Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1

Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.

Abstract: Bradykinin B1-receptor antagonists of formula 1

Abstract: A high-throughput molecular docking facility is presented for screening combinatorial libraries to identity binding ligands and ultimately pharmaceutical compounds. The facility employs a pre-coking conformational search to generate multiple solution conformations of a ligand. The molecular docking facility includes: generating a binding site image of the target molecule, the binding site image to atoms in at least one solution conformation of the multiple solution conformations of the ligand to obtain at least one ligand postion relative to the target molecule in a ligand-target molecule complex formation; and optimizing the at least one ligand position while allowing translation, orientation and rotatable bonds of the ligand to vary, and while holding the target molecule fixed. Docking results are clustered using as a metric the rms deviation between the core of two docked molecules.

Abstract: A method for identifying a solid support in combinatorial synthesis or determining the structure of a compound in combinatorial synthesis. The method involves attaching, detaching and identifying at least one tag by detaching the tag from the solid support and reacting the detached tag with a fluoroalkanoyl acid or its alcohol-reactive equivalent.

Abstract: A multi-channel fluid dispenser includes a reservoir (106) with multiple internal chambers (844) with ports (850) to fill each chamber (844), a multi-channel liquid dispensing head, a plurality of fluid-delivery conduits, and support and positioning elements.

Abstract: Compounds that selectively inhibit inappropriate kinase activities and methods for their preparation are disclosed.

Abstract: A magnetically recordable label embedded within a plastic object such as a microtiter plate. The label comprises a magnetic recording medium such as a recording wire, and is concealed within the object or within a sealed enclosure attached to the object. The label can be written to or read from by a recording head passing adjacent to the label. Because the label is completely enclosed, it is shielded from degrading effects that may be present in the environment.

Abstract: Molecules are represented as one dimensional strings of atoms having a linear position and a width. One dimensional representations are compared to assess the likelihood of similarity in chemical behavior.

Abstract: A hand-held, single-channel dispenser/aspirator is disclosed. The present dispenser/aspirator comprises a body portion for gripping the dispenser and a head portion. In some embodiments, the head portion includes a valve, a liquid conduit and a removable liquid reservoir. The liquid conduit places the liquid reservoir and the dispensing valve in fluid communication. A gas conduit received by the body portion of the dispenser is operable to pressurize the fluid reservoir, or draw a partial vacuum therein. Controls located on the body portion operate the dispenser. The liquid reservoir is advantageously disposed near the valve, so that a relatively short length of liquid conduit is required to operatively connect the reservoir and the dispensing valve, thereby improving the accuracy of the dispensing operation.

Abstract: The polar surface area of molecules is computed without reference to three dimensional molecular structures using a linear equation incorporating counts of nitrogens, oxygens, and related atom clusters. Methods and systems for predicting intestinal absorption of candidate compounds use the polar surface area and the octanol/water partition coefficient as descriptors.

Abstract: In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor.

Abstract: In one embodiment, a particle-retrieval device in accordance with the present teachings includes a receiver tube, vacuum-flow providing means and particle-disengaging means. The receiver tube is in fluid communication with the vacuum-flow providing means such that when flow is introduced into the vacuum-flow providing means, a suction or vacuum flow is developed at an end of the receiver tube. The suction causes a particle to adhere to the end of the receiver. A particle is disengaged by discontinuing the suction and, advantageously, by wetting the engaged particle.

Abstract: A method for photoeluting photocleavable linker-attached chemical compounds, and an apparatus suitable for implementing the method, are disclosed. According to the method, photocleavable linker-attached library compounds are photoeluted from solid support media under conditions of controlled light exposure and controlled temperature. An apparatus suitable for carrying out the present photoelution method includes means for substantially evenly illuminating the photocleavable linker, means for controlling illumination time and intensity, and means for controlling sample temperature.

Abstract: The genes for bradykinin B1 receptor from five mammalian species, vervet monkey, rhesus macaque, tree shrew, dog and pig have been cloned and characterized. In addition to the delineation of the nucleotide and amino acid sequences, methods for identifying modulators of bradykinin B1 receptor activity using these molecules is also described. Additionally, a method for identifying an animal model useful in the screening of potential therapeutic agents is provided.

Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.

Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or &agr;-hydroxyamide group and Z is an acyl or &agr;-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.