)d-R80, or (CH2)dR87; wherein R87 represents phosphonate or phosphorinate. What is also presented is a complex containing the above compound and a radionuclide. |
|
Ca-ix specific radiopharmaceutical agents for treating and imaging malignant tumours Invention refers to compounds of formula I , II or IV , wherein the radical values W, V, Ra, Rb, X, L, Rt, A are presented in the patent claim. |
|
Technetium- and rhenium-bis(heteroaryl) complexes and methods for using them for psma inhibition Invention refers to new radiopharmaceutical compounds of structural formula |
|
Method of producing binuclear 3,4,5-triaryl-1,2-diphosphacyclopentadienide manganese complexes Invention relates to a method of producing binuclear 3,4,5-triaryl-1,2-diphosphacyclopentadienide manganese complexes of general formula where Ar=C6H5, para-F-C6H4, para-Cl-C6H4. The method involves reacting a dimer of manganese tetracarbonyl bromide [MnBr(CO)4]2 with 1-trimethylstannyl-3,4,5-triaryl-1,2-diphosphacyclopenta-2,4-diene in molar ratio of 1:2 in pure tetrahydrofuran for 30 minutes at room temperature. |
|
Compositions containing certain metallocenes and use thereof Invention relates to a refractory composition for making casting moulds. The composition contains (a) at least 85 pts.wt refractory material, (b) 0.5-10 pts.wt binder and (c) manganese cyclopentadienyl tricarbonyl, a derivative thereof, in amount of about 0.0005 pts.wt to about 4 pts.wt, where the parts by weight are given with respect to 100 pts.wt of the refractory composition. Also disclosed are methods of making a casting mould and a method of moulding metal parts. |
|
|
Complex compound of magnetisable metal and salen Invention refers to a complex compound of a magnetisable metal and salen. The complex compound is presented by formula (I) , wherein M represents Fe, Cr, Mn, Co, Ni, Mo, Ru, Rh, Pd, W, Re, Os, Ir or Pt, and a-f and Y represents hydrogen, or -NHR3-, -NHCOR3 respectively provided a-f and Y are not hydrogen simultaneously, wherein -R3 represents a pharmaceutical molecule with R3 provides the transport of a charge equivalent to max. 0.5 electron (e); or by formula (II) , wherein M represents Fe, Y, a, c, d, f, g, i, j, 1 represent hydrogen respectively; b and k represent -NH2, h and e represent -NHR3, wherein -R3 represents taxol (paclitaxel), or M represents Fe, Y, a, c, d, f, g, i, j, 1 represent hydrogen respectively; b, e, h and k represent -NHR3-, wherein -R3 represent gemfibrozil. There are also presented a local anaesthetic, an antineoplastic agent, a complex metal molecule, an intermediate compound, methods for preparing the magnetic substance, methods for preparing the magnetisable compound. The present invention enables preparing the therapeutic agent using the magnetic properties of the complex of metal and salen for the purpose of magnetising the specific therapeutic agent by chemical binding of the therapeutic agent to the complex of metal and salen so that to deliver the therapeutic agent to an affected area. |
|
Invention refers to photosensitisers, namely to a conjugate of RGD-containing peptide or RGD-peptidomimetic and a photosensitiser selected from tetraarylporphyrin of formula: |
|
Method of producing bis-semiquinolates of cobalt (ii), manganese (ii) and nickel (ii) Invention relates to a method of producing bis(3,6-di(tert-butyl)benzosemiquinolates-1,2) of cobalt (II) or manganese (II) or nickel (II), of general formula: M(SQ)2 , where: SQ is 3,6-di(tert-butyl)benzoquinolate-1,2, and M = Mn(II) or Co(II) or Ni(II). The method is characterised by that a disubstituted salt of an alkali metal salt and 3,6-di(tert-butyl) pyrocatechol-1,2 is obtained, followed by reaction thereof with 3,6-di(tert-butyl)benzoquinoline-1,2. The formed 3,6-di(tert-butyl)benzosemiquinolate-1,2 of the alkali metal reacts with a Co(II) or Mn(II) or Ni(II) halide in an inert atmosphere in tetrahydrofuran. |
|
In the compound of formula I, M denotes identical or different metal atoms selected from a group comprising: Pd, Fe, Mn, Co, Ni, Cu, Zn or Mo, R1 and R2 independently denote hydrogen, amino, hydroxyl, carboxy, cyano, C1-12alkyl, C2-12alkenyl, C2-12alkynyl, C1-12alkoxy, C1-12alkylamino, C1-12alkoxycarbonyl, C1-12alkylamido,arylamido. Alkyl groups in the said substitutes may in turn be substituted with one or more of the following groups: hydroxyl, oxo, carboxy, amino or amido, R3-R10 independently denote hydrogen, or NHR3R4 and NHR5R6, taken together, and(or) NHR7R8 and NHR9R10, taken together, denote a ligand (or ligands) containing one or more donor aliphatic or aromatic nitrogen atoms and which occupy the cis-position near metal (M) atoms. The invention also discloses a pharmaceutical composition, use of the compound to prepare a medicinal drug and a therapeutic treatment method. |
|
