171178-45-3Relevant articles and documents
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.
, p. 2656 - 2660 (2010)
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.
Carbon-11 and Fluorine-18 Radiolabeled Pyridopyrazinone Derivatives for Positron Emission Tomography (PET) Imaging of Phosphodiesterase-5 (PDE5)
Chekol, Rufael,Gheysens, Olivier,Ahamed, Muneer,Cleynhens, Jan,Pokreisz, Peter,Vanhoof, Greet,Janssens, Stefan,Verbruggen, Alfons,Bormans, Guy
, p. 486 - 496 (2017)
The cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type 5 (PDE5) plays an important role in various pathologies including pulmonary arterial hypertension and cardiomyopathy. PDE5 represents an important therapeutic and/or prognostic targ
SULFONYL-SUBSTITUTED BICYCLIC COMPOUND WHICH ACTS AS ROR INHIBITOR
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Paragraph 0376; 0377, (2020/08/16)
Provided is a sulfonyl-substituted bicyclic compound (A) which acts as a RORγ inhibitor, said compound has good RORγ inhibitory activity and is expected to be used for treating diseases mediated by a RORγ receptor in mammals.