108 patents
Page 4 of 6
Utility
Processes for the Preparation of Pyrazole Derivatives Useful As Modulators of the 5-HT2A Serotonin Receptor
8 Apr 21
Ashwin M. KRISHNAN, Tawfik GHARBAOUI
Filed: 19 Aug 20
Utility
Cannabinoid Receptor Modulators
4 Mar 21
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: 15 Apr 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
SUBSTITUTED (1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
30 Dec 20
Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stirn
Filed: 7 Jun 20
Utility
Composition of a 5-HT2A Serotonin Receptor Modulator Useful for the Treatment of Disorders Related Thereto
23 Dec 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: 22 Jan 20
Utility
Diaryl and Arylheteroaryl Urea Derivatives As Modulators of the 5-HT2A Serotonin Receptor Useful for the Prophylaxis and Treatment of Disorders Related Thereto
23 Dec 20
Bradley TEEGARDEN, Honnappa JAYAKUMAR, Hongmei LI, Sonja STRAH-PLEYNET, Peter I. DOSA
Filed: 23 Feb 20
Utility
Pyrazolyl Substituted Carbonic Acid Derivatives As Modulators of the Prostacyclin (PGI2) Receptor Useful for the Treatment of Disorders Related Thereto
16 Dec 20
Thuy-Anh TRAN, Jason B. IBARRA, Young-Jun SHIN, Brett ULLMAN, Ning ZOU, Xi ZENG
Filed: 29 Apr 20
Utility
Substituted Pyridazines and 1,2,4-TRIAZINES As Prostacyclin Receptor Modulators
9 Dec 20
Thuy-Anh TRAN, Rena HAYASHI, Jason B. IBARRA, Brett ULLMAN, Ning ZOU
Filed: 24 Aug 20
Utility
Modulators of the BETA-3 Adrenergic Receptor Useful for the Treatment or Prevention of Heart Failure and Disorders Related Thereto
9 Dec 20
Thuy-Anh Tran, Brett Ullman, Bryan Aubrey Kramer, Quyen-Quyen Thuy Do, Young-Jun Shin
Filed: 5 Dec 18
Utility
5-HT2C Receptor Agonists and Compositions and Methods of Use
9 Dec 20
Juerg Lehmann, Konrad Feichtinger, Albert S. Ren, Graeme Semple
Filed: 13 Apr 20
Utility
Modulators of the Prostacyclin (PGI2) Receptor Useful for the Treatment of Disorders Related Thereto
2 Dec 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: 13 Apr 20
Utility
Methods of Treatment
25 Nov 20
Provided in some embodiments are methods of treating or preventing Raynaud's, comprising prescribing and/or administering to an individual 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.
John W. ADAMS, Christen M. ANDERSON, William R. SHANAHAN
Filed: 6 Aug 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(COMPOUND1) for Use In Sipi Receptor-associated Disorders
18 Nov 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: 29 Apr 20
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
26 Aug 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: 7 May 20
Utility
Modulators of the BETA-3 Adrenergic Receptor Useful for the Treatment or Prevention of Disorders Related Thereto
26 Aug 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: 11 May 20