40 patents
Utility
Method of treating conditions related to the PGI2 receptor
28 Nov 23
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.
Alan Glicklich
Filed: 12 Jul 22
Utility
Compositions comprising PGI2-receptor agonists and processes for the preparation thereof
28 Nov 23
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.
Zezhi Jesse Shao, Raizza Berania Florida, Ching-Yuan Li, Lee Alani Selvey
Filed: 12 Aug 21
Utility
Substituted 3-phenoxyazetidin-1-yl-pyrazines
10 Oct 23
Kai Gerlach, Graeme Semple, Yifeng Xiong, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Scott Hobson, Uta Friederike Lessel, Frank Runge, Ursula Mueller-Vieira, Julian Wippich
Filed: 29 Mar 21
Utility
Cannabinoid receptor modulators
3 Oct 23
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
Filed: 17 Sep 21
Utility
Cannabinoid receptor modulators
5 Sep 23
The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor.
Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
Filed: 18 Sep 20
Utility
5-HT2C receptor agonists and compositions and methods of use
21 Mar 23
The present invention relates to compounds of Formula A and pharmaceutical compositions thereof that modulate the activity of the 5-HT2C receptor.
Graeme Semple, Albert S. Ren, Thomas O. Schrader, Michelle Kasem, Xiuwen Zhu
Filed: 19 Oct 20
Utility
Crystalline forms and processes for the preparation of cannabinoid receptor modulators
24 Jan 23
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; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease.
Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter
Filed: 16 Mar 21
Utility
Modulators of the beta-3 adrenergic receptor useful for the treatment or prevention of disorders related thereto
24 Jan 23
The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor.
Thuy-Anh Tran, Quyen-Quyen Do, Brett Ullman, Anthony C. Blackburn, Maiko Nagura
Filed: 14 Dec 20
Utility
Compounds useful in the treatment of autoimmune and inflammatory disorders
17 Jan 23
Abu J. M. Sadeque, Daniel J. Buzard
Filed: 5 Sep 19
Utility
Compounds and methods for treatment of primary biliary cholangitis
27 Dec 22
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).
Cheryl Geraldine Lassen, Robert Mark Jones, Que Liu, Ronald J. Christopher
Filed: 16 Feb 18
Utility
Compounds and methods for treatment of inflammatory bowel disease with extra-intestinal manifestations
25 Oct 22
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).
Cheryl Geraldine Lassen
Filed: 16 Feb 18
Utility
Method of treating conditions related to the PGI2 receptor
30 Aug 22
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.
Alan Glicklich
Filed: 12 Apr 21
Utility
5-HT
26 Jul 22
Juerg Lehmann, Konrad Feichtinger, Albert S. Ren, Graeme Semple
Filed: 14 Apr 20
Utility
Modulators of the beta-3 adrenergic receptor useful for the treatment or prevention of heart failure and disorders related thereto
24 May 22
Thuy-Anh Tran, Brett Ullman, Bryan Aubrey Kramer, Quyen-Quyen Thuy Do, Young-Jun Shin
Filed: 6 Dec 18
Utility
Cannabinoid receptor modulators
4 Jan 22
The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor.
Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
Filed: 24 Sep 19
Utility
Processes for the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[B]indol-3-yl)acetic acid and salts thereof
19 Oct 21
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
Filed: 16 Aug 16
Utility
Compositions comprising PGI2-receptor agonists and processes for the preparation thereof
21 Sep 21
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.
Zezhi Jesse Shao, Raizza Berania Florida, Ching-Yuan Li, Lee Alani Selvey
Filed: 16 Apr 19
Utility
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
24 Aug 21
Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
Filed: 30 Apr 20
Utility
Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3, 4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(compound1) for use in S1P
17 Aug 21
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).
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
Filed: 30 Apr 20
Utility
Methods of treating conditions related to the S1P
18 May 21
Provided are methods of treatment of a sphingosine 1-phosphate subtype 1 (S1P1) receptor-associated disorder comprising prescribing and/or administering to an individual in need thereof a standard dose of (R)-2-(7-(4-cyclopentyl-3-(trifluoro-methyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, in an amount equivalent to about 1.5 to about 2.5 mg of Compound 1, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, ankylosing spondylitis, biliary cirrhosis, cancer, psoriasis, psoriatic arthritis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, inflammatory bowel disease, ulcerative colitis, type I diabetes, hypertensive nephropathy, glomerulosclerosis, myocardial ischemia-reperfusion injury, and acne.
Alan Glicklich, Maria Matilde Sanchez Kam, William R. Shanahan
Filed: 6 Jan 16