2227448-95-3Relevant academic research and scientific papers
Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases
Cheng, Peter T. W.,Kaltenbach, Robert F.,Zhang, Hao,Shi, Jun,Tao, Shiwei,Li, Jun,Kennedy, Lawrence J.,Walker, Steven J.,Shi, Yan,Wang, Ying,Dhanusu, Suresh,Reddigunta, Ramesh,Kumaravel, Selvakumar,Jusuf, Sutjano,Smith, Daniel,Krishnananthan, Subramaniam,Li, Jianqing,Wang, Tao,Heiry, Rebekah,Sum, Chi Shing,Kalinowski, Stephen S.,Hung, Chen-Pin,Chu, Ching-Hsuen,Azzara, Anthony V.,Ziegler, Milinda,Burns, Lisa,Zinker, Bradley A.,Boehm, Stephanie,Taylor, Joseph,Sapuppo, Julia,Mosure, Kathy,Everlof, Gerry,Guarino, Victor,Zhang, Lisa,Yang, Yanou,Ruan, Qian,Xu, Carrie,Apedo, Atsu,Traeger, Sarah C.,Cvijic, Mary Ellen,Lentz, Kimberley A.,Tirucherai, Giridhar,Sivaraman, Lakshmi,Robl, Jeffrey,Ellsworth, Bruce A.,Rosen, Glenn,Gordon, David A.,Soars, Matthew G.,Gill, Michael,Murphy, Brian J.
, p. 15549 - 15581 (2021/11/16)
The oxycyclohexyl acid BMS-986278 (33) is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM. The structure-activity relationship (SAR) studies starting from the LPA1 antagonist clinical compound BMS-986020 (1), which culminated in the discovery of 33, are discussed. The detailed in vitro and in vivo preclinical pharmacology profiles of 33, as well as its pharmacokinetics/metabolism profile, are described. On the basis of its in vivo efficacy in rodent chronic lung fibrosis models and excellent overall ADME (absorption, distribution, metabolism, excretion) properties in multiple preclinical species, 33 was advanced into clinical trials, including an ongoing Phase 2 clinical trial in patients with lung fibrosis (NCT04308681).
TRIAZOLE CARBAMATE PYRIDYL SULFONAMIDES AS LPA RECEPTOR ANTAGONISTS AND USES THEREOF
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Paragraph 0307-0308, (2021/05/21)
The present disclosure relates generally to compounds of Formula (I) that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non-alcoholic steatohepatitis (NASH).
CYCLOPENTYL ACIDS AS LPA ANTAGONISTS
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Page/Page column 121-122; 161, (2020/04/25)
The present invention provides compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
CYCLOBUTYL CARBOXYLIC ACIDS AS LPA ANTAGONISTS
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Page/Page column 100, (2021/01/22)
The present invention provides compounds of Formula (I): (I), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
TRIAZOLE CARBOXYLIC ACIDS AS LPA ANTAGONISTS
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Page/Page column 88-89, (2021/01/22)
The present invention provides compounds of Formula (I), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
Synergistic Effect of Copper and Ruthenium on Regioselectivity in the Alkyne-Azide Click Reaction of Internal Alkynes
Ramasamy, Sivaraj,Petha, Chittibabu,Tendulkar, Shankar,Maity, Prantik,Eastgate, Martin D.,Vaidyanathan, Rajappa
, p. 880 - 887 (2018/07/31)
Cu(I) salts have been shown to improve the regioselectivity and rate of the Ru-catalyzed alkyne-azide click reaction of internal alkynes with azides. While Cu and Ru individually provide complementary regioselectivity in the case of terminal alkynes, the
