药物化学 先导化合物发现.pptVIP

第二节先导化合物的发现 Lead discovery Vaudon only ch Asposeslides for NET 4o dient P Evaluation only. Created with Aspose Slides for NET 4.0 dient Profilo 71 Copyright 2004-2017Aspose Pty L  ■新药开发过程的几个阶段 先导化合物的探索和选定阶段 临床前实验研究阶段 临床研究 (临床治疗和效果验证阶段) 医药生产申请及审批阶段 售后效果以及副作用的调查统计阶段 药品合理性再审查阶段 Vaudon only ch Asposeslides for NET 4o dient P Evaluation only. Created with Aspose Slides for NET 4.0 dient Profilo 71 Copyright 2004-2017Aspose Pty L  新药的定义 口新的化学实体 I New Chemical Entity, NCE 口新的药用化合物 口制成各种制剂供临床上使用 Vaudon only ch Asposeslides for NET 4o dient P Evaluation only. Created with Aspose Slides for NET 4.0 dient Profilo 71 Copyright 2004-2017Aspose Pty L  New Chemical Entity aA new chemical entity(nce)is a compound not previously described in the literature Vaudon only ch Asposeslides for NET 4o dient P Evaluation only. Created with Aspose Slides for NET 4.0 dient Profilo 71 Copyright 2004-2017Aspose Pty L  新药的药物化学研究分两个阶段 口发现先导化合物( Lead Generation) ■为寻求新的先导化合物( Lead Compound) ■类型衍化 口对先导化合物进行优化 Lead Optimization) ■寻找该先导化合物系列衍生物中的最佳化合物 ■系列设计 Vaudon only ch Asposeslides for NET 4o dient P Evaluation only. Created with Aspose Slides for NET 4.0 dient Profilo 71 Copyright 2004-2017Aspose Pty L  Lead generation 口发现先导化合物 a Lead generation is the term applied to strategies developed to identify compounds which possess a desired but non-optimized biological activity Vaudon only ch Asposeslides for NET 4o dient P Evaluation only. Created with Aspose Slides for NET 4.0 dient Profilo 71 Copyright 2004-2017Aspose Pty L  Lead optimization 口先导化合物进行优化 o Lead optimization is the synthetic modification of a biologically active compound to fulfill all stereoelectronic physicochemical, pharmacokinetic and toxicologic required for clinical usefulness. Vaudon only ch Asposeslides for NET 4o dient P alveton o Created with Aspose Slides for NET 4.0 dient Profilo 71 Copyright 2004-2017Aspose Pty L  相互关系 口先导化合物的发现 ■为寻找最佳化合物提供了