40971-95-7Relevant academic research and scientific papers
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine
Koltun, Dmitry O.,Parkhill, Eric Q.,Elzein, Elfatih,Kobayashi, Tetsuya,Notte, Gregory T.,Kalla, Rao,Jiang, Robert H.,Li, Xiaofen,Perry, Thao D.,Avila, Belem,Wang, Wei-Qun,Smith-Maxwell, Catherine,Dhalla, Arvinder K.,Rajamani, Sridharan,Stafford, Brian,Tang, Jennifer,Mollova, Nevena,Belardinelli, Luiz,Zablocki, Jeff A.
, p. 3202 - 3206 (2016)
We started with a medium throughput screen of heterocyclic compounds without basic amine groups to avoid hERG and β-blocker activity and identified [1,2,4]triazolo[4,3-a]pyridine as an early lead. Optimization of substituents for Late INa curre
ARYLACETAMIDE ANALOGS OF PIPERAZINE-[1,2,4]TRIAZOLO[4,3-B]PYRIDAZINES
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Paragraph 0092; 0096, (2021/12/31)
Provided are compounds with the following structure: Formula (I), and methods of making and using same. The methods of using the compounds may be methods for treating or prophylaxis of a cryptosporidium infection.
COMPOUNDS AND THEIR METHODS OF USE
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Page/Page column 132, (2018/06/12)
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography
Guetzoyan, Lucie,Ingham, Richard J.,Nikbin, Nikzad,Rossignol, Julien,Wolling, Michael,Baumert, Mark,Burgess-Brown, Nicola A.,Strain-Damerell, Claire M.,Shrestha, Leela,Brennan, Paul E.,Fedorov, Oleg,Knapp, Stefan,Ley, Steven V.
supporting information, p. 540 - 546 (2014/04/17)
A combination of conventional organic synthesis, remotely monitored flow synthesis and bioassay platforms, were used for the evaluation of novel inhibitors targeting bromodomains outside the well-studied bromodomain and extra terminal (BET) family, here e
DERIVATIVES OF 6-SUBSTITUTED TRIAZOLOPYRIDAZINES AS REV-ERB AGONISTS
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Page/Page column 42, (2013/04/13)
The present invention provides novel 6-substituted [1,2,4]triazolo[4,3-b]pyridazines that are agonists of Rev-Erb. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the activation of Rev-Erb has therapeutic effects, for instance in inflammatory and circadian rhythm-related disorders or cardiometabolic diseases.
FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
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Page/Page column 36, (2011/02/18)
The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
