Abstract: A novel process for the purification of Pemirolast, whose potassium salt is an anti-allergic pharmaceutical product, is disclosed.

Abstract: This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: as MEK inhibitors, pharmaceutical compositions containing the same, and methods of using the same as for treatment and prevention of inflammatory disorders or as an anticancer radiosensitizing agent.

Abstract: A “one-pot” process is described herein for the production of pyrazole compounds of general formula (II) comprising the steps of reacting a compound of general formula (III) with an acylating agent in the presence of a base and an optional activating agent followed by the addition of a hydrazine compound in situ.

Abstract: A method for producing cyanoacetic acid esters of general formula (I): wherein R represents on optionally substituted linear or branched C1-8 alkyl group or an aryl C1-4 alkyl group. According to the method, an alkoxypropionitrile of the general formula (II): wherein R is defined above, is oxidized to form the desired product in the presence of a catalyst, based on lead or on one of the transition metals, using oxygen or an oxygen-forming reagent.

Abstract: A method and catalyst composition for economically producing aromatic carbonates from aromatic hydroxy compounds is disclosed. The present invention provides a method for carbonylating aromatic hydroxy compounds, comprising the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a halide-free carbonylation catalyst composition comprising an effective amount of at least one Group 8, 9, or 10 metal source, an effective amount of a first inorganic co-catalyst comprising at least one Group 14 metal source, an effective amount of a salt co-catalyst, and optionally an effective amount of a second inorganic co-catalyst selected from the group consisting of a Group 4 metal source, a Group 7 metal source, a Group 11 metal source, and a lanthanide element source, and optionally an effective amount of a base.

Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various mammalian cellular receptors, including G-protein coupled receptors. A third aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors or transporters. Another aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for mammalian dopamine, muscarinic or serotonin receptors.

Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as and antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergilus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicilium genus, some are obtained by treating the fermentation products using the method of chemical synthesis or they are the products of total chemical synthesis. The purity of the active ingredient is an important factor for manufacturing the safe and effective pharmaceutical, especially if the pharmaceutical product must be taken on a longer term basis in the treatment or prevention of high plasma cholesterol. The accumulation of the impurities from the pharmaceuticals of lower purity may cause many side effects during the medical treatment.

Abstract: The present invention provides compounds that act to suppress p53 activity in mammalian cells, and a method to effectively suppress p53 activity in the cells of a mammal subject to a stress or pathology that is ameliorated by such suppression.

Abstract: The invention relates to a process for the preparation of anhydrous or substantially anhydrous formic acid. The process has the special feature that a liquid of the general formula I where the radicals R1 and R2 are alkyl, cycloalkyl, aryl or aralkyl groups, or R1 and R2 jointly, together with the N atom, form a heterocyclic 5- or 6-membered ring, and only one of the radicals is an aryl group, and where R3 is hydrogen or a C1-C4-alkyl group, employed as extractant is also employed as washing liquid for the offgases produced in the process.

Abstract: A process for obtaining (nitroxymethyl)phenyl esters of salicylic acid derivatives of formula (I) wherein R1 is the OCOR3 group characterized in that it comprises the following steps: a) reaction of a halide of a salicylic acid derivative with hydroxybenzylacohol in the presence of a base: b) nutration of the obtained product in anhydrous conditions by a mixture of nitric acid with a different inorganic acid, or an organic acid, or an anhydride of one or two organic acids: c) recovery of the final product.

Abstract: An alkylene carbonate such as propylene carbonate is contacted with an alumina or silica solid adsorbent having a surface area of 50-400 m2/g such as basic alumina to remove impurities therefrom and improve color and color stability.

Abstract: There is provided a method for obtaining an alkyladamantyl ester efficiently by distilling and purifying a crude alkyladamantyl ester containing impurities which decompose the alkyladamantyl ester without decomposing the alkyladamantyl ester. The crude alkyladamantyl ester such as crude 2-methyl-2-adamantyl methacrylate is distilled in the presence of a heterocyclic compound and/or a basic compound such as 3-ethyl-3-hydroxymethyloxetane or diglycidyl bisphenol A.

Abstract: The present invention provides non-hygroscopic, crystalline salts of levodopa ethyl ester (LDEE), wherein the salt is the octanoate salt, the myristate salt, the succinate salt, the succinate dihydrate salt, the fumarate salt or the fumarate dihydrate salt of levodopa ethyl ester. The subject invention also encompasses compositions comprising a levodopa ethyl ester salt and a carrier and processes for making these compositions. In addition, the subject invention concerns pharmaceutical compositions comprising a levodopa ethyl ester salt and a pharmaceutically acceptable carrier, as well as processes for making these pharmaceutical compositions.

Abstract: Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5—, (f) —L4—N(R5)—C(W)—L7—L5—, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally subs

Abstract: A process for preparing saturated carboxylic acids having from 1 to 4 carbon atoms at a reaction temperature of from 100° C. to 400° C. and pressures of from 1.2×105 Pa to 51×105 Pa by gas phase oxidation of saturated and/or unsaturated C4-hydrocarbons, with an oxygen-containing gas and water vapor in the presence of at least one catalyst. The gas leaving the reactor is partly recirculated in a reaction gas circuit. This reaction gas circuit is configured such that part of the organic acids formed in the gas-phase oxidation is taken from the gas leaving the reactor so that the acid content of the recirculated part of the gas leaving the reactor is from 0.01% to 6.0% by volume.

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.

Abstract: The invention relates to a process for preparing constant-weight thrombin inhibitors of the formula I where n is 0, 1, 2, and tautomers thereof, wherein an aqueous solution of the active substance is spray dried.

Abstract: This invention concerns a process for the manufacture of anhydro- and dianhydro- hexitols, pentitols, and tetritols by the dehydration of sugar alcohols (alditols) in the presence of a dehydration catalyst and with the assistance of an inert gas sparge.

Abstract: The present invention relates to a novel compound 4,8-dodecadienedinitrile represented by the following formula (1): wherein means a cis or trans bond, and a process for preparing 4,8-dodecadienedinitrile which comprises reacting a 2-alkoxy-5,9-cyclododecadienone oxime or a 2-halogeno-5,9-cyclododecadienone oxime with formic acid and hydroxylamine.

Abstract: A mercaptocarboxylic acid of formula (I) is prepared by reacting an unsaturated carboxylic acid of formula (II) with a hydrosulphide of formula ASH, A being an alkali metal cation or a cation NR3R4R5R6+, R3 to R6 each representing H or a hydrocarbon radical, or of formula Q(SH)2, Q being an alkaline-earth metal cation, by acidifying the resulting reaction medium in order to obtain the desired compound (I). According to the present invention, the reaction is carried out with a supply of H2S other than that supplied by the neutralization of the acid (II). In particular, H2S is introduced into the medium by a direct external supply. H2S can also be produced in situ by reacting the hydrosulphide with at least one acid introduced into the medium. The compound (I) is obtained with a very good selectivity.