- CONDENSED HETEROCYCLIC 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, A, B, D, E, G, Q, Ar, n, m, and p 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 77
(2010/04/03)
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- ACYCLIC 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, Q, G, Ar, m, 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 54-55
(2010/03/02)
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- 4'-AMINO CYCLIC 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): formula (I) wherein Cy is selected from formula (Il) and wherein R1, R2, R3, Q, G, Ar, m, n and p 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 95
(2010/04/06)
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- 3' 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 Q, R1, R4, m and Ar 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 113
(2009/04/25)
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- Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[ω-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition
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A series of novel bicyclic 1-heteroaryl-4-[ω-(1H-indol-3-yl)alkyl] piperazines was synthesized and evaluated on binding to dopamine D2 receptors and serotonin reuptake sites. This class of compounds proved to be potent in vitro dopamine D2 receptor antagonists and in addition were highly active as serotonin reuptake inhibitors. Some key representatives showed potent pharmacological in vivo activities after oral dosing in both the antagonism of apomorphine-induced climbing and the potentiation of 5-HTP-induced behavior in mice. On the basis of the preclinical data, 8-{4-[3-(5-fluoro-1H- indol-3-yl)propyl]piperazin-1-yl}-4H-benzo[1,4]oxazin-(R)-2-methyl-3-one (45c, SLV314) was selected for clinical development. In vitro and in vivo studies revealed that 45c has favorable pharmacokinetic properties and a high CNS plasma ratio. Molecular modeling studies showed that the bifunctional activity of 45c can be explained by its ability to adopt two different conformations fitting either the dopamine D2 receptor pharmacophore or the serotonin transporter pharmacophore.
- Smid, Pieter,Coolen, Hein K. A. C.,Keizer, Hiskias G.,Van Hes, Rolf,De Moes, Jan-Peter,Den Hartog, Arnold P.,Stork, Bob,Plekkenpol, Rob H.,Niemann, Leonarda C.,Stroomer, Cees N. J.,Tulp, Martin Th. M.,Van Stuivenberg, Herman H.,McCreary, Andrew C.,Hesselink, Mayke B.,Herremans, Arnoud H. J.,Kruse, Chris G.
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p. 6855 - 6869
(2007/10/03)
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- Synthesis and structure-activity relationships of novel fungal chitin synthase inhibitors
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A novel Candida albicans chitin synthase 1 (CaChs1) inhibitor, RO-41-0986 (1) was discovered by random screening. Systematic modification led to the identification of a highly potent CaChs1 inhibitor, RO-09-3024 (2), having strong antifungal activity against Candida spp. in vitro. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Masubuchi, Kazunao,Taniguchi, Mikio,Umeda, Isao,Hattori, Kazuo,Suda, Hitomi,Kohchi, Yasunori,Isshiki, Yoshiaki,Sakai, Toshiya,Kohchi, Masami,Shirai, Michio,Okabe, Hisafumi,Sudoh, Masayuki,Yamazaki, Toshikazu,Shimma, Nobuo
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p. 1459 - 1462
(2007/10/03)
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