370879-78-0Relevant articles and documents
ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
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Page/Page column 49, (2011/08/04)
The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
TETRAHYDROTHIAZOLOPYRIDINE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
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Page/Page column 37, (2010/09/17)
The present invention relates to compounds (I) useful as inhibitors of PBK, particularly of PI3K gamma. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders
TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS
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Page/Page column 45, (2010/12/18)
The present invention relates to compounds useful as inhibitors of P13K, particularly of P13Kgamma. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of several diseases, such as cancer and autoimmune diseases.
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.
Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of β-secretase
Congreve, Miles,Aharony, David,Albert, Jeffrey,Callaghan, Owen,Campbell, James,Carr, Robin A. E.,Chessari, Gianni,Cowan, Suzanna,Edwards, Philip D.,Frederickson, Martyn,McMenamin, Rachel,Murray, Christopher W.,Patel, Sahil,Wallis, Nicola
, p. 1124 - 1132 (2007/10/03)
Fragment-based lead discovery has been successfully applied to the aspartyl protease enzyme β-secretase (BACE-1). Fragment hits that contained an aminopyridine motif binding to the two catalytic aspartic acid residues in the active site of the enzyme were the chemical starting points. Structure-based design approaches have led to identification of low micromolar lead compounds that retain these interactions and additionally occupy adjacent hydrophobic pockets of the active site. These leads form two subseries, for which compounds 4 (IC50 = 25 μM) and 6c (IC50 = 24 μM) are representative. In the latter series, further optimization has led to 8a (IC50 = 690 nM).
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.