Abstract: The invention provides compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 5-membered ring heteroaryl group containing 3 or 4 nitrogen heteroatoms which is linked to the quinoxalinedione ring by a ring carbon or nitrogen atom said group being optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by 1 or 2 substituents each independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, C3-C7 cycloalkyloxy, —COOH, C1-C4 alkoxycarbonyl, —CONR3R4, —NR3R4, —S(O)p(C1-C4 alkyl), —SO2NR3R4, aryl, aryloxy, aryl(C1-C4)alkoxy, and het, said C1-C4alkyl being optionally substituted by C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, halo(C1C4)alkoxy, C3-C7 cycloalkyloxy, C3-C7 cycloalkyl (C1-C4) alkoxy, —COOH, C1-C4 alkoxycarbonyl, —CONR3R4, —NR3R4,—S(O)p(C1-C4 alkyl), —SO2(aryl), —SO2NR3R4 morpholino, aryl, aryloxy, aryl(C1-C4)

Abstract: Spirolaxine, the compound of formula (I) wherein R is H, and the novel compounds of formula (I) wherein R is (C1-C5) alkyl or CH3(CH2)nCO and n is 1, 2, 3 or 4 are useful in treating gastroduodenal diseases such as gastric ulcers, duodenal ulcers and gastric cancer caused by Helicobacter pylori. Spirolaxine and spirolaxine methyl ether are isolated from the fermentation of Sporotrichum pruinosum ATCC 74278. Spirolaxine and the compounds of formula (I) are also useful in combination with H2 antagonist, colloidal bismuth subcitrate and other antibiotics.

Abstract: The present invention relates to 2-aminopyridine derivatives of the formula I: or pharmaceutically acceptable salts thereof, wherein A and B are each independently H, or together, A and B form a ring fused to the phenyl ring, said ring being saturated or unsaturated and containing from 5 to 7 ring member atoms, where said ring member atoms may optionally comprise from 1 to 2 heteroatoms selected independently from the group consisting of N, O or S, provided that no two adjacent ring members are heteroatoms; X is oxygen or a single bond; Y is (C1-C6)alkyl; R1 is hydrogen, (C1-C6)alkyl or a (C1-C6 alkyl) group substituted with —NR2R3 wherein R2 and R3 are either selected independently from the group consisting of H, alkyl, aryl, aralkyl or tetrahydronaphthalene, wherein said aryl group or said aryl moiety of said aralkyl group is phenyl or naphthyl, said alkyl group or said alkyl moiety of said aralkyl group contains from one to six carbon atoms and is straight-chained or branched,

Abstract: The present invention provides a device, preferably a collar or ear tag, capable of the controlled, sustained release of an effective amount of an active ingredient that can protect an animal against arthropod pests, comprising a reservoir containing a novel gel formulation comprising a fatty acid, an organic solvent which is a linear aliphatic ester, a silicone-based fluid, or a combination thereof, and an active ingredient that can protect the animal against one or more arthropod pests.

Abstract: The present invention provides the amino acid and nucleotide sequences of a CCV spike gene, and compositions containing one or more fragments of the spike gene and encoded polypeptide for prophylaxis, diagnostic purposes and treatment of CCV infections.

Abstract: Compounds of the formula (I): wherein A, Y, R, X, R1, R2, R3 and R4 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases or other disorders involving nerve damage.

Abstract: The present invention relates to compounds of the formula and the pharmaceutically acceptable salts and solvates thereof wherein X1, X2, X3, R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods of treating shizophrenic and shizo-affective disorders, and related disorders which may be treated by administering compounds having dopaminergic activity such as the above compounds of formula 1.

Abstract: Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.

Abstract: A method and device for mass spectrometry analysis, wherein a mass spectrometer is adapted for use with helium droplets, as an ionization site medium, with a proton being initially captured by a large helium droplet (˜10,000 helium atoms) and then cooled evaporatively to 0.4 Kelvin. The protonated helium droplet then picks up a neutral molecule of interest and the neutral molecule is protonated inside of the droplet with the liquid helium droplet acting as a heat bath to provide rapid cooling of the newly formed protonated molecule. As a result, there is essentially no energy available, at 0.4 Kelvin, for the protonated molecule to fragment. Remaining liquid helium is removed and the stably maintained protonated molecule is detected by a mass spectrometer. Since the molecules do not fragment when protonated (ionized), each compound in a mixture analyses gives one mass and the number of ions of a particular mass detected is directly proportional to the molar percentage of that mass in the sample.