Invention relates to a radiopharmaceutical agent for diagnosing or treating (therapy) skeletal bone injury, containing a complex of zoledronic acid with 99mtechnetium or 188rhenium isotopes, zoledronic acid, tin halide or possibly an antioxidant - ascorbic or gentisic acid. The invention also relates to a method of preparing said radiopharmaceutical agent, involving mixing a lyophilisate, obtained by mixing a zoledronic acid solution and a solution of tin dichloride in hydrochloric acid in an inert gas atmosphere and adding a metal hydroxide, with a salt of a metal from the group of isotopes and a radionuclide solution. |
|
Method involves reacting triethanol ammonium salts of o-cresoxyacetic and p-chloro-o-cresoxyacetic acid with the corresponding metal salt in alcohol or aqueous medium preferably at room temperature for 1-48 hours. The three-component complexes are extracted through solvent distillation with subsequent washing of the formed powder with ether and drying in a vacuum. The said complexes can be used as a base for making medicinal drugs. |
|
Method of producing manganese alcoholates Invention relates to method of producing manganese (II) alcoholates which can be used in different syntheses, in purification of complex multicomponent mixtures from alcohols, in analytical control and in scientific research. The method involves direct reaction of metal with alcohol in a vertical bead mill. The liquid phase used is the corresponding alcohol taken in mass ratio to glass beads of 1:1.5. Manganese is taken in amount of 5.81-43.3 % of the mass of the liquid phase. The process is initiated at room temperature and is carried out while controlling by taking samples and determination of content of manganese (II) compounds until all the loaded metal is virtually exhausted, after which stirring in the glass bead is stopped. The suspension of the reaction mixture is separated from the glass beads and taken for filtering. The alcoholate residue is washed with a liquid phase solvent and taken for purification by recrystallisation, and the filtrate and washing liquid phase with traces of dissolved alcoholate are returned for a repeated process. As a rule, the alcohol used is C1-C5-alcohol with normal and isomeric structure, cyclohexanol, ethyl cellosolve and ethylene glycol. |
|
Stereo-selective synthesis of amino acids for production of tumor image New pure syn-aminoacids of formulas I and II have ability of specific binding in biological system and may be used to produce image of tumor. II and I. In formulae I and II Y and Z are independently selected from group made of CH2 and (CR4R5)n, n=1, 2; R1-R3 are independently selected from group made of H and alkyl C1-C4; R4, R5 = H and R7 = 18F. Invention is related to method of synthesis of syn-aminoacids with formula II, which includes stages of ketone transformation into trans-spirit of formula I and transformation of produced trans-spirit into syn-aminoacid of formula II, and also to pharmaceutical composition for production of tumor image and method for production of tumor image. |
|
Manganese (ii) fumarate synthesis method Method of synthesis of manganese (II) fumarate through direct reaction of metal with acid is presented. The process is carried out in a vertical type bead mill with mass ratio of beads to the reaction mixture equal to 1:1, and the liquid phase is a solution of fumaric acid in an organic solvent with content of acid of 0.70-1.80 mol/kg. Manganese is taken in stoichiometric amount with acid or in deficiency of up to 5%. The process is started by loading the liquid phase solvent and acid and preparation of the acid solution in a bead mill, after which metal is loaded and the process is carried out at temperature ranging from 25 to 35°C while preventing spontaneous increase of temperature through forced cooling and controlling through sample taking and determination of manganese salt in the samples and residual amount of acid until attaining values close to calculated values during quantitative conversion of the reagent in deficiency. After that stirring and cooling are stopped. The suspension of the reaction mixture is separated from the glass beads, cooled to temperature between 5.2 and 6.2°C and filtered. The filtering residue is washed with the liquid phase solvent, cooled to approximately the same temperature, and taken for purification by recrystallisation. The filtrate and the washing solvent are returned to the repeated process. |
|
|
