1314396-07-0Relevant articles and documents
5-AMINOPYRAZOLE CARBOXAMIDE DERIVATIVE AS BTK INHIBITOR AND PREPARATION METHOD AND PHARMACEUTICAL COMPOSITION THEREOF
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Paragraph 0059, (2019/04/16)
The present application discloses novel 5-aminopyrazole carboxamide compounds as shown in formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof. In addition, the present application further discloses a method for the preparation of the compounds, a pharmaceutical composition comprising a compound of the invention and the use of the compounds.
Bis(difluoromethyl)trimethylsilicate Anion: A Key Intermediate in Nucleophilic Difluoromethylation of Enolizable Ketones with Me3SiCF2H
Chen, Dingben,Ni, Chuanfa,Zhao, Yanchuan,Cai, Xian,Li, Xinjin,Xiao, Pan,Hu, Jinbo
supporting information, p. 12632 - 12636 (2016/10/31)
A pentacoordinate bis(difluoromethyl)silicate anion, [Me3Si(CF2H)2]?, is observed for the first time by the activation of Me3SiCF2H with a nucleophilic alkali-metal salt and 18-crown-6. Further study on its reactivity by tuning the countercation effect led to the discovery and development of an efficient, catalytic nucleophilic difluoromethylation of enolizable ketones with Me3SiCF2H by using a combination of CsF and 18-crown-6 as the initiation system. Mechanistic investigations demonstrate that [(18-crown-6)Cs]+[Me3Si(CF2H)2]?is a key intermediate in this catalytic reaction.
THIOETHER-PIPERIDINYL OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 34, (2015/07/07)
The present invention is directed to thioether-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the thioether-piperidinyl compounds described herein in the potential treatment or prevention
Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties
Kuduk, Scott D.,Skudlarek, Jason W.,Dimarco, Christina N.,Bruno, Joseph G.,Pausch, Mark H.,O'brien, Julie A.,Cabalu, Tamara D.,Stevens, Joanne,Brunner, Joseph,Tannenbaum, Pamela L.,Garson, Susan L.,Savitz, Alan T.,Harrell, Charles M.,Gotter, Anthony L.,Winrow, Christopher J.,Renger, John J.,Coleman, Paul J.
, p. 2488 - 2492 (2015/06/02)
Abstract Antagonism of orexin receptors has shown clinical efficacy as a novel paradigm for the treatment of insomnia and related disorders. Herein, molecules related to the dual orexin receptor antagonist filorexant were transformed into compounds that w
2-PYRIDYLOXY-3-SUBSTITUTED-4-NITRILE OREXIN RECEPTOR ANTAGONISTS
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, (2014/05/24)
The present invention is directed to 2-pyridyloxy-3-substituted-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-substituted-4-nitrile 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.
Substituted Imidazopyridines as HDM2 Inhibitors
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Paragraph 0798, (2014/07/08)
The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
2-PYRIDYLOXY-4-ETHER OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 35, (2014/09/29)
The present invention is directed to 2-pyridyloxy-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention o
BRUTON'S TYROSINE KINASE INHIBITORS
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Page/Page column 150, (2014/05/24)
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I)
2-PYRIDYLOXY-4-NITRILE OREXIN RECEPTOR ANTAGONISTS
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, (2013/05/08)
The present invention is directed to 2-pyridyloxy-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyl-oxy-4-nitrile 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.