381247-99-0Relevant articles and documents
De novo Design of SARS-CoV-2 Main Protease Inhibitors
Fischer, Christian,Vep?ek, Nynke A.,Peitsinis, Zisis,Rühmann, Klaus-Peter,Yang, Chao,Spradlin, Jessica N.,Dovala, Dustin,Nomura, Daniel K.,Zhang, Yingkai,Trauner, Dirk
, p. 458 - 463 (2021/10/16)
The COVID-19 pandemic prompted many scientists to investigate remedies against SARS-CoV-2 and related viruses that are likely to appear in the future. As the main protease of the virus, M Pro, is highly conserved among coronaviruses, it has emerged as a prime target for developing inhibitors. Using a combination of virtual screening and molecular modeling, we identified small molecules that were easily accessible and could be quickly diversified. Biochemical assays confirmed a class of pyridones as low micromolar noncovalent inhibitors of the viral main protease.
METHODS AND COMPOSITION OF 4-SUBSTITUTED BENZOYLPIPERAZINE-1-SUBSTITUTED CARBONYLS AS BETA-CATENIN/B-CELL LYMPHOMA 9 INHIBITORS
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Paragraph 0429-0430, (2021/06/11)
In one aspect, the invention relates to 4-substituted benzoylpiperazine-1-substituted carbonyls, derivatives thereof, and related compounds; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders, e.g., various tumors and cancers, associated with β-catenin/BCL9 protein-protein interaction dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
TAM family kinase and/or CSF1R kinase inhibitor and application thereof
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Paragraph 0675; 0679-0681, (2019/08/06)
The invention provides a novel inhibitor compound shown in a general formula (I). The compound has good kinase inhibition activity and can be used for preventing and/or treating diseases mediated by abnormal expression of TAM family kinase and/or a ligand thereof. The compound can target CSF1R kinase and can be used for preventing and/or treating diseases mediated by abnormal expression of a TAM family kinase receptor and/or a CSF1R kinase receptor and/or ligands thereof.
PYRAZOLYL-SUBSTITUTED PYRIDONE COMPOUNDS AS SERINE PROTEASE INHIBITORS
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Paragraph 00203-00204; 00273-00274, (2016/04/09)
There are provided inter alia pyrazolyl-substituted pyridone compounds, which exhibit biological activity, e.g., inhibitory action, against serine proteases, including thrombin and various kallikreins. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of serine proteases, including thrombin and various kallikreins.
Structure-Based Design of 1,4-Dibenzoylpiperazines as β-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction Inhibitors
Wisniewski, John A.,Yin, Jinya,Teuscher, Kevin B.,Zhang, Min,Ji, Haitao
supporting information, p. 508 - 513 (2016/06/01)
A small-molecule inhibitor with a 1,4-dibenzoylpiperazine scaffold was designed to match the critical binding elements in the β-catenin/B-cell lymphoma 9 (BCL9) protein-protein interaction interface. Inhibitor optimization led to a potent inhibitor that can disrupt the β-catenin/BCL9 interaction and exhibit 98-fold selectivity over the β-catenin/cadherin interaction. The binding mode of new inhibitors was characterized by structure-activity relationships and site-directed mutagenesis studies. Cell-based studies demonstrated that this series of inhibitors can selectively suppress canonical Wnt signaling and inhibit growth of Wnt/β-catenin-dependent cancer cells.
CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR
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Paragraph 0042; 0562; 0563, (2014/02/16)
The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same.
CYCLOALKENYL ARYL DERIVATIVES FOR CETP INHIBITOR
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Page/Page column 39-40; 139, (2012/11/06)
The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF-211
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Page/Page column 296-297, (2009/10/21)
Chemical Compounds Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
3-Pyridinecarboxamide derivatives as HDL-cholesterol raising agents
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Page/Page column 15, (2008/06/13)
The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.