Abstract: The present invention is concerned with a crystalline, polymorphic form of a compound of formula (I) characterized by a powder X-ray diffraction pattern obtained using copper K-alpha1 radiation (&lgr;=0.15046 nm) which shows main peaks at 9.28, 10.38, 11.37, 12.40, 16.84, 17.46, 17.53, 17.78, 17.98, 19.48, 20.70, 21.29, 21.45, 22.21, 22.64, 23.08, 25.20 and 25.79. The invention also relates to processes for the preparation of said form, to pharmaceutical compositions containing same and to its use in medicine, particularly the treatment of conditions for which an agonist of 5-HT1 receptors is indicated, for example, migraine.

Abstract: The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of the formula wherein W, R1, R2, R3, A, X′, Y′ and Z′ are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formulae Ia and Ib are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: This invention relates to compounds of Formula I that inhibit the secretion of apolipoprotein B, to pharmaceutical compositions comprising the compounds, and to methods of treating and/or preventing atherosclerosis, obesity, diabetes, hyperlipidemia, hyperliproproteinemia, hypercholesterolemia, hypertriglyceridemia, hypoalphalipoproteinemia, pancreatitis, myocardial infarction, stroke, restenosis, or Syndrome X. This invention also relates to methods of reducing the secretion of apolipoprotein B and/or inhibiting microsomal triglyceride transfer protein.

Abstract: Quantitative analysis speed can be increased at least four-fold via use of liquid phase flow segmentation. An analysis device such as a mass spectrometer 40 is supplied with a single continuous stream 100 consisting of individual segments made from four different chromatographic or flow injection testing streams by use of a timed valve or injector 10. The stream is formed of solution segments A-D of the different compounds, with the compound solution segments being separated by known fluid or solvent segments S. The nature of the individual solution segments is controlled by a high pressure valve which comprises correlated timing elements and selection elements for determining which compounds are being directed to the analysis device at any given time, for correlation to separate analysis results.

Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted; R4 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted; L is absent; and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.

Abstract: The present invention relates to processes for the microbial oxidation of 2-methylquinoxaline to 2-quinoxalinecarboxylic acid which comprise contacting 2-methylquinoxaline with a microorganism, or a suitable mutant thereof, and incubating the resulting mixture under conditions sufficient to yield an amount of said 2-quinoxalinecarboxylic acid. The present processes optionally further comprise the isolation and purification of 2-quinoxalinecarboxylic acid.

Abstract: A method of analysing powder formed as a mixture of pharmaceutical ingredients and derived from a bulk preparation of powder by spectrophotometric analysis utilising transmission measurements. A sample powder is removed from the bulk mixture and pressed into a test wafer and spectrophotometrically analysed for the transmitted beam to provide an assay test spectrum of actual absorption characteristics of ingredients in the material of the wafer. These characteristics of the assay test spectrum are compared with predetermined assay standard spectra determined from individual standard wafers for each relevant ingredient in the powder mixture by measuring absorption characteristics of the individual ingredients from the transmitted beam at known wavelengths of the beam to assess acceptability of the homogenity and distribution of the relevant ingredient in the powder of the sample. The wafer is preferably pressed with flat and parallel opposed end faces through which the beam is directed.

Abstract: Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

Abstract: Compounds of the formula: wherein X represents a single or a double bond; R1 is H or OH; provided that when X is a single bond, R1 is H or OH, and when X is a double bond, R1 is absent; R2 is H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, alkoxy-alkyl or alkylthioalkyl containing from 1 to 6 carbon atoms in each alkyl or alkoxy group, wherein any of said alkyl, alkoxy alkenyl or alkynyl groups may be substituted by one or more halo atoms; or a C3-C8 cycloalkyl or C5-C8 cycloalkenyl group, either of which may be substituted by methylene or one or more C1-C4 alkyl groups or halo atoms; or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may be saturated, or fully or partially unsaturated and which may be substituted by one or more C1-C4 alkyl groups or halo atoms; or a group of the formula SR5 wherein R5 is C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, C5-C8 cycloalkenyl, phenyl or substituted phenyl wherein the substituent is C1-C4 alkyl, C1-C4 alkoxy or

Abstract: The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula wherein R1, R2, R3 and R4 are defined as in the specification, that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system and other disorders.

Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery, improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.