Patents Assigned to Arena Pharmaceuticals, Inc.
  • Patent number: 9085581
    Abstract: The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro -7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as 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).
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: July 21, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Robert M. Jones, Daniel J. Buzard, Tawfik Gharbaoui, Benjamin R. Johnson, Michelle Kasem, Thomas O. Schrader, Scott Stirn
  • Patent number: 9068983
    Abstract: 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.
    Type: Grant
    Filed: July 1, 2011
    Date of Patent: June 30, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Didier Bagnol, Chen W. Liaw
  • Patent number: 9045431
    Abstract: Processes and intermediates for preparing salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and pharmaceutically acceptable solvates and hydrates thereof, that are useful for, inter alia, weight management.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: June 2, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, Anna Shifrina
  • Patent number: 9034911
    Abstract: The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: May 19, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Lee Alani Selvey, Marlon Carlos, Paul Maffuid, Yun Shan, William L. Betts, III, Deam Windate Given, III, Ryan M. Hart, Zezhi Jesse Shao
  • Patent number: 9012478
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: April 21, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Patent number: 8999970
    Abstract: The present disclosure relates to methods for weight management in an individual in need thereof by determining the level of renal sufficiency of the individual and prescribing or administering a therapeutically effective amount of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof to the individual, provided that the individual has a level of renal sufficiency selected from the group consisting of: no renal impairment, mild renal impairment, and moderate renal impairment.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: April 7, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Christen M. Anderson, William R. Shanahan
  • Patent number: 8993750
    Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Grant
    Filed: July 9, 2014
    Date of Patent: March 31, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Brian Smith, Jeffrey Smith
  • Patent number: 8980891
    Abstract: Provided are certain solvates of 3-methoxy-N-[3-(2-methyl-2H-pyrazol-3-yl)-4-(2-morpholin-4-yl-ethoxy)-phenyl]-benzamide or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions comprising such solvates and methods for their use.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: March 17, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Scott Stirn, Edward A. Lally
  • Patent number: 8980881
    Abstract: 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.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: March 17, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Rajesh K. Agarwal, William L. Betts, III, James A. Henshilwood, Yuan-Hon Kiang, Noah Post
  • Patent number: 8952197
    Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (lorcaserin), a serotonin (5-HT) receptor modulator that is useful in the treatment of for example, central nervous system disorders, such as obesity.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: February 10, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: John A. DeMattei, Carlos Marlon, Ryan O. Castro, Tsung-Hsun Chuang, Mark Allen Hadd, Xiao-Xiong Lu, Mark Macias, Stephen M. Shaw
  • Patent number: 8946207
    Abstract: The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: February 3, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Beverly L. Wolgast, Charles A. Gilson, III, Shelley Aytes, Scott A. Estrada, Dipanjan Sengupta, Brian Smith, Ulrich Weigl, Heidedore Jlsabeth Rey-Papina
  • Patent number: 8940891
    Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: January 27, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
  • Patent number: 8933083
    Abstract: The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Formula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: January 13, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Robert M. Jones, Graeme Semple, Beatriz Fioravanti, Guilherme Pereira, Imelda Calderon, Jane Laguerta Uy, Kameshwari Duvvuri, Jin Sun Karoline Choi, Yifeng Xiong, Vibha Dave, Mihai D. Azimioara
  • Publication number: 20140357690
    Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) 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).
    Type: Application
    Filed: August 20, 2014
    Publication date: December 4, 2014
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Kuhlman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
  • Patent number: 8895776
    Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: November 25, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J. M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou
  • Patent number: 8883714
    Abstract: The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: November 11, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Zhi-Liang Chu, James N. Leonard, Robert M. Jones
  • Patent number: 8871797
    Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: October 28, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter I. Dosa
  • Patent number: 8853419
    Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) 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).
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: October 7, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Khulman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
  • Patent number: RE45336
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: January 13, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
  • Patent number: RE45337
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: January 13, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, Honnappa Jayakumar, Thuy-Anh Tran, Sonja Strah-Pleynet, Jay Xu