- Fe(III) Complex Compounds For The Treatment And Prophylaxis Of Iron Deficiency Symptoms And Iron Deficiency Anemias
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The invention relates to iron(III) complex compounds and pharmaceutical compositions comprising them for the use as medicaments, in particular for the treatment and/or prophylaxis of iron deficiency symptoms and iron deficiency anemias.
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Paragraph 0568; 0569; 0570; 0571; 0572
(2013/05/09)
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- Hydrolysis of organophosphate esters: Phosphotriesterase activity of metallo-ss-lactamase and its functional mimics
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The phosphotriesterase (PTE) activity of a series of binuclear and mononuclear zinc(II) complexes and metallo-β-lactamase (mβl) from Bacillus cereus was studied. The binuclear complex 1, which exhibits good mβl activity, shows poor PTE activity. In contrast, complex 2, a poor mimic of mβl, exhibits much higher activity than 1. The replacement of Cl - ligands by OH- is important for the high PTE activity of complex 2 because this complex does not show any catalytic activi-ty in methanol. The natural enzyme mssl from B. cereus is also found to be an inefficient catalyst in the hydrolysis of phosphotriesters. These observations indicate that the binding of -lactam substrates at the binuclear zinc(II) center is different from that of phosphotriesters. Furthermore, phospho diesters, the products from the hydrolysis of triesters, significantly inhibit the PTE activity of mβl and its functional mimics. Although the mononuclear complexes 3 and 4 exhibited significant mβl activity, these complexes are found to be almost inactive in the hydrolysis of phosphotriesters. These observations indicate that the elimination of phosphodiesters from the reaction site is important for the PTE activity of zinc(II) complexes.
- Tamilselvi,Mugesh, Govindasamy
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experimental part
p. 8878 - 8886
(2010/11/02)
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- The thermodynamics of phosphate versus phosphorothioate ester hydrolysis
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Phosphorothioate esters are phosphate esters in which one of the nonbridging oxygen atoms has been replaced by sulfur. In the comparative hydrolysis reactions of phosphorothioate and phosphate esters, the sulfur substitution accelerates the rates of the monoesters while slowing the rates of diesters and of triesters. Previously measured enthalpies and entropies of activation for the hydrolysis reactions of the monoesters, p-nitrophenyl phosphate and p-nitrophenyl phosphorothioate, were compared to the activation parameters measured herein for the diesters, ethyl p-nitrophenyl phosphate and ethyl p-nitrophenyl phosphorothioate, and the triesters, diethyl p-nitrophenyl phosphate and diethyl p-nitrophenyl phosphorothioate. A consistent trend of a greater ΔH? for the phosphorothioate analogue was found in all three classes of ester. In the monoester case, a more positive ΔS? arising from a mechanistic difference (DN + AN for the phosphorothioate versus ANDN for the phosphate) compensates, resulting in a lower ΔG? for the phosphorothioate monoester. Spectroscopic investigations indicate there is no significant difference in bond order to the leaving group in phosphates, as compared to their phosphorothioate analogues, ruling this out as a contribution to the consistently higher enthalpies of activation.
- Purcell, Jamie,Hengge, Alvan C.
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p. 8437 - 8442
(2007/10/03)
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- Process for obtaining acyloins, pyruvate decarboxylases suitable therefor and their production and DNA sequence of the PDC gene coding them
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A process for obtaining a pyruvate decarboxylase by isolation from a producer organism. The pyruvate decarboxylase is capable of forming (R)-(-)-phenylacetylcarbinole (I) in ≥95% enantiomer unit with a product ratio of (I) to 2-hydoxypropiophenone of ≥95%. In addition, the pyruvate decarboxylase has a specific activity with regard to phenylacetylcarbinole formation of >1U/mg. It is the aim of the invention to obtain a pyruvate decarboxylase with improved synthesis capacity concerning the formation of (R)-(-)-phenylacetylcarbinole. The process of the invention developed for this purpose is characterized in that use is made of a producing organism with a gene coding for pyruvate decarboxylase from Zymomonas mobilis, in the DNA sequence of which the tryptophane radical coding codon TGG is replaced at position 1174-1176 by a codon which codes for an amino acid radical with a reduced volume ratio.
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- Selected O-quinonediazide sulfonic acid esters of phenolic compounds and their use in radiation-sensitive compositions
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A photosensitive compound comprising at least one o-quinonediazide sulfonic acid ester of a phenolic compound, said esters selected from the group consisting of formulae (IB) and (IIB): STR1 wherein the variables are as defined in the description.