Method of producing manganese (ii) fumarate from manganese metal and manganese (iii) oxide Invention relates to an improved method of producing manganese (II) fumarate from manganese metal and its oxide (III) through direct reaction of the metal and its oxide Mn2O3 with an acid in the presence of a liquid phase and a stimulating iodine additive in a vertical type bead mill with glass beads as grinding agent. The metal and its oxide are loaded in molar ratio (2±0.1):1 in total amount of 7.87 to 10.93% of the mass of the load. Acid is added with 15 to 25% excess of the calculated value, equal to the number of moles of metal and twice the number of moles of metal oxide in the load. The base of the liquid phase is isoamyl alcohol, in which the iodine stimulating additive is dissolved in amount of 0.02 to 0.05 mol/kg. Glass beads are loaded first, in mass ratio to the reaction mixture of 1.35:1, and then later the liquid phase solvent, acid and stimulating additive, and after brief stirring, metal oxide and metal, stirring all the while. Taking this moment as the beginning of the process, forced cooling is introduced right away. Operating temperature is stabilised in the range 33 to 45°C and in this mode, the process is carried out until virtually quantitative conversion of metal and its oxide to the target salt, after which stirring and forced cooling are stopped. The reaction mixture is separated from the glass beads, cooled to temperature 5 to 6°C and kept at that temperature for 1 to 2 hours. The solid phase of the target salt is filtered off and washed with isoamyl on a filter cooled to approximately the same temperature, after which it is taken for purification by recrystallisation. The filtrate and the cleaning solvent, containing excess acid, the bulk of the stimulating additive and a certain amount of dissolved target salt, are returned for loading in the repeated process. The process is carried out in light temperature conditions. The target substance can be easily separated. |
|
Improved conjugates n4 of chelating agents Invention refers to chelating agents and their technetium complexes to be used as radiopharmaceuticals and characterised by formula I where X is -NR-, -CO2-, -CO-, -NR(C=S)-, -NR(C=O)-, -CONR- or Q; Y represents amino acid, -CH2-, -CH2OCH2-, -OCH2CH2O- or X; Z is an aggregation from peptides, their analogues, substrata, antagonists or enzyme inhibitors, receptor-bonding compounds, oligonucleotides, oligo-DNA- or oligo-RNA-fragments; n is a number 1 to 8; m is a number 0 to 30; R represents H, C1-4alkyl, C2-4alkoxyalkyl, C1-4hydroxyalkyl or C1-4fluoroalkyl; Q represents remains of succinimide , A is a pharmaceutically acceptable anion. |
|
Method for preparation of manganese oxalate (ii) Invention is related to improved method for preparation of manganese oxalate (II) by means of direct interaction of metal with acid in bead mill in presence of liquid phase, in which manganese and oxalic acid are loaded into bead mill in stoichiometric ratio in amount of 0.75-2.4 mole/kg of load at mass ratio of load and glass beads of 1:1.2, liquid phase dissolvent used is water or organic substance, or mixture of organic substances; loading is carried out in the following sequence: liquid phase dissolvent, acid, then metal; process is started at room temperature and is carried out under conditions of forced cooling in the temperature range of 18-39°C with control over procedure by sampling method to practically complete spend of loaded reagents for product making, afterwards mixing and cooling are terminated, suspension of reaction mixture is separated from glass beads and filtered, salt deposit is sent for product cleaning from traces of non-reacted metal, and filtrate is returned into repeated process. |
|
Method of production of the formiate of manganese (ii) The invention is pertaining to production of the manganese salts with the organic acids in particular, to the salt of the divalent manganese and formic acid. The method is exercised by interaction of manganese, its oxides in the state of the highest valence with the formic acid solution in the organic solvent in the presence of iodine as the stimulating additive. The production process is conducted in the bead grinder of the vertical type having the revertive cooler-condenser, the high-speed paddle stirrer and the glass beads of in the capacity of the grinding agent loaded in the mass ratio to the loading of the liquid phase as (1÷2): 1. The liquid phase consists of the formic acid solution in the organic solvent. The concentration of the acid is taken within the range of 3.5÷10.8 mole/kg. In the loaded liquid phase they dissolve the stimulating additive of iodine in the amount of 0.025-0.100 mole/kg of the liquid phase. The ratio of the masses of the liquid phase and the total of the metallic manganese and the manganese oxide are as(4.9÷11):1. The molar ratio of the metal and the oxide in the loading is as (1.8÷2.,2):1. The metal and the oxide are loaded the last. It is preferable in the capacity of the dissolvent to use the butyl alcohol, ethyl acetate, ethylene glycol, 1.4-dioxane, dimethyl formamide. The production process is started and conducted at the indoor temperature up to practically complete(consumption of the whole loaded manganese oxide. Then the stirring is stopped, the suspension of the salt is separated from the beads and the nonreacted manganese and after that conduct filtration. The filtrate and the nonreacted manganese are returned into the repeated production process, and the filtered out settling of the manganese salt is exposed to purification by recrystallization. The technical result of the invention is - simplification of the method at usage of accessible reactants. |
