Patents Assigned to Arena Pharmaceuticals, Inc.
  • Patent number: 10793529
    Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: October 15, 2018
    Date of Patent: October 6, 2020
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
  • Patent number: 10787437
    Abstract: The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.
    Type: Grant
    Filed: July 25, 2018
    Date of Patent: September 29, 2020
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
  • Patent number: 10781180
    Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives 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, 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, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: November 1, 2018
    Date of Patent: September 22, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Yifeng Xiong, Sonja Strah-Pleynet, Honnappa Jayakumar, Peter I. Dosa, Konrad Feichtinger, Martin Casper, Juerg Lehmann, Robert M. Jones, David J. Unett, Jin Sun Karoline Choi
  • Patent number: 10689372
    Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: November 6, 2018
    Date of Patent: June 23, 2020
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
  • Patent number: 10688076
    Abstract: Provided in some embodiments are titration packages, kits, and methods of treating pulmonary arterial hypertension comprising prescribing and/or administering to a patient in need thereof 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, via a titration scheme that comprises the up-titration of Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, over a period of no more than about nine weeks until an optimized dose is administered.
    Type: Grant
    Filed: December 6, 2019
    Date of Patent: June 23, 2020
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventor: Alan Glicklich
  • Patent number: 10676435
    Abstract: The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) 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 the 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: April 9, 2019
    Date of Patent: June 9, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, Ryan O. Castro, Mark Allen Hadd, You-An Ma, Antonio Garrido Montalban, Jaimie Karyn Rueter, Lee Alani Selvey, Sagar Raj Shakya, Marlon Carlos
  • Patent number: 10668033
    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 2, 2017
    Date of Patent: June 2, 2020
    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: 10662200
    Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a beta-3 adrenergic receptor-mediated disorder, such as, heart failure; cardiac performance in heart failure; mortality, reinfarction, and/or hospitalization in connection with heart failure; acute heart failure; acute decompensated heart failure; congestive heart failure; severe congestive heart failure; organ damage associated with heart failure (e.g.
    Type: Grant
    Filed: September 6, 2019
    Date of Patent: May 26, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Quyen-Quyen Do, Brett Ullman, Anthony C. Blackburn, Maiko Nagura
  • Patent number: 10632134
    Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
    Type: Grant
    Filed: February 8, 2017
    Date of Patent: April 28, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Jayant Thatte, Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Jae-Kyu Jung, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter, Sonja Strah-Pleynet, Lars Thoresen, Yifeng Xiong, Dawei Yue, Xiuwen Zhu
  • Patent number: 10624900
    Abstract: Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: April 21, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Juerg Lehmann, Konrad Feichtinger, Albert S. Ren, Graeme Semple
  • Patent number: 10543193
    Abstract: The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: January 28, 2020
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventors: Marlon Carlos, Weitong Dong, Mark Macias, Suzanne Michiko Sato, Lee Alani Selvey
  • Patent number: 10537546
    Abstract: Provided in some embodiments are titration packages, kits, and methods of treating pulmonary arterial hypertension comprising prescribing and/or administering to a patient in need thereof 2-(((1r,4r)-4-(((4-chlorophenyl) (phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, via a titration scheme that comprises the up-titration of Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, over a period of no more than about nine weeks until an optimized dose is administered.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: January 21, 2020
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventor: Alan Glicklich
  • Publication number: 20200000770
    Abstract: The present invention relates to, inter alia, methods of treatment and combinations of (R)-2-(7-(4-cyclopentyl-3-(tri-fluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1) useful for the treatment of primary biliary cholangitis (PBC). In some embodiments, the methods further comprise administering Compound 1, or a pharmaceutically salt, solvate, or hydrate thereof, in combination with a compound selected from the group consisting of: an antihistamine (diphenhydramine), cholestyramine (questran, prevalite), rifampin, an opioid antagonist (naloxone), pilocarpine (isopto carpine, salagen), cevimeline (evoxac), calcium and/or vitamin D supplement, and vitamin A, D, E and/or K supplement. Other embodiments, relate to titration packages for enabling compliance with a regimen of changing dosage of a medication over a period of time for the treatment of primary biliary cholangitis (PBC).
    Type: Application
    Filed: February 16, 2018
    Publication date: January 2, 2020
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Cheryl Geraldine Lassen, Robert Mark Jones, Que Liu, Ronald J. Christopher
  • Patent number: 10479797
    Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a beta-3 adrenergic receptor-mediated disorder, such as, heart failure; cardiac performance in heart failure; mortality, reinfarction, and/or hospitalization in connection with heart failure; acute heart failure; acute decompensated heart failure; congestive heart failure; severe congestive heart failure; organ damage associated with heart failure (e.g.
    Type: Grant
    Filed: June 4, 2019
    Date of Patent: November 19, 2019
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Quyen-Quyen Do, Brett Ullman, Anthony C. Blackburn, Maiko Nagura
  • Patent number: 10463676
    Abstract: The present invention relates to methods for weight management that utilize modified-release dosage forms comprising (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts and crystalline forms thereof. The present invention further relates to (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts, crystalline forms thereof and modified-release dosage forms comprising them.
    Type: Grant
    Filed: January 7, 2019
    Date of Patent: November 5, 2019
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Zezhi Jesse Shao, Anthony C. Blackburn, Andrew J. Grottick, Michael E. Morgan, Jaimie Karyn Rueter, Anna Shifrina, Scott Stirn, Libo Yang, Woo Hyun Yoon
  • Patent number: 10450276
    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: August 22, 2016
    Date of Patent: October 22, 2019
    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
  • Patent number: 10392390
    Abstract: Provided in some embodiments are compounds herein. Also provided in some embodiments are methods for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: August 27, 2019
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Albert S. Ren, Graeme Semple, Xiuwen Zhu, Carleton R. Sage
  • Patent number: 10351531
    Abstract: Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, 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 symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: July 24, 2017
    Date of Patent: July 16, 2019
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventors: Yifeng Xiong, Martin C. Cherrier, Jin Sun Karoline Choi, Peter I. Dosa, Brian M. Smith, Sonja Strah-Pleynet, Brett Ullman, Bradley Teegarden
  • Patent number: 10301262
    Abstract: The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) 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 the 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: June 21, 2016
    Date of Patent: May 28, 2019
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, Ryan O. Castro, Mark Allen Hadd, You-An Ma, Antonio Garrido Montalban, Jaimie Karyn Rueter, Lee Alani Selvey, Sagar Raj Shakya, Marlon Carlos
  • Patent number: 10272094
    Abstract: Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: April 30, 2019
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Juerg Lehmann, Konrad Feichtinger, Albert S. Ren, Graeme Semple