Abstract: Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a —CH(R3)N(R2)B—R1 and —OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is an optionally-substituted pyridyl ring and the group R1 is positioned on B in a 1,3 or 1,4 relationship with the —CH(R3)N(R2)B- linking group. R1, R2 and R3 and D can be a number of different organic or halogen moieties. N-oxides of —NR2 and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.

Abstract: Compounds of formula (I) in which all variables are defined in the description and their salts inhibit the enzyme oxido squalene cyclase and are useful in treating hypercholesterolemia and also as anti-fungal agents. Processes for their preparation are also described together with their use in medicine.

Abstract: The invention relates to azolobenzazepine derivatives of the formula I: wherein: X is O or S; R1, R2, R3 and R4 are independently hydrogen, perfluorolower-alkyl, halogen, nitro or cyano; and C together with the carbon atoms to which it is attached forms a 5-membered aromatic heterocycle, to pharmaceutical compositions containing them and to methods for the treatment of neurological disorders utilizing them.

Abstract: Stable aqueous dispersions of 1,2-benzisothiazolin-3-one containing Xanthan gum which is substantially free from organic solvents.

Abstract: The invention provides an improved process for preparing compounds of formula (I)

Abstract: The invention relates to heterocyclic derivatives of the formula (I): A—B—X1—T1(R2)—L1—T2(R3)—X2—Q or pharmaceutically acceptable salts thereof, which possess antithrombotic and anticoagulant properties due to their inhibition of Factor Xa and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.

Abstract: An isolated and purified human Ste20-like serine/threonine signal transduction kinase is described. A cDNA sequence which encodes the native signal transduction molecule is disclosed as well as the structural coding region and the amino acid residue sequence. Methods are provided which employ the sequences to identify compounds that modulate the biological and/or pharmacological activity of the transduction molecule and hence regulate cell physiology. Biologically-effective antisense molecules, as well as dominant negative mutant versions of the biomolecule are described which are suitable for therapeutic use. The invention is also drawn toward the diagnosis, prevention, and treatment of pathophysiological disorders mediated by the signal transduction molecule.

Abstract: The invention relates to compounds of formula (I) and salts thereof as further defined herein, wherein ring Z is a 6-membered heterocyclic ring containing 1 to 3 nitrogen atoms, and the use of such compounds and salts to inhibit the effects of VEGF and FGF, and in the treatment of a number of disease states including cancer and rheumatoid arthritis.

Abstract: A process for producing an image on a substrate comprising printing an ink onto the substrate, characterized in that the ink contains a reactive dye, the substrate is an acid paper and the printing is performed by an ink jet printer. Also claimed is an acid paper printed by means of the process.

Abstract: The invention relates to quinazoline derivatives of formula (I) (wherein: R1 represents hydrogen or methoxy; R2 represents methoxy, ethoxy, 2-methoxyethoxy, 3-methoxypropoxy, 2-ethoxyethoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, 2-hydroxyethoxy, 3-hydroxypropoxy, 2-(N,N-dimethylamino)ethoxy, 3-(N,N-dimethylamino)propoxy, 2-morpholinoethoxy, 3-morpholinopropoxy, 4-morpholinobutoxy, 2-piperidinoethoxy, 3-piperidinopropoxy, 4-piperidinobutoxy, 2-(piperazin-1-yl)ethoxy, 3-(piperazin-1-yl)propoxy, 4-(piperazin-1-yl)butoxy, 2-(4-methylpiperazin-1-yl)ethoxy, 3-(4methylpiperazin-1-yl)propoxy or 4-(4-methylpiperazin-1-yl)butoxy; the phenyl group bearing (R3)2 is selected from: 2-fluoro-5-hydroxyphenyl, 4-bromo-2-fluorophenyl, 2,4-difluorophenyl, 4-chloro-2-fluorophenyl, 2-fluoro-4-methylphenyl, 2-fluoro-4-methoxyphenyl, 4-bromo-3-hydroxyphenyl, 4-fluoro-3-hydroxyphenyl, 4-chloro-3-hydroxyphenyl, 3-hydroxy-4-methylphenyl, 3-hydroxy-4-methoxyphenyl and 4-cyano-2-fluorophenyl); and salts thereof, processes for their p

Abstract: A compound of formula (I): or a salt, enamine or the like, acylate, sulphonate, carbamate or ether derivative thereof; wherein X, X1 and X2 are independently oxygen or sulphur, R1 is an optionally substituted heterocyclic or cycloalkyl group, and Y is an optionally substituted C2-C4 alkylene group which is optionally interposed by an oxygen atom, a group a group or an optionally mono-substituted nitrogen atom, wherein p is 0, 1 or 2, s is 0 or 1 and Rb is alkyl or alkoxy; provided that when X, X1 and X2 are oxygen, R1 is not pyridyl or pyrimidinyl. Processes for the preparation of these compounds and herbicidal compositions containing them are also described and claimed.

Abstract: A method for the preparation of a fluorescence resonance energy transfer (FRET) substrate having donor and acceptor species on opposite sides of a proteolytic cleavage site and wherein the donor and/or acceptor species are attached via the side chain(s) of amino acid(s) therein. The method comprises contacting a reactive donor or acceptor species with a polypeptide substrate having the side chain(s) of amino acid(s) therein adapted for reaction with the reactive species and then contacting the substrate so obtained with a corresponding reactive donor or acceptor species. Novel FRET substrates so prepared and their use in assays to identify modulators of protease activity.

