NIH BLUEPRINT NEUROTHERAPEUTICS NETWORK (BPN) MEDICINAL CHEMISTRY SUPPORT PROGRAM (MCSP)

国家神经疾病和中风研究所(NINDS)和美国国立卫生研究院的蓝图 神经治疗网络(BPN)http://neuroscienceblueprint.nih.gov/bpdrugs/index.htm有需求 为药物化学支持计划(MCSP)提供全方位服务的设施和工作人员 支持晚期铅优化阶段的药物化学计划，以提供体外吸收； 分布、代谢、排泄和毒理学(ADMET)支持，以确定以下主要候选铅的特征 确定最佳临床前候选对象，并提供存储和运输的复合物流以支持 贡献者(埃默里大学Dingledine)开发一种新的认知治疗效果 缺乏症/癫痫。这将通过提高它们的小分子杂环起始的SPR来实现 化合物利用体外ADMET鉴定新的区分顶端先导化合物。侯选人 分子已经经历了一些与物理化学性质和生物学特性相关的剖析 活动。目标是将项目推进到由提供的顶级化合物中进行/不进行决策 贡献者。本合同生成的数据将由NINDS、贡献者或赞助商使用 支持研究性新药(IND)申请的研究人员指导临床前活动。这个 该合同的努力结果将成为推进临床前候选化合物的基础 进一步的发展，即在准备IND文件方面进行高级PK和毒理学评估。

The National Institute on Neurological Disorders and Stroke (NINDS) and the NIH Blueprint Neurotherapeutics Network (BPN) http://neuroscienceblueprint.nih.gov/bpdrugs/index.htm have a need for the Medicinal Chemistry Support Program (MCSP) to provide a full-service facility and staff who would support a medicinal chemistry program in the late Lead Optimization phase to provide in vitro absorption, distribution, metabolism, excretion and toxicology (ADMET) support to characterize top lead candidates to determine best preclinical candidate and to provide compound logistics of storage and shipping to support the Contributor (Dingledine, Emory University) to develop a novel therapeutic effective in cognitive deficits/epilepsy. This will be achieved by advancing the SPR of their small molecule heterocyclic starting compound utilizing in vitro ADMET to identify novel to differentiate top lead compounds. Candidate molecules have undergone some profiling related to the physicochemical properties and biological activity. The goal is to advance the project to go/no go decision amongst the top compounds provided by the Contributor. The data generated from this contract will be used by NINDS, contributors or sponsored investigators in support of Investigational New Drug (IND) application directed preclinical activities. The results of the efforts of this contract will be the basis to advance preclinical candidate compounds for further development i.e., advanced PK and toxicological evaluation in preparation of IND filings.