26663-42-3Relevant articles and documents
Discovery, synthesis and biological characterization of a series of: N -(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1 H -pyrazol-5-yl)acetamide ethers as novel GIRK1/2 potassium channel activators
Alnouti, Yazen,Aretz, Christopher D.,Chhonker, Yashpal S.,Dhuria, Nikilesh V.,Du, Yu,Gautam, Nagsen,Hopkins, Corey R.,Kumar, Sushil,Lesiak, Lauren,Sharma, Swagat,Weaver, C. David
, p. 1366 - 1373 (2021/09/28)
The present study describes the discovery and characterization of a series of N-(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1H-pyrazol-5-yl)acetamide ethers as G protein-gated inwardly-rectifying potassium (GIRK) channel activators. From our previous lead optimization efforts, we have identified a new ether-based scaffold and paired this with a novel sulfone-based head group to identify a potent and selective GIRK1/2 activator. In addition, we evaluated the compounds in tier 1 DMPK assays and have identified compounds that display nanomolar potency as GIRK1/2 activators with improved metabolic stability over the prototypical urea-based compounds. This journal is
PF74 and its novel derivatives stabilize hexameric lattice of HIV-1 mature-like particles
?kach, Kry?tof,Dostálková, Al?běta,Flegel, Martin,Hadravová, Romana,Hrabal, Richard,K?í?ová, Ivana,Kaufman, Filip,Ruml, Tomá?,Rumlová, Michaela
, (2020/04/27)
A major structural retroviral protein, capsid protein (CA), is able to oligomerize into two different hexameric lattices, which makes this protein a key component for both the early and late stages of HIV-1 replication. During the late stage, the CA prote
NITROGEN-CONTAINING FUSED RING COMPOUNDS FOR USE AS CRTH2 ANTAGONISTS
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Paragraph 0099, (2014/11/13)
The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.
NITROGEN-CONTAINING FUSED RING COMPOUNDS AS CRTH2 ANTAGONISTS
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Paragraph 0224, (2014/10/16)
The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase
Gomez, Robert,Jolly, Samson,Williams, Theresa,Tucker, Thomas,Tynebor, Robert,Vacca, Joe,McGaughey, Georgia,Lai, Ming-Tain,Felock, Peter,Munshi, Vandna,Destefano, Daniel,Touch, Sinoeun,Miller, Mike,Yan, Youwei,Sanchez, Rosa,Liang, Yuexia,Paton, Brenda,Wan, Bang-Lin,Anthony, Neville
, p. 7344 - 7350 (2012/02/04)
Next generation NNRTIs are sought which possess both broad spectrum antiviral activity against key mutant strains and a high genetic barrier to the selection of new mutant viral strains. Pyridones were evaluated as an acyclic conformational constraint to
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-β: Synthesis, biological activity, and cardiovascular safety
Zhang, Han-Cheng,Derian, Claudia K.,McComsey, David F.,White, Kimberly B.,Ye, Hong,Hecker, Leonard R.,Li, Jian,Addo, Michael F.,Croll, Diane,Eckardt, Annette J.,Smith, Charles E.,Li, Quan,Cheung, Wai-Man,Conway, Bruce R.,Emanuel, Stuart,Demarest, Keith T.,Andrade-Gordon, Patricia,Damiano, Bruce P.,Maryanoff, Bruce E.
, p. 1725 - 1728 (2007/10/03)
Novel indolylindazolylmaleimides were synthesized and examined for kinase inhibition. We identified low-nanomolar inhibitors of PKC-β with good to excellent selectivity vs other PKC isozymes and GSK-3β. In a cell-based functional assay, 8f and 8i effectiv
Orally Active Aldose Reductase Inhibitors: Indazoleacetic, Oxopyridazineacetic, and Oxopyridopyridazineacetic Acid Derivatives
Mylari, Banavara L.,Zembrowski, William J.,Beyer, Thomas A.,Aldinger, Charles E.,Siegel, Todd W.
, p. 2155 - 2162 (2007/10/02)
Benzothiazole side chains featured in zopolrestat (1a) and its congeners were incorporated into oxophthalazineacetic acid replacements, including indazole, pyridazinone, and pyridopyridazinone with a pendant acetic acid moiety.Potent aldose reductase inhi
