915307-78-7Relevant articles and documents
PIKFYVE KINASE INHIBITORS
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Page/Page column 206-207; 399, (2021/08/20)
The present invention relates to compounds useful as inhibitors of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) as well as their use for treating diseases and disorders associated with PIKfyve.
Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl) piperazin-l-yl]7-(6-methoxypyridin-3-yl)-l-(2-propoxyethyl)pyrido[3,4-b] pyrazin-2(lH)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5)
Hughes, Robert O.,Rogier, D. Joseph,Jacobsen, E. Jon,Walker, John K.,Maclnnes, Alan,Bond, Brian R.,Zhang, Lena L.,Yu, Ying,Zheng, Yi,Rumsey, Jeanne M.,Walgren, Jennie L.,Curtiss, Sandra W.,Fobian, Yvette M.,Heasley, Steven E.,Cubbage, Jerry W.,Moon, Joseph B.,Brown, David L.,Acker, Brad A.,Maddux, Todd M.,Tollefson, Mike B.,Mischke, Brent V.,Owen, Dafydd R.,Freskos, John N.,Molyneaux, John M.,Benson, Alan G.,Blevis-Ba, Rhadika M.
supporting information; experimental part, p. 2656 - 2660 (2010/08/22)
We recently described a novel series of aminopyridopyrazinones as PDE5 inhibitors. Efforts toward optimization of this series culminated in the identification of 3-[4-(2-hydroxyethyl)piperazin-l-yl]7-(6-methoxypyridin-3-yl)- l-(2-propoxyethyl)pyrido[3,4-è]pyrazin-2(l//)-one, which possessed an excellent potency and selectivity profile and demonstrated robust in vivo blood pressure lowering in a spontaneously hypertensive rat (SHR) model. Furthermore, this compound is brain penetrant and will be a useful agent for evaluating the therapeutic potential of central inhibition of PDE5. This compound has recently entered clinical trials.
Pyridine [3,4-b] Pyrazinones
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Page/Page column 29; 31-32; 34, (2008/06/13)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R2, R6A, R6B and R8 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, synthetic methods, and intermediates are also disclosed.