146257-03-6Relevant articles and documents
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors
Liang, Jun,Labadie, Sharada,Zhang, Birong,Ortwine, Daniel F.,Patel, Snahel,Vinogradova, Maia,Kiefer, James R.,Mauer, Till,Gehling, Victor S.,Harmange, Jean-Christophe,Cummings, Richard,Lai, Tommy,Liao, Jiangpeng,Zheng, Xiaoping,Liu, Yichin,Gustafson, Amy,Van der Porten, Erica,Mao, Weifeng,Liederer, Bianca M.,Deshmukh, Gauri,An, Le,Ran, Yingqing,Classon, Marie,Trojer, Patrick,Dragovich, Peter S.,Murray, Lesley
supporting information, p. 2974 - 2981 (2017/05/31)
A high-throughput screening (HTS) of the Genentech/Roche library identified a novel, uncharged scaffold as a KDM5A inhibitor. Lacking insight into the binding mode, initial attempts to improve inhibitor potency failed to improve potency, and synthesis of
FUSED HETEROCYCLIC COMPOUND
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Page/Page column 31, (2011/07/29)
The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same.
NEW BRADYKININ B1 ANTAGONISTS
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Page/Page column 200-201, (2010/04/03)
The invention relates to compounds of formula (I) where in R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof
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Page/Page column 77, (2010/11/26)
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
1 H-INDAZOLES, BENZOTHIAZOLES, 1,2-BENZOISOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND CHROMONES AND PREPARATION AND USES THEREOF
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Page/Page column 87-88, (2010/11/27)
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of -disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.