Chinese Academy of Sciences

Shanghai Institute of Materia Medica, Chinese Acad

Yu Xue

Jian Ding

Meiyu Geng

Ao Zhang

Zilan Song

Hua Xie

Linjiang Tong

Li Xing

The present invention relates to a pyrimido[5,4-b]pyrrolizin compound represented by general formula I, an optical isomer thereof, a preparation method therefor, a pharmaceutical composition containing same, and a use thereof. The compound according to the present invention has good inhibitory activity on the kinase BTK at both the molecular level and the cellular level. Meanwhile, the compound also has good anti-tumor activity and pharmacokinetic properties in vivo.

Pyrimido[5,4-b]pyrrolizin compound, optical isomer thereof, preparation method therefor and use thereof

The present disclosure relates to a Pyrimido[5,4-b]indolizine or pyrimido[5,4-b]pyrrolizine compound, preparation method thereof and use thereof. The compounds of the present invention have good inhibitory activities against BTK at the molecular and cellular levels. Importantly, the compounds of the present invention have low activity against Ramos cells of normal human B lymphoma cells, and have high activity against BTK-sensitive human diffuse large B lymphoma TMD8 cells, indicating that these type of compounds with novel structural are highly selective, off-target phenomenon and corresponding side effects are low. Thus it is a selective inhibitor of BTK with development potential. 

Pyrimido[5,4-B]indolizine or pyrimido[5,4-B]pyrrolizine compound, preparation method and use thereof

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Shanghai, China

Yu Xue