Abstract: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.

Abstract: The present invention provides a unique and highly accurate method for generating molecular arrays of very high density on porous surfaces. The method involves the application of focused acoustic energy to each of a plurality of fluid-containing reservoirs to eject a small fluid droplet—on the order of 1 picoliter or less—from each reservoir to a site on a porous substrate surface. High density molecular arrays are provided as well, in which greater than about 62,500 molecular moieties, serving as array elements, are present on a porous surface. Biomolecular arrays that can be generated using focused acoustic ejection include oligonucleotide arrays and peptidic arrays.

Abstract: The present invention features processes and compositions for producing a metallic-looking image on a substrate having a reflective or luminescent surface. The process utilizes an opaque coating composition containing an opaque coating agent comprising a mixture of a polyacid and a polybase. When applied to a light-emitting, reflective or luminescent substrate, the opaque coating composition at least partially masks the light-emitting reflective or luminescent surface of the substrate, but becomes increasingly translucent or transparent when contacted with a recording liquid such as an ink, revealing the light-emitting, reflective or luminescent surface.

Abstract: The invention provides conjugated polymers that have good solubility and semiconductivity, and that display high photoluminescent and electroluminescent efficiency.

Abstract: Methods, compositions and drug delivery systems are provided for the transdermal administration of a pharmacologically active amine. The active agent is administered with a hydroxide-releasing agent that serves as a permeation enhancer. Exemplary hydroxide-releasing agents are inorganic hydroxides, inorganic oxides, and alkali metal or alkaline earth metal salts of weak acids. Inorganic hydroxides include, for example, ammonium hydroxide, alkali metal hydroxides and alkaline earth metal hydroxides, such as sodium hydroxide, calcium hydroxide, potassium hydroxide, magnesium hydroxide, and the like.

Abstract: Phosphinoamidite carboxylates and analogs are provided that have the structure of formula (I) wherein R1, R2, R3, R4, X, Y, Z and n are as defined herein. The compounds are useful as phosphitylating agents, e.g., in the phosphitylation of 3′ and 5′ hydroxyl groups of nucleosides and oligonucleotides. Also provided are phosphonocarboxylate and H-phosphonite carboxylate analogs of the compounds of formula (I). The compounds enable synthesis of phosphinocarboxylate and phosphonocarboxylate oligonucleotides having reduced internucleotide charge and enhanced nuclease resistance.

Abstract: Methods are provided for enhancing the permeability of skin or mucosal tissue to topical or transdermal application of local anesthetic agents. The methods entail the use of a base in order to increase the flux of the agent through a body surface while minimizing the likelihood of skin damage, irritation or sensitization. The permeation enhancer can be an inorganic or organic base. Compositions and transdermal systems are also described.

Abstract: An orally administrable pharmaceutical formulation is provided that combines, as active agents, a cholesterol-lowering agent, an inhibitor of the renin-angiotensin system, aspirin, and optionally at least one of vitamin B6, B12, and folate; the active agents are each present in a unit dose appropriate for once-daily dosing, and at least one of the active agents is contained in a dosage unit within the dosage form that physically separates it from the other active agents. The formulation is provided as a simple and convenient therapy to reduce the risk of cardiovascular events in individuals who are at elevated cardiovascular risk, including individuals who have systemic lupus erythematosus. The formulation is also therapeutic for individuals during or immediately following an occurrence of acute myocardial infarction.

Abstract: The present invention provides a method and device for the acoustic ejection of fluid droplets from each of a plurality of fluid-containing reservoirs. The droplets are ejected toward sites on a substrate surface for deposition thereon. The device is comprised of: a plurality of reservoirs each adapted to contain a fluid; an ejector comprising a means for generating acoustic radiation and a means for focusing the generated acoustic radiation so as to eject fluid droplets from the reservoir fluids; and a means for positioning the ejector in acoustically coupled relationship to each of the reservoirs. The invention is useful in a number of contexts, particularly in the preparation of biomolecular arrays.

Abstract: Water-dispersible nanoparticles are prepared by applying a coating of a multiply amphipathic dispersant to the surface of a hydrophobic nanoparticle comprised of a semiconductive or metallic material. The multiply amphipathic dispersant has two or more hydrophobic regions and two or more hydrophilic regions, and is typically polymeric. Preferred polymeric dispersants are comprised of (1) a hydrophobic backbone with hydrophilic branches, (2) a hydrophilic backbone with hydrophobic branches, or (3) a backbone that may be either hydrophobic or hydrophilic, and substituted with both hydrophilic and hydrophobic branches. Monodisperse populations of water-dispersible nanoparticles are also provided, as are conjugates of the water-dispersible nanoparticles with affinity molecules such as peptides, oligonucleotides, and the like.

Abstract: A method is provided for increasing the permeability of skin or mucosal tissue to transdermally administered nonsteroidal anti-inflammatory drugs (NSAIDs). The method involves use of a specified amount of a hydroxide-releasing agent, the amount optimized to increase the flux of the NSAID through a body surface while minimizing the likelihood of skin damage, irritation or sensitization. Formulations and drug delivery systems for co-administering a hydroxide-releasing agent with an NSAID are provided as well.

