- COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
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This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
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Page/Page column 177
(2020/07/31)
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- Dihydro quinazolinone derivative, as well as preparation method and application thereof
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The invention relates to the technical field of medicines, in particular to a new dihydro quinazolinone derivative with the following chemical structure general formula and pharmaceutically acceptablesalts thereof, (the formula is shown in the description.), A pharmacological experiment shows that the derivative or the salt provided by the invention has higher inhibitory activity on KRAS-PDE delta protein interaction, and has higher anti-tumor activity in vitro. The invention also provides a preparation method of the derivative and the pharmaceutically acceptable salts thereof, and application to preparatioin of a KRAS-PDE delta inhibitor and an anti-tumor drug.
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Paragraph 0117; 0120; 0121
(2018/07/30)
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- Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design
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Targeting KRAS-PDEδ protein-protein interactions with small molecules represents a promising opportunity for developing novel antitumor agents. However, current KRAS-PDEδ inhibitors are limited by poor cellular antitumor potency and the druggability of the target remains to be validated by new inhibitors. To tackle these challenges, herein, novel, highly potent KRAS-PDEδ inhibitors were identified by fragment-based drug design, providing promising lead compounds or chemical probes for investigating the biological functions and druggability of KRAS-PDEδ interaction.
- Chen, Long,Zhuang, Chunlin,Lu, Junjie,Jiang, Yan,Sheng, Chunquan
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supporting information
p. 2604 - 2610
(2018/03/26)
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- Superacid-promoted cyclodehydration leading to the imidazo[2,1-a] isoquinoline ring system
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A series of heterocycle-substituted acetophenones were prepared and reacted with the Bronsted superacid CF3SO3H (triflic acid=trifluoromethanesulfonic acid). Cyclodehydration provided aryl-substituted imidazo[2,1-a]isoquinolines and related products (28-85%, seven examples). A mechanism is proposed involving dicationic intermediates. Copyright
- Kethe, Anila,Naredla, Rajasekhar Reddy,Klumpp, Douglas A.
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p. 1457 - 1461
(2013/09/02)
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