Abstract: Designed iminocylitols that have potent inhibition activity with respect to hexominidases and glycosides are disclosed.

Abstract: The present invention provides new crystalline Forms III, IV and V of clopidogrel hydrogensulfate and the amorphous form of clopidogrel hydrogensulfate, as well as their pharmaceutical compositions, and method of treatments with such compositions. The present invention also provides novel processes for preparation of clopidogrel hydrogensulfate Form I, Form III, Form IV, Form V and the amorphous form. The present invention further provides a novel process where the amorphous form is converted to Form I by contacting Form I with an ether.

Abstract: 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity. The compounds of the present invention have the following formula: or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R1, R2, R3, R4, X, and Z are set in the specification. The invention is also directed to pharmaceuticals compositions comprising one or more compounds of Formula I, optionally further comprising one or more anti-viral agents or immunostimulating agents. Further, the invention is directed to the use of compounds of Formula I for the inhibition of a retroviral infection in cells or tissue of an animal, for the treatment of a patient suffering from a retroviral-related pathology, for the prevention of transmission of HIV infection from an HIV infected pregnant woman to a fetus, and for the prevention of transmission of HIV infection during sexual intercourse.

Abstract: A method and apparatus for synthesizing at least one of alkylene oxides and alkylene glycols from lower alkanes and/or lower alkenes. In the preferred embodiment, the apparatus includes a lower alkane/alkene supply; an oxygen supply for providing a source of oxygen; and a metal oxide catalytic reactor. The metal oxide catalytic reactor includes a reactor chamber; and a catalyst in the chamber for reacting the lower alkane/alkene supply with the source of oxygen to convert the lower alkane/alkene by selective partial oxidation to at least one of the alkylene oxides and alkylene glycols. Also, in the preferred embodiment, a separator, downstream from the reactor, separates the alkylene oxides and alkylene glycols from the total product stream and the unconverted reactants.

Abstract: The present invention relates to the oxidation, by means of oxygen or a gas containing it, of hydrocarbons to the corresponding carboxylic acids, alcohols and/or ketones or of alcohols and/or ketones to the corresponding carboxylic acids. It consists more precisely in a process for oxidizing hydrocarbon, alcohol and/or ketone, using oxygen or a gas containing it, in liquid phase and in the presence of a catalyst dissolved in the reaction medium, characterized in that the catalyst comprises a soluble manganese compound and at least one soluble chromium compound.

Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with a 2,6-dioxo-3-hydroxypiperidin-5-yl group, which may be further substituted in the 5-position with alkyl or halogeno, and in the 4-position with alkyl or a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF&agr;. A typical embodiment is 2-(2,6-dioxo-3-hydroxy-5-fluoro-piperidin-5-yl)-4-aminoisoindolin-1-one.

Abstract: This application relates to matrix metalloprotease inhibitors having the generalized formula in which r is 0-2, T is selected from and R40 is a mono-or bi-heterocyclic structure. More particularly, the present application claims the various stereoisomeric forms of 4-(4′-choloro-biphenyl-4-yl)-4-oxo-2-[2-(4-oxo-4H-benzo[d][1,2,3]triazin-3-yl)ethyl]butyric acid, as well as their pharmaceutically acceptable salts. Pharmaceutical compositions containing these compounds, and methods for inhibiting matrix metalloprotease activity in mammals such as humans and for treating various conditions by administering such compounds are also claimed.

Abstract: The present invention provides a novel bioactive compound 12-(12′-CARBOXY-5′-METHOXYPHENYL)-2,12-DIHYDROXY-DODECA-4-ONE “Sporotricolone”, mainly as acetylcholinesterase (AchE) inhibitor, along with a process for the isolation of said compound from fungus Sporotrichum species.

Abstract: A method for purifying crude 2,6-naphthalenedicarboxylic acid includes a reduction step of reducing crude 2,6-naphthalenedicarboxylic acid containing 6-formyl-2-naphthoic acid with hydrogen and a cleaning step of cleaning the reduction product with alcohol. Preferably, in the reduction step, the crude 2,6-naphthalenedicarboxylic acid and the hydrogen is brought into contact with a hydrogenation catalyst in a liquid phase, and particularly in water. The method makes the purification process less complex and makes it possible to produce high-purity 2,6-naphthalenedicarboxylic acid without damaging equipment or increasing cost.

Abstract: Liquid lysine can be made with almost any particular specification that may be reasonably expected. A multistep process for producing lysine includes at least: fermentation, ultrafiltration, evaporation, and mixing. Depending upon the particular specifications that are to be met, at least two liquids may be taken from selected points in the multistep process. The lysine in these two liquids is concentrated to a desired level and then the liquids are mixed together and returned to the processing feed stream. The process may be applied to any amino acid which can be produced by fermentation.

Abstract: A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.

Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula IIIB have the structure: wherein R1, R2, R, Ar and n are as described in the specification.

Abstract: A process is provided for preparing a compound having the formula wherein R is H or Cl.

Abstract: The present invention relates to optically pure S-(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantially free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof.

Abstract: A compound according to formula (I) wherein: is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; which shows high affinity for muscarinic M3 receptors (Hm3).

Abstract: N-substituted dithiocarbamate esters, pharmaceutical compositions containing them, and methods of treating hyperproliferative disorders such as cancer by administering the N-substituted dithiocarbamate esters.

Abstract: The present application describes novel cyclic &bgr;-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease and/or as TNF-&agr; inhibitors.

Abstract: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof compositions that are 2,3-diacyltartaric acid salts of E-metanicotine.

Abstract: This process for the production of the methyl ethyl ketone cyanohydrin of formula (I) is characterized by the fact that hydrocyanic acid and methyl ethyl ketone are reacted in the presence of diethylamine as a catalyst.

Abstract: A compound selected from those of formula (I): wherein: n represents integer from 0 to 6, R1 represents a group selected from hydrogen, hydroxy, cyano, alkoxy, alkoxycarbonyl, carboxy, optionally substituted aminocarbonyl, and NR4R5 wherein R4, and R5 are as defined in the description, R2 represents a group selected from hydrogen, alkyl, hydroxymethyl, and —U—V—W wherein T, U, V, and W are as defined in the description, and R3 represents a group selected from hydrogen, linear or branched (C1-C6)alkyl, aryl, and, heteroaryl, its isomers, and also addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful in the treatment of CNS disorders.