Compound as well as preparation method, pharmaceutical composition and application thereof

• Main Authors: RUCH WERNECK GUIMARAES CRISTIANO, FELYPE ZANETTI DE AZEVEDO HATYLAS, FREIRE TORRES RUSSO VALTER, MASGARELLO, ARTURO, MANNOCHIO DE SOUZA RUSSO ELISA, WATANABE DA COSTA RENATA
• Format: Patent
• Language: Chinese; English
• Published: 14.10.2022
• 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 compound as well as a preparation method, a pharmaceutical composition and application thereof. The present invention relates to novel and inventive pharmacologically active benzimidazole derivative compounds which surprisingly have a high affinity for the melatonin MT1 and MT2 receptors and a low affinity for CYP450 complex enzymes, in particular CYP1A2. In addition to the method for preparing the composition, the invention also relates to novel and creative synthetic routes of the compounds. Pharmaceutical compositions comprising said compounds and the use of these compounds in the treatment of subjects affected by psychiatric and/or sleep disorders associated with these receptors, in particular depression, anxiety, diurnal cycle disorders. 本发明涉及化合物及其制备方法、药物组合物和用途。本发明涉及新颖的和有创造性的药理活性苯并咪唑衍生物化合物，其令人惊讶地对褪黑激素MT1和MT2受体具有高亲和力并且对CYP450复合酶特别是CYP1A2具有低亲和力。除了制备组合物的方法之外，本发明还涉及这些化合物的新颖的和有创造性的合成途径，包含所述化合物的药物组合物以及这些化合物在治疗受这些受体相关的精神障碍和/或睡眠障碍(特别是抑郁症、焦虑症、昼夜周期障碍)影响的个体中的用途。