Patents Assigned to Arena Pharmaceuticals, Inc.
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Patent number: 11826337Abstract: 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: GrantFiled: July 12, 2022Date of Patent: November 28, 2023Assignee: ARENA PHARMACEUTICALS, INC.Inventor: Alan Glicklich
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Patent number: 11826471Abstract: Provided herein in some embodiments are pharmaceutical compositions comprising a prostacyclin (PGI2) receptor agonist selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1) and pharmaceutically acceptable salts, solvates, and hydrates thereof, as disclosed herein. In some embodiments the pharmaceutical compositions comprise a compound selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1), and pharmaceutically acceptable salts, solvates, and hydrates thereof, in an amount equivalent to a therapeutically effective amount of Compound 1, the composition having a release rate by weight of the compound in an aqueous medium that is one or more of release rates (a), (b) and (c) as disclosed herein. The compositions of the present invention are useful in the treatment of PGI2 related disorders, such as those disclosed herein.Type: GrantFiled: August 12, 2021Date of Patent: November 28, 2023Assignee: ARENA PHARMACEUTICALS, INC.Inventors: Zezhi Jesse Shao, Raizza Berania Florida, Ching-Yuan Li, Lee Alani Selvey
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Patent number: 11780827Abstract: The invention relates to substituted 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) for use as a medicament, pharmaceutical compositions comprising the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.Type: GrantFiled: March 29, 2021Date of Patent: October 10, 2023Assignees: Boehringer Ingelheim International GmbH, Arena Pharmaceuticals, Inc.Inventors: Kai Gerlach, Graeme Semple, Yifeng Xiong, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Scott Hobson, Uta Friederike Lessel, Frank Runge, Ursula Mueller-Vieira, Julian Wippich
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Patent number: 11771695Abstract: Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;Type: GrantFiled: September 17, 2021Date of Patent: October 3, 2023Assignee: 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
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Patent number: 11746091Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.Type: GrantFiled: September 18, 2020Date of Patent: September 5, 2023Assignee: Arena Pharmaceuticals, Inc.Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
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Patent number: 11674163Abstract: 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: GrantFiled: September 14, 2021Date of Patent: June 13, 2023Assignee: 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
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Publication number: 20230131465Abstract: The invention relates to 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) for use as a medicament, pharmaceutical compositions comprising at least a compound of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.Type: ApplicationFiled: September 9, 2022Publication date: April 27, 2023Applicants: Boehringer Ingelheim International GmbH, Arena Pharmaceuticals, Inc.Inventors: Kai Gerlach, Daniela Gavina Berta, Marco Ferrara, Kirsten Gutsche, Ursula Mueller-Vieira, Scott Hobson, Frank Runge, Graeme Semple, Viktor Vintonyak, Yifeng Xiong
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Patent number: 11608339Abstract: The present invention relates to compounds of Formula A and pharmaceutical compositions thereof that modulate the activity of the 5-HT2C receptor.Type: GrantFiled: October 19, 2020Date of Patent: March 21, 2023Assignee: Arena Pharmaceuticals, Inc.Inventors: Graeme Semple, Albert S. Ren, Thomas O. Schrader, Michelle Kasem, Xiuwen Zhu
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Patent number: 11560386Abstract: 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: GrantFiled: December 14, 2020Date of Patent: January 24, 2023Assignee: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Quyen-Quyen Do, Brett Ullman, Anthony C. Blackburn, Maiko Nagura
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Patent number: 11560369Abstract: The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in the treatment of CB2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough;Type: GrantFiled: March 16, 2021Date of Patent: January 24, 2023Assignee: Arena Pharmaceuticals, Inc.Inventors: Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter
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Patent number: 11555015Abstract: The present invention relates to certain compounds of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor: Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, an inflammatory skin disease or disorder, cancer, psoriasis, atopic dermatitis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, and acne, microbial infections or diseases and viral infections or diseases.Type: GrantFiled: September 5, 2019Date of Patent: January 17, 2023Assignee: Arena Pharmaceuticals, Inc.Inventors: Abu J. M. Sadeque, Daniel J. Buzard
