Pyraxolidinone CCK and gastrin antogonists and pharmaceutical formulations thereof
申请人:ELI LILLY AND COMPANY
公开号:EP0467614A1
公开(公告)日:1992-01-22
Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.
研究发现,新型取代的吡唑烷酮类化合物与大脑和/或胰腺、胃和回肠等外周部位的胆囊收缩素(CCK)受体和胃泌素受体有明显的结合。吡唑烷酮是 CCK 和胃泌素受体拮抗剂,可用于治疗温血脊椎动物的胃肠道疾病、中枢神经系统疾病和食欲调节。本文介绍了用于此类适应症的药物制剂。