发明名称 N-(AMINOHETEROARYL)-1H-INDOLE-2-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
摘要 <p>The invention relates to compounds of general formula (I): in which X&lt;SUB&gt;1&lt;/SUB&gt; is a hydrogen or halogen atom or a (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;3&lt;/SUB&gt;)-alkylene, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-fluoroalkyl, cyano, C(O)NR&lt;SUB&gt;1&lt;/SUB&gt;R&lt;SUB&gt;2&lt;/SUB&gt;, nitro, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-thioalkyl, -S(O)-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkyl, -S(O)&lt;SUB&gt;2&lt;/SUB&gt;-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkyl, SO&lt;SUB&gt;2&lt;/SUB&gt;NR&lt;SUB&gt;1&lt;/SUB&gt;R&lt;SUB&gt;2,&lt;/SUB&gt; aryl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkylene, aryl or heteroaryl group, the aryl and the heteroaryl being optionally substituted; X&lt;SUB&gt;2&lt;/SUB&gt; is a hydrogen or halogen atom or a (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;3&lt;/SUB&gt;)-alkylene, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-fluoroalkyl, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkoxyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkylene-O-, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-fluoroalkoxyl, cyano, C(O)NR&lt;SUB&gt;1&lt;/SUB&gt;R&lt;SUB&gt;2&lt;/SUB&gt;, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-thioalkyl, -S(O)-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkyl, -S(O)&lt;SUB&gt;2&lt;/SUB&gt;-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkyl, SO&lt;SUB&gt;2&lt;/SUB&gt;NR&lt;SUB&gt;1&lt;/SUB&gt;R&lt;SUB&gt;2&lt;/SUB&gt;, aryl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkylene, aryl or heteroaryl group, the aryl and the heteroaryl being optionally substituted; X&lt;SUB&gt;3&lt;/SUB&gt; and X&lt;SUB&gt;4&lt;/SUB&gt; are, independently of one another, a hydrogen or halogen atom or a (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;3&lt;/SUB&gt;)-alkylene, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-fluoroalkyl, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkoxyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkylene-O-, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-fluoroalkoxyl, cyano, C(O)NR&lt;SUB&gt;1&lt;/SUB&gt;R&lt;SUB&gt;2&lt;/SUB&gt;, nitro, NR&lt;SUB&gt;1&lt;/SUB&gt;R&lt;SUB&gt;2&lt;/SUB&gt;, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-thioalkyl, -S(O)-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkyl, -S(O)&lt;SUB&gt;2&lt;/SUB&gt;-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkyl, SO&lt;SUB&gt;2&lt;/SUB&gt;NR&lt;SUB&gt;1&lt;/SUB&gt;R&lt;SUB&gt;2&lt;/SUB&gt;, NR&lt;SUB&gt;3&lt;/SUB&gt;COR&lt;SUB&gt;4&lt;/SUB&gt;, NR&lt;SUB&gt;3&lt;/SUB&gt;SO&lt;SUB&gt;2&lt;/SUB&gt;R&lt;SUB&gt;5&lt;/SUB&gt;, aryl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkylene, aryl or heteroaryl group, the aryl and the heteroaryl being optionally substituted; Z&lt;SUB&gt;1&lt;/SUB&gt;, Z&lt;SUB&gt;2&lt;/SUB&gt;, Z&lt;SUB&gt;3&lt;/SUB&gt; and Z&lt;SUB&gt;4&lt;/SUB&gt; are, independently of one another, a nitrogen atom or a C(R&lt;SUB&gt;6&lt;/SUB&gt;) group; n is equal to 0, 1, 2 or 3; Y is an optionally substituted aryl or heteroaryl; Ra and Rb are, independently of one another, a hydrogen atom or a (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)&lt;SUB&gt;-&lt;/SUB&gt;alkyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;3&lt;/SUB&gt;)-alkylene, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-fluoroalkyl, hydroxyl, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkoxyl, (C&lt;SUB&gt;3&lt;/SUB&gt;-C&lt;SUB&gt;7&lt;/SUB&gt;)-cycloalkyl-(C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-alkylene-O-, (C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt;)-fluoroalkoxyl, aryl or heteroaryl group, wherein Ra and Rb may be optionally substituted; in the form of a base or an addition salt with an acid, and also in the form of a hydrate or of a solvate. Process for the preparation thereof and therapeutic use.</p>
申请公布号 WO2008012418(A1) 申请公布日期 2008.01.31
申请号 WO2007FR01250 申请日期 2007.07.20
申请人 SANOFI AVENTIS;DUBOIS, LAURENT;EVANNO, YANNICK;MALANDA, ANDRE 发明人 DUBOIS, LAURENT;EVANNO, YANNICK;MALANDA, ANDRE
分类号 C07D401/12;A61K31/435;A61P3/00;A61P11/00;A61P13/00;A61P15/00;A61P17/00;A61P25/00;A61P29/00;A61P31/00 主分类号 C07D401/12
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