113082-27-2Relevant academic research and scientific papers
INHIBITORS OF CYCLIN-DEPENDENT KINASES
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, (2019/11/19)
Provided herein are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
AhR MODULATORS
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, (2019/08/29)
Provided herein are compounds, compositions and methods of using the compounds and compositions for the treatment of diseases modulated, as least in part, by AhR. The compounds are represented by formulae: (I) wherein the letters and symbols X1, X2, Z, R1b, R1c, R1d, R1e, R2a, R2b, R2c and R2d have the meanings provided in the specification.
OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF
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Paragraph 00215, (2017/07/04)
The invention relates to octahydropyrrolo [3, 4-c] pyrrole derivatives and uses thereof. Compounds and pharmaceutical compositions comprising the compounds provided herein are used for antagonizing orexin receptors. The invention also relates to processes for preparing the compounds and pharmaceutical compositions, and uses thereof in treating or preventing a disease related to orexin receptors.
Substituted piperazine compounds, application method and applications thereof
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Paragraph 0206; 0207; 0208; 0209, (2016/10/09)
The invention discloses substituted piperazine compounds, an application method and applications thereof. Specifically, the invention relates to piperazine compounds and pharmaceutical compositions thereof for inhibiting reuptake of 5-hydroxytryptamine and/or stimulation of 5-HT1A acceptor. The invention also relates to a preparation method of the compounds and pharmaceutical compositions thereof, and an application of the compounds and pharmaceutical compositions thereof in the treatment of central nervous system dysfunction.
NOVEL COMPOUNDS AND COMPOSITIONS FOR INHIBITION OF FASN
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Page/Page column 320, (2014/10/18)
The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
Enantioselective synthesis of diaryl aziridines using tetrahydrothiophene- based chiral sulfides as organocatalysts
Huang, Meng-Ting,Wu, Hsin-Yi,Chein, Rong-Jie
supporting information, p. 1101 - 1103 (2014/01/17)
This work describes catalytic and asymmetric aziridinations (15 examples, 95-98% ee) of benzyl bromide and imines via the imino Corey-Chaykovsky reaction using (thiolan-2-yl)diarylmethanol benzyl ether as an organocatalyst. The catalyst and analogues thereof were prepared through an expeditious and efficient synthetic route featuring a double nucleophilic substitution and Shi epoxidation as key steps.
HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 77, (2013/08/28)
Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
Discovery of the dual orexin receptor antagonist [(7 R)-4-(5-chloro-1,3- benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2 H -1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia
Cox, Christopher D.,Breslin, Michael J.,Whitman, David B.,Schreier, John D.,McGaughey, Georgia B.,Bogusky, Michael J.,Roecker, Anthony J.,Mercer, Swati P.,Bednar, Rodney A.,Lemaire, Wei,Bruno, Joseph G.,Reiss, Duane R.,Harrell, C. Meacham,Murphy, Kathy L.,Garson, Susan L.,Doran, Scott M.,Prueksaritanont, Thomayant,Anderson, Wayne B.,Tang, Cuyue,Roller, Shane,Cabalu, Tamara D.,Cui, Donghui,Hartman, George D.,Young, Steven D.,Koblan, Ken S.,Winrow, Christopher J.,Renger, John J.,Coleman, Paul J.
supporting information; experimental part, p. 5320 - 5332 (2010/10/20)
Despite increased understanding of the biological basis for sleep control in the brain, few novel mechanisms for the treatment of insomnia have been identified in recent years. One notable exception is inhibition of the excitatory neuropeptides orexins A and B by design of orexin receptor antagonists. Herein, we describe how efforts to understand the origin of poor oral pharmacokinetics in a leading HTS-derived diazepane orexin receptor antagonist led to the identification of compound 10 with a 7-methyl substitution on the diazepane core. Though 10 displayed good potency, improved pharmacokinetics, and excellent in vivo efficacy, it formed reactive metabolites in microsomal incubations. A mechanistic hypothesis coupled with an in vitro assay to assess bioactivation led to replacement of the fluoroquinazoline ring of 10 with a chlorobenzoxazole to provide 3 (MK-4305), a potent dual orexin receptor antagonist that is currently being tested in phase III clinical trials for the treatment of primary insomnia.
SUBSTITUTED DIAZEPAN OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 35; 36, (2009/06/27)
The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which orexin receptors are involved.
OXO BRIDGED DIAZEPAN OREXIN RECEPTOR ANTAGONISTS
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, (2009/01/20)
The present invention is directed to oxo bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
