Abstract: The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.

Abstract: This invention relates to lactam and thiolactam derivatives having useful anticonvulsant and anxiolytic activity, pharmaceutical compositions containing these compounds and therapeutic applications using such compositions.

Abstract: The present invention addresses substituted pyridyl pyrroles, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists and inhibitors of the biosynthesis and action of TNF-.alpha. and IL1. The compounds block the action of glucagon at its receptors and thereby decrease the levels of plasma glucose. The instant pyrroles are also inhibitors of TNF-.alpha. and IL1 and may be used as antidiabetic agents as well as other cytokine mediated diseases. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production of one or more cytokines occurs. Interleukin-1 (IL-1) and Tumor Necrosis Factor (TNF) are cytokines produced by a variety of cells, which are involved in immunoregulation and other physiological conditions, such as inflammation.

Abstract: A process for the production of a solid dispersion of at least one therapeutic agent in a hydrophilic carrier having enhanced solubility in an aqueous media comprising dissolving at least one therapeutic agent in a volatile organic solvent containing a very hydrophilic polymer and evaporating the solvent to dryness to form a co-precipitate of therapeutic agent and hydrophilic polymer and the resulting products and their therapeutic method of use.

Abstract: The present invention is concerned with diaryl compounds of formula (l) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.

Abstract: Recovery of carboxylic acid from an amine-based, water-immiscible organic extractant solution thereof that contains an extraction enhancer, by extraction of acid into an aqueous phase. In a preliminary step the enhancer is removed from the extractant solution by extraction with an aqueous solution containing at least 50 % by weight of a salt of the carboxylic acid present in the extractrant. The process is applicable to the recovery of carboxylic acid from a fermentation broth.

Abstract: To provide an azeotropic composition comprising cis-1,1,2,2,3,4-hexafluorocyclobutane and at least one compound selected from the group consisting of methanol, ethanol, isopropanol, n-propanol, tert-butanol, cyclopentane, n-octane, isooctane, n-heptane and methylcyclohexane, and a detergent, drying agent and foaming agent, which use the above-mentioned azeotropic composition. The azeotropic composition of the present invention is an alternative fleon composition having less influence on plastics, being excellent in solvency and having less influence on the ozone layer.

Abstract: The liquid and gaseous products formed by reacting oxygen with isobutane in an oxidation reactor are separately processed; the liquid reaction product being charged to a distillation zone and separated into a lower boiling isobutane fraction and a higher boiling fraction comprising tertiary butyl alcohol and tertiary butyl hydroperoxide; the gaseous reaction product comprising inert gases and vaporized and/or entrained isobutane being cooled by an amount sufficient to condense isobutane contained therein for recycle to the oxidation reactor; the remaining gases, including isobutane being charged to a tertiary butyl alcohol absorber to obtain a solution of isobutane in tertiary butyl alcohol that is recycled to the distillation zone.

Abstract: A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 represents ##STR2## in which r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1;R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl or a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4 ; andR.sub.3 is CN;said process comprising reacting a compound of formula (II): ##STR3## wherein R.sub.1 ' is R.sub.1 or a group convertible thereto, and R.sub.3 ' is an electron withdrawing group, with a source of nitrous acid, and thereafter converting the resulting .dbd.NOH group to .dbd.NR.sub.2 wherein R.sub.2 is as defined in formula (I), converting R.sub.1 ' and R.sub.3 ' when other than R.sub.1 and R.sub.3 to R.sub.1 and R.sub.3, and thereafter optionally forming a pharmaceutically acceptable salt.

Abstract: The present invention relates to quaternary nitrogen-containing phosphate compounds, and the pharmaceutically-acceptable salts and esters thereof having the general structure: ##STR1## wherein: Z is a saturated, unsaturated, or aromatic, monocyclic or polycyclic carbocycle or monocyclic or polycyclic heterocycle containing one or more heteroatoms selected from O, S, or N;Y is N.sup.+ (R.sup.8).sub.2 or C(R.sup.1).sub.2 and when Y is C(R.sup.1).sub.2, at least one R.sup.2 must be N.sup.+ (R.sup.8).sub.3 ;R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are defined in claim 1, m and n are integers from 0 to 10; m+n is from 0 to 10;R is COOH; PO.sub.3 H.sub.2 ; SO.sub.3 H; or P(O)(OH)R.sub.4, wherein R.sub.4 is substituted or unsubstituted alkyl of 1-8 carbons atoms.The present invention further relates to pharmaceutical compostions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients.

