Substituted Benzofurans, Benzothiophenes, Benzoselenophenes and Indoles And Their Use as Tubulin Polymerisation Inhibitors
申请人:Bionomics Limited
公开号:EP2460793A1
公开(公告)日:2012-06-06
The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.
wherein;
X represents O, S, SO, SO2, Se, SeO, SeO2 or NR where R is selected from H, O, optionally substituted acyl, optionally substituted alkenyl, optionally substituted alkyl, optionally substituted aryl, optionally substituted cycloalkenyl, optionally substituted cycloalkyl, optionally substituted heteroaryl, optionally substituted heterocyclyl, and optionally substituted sulfonyl;
R1C represents C1-3 alkoxy, C1-3 alkylthio, C1-3 alkylamino, or C1-3 dialkylamino;
R1D represents hydroxy or amino;
L represents C=O, O, S, SO, SO2, Se, SeO, SeO2, C=NZ', or NR' where Z' is H, optionally substituted alkyl, optionally substituted aryl or optionally substituted amino; and where R' is selected from H, O, optionally substituted acyl, optionally substituted alkenyl, optionally substituted alkyl, optionally substituted aryl, optionally substituted cycloalkenyl, optionally substituted cycloalkyl, optionally substituted heteroaryl, optionally substituted heterocyclyl, or optionally substituted sulfonyl;
The other variables are as defined in the claims.
本发明一般涉及取代的苯并呋喃、苯并噻吩和吲哚,以及它们作为微管蛋白聚合抑制剂的用途。
其中
X代表O、S、SO、SO2、Se、SeO、SeO2或NR,其中R选自H、O、任选取代的酰基、任选取代的烯基、任选取代的烷基、任选取代的芳基、任选取代的环烯基、任选取代的环烷基、任选取代的杂芳基、任选取代的杂环基和任选取代的磺酰基;
R1C 代表 C1-3 烷氧基、C1-3 烷硫基、C1-3 烷氨基或 C1-3 二烷基氨基;
R1D 代表羟基或氨基;
L 代表 C=O、O、S、SO、SO2、Se、SeO、SeO2、C=NZ'或 NR',其中 Z'是 H、任选取代的烷基、任选取代的芳基或任选取代的氨基;R'选自 H、O、任选取代的酰基、任选取代的烯基、任选取代的烷基、任选取代的芳基、任选取代的环烯基、任选取代的环烷基、任选取代的杂芳基、任选取代的杂环基或任选取代的磺酰基;
其他变量如权利要求中所定义。