108 patents
Page 3 of 6
Utility
Methods for the Treatment of Scleroderma
16 Dec 21
John W. Adams
Filed: 3 Oct 19
Utility
Compositions Comprising PGI2-RECEPTOR Agonists and Processes for the Preparation Thereof
9 Dec 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: 12 Aug 21
Utility
Pyrazole Derivatives As Modulators of the 5-HT2A Serotonin Receptor Useful for the Treatment of Disorders Related Thereto
9 Dec 21
Yifeng XIONG, Martin C. CHERRIER, Jin Sun Karoline CHOI, Peter I. DOSA, Brian M. SMITH, Sonja STRAH-PLEYNET, Brett ULLMAN, Bradley TEEGARDEN
Filed: 18 Feb 21
Utility
Crystalline Forms and Processes for the Preparation of Cannabinoid Receptor Modulators
9 Dec 21
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
Methods of Treating Conditions Related to the S1P1 Receptor
4 Nov 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-(trifluoromethyl)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: 20 Apr 21
Utility
Compounds Useful In the Treatment of Autoimmune and Inflammatory Disorders
4 Nov 21
Abu J.M. Sadeque, Daniel J. Buzard
Filed: 5 Sep 19
Utility
Modulators of the GPR119 Receptor and the Treatment of Disorders Related Thereto
4 Nov 21
The present invention relates to the GPR119 receptor agonists: 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-dimethylbenzanide; -fluoro-4-(5-fluoro-6-(4-(3-(2-fluoro-propan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
Robert M. Jones, Juerg Lehmann, Weichao Chen, Jeffrey Edwards, Glen Marquez, Michael E. Morgan, Abu J.M. Sadeque, Sun Hee Kim
Filed: 15 Dec 20
Utility
Modulators of the BETA-3 Adrenergic Receptor Useful for the Treatment or Prevention of Disorders Related Thereto
4 Nov 21
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
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
Method of Treating Conditions Related to the PGI2 Receptor
23 Sep 21
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
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 S1P1 Receptor
29 Jul 21
Provided are methods of treatment of a sphingosine 1-phosphate subtype 1 (S1PI) receptor-associated disorder comprising prescribing and/or administering to an individual in need thereof a standard dose of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indo1-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof.
Ronald J. Christopher, Abu J.M. Sadeque
Filed: 5 Jun 19
Utility
5-HT2C Receptor Agonists and Compositions and Methods of Use
15 Jul 21
Graeme Semple, Albert S. Ren, Thomas O. Schrader, Michelle Kasem, Xiuwen Zhu
Filed: 19 Oct 20
Utility
Compositions Comprising PGI2-RECEPTOR Agonists and Processes for the Preparation Thereof
15 Jul 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)cyclohexl)methoxy)acetic acid (Compound 1) and pharmaceutically acceptable salts, solvates, and hydrates thereof, as disclosed herein.
John W. ADAMS
Filed: 23 May 19
Utility
Cannabinoid Receptor Modulators
24 Jun 21
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
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
Utility
Method of treating conditions related to the PGI2 receptor
11 May 21
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: 8 May 20
Utility
IMIDAZO[1,2-A]PYRIDINE Derivatives As Modulators of the 5-HT2A Serotonin Receptor Useful for the Treatment of Disorders Related Thereto
6 May 21
Imidazo[1,2-α]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor.
Yifeng XIONG, Konrad FEICHTINGER, Albert S. REN, Brett ULLMAN
Filed: 9 Sep 20