|
Nucleophilic fluorination in solid phase Invention relates to an improved solid-phase method for synthesis of radioisotope indicators, in particular, for synthesis of compounds labeled with 18F that can be used as radioactive indicators for positron- emission tomography (PET). In particular, invention relates to a method for synthesis of indicator labeled with 18F that involves treatment of a precursor fixed on resin if the formula (I): SOLID CARRIER-LINKER-X-INDICATOR wherein X means a group promoting to nucleophilic substitution by a definite center of a fixed INDICATOR with 18F- ion for preparing a labeled indicator of the formula (II): 18F-INDICATOR; to compound of the formula (Ib): |
|
Method of production of the bromine derivatives of the fullerene c60 The invention is pertaining to the method of production of the bromine derivatives of fullerene С60. The process consists in the interaction of the bromoform and the tetra bromomethane with fullerene С60 at presence of the rhodium-containing catalyst - Wilkinson's complex [RhCl(PPh3)3] at the temperature of 100°С within 10-20 hours, at the molar ratio of [Rh]:[C60]:[CHBr3 or CBr4]= 1:100:100-500. The technical result of the invention is the increased output of the product, the reduced amount of the wastes, the insignificant consumption of the catalyst. |
|
Method for preparing manganese (ii) acetate Invention relates to technology for synthesis of acetic acid inorganic salts. Method involves interaction of metallic manganese or its dioxide with acetic acid in the presence of oxidizing agent. Process is carried out in beaded mill of vertical type fitted with reflux cooling-condenser, high-speed blade mixer and glass beads as grinding agent loaded in the mass ratio to liquid phase = 1.5:1. Liquid phase represents glacial acid solution in ethylcellosolve, ethylene glycol, 1,4-dioxane, isoamyl alcohol and n-butyl alcohol as a solvent. The concentration of acid in liquid phase is 3.4-4 mole/kg. Then method involves loading iodine in the amount 0.025-0.070 mole/kg of liquid phase, metallic manganese and manganese dioxide in the mole ratio = 2:1 and taken in the amount 11.8% of liquid phase mass. The process starts at room temperature and carries out under self-heating condition to 30-38°C to practically complete consumption of manganese dioxide. Prepared salt suspension is separated from beads and unreacted manganese and filtered off. Filtrate is recovered to the repeated process and prepared precipitate is purified by recrystallization. Invention provides simplifying method using available raw and in low waste of the process. |
|
|
Manganese (iii) acetylacetonate preparation method Invention relates to preparation of manganese (III) acetylacetonate, which can be used as catalyst as well as vinyl monomer polymerization initiator. Method is implemented in aqueous medium with ammonium acetylacetonate freshly prepared by mixing acetylacetone with aqueous ammonia solution. Hydrogen peroxide is used as oxidant and sodium bicarbonate is additionally introduced into reaction mixture. Following consecutive operations are carried out: reaction of manganese (II) chloride tetrahydraye with sodium bicarbonate; separating thus formed manganese (II) bicarbonate in the form of paste; adding ammonia acetylacetonate and then hydrogen peroxide aqueous solution to the paste; and recovering manganese (III) acetylacetonate with yield 95%. |
|
|
Invention relates to agents for regulation (maintaining or suppression) of physical working ability and/or adaptation to different variants represented by solvated complex compounds of the general formula (I): Katm+[L1 qEL2]Ann- x p.Solv (I) wherein L1 means aminothiols of the formula: R1NHCH(R2)(CH2)1-2SR3 wherein R1 means hydrogen atom (H), (C1-C20)-alkyl or RCO; R means (C1-C19)-alkyl; R2 means H or carboxyl; R3 means H, (C1-C20)-alkyl, (C2-C20)-alkenyl or benzyl; q = 1, 2 or 3; L2 means halogen atom, water and/or organic ligand. For example, bis-(N-acetyl-L-cysteinato)aquozinc (II) diheptahydrate suppresses physical working ability and in the dose 50 mg/kg increases reviving time of mice by 6 times and cats - by 2.8fold under conditions of acute hypoxia with hypercapnia, and increases reviving time of mice by 4 times under conditions of acute hypobaric hypoxia. Under the same conditions the known antihypoxic agents amtizol, acizol or mexidol are inactive or less active significantly by their activity. Bis-(N-acetyl-L-cysteinato)-ferrous (II) pentahydrate is more active as compared with the known antihypoxic agents and protects experimental animals in 4 variants of hypoxia. Bis-(N-acetyl-L-cysteinato)zinc (II) sulfate octahydrate is similar to enumerated compounds by its antihypoxic activity. |
Another patent 2551071.