192650-53-6Relevant academic research and scientific papers
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND METHODS OF USE THEREOF
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Page/Page column 355-356, (2021/06/26)
Provided herein are compounds, compositions, and methods useful for degrading protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer 5 or a metabolic disease.
Synthetic method of poly-substituted dimethyl amino phenyl acetic acid compound
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Paragraph 0046-0049; 0053-0056, (2021/03/05)
The invention relates to a synthesis method of a poly-substituted dimethyl amino phenyl acetic acid compound. The synthesis method comprises the following steps: carrying out methyl esterification reaction on a compound shown in a formula I to obtain a co
Structural optimization and in vitro profiling of N-phenylbenzamide-based farnesoid X receptor antagonists
Schmidt, Jurema,Schierle, Simone,Gellrich, Leonie,Kaiser, Astrid,Merk, Daniel
, p. 4240 - 4253 (2018/07/21)
Activation of the nuclear farnesoid X receptor (FXR) which acts as cellular bile acid sensor has been validated as therapeutic strategy to counter liver disorders such as non-alcoholic steatohepatitis by the clinical efficacy of obeticholic acid. FXR antagonism, in contrast, is less well studied and potent small molecule FXR antagonists are rare. Here we report the systematic optimization of a novel class of FXR antagonists towards low nanomolar potency. The most optimized compound antagonizes baseline and agonist induced FXR activity in a full length FXR reporter gene assay and represses intrinsic expression of FXR regulated genes in hepatoma cells. With this activity and a favorable toxicity-, stability- and selectivity-profile it appears suitable to further study FXR antagonism in vitro and in vivo.
THIAZOLIDINONE COMPOUNDS AND USE THEREOF
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, (2017/09/21)
A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
2-PHENYL BENZOYLAMIDES
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, (2011/12/04)
Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein.
