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    • 1. 发明申请
    • DERIVATIVES OF 1,5-DIPHENYL PYRROLE-3-CARBOXAMIDE, PREPARATION THEREOF AND USE OF SAME AS CANNABINOID CB1 RECEPTOR ANTAGONISTS
    • 1,5-二苯基吡咯-3-羧酰胺的衍生物,其制备及其作为CANNABINOID CB1受体拮抗剂的用途
    • WO2009141532A3
    • 2010-02-11
    • PCT/FR2009000535
    • 2009-05-07
    • SANOFI AVENTISBARTH FRANCISBICHON DANIELCONGY CHRISTIANRINALDI-CARMONA MURIELLE
    • BARTH FRANCISBICHON DANIELCONGY CHRISTIANRINALDI-CARMONA MURIELLE
    • C07D401/12A61K31/4025A61P1/00A61P3/00A61P25/00A61P29/00C07D401/14
    • C07D401/14C07D401/06
    • The subject of the invention is compounds corresponding to the formula (I): in which: - A represents an unsubstituted or substituted (C1-C6)alkylene group; - R1 represents a hydrogen atom or an unsubstituted or substituted (C1-C4)alkyl group; - R2 represents a homopiperidin-1-yl, piperidin-1-yl, pyrrolidin-1-yl or azetidin-1-yl radical, or an amino (C1-C6)alkyl group; - or R1 and R2, together with the nitrogen atom to which they are attached, constitute a piperazin-1-yl, 1,4-diazepan-1-yl, homopiperidin-1-yl, piperidin-1-yl, pyrrolidin-1-yl or azetidin-1-yl radical; - R3, R4, R5, R6, R7, R8 each independently represent a hydrogen atom, a halogen atom, a -CN, -S(O)nR14, or -OS(O)nR14 group, or an unsubstituted or substituted (C1-C6)alkyl group; - R9 represents an -OR12, -CN, -CO2H, NR12R13,-CONR12R13, -NR15COR12, -CONHNH2, -CONHOH, -CONHSO2R14, -S(O)nR14,-SO2NR12R13, -NR18SO2R14, or -NR15SO2NR12R13 group, or an aromatic heterocycle. The present invention also relates to the methods of preparation and the therapeutic applications of the compounds of formula (I) as cannabinoid CB1 receptor antagonists.
    • 本发明的主题是对应于式(I)的化合物:其中:A表示未取代或取代的(C1-C6)亚烷基; -R 1表示氢原子或未取代或取代的(C 1 -C 4)烷基; -R 2表示高哌啶-1-基,哌啶-1-基,吡咯烷-1-基或氮杂环丁烷-1-基或氨基(C 1 -C 6)烷基; - 或R 1和R 2与它们所连接的氮原子一起构成哌嗪-1-基,1,4-二氮杂环庚烷-1-基,高哌啶-1-基,哌啶-1-基,吡咯烷-1-基 - 基或氮杂环丁烷-1-基; -R 3,R 4,R 5,R 6,R 7,R 8各自独立地表示氢原子,卤素原子,-CN,-S(O)nR 14或-OS(O)nR 14基团,或未取代或取代的(C1 -C 6)烷基; -R 9表示-OR 12,-CN,-CO 2 H,NR 12 R 13,-CONR 12 R 13,-NR 15 COR 12,-CONHNH 2,-CONHOH,-CONHSO 2 R 14,-S(O)n R 14,-SO 2 NR 12 R 13,-NR 18 SO 2 R 14或-NR 15 SO 2 NR 12 R 13基团, 芳香杂环。 本发明还涉及式(I)化合物作为大麻素CB1受体拮抗剂的制备方法和治疗应用。