AbstractExtensive research has gone into proposing a promising link between melatonin administration and attenuation of epileptic activity, the majority of which suggest its propensity as an antiseizure with antioxidant and neuroprotective properties. In the past few years, a number of studies highlighting the association of the melatonergic ligands with epilepsy have also emerged. In this context, our review is based on discussing the recent studies and various mechanisms of action that the said category of drugs exhibit in the context of being therapeutically viable antiseizure drugs. Our search revealed several articles on the four major drugs i.e. melatonin, agomelatine, ramelteon and piromelatine along with other melatonergic agonists like tasimelteon and TIK-301. Our review is suggestive of antiseizure effects of both melatonin and its analogues; however, extensive research work is still required to study their implications in the treatment of persons with epilepsy. Further evaluation of melatonergic signaling pathways and mechanisms may prove to be helpful in the near future and might prove to be a significant advance in the field of epileptology.

19 Oct 2018·Current Pharmaceutical DesignQ4 · MEDICINE

Circadian Rhythm and Melatonin in the Treatment of Depression

Q4 · MEDICINE

Review

Author: Su, Kuan-Pin ; Lin, Yi-Wen ; Su, Huanxing ; Satyanarayanan, Senthil Kumaran

Background: Circadian rhythm disruption underlies the pathophysiology of psychiatric disorders, especially depression. Both pharmacological and non-pharmacological strategies affecting endogenous circadian rhythms have been developed with specificity to alter the circadian dysfunction. The current management strategy with antidepressants is far from being satisfactory in addressing this issue. In recent years, attempts at discovering new antidepressants focused on a melatonergic system which is known to be altered in depression have led to a potential option for treatment of depression. Methods: We reviewed all recently published relevant articles on melatonin and its analogues to look for their implication in the treatment of circadian rhythm disruption and depression. Results: Melatonin, a pleiotropic regulator molecule and its analogues (ramelteon, agomelatine, TIK-301, Neu- P11 and tasimelteon) have been observed to resynchronize the circadian rhythm and some were said to alleviate depressive symptoms in depressed subjects. Conclusion: This review focuses on substantial advances in the melatonin-based chronobiologic intervention and its responses in the treatment of depression.

07 Sep 2018·Organic LettersQ1 · CHEMISTRY

Synthesis of Chiral Tryptamines via a Regioselective Indole Alkylation

Q1 · CHEMISTRY

Article

Author: Xu, Jie ; Zhang, Haiming ; Wolfard, Jens ; Chung, Cheol K.

A practical synthesis of chiral tryptamines from simple, unprotected indoles has been developed. Indole nucleophiles prepared with MeMgCl in the presence of CuCl reacted with chiral cyclic sulfamidates almost exclusively at the C³-position of indole to form a variety of α- and/or β-substituted chiral tryptamines in good yield with excellent regioselectivity. The utility of this simple alkylation process has been demonstrated with the practical synthesis of two biologically active targets, cipargamin and TIK-301, which were completed in three steps, starting from the corresponding indole starting materials.

100 Deals associated with LY-156735

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Indication	Highest Phase	Country/Location	Organization	Date
Sleep Initiation and Maintenance Disorders	Phase 2	-	Phase 2 Discovery, Inc.	-
Sleep Initiation and Maintenance Disorders	Phase 2	-	Tikvah Therapeutics, Inc.	-
Sleep Initiation and Maintenance Disorders	Phase 2	-	Eli Lilly & Co.	-
Sleep Wake Disorders	Phase 2	US	Tikvah Therapeutics, Inc.	-

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