描述了平面聚吡啶的合成路线。从 2,5-二甲基吡啶开始,通过 2,5-二溴吡啶-3,6-二羧酸作为常用中间体,制备用于逐步增长聚合的两种吡啶单体。二元羧酸是制备用于逐步增长聚合的 A 和 B 组分的关键中间体。在制备用于缩聚的单体时,公开了敏感吡啶核上的几种新转化。双(Curtius) 重排,然后用叔丁醇捕获双(异氰酸酯) 会影响羰基部分向叔丁氧羰基保护的芳基二胺的高产率转化。在受保护的二氨基吡啶上进行锂-卤素交换,然后进行甲锡酰化,得到所需的二金属化二胺单体。用温和的铜酸盐或有机铜试剂处理吡啶(二溴二酰氯)得到吡啶(二溴二酮)。Pd/Cu 催化的二溴吡啶偶联与...
描述了平面聚吡啶的合成路线。从 2,5-二甲基吡啶开始,通过 2,5-二溴吡啶-3,6-二羧酸作为常用中间体,制备用于逐步增长聚合的两种吡啶单体。二元羧酸是制备用于逐步增长聚合的 A 和 B 组分的关键中间体。在制备用于缩聚的单体时,公开了敏感吡啶核上的几种新转化。双(Curtius) 重排,然后用叔丁醇捕获双(异氰酸酯) 会影响羰基部分向叔丁氧羰基保护的芳基二胺的高产率转化。在受保护的二氨基吡啶上进行锂-卤素交换,然后进行甲锡酰化,得到所需的二金属化二胺单体。用温和的铜酸盐或有机铜试剂处理吡啶(二溴二酰氯)得到吡啶(二溴二酮)。Pd/Cu 催化的二溴吡啶偶联与...
Thiazolidinedione compounds, compositions, and methods of inhibiting telomerase activity in vitro and treatment of telomerase mediated conditions or diseases ex vivo and in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer. Also disclosed are methods for assaying or screening for inhibitors of telomerase activity.
[EN] INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS<br/>[FR] INDAZOLES ET AZAINDAZOLES UTILISÉS EN TANT QU'INHIBITEURS DE LRRK2
申请人:ESCAPE BIO INC
公开号:WO2022155419A1
公开(公告)日:2022-07-21
The present invention is directed to indazole and azaindazole derivatives of formulae as shown below which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders such as Parkinson's disease.