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

国家神经疾病和中风研究所（NINDS）和NIH蓝图 神经治疗学网络（BPN）http://neuroscienceblueprint.nih.gov/bpdrugs/index.htm有需求 药物化学支持计划（MCSP）提供全方位服务的设施和工作人员， 在电极导线优化后期阶段支持药物化学项目，以提供体外吸收， 分布、代谢、排泄和毒理学（ADMET）支持，以表征主要候选药物， 确定最佳临床前候选药物，并提供化合物的储存和运输物流，以支持 贡献者（Dingledine，埃默里大学）开发一种有效的认知治疗新方法， 缺陷/癫痫。这将通过推进其小分子杂环的SPR来实现 化合物利用体外ADMET来鉴定新的以区分顶级先导化合物。候选 分子已经经历了一些与物理化学性质和生物学相关的分析 活动其目标是在由以下人员提供的顶级化合物中推进项目的进行/不进行决策： 贡献者。本合同产生的数据将由NINDS、贡献者或赞助者使用。 研究者支持研究性新药（IND）申请指导临床前活动。的 该合同的努力结果将成为推进临床前候选化合物的基础， 进一步发展，即，在准备IND申请时进行先进的PK和毒理学评价。

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.