在合成具有关键官能团基序的基本结构单元的长期探索中,光化学在最近已经全面确立了其吸引力。氨基醇不仅功能多样,而且在化合物的生物活性领域中普遍存在。我们开发了实验室稳定的双功能试剂,然后可以通过能量转移(EnT)光催化直接从原料烯烃中获取报道较少的γ-氨基醇。通过激进的布鲁克重排的干预,设计的跨烯烃 1,3-连接成为可能,该重排发生在我们的试剂的 EnT 介导的均裂下游。实验机制研究和详细计算研究(DFT)的结合表明了自由基链传播反应途径。
The invention relates to a novel group of compounds of Formula (I) or salts thereof:
wherein Y, Z
1
, Z
2
, R
1
, R
4
, R
5
and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
The invention relates to a novel group of compounds of Formula (I) or salts thereof:
wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
本发明涉及一组新型的式 (I) 化合物或其盐类:
其中 Y、Z1、Z2、R1、R4、R5 和 n 如说明书所述,可用于治疗或预防通过蛋白激酶 B (PKB)介导的疾病或病症,如癌症。本发明还涉及包含所述化合物的药物组合物、使用所述化合物治疗由PKB介导的疾病的方法以及制备式(I)化合物的方法。
Protein Kinase B Inhibitors
申请人:AstraZeneca AB
公开号:US20180312516A1
公开(公告)日:2018-11-01
The invention relates to a novel group of compounds of Formula (I) or salts thereof:
wherein Y, Z
1
, Z
2
, R
1
, R
4
, R
5
and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
PROTEIN KINASE B INHIBITORS
申请人:AstraZeneca AB
公开号:US20200239483A1
公开(公告)日:2020-07-30
The invention relates to a novel group of compounds of Formula (I) or salts thereof:
wherein Y, Z
1
, Z
2
, R
1
, R
4
, R
5
and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).