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蓝图

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.