944904-60-3Relevant academic research and scientific papers
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties ()
Vachal, Petr,Duffy, Joseph L.,Campeau, Louis-Charles,Amin, Rupesh P.,Mitra, Kaushik,Murphy, Beth Ann,Shao, Pengcheng P.,Sinclair, Peter J.,Ye, Feng,Katipally, Revathi,Lu, Zhijian,Ondeyka, Debra,Chen, Yi-Heng,Zhao, Kake,Sun, Wanying,Tyagarajan, Sriram,Bao, Jianming,Wang, Sheng-Ping,Cote, Josee,Lipardi, Concetta,Metzger, Daniel,Leung, Dennis,Hartmann, Georgy,Wollenberg, Gordon K.,Liu, Jian,Tan, Lushi,Xu, Yingju,Chen, Qinghao,Liu, Guiquan,Blaustein, Robert O.,Johns, Douglas G.
, p. 13215 - 13258 (2021/09/02)
Cholesteryl ester transfer protein (CETP) represents one of the key regulators of the homeostasis of lipid particles, including high-density lipoprotein (HDL) and low-density lipoprotein (LDL) particles. Epidemiological evidence correlates increased HDL and decreased LDL to coronary heart disease (CHD) risk reduction. This relationship is consistent with a clinical outcomes trial of a CETP inhibitor (anacetrapib) combined with standard of care (statin), which led to a 9% additional risk reduction compared to standard of care alone. We discuss here the discovery of MK-8262, a CETP inhibitor with the potential for being the best-in-class molecule. Novel in vitro and in vivo paradigms were integrated to drug discovery to guide optimization informed by a critical understanding of key clinical adverse effect profiles. We present preclinical and clinical evidence of MK-8262 safety and efficacy by means of HDL increase and LDL reduction as biomarkers for reduced CHD risk.
IMIDAZOPYRIMIDINES AS EED INHIBITORS AND THE USE THEREOF
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Paragraph 0423, (2021/02/12)
The present disclosure provides compounds represented by Formula (I) wherein R1, R2, R3, and R4 are as defined in the specification, and the salts and solvates thereof. Compounds of Formula (I) are FED inhibitors. FED inhibitors are useful for the treatment of cancer and other diseases.
Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression
Chen, Jianyong,Chinnaswamy, Krishnapriya,Li, Ruiting,Lu, Jianfeng,McEachern, Donna,Petrunak, Elyse,Rej, Rohan Kalyan,Stuckey, Jeanne A.,Sun, Duxin,Tang, Guozhi,Wang, Changwei,Wang, Lu,Wang, Mi,Wang, Shaomeng,Wen, Bo,Yang, Chao-Yie,Zawacki, Kaitlin P.,Zhou, Yunlong
, p. 14540 - 14556 (2021/10/26)
Embryonic ectoderm development (EED) is a promising therapeutic target for human cancers and other diseases. We report herein the discovery of exceptionally potent and efficacious EED inhibitors. By conformational restriction of a previously reported EED
COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF HIF2-ALPHA AND THEIR METHODS OF USE
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Page/Page column 120, (2021/11/06)
The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease. The compounds are inhibitors or modulators of HIF2alpha.
NOVEL SUBSTITUTED BIARYL COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
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Paragraph 1183; 1184, (2019/05/24)
Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
FUSED BICYCLIC OXAZOLIDINONE CETP INHIBITOR
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Paragraph 0218; 0219, (2013/05/09)
Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
