Abstract: The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pyl

Abstract: The present invention provides analogues of autoinducer molecules that are derivatized to allow their attachment to other molecules and surfaces. Libraries of the autoinducer analogues are also contemplated. Also provided are methods for using the compounds of the invention to produce compositions, such as immunoconjugates, antibodies and vaccines, which are useful for treating and preventing disease states in a subject. The compositions of the invention are also useful in various assays, including assessing the autoinducer load in a subject.

Abstract: Disclosed is a process wherein a first olefin selected from certain &agr;,&bgr;-dihydroxyalkenes and 4-(alkenyl)ethylenecarbonates is reacted with a second olefin reactant to produce an olefin metathesis product. When the first olefin reactant is an optically enriched or enantiomerically pure &agr;,&bgr;-dihydroxyalkene, cross metathesis reactions produce products possessing the same optical purity. The &agr;,&bgr;-dihydroxyalkenes and the 4-(alkenyl)ethylene carbonates may be converted to hydrogenated products, and the 4-(alkenyl)ethylenecarbonates may be decarboxylated to provide the corresponding epoxides. The products of the disclosure may be used as monomers for the preparation of specialty polyesters and as intermediates in the manufacture pharmaceuticals and other chemicals.

Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2 , R3 and R4 are as defined herein.

Abstract: A non-aqueous electrolyte comprising a non-aqueous solvent and a lithium salt dissolved therein, and a cyclic carbonate, linear carbonate, and vinylene carbonate having a chlorine content of 100 ppm or less, and a lithium secondary battery using the same.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, W and Y independently of one another each represent hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups  in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: A process for the preparation of the compound 13-(N-Boc-&bgr;-isobutylisoserinyl)-14&bgr;-hydroxybaccatine III 1,14-carbonate.

Abstract: The present invention provides an alkylene-carbonate synthesis catalyst comprising a compound insoluble to one phase containing alkylene carbonate produced when the alkylene oxide and carbon dioxide are reacted with the catalyst and soluble to the other phase substantially free of alkylene carbonate. The catalyst allows alkylene carbonate to be produced with high yield and selectivity and be readily collected. The catalyst also facilitates repeated or continuous reaction process in a cost-effective manner. The present invention also provides an apparatus for producing alkylene carbonate using the catalyst.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: 1

Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.

Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I)

Abstract: Novel compounds of the formula I, in which R, R1 and R2 are as defined in patent claim 1, are inhibitors of coagulation factor Xa and VIIa and can be employed for the treatment of thromboses, myocardial infarction, arteriosclerosis, inflammation, apoplexis, angina pectoris, restenosis after angioplasty, claudicatio intermittens, tumours, tumour diseases and/or tumour metastases.

Abstract: Compounds of the formula: wherein R1 is H or methyl, R2 is H or alkyl, R3 is C2-C4 alkylene, n is 0-4, n′ is 1-4, x is one or more, y is one or more, x+y=z, and A is a z-valent organic group linked to the group or groups on the left thereof through a carbon atom and is linked to the group or groups on the right thereof through an ether or ester oxygen atom, or, provided that x and y are both 1, a direct bond.

Abstract: This invention encompasses a method for the treatment or prevention of prostaglandin mediated diseases comprising administering to a mammalian patient a compound of formula I: in an amount that is effective to treat or prevent said prostaglandin mediated disease. Novel compounds are also disclosed.

Abstract: The present invention provides a more economical method of producing multifunctional carbonate resins. It overcomes the disadvantage of using relatively expensive starting material, such as polyglycidyl ethers, that have traditionally been used. The present invention makes use of readily available and inexpensive multi-isocyanate compounds reacted with organic carbonates that contain pendant hydroxyl groups to produce products that contain two or more carbonate functionalities. One form of the present invention is a method for preparing a carbonate urethane compound by reacting a carbonate containing compound that also contains a reactive hydroxyl group with a compound containing at least two isocyanate groups. The reaction is performed in a solvent and in the presence of a base.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: 1

Abstract: This invention provides a precursor compound of a novel fluorescence-labeled probe for DNA, prepared by covalent binding of a fluorescent substance such as fluorescein isothiocyanate, wherein a conjugating group was bounded, with aminoalkylate phenylamine. This invention also provides a novel fluorescence-labeled probe for DNA by diazotizing amino group of phenylamine contained in the precursor compound. Furthermore, a fluorescence labeled plasmid can be produced by conjugating the fluorescence-labeled probe and purine ring of guanine contained in the DNA plasmid through diazonium group.

