SBIR Phase I: High Speed Chemical Analysis of Combinatorial Libraries

SBIR 第一阶段：组合文库的高速化学分析

• 批准号: 9861093
• 负责人: Jack Syage
• 金额: $ 10万
• 依托单位: SYAGEN TECHNOLOGY INC
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-01-01 至 1999-06-30
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=9861093&HistoricalAwards=false
• 关键词: SBIR; Phase; Speed; Chemical; Analysis

9861093 A revolution in drug discovery is unfolding in the form of high throughput organic synthesis by parallel and combinatorial methods. Methods of conducting rapid screening for biological activity are keeping pace with the rapid growth of combinatorial libraries. The current limitation in fully characterizing these libraries is in the chemical analysis of purity and component composition. The currently accepted standard for high throughput analysis is liquid chromatography/mass spectrometry (LC/MS). With a cycle time of about 5 minutes, an LC/MS instrument can analyze about 300 samples in a 24-hour period. We propose an innovative MS concept that reduces cycle time to about 5 seconds, thus raising the potential analysis rate to greater than 10,000 samples/day. The innovation is based on a novel ionization source that (1) ionizes nearly all drug candidates efficiently, (2) leads to nearly pure parent molecular ion for definitive analysis of complex mixtures, and (3) is immune to detection of common air constituents and many commonly used solvents. Our market research indicates the potential for exponential growth on the basis of quick penetration of the chemical analysis niche of the rapidly growing field of combinatorial and parallel synthesis methods for drug discovery. The proposed high throughput chemical analysis system has the potential to dominate the market for combinatorial library analysis, which is a rapidly growing field of drug discovery. Our real-time, complex mixture analyzers will also be marketed for applications in drug testing, environmental monitoring, and on-line process monitoring.

9861093 药物发现领域的一场革命正在以并行和组合方法的高通量有机合成的形式展开。快速筛选生物活性的方法正在与组合文库的快速增长保持同步。目前全面表征这些库的局限性在于纯度和成分组成的化学分析。目前公认的高通量分析标准是液相色谱/质谱 (LC/MS)。 LC/MS 仪器的循环时间约为 5 分钟，可在 24 小时内分析约 300 个样品。我们提出了一种创新的 MS 概念，可将循环时间缩短至约 5 秒，从而将潜在分析率提高至每天 10,000 个样本以上。该创新基于一种新型电离源，该电离源 (1) 有效电离几乎所有候选药物，(2) 产生几乎纯净的母分子离子，用于复杂混合物的明确分析，(3) 不受常见空气成分和许多常用溶剂检测的影响。我们的市场研究表明，在快速渗透药物发现组合和平行合成方法领域的化学分析利基市场的基础上，该领域具有指数增长的潜力。 所提出的高通量化学分析系统有可能主导组合文库分析市场，这是一个快速发展的药物发现领域。我们的实时复杂混合物分析仪也将用于药物测试、环境监测和在线过程监测应用。