[2,4-dioxo-1,3 - bis (5-methyl-3-tyuhexjl) -6-methyl-1,2,3, 4 - tetrahydropyrimidin-s,s] cis-dichloroplatinum showing immunotropic activity
(57) Abstract:Usage: in medicine as a means of manifesting immunotropic activity. The inventive product -[2,4-dioxo - 1,3-bis(5-methyl-3-tyuhexjl)-6-methyl -1,,2,3,4-Tetra hydropyridine - S,S]CIS - dichloroplatinum. Yield 35 g (90% ). Reagent 1: an aqueous solution of K2PtCl4Reagent 2: 1,3-bis(isopotential)-6-methyluracil in acetone. table 1. The invention relates to organic chemistry, specifically to a new chemical compound - complex PtCl2with 1,3-bis(isopotential)-6-methyluracil formula
showing immunotropic activity.This complex synthesis method and its properties are not described in literature.Similar in structure and purpose is a 4-cisplatin.It is known that 4-cisplatin (1)
exhibits antitumor activity, inhibits DNA synthesis, used in breast cancer, prostate cancer, ovarian cancer. However, immunotropic activity not described (GST and AOK).It is also known that the platinum-containing coordination compounds lot - so Dyachenko S. A. with co (2) received complex compounds of Pt (II) and Pd (II) with 5-aminouracil and its methyl producing CLASS="ptx2">Known (3) CIS-Pt(NH3)2(I-MeY)2and (NH3)2Pt(I-MeY)2Pt(en)NO35H2O
(4), but their immunotropic activity has not been studied.Of these complexes could be taken as a structural analogue, for example, coordination compounds (NH3)2Pt(I-MeY)2but it immunotropic activity has not been studied, no LD50. Therefore was taken as the equivalent of hydrocortisone, immunotropic properties of which are studied.The aim of the invention is the expansion of means of influence on a living organism characterized by pronounced immunotropic activity.This goal is achieved by a new compound - complex PtCl2with 1,3-bis(isopotential)-6-methyluracil. How to obtain it is through the interaction of K2PtCl4in odnourovnevoi environment with 1,3-bis(isopotential)-6-methyluracil at room temperature for 3 hoursP R I m e R 1. In a flat-bottomed flask with a capacity of 50 ml asleep 1 g K2PtCl4, dissolved in 10 ml of water and the resulting solution was added dropwise with stirring on a magnetic stirrer 0,86 g (0,0024 mole) of 1,3-bis(isopotential)-6-methyluracil in 10 ml of acetone. When intense shutovskoy funnel, washed with water from salts, pererastayut in chloroform and obtain 1.35 g (90%) of the chloride complex of platinum with 1,3-bis(isopotential)-6-methyluracil soluble in chloroform and acetone.Found,%: C 32,90; H 4,81; Cl To 12.44; S 10,32; Pt 31,43; N 4,35.C17H30N2O2S2PtCl2.Calculated, % : C 32,69; H 4,84; N 4,48; Cl 11,35; S 10,27; Pt 31,24; O 5,12.IR spectrum (cm-1): 320, 330 (YPtCl); 305 (YPtS).In the work Dyachenko et al. (2) the obtained complex compounds of Pt (II) and Pd (II) with 5-aminouracil and its methyl derivatives with monodentate coordination of the ligands only through the nitrogen atom ekzoticheskoy amino group.The structure of the proven IR spectra.(3) the obtained complex compounds connected through the N3-platinum pyrimidine-2,4-dioxy and the second ligand through ekzoticeski oxygen atom.(4) a series of dual complexes (X2)PtL2M(Y2)ZnH2O; L = (-MeUC5H5P2O2or-Met, C6H7N2O2) link Pt N3position and the second metal through the O4- position. X2and Y2= (NH3)2, Ethylenediamine, EN: 2,21-beparis (NH3)2Pt(I-MeU)Pd(en)(NO3)6H2O by X-ray analysis.In this case, the complex is formed by communication with gray.The structure of the target product 2,4-dioxo-1,3-bis(5-methyl-3-tyuhexjl)-6-methyl-1,2,3,4 - tetrahydropyrimidin-S, S-CIS-dichloroplatinum proven IR and PMRN spectra.In the IR spectrum of compound has absorption bands in the region 318, 332 cm-1related to the stretching vibrations due PtCl2and clearly indicating the formation of coordination compounds of the type CIS-PtCl2L (9). Absorption bands in the region 307 cm-1refer to the stretching vibrations of communication PtS. The absorption band of stretching vibrations of (N-1)N is absent. Absorption bands in the region 1660, 1720 cm-1characteristic ring of uracil (C=ON - C = 0).That the complexation is carried out by forming a coordination Pt-S spectrum shows AMRN complex, which in comparison with the spectrum of the ligand greatest additional chemical shift, there are signals of protons of methylene groups at the sulfur atom in the weak field 0.7-0.8 M. D.It is established that CIS-PtCl2(1,3-CH2CH2SCH2CH(CH3)2< / BR>
FIELD: pharmaceutical engineering; medical engineering.
