Truncated Evans Blue modified fibroblast activation protein inhibitor, preparation method and application thereof

US11975079B2 · kind B2 · utility

Assignee

• YANTAI LANNACHENG BIOTECHNOLOGY CO., LTD. · CN

Inventors

• Xiaoyuan Chen · Acton, US
• Pengfei Xu · Beijing, CN
• Zhide GUO · Shandong, CN
• Xiaoming Wu · Jinan, CN
• Qingbao YANG · Shandong, CN
• Tian He · Houston, US

Key dates

• Filing date: Jul 11, 2021
• Grant date: May 7, 2024
• Expiry date: Jul 11, 2041

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present disclosure provides a truncated Evans Blue modified fibroblast activation protein inhibitor compound. The compound is formed by connecting truncated Evans Blue, a fibroblast activation protein inhibitor and a nuclide chelating group by means of connecting groups L1, L2, L3, L4 and X. The compound has the following structure shown in Formula (I), where R1 is a fibroblast activation protein inhibitor; L1 is lysine, glutamic acid, or a derivative structure thereof; L2 is —(CH2)n—, n is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; L3 is —(CH2)m—, m is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O— or —(CO)—; L4 is —(CH2)p—, p is an integer from 0 to 30, and each —CH2— may be individually substituted or unsubstituted with —O—, —NH—, —(CO)—, —NH(CO)—, or —(CO)—NH—; X is selected from N, C, O, S, or and R2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have the characteristics of significantly prolonging the half-…