Abstract: Azo dyes of Formula (1) have utility as dyes for ink-jet printing, where Formula (1) represents: which comprises any suitable form of the compound: such as salt; stereoisomer, zwitterion, polymorph, complex, isotopic form, combinations thereof in the same species and mixtures thereof; where: n represents from 1 to 5 inclusive; R1, R1B, R4 and R4B each independently comprises at least one of the following substituents, optionally substituted: H, C1-8alkyl; C1-8,alkoxy; —NHCOH, C1-8alkylcarbonylamino; and —NHCONR5R6 where R5 and R6 each independently comprises at least one of the following substituents: H, C1-8alkyl and aryl; and R2 and R3 each independently comprises at least one of the following substituents, optionally substituted: H; C1-8alkoxy; -NHC1-8alkyleneOH, —SC1-8-alkyleneSO3H; -NHC1-8alkyleneN(C1-8alkyl)2; where X comprises one of the following: —NHC1-8alkylene; —NHphenylSO2NHC1-8alkylene; and a direct link,

Abstract: The invention provides a compound of formula (I): wherein A is CH═CH; Ar is an optionally substituted 5-membered heterocyclic ring system containing from 1 to 3 heteroatoms individually selected from nitrogen, oxygen and sulfur atoms, and at least one unsaturation (double bond) between adjacent atoms in the ring, said heterocyclic ring being optionally fused to a benzene ring, and R′ is hydrogen, cyano, hydroxy, alkyl, alkoxy, amino, nitro, isocyanato, acylamino, hydroxyalkyl, optionally substituted heteroaryl, alkoxyalkyl, haloalkyl, halohydroxyalkyl, aralkyloxyalkyl, acyloxyalkyl, amidoximido, sulfonyloxyalkyl, aminoalkyl, alkoxycarbonylamino, acylaminoalkyl, cyanoalkyl, imino, formyl, acyl or carboxylic acid or an ester or amide thereof, or alkenyl or alkynyl either of which is optionally substituted by halogen, alkoxy, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or cyano; or an acid addition salt, quaternary ammonium salt or N-oxide derived there

Abstract: The invention concerns pharmaceutically useful indoles of formula (I), in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, as well as pharmaceutical compositions containing them. The novel compounds possess inhibitory activity against monocyte chemoattractant protein-1 (MCP-1). The invention further concerns the use of such indoles in the treatment of a disease or condition mediated by MCP-1.

Abstract: Azo dyes of Formula (1) have utility as dyes for ink-jet printing where Formula (1) represents: which comprises any suitable form of the compound: such as salt; stereoisomer, zwitterion, polymorph, complex, isotopic form, combinations thereof in the same species and mixtures thereof; where: p represents from 1 to 7 inclusive; the napthyl moiety may be optionally substituted; R1 comprises at least one of the following substituents, optionally substituted: H, C1-4-alkyl, NHCOC1-4 alkyl, C1-4 alkoxy, NHCOaryl, NHSO2C1-4 alkyl, NHSO2aryl, NHCONR3R4 where R3 and R4 each independently comprises H, C1-4alkyl or aryl; R2 comprises H, C1-4 alkyl or C1-4 alkoxy; L1 and L2 each independently comprises at least one of the following substituents, optionally substituted: —NH2, —NHC1-4 alkyleneOH, —SC1-4alkylene —SO3H, —NHC1-4alkyleneN(C1-4alkyl)2, —N(C1-4alkyleneOH)2, —NHC1-4alkyleneSO3H, —NHC1-4alkylene(CO2H)n where n is 1, 2 or 3, —SC1-4alkyl

Abstract: A composition for use in extracting metals from aqueous solutions of metals salts comprises at least one o-hydroxyaryloxime containing at least 5 aliphatic or alicyclic carbon atoms and at least one ester containing from 10 to 30 carbon atoms, the weight ratio of o-hydroxyaryloximes to the esters being in the range of 10:1 to 1:3. A process for extracting metal from aqueous solutions using the composition is also disclosed.

Abstract: An anti-CEA monoclonal antibody, designated 806.077, of murine origin is useful for the diagnosis and therapy of cancer. The antibody complementarity determining regions have the following sequences: heavy chain CDR1 DNYMH, CDR2 WIDPENGDTE YAPKFRG, CDR3 LIYAGYLAMD Y; and light chain CDR1 SASSSVTYMH, CDR2 STSNLAS, CDR3 QQRSTYPLT. The antibody optionally is humanized and can be in the form of a conjugate with either an enzyme, such as carboxypeptidase, or a co-stimulatory molecule such as the extracellular domain of human B7.1.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalysed reactions.

Abstract: Biocidal proteins isolated from seeds have been characterized, in particular proteins isolated from members of the Brassicaceae, Compositae and Leguminosae families including Raphanus, Brassica, Sinapis, Arabidopsis, Dahlia, Cnicus, Lathyrus and Clitoria. The proteins show a wide range of antifungal activity and some are active against Gram-positive bacteria. All share a common amino acid sequence. DNA encoding the proteins has been isolated and incorporated into vectors. Plants transformed with this DNA may be produced. The proteins find commercial application as antifungal or antibacterial agents; transformed plants will show increased disease-resistance.