Orexin receptor antagonists – a patent review (2010 to August 2014)

@article{Boss2014OrexinRA,
  title={Orexin receptor antagonists – a patent review (2010 to August 2014)},
  author={Christoph Boss},
  journal={Expert Opinion on Therapeutic Patents},
  year={2014},
  volume={24},
  pages={1367 - 1381}
}
  • C. Boss
  • Published 19 November 2014
  • Medicine
  • Expert Opinion on Therapeutic Patents
Introduction: The orexin (hypocretin) system is an evolutionarily conserved neuropeptide-G-protein-coupled receptor system, consisting of two neuropeptides the orexin-A and the orexin-B peptides as well as two receptors the orexin-1 and the orexin-2 receptors. The orexin system is crucially involved in the regulation of the circadian rhythm, states of wakefulness and arousal and the modulation of emotions and has attracted the interest of many researchers which resulted in an enormous amount of… 
Orexin research: patent news from 2016
TLDR
The patent applications from Thomson Reuters Integrity Database added in 2016 are summarized and discussed together with the most important findings published in the scientific literature to show the continuing interest in the orexin receptors as targets.
An overview of the orexinergic system in different animal species.
TLDR
This review highlights the distinct variabilities in the morphophysiological aspects of the orexinergic system in the vertebrate animals, mammals and non-mammals, its presence in other brain-related structures, including its involvement in ageing and neurodegenerative diseases.
Recent trends in orexin research--2010 to 2015.
  • C. Boss, C. Roch
  • Chemistry, Medicine
    Bioorganic & medicinal chemistry letters
  • 2015
TLDR
The Orexin system, consisting of the two orexin-neuropeptides and two G-protein-coupled receptors, is as well involved in reward and addictive behaviors.
Substituted cyclopentanes, tetrahydrofurans and pyrrolidines as orexin-1-receptor antagonists for treatment of various CNS disorders (WO2015/055994; WO2015/124932; WO2015/124934)
TLDR
Structurally, the building blocks used to prepare the compounds are reminiscent of other orexin antagonist programs recently disclosed in the literature, however, the templates used are novel in the orexIn antagonist field and are probably the key feature for the selectivity of the derivatives towards the Orexin-1 receptor.
Emerging role of orexin antagonists in insomnia therapeutics: An update on SORAs and DORAs.
TLDR
The present review focuses on the orexin peptides and receptors signifying their physiological profile as well as the development of Orexin receptor antagonists as novel strategies in sleep medicine.
Discovery of HTL6641, a dual orexin receptor antagonist with differentiated pharmacodynamic properties
A novel series of potent, selective, and orally efficacious dual antagonists of the orexin receptors has been investigated, resulting in the identification of lead compound 27 (HTL6641).
1,2-Benzisoxazole compounds: a patent review (2009 – 2014)
  • Y. Uto
  • Medicine
    Expert opinion on therapeutic patents
  • 2015
TLDR
This review puts emphasis on the recent progress in therapeutically attractive benzisoxazole derivatives especially 1,2-benzis oxazoles, which were published in the patent literature between 2009 and 2014, and the main focus is on atypical antipsychotics and potential therapeutic treatments for other CNS disorders.
Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist.
TLDR
The design, synthesis, characterization, and structure-activity relationships (SARs) of novel orexin receptor antagonists are reported and various modifications made to the core structure of a previously developed compound resulted in compounds with improved chemical and pharmacological profiles.
Arcuate Nucleus Orexin-A Signaling Alleviates Cisplatin-Induced Nausea and Vomiting Through the Paraventricular Nucleus of the Hypothalamus in Rats
TLDR
A novel neurobiological circuit from the ARC to the PVN that might provide a potential target for the prevention and treatment of cisplatin-induced nausea and vomiting is revealed.
Orexin A and Central Precocious Puberty
TLDR
Maternally expressed gene 3 (MEG3) is an imprinted long non-coding RNAs (LncRNAs) which is highly expressed in the brain and pituitary gland, which may involve in pituitaries hyperplasia of CPP.
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