Abstract: A method of synthesizing trimethylene carbonate, which includes the steps of reacting 1,3-propanediol and phosgene in vapor form, providing a combination of temperature and pressure at which trimethylene carbonate is in its vapor phase, providing a residence time sufficient to react 1,3-propanediol and phosgene to trimethylene carbonate, condensing the trimethylene carbonate vapors, and isolating the condensed trimethylene carbonate.

Abstract: Compounds of formula (I); wherein R1=alkyl, alkenyl or alkynyl, O-alkyl, O-alkenyl or optionally substituted, optionally interrupted O-alkynyl; R2=hydrogen or halogen; R3=hydrogen, alkyl or halogen; R4=NHR′ or NHOR″, R′ or R″ are identical or different and represent hydrogen, alkyl, alkenyl or alkynyl, aryl; R5=hydrogen or O-alkyl; R6=alkyl or CH2—O-alkyl; R7=hydrogen or alkyl or R6 et R7 form a cycle together with the carbon carrying them in addition to the addition salts thereof with bases. The compounds of formula (I) have antibiotic properties.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The present invention relates to a lithium ion battery, more particularly to a new electrolyte and a lithium ion battery which comprises the same using an anode including graphitized carbon and a cathode including lithium-containing transition metal oxide. The present invention provides a compound of 4-carbomethoxymethyl-1,3-dioxan-2-one or 4-carboethoxymethyl-1,3-dioxolan-2-one represented by formula (1) which comprises both a cyclic ring carbonate structure and a linear carbonate structure, a lithium-containing electrolyte which includes the compound of formula (1), and a lithium ion battery which includes the electrolyte using the anode including graphitized carbon and the cathode including lithium-containing transition metal oxide. The lithium ion battery of the present invention fabricated by using the new compound has high electric capacity because of the graphitized carbon, and superior charge-discharge cyclic life characteristic and low temperature performance.

Abstract: The synthesis of taxol and other tricyclic and tetracyclic taxanes.

Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

Abstract: A method for preparing carbonates includes reacting an alkylene oxide with carbon dioxide in the presence of a catalyst and a non-protic solvent. The method further includes having the boiling point of the solvent greater than about 70 ° C., and removing the solvent from the reaction product. The solvent used in the various forms of the present invention can be glyme, diglyme, tetraglyme, cumene, toluene, tetrahydofuran, cyclohexanone, ethylbenzene, aromatic hydrocarbons, or ethers. The catalyst used can be a tetraalkyl ammonium halide, such as tetraethyl ammonium bromide. The alkylene oxide that can be used in the invention can include Bisphenol A, Bisphenol B, Bisphenol F, alkylene oxides that have alkyl substituent groups, alkylene oxides that have aryl substituent groups, and alkylene oxides that contain both alkyl and aryl substituent groups. An essentially solvent free carbonate can be prepared by flash removal of the solvent.

Abstract: The present invention provides a simple and inexpensive process for preparing glycerol carbonate. Namely, according to the present invention, glycerol carbonate is prepared by reacting glycerol with urea.

Abstract: Diels-Alder adducts of dienophiles such as epoxybutene with dienes such as cyclopentadiene and cyclohexadiene are produced by carrying out the Diels-Alder reaction thereof at an elevated pressure. Addional dienophiles disclosed include 2,5-dihydrofuran and derivatives thereof; Additional dienes include isoprene and butadiene. Compounds produced from such reactions are also disclosed.

Abstract: Compounds of the Formula 1, Formula 2, Formula 3 and Formula 4 wherein the symbols have the meaning assigned to them in the disclosure have retinoid-like biological activity.

Abstract: Compounds of Formula 1 and of Formula 2 where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid negative hormone like biological activity.

Abstract: This invention concerns a process to provide high purity alkylene carbonate though use of multiple distillations wherein the unused fractions are recycled to the reactor. The high purity alkylene carbonate may be further purified by use of carbon to produce electrochromic or photochromic grade alkylene carbonate by reducing its UV absorbance.

Abstract: The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Abstract: The synthesis of taxol and other tricyclic and tetracyclic taxanes.

Abstract: The present invention relates to a method to prepare alkylene carbonate of the formula (1) wherein, R1 and R2 are each independently H; C1-C4 alkyl or phenyl group; which method characterized by reacting alkylene oxide with carbon dioxide in the presence of a catalyst system comprising a) metal halide [MXm] and b) pyridine or pyridine derivative [Py], wherein Py is selected from a group of pyridines; M is a metal atom selected from the group consisting of Zn, Fe, Mn, Pb and In; X is a halogen selected from the group consisting of Cl, Br and I; and m is 2 or 3.

