Abstract: This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases, or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses pharmaceutical compositions and methods for treatment of prostaglandin mediated diseases.

Abstract: The invention encompasses compounds represented by formula I: as well as compositions and methods of treatment. The compounds are inhibitors of the PTP-1B enzyme.

Abstract: Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.

Abstract: Substituted benzimidazole derivatives that are NMDA NR2B antagonists are utilized to treat pain.

Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent as the 3-position and an amino moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.

Abstract: Compounds according to Formula (I) or a salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition:

Abstract: Compounds according to Formula (I) or a salt thereof are selective ligands for GABAA receptors useful for treatment of disorders of the central nervous system:

Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Abstract: The present invention is concerned with a novel process for the preparation of 1-(3,5-bis(trifluromethyl)phenyl)ethan-1-one (CAS 30071-93-3). This compound is useful as an intermediate in the synthesis of therapeutic agents.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.

Abstract: A recombinant human neurokinin-3 receptor (hereinafter identified as human NK3R) is disclosed which has been prepared by polymerase chain reaction techniques. Also disclosed is the complete sequence of human NK3R complementary DNA; expression systems, including a CHO (chinese hamster ovarian cell line) stable expression system; and an assay using the CHO expression system. Human NK3R can be used in an assay to identify and evaluate entities that bind to the neurokinin-3 receptor.

Abstract: Disclosed are novel chromophore containing compounds of Formula I and their use in determining interleukin-1&bgr; convertase (ICE) activity. ICE has been implicated in inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes.

Abstract: 9a-Azalides, and pharmaceutical compositions containing them, are useful in the treatment and prevention of bacterial respiratory and enteric infections in livestock animals, particularly in cattle and swine.

Abstract: Substituted or 6,7-ring fused 1,2,3-triazolo[1,5-&agr;]-pyrimidine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system, including anxiety and convulsions.

Abstract: The invention relates to an intact cell assay for direct quantitation of protein tyrosine phosphatase (PTP) activity using the baculovirus expression system. A PTP expressed in transformed host insect cells is processed and localized in their predicted subcellular compartments. Assays are performed on the PTP expressing host cells challenged with a substrate such as, p-nitrophenyl phosphate. This substrate is hydrolysed to p-nitrophenol by expressed phosphatase activity. Emergence of p-nitrophenol is determined spectrophotometrically and is a measure of PTP activity. Further, the assay and transformed host cells of this invention are particularly useful in a screening method for selecting potential inhibitors to PTPs. Basically, transformed host cells are pre-incubated with or without inhibitors and the assay conducted as described. This invention relates to an intact cell assay with a direct readout of PTP activity that is useful in a cell-based screening method for selecting inhibitors of PTPs.

Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep.

Abstract: A method of treatment for enhancing cognition in the treatment of Alzheimer's disease, for example, employs a specific GABAA Alpha5 receptor ligand.

Abstract: Compounds represented by formula I: or a pharmaceutically acceptable salt or hydrate thereof, are disclosed. Pharmaceutical compositions and methods of treatment are also included.