Abstract: The present invention provides compounds having the formula: wherein R1, R2, X1, X2, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases.

Abstract: The present invention provides compounds having the formula: wherein R1, R2, X1, X2, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases.

Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.

Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.

Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof; wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof; and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

Abstract: The present invention relates to methods for identifying compounds that modulate enzymatic activity by contacting covalently bonded PTP-extender complexes or modified covalently bonded PTP-extender complexes with ligand candidates.

Abstract: The invention concerns the identification of protein kinase inhibitors that preferentially bind to the inactive conformation of a target protein kinase. The inhibitors are identified by locking the target protein kinase in an inactive conformation, and using a covalent tethering approach to identify inhibitors preferentially targeting the inactive conformation.

Abstract: The present invention provides compounds having formula (I): wherein R?, R0, R1, X1, R2, R3, R3?, X2, X3 and R4 are as defined herein, and pharmaceutical compositions thereof. The present invention also provides methods of inhibiting proteases, more specifically aspartyl proteases. In certain embodiments, compounds inhibit BACE (?-site APP-cleaving enzyme), and thus are useful in the treatment or prevention of a disease characterized by ?-amyloid deposits in the brain (including, but not limited to, Alzheimer's Disease). The present invention also provides methods for preparing compounds of the invention.

Abstract: In one aspect, the present invention provides a process for producing a sodium salt of an immunosupressant of Formula I

Abstract: The present invention provides compounds having the formula: wherein R1, R?, R2, R3, R3?, R4, X1, X2 and X3 are as defined herein, and pharmaceutical compositions thereof. The present invention also provides methods of inhibiting proteases, more specifically aspartyl proteases. In certain embodiments, compounds inhibit BACE (?-site APP-cleaving enzyme), and thus are useful in the treatment or prevention of a disease characterized by ?-amyloid deposits in the brain (including, but not limited to, Alzheimer's Disease). The present invention also provides methods for preparing compounds of the invention.

Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: wherein: R1 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; L is a linker; R2 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; and or single stereoisomers, mixtures of stereoisomers, or the pharmaceutically acceptable salts, amides, or esters thereof.

Abstract: The present invention provides novel methods for ligand discovery. The inventive methods rely on a process termed “tethering” where potential ligands are covalently bonded or “tethered” to a target and subsequently identified.

Abstract: The invention concerns a method for rapid identification and characterization of binding partners for a target molecule, and for providing binding partners with improved binding affinity. More specifically, the invention concerns an improved tethering method for the rapid identification of at least two binding partners that bind near one another to a target molecule.

Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein A, B, D, E, G, J, n, and R1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof as caspase inhibitors and for the treatment of disorders caused by excessive apoptotic activity.

Abstract: The present invention is directed to novel methods for rapidly and unambiguously identifying small organic molecule ligands for binding to biological target molecules. Small organic molecule ligands identified according to the methods of the present invention may find use, for example, as novel therapeutic drug lead compounds, enzyme inhibitors, labeling compounds, diagnostic reagents, affinity reagents for protein purification, and the like. Also presented are novel methods for identifying high affinity binding ligands for a biological target molecule of interest, wherein those methods comprise linking two or more small organic molecule ligands previously identified as being capable of binding to the biological target molecule of interest. Biological target molecules include, for example, polypeptides, nucleic acids, carbohydrates, nucleoproteins, glycoproteins, glycolipids and lipoproteins.

Abstract: Compounds of formulae I and I′, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are antagonists of IL-2/IL-2R binding; and are useful for the treatment of interleukin-2 mediated diseases, such as autoimmune diseases (such as rheumatoid arthritis, multiple sclerosis, uveitis, and psoriasis), allograft rejection, and graft-versus-host disease.

Abstract: The present invention relates to a new and improved method for treating diabetes and or its associated complications by modulating the activity of protein tryosin phosphatase 1B (“PTP-1B”). The inventive compounds modulate the activity PTP-1B by binding to a novel binding site referred herein as the PTP-1B exosite that is distal to the active site of PTP-1B. The present invention also relates to a new and improved method of treating immune system disorders by modulating the activity of T-cell protein tyrosine phosphatase (“TC-PTP”). The inventive compound modulate the activity of TC-PTP by binding to a novel binding site referred herein as the TC-PTP exosite that is distal to the active site of PTP-1B.

Abstract: Triphenyl compounds of the formulae I, II, and VI: methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are compounds are interleukin-4 antagonists; and are useful for the treatment of asthma and allergies.

Abstract: The present invention is directed to novel methods for rapidly and unambiguously identifying small organic molecule ligands for binding to biological target molecules. Small organic molecule ligands identified according to the methods of the present invention may find use, for example, as novel therapeutic drug lead compounds, enzyme inhibitors, labeling compounds, diagnostic reagents, affinity reagents for protein purification, and the like. Also presented are novel methods for identifying high affinity binding ligands for a biological target molecule of interest, wherein those methods comprise linking two or more small organic molecule ligands previously identified as being capable of binding to the biological target molecule of interest. Biological target molecules include, for example, polypeptides, nucleic acids, carbohydrates, nucleoproteins, glycoproteins, glycolipids and lipoproteins.