Abstract:
INTRODUCTION:The orexin system consists of two G-protein-coupled receptors, orexin 1 and orexin 2 and two endogenous ligands, orexin A and orexin B . It is evolutionarily highly conserved. It is involved in the promotion of wakefulness as well as in anxiety and addictive disorders. In addition, its activation via the Ox1 receptor triggers apoptosis in several cancer cell lines. Dual orexin receptor antagonists are successfully used to treat primary insomnia. The major open questions are now related to the clinical validation of Ox1 selective antagonists. A strong rationale exists for orexin agonism in the treatment of narcolepsy with cataplexy. Areas covered: 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. Expert opinion: The large number of patents shows the continuing interest in the orexin receptors as targets. The structural scope covered is narrow. Questions about novelty and inventiveness are evident. The additional information published on X-ray structures on both orexin receptors opens new ways of optimizing antagonists. It might also influence the efforts in the identification of orexin receptor agonists. Being potential treatments for narcolepsy with cataplexy.
journal_name
Expert Opin Ther Patjournal_title
Expert opinion on therapeutic patentsauthors
Boss C,Roch Cdoi
10.1080/13543776.2017.1344221subject
Has Abstractpub_date
2017-10-01 00:00:00pages
1123-1133issue
10eissn
1354-3776issn
1744-7674journal_volume
27pub_type
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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