250275-15-1Relevant articles and documents
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
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, (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.
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
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.