856832-08-1Relevant academic research and scientific papers
JAK INHIBITOR
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Page/Page column 110-111, (2009/10/21)
A JAK inhibitor comprising, as an active ingredient, a nitrogen-containing heterocyclic compound represented by formula (I) {wherein W represents a nitrogen atom or -CH-; X represents -C (=O) - or -CHR4- (wherein R4 represents a hydrogen atom, or the like); R1 represents the formula described below [wherein Q1 represents-CR8-(wherein R8 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like); Q2 represents -NR15- (wherein R15 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like); and R5 and R6 may be the same or different and each represents a hydrogen atom, halogen, carboxy, substituted or unsubstituted lower alkyl, or the like], or the like; and R2 and R3 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like} or a pharmaceutically acceptable salt thereof.
7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: Design, synthesis, and biological activity
Hughes, Terry V.,Emanuel, Stuart L.,O'Grady, Harold R.,Connolly, Peter J.,Rugg, Catherine,Fuentes-Pesquera, Angel R.,Karnachi, Prabha,Alexander, Richard,Middleton, Steven A.
scheme or table, p. 5130 - 5133 (2009/05/26)
A novel series of 7-[1H-indol-2-yl]-2,3-dihydro-isoindol-1-ones designed to be inhibitors of VEGF-R2 kinase was synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, and initial SAR of the series are discussed.
SUBSTITUTED DIHYDRO-ISOINDOLONES USEFUL IN TREATING KINASE DISORDERS
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Page/Page column 70, (2008/06/13)
The present invention is directed to novel substituted dihydro-isoindolone compounds of formula (I): and forms thereof, wherein Ring A, X3, R1, R2, R3, R4 and R6 are as herein defined, and their synthesis and use as protein kinase inhibitors and interactions thereof.
DIARYLSULFONES AS 5-HT2A ANTAGONISTS
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Page/Page column 87, (2008/06/13)
Compounds of formula (I) are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.