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Patent number: 11534424Abstract: 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: GrantFiled: February 16, 2018Date of Patent: December 27, 2022Assignee: Arena Pharmaceuticals, Inc.Inventors: Cheryl Geraldine Lassen, Robert Mark Jones, Que Liu, Ronald J. Christopher
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Publication number: 20220356172Abstract: The invention relates to substituted 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) for use as a medicament, pharmaceutical compositions comprising the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.Type: ApplicationFiled: March 29, 2021Publication date: November 10, 2022Applicants: Boehringer Ingelheim International GmbH, Arena Pharmaceuticals, Inc.Inventors: Kai Gerlach, Graeme Semple, Yifeng Xiong, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Scott Hobson, Uta Friederike Lessel, Frank Runge, Ursula Mueller-Vieira, Julian Wippich
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Patent number: 11478448Abstract: The present invention relates to, inter alia, methods of treatment and combinations of (R)-2-(7-(4-cyclopentyl-3-(triflu-oromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1) useful for the treatment of extra-intestinal manifestations (EIM) in an individual with inflammatory bowel disease (BBD) and for the treatment of pyoderma gangrenosum (PG). In some embodiments, the methods further comprise administering Compound 1, or a harmaceutically salt, solvate, or hydrate thereof, in combination with a therapeutically effective amount of a compound selected from the group consisting of: a corticosteroid, a 5-ammosalicylic acid derivative, and a TNF-alpha inhibitor; or a corticosteroid, an immunosuppressant, a biologic, an anti-inflammatory agent, and an antibiotic.Type: GrantFiled: February 16, 2018Date of Patent: October 25, 2022Assignee: Arena Pharmaceuticals, Inc.Inventor: Cheryl Geraldine Lassen
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Patent number: 11426377Abstract: 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-chloropbenyl)(pbenyl)carbamoyloxy)methyl)cyclohexyi)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: GrantFiled: April 12, 2021Date of Patent: August 30, 2022Assignee: ARENA PHARMACEUTICALS, INC.Inventor: Alan Glicklich
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Patent number: 11395824Abstract: Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor.Type: GrantFiled: April 14, 2020Date of Patent: July 26, 2022Assignee: Arena Pharmaceuticals, Inc.Inventors: Juerg Lehmann, Konrad Feichtinger, Albert S. Ren, Graeme Semple
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Patent number: 11339172Abstract: 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 and related disorders thereto.Type: GrantFiled: December 6, 2018Date of Patent: May 24, 2022Assignee: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Brett Ullman, Bryan Aubrey Kramer, Quyen-Quyen Thuy Do, Young-Jun Shin
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Patent number: 11214548Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.Type: GrantFiled: September 24, 2019Date of Patent: January 4, 2022Assignee: Arena Pharmaceuticals, Inc.Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
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Patent number: 11149292Abstract: 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: GrantFiled: August 16, 2016Date of Patent: October 19, 2021Assignee: 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
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Patent number: 11123298Abstract: Provided herein in some embodiments are pharmaceutical compositions comprising a prostacyclin (PGI2) receptor agonist selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1) and pharmaceutically acceptable salts, solvates, and hydrates thereof, as disclosed herein. In some embodiments the pharmaceutical compositions comprise a compound selected from 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyloxy)methyl)cyclohexyl)methoxy)acetic acid (Compound 1), and pharmaceutically acceptable salts, solvates, and hydrates thereof, in an amount equivalent to a therapeutically effective amount of Compound 1, the composition having a release rate by weight of the compound in an aqueous medium that is one or more of release rates (a), (b) and (c) as disclosed herein. The compositions of the present invention are useful in the treatment of PGI2 related disorders, such as those disclosed herein.Type: GrantFiled: April 16, 2019Date of Patent: September 21, 2021Assignee: ARENA PHARMACEUTICALS, INC.Inventors: Zezhi Jesse Shao, Raizza Berania Florida, Ching-Yuan Li, Lee Alani Selvey