2-substituted aromatic ring-pyrimidine derivative and preparation and application thereof

US10822327B2 · kind B2 · utility

Assignees

• ZHEJIANG UNIVERSITY · CN
• SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES · CN

Inventors

• Tao Liu · Shanghai, CN
• Jia-He Li · Cockeysville, US
• Yongzhou Hu · Zhejiang, CN
• Yubo Zhou · Shanghai, CN
• Xiaowu Dong · Zhejiang, CN
• Anhui Gao · Shanghai, CN
• Pinrao Song · Zhejiang, CN
• Peipei Wang · Shanghai, CN
• Lexian Tong · Zhejiang, CN
• Xiaobei Hu · Shanghai, CN
• Mingbo Su · Shanghai, CN

Key dates

• Filing date: Nov 8, 2017
• Grant date: Nov 3, 2020
• Expiry date: Nov 8, 2037

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A 2-substituted aromatic ring-pyrimidine derivative as shown in a general formula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chk1 kinase inhibitory activity and are promising Chk1 inhibitors. The compounds can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal.