Chinese Academy of Sciences

Shanghai Institute of Materia Medica, Chinese Acad

Shanghai Acebright Pharmaceuticals Co., Ltd.

Zilan Song

Jian Ding

Ao Zhang

Meiyu Geng

Zehong Miao

Hua Xie

Xiajuan Huan

Li Xing

Yu Xue

Linjiang Tong

Yi Chen

Jing Ai

Xia Peng

Shanshan Song

Zhoulong Fan

Wangting Gu

Chuanhuizi Chen

Na Ye

Pingyuan Wang

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

Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.

Substituted amino six-membered nitric heterocyclic ring compound and preparation 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

A class of substituted triazolopiperazine compounds represented by formula (I), tautomers, enantiomers, diastereomers, racemates, metabolites, metabolic precursors, and pharmaceutically acceptable salts, esters, prodrugs or hydrate thereof, a preparation methods therefor, intermediates and a use thereof in the preparation of drugs for prevention and treatment of diseases associated with PARP including various ischemic diseases, neurodegenerative diseases and cancers. 

Substituted triazolopiperazine PARP inhibitor, preparation method therefor and use thereof

Provided is a piperazinotriazole compound represented by general formula I or a pharmaceutically acceptable salt, stereoisomer, tautomer or hydrate thereof. Also provided are a pharmaceutical composition comprising the compound, a method for preparing the compound and a method of use thereof as a high-selectivity poly(adenosine diphosphate-ribose)polymerase-1 (PARP-1) inhibitor in the preparation of drugs for the prevention and/or treatment of PARP-related diseases. 

Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors

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Shanghai, China

Zilan Song