Arena Pharmaceuticals, Inc. is a biopharmaceutical company located in San Diego, California. The company is developing oral medications that target G-protein-coupled receptors. On June 27, 2012, the FDA approved lorcaserin, initially sold under the brand name Belviq with a launch sales force commitment of 200. Lorcaserin is approved for use in adults with a body mass index of 30 or greater, which is considered obese, or adults with a BMI of 27 or greater and who have at least one weight-related health condition, such as high blood pressure, type 2 diabetes, or high cholesterol.As of September 2014, Arena has other drugs in their pipeline that have not yet been approved by the U.S. Food and Drug Administration, namely: Temanogrel, Phase I, Thrombotic Diseases. Ralinepag, Planned Phase II trial, Pulmonary Arterial Hypertension. APD334, Phase I, Autoimmune Diseases APD371, Phase I, Pain↑ ↑ ↑ ↑ ↑ Wikipedia.
Jones G.,Arena Pharmaceuticals
Journal of Chemical Information and Modeling | Year: 2010
Prediction of the binding mode for a series of active compounds, in the absence of known protein structure, is a problem of paramount importance in rational drug design. GAPE (genetic algorithm for pharmacophore elucidation) is an automated multicompound overlay creation program, based on the original GASP program, that uses a genetic algorithm to fully explore the conformational space of the input structures and their alignments, so as to elucidate a pharmacophore. The software was evaluated on 13 test systems from nine protein targets using overlaid ligands extracted from the PDB. Using objective rmsd criteria and starting from 2D structures, in the absence of any protein information, GAPE was observed in eight systems to approximate the crystallographically observed binding mode. In the predicted alignments for each of those eight systems, at least half the input structures were within 2 Å rmsd of the crystal structure coordinates. Further analysis, using stricter subjective criteria, showed considerable success in five systems. For example, the prediction for a set of 12 ligands targeting P38 had 11 ligands with a 1.8 Å rmsd to crystal structure coordinates. Finally, the algorithm was favorably compared with the current GASP and Galahad programs. © 2010 American Chemical Society. Source
Arena Pharmaceuticals | Date: 2015-04-06
Arena Pharmaceuticals | Date: 2015-09-30
The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (I) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).
Arena Pharmaceuticals | Date: 2015-03-02
The present invention is directed to crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, compositions containing the same and uses thereof.
Arena Pharmaceuticals | Date: 2015-05-21
The present invention relates to methods of using a G protein-coupled receptor (GPCR) to screen one or more candidate compounds as a modulator of body mass or of adiposity or of percentage body fat in a subject or as a pharmaceutical agent for obesity and conditions related thereto. Inverse agonists and antagonists of the invention are useful as therapeutic agents for the prevention or treatment of obesity and conditions related thereto, including hypertension, insulin resistance, metabolic syndrome, Type 2 diabetes, dyslipidemia, atherosclerosis, coronary heart disease, and stroke. Agonists and partial agonists of the invention are useful as therapeutic agents for the prevention or treatment of disorders ameliorated by increasing body mass including, but not limited to, cachexia.