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- Selective Sulfur Oxygenation in Phosphoroamidate, Thionophosphate, and Thiophosphate Agrochemicals by Perfluoro-cis-2,3-dialkyloxaziridine
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Several organophsophorus agrochemicals 2a-g with thioether, phosphoramidic, phosphorothioic, and phosphorothionic functions were reacted with perfluoro-cis-2-n-butyl-3-n-propyloxaziridine 1.The selective oxygenation of sulfide function to give sulfoxide derivatives 3a-g occured in high yields without overoxidation to sulfone products.Sulfoxides 3a-e were further oxidized under mild conditions to the corresponding sulfones 4a-e.All the products are themselves of interest as analytical environmental standards and their preparation is described in detail.
- Terreni, Marco,Pregnolato, Massimo,Resnati, Giuseppe,Benfenati, Emilio
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p. 7981 - 7992
(2007/10/02)
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- Oil-in-water emulsions and a process for their preparation and their use
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Oil-in-water emulsions (microemulsions) containing 0.01-80% by weight of at least one agrochemical active substance of low water-solubility, one active substance for combating pests in the domestic and hygiene sector and/or one pharmacologically active substance, 1% to 30% by weight of an emulsifier mixture of non, ionic and anionic compounds and at least one alkylarylsulfonic acid salt, as defined in the description, as well as water and, if appropriate, 1% to 30% by weight of at least one solvent of low water-miscibility and/or one solubilizer, and if appropriate 0.05% to 15% by weight of additives, the sum of the components in each case being 100% by weight, a process for the preparation of these aqueous microemulsions and their use.
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- Biocidal macroemulsions containing polyvinyl alcohol
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The present invention relates to new macroemulsions which contain 0.001 to 60 percent by weight of at least one active compound from the class comprising the phosphates and/or carbamates, 0 to 50 percent by weight of aromatic diluents, 0.001 to 20 percent by weight of polyvinyl alcohol having a mean molecular weight of between 5,000 and 150,000 and a content of acetate groups of between 2 and 30 mol %, and/or 0.001 to 20 percent by weight of a nonlphenol/propylene oxide/ethylene oxide adduct of the formula STR1 in which X represents integers from 10 to 50 and Y represents integers from 15 to 65, and/or 0.001 to 20 percent by weight of ethylene oxide/propylene oxide/ethylene oxide block copolymers having a mean molecular weight of between 2,000 and 8,000 and HLB values of between 8 and 30, and water and, if appropriate, additives, and in which the oil phase is dispersed in the aqueous phase in the form of droplets having a mean particle diameter of 0.1 to 3.0 μm.
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- Oil-in-water emulsions, and their use
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Novel oil-in-water emulsions, which contain (a) 0.1 to 80% by weight of at least one sparingly water-soluble active compound (as herein defined) selected from agrochemical active compounds, active compounds for combating pests in the domestic field and hygiene field and/or pharmacologically active compounds, (b) 1 to 20% by weight of at least one alkylaryl polyglycol ether of the general formula STR1 wherein R1 represents a hydrogen atom or an alkyl group having 1 to 16 carbon atoms, R3 represents a hydrogen atom or a methyl group, m is 1, 2 or 3, and n is an integer from 10 to 50, if appropriate in a mixture with an alkylarylsulphonic acid salt of the general formula STR2 wherein R3 represents an alkyl group having 8 to 35 carbon atoms and Me≈ represents an alkali metal cation, an equivalent of an alkaline earth metal cation or a cation of the general formula STR3 wherein R', R", R'" and RIV independently of one another represent a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a hydroxyalkyl group having 1 to 4 carbon atoms, (c) water, (d) if necessary, 1 to 30% by weight of at least one poorly water-miscible organic solvent and/or a solubilizer, and (e) if appropriate 0.05 to 15% by weight of one or more additives, the sum of the components being 100% by weight in each case, a process for the preparation of these emulsions and their use in the field appropriate to the active compound.
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- Bioactant translocation agent
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The present invention relates to novel agents for increasing the basipetal translocation of agricultural chemicals such as plant growth promoters, inhibitors, fungicides, insecticides or herbicides hereinafter referred to as bioactants . The present agent comprises a mixture of N-heterocyclic amide and a haloethyl phosphonic acid in a mole ratio of between about 5:1 and about 1:10, employed in an inert carrier at a concentration between about 25 ppm to about 10,000 ppm which mixture can be applied to a plant prior to, or simultaneously with, the bioactant. The translocating agent may be a mixture of the N-heterocyclic amide, e.g. N-methyl-2-pyrrolidone, and the haloethylphosphonic acid, e.g. 2-chloroethylphosphonic acid, it may comprise a mixture of said components with the complexed compound derived from the addition of said components or it may be the complexed compound per se.
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- Organic complex of platinum, its preparation and its use for treating malignant tumors
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An organic complex of platinum, cis-isocitrato (1,2 diaminocyclohexane) platinum (II) having improved anti-tumor activity and water-solubility. The complex is prepared by reacting cis-dichloro (1,2-diaminocyclohexane) platinum (II) with silver nitrate, removing the silver chloride formed, and reacting the resulting liquid with trisodium isocitrate. The complex is administered in the form of a pharmaceutical composition.
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