SUBSTANCE: method involves carrying out nuclear magnetic resonance tomography of human or animal blood circulation system containing chelating ion complexes of bivalent and valence three paramagnetic metals of (I)X-L-Y formula, where X is the polyamide carbonyl ligand residue and Y is the gallic acid derivative, .
EFFECT: high accuracy of diagnosis.
FIELD: pharmaceutics, veterinary science.
SUBSTANCE: the present innovation deals with preventing and treating hypomicroelementosis in different farm and domestic animals, furred animals, and, also, for enhancing the growth in animals, and treating a number of specific diseases and, also, for maintaining microelemental composition of feedstuffs. The suggested preparation includes chelated complex of iron, manganese, zinc, copper, cobalt, selenium and iodine with organic ligand of complexone type and water. According to the innovation as a chelation ligand it contains trisodium salt of methionine succinic (α-amino-γ-methylthiobutyric-N-succinic) acid at a certain ratio of components. The innovation provides to obtain preparation in soluble form being capable to be well digested by the animal.
EFFECT: higher efficiency.
FIELD: agriculture, animal husbandry, fur farming.
SUBSTANCE: invention relates to preparations used in prophylaxis and treatment of domestic and agricultural animals and for maintaining trace elements composition of fodders. The preparation allows balancing the nutrition diet for animals with the optimal ratio of trace elements providing prophylaxis of many diseases. Proposed preparation comprising complex of iron, manganese, copper, cobalt, selenium and zinc with ethylenediamine-N,N1-disuccinic acid disodium or dipotassium salt and water comprises additionally iodine in the following ratio of components: ethylenediamine-N,N1-disuccinic acid disodium or dipotassium salt, 15-25; iron (III), 1.5-5.5; manganese (II), 0.25-3.0; copper (II), 0.12-0.55; cobalt (II), from above 0.05 to 0.3; zinc (II), 0.05-1.5; selenium (IV), from above 0.03 to 0.06; iodine (I), 0.01-0.08; water, the balance.
EFFECT: improved and valuable properties of preparation.
1 cl, 4 tbl
FIELD: veterinary medicine.
SUBSTANCE: composition comprises in % by mass: 2Na- or 2K-salt of ethylene diamine-N,N1-disuccinic acid 15.0-35.0; Na- or K-salt of amino acid 2.0-10.0; salts of iron (III) 0.6-3.0; manganese (II) 0.5-2.5; copper (II) 0.05-0.25; zinc (II) 0.3-2.5; cobalt (II) 0.005-0.05; selenium (IV) 0.01-0.03; iodine (I) 0.03-0.08; water takes the rest. Amino acid is selected from group containing glycine, alanine, valine, aspartic acid, glutamic acid, lysine, methionine, cystine, threonine and tryptophan.
EFFECT: eliminated microelement deficiency; stimulated erythropoiesis and nonspecific organism resistance.
2 cl, 10 tbl
FIELD: veterinary science.
SUBSTANCE: invention relates to a composition used in prophylaxis and treatment of anemia in agricultural animals and poultry that comprises a mixture of chelates of iron, copper, zinc, cobalt, sodium, calcium with ethylenediamine-N,N'-disuccinic acid in the following ratio of components, wt.-%: copper chelates with ethylenediamine-N,N'-disuccinic acid, 0.45-0.60; zinc chelates with ethylenediamine-N,N'-disuccinic acid, 1.40-1.45; cobalt chelates with ethylenediamine-N,N'-disuccinic acid, 0.075-0.08; sodium chelates with ethylenediamine-N,N'-disuccinic acid 42.0-44.0; calcium chelates with ethylenediamine-N,N'-disuccinic acid, 12.0-13.0, and iron chelates with ethylenediamine-N,N'-disuccinic acid, the balance. Agent provides enhancing the blood hemoglobin content in animals by 28% as compared with animals receiving neither anti-anemic agents and by 12% as compared with animals receiving the preparation-analog.