Abstract: Novel pharmaceutical dosage forms provide for pulsatile delivery of an antiarrhythmic agent that releases the drug in spaced apart “pulses.” The dosage forms are comprised of first, second and optional third dosage units, with each dosage unit having a different drug release profile. The dosage forms may comprise capsules housing compressed tablets or drug-containing beads, granules, or particles or may comprise a single tablet with the first, second and optional third dosage units incorporated therein, or a “coated core” dosage form. Methods of treatment using the pharmaceutical dosage forms are provided as well.

Abstract: A process is provided for synthesizing metal salts of perfluorinated polyethers containing at least one carboxylic acid group. The polymeric salts so provided are effective as anti-wetting and corrosion-protective agents. The metal salts of perfluorinated polyether acids may be used to prepare corrosion-protected substrates, including magnetic recording disks and magnetic recording heads.

Abstract: Multi-analyte reference solutions having a stable partial pressure of oxygen (pO2) in zero headspace packaging and methods for preparing such solutions are disclosed. The solutions have long shelf and use lives when stored at room temperature and are packaged in laminated foil containers having low or no oxygen reactivity. Access devices are also disclosed.

Abstract: The present invention features methods for preparing stabilized &agr;-AlH3 and &agr;′-AlH3, compositions containing these alane polymorphs, e.g., energetic compositions such as rocket propellants, and methods for using the novel polymorphs as chemical reducing agents, polymerization catalysts, and as a hydrogen source in fuel cells and batteries. The method produces stabilized alane by treating &agr;-AlH3 with an acidic solution that optionally contains a stabilizing agent such as an electron donor, an electron acceptor, or a compound which coordinates the Al3+ ion.

Abstract: An electrochromatographic device is provided for conducting enantioselective separation of enantiomers. The device is comprised of a conduit containing a monolithic enantioselective separation medium, and may be, for example, a capillary tube or a microchannel in a substrate. The enantioselective separation medium is prepared by copolymerization of (a1) an ionizable chiral monomer or (a2) a chiral monomer and an ionizable comonomer, along with (b) a crosslinking comonomer and (c) a polymerization initiator, in (d) a porogenic solvent. Following ionization, the enantioselective separation medium serves as a charge carrier as well as a chiral separation medium, and further acts as an electroosmotic pump to facilitate the flow of a fluid. The invention also provides methods for preparing the enantioselective separation medium and electrochromatographic devices fabricated therewith.

Abstract: The invention provides a novel method for synthesizing transition metal carbene complexes useful as olefin metathesis catalysts. The method is a convenient one-pot synthesis in which transition metal carbenes are prepared in high yield from readily available starting materials via a dihydrogen complex containing two different anionic ligands, preferably a phosphine and a heteroatom-stabilized carbene. The invention additionally provides a method for synthesizing precursors to carbene ligands useful, inter alia, in the aforementioned one-pot synthesis. The precursors are in the form of trichloromethyl adducts of the formula L1-CCl3, where L1 is a heteroatom-stabilized carbene ligand, and are prepared by contacting an unsaturated, ionized analog of L-CCl3 with a non-nucleophilic base in the presence of chloroform.

Abstract: Novel compounds are provided in the form of nucleoside pyrophosphate and triphosphate analogs. In these analogs, the pyrophosphate or triphosphate group is replaced with a moiety that is isosterically and electronically identical thereto, but is hydrolytically and enzymatically more stable. The compounds are useful as therapeutic agents, e.g., as antiviral agents, anticancer agents, metabolic moderators and the like. The invention also provides pharmaceutical compositions containing a compound of the invention as an active agent, and in addition provides methods of treating disease, including viral infections, cancer, bacterial infections, inflammatory and/or autoimmune diseases, and the like, by administering a compound of the invention to a patient in need of such treatment.

Abstract: Copolymers prepared by radical polymerization of a fluorine-containing aromatic monomer and an acrylate-based comonomer that may or may not be fluorinated. The polymers are useful in lithographic photoresist compositions, particularly chemical amplification resists. In a preferred embodiment, the polymers are substantially transparent to deep ultraviolet (DUV) radiation, i.e., radiation of a wavelength less than 250 nm, including 157 nm and 248 nm radiation, and are thus useful in DUV lithographic photoresist compositions. A method for using the composition to generate resist images on a substrate is also provided, i.e., in the manufacture of integrated circuits or the like.

Abstract: A method and device for generating solid particles using focused acoustic energy are provided. A solution of a compound of interest is provided in a solvent, which may be an aqueous fluid, a nonaqueous fluid, or a supercritical fluid. Focused acoustic energy is used to eject a droplet of the solution, which is then directed into or through an antisolvent that upon admixture with the solution droplet causes the compound in the droplet to precipitate. In a preferred embodiment, the solvent is an aqueous or organic liquid, and the antisolvent is a supercritical fluid.