Abstract: The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genus Plasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing such compounds and a process for making the compounds. This and other aspects of the invention are realized upon review of the entire specification.

Abstract: It is intended to enable an apparatus for synthesizing urea and a method for revamping the same to place a heavy condenser at a relatively low position and to circumvent problems associated with letting a process fluid flow within a tube in the condenser. The present invention provides an apparatus for synthesizing urea including: a synthesis reactor for reacting NH3 with CO2 to obtain a urea synthesis solution containing urea, unreacted NH3 and CO2, and water; a stripper for stripping the urea synthesis solution with use of at least a part of raw material CO2 to separate a gas containing the unreacted NH3 and CO2; a vertical submerged condenser having a shell and tube structure for condensing the gas in an absorbing medium on the shell side while cooling the gas with a cooling medium passing through the tube side; and recycling means for recycling a liquid obtained from this condenser to the synthesis reactor, wherein this condenser is placed below the synthesis reactor.

Abstract: A cyclic polycarboxylic acid anhydride, a polycarboxylic acid, or a mixture of them is allowed to react with hydroxylamine or a salt thereof in an organic solvent under dewatering conditions to yield a corresponding cyclic N-hydroxyimide compound. The cyclic polycarboxylic acid anhydride can be, for example, succinic anhydride or glutaric anhydride. The polycarboxylic acid can be, for example, succinic acid, glutaric acid, or adipic acid. In this process, the reaction is preferably carried out using an organic solvent capable of undergoing azeotropy with water as all or part of a reaction solvent while removing water from the reaction system by azeotropy with the organic solvent. This process produces a cyclic N-hydroxyimide compound in a good yield from any of a cyclic polycarboxylic acid anhydride and a polycarboxylic acid.

Abstract: It is intended to enable more smooth operation in an apparatus for synthesizing urea by circumventing the downward flow of a urea synthesis solution which is a gas-liquid two-phase flow and stabilizing the flow of the urea synthesis solution still remaining the gas-liquid two-phase flow and to reduce energy loss by giving smaller flow resistance.

Abstract: An article is sulfonated by forming a sulfonating gas composition containing a gaseous sulfur-containing compound provided from a gas source. The gas source may utilize a chemical feed stock that includes a precursor sulfur-containing compound. The article is then contacted with the sulfur-containing gas until a surface treatment is effected. Next, the article is then optionally contacted with a gaseous neutralization composition, and then a liquid neutralization composition. In another sulfonation method, a first test sample is sulfonated and then analyzed by inductively coupled plasma analysis and X-ray fluorescence spectroscopy. A calibration relationship between the two spectroscopic techniques is determined with the inductively coupled plasma atomic spectroscopic value taken as the accurate value. In subsequent sulfonation runs, test samples are included and monitored by X-ray fluorescence.

Abstract: Pro-drug forms of linear polyamine-bridged platinum compounds and methods for their production and use are provided. The polyamine-bridge portion of the compounds is based on spermine or spermidine, and the central amines of the polyamine-bridge are chemically bonded to labile blocking groups. The presence of the blocking groups serves to minimize the toxicity of the Pt compounds upon administration. Selective removal of the blocking groups and release of the active, unblocked species occurs upon exposure to suitable environmental conditions.

Abstract: The invention relates to sulfonamido derivatives of formula (I) wherein R1-R7 are as defined in the description. Compounds (I) antagonize the vanilloid receptor and can be used for the preparation of medicaments for the treatment of inflammatory states.

Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.

Abstract: The present invention relates to a sequence for the preparation of amino acids, for example alpha amino acids, in particular methionine, by making use of an amidocarbonylation reaction and reuse of the catalyst.

Abstract: An improved process for production of dialkyldithiophosphinic acid including sulfurizing a purified dialkylphosphinic acid by: reacting a hypophosphorous acid or salt with a stoichiometric excess of an alpha olefin in the presence of a free radical initiator to form a reaction product comprising monoalkylphosphinic acid and dialkylphosphinic acid; adding sufficient aqueous base to the reaction product to i) form the salts of the phosphinic acids, and ii) establish an aqueous phase and an organic phase, wherein a monoalkylphosphinic acid solubilizes into an aqueous phase; separating the organic phase from the aqueous phase; acidifying the organic phase and removing the olefin from the organic phase; isolating the purified dialkylphosphinic acid product; and sulfurizing the purified dialkylphosphinic acid product to form a dialkydithiophosphinic acid.

