Indolin-2-ones with High in Vivo Efficacy in a Model for Multiple Sclerosis

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J. Med. Chem., 48 (17), 5412 -5414, 2005. 10.1021/jm0504151 S0022-2623(05)00415-2
Web Release Date: July 27, 2005

Indolin-2-ones with High in Vivo Efficacy in a Model for Multiple Sclerosis

Laëtitia Bouérat,* Jef Fensholdt, Xifu Liang, Sophie Havez, Simon F. Nielsen, Jens R. Hansen, Simon Bolvig, and Christina Andersson*

LEO Pharma A/S, Industriparken, DK-2750 Ballerup, Denmark

Received May 2, 2005

Abstract:

The known KDR inhibitor SU5416 and several analogues of the indolin-2-one family were surprisingly found to be highly efficacious in the EAE model, an established model for multiple sclerosis. The high in vivo effect could be correlated to in vitro inhibition of the pro-inflammatory cytokine IL-2. Activity following po administration was obtained with several analogues and via the use of prodrugs.

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