Guangdong Lewwin Pharmaceutical Research Institute Co., Ltd.

Guangdong Cs-lewwin Drug Research Co., Ltd.

Xingshu Li

Wei Yang

Jianmin Guo

Xinzi Chen

The present invention discloses a method of treating tumor using a novel pyrimidine derivative. It is demonstrated through the tests on anti-tumor activity at the cellular level (tumor cells expressed with c-Met) that, through the introduction of a chiral structure in the molecule, the introduction of an isotope of hydrogen (deuterium) at the sites that are prone to metabolism in the molecule, and the introduction of atoms or groups such as sulfur, selenium and sulfoxide in the molecule, the compounds of the invention have excellent anti-tumor activities, and the stabilities of the anti-tumor compounds are significantly improved.

Pyrimidine derivative and preparation process and use thereof

The present invention discloses a novel pyrimidine derivative and a preparation process thereof and a use thereof in anti-tumor drugs. It is demonstrated through the tests on anti-tumor activity at the cellular level (tumor cells expressed with c-Met) that, through the introduction of a chiral structure in the molecule, the introduction of an isotope of hydrogen (deuterium) at the sites that are prone to metabolism in the molecule, and the introduction of atoms or groups such as sulfur, selenium and sulfoxide in the molecule, the compounds of the invention have excellent anti-tumor activities, and the stabilities of the anti-tumor compounds are significantly improved.

The present invention discloses a pyrimidine derivative containing one deuterium atom, a preparation process thereof and a use thereof. It is demonstrated through in vivo and in vitro animal experiments that the antitumor activity of the pyrimidine derivative containing one deuterium atom provided in the disclosure is significantly superior to that of the positive drug Tepotinib, and the preparation process is simple and low in cost.

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Guangdong, China

Xingshu Li