Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.

Abstract: Disclosed are a novel phosphorylating reagent and related methods. Specifically disclosed is a compound represented by general formula (A). In the formula, WG1 and WG2 independently represent a cyano group, a nitro group, a halogen atom, an alkylsulfonyl group or an arylsulfonyl group; X1, X2, X3 and X4 independently represent CR or N; and R represents H, a methyl group, a halogen atom, a trifluoromethyl group, a cyano group, a nitro group, an alkoxycarbonyl group, a carbamoyl group, a monoalkylcarbamoyl group, a dialkylcarbamoyl group, a sulfamoyl group, a monoalkylsulfamoyl group, a dialkylsulfamoyl group, or an alkylsulfonyl group.

Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.

Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.

Abstract: The present invention relates in particular to novel chemical compounds, particularly to novel organophosphorus derivatives of indazoles, to the compositions containing them, and to the use thereof as medicinal products for treating cancers.

Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.

Abstract: The invention relates a compound represented by the formula (1): Q1-Q2-C(?O)—N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.

Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo [1,2-&agr;]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.

Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-a]imidazol-2-one (1): 1

Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infrections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: A bisphosphite compound of the following formula (A): ##STR1## wherein --Ar--Ar-- is a bisarylene group represented by any one of the formulae (A-I) to (A-III) defined in the specification, and each of Z.sub.1 to Z.sub.4 is a C.sub.4-20 aromatic or heteroaromatic group which may have a substituent, wherein each of substituents on carbon atoms of an aromatic ring adjacent to the carbon atom bonded to the oxygen atom in each of Z.sub.1 to Z.sub.4, is a C.sub.0-2 group, and each pair of Z.sub.1 and Z.sub.2, and Z.sub.3 and Z.sub.4, are not bonded to each other.

Abstract: A phenylalkyl derivative of the formula ##STR1## wherein R.sub.a to R.sub.f, A and B are substituents and n is the number 0 or 1.These phenylalkyl derivatives possess angiotensin antagonist activity.

Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## The new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) have a particularly pronounced activity against animal pests, in particular against insects and arachnids, and against weeds.

Abstract: Novel benzothiazole derivatives having a fluorescence inhibiting group linked by an enzyme cleavable bond and methods for their synthesis are provided. Upon cleavage of the enzyme-cleavable bond, a strongly fluorescent reaction product is produced. These compounds may be used to detect enzymatic activity. The fluorescent reaction products are detectable at an attomolar level using a fluorometer.

Abstract: Substituted imidazoles such as ##STR1## which are useful as angiotensin II receptor inhibitors. These compounds have activity in treating hypertension and congestive heart failure.

Abstract: A phosphorylating agent represented by the following general formula [1]: ##STR1## wherein R represents a protective group of the phosphoric acid; and X represents a heterocyclic residue represented by the following general formula [2]: ##STR2## wherein Y represents a single bond or an oxygen or sulfur atom; Z represents a heterocyclic nucleus comprising at least one nitrogen atom as a ring-forming element and may be condensed with another aromatic ring; and W represents one or more substituents other than a hydrogen atom. The phosphorylating agent is stable, can rapidly proceed phosphodiester bond-forming reactions in good selectivity under mild conditions and thus makes it possible to perform a reaction even in a relatively large scale.

Abstract: Insecticidal, acaricidal and herbicidal polycyclic 3-aryl-pyrrolidine-2,4-dione derivatives of the formula ##STR1## in which A represents the radical of a bi-, tri- or polycyclic system which is optionally interrupted by further hetero atoms or groups of hetero atoms,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number from 0-3, andG represents hydrogen or various organic radicals.

Abstract: The object of the invention consists of D-luciferin derivatives of General Formula (I) ##STR1## wherein R.sup.1 =OH, alkoxy, alkenyloxy, amino acid, NH.sub.2 or oligopeptide andR.sup.2 =H; H.sub.2 PO.sub.3 --; HSO.sub.3 --; alkyl or alkenyl, optionally substituted by phenyl; aryl; ##STR2## with R.sup.3 =alkyl or alkenyl, optionally substituted by phenyl; mono- or disaccharide or nucleotide.An object of the invention is further the use of said luciferin derivatives for the detection of ligands in the determination of biochemical substances, in particular in enzyme immuno assays, in blot processes and in nucleic acid hybridization. These ligands are attached to an enzyme (enzyme conjugate). In the process, for example an antigen, a hapten or an antibody is conjugated with an enzyme. The enzyme conjugate is capable of releasing luciferin from the luciferin derivative. The luciferin released is reacted with luciferase. The amount of light emitted in the process is determined.

Abstract: Triggerable dioxetanes with a fluorescent molecule containing group bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.

Abstract: In the preparation of a (thiono)phosphoric ester of the formula ##STR1## in which X represents oxygen or sulphur,R and R.sup.1 are identical or different and represent alkyl, andR.sup.2 represents optionally substituted aryl or represents optionally substituted hetaryl having at least one nitrogen atom,wherein a hydroxyl derivative of the formulaR.sup.2 --OHor an ammonium, alkali metal or alkaline earth metal salt thereof is reacted with a (thiono)phosphoric halide of the formula ##STR2## in which Hal represents halogen,the improvement which comprises effecting the reaction in the presence of a bicyclic organic amine as catalyst. Advantageously the reaction is effected in a diluent in the presence of potassium carbonate as an acid acceptor at 20.degree. to 100.degree. C., and 0.8 to 1.5 mols of the halide and 0.005 to 0.5 mol of 1,4-diazabicayclo-(2,2,2)-octane are used as bicyclic organic amine per mol of the hydroxyl compound.

Abstract: Phenanthroimidazole compounds, a process for their preparation, photopolymerizable coating and recording materials and lithographic layers produced using these.The novel phenanthroimidazole compounds are useful as photoinitiators for photopolymerizable coating and recording materials.

Abstract: The invention relates to phosphorylating agents containing at least one protected hydroxyl group and at least one leaving group. According to the invention, a methylsulphonylethyl group (Mse) is used as the hydroxyl protecting group. Typical examples of such phosphorylating agents are the compounds (MseO).sub.2 POL, (MseO)POLL', (MseO).sub.2 PL and (MseO)PLL', in which L and L' are leaving groups. The invention also relates to processes for preparing these phosphorylating agents and processes for the phosphorylation of organic hydroxyl or amine compounds, in particular nucleosides and (poly)nucleotides.

Abstract: This invention relates to novel benzodiimidazole diols and diones and their ability to sensitize hypoxic cells to radiation, thus demonstrating utility for enhancing the treatment of solid tumors by radiation in a subject in need of such treatment.

Abstract: The invention relates to new phosphorylating agents, a process for producing said compounds and their use in a process for the phosphorylation of organic hydroxyl compounds to obtain intermediate products useful for the production of polynucleotides. The phosphorylation is achieved without side reactions at the purine- or pyrimidine bases.

Abstract: Novel phosphates of 6(or 5)-hydroxy-2-benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions include drops and inserts.