Guangzhou Maxinovel Pharmaceuticals Co., Ltd.

Shanghai Yingli Pharmaceutical Co., Ltd

Beijing Maxinovel Pharmaceuticals Co., Ltd.

Tianzhi Wu

Nong Zhang

Yuguang Wang

Zusheng Xu

Min He

Qingrui Sun

Disclosed are a thienopyrimidine derivative and a preparation method therefor. Provided is a method for preparing a compound as shown in formula B, which method is characterized by comprising the following steps: subjecting a compound as shown in formula C with a compound as shown in formula K to a coupling reaction as shown below under a protective gas atmosphere, in a solvent and in the presence of a catalyst and a base, wherein the catalyst comprises a palladium compound and a phosphine ligand. The preparation method of the present invention can improve the yield of products, and reduce the production cost; in addition, the preparation method has simple reaction conditions and a strong process operability, which is beneficial to industrial production and the reduction of the generation of three wastes.

Thienopyrimidine derivative and preparation method therefor

Disclosed in the present invention are an aromatic vinyl or aromatic ethyl derivative, a preparation method therefor, an intermediate, a pharmaceutical composition, and an application. The aromatic vinyl or aromatic ethyl derivative in the present invention is as represented by general formula (I). The aromatic vinyl or aromatic ethyl derivative in the present invention has an obvious inhibitory effect on PD-1/PD-L1, is a very effective small-molecule PD-1/PD-L1 inhibitor, and can effectively alleviate or treat relevant diseases such as cancer. 

Aromatic vinyl or aromatic ethyl derivative, preparation method therefor, intermediate, pharmaceutical composition, and application

Disclosed are an aromatic acetylene or aromatic ethylene compound, an intermediate, a preparation method, a pharmaceutical composition and a use thereof. The aromatic acetylene or aromatic ethylene compound has a significant inhibitory effect on PD-1 and PD-L1, and can effectively relieve or treat cancers and other related diseases. 

Aromatic acetylene or aromatic ethylene compound, intermediate, preparation method, pharmaceutical composition and use thereof

Disclosed in the present invention is an aminopyrimidine five-membered heterocyclic compound, and an intermediate, preparation method, pharmaceutical composition and application thereof. The aminopyrimidine five-membered heterocyclic compound provided by the present invention has a significant antagonistic effect on adenosine A2A receptors, and may be used as an antagonist for adenosine A2A receptors to effectively relieve or treat immune tolerance, diseases of the central nervous system, inflammatory diseases and like related diseases, while the preparation method is simple. 

Aminopyrimidine five-membered heterocyclic compound, and intermediate, preparation method, pharmaceutical composition and application thereof

Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.

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Guangzhou, China

Tianzhi Wu