Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.

Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.

Abstract: This invention provides a process for preparing an N-substituted 2-sulfanylimidazole compound of the formula (I) by reacting an isothiocyanate of the formula R1NCS with an &agr;-aminocarbonyl compound of the formula NH2CHR4C(OP)2R3 and an alkyl halide or an activated aryl halide of the formula R2X in a solvent, alternatively, by reacting an isothiocyanate of the formula R1NCS with an &agr;-aminocarbonyl compound of the formula NH2CHR4C(OP)2R3 before adding an alkyl halide of the formula R2X, wherein R1 and R2 independently represent alkyl, heterocyclyl, aryl, or heteroaryl groups; R3 and R4 independently represent hydrogen, alkyl, heterocyclyl, aryl or heteroaryl or may form a non-aromatic ring; P represents a protecting group of a carbonyl group.

Abstract: Clones isolated from phage display libraries that bound to an erythropoietin (EPO) receptor probe are disclosed. Peptides encoded by sequences of those clones that bound to the EPO receptor are disclosed. A 12-mer amino acid consensus sequence, CXXGWVGXCXXW (where X represents one of many amino acids), common to the peptides that bound to the EPO receptor, but unrelated to the primary structure of EPO, is disclosed.

Abstract: Compounds of formula (I) compounds of formula (II) compounds of formula (III) and compounds of formula (IV) or pharmaceutically acceptable salts thereof are useful as H3 receptor antagonists. Processes to make the compounds and methods of treatment using the compounds are also disclosed.

Abstract: The present invention relates to an efficient process for the preparation of 5-(substituted)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno[3,4-f]quinolines.

Abstract: Compounds of formula (I) or therapeutically acceptable salts thereof, are protein tyrosine kinase PTP1B inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.

Abstract: The instant invention relates to compounds of formula I which are useful as antagonists of the glucocorticoid receptor and for treating diabetes in a mammal. In addition, any glucocorticoid receptor antagonist(s) is useful for the treatment of diabetes.

Abstract: Novel 3-pyridyloxymethyl heterocyclic ether compounds of the formula: or the pharmaceutically-acceptable salts or prodrugs thereof are selective and potent ligands at neuronal nicotinic cholinergic channel receptors, and are effective in controlling synaptic transmission. Key intermediates and processes using this key intermediates to produce compounds of formula I with the variables defined in the specification are also described.

Abstract: The present invention relates to a method of controlling pain in mammals, including humans, comprising administering to a mammal or patient in need of treatment thereof selected compounds of formula I: or a pharmaceutically acceptable salt thereof. The invention further relates to selected (R) and (S) compounds of formula I above which are useful as analgesics as well as neuronal cell death preventors and anti-inflammatories.

Abstract: The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.

Abstract: Compounds of formula I are useful for treating type II diabetes, obesity, hyperglycemia, inadequate glucose clearance, hyperinsulinemia, hypertriglyceridemia, and high-circulating glucocorticoid levels, preparations of the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: X-ray crystallography can be used to screen compounds that are not known ligands of a target biomolecule for their ability to bind the target biomolecule. The method includes obtaining a crystal of a target biomolecule; exposing the target biomolecule crystal to one or more test samples; and obtaining an X-ray crystal diffraction pattern to determine whether a ligand/receptor complex is formed. The target is exposed to the test samples by either co-crystallizing a biomolecule in the presence of one or more test samples or soaking the biomolecule crystal in a solution of one or more test samples. In another embodiment, structural information from ligand/receptor complexes are used to design ligands that bind tighter, that bind more specifically, that have better biological activity or that have better safety profile. A further embodiment of the invention comprises identifying or designing biologically-active moieties by the instant process.

Abstract: The present invention relates to a process of coding and identifying individual members of a chemical combinatorial library synthesized on a plurality of solid supports which undergo mix and split synthesis. The process provides for tagging the solid supports with a coding identifier that is attached to the solid support and which can be decoded by infrared or raman spectroscopy when directly attached to the support.

Abstract: The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching “tags” that comprise fluorine containing compounds in combinations and/or ratios. The tags can be decoded while attached to the solid support by fluorine nuclear magnetic resonance spectroscopy to follow the reaction history of individual beads, and to determine the particular member of the library that is attached on the bead.

Abstract: The invention is a catalyst, the use of the catalyst and a method of using the catalyst in the formation of a compound with an amide bond. The catalyst is an HOBT derivative having the following formula (1): ##STR1## where R.sup.1 is a group bearing a positive charge at pH 5-7; where Y is a bond or a substituted or unsubstituted alkylene chain containing 1-10 carbon atoms and 0-2 heteroatoms selected from the group consisting of N, S and O; and where X is a linker group selected from --CO-- or --SO.sub.2 --. In the method, an amine, a carboxylic acid, an amide coupling agent and a catalyst of formula (1) are reacted for a time sufficient to produce an amide bond between the amine and the carboxylic acid. Thereafter, the compound containing the amide bond is isolated.

Abstract: Methods for rapidly generating large rationally designed libraries of structurally-diverse small molecular weight compounds using a multicombinatorial approach.

Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.

Abstract: This invention relates to a combinatorial process for synthesizing a library of azetidinone peptide-like compounds. The compounds are synthesized as mixtures from a common azetidinone intermediate. The compounds are biologically active as inhibitors of the Vasopressin (V1a) receptor.

Abstract: A method for photochemical cleavage of carbon-sulfur bonds in conjunction with solid-phase synthesis utilizing a deoxygenated solvent and light to cleave the carbon-sulfur bond from a heterogeneous support. Also disclosed are compounds for use with said photochemical cleavage and methods of preparing them.