Almorexant - CAS 871224-64-5
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Not Intended for Therapeutic Use. For research use only.
Orexin Receptor (OX Receptor)
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.
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1. Polycyclic indole alkaloid-type compounds by MCR
Wei Wang, Eberhardt Herdtweckb, Alexander Domling*. Chem. Commun., 2010, 46, 770–772
The Pictet–Spengler reaction (PS-2CR) is an intramolecular variant of the Mannich three component reaction and is very useful for the assembly of natural products and biopharmaceutical compounds. Several years ago we reported on the combination of the Ugi and PS-2CR2 and in the meantime the combination of MCRs and PS-2CR became quite popular to rapidly assemble molecular diversity. For example the orexin I antagonist almorexant currently undergoing phase III clinical trials for sleeping disorders has been discovered by a combination of the Ugi-3CR and a subsequent PS-2CR. Herein we wish to report on the first Ugi–PS combination where electron rich indolethylamine-derived isocyanides react in the Ugi–PS reactions with a diversity of bifunctional ketocarboxylic acid derivatives and orthogonally protected aminoacetaldehyde, to yield structurally intriguing polycyclic indole alkaloid-type compounds.
2. Discovery of HTL6641, a dual orexin receptor antagonist with differentiated pharmacodynamic Properties
John A. Christopher,* Sarah J. Aves, Jason Brown. Med. Chem. Commun.,2015, 6, 947–955
Several clinical studies have confirmed the therapeutic utility and safety of DORAs in the treatment of insomnia. Almorexant, developed by Actelion and subsequently licensed to GlaxoSmithKline, demonstrated efficacy in a phase II trial, increasing sleep efficiency in primary insomnia patients. Secondary end points, dose-dependent decreases in latency to persistent sleep (LPS) and wake after sleep onset (WASO), were also met. Although in 2009 almorexant was reported to have achieved its primary end point in an initial phase III trial, development of the molecule was discontinued in 2011 after a review of additional studies conducted to further establish the clinical profile, including tolerability. A second DORA from GSK, SB-649868, promoted sleep in male insomnia patients, but clinical development was subsequently stopped due to a preclinical safety observation in rats. Merck's suvorexant is the most advanced DORA, which was approved for use in adults with insomnia in August 2014. Additionally, Merck have progressed MK-6096 (filorexant) into phase II trials in patients with primary insomnia, and data from phase I trials of a further DORA from Actelion, ACT-462206 5, together with preclinical data, have recently been published. The clinical DORAs largely originate from high-throughput screening and it has been challenging to optimize properties such as lipophilicity, for example almorexant has c log P 5.9, which may be linked to the failure of several compounds due to safety issues unrelated to the mechanism of action.
3. Discovery and optimisation of 1-acyl-2-benzylpyrrolidines as potent dual orexin receptor antagonists
Jodi T. Williams,* John Gatfield, Catherine Roch. Med. Chem. Commun.,2015, 6, 1054–1064
Behaviourally, it significantly decreased home cage activity by 47% over the first 6 h of the night period following administration compared to vehicle-treated animals (−42% and −31% vs. vehicle for almorexant and suvorexant at 100 mg kg−1 po, respectively, p < 0.001 for 27 and almorexant and p < 0.01 for suvorexant, paired t-test). Electrophysiologically, it decreased significantly the time spent in active wake compared to vehicle-treated animals (−29%, −20% and −16% vs. vehicle for 27, almorexant, and suvorexant, respectively, p < 0.001 for 27 and almorexant and p < 0.01 for suvorexant, paired t-test). Compound 27 increased the time spent in quiet wake by 17% compared to vehicle-treated animals ( p < 0.05, paired t-test). However, the impact on this parameter is not predictive for sleep quality and depends on the compound tested (−8% for almorexant and +9% for suvorexant vs. vehicle, p < 0.05 and p > 0.05, respectively, paired t-test). As a consequence of the decrease in time spent in wake stages, the time spent in non-REM (rapid eye movement) sleep was significantly increased vs. vehicle over the 6 h period following administration, by +18% for 27, by +19%, for suvorexant and by +22% for almorexant ( p < 0.01 for 27 and suvorexant and p < 0.001 for almorexant, paired t-test). Finally, as observed with other DORAs, the time spent in REM sleep was also increased compared to vehicle-treated rats, significantly for 27 and almorexant (+84 and +50%, respectively, p < 0.01, paired t-test) and non-significantly for suvorexant (+20%, p > 0.05, paired t-test).
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CAS 871224-64-5 Almorexant

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