Boron-containing compound as well as preparation method and application thereof

• Main Authors: HUANG XIAOHONG, HUANG SHUN, SHI DAZHI, WU HUBING
• Format: Patent
• Language: Chinese; English
• Published: 12.07.2024
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; APPARATUS THEREFOR; CHEMISTRY; GENERAL METHODS OF ORGANIC CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention discloses a boron-containing compound and a preparation method and application thereof, the boron-containing compound is a compound as shown in a formula I or a formula II or pharmaceutically acceptable salts, esters, solvates and isomers thereof, and in the formula II, M is selected from AlF18, 64Cu and 177Lu. The boron-containing compound provided by the invention has the effect of targeting fibroblast activating protein, can be used as a BNCT therapeutic drug or a PET probe, takes a fibroblast activating protein inhibitor with high affinity as a targeting ligand, and introduces borane as a BNCT therapeutic pharmacodynamic group. # imgabs0 # 本发明公开了一种含硼化合物及其制备方法和应用，所述含硼化合物为式I或式II所示的化合物或它们的药学上可接受的盐、酯、溶剂化物、异构体，其中，式II中，M选自AlF18、64Cu、177Lu。本发明中的含硼化合物具有靶向成纤维细胞活化蛋白的作用，可以作为BNCT治疗药物或PET探针，以具有高亲和力的成纤维细胞活化蛋白抑制剂为靶向配体，引入硼烷作为BNCT治疗药效基团。#imgabs0#