Abstract: A catalyst of the formula (1) for the synthesis of alkylene carbonate by reacting alkylene oxide and carbon dioxide LmMXn  (1) wherein L is selected from a group of pyridines; M is a metal atom selected from Zn, Fe, Mn, Pb and In; X is a halogen atom selected from Cl, Br and I; m is 1 or 2, and n is 2 or 3.

Abstract: The invention relates to a process for the preparation of vinylene carbonate of the formula (I) by reacting a monohaloethylene carbonate of the formula (II) in which X is a halogen atom, with a dehydrohalogenating agent at elevated temperature in the presence of an organic solvent, characterized in that the organic solvent employed is ethylene carbonate. The process according to the invention enables vinylene carbonate to be prepared in a simple manner and in high yield. The vinylene carbonate prepared in accordance with the invention can be used for various applications.

Abstract: Intermediates for the preparation of himbacine exhibiting muscarinic M2 receptor antagonism, which are hydronaphtho[2,3-c]furan derivatives represented by general formula (1) or intermediates for the preparation thereof: wherein R1 is lower alkyl or aralky; R2 is hydrogen, lower alkyl or aralkyl; R3 and R4 together represent oxygen or methylene, or alternatively R4 is hydroxyl, lower alkoxy, aralkyloxy or lower acyloxy, with R3 being hydrogen; R5 and R6 together represent oxygen, or alternatively R6 is hydroxyl, lower alkxy, aralkyloxy or lower acyloxy, with R5 being hydrogen; and either of the broken lines is a single bond and the other thereof is a double bond, or alternatively both are single bonds.

Abstract: This invention concerns a process to provide high purity alkylene carbonate though use of multiple distillations wherein the unused fractions are recycled to the reactor. The high purity alkylene carbonate may be further purified by use of carbon to produce electrochromic or photochromic grade alkylene carbonate by reducing its UV absorbance.

Abstract: The invention relates to a process for the preparation of monohalogenated 2-oxo-1,3-dioxolanes of the general formula C3H3XO3  (I) in which X is Cl or Br, characterized in that the monohalogenation is carried out starting from ethylene carbonate with sulfuryl dihalides under UV irradiation and in the absence of solvents.

Abstract: The present invention relates to novel substituted bicyclic lactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, cranial cerebral trauma, states of pain or CNS-mediated spasms.

Abstract: Described are benzoxazine and benzothiazine compounds of the formula I defined herein, methods for their preparation and methods for their use in pharmaceuticals based on their activity as NO-synthases (NOS) inhibitors.

Abstract: Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences.

Abstract: The synthesis of taxol and other tricyclic and tetracyclic taxanes.

Abstract: Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the &agr;1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer; R1 represents an organic or inorganic group; R2 represents halogen or C1-C6 alkyl; RN is an alkylene carrying a substituted piperazine, piperidine, or tetrahydropyridine; and R4 is hydrogen or C1-C6 alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

Abstract: A process for the continuous production of 1,3-dioxolan-2-ones such as ethylene carbonate or propylene carbonate by reacting a corresponding oxirane with carbon dioxide in the liquid phase in the presence of a catalyst comprises conducting the reaction in a two-part reactor in whose first part the reaction is taken with backmixing to a conversion of not less than 80% of the oxirane II and in whose second part the reaction is completed under nonbackmixing conditions, and passing the carbon dioxide in countercurrent to the oxirane II in the entire reactor.

Abstract: A process for the synthesis of alkylene carbonates, such as ethylene carbonate, by reacting alkylene oxides with carbon dioxide in the presence of a porous solid support catalyst containing an alkali or alkaline earth metal component.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: The present invention relates to dioxocyclopentyl hydroxamide derivatives of the formula wherein X, Z and Q are as defined in the specification, and to pharmaceutical compositions and methods of treatment thereof.

Abstract: Monofluoromethyl ethylene carbonate, difluoromethyl ethylene carbonate and trifluoromethyl ethylene carbonate are provided as novel compounds. These compounds are very useful as solvents because they are chemically and physically stable, have a high dielectric constant, can readily dissolve organic substances and have a wide application temperature range. These compounds have excellent charge and discharge cycle characteristics, have a high flash point, and are safe as non-aqueous elecytrolytes. Hence, batteries using these compounds withstand voltage and have excellent charge and discharge cycle characteristics.

Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.