EFFECT: enhanced effectiveness of composition.
4 tbl, 4 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention describes water-soluble iron-carbohydrate complexes containing 10-40 wt.-% of iron. Complexes can be prepared from ferric (III) salt aqueous solution and oxidation product aqueous solution of one or more maltodextrins with hypochlorite aqueous solution at alkaline pH value. In using one maltodextrin its dextrose equivalent is from 5 to 20, and in using mixture of maltodextrins the dextrose equivalent is from 5 to 20 and dextrose equivalent of each maltodextrin as component of mixture is from 2 to 40. Also, invention describes a method for preparing this complex and medicinal agents used in treatment and prophylaxis of states associated with iron deficiency.
EFFECT: improved preparing method, valuable medicinal properties of complexes.
15 cl, 1 tbl, 8 ex
FIELD: animal science.
SUBSTANCE: the suggested preparation contains disodium or dipotassium salt of ethylenediamine-N,N1succinic acid, iron (III), manganese (II), zinc (II), copper (II), cobalt (II), iodine (I), selenium (IV) and water at the following ratio of components, weight%: disodium or dipotassium salt of ethylenediamine-N,N1disuccinic acid 25.1-57.5; iron (III) 0.5-5.5; manganese (II) 0.25-4.9; zinc (II) 0.05-2.0; copper (II) 0.10-0.55, cobalt (II) 0.05-0.3, iodine (I) 0.01-0.08, selenium (IV) 0.01-0.06, water - the rest. The preparation suggested enables to increase vitamin full value of feedstuffs.
EFFECT: higher efficiency.
4 ex, 4 tbl
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to compound of the formula (I) possessing inhibitory effect on production of interleukin-12 (IL-12) wherein R1 represents group of the formula , aryl or heteroaryl; each among R2 and R4 represents independently hydrogen atom, (C1-C6)-alkyl or (C1-C6)-alkoxy group; R3 represents Rc, alkenyl, -ORc, -OC(O)Rc, -SRc, -NRcCORd, -NRcC(O)ORd, -NRcC(O)NRcRd, -NRcSO2Rd, -CORc, -C(O)ORc or -C(O)NRcRd; R5 represents hydrogen atom (H); n = 0, 1, 2, 3, 4, 5 or 6; X represents oxygen atom (O) or -NRc; Y represents a covalent bond. -CH2, O or -NRc; Z represents nitrogen atom (N); one of values U and V represents N and another represents -CRc; W represents O, sulfur atom (S) or -S(O)2 wherein each radical among Ra and Rb represents independently H, (C1-C6)-alkyl, aryl or heteroaryl; each radical among Rc and Rd represents independently H, (C1-C6)-alkyl, phenyl, heteroaryl, cyclyl, heterocyclyl or (C1-C6)-alkylcarbonyl wherein term "aryl" relates to hydrocarbon cyclic system (monocyclic or bicyclic) comprising at least one aromatic ring; term "heteroaryl" relates to hydrocarbon cyclic system (monocyclic or bicyclic) comprising at least one aromatic ring that comprises at least one heteroatom, such as O, N or S as a part of cyclic system and wherein other atoms mean carbon; term "cyclyl" and "heterocyclyl" relate to partially or completely saturated monocyclic or bicyclic system comprising from 4 to 14 carbons in rings wherein heterocyclic ring comprises one or some heteroatoms (for example, O, N or S) as part of cyclic system and wherein other atoms mean carbon, and under condition that when X represents -NH, Y represents a covalent bond, n = 0, and R3 represents H or CH3 then R1 doesn't mean thiazolyl or pyrimidinyl. Also, invention relates to a pharmaceutical composition and a method for treatment of disorder associated with hyperproduction of interleukin-12.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.
49 cl, 43 ex
FIELD: medicine, veterinary science.
SUBSTANCE: method involves prescription of intramuscular injection of ferroglucinum by 150 mg (2 ml) twice over 10 day interval, intramuscular injection of phosprenyl thrice by different syringes into different points, by 0.08 ml/kg for the first time together with iron agent, by 0.07 ml/kg over five days after the first injection, by 0.05 ml/kg for the third time together with the second injection. Additionally, 0.016 ml/kg of gamavit is injected intramuscularly once per day for six days beginning from the first ferroglucinum injection.
