Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists having the following structure: wherein R1 and R2 are independently chosen from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, and optionally substituted heteroaryl, and R4 is an optionally substituted heteroaryl moiety. The compounds of the invention are useful for treating various disease states, including asthma, chronic obstructive pulmonary disorder, pulmonary inflammation, emphysema, diabetic disorders, inflammatory gastrointestinal tract disorders, immunological/inflammatory disorders, cardiovascular diseases, neurological disorders, and diseases related to angiogenesis.

Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists having the structure of Formula I: which are useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.

Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.

Abstract: Disclosed is a synthesis suitable for large scale manufacture of novel compounds that are partial and full A1 adenosine receptor agonist having the structure of Formula I: wherein R is optionally substituted phenyl, that are useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.

Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.

Abstract: A compliant cantilevered three-dimensional micromold is provided. The compliant cantilevered micromold is suitable for use in the replication of cantilevered microparts and greatly simplifies the replication of such cantilevered parts. The compliant cantilevered micromold may be used to fabricate microparts using casting or electroforming techniques. When the compliant micromold is used to fabricate electroformed cantilevered parts, the micromold will also comprise an electrically conducting base formed by a porous metal substrate that is embedded within the compliant cantilevered micromold. Methods for fabricating the compliant cantilevered micromold as well as methods of replicating cantilevered microparts using the compliant cantilevered micromold are also provided.

Abstract: Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes, and for increasing HDL plasma levels in mammals.

Abstract: Disclosed are novel methods of antagonizing the A1 adenosine receptor in a mammal, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of the formula: wherein R1 is optionally substituted C1-14 alkyl; Y is C1-14 alkylene; and Z is phenyl that is optionally substituted with halo, hydroxy, amino, cyano, or optionally substituted C1-4 alkyl or a pharmaceutically acceptable salt, ester, or prodrug thereof. The A1 adenosine receptors are antagonized in order to treat a disease state is chosen from renal failure, renal dysfunction, nephritis, hypertension, edema, Alzheimers disease, stress, depression, cardiac arrhythmia, restoration of cardiac function, congestive heart failure, diabetes, asthma, respiratory disorders, ischemia-induced injury of the brain, heart and kidney, and diarrhea.

Abstract: Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes, and for increasing HDL plasma levels in mammals.

Abstract: Disclosed are novel A2B adenosine receptor antagonists compounds having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

Abstract: A compound having the formula: wherein: R1 is —X—R1′; in which R1′ is lower alkyl, substituted lower alkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl, or heterocyclic, and X is —NH—; R2 is isopropyl; and R3 is —NR4R5; in which R4 is hydrogen and R5 is lower alkyl substituted with amino or R4 and R5 are both lower alkyl substituted with one, two or three groups chosen from hydroxy and amino, or an acid addition salt or cationic salt thereof. The compounds inhibit CDK-2 activity and are useful for treating disorders characterized by undesirable cell proliferation.

Abstract: Disclosed are novel A2B adenosine receptor antagonists of Formula I: A compound of the formula: wherein: R1 is optionally substituted alkyl or a group —Y—Z, in which Y is a covalent bond or optionally substituted alkylene, and Z is optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted alkenyl or optionally substituted alkynyl, with the proviso that when Y is a covalent bond Z cannot be alkenyl or alkynyl; and X is oxygen, sulfur, or NH—, or a pharmaceutically acceptable salt, ester, or prodrug thereof. The compounds are particularly useful for treating asthma and diabetic retinopathy.

Abstract: A process is provided for use in the conversion of alkanes into alkylene oxides, having particular utility in the conversion of propane to form propylene oxide, using a lanthanide-promoted, supported, silver catalyst prepared via precipitation. A preferred embodiment uses silver nitrate and lanthanum nitrate to form the catalyst on a BaCO3 support.

Abstract: The present invention features novel methods and compositions for coating textile substrates, wherein the coating compositions are composed of a coating agent selected from one of (a) an azetidinium polymer, (b) a guanidine polymer, (c) a mixture of an azetidinium polymer and a guanidine polymer, and (d) a copolymer of an azetidinium monomer and a guanidine monomer. Textile substrates coated with the compositions provide high quality printed images when printed with an ink containing a reactive dye having ionizable and/or nucleophilic groups capable of reacting with the coating agent in the textile coating composition. Images printed on a textile substrate coated with a coating composition of the invention are bleed-resistant, water-resistant (e.g., water-fast), detergent-resistant (e.g., detergent-fast), and/or are characterized by an enhanced chroma and hue.

Abstract: A method is provided for fabricating metallic microstructures, i.e., microcomponents of micron or submicron dimensions. A molding composition is prepared containing an optional binder and nanometer size (1 to 1000 nm in diameter) metallic particles. A mold, such as a lithographically patterned mold, preferably a LIGA or a negative photoresist mold, is filled with the molding composition and compressed. The resulting microstructures are then removed from the mold and the resulting metallic microstructures so provided are then sintered.

Abstract: Oligomers are prepared substantially free of error sequences by sequentially adding monomers to a growing chain bound to a support through a first selectably cleavable linkage, a first capture moiety and a second selectably cleavable linkage. At the completion of monomer addition, the completed oligomer is cleaved from the support to reveal the first capture moiety and purified by virtue of the presence of a second capture moiety, e.g., a terminal blocking group, and the first capture moiety. A support-bound oligomer having the structural formula (I) S—[X1]n1—SC1—CP2—[X2]n2—SC3—T1—X—T2—SC2—CP1  (I) is also provided wherein T1, T2, X1, X2, n1, n2, SC1, SC2, SC3, CP1 and CP2 are as defined herein.

Abstract: Methods are provided for reducing background signals encountered in nucleic acid hybridization assays and other assays that involve hybridization of a labeled oligomer to its complement. The method is premised on the significant reduction of signal generation that occurs when a quenchable dye-labeled oligomer forms a hybrid complex. In addition, a method is provided for enhancing the detectable signal emitted from an amplification multimer hybridized to an oligomer probe to which a quenchable dye has been conjugated through a linker such that the emission from the dye is not quenched upon hybrid complex formation. Novel oligonucleotide probes are also provided that comprise an oligomer to which has been directly or indirectly through a linker a quenchable dye.

Abstract: In the formation of multilevel LIGA microstructures, a preformed sheet of photoresist material, such as polymethylmethacrylate (PMMA) is patterned by exposure through a mask to radiation, such as X-rays, and developed using a developer to remove the exposed photoresist material. A first microstructure is then formed by electroplating metal into the areas from which the photoresist has been removed. Additional levels of microstructure are added to the initial microstructure by covering the first microstructure with a conductive polymer, machining the conductive polymer layer to reveal the surface of the first microstructure, sealing the conductive polymer and surface of the first microstructure with a metal layer, and then forming the second level of structure on top of the first level structure. In such a manner, multiple layers of microstructure can be built up to allow complex cantilevered microstructures to be formed.

Abstract: An antigen-containing formulation is provided, comprising: (a) an antigen; (b) a TH1-inducing adjuvants; and (c) a sparingly soluble amino acid or a derivative thereof. The adjuvants may be, for example, monophosphoryl lipid A, 3′-de-O-acetylated monophosphoryl lipid A, derivatives thereof, or any other adjuvants that enhances an individual's TH response to the antigen. Suitable amino acids include tyrosine, tryptophan, derivatives thereof, and the like. Methods for using the formulation are also provided; in a particularly preferred embodiment, the formulation is used as a vaccine.