136540-80-2Relevant academic research and scientific papers
6,5-BICYCLIC OCTAHYDROPYRROLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS
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, (2016/07/05)
The present invention is directed to 6,5-bicyclic octahydropyrrolopyridine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS
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, (2016/07/05)
The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
BRIDGED DIAZEPANE OREXIN RECEPTOR ANTAGONISTS
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, (2016/06/14)
The present invention is directed to bridged diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
PIPERIDINE ISOXAZOLE AND ISOTHIAZOLE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 46-47, (2016/05/19)
The present invention is directed to piperidine isoxazole and isothiazole orexin compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
OXAZOLE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 36; 37, (2015/02/25)
The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential 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.
OXAZOLE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 42, (2015/02/25)
The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential 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.
Efficient Intramolecular General Acid Catalysis of Enol Ether Hydrolysis. Hydrogen-bonding Stabilisation of the Transition State for Proton Transfer to Carbon
Kirby, Anthony J.,Williams, Nicholas H.
, p. 643 - 648 (2007/10/02)
The intrinsically low efficiency of intramolecular general acid-base catalysis is enhanced when the proton transfer generates a strong intramolecular hydrogen bond.This principle is shown to apply to proton transfer to carbon: the carboxy groups of methyl vinyl ethers 3E and 3Z derived from 2-carboxyphenylacetaldehyde act as general acids to catalyse the hydrolysis of the neighbouring enol ether groups with effective molarities (EM) of about 300 and 2000 M, respectively.The solvent deuterium isotope effects confirm that the usual mechanism for enol ether hydrolysis is operative.In this system the oxocarbocation intermediate is trapped by the neighbouring carboxylate group to give the acylal 6, rather than the formal product of hydrolysis.
Efficient Intramolecular General Acid Catalysis of Vinyl Ether Hydrolysis by the Neighbouring Carboxylic Acid Group
Kirby, Anthony J.,Williams, Nicholas H.
, p. 1643 - 1644 (2007/10/02)
Intramolecular catalysis by the CO2H group of the hydrolysis of E-1-methoxy-2-(2-carboxyphenyl)ethylene 5, shows an effective molarity of almost 300 M, the highest measured for intramolecular proton transfer to carbon.
