250275-15-1Relevant articles and documents
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
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Page/Page column 86, (2016/12/16)
Compounds of formula (I) that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
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Page/Page column 139; 140, (2015/09/23)
Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for
Novel Octahydropyrrolo[3,4- c ]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate
Letavic, Michael A.,Bonaventure, Pascal,Carruthers, Nicholas I.,Dugovic, Christine,Koudriakova, Tatiana,Lord, Brian,Lovenberg, Timothy W.,Ly, Kiev S.,Mani, Neelakandha S.,Nepomuceno, Diane,Pippel, Daniel J.,Rizzolio, Michele,Shelton, Jonathan E.,Shah, Chandra R.,Shireman, Brock T.,Young, Lana K.,Yun, Sujin
, p. 5620 - 5636 (2015/08/03)
The preclinical characterization of novel octahydropyrrolo[3,4-c]pyrroles that are potent and selective orexin-2 antagonists is described. Optimization of physicochemical and DMPK properties led to the discovery of compounds with tissue distribution and d
Selective Ligands for the Neuronal Nicotinic Receptors and Uses Thereof
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Page/Page column 10, (2009/12/04)
The present application describes selective ligands of formula (I) for neuronal nicotinic receptors (NNRs), more specifically for the α4β2 NNR subtype, compositions thereof, and methods of using the same, wherein X, R1, X, R2, R3, L1, m, n, p, and q are defined in the specification.
Octahydropyrrolo[3,4-c]pyrrole: A diamine scaffold for construction of either α4β2 or α7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity
Bunnelle, William H.,Tietje, Karin R.,Frost, Jennifer M.,Peters, Dan,Ji, Anguo,Li, Tao,Scanio, Marc J. C.,Shi, Lei,Anderson, David J.,Dyhring, Tino,Gr?nlien, Jens H.,Ween, Hilde,Thorin-Hagene, Kirsten,Meyer, Michael D.
experimental part, p. 4126 - 4141 (2010/03/02)
A series of 5-(pyridine-3-yl)octahydropyrrolo[3,4-c]pyrroles have been prepared that exhibit high affinity to α4β2 and/or α7 nicotinic acetylcholine receptors (nAChRs). Simple substitution patterns have been identified that allow construction of ligands that are highly selective for either nAChR subtype. The effects of substitution on subtype selectivity provide some insight into the differences in the ligand binding domains of the α4β2 and R7 receptors, especially in regions removed from the cation binding pocket.
Diazabicyclic central nervous system active agents
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, (2008/06/13)
Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.