Abstract: The present invention relates to an N-substituted benzothiophenesulfonamide derivative or a pharmaceutically acceptable salt thereof and applications thereof. Furthermore, it provides an agent for preventing or treating cardiac or circulatory disease and so on caused by abnormal increase of production of angiotensin II or endothelin I based on chymase activity, or by activation of mast cell, and an agent for preventing adhesion after surgery, wherein the agent has a selective inhibitory action on chymase.

Abstract: The use of ?-lipoic acid or ?-dihydrolipoic acid for increasing the bioavailability of mineral salts, the use of ?-lipoic acid or ?-dihydrolipoic acid in combination with metal salts, in particular the use of metal ?-lipoates, metal ?-dihydrolipoates or metal-?-lipoic acid complexes, in particular in mineral preparations or drugs and the metal ?-lipoates, metal ?-dihydrolipoates or metal-?-lipoic acid complexes themselves are described.

Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein A, B, D, E, G, J, n, and R1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof as caspase inhibitors and for the treatment of disorders caused by excessive apoptotic activity.

Abstract: Crystals of (E)-4-[4-(5-methyl-2-phenyl-4-oxazolylmethoxy)benzyloxyimino]-4-phenylbutyric acid (provided that crystals having a melting point of 126° C. to 127° C. are excluded), which have an excellent anti-diabetic action.

Abstract: Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 aklene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 akylene group.

Abstract: The invention relates to a novel process that makes it possible to epoxidize &agr;,&bgr;-unsaturated enones or &agr;,&bgr;-unsaturated sulfones with high conversions and enantiomeric excesses in the presence of a water-soluble base, an oxidant, water, an organic solvent that is immiscible or has only limited miscibility with water, a preactivated diastereomer- and enantiomer-enriched homo-polyamino acid as catalyst, and a specific phase-transfer catalyst as cocatalyst.

Abstract: The present invention has for its object to provide a production method of a pyromellitic anhydride which is not only conducive to an increased catalyst life and, hence, an enhanced operating rate of a plant (reduced downtime) and a reduction in catalyst cost but also conducive to reductions in byproducts and, hence, savings in the cost of after-treatments such as collection and purification. A production method of a pyromellitic anhydride comprising a step for catalytic gas-phase oxidation of a starting mixture gas consisting of a tetraalkylbenzene and/or a trialkylbenzaldehyde and a molecular oxygen-containing gas in a fixed-bed type reactor having a catalyst bed wherein the production method of a pyromellitic anhydride is carried out under the condition that the moisture content of said starting mixture gas to be introduced into the catalyst bed is not more than 2 volume %.

Abstract: The invention relates to the use of bisphosphonic acids of general formula (I) and derivatives thereof for the therapeutic and prophylactic treatment of infectious processes caused by viruses, bacteria, fungi or parasites in humans and animals, by deactivating the &ggr;&dgr;T cells.

Abstract: An optically active cyanohydrin represented by the following general formula (1): ##STR1## wherein each of R1 and R2 is a hydrogen atom or an amino-protecting group, and the configurations relating to the carbon atoms at the *2-position and *3-position are as follows: in the case of the carbon atom at the *2-position being in R-configuration, the carbon atom at the *3-position is in S-configuration, and in the case of the carbon atom at the *2-position being in S-configuration, the carbon atom at the *3-position is in R-configuration, can be efficiently produced by crystallizing one of the optically active cyanohydrins while treating a mixture of cyanohydrin diastereomers in the presence of an amine and an organic solvent to change the configuration relating to the carbon atom at the 2-position and thereby cause isomerization.

Abstract: In a method for treating or preventing allergy or allergic disorders an effective amount of a compound that inhibits intracellular generation of phosphatidic acid and diacylglycerol is administered. The intracellular generation of phosphatidic acid and diacylglycerol results from allergen presentation or mast cell/basophil activation.

Abstract: Bridged bicyclic aromatic compounds are provided having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as defined herein. The novel compounds are useful for modulating gene expression of retinoic acid receptors, vitamin D receptors and thyroid receptors. Pharmaceutical compositions and methods for modulating gene expression are provided as well.

Abstract: The invention relates to methods employing pH-buffered, redox-stabilized compositions comprising halide and oxyhalide ions. The compositions can be administered to food animals to effect enhanced food utilization, lower mortality, decreased nitrogen excretion, decreased dependence on antibiotics and vaccines, overall enhanced health and immunostimulation in the animals. Additionally, the compositions can be used to treat food animal carcasses to reduce foodborne pathogens and spoilage organisms.

Abstract: Compositions and methods for relaxing smooth muscle in a warm-blooded animal are provided, comprising the step of administering to the animal a transition-metal nitrosyl complex. In one aspect, the transition-metal nitrosyl complex is represented by the formula L.sub.3 M(NO).sub.y X.sub.3-y where L is a two-electron Lewis base or L.sub.3 is a six-electron Lewis base, M is a Group 6 or 8 transition-metal, and when y is 1, X is carbon monoxide, and when y is 2, X is a halide or pseudohalide. In another aspect, the transition-metal nitrosyl complex is represented by the formula ?M(NO).sub.2 X.sub.y !.sub.2 where X is a halide or pseudohalide, and when M is a Group 6 transition-metal, y is 2, and when M is a Group 8 transition-metal, y is 1. Methods are also described for treating hypertension, angina pectoris, congestive heart disease, and impotence utilizing pharmaceutical compositions comprising the above-described transition-metal nitrosyl complexes.

Abstract: Compounds of formula (I) wherein R.sup.1 -R.sup.7, R.sup.10, X and the dotted bond have the meaning given in the specification, bind selectively to retinoid RXR receptors and are useful as antiproliferative agents for dermatological and oncological indications.

Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted biaromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a')-(f'): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.

Abstract: The present invention discloses novel sodium channel active compounds, processes for making such compounds, and the use of such compounds as local anesthetics and pesticides.

Abstract: Particularly the invention relates to the compounds of formula I ##STR1## wherein Ar represents carbocyclic aryl, heterocyclic aryl or biaryl;R.sub.1 represents lower alkyl, cycloalkyl, aryl-lower alkyl, lower alkoxy-lower alkyl, aryl, cycloalkyl-lower alkyl, halo-lower alkyl;R.sub.2 represents hydrogen or lower alkyl;R.sub.3 and R.sub.4 represent independently hydrogen, lower alkyl, lower alkoxy, halo, hydroxy, acyloxy, lower alkoxy-lower alkoxy, trifluoromethyl or cyano; or R.sub.3 and R.sub.4 together represent lower allylenedioxy;n represents an integer from 1 to 5;pharmaceutically acceptable prodrug derivatives; and pharmaceutically acceptable salts thereof; methods for preparation thereof;pharmaceutical compositions comprising said compounds; and a method of inhibiting TNF-alpha activity and matrix-degrading metalloproteinases in mammals using such compounds.

Abstract: A chiral ligand having the following structure: ##STR1## wherein AR is any aromatic and/or ring structure, and R is selected from the group consisting of aryl, oxygenated aryl, alkyl, oxygenated alkyl, AR, oxygenated AR and combinations thereof.

Abstract: The invention relates to dithiane adducts of substituted benzoins and substituted benzoins derived therefrom each of which are useful as protecting groups, photolabile linkers, and fluorescent probes.