Abstract: Certain novel compounds and derivatives thereof are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Abstract: The present invention relates to methods of gene therapy for inhibiting angiogenesis associated with solid tumor growth, tumor metastasis, inflammation, psoriasis, rheumatoid arthritis, hemangiomas, diabetic retinopathy, angiofibromas, and macular degeneration Gene therapy methodology is disclosed for inhibition of primary tumor growth and metastasis by gene transfer of a nucleotide sequence encoding a soluble form of a VEGF tyrosine kinase receptor to a mammalian host. The transferred nucleotide sequence transcribes mRNA and a soluble receptor protein which binds to VEGF in extracellular regions adjacent to the primary tumor and vascular endothelial cells. Formation of a sVEGF-R/VEGF complex will prevent binding of VEGF to the KDR and FLT-1 tyrosine kinase receptors, antagonizing transduction of the normal intracellular signals associated with vascular endothelial cell-induced tumor angiogenesis.

Abstract: In accordance with the present invention, there are provided nucleic acids encoding human NMDA receptor protein subunits and the proteins encoded thereby. The NMDA receptor subunits of the invention comprise components of NMDA receptors that have cation-selective channels and bind glutamate and NMDA. In one aspect of the invention, the nucleic acids encode NMDAR1 and NMDAR2 subunits of human NMDA receptors. In a preferred embodiment, the invention nucleic acids encode NMDAR1, NMDAR2A, NMDAR2B, NMDAR2C and NMDAR2D subunits of human NMDA receptors. In addition to being useful for the production of NMDA receptor subunit proteins, these nucleic acids are also useful as probes, thus enabling those skilled in the art, without undue experimentation, to identify and isolate related human receptor subunits.

Abstract: The present invention relates to a novel vaccine formulation comprising nucleic acid molecules and an mineral-based adjuvant provided in a biologically effective concentration so as to improve induction of an immune response subsequent to vaccination which correlates to expression of one or more specific antigens encoded by the nucleic acid molecule.

Abstract: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.

Abstract: Novel phenylcyclohexanes of the formula I 1

Abstract: A multi-layer tablet for the instant and prolonged release of active substances comprises at least two layers where the first outer layer comprises a mixture of excipients and an active substance, allowing for the immediate release of the active substance within the first layer, and a second layer, arranged in contact with the first layer. The second layer comprises a nonbiodegradable inert porous polymeric matrix in which an active substance is dispersed, allowing for the prolonged release of the active substance within the second layer.

Abstract: The present invention relates to a pigment preparation containing a mixture of coated or uncoated Al2O3 flakes, and one or more special-effect pigments, and a phosphate derivative, and to the use thereof, especially in printing inks.

Abstract: A process for preparing a &bgr;-hydroxy carbamate product is disclosed. The process comprises reacting an olefin compound containing at least one carbon-carbon double bond with a carbamate in an aqueous solvent and in the presence of a base, an osmium catalyst, a co-oxidant selected from a halohydantoin, a haloisocyanuric acid, and an alkali metal salt of a haloisocyanuric acid, and optionally an asymmetric ligand, to form a reaction mixture containing the &bgr;-hydroxy carbamate product. The process optionally further comprises treating the &bgr;-hydroxy carbamate product with additional base to form an oxazolidinone. The oxazolidinones are useful as chiral auxiliary agents and as intermediates for the formation of pharmaceutically active substances such as alpha 1 a adrenergic receptor antagonists. A process for preparing nitrogen-functionalized derivatives of the oxazolidinones is also disclosed.

Abstract: The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4 and R5 represent a variety of substituents; R6 represents hydrogen, CORa, CO2Ra, COCONRaRb, COCO2Ra, C1-6alkyl optionally substituted by a group selected from (CO2Ra, CONRaRb, hydroxy, CN, CORa, NRaRb, C(NOH)NRaRb, CONHphenyl(C1-4alkyl), COCO2Ra, CONHNRaRb, C(S)NRaRb, CONRaC1-6alkylR12, CONR13C2-6alkenyl, CONR13C2-6alkynyl, COCONRaRb, CONRaC(NRb)NRaRb, CONRaheteroaryl, and phenyl optionally substituted by one, two or three substituents selected from C1-6alky, C1-6alkoxy, halogen and trifluoromethyl); or R6 represents a group of formula —CH2C≡CCH2NR7R8 where R7 and R8 are as defined below; or R6 represents C1-6alkyl, optionally substituted by oxo, substituted by a 5-membered or 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen atoms optionally substituted by ═O or ═S and optionally substituted by a group of the formula ZNR7R8; or a pharmaceutical acceptable salt thereof.

Abstract: A pharmaceutical composition comprising: (i) metformin, optionally in the form one of its pharmaceutically acceptable salts; (ii) a fibrate selected from fenofibrate and bezafibrate; and optionally one or more pharmaceutically acceptable excipients, is suitable for use in the treatment of non-insulin-dependent diabetes.

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.

Abstract: Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation.

Abstract: Automated measurement apparatus and methods for automated drug screening procedures are provided. The apparatus is capable of initiating and measuring rapid or transient events, such as cell receptor and/or ion channel activity. In particular, the apparatus is capable of aligning with predetermined positions, one or more samples contained in a multi-well container, initiating the reaction with reagent addition and measuring a resultant attribute for a period of time. The apparatus can substantially continuously measure and record data corresponding to the measured attribute before, during and after initiation of the reaction so that a time course of the rapid or transient event may be determined. After the reaction(s) are complete in one or more wells of the multi-well container, the apparatus can align one or more different wells to be assayed with the predetermined position and repeat the cycle until a predetermined number of wells are assayed.

Abstract: A process of purifying target molecules is described that involves the selection of ligands based on identifying, in real time, association and dissociation constants with a given target molecule; using this information to select at least one ligand that exhibit predetermined association and dissociation constants with a given target molecule; anchoring a quantity of ligand to an activated solid support; contacting a quantity of target molecules with the anchored ligand(s); removing low affinity target molecules from anchored ligand and eluting particularly pure target molecules.

Abstract: The present invention relates to the treatment or prevention of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or anti-anxiety agent. The present invention also provides preclinical screens for anxiolytic and antidepressant activity of NK-1 receptor antagonists.

Abstract: The instant invention involves a process for oxidizing compounds containing an allylic group, i.e. those containing an allylic hydrogen or allylic alcohol group, to the corresponding enones, using a ruthenium-based catalyst in the presence of a hydroperoxide. Particularly, &Dgr;-5-steroidal alkenes can be oxidized to the corresponding &Dgr;-5-7-keto alkenes.

Abstract: Novel 5-benzyl-octahydroindoles and 6-benzyl-decahydroquinolines substituted in the 1-position are effective as NMDA NR2B antagonists useful for relieving pain.

Abstract: This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases, or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses pharmaceutical compositions and methods for treatment of prostaglandin mediated diseases.

Abstract: A housing for micromixers has two flat circular disk-shaped housing parts situated adjacent to each other in a parting plane. Each of the housing parts has a truncated cone surface on its peripheral edge. A multipart clamping ring which can be tightened in the peripheral direction encompasses the two housing parts and is adjacent to the truncated cone surfaces.