REACTOR FOR GENERATION OF COMPOUND DERIVATIVE LIBRARIES

描述：（改编自申请人的摘要） 计划是开发一种新的方法，用于快速生成混合物， 衍生物（即，衍生物库）的化合物与药物 活动 此类衍生物由具有生物活性的化合物制成。 活性或这些化合物的类似物，目的是 鉴定具有更有吸引力的药物的相关化合物 性质，如水溶性、GI道渗透性或靶向 选择性 拟议的程序应能够在结构上产生 快速产生不同的衍生物， 使用传统的化学方法从母体化合物中获得。 该过程有望大大加快优化， 开发制药先导产品。 在第一阶段，计划证明这一进程的可行性 通过衍生已知的三种烟碱乙酰胆碱受体激动剂 - 具有令人感兴趣的神经保护活性， 尚未开发成商业药物。 在第二阶段，将对工艺和反应器设计进行优化， 从一系列起始材料产生衍生文库， 一系列的衍生分子 由于这一承诺， 技术，一家大型制药公司已同意与 弯曲研究通过筛选衍生文库的生物活性， 广泛的治疗用途。

DESCRIPTION: (Adapted from the applicant's abstract) The goal of this program is to develop a new process for rapidly generating mixtures of derivatives (i.e., derivative libraries) of compounds with pharmaceutical activity. Such derivatives are made from compounds possessing biological activity or from close analogues of these compounds, with the goal of identifying related compounds with more attractive pharmaceutical properties, such as aqueous solubility, GI-tract permeability, or target selectivity. The proposed process should make it possible to produce structurally distinct derivatives rapidly and to produce derivatives not readily accessible from the parent compound using traditional chemical methods. The process promises to greatly accelerate the optimization and development of pharmaceutical leads. In Phase I, it is planned to demonstrate the feasibility of this process by derivatizing known agonists of three nicotinic acetylcholine receptors - compounds that exhibit interesting neuroprotective activities but have not yet been developed into commercial pharmaceuticals. In Phase II, the process and reactor design would be optimized for rapidly generating derivative libraries from a range of starting materials using a series of derivatizing molecules. Due to the promise of this technology, a major pharmaceutical company has agreed to collaborate with Bend Research by screening the derivative libraries for bioactivity for a broad range of therapeutic uses.