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3-arylthioindole-2-carboxamide derivatives and analogs thereof as inhibitors of casein kinase i

一种酪蛋白激酶、甲酰胺的技术，应用在作为酪蛋白激酶Iε抑制剂的3－芳基硫代吲哚－2－甲酰胺衍生物及其类似物领域，能够解决蛋白稳定性降低等问题

Inactive Publication Date: 2007-09-19
AVENTIS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This suggests that phosphorylation of hPER1 causes a decrease in protein stability (Kessler, G.A. et al. (2000) NeuroReport, 11, 951-955)

Method used

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  • 3-arylthioindole-2-carboxamide derivatives and analogs thereof as inhibitors of casein kinase i
  • 3-arylthioindole-2-carboxamide derivatives and analogs thereof as inhibitors of casein kinase i
  • 3-arylthioindole-2-carboxamide derivatives and analogs thereof as inhibitors of casein kinase i

Examples

Experimental program
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Embodiment

[0173] The following examples are intended to illustrate the present invention in more detail, but do not limit the scope of the present invention in any way.

[0174] General Synthetic Method

[0175] Materials were purchased from suppliers and used without further purification unless otherwise stated. All reactions are performed under an inert atmosphere such as nitrogen or argon using anhydrous reagents and solvents. Flash chromatography was performed using EM Science Silica Gel 60 (40-63 mm) and using the solvent system described. TLC using 0.25 mm silica gel coated 60F-254 plates (EM) and using iodine vapor, UV light or stains such as KMnO 4 The solution develops color.

[0176] Infrared (IR) spectra were recorded on a Nexus 670 FTIR (Nicolet) spectrometer, the samples were prepared according to the instructions, and the results were expressed in wavenumbers (cm -1 )express. 1 H NMR spectra were recorded on Varian Gemini and / or mercury 300, Unity 400 or Unity plus an...

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Abstract

The present invention relates to methods with 3-arylthioindole-2-carboxamides, 5-substituted-3-arylthioindole-2-carboxamides and related analogues for treating a patient suffering from diseases or disorders of the central nervous system associated with the disturbance of the human circadian clock that are ameliorated by inhibition of casein kinase Ie activity such as , for example, mood disorders including major depressive disorder, bipolar I disorder and bipolar II disorder, and sleep disorders including circadian rhythm sleep disorders such as, for example, shift work sleep disorder, jet lag syndrome, advanced sleep phase syndrome and delayed sleep phase syndrome.

Description

technical field [0001] The present invention relates to methods of using 3-arylthioindole-2-carboxamides, 5-substituted-3-arylthioindole-2-carboxamides and related analogs, said compounds being useful as Inhibitors of human casein kinase Iε phosphorylation of the human clock protein phase (hPER), these compounds are therefore useful as medicaments, in particular for the treatment and / or prophylaxis of diseases and disorders related to the central nervous system. Background technique [0002] Rhythmic changes are shown in the behavior of many organisms, from single cells to humans. When the rhythm occurs continuously under constant conditions with a period of about one day and little dependence on temperature, then the rhythm is called "circadian rhythm" (Konopka, R.J. and Benzer, S. (1971) Proc . Nat. Acad. Sci. USA 68, 2112-2116). [0003] Circadian rhythms are generated by an endogenous biological pacemaker (circadian clock) and are present in most organisms including hu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61P25/00A61P25/24
CPCA61K31/404A61P25/00A61P25/20A61P25/24A61P43/00A61P9/00A61K31/403C07D209/42C07D403/06
Inventor W·A·小梅兹
Owner AVENTIS PHARMA INC
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