2-arylbenzofuran-7-formamide compounds, preparation method and use thereof

US9533965B2 · kind B2 · utility

Assignees

• SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES · CN
• CISEN PHARMACEUTICAL CO., LTD · CN

Inventors

• Chunhao Yang · Shanghai, CN
• Zehong Miao · Shanghai, CN
• Jian Ding · Shanghai, CN
• Meng Wang · Taichung, TW
• Jinxue He · Shanghai, CN
• Cun Tan · Shanghai, CN
• Yi Chen · Shanghai, CN

Key dates

• Filing date: Jan 14, 2013
• Grant date: Jan 3, 2017
• Expiry date: Apr 8, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D407/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Provided in the present invention are a 2-arylbenzofuran-7-formamide compound as shown in general formula I or a pharmacologically or physiologically acceptable salt thereof, a preparation method thereof and use thereof in preparing anti-tumour drugs, wherein R1 and R2 are each independently hydrogen, straight or branched chained C1-C4 alkyl, C3-C4 cycloalkyl or saturated 5- or 6-membered heterocyclyl containing oxygen or nitrogen; or R1 and R2 together with N form an unsubstituted or substituted saturated 5- or 6-membered heterocyclyl containing at least one heteroatom, wherein the heteroatom is O, N and S, the substituent is a methyl on N; R3 is a hydrogen atom or a chlorine atom; R4 is a hydrogen atom or a fluorine atom; X is CH, CF or N; and Y is CH, CF or N.