Si-ROMP Hybrid Reagent/Scavengers for High Throughput Chemistry

描述（由申请人提供）：Materia，Inc.和堪萨斯大学打算建立在我们目前的STTR第二阶段赠款（R41 GM 076765 -02），2011年3月31日到期的成功。该提案是堪萨斯大学和Materia公司之间的合作成果。在Pasadena，CA，旨在开发和扩大Si-ROMP混合试剂/清除剂，并优化其商业化的过程。（1）利用SiO2表面上的表面引发的ROM聚合，由现有的和新的环己烯基官能化的单体产生Si-ROMP试剂/清除剂的阵列，其中阶段I的里程碑目标是合成六种Si-ROMP试剂：Si-OBAC、Si-ODCT、Si-OTPP、Si-OTP、Si-OACC和Si-OBP，（2）在流通技术中利用所开发的Si-ROMP杂化材料，用于高通量方法中的简易和免纯化方案，第一阶段的另一个里程碑目标是证明在连续流方案中利用Si-ROMP杂化材料。第二阶段的目标是（3）Si-ROMP试剂和清除剂的工艺开发和规模扩大，包括工业和非营利组织/合作者对Si-ROMP试剂和清除剂的关键β测试，（4）利用表面引发的ROM聚合，从现有的和新的异戊二烯基官能化单体继续产生表面固定化的试剂/清除剂（第1阶段中的目标#1），（5）在流通技术中继续利用所开发的Si-ROMP杂化材料，用于高通量方法中的简易和无纯化的方案（第1阶段目标2），和（6）利用Nb标记的Si颗粒以简单和免纯化的方案螯合Nb标记的试剂/清除剂，并研究废Si的再循环。ROMP盒。 在我们目前资助的II期以及最近的出版物中，已经通过许多研究证明了可溶形式的ROMP试剂用于药物发现。通过Materia，Inc.的科学家团队，我们已做好充分准备，以满足拟议的快速通道计划的挑战性技术方面。和堪萨斯大学。此外，Materia的技术平台、业务开发部门和大规模生产设施将促进开发的技术从实验室向商业领域的计划过渡。Materia已经建立了广泛的战略联盟网络，以充分利用其技术和业务资源，加快下游产品的开发。主要研究者实验室、堪萨斯大学（KU-CMLD）的NIH图书馆开发化学方法中心和Materia，Inc.将用于产品开发和广泛的beta测试的所有产品提供的商业化。 公共卫生相关性：该项目名为Si-ROMP Hybrid Reagent/Scavengers for High Throughput Chemistry，旨在生产和商业化用于高通量化学的高负载Si-ROMP衍生的杂合试剂/清除剂。

DESCRIPTION (provided by applicant): This Fast Track Small Business Technology Transfer study between Materia, Inc. and the University of Kansas intends to build upon successes of our current STTR Phase II grant (R41GM076765-02) which expires on March 31, 2011. This proposal is a collaborative effort between the University of Kansas and Materia, Inc. in Pasadena, CA that aims to develop and scale-up Si-ROMP hybrid reagents/scavengers and optimize the process for their commercialization. More specifically, Phase I will focus on three key areas: (1) Generation of an array of Si-ROMP reagent/scavengers from existing and new norbornenyl-functionalized monomers utilizing surface-initiated ROM polymerization off SiO2 surfaces, with a Phase I milestone goal to synthesize six Si- ROMP reagents: Si-OBAC, Si-ODCT, Si-OTPP, Si-OTP, Si-OACC and Si-OBP, (2) Utilization of the developed Si-ROMP hybrid materials in flow-through technology for facile and purification-free protocols in high throughput methods, with another Phase I milestone goal demonstrating utilization of Si-ROMP hybrid materials in continuous-flow protocols. The Phase II goals are (3) process development and scale-up of Si-ROMP reagents and scavengers including key beta-testing of Si-ROMP reagents and scavengers by industrial and non-profit organization/collaborators, (4) continued generation of surface-immobilized reagent/scavengers from existing and new norbornenyl-functionalized monomers utilizing surface-initiated ROM polymerization (Aim #1 in Phase 1), (5) continued utilization of the developed Si-ROMP hybrid materials in flow-through technology for facile and purification-free protocols in high throughput methods (Aim #2 in Phase 1), and (6) utilization of Nb-tagged Si-particles to sequester Nb-tagged reagents/scavengers in facile and purification-free protocols and investigation into recycling of spent Si-ROMP cartridges. Application of soluble versions of ROMP reagents for drug-discovery has been demonstrated through a number of studies in our currently funded Phase II as well as in recent publications. We are well positioned to meet the challenging technical aspects of the proposed Fast Track program through teaming of scientists at Materia, Inc. and the University of Kansas. Moreover, Materia's technology platforms, its business development unit, and large scale manufacturing facilities will facilitate the planned transition of the developed technologies out of the laboratory and into the commercial realm. Materia has developed an extensive strategic alliance network to leverage its technical and business resources and accelerate downstream product development. Extensive resources in the Principal Investigator's laboratory, the NIH Center in Chemical Methodologies for Library Development at the University of Kansas (KU-CMLD), and at Materia, Inc. will be utilized toward product development and extensive beta testing of all products offered for commercialization. PUBLIC HEALTH RELEVANCE: This project entitled Si-ROMP Hybrid Reagent/Scavengers for High Throughput Chemistry aims for the production and commercialization of high-load, Si-ROMP-derived hybrid reagents/scavengers for use in high throughput chemistry.