Compound used as GPR17 (G-Protein Receptor 17) and CysLT1 (Cysteinyl Leukotrienes Receptor 1) DARAs (Dual Action Receptor Antagonists), and preparation method and application thereof

• Main Authors: CHEN HUAYAN, GONG CHAOJUN, WANG ZHILONG, XIE XIN, GUO YU'E, NAN FAJUN
• Format: Patent
• Language: Chinese; English
• Published: 09.06.2017
• Subjects: CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; 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; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

The invention discloses a compound used as GPR17 (G-Protein Receptor 17) and CysLT1 (Cysteinyl Leukotrienes Receptor 1) DARAs (Dual Action Receptor Antagonists), and a preparation method and application thereof, and relates to the compound as shown in a general formula I, and the preparation method and the application thereof. The compound has weak antagonistic activity on GPR17 and strong antagonistic activity on CysLT1, and can be used for preventing and treating central nervous system injury and neurodegenerative diseases (such as multiple sclerosis and leukodystrophy); the compound can also be used for treating asthma and rhinitis which are mediated by the CysLT1, allergy and other inflammatory diseases. 本发明类用作GPR17和CysLT双重拮抗剂的化合物、其制备方法和用途，涉及类通式I所示的化合物，其制备方法和用途。该类化合物对GPR17有弱的拮抗活性，对CysLT有强的拮抗作用，可用于预防、治疗中枢神经系统损伤和神经退行性疾病(如多发性硬化症，脑白质营养不良)；还可用于治疗CysLT介导的哮喘和鼻炎、过敏、其他炎症性疾病。