Small molecule ligand for targeted administration, ligand drug conjugate, rheumatoid arthritis treatment drug and application

• Main Authors: LIU YUAN, QIAN HONGYAN, HE YAN, SHI GUIXIU, ZHANG XINWEI, CHEN SHIJU
• Format: Patent
• Language: Chinese; English
• Published: 28.03.2025
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention belongs to the technical field of biological medicines, and discloses a small molecule ligand for targeted administration, a ligand medicine conjugate, a rheumatoid arthritis treatment medicine and application. The small molecule ligand for targeted administration provided by the invention takes a structure as shown in a formula (1) as a linker, and meanwhile, a group M1 derived from a fibroblast activating protein inhibitor is introduced, so that the small molecule ligand can be well applied as a drug delivery platform for RA treatment; the molecular biological activity of the anti-rheumatism medicine is kept, and meanwhile, the anti-rheumatism medicine is fully released in an inflammation joint area, so that a better rheumatoid arthritis treatment effect is achieved, and the anti-rheumatism medicine has a good application prospect. # imgabs0 # 本发明属于生物医药的技术领域，公开了一种靶向给药用小分子配体、配体药物偶联物和类风湿关节炎治疗药物及应用。本发明提供的靶向给药用小分子配体以式(1)所示的结构作为连接子，同时引入有衍生自成纤维细胞活化蛋白抑制剂的基团M1，其能够很好被应用作为用于RA治疗的药物递送平台，在保持抗风湿药物分子生物活性的同时