September 17, 2012

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The following patent record is from the CAplusSM database.


Patent Number: WO 2012080220
Title: Method for producing 2-(2-amino-pyrimidin-4-yl)-1H-indole-5-carboxylic acid derivatives
Inventor(s): Griffioen, Gerard; Van Dooren, Tom; Rojas de la Parra, Veronica; Marchand, Arnaud; Allasia, Sara; Kilonda, Amuri; Chaltin, Patrick
Patent Assignee(s): Katholieke Universiteit Leuven, K.U. Leuven R&D, Belg.; Remynd
Source: PCT Int. Appl., 134pp. CODEN: PIXXD2
Language: English


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.

Please note:  Abstracts for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced the abstract using additional information found in the patent.


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