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1. 发明申请

US20040014168A1 Reagents and methods for library synthesis and screening 审中-公开
标题翻译：用于图书馆合成和筛选的试剂和方法
公开(公告)号：US20040014168A1
公开(公告)日：2004-01-22
申请号：US10243974
申请日：2002-09-13
申请人： Howard Hughes Medical Institute
发明人： Stuart L. Schreiber , Helen E. Blackwell , Lucy Perez Fernandez , John A. Tallarico
IPC分类号： C12P021/06 , C08G063/48 , C08G063/91
CPC分类号： C07D311/78 , C07B2200/11 , C40B40/00
摘要： The invention provides novel solid supports for the synthesis of compound libraries. The solid supports have the physical capacity to deliver at least 50 nmol of compound and are functionalized with a silicon-containing linker. In one embodiment of the invention the solid support comprises a bead having a diameter of between approximately 400 and 600 nullm functionalized with a silicon-containing linker. According to certain embodiments of the invention the bead is a polystyrene bead. According to certain embodiments of the invention the linker is a diisopropylalkyl-substituted silyl ether. The invention further provides grafted polymeric supports such as lanterns functionalized with a silicon-containing linker. The invention provides methods for screening in which compounds are synthesized on solid supports in a quantity so that a single solid support such as a bead provides a stock solution sufficient to perform hundreds or thousands of biological or chemical assays. The methods include decoding the sequence of chemical reactions used to synthesize the compound by identifying tags incorporated into the compound during synthesis.
摘要翻译：本发明提供用于合成化合物文库的新型固体载体。固体载体具有递送至少50nmol化合物的物理能力，并用含硅连接体官能化。在本发明的一个实施方案中，固体支持物包含直径为约400-600μm的用含硅连接体官能化的珠粒。根据本发明的某些实施方案，珠是聚苯乙烯珠。根据本发明的某些实施方案，连接体是二异丙基烷基取代的甲硅烷基醚。本发明还提供接枝聚合物载体，例如用含硅接头官能化的灯。本发明提供筛选方法，其中化合物在固体支持物上合成，其量使得单个固体支持物如珠提供足以进行数百或数千种生物或化学测定的储备溶液。所述方法包括通过鉴定合成期间掺入到化合物中的标记来解码用于合成化合物的化学反应序列。

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