1409947-13-2Relevant academic research and scientific papers
Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function
Ashcraft, Luke,Bergnes, Gustave,Chuang, Chihyuan,Collibee, Scott E.,Durham, Nickie,Garard, Marc,Gardina, Jeffrey,Hartman, James,Hinken, Aaron,Hwee, Darren T.,Jamison, Chris R.,Lu, Kevin,Lu, Pu-Ping,Malik, Fady I.,Marquez, Anna,Morgan, Bradley P.,Morgans, David,Muci, Alexander,Romero, Antonio,Schaletzky, Julia,Valkevich, Ellen,Wang, Wenyue,Warrington, Jeffrey,Xu, Donghong,Yao, Bing
supporting information, p. 14930 - 14941 (2021/11/01)
The discovery of reldesemtiv, a second-generation fast skeletal muscle troponin activator (FSTA) that increases force production at submaximal stimulation frequencies, is reported. Property-based optimization of high throughput screening hit 1 led to compounds with improved free exposure and in vivo muscle activation potency compared to the first-generation FSTA, tirasemtiv. Reldesemtiv demonstrated increased muscle force generation in a phase 1 clinical trial and is currently being evaluated in clinical trials for the treatment of amyotrophic lateral sclerosis.
CERTAIN HETEROCYCLES, COMPOSITIONS THEREOF, AND METHODS FOR THEIR USE
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Page/Page column 29; 54, (2012/12/13)
Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
