TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF

    公开(公告)号:US20120135958A1

    公开(公告)日:2012-05-31

    申请号:US13386827

    申请日:2010-07-23

    CPC分类号: C07D401/10 C07D401/12

    摘要: The invention relates to compounds of formula (I), where: A is a bond, an oxygen, or an —CH2— group; Ar1 is a phenyl or heteroaryl group; Ar2 is a phenyl, heteroaryl, or heterocycloalkyl group; R1a,b,c and R2a,b,c are hydrogen or halogen, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally, substituted by one or more halogen atoms, or a —OR5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, —O-halogenoalkyl, oxo, —CO-alkyl, —CO-alkyl-NR6R7, —CO-halogenoalkyl, —COOR5, alkyl-COOR5, —O-alkyl-COOR5, —SO2-alkyl, —SO2-cycloalkyl, —SO2-alkyl-cycloalkyl, —SO2-alkyl-OR5, —SO2-alkyl-COOR5, —SO2-alkyl-NR6R7, —SO2-halogenoalkyl, alkyl-SO2-alkyl, —SO2—NR6R7, —SO2-alkyl-O-alkyl-OR5, —CONR6R7, -alkyl-CONR6R7, or -alkyl-NR6R7 group, or further R1a, R1b, and R1c are bonded to R2a, R2b, R2c, respectively, and to the carbon atom having same, and are -alkyl-O—; R3 is a hydrogen atom or an alkyl group; R4 is a hydrogen or halogen atom or a cyano, —OR5, hydroxyalkyl, —COOR5, —NR6R7, ONR6R7, —SO2-alkyl, SO2—NR6R7, —NR6—COOR5, —NR6—COR5, or —CO—NR6-alkyl-OR5 group; R5, R6, and R7 are a hydrogen, or an alkyl or alkyl-phenyl group; and R8 is an alkyl, alkyl-Si(alkyl)3, —SO2-alkyl-Si(alkyl)3, phenyl, alkoxy-imino group, or alkyl-cycloalkyl group optionally substituted by one or more halogen atoms or one or more hydroxyl or hydroxyl-alkyl groups; or R8 and R9, together with the carbon atoms to which they are bonded, form a cycloalkyl group optionally substituted by one or more halogen atoms or one or more carboxy groups; and R9 is a hydrogen atom or an alkyl group; with the proviso that, when R8 is an alkyl group, it is bonded onto the Ar2 silicon atom. The invention also relates to a method for preparing same and to the therapeutic use thereof.