Pheny-ithiaxal derivative and preparing method and application thereof

• Main Authors: TIAN JINGWEI, LYU GUANGYAO, ZHAI RONG, FU FENGHUA, LEI LEI, MA JINBO, HONG XUECHUAN, LYU ZHENBIN, WANG HONGBO
• Format: Patent
• Language: Chinese; English
• Published: 11.01.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; 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 relates to a new inhibitor of pheny-ithiaxal TRPC6 ion channel and a preparing method thereof as well as the application in preparing drugs relating to stomach cancer treatment, and belongs to the pharmaceutical chemistry field. Based on long-term R&D of stomach cancer drugs, the invention screens a large number of chemical compounds with TRPC6 as the target and obtains the pheny-ithiaxal chemical compounds with obvious inhibitory activities in TRPC6 and stomach cancer cells. Through the test, the invention finds out that the chemical compound in general formula (1) is the outstanding TRPC6 channel inhibitor and characterized by simple synthetic method and excellent inhibitory activity in stomach cancer cells, and can be used for treating the stomach cancer arising from abnormal expression of TRPC6. 本发明涉及种新的苯基噻唑类TRPC6离子通道的抑制剂及其制备方法，以及在制备胃癌治疗相关药物中的应用，属于药物化学领域。本发明在长期充实胃癌药物研究与开发的基础上，以TRPC6为靶标筛选大量化合物，得到了具有显著TRPC6抑制活性和胃癌细胞抑制活性的苯基噻唑类化合物。本发明通过实验发现，通式（1）化合物是优秀的TRPC6通道抑制剂，具有合成方法简单，对胃癌细胞抑制活性良好等优点，可用于治疗因TR