Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Shanghai Institute of Pharmaceutical Industry

China State Institute of Pharmaceutical Industry

Taizhou Mabtech Pharmaceutical Co., Ltd.

Shanghai Guojian Bio-tech Institute

Yajun Guo

Hao Wang

Yu Huang

Zhedong Yuan

Hanbin Shan

Xiong Yu

Xueyan Zhu

Meng Guo

Mingtong Hu

Jing Ma

Weizhu Qian

Bohua Li

Duzheng Wang

Sheng Hou

A bifunctional fusion protein targeting CD47 and PD-L1, which belongs to the field of biomedicine and solves the problems that anti-PD-1/PD-L1 treatment has poor effect on low immunogenic tumors and anti-CD47 treatment has poor targeting properties. The fusion protein consists of a CD47-binding moiety and a PD-L1-binding moiety linked by means of a disulfide bond, can block both the binding of CD47 to SIRPa and the binding of PD-L1 to PD-1, not only activating macrophage phagocytosis of tumor cells and promoting antigen presentation in innate immunity, but also promoting tumor-specific T cell activation in acquired immunity, and has lower hematological toxicity. The fusion protein has better anti-tumor efficacy and hematological safety than anti-PD-L1 or anti-CD47 therapy alone, and animals from which a tumor has disappeared after the treatment of the fusion protein produce immunity against re-inoculation of the same tumor cell.

Bifunctional fusion protein targeting CD47 and PD-L1

Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises: reacting a compound 3 with a C-Calkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production. 

Method for preparing dabigatran etexilate intermediate, and intermediate compound

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Shanghai, China

Yajun Guo