88485-78-3Relevant academic research and scientific papers
Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators
Barnes, Keith D.,Buckle, Ronald N.,Chen, Xinchao,Herr, R. Jason,Johnson, Graham,Lin, Juinn H.,Mayhew, Nicholas J.,Mobley, William C.,Nguyen, Phuong,Paquette, William D.,Rynearson, Kevin D.,Sakwa, Samuel A.,Tanzi, Rudolph E.,Wagner, Steven L.,Yang, Jinhai
supporting information, (2020/09/22)
The evolution of gamma-secretase modulators (GSMs) through the introduction of novel heterocycles with the goal of aligning activity for reducing the levels of Aβ42 and properties consistent with a drug-like molecule are described. The insertion of a methoxypyridine motif within the tetracyclic scaffold provided compounds with improved activity for arresting Aβ42 production as well as improved properties, including solubility. In vivo pharmacokinetic analysis demonstrated that several compounds within the novel series were capable of crossing the BBB and accessing the therapeutic target. Treatment with methoxypyridine-derived compound 64 reduced Aβ42 levels in the plasma of J20 mice, in addition to reducing Aβ42 levels in the plasma and brain of Tg2576 mice.
BIARYL COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 198-199, (2011/04/13)
Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
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Page/Page column 38, (2010/10/19)
Disclosed herein are compounds of formula (I) wherein Ring A and R1 are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions are also disclosed.
NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
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Page/Page column 46; 47, (2010/04/23)
Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Pyridyloxyindoles Inhibitors of VEGF-R2 and Use Thereof for Treatment of Disease
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Page/Page column 53-54, (2010/06/22)
The invention relates to novel organic compounds of formula (I), and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.
NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
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Page/Page column 35, (2009/05/29)
The present invention relates compounds of formula (I) wherein A and R1 are as defined in the specification, pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions.
PYRAZOLE-ISOQUINOLINE UREA DERIVATIVES AS P38 KINASE INHIBITORS
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Page/Page column 16, (2008/06/13)
The present invention provides kinase inhibitors of Formula (I) wherein R1, R2, and X are as described herein, or a pharmaceutically acceptable salt thereof.
KINASE INHIBITORS
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Page/Page column 27, (2010/11/27)
The present invention provides kinase inhibitors of Formula (I). Wherein R1, R2, X and Z are as described herein, or a pharmaceutically acceptable salt thereof.
