40 patents
Page 2 of 2
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
Modulators of the beta-3 adrenergic receptor useful for the treatment or prevention of disorders related thereto
23 Feb 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: 12 May 20
Utility
Modulators of the GPR119 receptor and the treatment of disorders related thereto
19 Jan 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-imethylbenzamide; 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-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 GPRI19-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: 21 Sep 11
Utility
5-HT2C receptor agonists and compositions and methods of use
16 Nov 20
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: 17 Aug 17
Utility
Substituted pyridazines and 1,2,4-triazines as prostacyclin receptor modulators
5 Oct 20
Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
Filed: 14 Oct 18
Utility
Processes for the preparation of pyrazole derivatives useful as modulators of the 5-HT2A serotonin receptor
28 Sep 20
Ashwin M. Krishnan, Tawfik Gharbaoui
Filed: 24 Jul 18
Utility
3-phenyl-pyrazole derivatives as modulators of the 5-HT
21 Sep 20
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
Filed: 31 Oct 18
Utility
Method of treating conditions related to the PGI2 receptor
22 Jun 20
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: 5 Dec 19
Utility
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
22 Jun 20
Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
Filed: 5 Nov 18
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(Compound 1) for use in SIPI receptor-associated disorders
8 Jun 20
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: 8 Apr 19
Utility
Modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
1 Jun 20
The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J. M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou
Filed: 1 Mar 17
Utility
Modulators of the beta-3 adrenergic receptor useful for the treatment or prevention of disorders related thereto
25 May 20
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: 5 Sep 19
Utility
Cannabinoid receptor modulators
27 Apr 20
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: 7 Feb 17
Utility
5-HT
20 Apr 20
Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor.
Juerg Lehmann, Konrad Feichtinger, Albert S. Ren, Graeme Semple
Filed: 11 Mar 19
Utility
Composition of a 5-HT2A serotonin receptor modulator useful for the treatment of disorders related thereto
9 Mar 20
The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation.
Lee Alani Selvey, Marlon Carlos, Paul Maffuid, Yun Shan, William L. Betts, III, Deam Windate Given, III, Ryan M. Hart, Zezhi Jesse Shao
Filed: 26 Sep 18
Utility
Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and crystalline forms related thereto
27 Jan 20
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.
Marlon Carlos, Weitong Dong, Mark Macias, Suzanne Michiko Sato, Lee Alani Selvey
Filed: 6 Aug 18
Utility
Method of treating conditions related to the PGI2 receptor
20 Jan 20
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: 21 Oct 15
Utility
Modulators of the beta-3 adrenergic receptor useful for the treatment or prevention of disorders related thereto
18 Nov 19
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: 3 Jun 19
Utility
Modified-release dosage forms of 5-HT
4 Nov 19
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.
Zezhi Jesse Shao, Anthony C. Blackburn, Andrew J. Grottick, Michael E. Morgan, Jaimie Karyn Rueter, Anna Shifrina, Scott Stirn, Libo Yang, Woo Hyun Yoon
Filed: 6 Jan 19
Utility
Ethers, secondary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
21 Oct 19
Bradley Teegarden, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, Honnappa Jayakumar, Thuy-Anh Tran, Sonja Strah-Pleynet, Jay Xu
Filed: 21 Aug 16