172739-04-7Relevant 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.
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
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, (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
Practical asymmetric synthesis of RO5114436, a CCR5 receptor antagonist
Huang, Xiaojun,O'Brien, Erin,Thai, Felicia,Cooper, Gary
, p. 592 - 599 (2011/07/08)
A practical asymmetric synthesis of a 3,7-diazabicyclo[3.3.0]octane derivative (1), a representative of a new class of potent CCR5 receptor antagonists, is described. The benzylamine stereogenic center of 1 was introduced by a ruthenium-catalyzed asymmetric reductive amination using (R)-MeOBIPHEP as ligand. Aldehyde 4, prepared by Parikh-Doering oxidation, was used without workup in the reductive amination reaction, which not only simplified the process but also overcame the instability of 4. The 3,7-diazabicyclo[3.3.0]octane core was obtained by a [3 + 2] cycloaddition.
Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists
Rotstein, David M.,Melville, Chris R.,Padilla, Fernando,Cournoyer, Dick,Lee, Eun K.,Lemoine, Remy,Petersen, Ann C.,Setti, Lina Q.,Wanner, Jutta,Chen, Lijing,Filonova, Lubov,Loughhead, David G.,Manka, Jason,Lin, Xiao-Fa,Gleason, Shelley,Sankuratri, Surya,Ji, Changhua,deRosier, Andre,Dioszegi, Marianna,Heilek, Gabrielle,Jekle, Andreas,Berry, Pamela,Mau, Cheng-I,Weller, Paul
scheme or table, p. 3116 - 3119 (2010/10/02)
Starting with a high-throughput screening lead, a novel series of CCR5 antagonists was developed utilizing an information-based approach. Improvement of pharmacokinetic properties for the series was pursued by SAR exploration of the lead template. The synthesis, SAR and biological profiles of the series are described.
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.
Diazabicyclooctane derivatives having selective 5-HT1Dalpha agonist activity
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, (2008/06/13)
PCT No. PCT/GB96/02310 Sec. 371 Date Mar. 9, 1998 Sec. 102(e) Date Mar. 9, 1998 PCT Filed Sep. 19, 1996 PCT Pub. No. WO97/11945 PCT Pub. Date Apr. 3, 1997A class of 3-substituted 3,7-diazabicyclo[3.3.0]octane derivatives, further substituted at the 7-posi