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 D-arabinitol dehydrogenase enzyme is disclosed. The enzyme is capable of catalyzing the oxidation of D-arabinitol and substantially incapable of catalyzing the oxidation of D-mannitol and is substantially free of other enzymes capable of oxidizing D-mannitol. Also disclosed are methods for determining D-arabinitol. In one embodiment the method comprises the steps of providing in combination (1) a medium suspected of containing D-arabinitol and (2) a D-arabinitol dehydrogenase enzyme and examining the medium for the product of the oxidation of the D-arabinitol. The enzyme utilized is capable of catalyzing the oxidation of D-arabinitol and substantially incapable of catalyzing the oxidation of D-mannitol. Kits for conducting the present method are also disclosed.

Abstract: The invention is directed to a device for delivering an active agent formulation for a predetermined administration period. An impermeable reservoir is divided into a water-swellable agent chamber and an active agent formulation chamber. Fluid from the environment is imbibed through a semipermeable plug into the water-swellable agent chamber and the active agent formulation is released through a back-diffusion regulating outlet. Delivery periods of up to 2 years are achieved.

Abstract: The present invention relates to an osmotically driven agent delivery system for delivering a beneficial agent. The osmotic delivery system includes an osmotic agent which operates by imbibing fluid from an outside environment, causing the release of a beneficial agent. The osmotic delivery system includes a liquid or gel additive surrounding the osmotic agent for enhancing start-up and lubricating the osmotic agent. The liquid or gel additive is an incompressible lubricating fluid which fills any air gaps between the osmotic agent and the walls of a chamber and substantially reduces start-up delays.

Abstract: The invention is directed to a device for delivering an active agent formulation for a predetermined administration period. An impermeable reservoir is divided into a water-swellable agent chamber and an active agent formulation chamber. Fluid from the environment is imbibed through a semipermeable plug into the water-swellable agent chamber and the active agent formulation is released through a back-diffusion regulating outlet. Delivery periods of up to 2 years are achieved.

Abstract: This invention relates to stable non-aqueous protic formulations of peptide compounds. These stable formulations comprise peptide in non-aqueous protic solvent. They may be stored at elevated temperatures for long periods of time and are especially useful in implantable delivery devices for long term delivery of drug.

Abstract: This invention relates to stable non-aqueous polar aprotic formulations of peptide compounds. These stable formulations comprise peptide in non- aqueous polar aprotic solvent. They may be stored at elevated temperatures for long periods of time and are especially useful in implantable delivery devices for long term delivery of drug.

Abstract: A delivery system is disclosed for delivering a fluid-sensitive active agent such as a somatotropin, or an analogue or derivative thereof, to an animal such as a bovine. The delivery system comprises a first wall section, a second wall section and a locking coupling therebetween. The coupled wall sections define a compartment, enclosing an active agent and an expandable driving member. Various embodiments of the locking coupling are disclosed.

Abstract: This invention relates to stable liquid aqueous formulations of peptide compounds at high concentrations. These stable formulations comprise at least about 10% peptide in water. They may be stored at elevated temperatures for long periods of time and are especially useful in implantable delivery devices for long term delivery of drug.

Abstract: The present invention provides improved compositions for improving the chemical and physical stability of peptides and proteins. The invention provides a liquid beneficial agent formulation containing a liquid suspension comprising at least 5% by weight beneficial agent and having a viscosity and beneficial agent size which minimizes settling of the agent in suspension over the extended delivery period.

Abstract: The present invention is concerned with improving the delivery of a drug from a ruminal delivery device to give a consistent delivery of drug to the ruminal environment. Thus, the invention is directed to an improved ruminal drug delivery device comprising a semipermeable membrane having an exit orifice and defining a compartment, the compartment containing a swellable osmotic agent expandable driving member, a drug to be dispensed, a density element and, optionally, a partition layer between the osmotic expandable driving member and the drug formulation, wherein the improvement comprises an essentially gas-impermeable barrier means that separates the density element from the other components within the delivery device for isolating gases evolved from the density element from the other components within the delivery device. The barrier means further includes a coupling to transfer osmotic pressure to the semipermeable wall.

Abstract: A dosage form is disclosed for delivering an antiepileptic drug, which dosage form comprises a laminated wall for maintaining the integrity of the dosage form and of the antiepileptic drug.

Abstract: A delivery system (10) is disclosed for delivering a fluid-sensitive beneficial agent (7) such as a somatotropin, or an analogue or derivative thereof, to an animal such as a bovine. The delivery system comprises a wall that surrounds an internal compartment, said wall comprising a first wall section that limits the passage of fluid into the system and a second wall section that permits the passage of fluid into the system. An exit passageway is provided for delivering the beneficial agent an interior compartment (18) to the animal. The exit passageway is sealed with a wax seal (30) which is expelled through the passageway (13) as the internal pressure within the device (10) reaches a predetermined "bursting" pressure.

Abstract: This invention relates to fluid-imbibing delivery devices for delivering a beneficial agent to a biological environment of use. In particular, the devices include a rigid housing defining an internal compartment comprising a substantially impermeable first wall section and a second wall section permeable to fluid in the environment of use. The first wall section may be shape-retaining, with exit means and an open end, and extend for at least 85% of the entire length of the device to define the internal compartment.

Abstract: Methods are disclosed for determining an analyte in a medium suspected of containing the analyte. One method comprises treating a medium suspected of containing an analyte under conditions such that the analyte, if present, causes a photosensitizer and a photoactive indicator precursor molecule to come into close proximity. The photosensitizer generates singlet oxygen which activates the photoactive indicator precursor to generate a photoactive indicator molecule. Upon irradiation with light the photoactive indicator molecule produces light, which is measured. The amount of light produced by the photoactive indicator is related to the amount of analyte in the medium. Compositions, kits, and compounds are also disclosed.

Abstract: This invention relates to use of oligonucleotides having at least one nucleotide that is substituted at the 4'-position of the sugar moiety with a substituent other than hydrogen as nucleotide probes in methods for detecting the presence or amount of a polynucleotide analyte in a sample suspected of containing the polynucleotide analyte. These oligonucleotides can also be packaged in diagnostic assay kits.

Abstract: A delivery system is disclosed for delivering a fluid-sensitive beneficial agent such as a somatotropin, or an analogue or derivative thereof, to an animal such as a bovine. The delivery system comprises a wall that surrounds an internal compartment, said wall comprising a first wall section that limits the passage of fluid into the system and a second wall section that permits the passage of fluid into the system. The wall may further comprise an end cap which may include means for adapting the end cap for ultrasonic welding to the first wall section and means for maintaining the beneficial agent in contact with exit means. The compartment comprises a beneficial agent and an expandable means. The delivery system comprises exit means for delivering the beneficial agent to the animal.