Abstract: Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.

Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-? by adipose tissue.

Abstract: The invention relates to a method for the production of trifluoroethoxy-substituted benzoic acids, by reaction of a corresponding halogenated benzoic acid with trifluoroethanol in the solvent tetrahydrofuran, in the presence of a base and a copper salt, followed by an acidic work-up.

Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.

Abstract: The invention relates to a process for the preparation, in a single step, of enones by an aldol condensation of a ketone, such as a gem-dimethyl cyclohexylethanone or gemdimethyl cyclohexenylethanone derivative, with an aldehyde in the presence of a novel catalytic system and a co-ingredient, such as a carboxylic acid anhydride or an anhydrous salt, and without the pre-formation of an enolate. The catalytic system is a metal complex, such as a [(Cl)n(alkoxy)4-nTi] or [(Cl)n(alkoxy)4-nZr] complex where n is 1 to 3.

Abstract: The instant invention relates to a process for preparing a compound of formula (I): said process comprising a step (B) which consists in performing a Michael addition of a thioacid RS4H on to an &agr;-substituted acrylamide derivative.

Abstract: A first process for producing an optically active perfluoroalklylcarbinol derivative includes (a) reacting an optically active imine with a compound that is a hemiacetal of a perfluoroalkylaldehyde or a hydrate of a perfluoroalkylaldehyde to obtain a condensate; and (b) hydrolyzing the condensate under an acid condition. A second process for increasing optical purity of an optically active 4,4,4-trifluoro-3-hydroxy-1-aryl-1-butanone derivative includes (a) precipitating a racemic crystal of the derivative, from the derivative; and (b) removing the racemic crystal from the derivative. A third process for increasing optical purity of the butanone derivative includes recrystallizing the derivative. Novel compounds are optically active and inactive 4,4,4-trifluoro-3-hydroxybotanoic aryl ester derivatives.

Abstract: A compound of formula I wherein A is a moiety which provides UV absorbing activity to the compound of formula I that comprises 1 divalent group or 2 monovalent groups, with at least one group having carbonyl (C═O) functionality. R6 is linear or branched C1-C8 alkyl and R5 is a linear or branched C1-C8 alkyl or hydrogen. Sunscreen formulations which contain these compounds and methods for using these compounds to prepare formulations are also provided.

Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.

Abstract: The object of the present invention is to provide a method to suppress changes the concentration of (meth)acrylic acid in the bottom solution discharged from the absorption column, and to enable stable operation for separating and purifying (meth)acrylic acid in the subsequent steps onward. The above-mentioned object can be achieved by way of changing the water amount contained in the gas exhausted from the top portion of the absorption column.

Abstract: This invention relates to process for dihydroxylation of olefins using transition metal catalysts to obtain monofunctional, bifunctional, and/or polyfunctional 1,2-diols of the formula (I) R1R2C(OH)—C(OH)R3R4  (I) where R1 to R4 are defined herein, by reacting an olefin of the formula (II) R1R2C═CR3R4  (II) where R1 to R4 are defined as for formula (I), with molecular oxygen in the presence of an osmium, ruthenium, or manganese compound in water or a water-containing solvent mixture at a pH of from 7.5 to 13.

Abstract: The present invention provides a process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1). The present invention more particularly relates to a process using cyclohexylphenyl ketone for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1).

Abstract: A process for producing a lower aliphatic ester by catalytically reacting a lower olefin and a lower aliphatic carboxylic acid in a gas phase, where the lower aliphatic carboxylic acid is gasified at a relatively low temperature and thereby a mixed gas of the lower olefin and the lower aliphatic carboxylic acid is produced.

Abstract: The invention relates to a process for producing 3,3,3-trifluoro-2-hydroxypropionic acid. This process includes the step of (a) bringing a 1,1-dihalogeno-3,3,3-trifluoroacetone into contact with a basic aqueous solution. The obtained 3,3,3-trifluoro-2-hydroxypropionic acid may be reacted with a C1-C6 lower alcohol under an acidic condition, thereby producing a 3,3,3-trifluoro-2-hydroxypropionate. This propionate may be reacted with a hydride reducing agent (e.g., sodium borohydride), thereby producing 3,3,3-trifluoro-2-hydroxypropanol. These products (i.e., 3,3,3-trifluoro-2-hydroxypropionic acid and its derivatives) are important intermediates for medicines and liquid crystals.

Abstract: A process for preparing racemic mixtures containing nearly equal amounts of stereo isomers of compounds of formula (I), or their salts, by heating an enantiomerically enriched material with thionyl chloride. A required useful enantiomer may thereby be recovered from unwanted mother liquors that would otherwise be otherwise be discarded.

Abstract: A method of effecting a nucleophilic substitution of an alcohol to produce a target product includes the steps of: reacting the alcohol and a nucleophile with an azodicarboxylate and a phosphine. At least one of the azodicarboxylate and the phosphine includes at least one fluorous tag. In several embodiments, the azodicarboxylate includes at least one fluorous tag, and the phosphine includes at least one fluorous tag. A compound has the formula: In the above formula n1, n2, n3, n4, n5, n6, n7, n8, n9 and n10 are independently 1 or 0. X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, X13, X14, X15, X16, X17, X18, X19 and X20 are independently H, F, Cl, an alkyl group, an aryl group or an alkoxy group.

Abstract: Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.

Abstract: The present invention concerns the use of compounds of the Formula (I) for treating different types and symptoms of acute and chronic pain, especially non neuropathic inflammatory pain in mammals. The pain to be treated may be e.g. chronic inflammatory pain, rheumatoid arthritis pain and/or secondary inflammatory osteoarthritic pain. The compounds show an antinociceptive profile and differ from classical analgesics like opioids and non-steroidal anti-inflammatory drugs (NSAIDS) and are useful as specific analgesics.

Abstract: A process for the purification of toluenediisocyanate by fractionating a crude distillation feed containing toluenediisocyante, an organic solvent and less than 2% by weight of phosgene in a heat integrated system having an upstream distillation column, an interchanger and a downstream distillation column which are connected in series. The vapor which is recovered from the upstream distillation column is used to reboil the bottoms product of the downstream distillation column or the feed to the downstream distillation column in the interchanger. The crude distillation feed comprising less than 2% by weight of phosgene is fractionated into three product fractions P1-P3 and optionally a fourth fraction P4. P1 is a noncondensible gas stream enriched with phosgene and/or low-boilers. P2 is a solvent-enriched product. P3 is a high boiler enriched bottoms product comprising toluenediisocyanate, and P4 is a toluenediisocyanate enriched stream lean in highboilers and reaction residues.

Abstract: The present invention provides a process for quenching a gaseous reaction mixture during the phosgenation of diamines in the gas phase to produce diisocyanates. The gaseous reaction mixture contains at least a diisocyanate, phosgene and hydrogen chloride. The quenching liquid is injected into the gas mixture continuously flowing out of a cylindrical reaction zone into the downstream cylindrical quenching zone with the aid of at least two spray nozzles which are arranged at the entrance to the quenching zone at equal distances along the circumference of the quenching zone.