Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: The present invention is directed to novel amide-containing compounds which have an improved solubility and a method of improving the solubility of amide-containing compounds. The amide-containing compounds include oxazolidinone compounds and the bioavailability of these oxazolidinone compounds is improved by improving the solubility thereof.

Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases

Abstract: The present invention provides the enzyme and enzymatic procedures for cleaving the ? secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cell and cell isolates and assays. The invention further provides a modified APP protein and associated nucleic acids, peptides, vectors, cells, and cell isolates, and assays that are particularly useful for identifying candidate therapeutics for treatment or prevention of Alzheimer's disease.

Abstract: The present invention relates to a method of assaying modulators of the interaction between Wolframin protein and its identified cellular binding partner.

Abstract: Compounds which are 2-amino-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C1–C8 alkyl, C2–C6 alkenyl or C2–C6 alkynyl; ii) C3–C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R1 is an optionally further substituted group selected from: i) straight or branched C1–C8 alkyl or C2–C6 alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

Abstract: Compounds which are 3-amino-pyrazole derivatives represented by formula (I) wherein R is C3–C6 cycloalkyl group optionally substituted by a straight or branched C1–C6 alkyl or arylalkyl group; R1 is a straight or branched C1–C6 alkyl, C2–C4 alkenyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl or arylalkenyl group, each of which may be optionally further substituted as indicated in the description; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.

Abstract: The present invention discloses radioligands of 9-arylsulfone of the formula (X) or a pharmaceutically acceptable salt or enantiomer thereof, which are useful in diagnosing depression, obesity and other CNS disorders.

Abstract: The present invention provides compounds of Formula (I): wherein R1, R2, R3, R4, R5, R6 and --- have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are useful as 5-HT ligands.

Abstract: The invention provides pyrido[2,3-d]pyrimidin-7(8H)-one telomerase inhibitors of the formula where R1, R2 are as defined herein. The invention also provides methods for preparing the compounds of formula I, methods of using the compounds to treat diseases such as cancer, and pharmaceutical compositions comprising the compounds.

Abstract: The present invention provides antibacterial agents of formula I described herein and intermediates for their preparation.

Abstract: The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: According to the invention there is provided a sterile, pyrogen-free, ready-to-use solution of an anthracycline glycoside, especially doxorubicin, which consists essentially of a physiologically acceptable salt of an anthracycline glycoside dissolved in a physiologically acceptable solvent therefor, which has not been reconstituted from a lyophilizate and which has a pH of from 2.5 to 6.5. The solution of the invention is particularly advantageous for the administration by injection of the anthracycline glycoside drugs. e.g. doxorubicin, in the treatment of both human and animal tumors.

Abstract: The present invention concerns novel pharmaceutically active compounds, pharmaceutical compositions containing the same, the compounds for use as medicaments, and use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are pharmaceutically acceptable salts of tolterodine or hydroxytolterodine, wherein the salt is of an acid selected from the group consisting of aliphatic mono- and dicarboxylic acids comprising from 7 to 24 carbon atoms, alkanedisulfonic acids comprising from 2 to 4 carbon atoms, naphthoic acid derivatives comprising from 11 to 27 carbon atoms, maleic acid and fumaric acid.

Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

Abstract: The present invention provides materials and methods for predicting the in vivo toxicity of a given compound. For example, the invention comprises conducting at least three distinct assays in parallel to provide information about three distinct parameters of cytotoxicity of a chemical in a given target cell, which information is useful for predicting in vivo cytotoxicity.

Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.

Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.

Abstract: An unliganded form of Staphylococcus aureus NAD synthetase (S. aureus NadE) has been crystallized, and the three-dimensional x-ray crystal structure has been solved to 2.3 ? resolution. The x-ray crystal structure is useful for solving the structure of other molecules or molecular complexes, and designing inhibitors of S. aureus NadE activity.