1207853-72-2Relevant academic research and scientific papers
INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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, (2020/05/28)
The present invention provides various compositions, including compounds of Formula (I) or (la), or a species thereof, and pharmaceutically acceptable salts, solvates (e.g., hydrates), stereoisomer, tautomers, isotopic and other specified forms thereof. Also provided are methods (or uses) and kits involving the compounds or pharmaceutically acceptable compositions containing them for treating or preventing a disease (e.g., a proliferative disease such as cancer) in a subject. Administration of a compound or pharmaceutical composition described herein is expected to inhibit cyclin-dependent kinase 7 (CDK7), and thereby, induce apoptosis in tumor cells in the subject.
Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists
Skudlarek, Jason W.,DiMarco, Christina N.,Babaoglu, Kerim,Roecker, Anthony J.,Bruno, Joseph G.,Pausch, Mark A.,O'Brien, Julie A.,Cabalu, Tamara D.,Stevens, Joanne,Brunner, Joseph,Tannenbaum, Pamela L.,Wuelfing, W. Peter,Garson, Susan L.,Fox, Steven V.,Savitz, Alan T.,Harrell, Charles M.,Gotter, Anthony L.,Winrow, Christopher J.,Renger, John J.,Kuduk, Scott D.,Coleman, Paul J.
, p. 1364 - 1370 (2017/03/08)
In an ongoing effort to explore the use of orexin receptor antagonists for the treatment of insomnia, dual orexin receptor antagonists (DORAs) were structurally modified, resulting in compounds selective for the OX2R subtype and culminating in the discovery of 23, a highly potent, OX2R-selective molecule that exhibited a promising in vivo profile. Further structural modification led to an unexpected restoration of OX1R antagonism. Herein, these changes are discussed and a rationale for selectivity based on computational modeling is proposed.
FUSED HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 58; 59, (2016/07/27)
Fused heteroaryl derivative compounds which are antagonists of orexin receptors are provided. The compounds can be used in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. Also provided is a composition which comprises the compound can be use to prevent or treat such diseases in which orexin receptors are involved.
2-AMINO-3-ESTER-PYRIDYL OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 33, (2015/07/07)
The present invention is directed to 2-amino-3-ester pyridyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-amino-3-ester pyridyl compounds described herein in the potential treatment or preven
PIPERIDINYLOXY LACTONE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 56, (2015/07/07)
The present invention is directed to piperidinyloxy lactone compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyloxy lactone compounds described herein in the potential treatment or preventi
2-PYRIDYLAMINO-4-NITRILE-PIPERIDINYL OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 32; 33, (2014/06/23)
The present invention is directed to 2-pyridylamino-4-nitrile-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridylamino-4-nitrile-piperidinyl compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
