34843-84-0Relevant academic research and scientific papers
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia
Brown, Scott,Campbell, John E.,Dedic, Nina,Heffernan, Michele L. R.,Herman, Lee W.,Hewitt, Michael C.,Hopkins, Seth C.,Jones, Philip G.,Koblan, Kenneth S.,Shao, Liming,Xie, Linghong
supporting information, (2021/12/17)
Ulotaront (SEP-363856) is a trace-amine associated receptor 1 (TAAR1) agonist with 5-HT1A receptor agonist activity in Phase 3 clinical development, with FDA Breakthrough Therapy Designation, for the treatment of schizophrenia. TAAR1 is a G-protein-coupled receptor (GPCR) that is expressed in cortical, limbic, and midbrain monoaminergic regions. It is activated by endogenous trace amines, and is believed to play an important role in modulating dopaminergic, serotonergic, and glutamatergic circuitry. TAAR1 agonism data are reported herein for ulotaront and its analogues in comparison to endogenous TAAR1 agonists. In addition, a human TAAR1 homology model was built around ulotaront to identify key interactions and attempt to better understand the scaffold-specific TAAR1 agonism structure-activity relationships.
Compound as potassium channel modulator
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Paragraph 0698; 0700; 0701; 0702, (2018/07/30)
The invention relates to a compound as a potassium channel modulator, which is a compound of a formula (I) or a pharmaceutically acceptable salt thereof. The compound or the pharmaceutically acceptable salt thereof is effective for curing and preventing diseases and symptoms influenced by the activity of potassium ion channels.
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility
Cao, Xufeng,Sun, Zhaoshuan,Cao, Yongbing,Wang, Ruilian,Cai, Tongkai,Chu, Wenjing,Hu, Wenhao,Yang, Yushe
supporting information, p. 3687 - 3706 (2014/05/20)
Triazoles with fused-heterocycle nuclei were designed and evaluated for their in vitro activity on the basis of the binding mode of albaconazole using molecular docking, along with SAR of antifungal triazoles. Tetrahydro-[1,2,4] triazolo[1,5-a]pyrazine and tetrahydro-thiazolo[5,4-c]pyridine nuclei were preferable to the other four fused-heterocycle nuclei investigated. Potent in vitro activity, broad spectrum and better water solubility were attained when triazoles containing nitrogen aromatic heterocycles were attached to these two nuclei. The most potent compounds 27aa and 45x, with low hERG inhibition and hepatocyte toxicity, both exhibited excellent activity against Candida, Cryptococcus, and Aspergillus spp., as well as selected fluconazole-resistant strains. A high water-soluble compound 58 (the disulfate salt of 45x) displayed unsatisfactory in vivo activity because of its poor PK profiles. Mice infected with C.alb. SC5314 and C.alb. 103 (fluconazole-resistant strain) and administered with 27aa displayed significantly improved survival rates. 27aa also showed favorable pharmacokinetic (PK) profiles.
NOVEL INDOLE AND PYRROLOPYRIDINE AMIDES
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Page/Page column 46, (2012/09/11)
The present invention relates to indole and pyrrolopyridine amide derivatives of formula (I) wherein R1, R 2, R 3, U, V, W, X, Y, Z and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
NOVEL MCH RECEPTOR ANTAGONISTS
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Page/Page column 24, (2008/06/13)
The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
NOVEL MCH RECEPTOR ANTAGONISTS
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Page/Page column 33, (2008/06/13)
The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
Thieno tetrahydropyridines useful as class III antiarrhythmic agents
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, (2008/06/13)
This invention relates to thieno tetrahydropyridine and isoquinoline derivative compounds which are useful as antiarrhythmic agents, pharmaceutical compositions comprising such compounds, novel intermediates for their preparation and their methods of use. More particularly these thieno tetrahydropyridine and isoquinoline derivative compounds have been demonstrated to increase the effective refractory period (ERP) of isolated perfused cardiac tissue in vitro.