Abstract: Various 13C and 14C carbon labeled compounds Rf—bCF(U)y(T)z??Formula 1A or Rf—bCF2bCF(U)y(T)z??Formula 1B wherein Rf is a linear or branched perfluoroalkyl radical Z(CmF2m)—, m is 1, 3 to 20, or a mixture thereof; Z is F when m is 1, and Z is F, Cl, or H when m is 3 to 20 or a mixture thereof; b is 13 or 14; y is 1, and z is 0 or 1; and when y and z are each 1, U is F, and T is selected from the group consisting of monovalent radicals —X wherein X is I or Br, —CH2—CH2—X, —CH?CH2, —CH2—CH2—OH, —CH2—COOH, —CH2OH, —bCH2OH, —COOH, —bCOOH, —O—CF(CF3)—C(O)F, —O—CF(CF3)—X, —SO2Y wherein Y is H, F or Cl, and —SO3H; and when y is 1, and z is 0, U is selected from the group consisting of divalent radicals ?CH—COOH, ?CH—CH2—OH, and ?O, are disclosed, and a process for their preparation which selectively introduces 13C and 14C carbon labels into a fluoroalkyl chain.

Abstract: The present invention provides BZPA products with improved flowability and two methods of producing such BZPA products. Both methods successfully produce BZPA products that are not prone to agglomerate upon storage, and thus the flowability of such BZPA products does not degrade over time. The first method includes mechanically forming the BZPA crystals into large compacted pellets or briquettes without the introduction of any additives or binders. The compacted pellets are large enough that the physical and chemical effects that occur on the surface of small crystal particles are eliminated or minimized, but small enough that the BZPA can be easily handled and used in commercial applications. The second method includes adding a substantially inert anti-caking agent to the BZPA crystals to minimize or retard their tendency to agglomerate. The preferred anti-caking agent is silicon dioxide (SiO2), which is blended with the BZPA crystals in small amounts.

Abstract: This invention provides compounds of the formula (I) useful for the treatment of disease conditions caused by over activation of Vr1 receptors such as pain or the like in mammals as well as compositions comprising them.

Abstract: The preparation of alkylaryl compounds takes place, inter alia, by a1) preparation of a C4 -olefin mixture from LPG, LNG or MTO streams, b 1) reaction of the C4-olefin mixture obtained in this way over a metathesis catalyst for the preparation of an olefin mixture comprising 2-pentene and/or 3-hexene, and optional removal of 2-pentene and/or 3-hexene, c1) dimerization of the 2-pentane and/or 3-hexene obtained in stage b1) over a dimerization catalyst to give a mixture comprising C10-12-olefins, and optional removal of the C10-12- olefins, d1) reaction of the C10-12-olefin mixtures obtained in stage a1) with an aromatic hydrocarbon in the presence of an alkylation catalyst to form alkylaromatic compounds, it being possible to add additional linear olefins prior to the reaction.

Abstract: A new approach is described to making luminophores which display long emission wavelengths, long decay times, and high quantum yields. These luminophores are covalently linked or otherwise closely associated pairs with a long lifetime resonance energy transfer (RET) donor e.g., a ruthenium (Ru) metal-ligand complex, and a long wavelength acceptor, e.g., Texas Red. The donor and acceptor can be covalently linked by, e.g., poly-proline spacers. The long lifetime donor results in a long lived component in the acceptor decay which is due to RET. The quantum yield of the luminophores approaches that of the higher quantum yield acceptor, rather than the lower quantum yield typical of metal-ligand complexes. The emission maxima and decay time of such tandem luminophores can be readily adjusted by selection of the donor, acceptor and distance between them. Luminophores with these useful spectral properties can also be donor-acceptor pairs brought into close proximity by some biochemical association reaction.

Abstract: The present invention relates to new synthetic methods for preparing 2-methoxyisobutylisonitrile and metal isonitrile complexes, such as tetrakis(2-methoxyisobutylisonitrile)copper(I) tetrafluroroborate, which are used in the preparation of technetium (99mTc) Sestamibi, and novel intermediate compounds useful in such methods.

Abstract: Disclosed is a bis(urea-urethane) compound of the formula wherein R1 and R1? each, independently of the other, is an alkyl group, wherein at least one of R1 and R1? has at least about 6 carbon atoms, R2 and R2? each, independently of the other, is an alkylene group, wherein at least one of R2 and R2? has at least about 3 carbon atoms, R3 is an alkylene group having at least about 2 carbon atoms, and R4 and R5 each, independently of the other, is a hydrogen atom or an alkyl group, and wherein R1 and R1? each contain no more than 2 fully fluorinated carbon atoms.

Abstract: Disclosed is an improved process for producing nitroisourea derivatives which is necessary for producing nitroguanidine derivatives having an insecticidal activity.

Abstract: This invention features permeability enhancer molecules, and methods, to increase membrane permeability of various molecules, such as nucleic acids, polynucleotides, oligonucleotides, enzymatic nucleic acid molecules, antisense nucleic acid molecules, 2-5A antisense chimeras, triplex forming oligonucleotides, decoy RNAS, dsRNAs, siRNAs, aptamers, or antisense nucleic acids containing nucleic acid cleaving chemical groups, peptides, polypeptides, proteins, carbohydrates, steroids, metals and small molecules, thereby facilitating cellular uptake of such molecules.

Abstract: A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.