Abstract: This invention relates to nicotinamide derivatives of general formula (I): in which R1, X, Y, Z and R2 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.

Abstract: This invention relates to certain ?-amino acids that bind to the alpha-2-delta (?2?) subunit of a calcium channel. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders.

Abstract: This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing hyperlipidemia and hypercholesteremia in a mammal. The present invention also discloses method for making the disclosed compounds.

Abstract: A hematopoetic factor called “colony stimulating factor” (CSF) is capable of synergizing the attracting capabilities of chemokines and of inducing the accumulation and/or activation in vitro and in vivo of key components of inflammatory responses. Various types of agents that inhibit or otherwise hinder the production, release or activity of CSF could be used therapeutically in the treatment of ischemia and other inflammatory diseases, such as autoimmune disease, and various chronic inflammatory diseases such as rheumatoid arthritis and psoriasis.

Abstract: A method for preparing 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide (I), a key intermediate in the synthesis of atorvastatin calcium, is described

Abstract: Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I): including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) R1 and R2 are independently selected from H, Me or OMe.

Abstract: A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: The compounds of formula (I) are useful in the treatment of faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, neuropathic pain, neuropathological disorders and sleep disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.

Abstract: This invention relates to novel cyclopropyl ?-amino acids derivatives of the formula wherein R1 through R4 are defined as in the specification, pharmaceutical compositions containing them and their use for the treatment of various central nervous system and other disorders. The cyclopropyl ?-amino acids derivatives of this invention exhibit activity as alpha2delta ligands (?2? ligands). Such compounds have affinity for the ?2? subunit of a calcium channel.

Abstract: The invention relates to a method of treating tinnitus by administering an alpha2delta ligand such as, for example, a compound of Formula and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or straight or branched lower alkyl, and n is an integer of from 4 to 6.

Abstract: In accordance with the present invention, there is provided pregabalin lactose conjugate compounds. Also provided as part of the present invention is a novel method of central nervous system disorders or diseases including seizure disorders, pain, depression, anxiety, sleep disorders, consumptive disorders, psychosis, tardive dyskinesia, Huntington's disease, or Parkinson's disease in a subject by administering to the subject a pharmaceutically effective amount of a pregabalin lactose conjugate.

Abstract: There is provided a pharmaceutical composition for therapeutic or prophylactic administration to a subject having an infective disease or condition or at risk thereof. The composition comprises an aqueous carrier having in solution therein (a) an oxazolidinone antimicrobial drug, for example linezolid, in a therapeutically or prophylactically effective drug concentration that is above the practical limit of solubility of the drug in a substantially isotonic aqueous solution at a physiologically compatible pH, and (b) a pharmaceutically acceptable cyclodextrin compound in a concentration sufficient to maintain the drug in solution at such a drug concentration. The composition is particularly useful for intravenous delivery of the drug.

Abstract: An assay and method for selecting analogs and derivatives of gabapentin based on the compounds inhibitory activity toward MAP kinase and MAP kinase mediated reporter gene expression. The method includes the steps of activating the MAP kinase signaling pathway, detecting the MAP kinase signal, and screening the gabapentin analogs and derivatives for inhibitory activity against the MAP kinase signal.

Abstract: A method for screening chemical compounds for electrophilic properties comprising the steps of: (a) providing an assay having one or more reaction vessels; (b) adding a predetermined amount of separate chemical compounds for screening to each reaction vessel; (c) adding a predetermined amount of a surrogate chemical marker to each reaction vessel and allowing said separate chemical compounds and surrogate chemical marker to incubate for a period of time; (d) adding a reactive chemical to each reaction vessel which is capable of reacting with residual surrogate chemical marker such that the amount of residual surrogate chemical marker present after step (c) can be quantitatively or qualitatively measured; and (e) quantitatively or qualitatively measuring said residual chemical marker is provided.

Abstract: A composition comprising: (a) a pharmaceutically effective amount of reboxetine; and selected from the group consisting of clozapine, olanzapine, risperidone and mixtures thereof (b) a pharmaceutically effective amount of one or more neuroleptic agents or a pharmaceutically effective salt thereof is provided.

Abstract: The invention relates to a method of preparing compounds of the formula and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.

Abstract: The present invention provides an improved process for the preparation of ?-polymorphic eletriptan hydrobromide.

Abstract: The present invention is concerned with the acylation of indoles, specifically the preparation of 3-acylated indoles which may be further treated to provide indoles having an alternative substituent at the 3-position.

Abstract: The present invention provides compounds of formula (I) wherein R, Z, Y, W, R5, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.

Abstract: The present invention are substituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (X) and unsubstituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (XI) such as the compound of EXAMPLE 13 which are useful in treating depression, obesity and other CNS disorders.