- A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties
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The complex etiology of Alzheimer's disease has initiated a quest for multi-target ligands to address the multifactorial causes of this neurodegenerative disorder. In this context, we designed dual-acting 5-HT6 receptor (5-HT6R) anta
- Canale, Vittorio,Grychowska, Katarzyna,Kurczab, Rafa?,Ryng, Mateusz,Keeri, Abdul Raheem,Sata?a, Grzegorz,Olejarz-Maciej, Agnieszka,Koczurkiewicz, Paulina,Drop, Marcin,Blicharz, Klaudia,Piska, Kamil,P?kala, El?bieta,Janiszewska, Paulina,Krawczyk, Martyna,Walczak, Maria,Chaumont-Dubel, Severine,Bojarski, Andrzej J.,Marin, Philippe,Popik, Piotr,Zajdel, Pawe?
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supporting information
(2020/09/21)
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- Deprotection of N-BOC compounds
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Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.
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Page/Page column 5-6
(2009/08/18)
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- Deprotection of N-BOC compounds
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Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.
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Page/Page column 9
(2009/07/10)
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- Novel practical deprotection of N-Boc compounds using fluorinated alcohols
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The thermolytic deprotection of N-Boc compounds was accomplished using TFE (2,2,2-trifluoroethanol) or HFIP (hexafluoroisopropanol) as solvents. Even though the cleavage of the t-butylcarbamate (Boc) group can be achieved at solvent reflux temperature, the deprotection process was significantly accelerated under microwave-assisted conditions. The practicality of this methodology was demonstrated on alkyl, aryl, and heteroaromatic N-Boc-amines. Copyright Taylor & Francis Group, LLC.
- Choy, Jason,Jaime-Figueroa, Saul,Jiang, Laurence,Wagner, Paul
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p. 3840 - 3853
(2008/12/23)
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- 4' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, R6, B, D, E, G, Q, x and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 19-20
(2009/01/24)
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- 1-Aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands
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The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
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- 4,5,6 and 7-indole and indoline derivatitives, their preparation and use
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A substituted 4-, 5-, 6-, and 7-indole derivative of Formula (I) wherein A is a group having formula (IIA), (IIB), (IIC) wherein X, U, Y, R3to R12, Z, W, n and m are as defined above. The compounds are potent serotonin reuptake inhib
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- 1-Aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands
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The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
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- Novel compounds, their use and preparation
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The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.
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