EFFECT: possible thrombin time stabilisation for newborn piglets with anaemia.
FIELD: medicine, veterinary science.
SUBSTANCE: method involves prescription of intramuscular injection of ferroglucinum by 150 mg (2 ml) twice over 10 day interval, intramuscular injection of phosprenyl thrice by different syringes into different points, by 0.08 ml/kg for the first time together with iron agent, by 0.06 ml/kg over five days after the first injection, by 0.04 ml/kg for the third time together with the second injection. Additionally, 0.012 ml/kg of gamavit is injected intramuscularly once per day for ten days beginning from the first ferroglucinum injection.
EFFECT: possible fibrinogen level stabilisation for newborn piglets with anaemia.
FIELD: chemistry of metalloorganic compounds, medicine, oncology.
SUBSTANCE: invention relates to derivatives of platinum tetrachloride and to a method for their preparing also. Invention proposes compounds of the formula PtCl4 x 2 Li wherein Li represents N-(2-nitroxyethyl)nicotinamide or N-(2-nitroxyethyl)isonicotinamide, or nicotine hydroxamic acid, or isonicotine hydroxamic acid. Also, invention proposes a method for preparing these compounds that involves interaction of pyridine carboxylic acid nitroxyethylamides or hydroxamic acids, or their hydrochlorides with potassium hexachloroplatinate followed by isolation of the end product. Invention provides synthesis of the unknown early chelate platinum compounds that are physiologically active substances and can be used in medicinal practice instead cisplatin as effective anti-metastatic medicinal agents with low toxicity.
EFFECT: improved preparing method, enhanced and valuable medicinal properties of compounds.
2 cl, 3 ex
FIELD: metalloorganic chemistry, chemical technology.
SUBSTANCE: invention relates to the improved method for preparing platinum complexes having the formula (Ia) or (Ib) given in the description. Method involves: 1a) the first stage wherein [PtA4]2- interacts with L under corresponding conditions in the first solvent to yield [PtA3(L)]-; 1b) the second stage wherein [PtA3(L)]- interacts with L' under corresponding conditions in the second solvent to yield cis-[PtA2(L')(L)]; 1c) in the case when Y represents halogen atom or hydroxy-group the third stage wherein cis-[PtA2(L')(L)] interacts with H2O2, Y2 or halogen containing oxidant to yield c,t,c-[PtA2Y2(L')(L)]; in the case when Y represents ester of carboxylate, carbamate or carbonate the forth stage wherein intermediate compound and wherein Y represents hydroxy-group obtained at the stage 1c) is functionalized with corresponding acylating agent; and 1d) in the case when A doesn't represent halide or differs from the parent halide the additional stage (stages) wherein at the first stage halide A of intermediate compound obtained at stage 1a), 1b), 1c) or 1d) is converted to another halide and new removing group (groups) A, such as monodentate hydroxy-, alkoxy-, carboxylate or bidentate carboxylate, phosphonocarboxylate, diphosphonate or sulfate wherein L, L' and Y have values in the description.
EFFECT: improved preparing method, expanded assortment of platinum-containing medicinal agents.
33 cl, 3 tbl, 9 dwg, 23 ex
FIELD: organic chemistry.
SUBSTANCE: invention relates to new derivatives of metalloporphyrazine of the general formula (I): wherein M means Cu, Co. These compounds can be used as dyes, catalysts in different processes and materials of sensitive members of gas sensor.
EFFECT: valuable properties of compounds.
2 cl, 6 sch, 1 dwg, 5 ex
FIELD: chemical industry, in particular two-component heterogeneous immobilized catalyst for ethylene polymerization.
SUBSTANCE: claimed catalyst includes alumina, mixture of transition metal complexes with nitrogen skeleton ligands (e.g., iron chloride bis-(imino)pyridil complex and nickel bromide bis-(imino)acetonaphthyl complex). According the first embodiment catalyst is prepared by application of homogeneous mixture of transition metal complexes onto substrate. iron chloride bis-(imino)pyridil complex and nickel bromide bis-(imino)acetonaphthyl complex (or vise versa) are alternately applied onto substrate. According the third embodiment catalyst is obtained by mixing of complexes individually applied onto substrate. Method for polyethylene producing by using catalyst of present invention also is disclosed.
EFFECT: catalyst for producing polyethylene with various molecular weights, including short chain branches, from single ethylene as starting material.
7 cl, 5 tbl, 27 ex