Abstract: A process for the preparation of 1,2-butylene oxide by the catalytic hydrogenation of vinyl oxirane, in which use is made of a palladium catalyst on a support of barium sulfate, zirconium oxide or titanium dioxide or a rhenium-containing supported palladium catalyst.

Abstract: The invention relates to a pharmaceutical preparation comprising a plasma protein wherein said preparation is free of infectious agents as well as essentially free of denaturation products and is obtainable by a method that encompasses the following steps:a) addition of a polyether and a chaotropic agent to a solution comprising the plasma protein, optional lyophilization of the solution;b) inactivation of infectious agents in the presence of the polyether by a physio-chemical or chemical treatment, andc) removal of the polyether and the chaotropic agent.

Abstract: A propylene epoxidation process wherein a supported silver catalyst is utilized may be operated at high efficiency even in the absence of any organic chloride in the feedstream, provided the catalyst is first contacted at an elevated temperature with a treatment stream comprised of an organic chloride and molecular oxygen.

Abstract: The present invention is directed to certain novel compounds identified as 4-heterocycle substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.4, R.sup.5, A, R.sup.3 and the dashed line are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: This invention is concerned with polymorphic forms of the compound N-?1(R)-?(1,2-dihydro-1-methanesulfonylspiro?3H-indole-3,4'-piperdin!-1'-y l)carbonyl!-2-(phenylmethyloxy)ethyl!-2-amino-2-methylpropanamide methanesulfonate which is a growth hormone secretagogue that is useful in food animals to promote their growth thereby rendering the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, and to treat medical conditions which are improved by the anabolic effects of growth hormone. The instant polymorphic forms have advantages over the other known forms of N-?1(R)-?(1,2-dihydro-1-methanesulfonylspiro?3H-indole-3,4'-piperdin!-1'-y l)carbonyl!-2-(phenylmethyloxy)-ethyl!-2-amino-2-methylpropanamide methanesulfonate in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

Abstract: Disclosed are degradable materials including molded products, laminates, foams, nonwoven materials, adhesives, coatings and films, and particularly packaging films. The materials are made using polydioxaneone polymers comprising at least two different dioxaneone-based repeating units. Preferred polymers are polydioxanediones. First repeating units have less carbon atoms in constituent groups extending from the polymer backbone than second repeating units. Physical characteristics and degradation of the materials can be varied by varying the choice and/or relative proportions of first and second repeating units in the polydioxaneone polymers. Methods for preparing polydioxaneone polymers that can be used in the manufacture of the materials are also discussed, as are suitable monomers and methods for preparing such monomers.

Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.

Abstract: The invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the structure: ##STR1## wherein Y is --(CH.sub.2).sub.n --, where n is 1, 2, 3, 4 or 5; --(CH.sub.2).sub.h --O--(CH.sub.2).sub.k --, where h and k are independently the same or different and are 2, 3 or 4; --(CH.sub.2).sub.h --CH.dbd.CH--(CH.sub.2).sub.k --; or --(CH.sub.2).sub.h --C.tbd.C--(CH.sub.2).sub.k --, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is O, NH, or CH.sub.2 ; wherein R.sup.1 is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R.sup.2 and R.sup.4 are independently the same or different and are H, or a linear or branched chain alkyl group; wherein R.sup.3 is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R.sup.5 and R.sup.6 are independently the same or different and are H, OH, Cl, Br, F, NO.sub.2, CN, CF.

Abstract: A process for the trimerization of aqueous formaldehyde solution to produce trioxane in a multistage in situ catalyst reactor-extractor column containing a cationic exchange resin. The process entails countercurrent flow of formaldehyde solution and solvent across reactor and extractor stages wherein trioxane, produced from formaldehyde at the reactor stages, is subsequently separated at the extractor stages utilizing a suitable solvent.

Abstract: An antiproliferative and antiviral preparation of a metal ion chelating agent such as picolinic acid or derivatives thereof. The chelating agent is provided in an ointment base or in solution for topical or intravaginal use. The topical preparations have antiviral and antiproliferative effects and are used in the treatment of warts, psoriasis, skin cancers and other proliferative diseases and in the prevention of sexually transmitted diseases such as genital warts, herpes and AIDS.