Abstract: The present invention provides thioalkeneamides of formula (I) which are useful as transketolase inhibitors: wherein R1, R2, R3, R4, R5, R6, Ra-Rd, n and ring A are as defined herein. The present invention also provides pharmaceutical compositions comprising the compounds of formula (I). The invention provides methods for inhibiting transketolase activity, reducing cellular ribose-5-phosphate levels, inhibiting nucleic acid synthesis, inhibiting cell proliferation and tumor cell growth in vitro and in vivo, stimulating apoptosis in tumor cells and treating cancer by administering a compound of formula (I) or a pharmaceutical composition thereof.

Abstract: The present subject matter relates to phenylurea capreomycin derivatives, and to metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present subject matter are useful as antibacterial agents for treating bacterial infections and for treating disorders caused by bacterial infections. The present subject matter also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial infections by administering such compounds. The present subject matter also relates to methods of preparing such compounds.

Abstract: Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, R10, R11 and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: Disclosed are compounds of the formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: Provided are novel cyclosporin analogs, methods for their production, and their use for treating immunoregulatory and respiratory diseases, disorders, and conditions.

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Compounds are provided which may be used to inhibit DPP-IV comprising the formula: wherein the substituents are as described in the specification and claims.

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: Crystals comprising a modified interleukin-1 type 1 receptor (IL-1R1) and one or more modulators of IL-1 activity are described. Methods of identifying potential inhibitors of IL-1 activity are also described. Compositions and methods for the treatment of IL-1 mediated diseases, such as rheumatoid arthritis, osteoarthritis, and other inflammatory conditions, are described.

Abstract: This invention relates to inhibitors of p38, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by p38.

Abstract: Disclosed are compounds of the Formula III and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 R10, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: Disclosed are methods of inhibiting MEK activity, comprising administering to a mammal an effective amount of a compound of Formula I or IV or a solvate or pharmaceutically acceptable salt thereof, wherein R1, R2, R7, R8, R9, R10, W and Y are as defined in the specification. Also disclosed are methods of treating hyperproliferative diseases, such as cancer and inflammation, in mammals, said method comprising administering to a mammal an effective amount of a compound of Formula I or IV.

Abstract: Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, R10, R11 and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: Disclosed are compounds of the Formula (I) and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, R1, R2, R3, and R4 are as defined in the specification. Such compounds are tyrosine phosphatase inhibitors and useful in the treatment or prevention of Type II Diabetes Mellitus.

Abstract: This invention relates to compounds comprising isocyano derivatives tethered to solid supports for use in 3 and 4 component condensation reactions. The invention also relates to methods for synthesizing cyclic derivatives by a 3 and 4 component condensation reaction using the compounds of the invention.

Abstract: Crystals comprising a modified interleukin-1 type 1 receptor (IL-1R1) and one or more modulators of IL-1 activity are described. Methods of identifying potential inhibitors of IL-1 activity are also described. Compositions and methods for the treatment of IL-1 mediated diseases, such as rheumatoid arthritis, osteoarthritis, and other inflammatory conditions, are described.

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B; R1, R2, R3, R4 and R5 are as defined in the specification. Such compounds are tyrosine phosphatase inhibitors and useful in the treatment or prevention of Type II Diabetes Mellitus. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds, a method for treating or preventing Type II Diabetes Mellitus.

Abstract: Disclosed is a process for selectively reducing a nitrile containing organic compound that also contains a sulfone moiety, the nitrile being reduced to a primary amine.

Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.