335030-38-1Relevant articles and documents
15-PGDH INHIBITOR
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Paragraph 0417-0419, (2021/12/23)
[Problem] To provide a compound having a 15-PGDH inhibitory effect. [Solution] A compound represented by general formula (1) or a pharmacologically acceptable salt thereof.
CARBOXAMIDES AS UBIQUITIN-SPECIFIC PROTEASE INHIBITORS
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, (2019/02/25)
The present disclosure relates to modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25, pharmaceutical compositions comprising the inhibitors, and methods of using the inhibitors. The modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25 can be useful in the treatment of cancers, among other ailments.
ALDOSTERONE SYNTHASE INHIBITORS
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, (2014/11/11)
The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
FAB I INHIBITORS
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, (2008/06/13)
Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.
Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK
Seefeld, Mark A.,Miller, William H.,Newlander, Kenneth A.,Burgess, Walter J.,DeWolf Jr., Walter E.,Elkins, Patricia A.,Head, Martha S.,Jakas, Dalia R.,Janson, Cheryl A.,Keller, Paul M.,Manley, Peter J.,Moore, Terrance D.,Payne, David J.,Pearson, Stewart,Polizzi, Brian J.,Qiu, Xiayang,Rittenhouse, Stephen F.,Uzinskas, Irene N.,Wallis, Nicola G.,Huffman, William F.
, p. 1627 - 1635 (2007/10/03)
Bacterial enoyl-ACP reductase (FabI) is responsible for catalyzing the final step of bacterial fatty acid biosynthesis and is an attractive target for the development of novel antibacterial agents. Previously we reported the development of FabI inhibitor 4 with narrow spectrum antimicrobial activity and in vivo efficacy against Staphylococcus aureus via intraperitoneal (ip) administration. Through iterative medicinal chemistry aided by X-ray crystal structure analysis, a new series of inhibitors has been developed with greatly increased potency against FabI-containing organisms. Several of these new inhibitors have potent antibacterial activity against multidrug resistant strains of S. aureus, and compound 30 demonstrates exceptional oral (po) in vivo efficacy in a S. aureus infection model in rats. While optimizing FabI inhibitory activity, compounds 29 and 30 were identified as having low micromolar FabK inhibitory activity, thereby increasing the antimicrobial spectrum of these compounds to include the FabK-containing pathogens Streptococcus pneumoniae and Enterococcus faecalis. The results described herein support the hypothesis that bacterial enoyl-ACP reductases are valid targets for antibacterial agents.