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CAPLUS COPYRIGHT 2012 ACS
||Method for producing 2-(2-amino-pyrimidin-4-yl)-1H-indole-5-carboxylic acid derivatives
||Griffioen, Gerard; Van Dooren, Tom; Rojas de la Parra, Veronica; Marchand, Arnaud; Allasia, Sara; Kilonda, Amuri; Chaltin, Patrick
||Katholieke Universiteit Leuven, K.U. Leuven R&D, Belg.; Remynd
||PCT Int. Appl., 134pp. CODEN: PIXXD2
Title compds. I [E independently = CR3 or N; R1, R3, R4 and R6 independently = H, halo, OH, etc.; R2 = H, alkyl, alkenyl or alkynyl; R5 = halo, OH, SH, etc.; n = 1-2; Y1-5 independently = CH, N, NH, etc.; ring B = aryl, cycloalkyl, cycloalkenyl, cycloalkynyl or heterocycle; m = 0-5; each R8 independently = H, halo, alkyl, etc.], and their stereoisomers, enantiomers, tautomers or pharmaceutically acceptable salts, are prepared. Thus, e.g., II was prepared by Suzuki reaction of N-[2-(5-chloro-1H-indol-3-yl)ethyl]-4-iodobenzamide with 4-hydroxyphenylboronic acid. II inhibited LDH leakage of M17-TAU P301L cells with EC50 value of 7 nM. The invention compds. are useful as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurol. disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic alpha-synuclein amyloidogenesis.
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