公开(公告)号：US20140308303A1

公开(公告)日：2014-10-16

申请号：US14201523

申请日：2014-03-07

Applicant: PEPSCAN SYSTEMS B.V.

Inventor： Peter TIMMERMAN ,  Joris BELD ,  Robbert H. MELOEN ,  Wouter C. PUIJK

IPC: G01N33/543

CPC classification number: G01N33/54306 ,  C07K17/02 ,  C40B30/04 ,  G01N33/54353

Abstract: The disclosure relates to the field of candidate drug testing and drug development. A method is provided for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, the method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule capable of reacting with the at least first and second reactive group; contacting the scaffold with at least one molecule to form at least two linkages between the scaffold and the at least one molecule in a coupling reaction, wherein the formation of a linkage accelerates the formation of a consecutive linkage, preferably wherein the coupling reaction is performed in solution, more preferably in an aqueous solution. Furthermore, a method is provided for selecting a candidate drug compound comprising providing a library of compounds hereof and determining the binding of a target molecule to the compounds.

Abstract translation: 本公开涉及候选药物检测和药物开发领域。 提供了一种提供由至少一个分子通过至少两个键连接到分子支架构成的化合物的方法，所述方法包括提供包含至少第一和第二反应性基团的支架; 提供至少一个能够与至少第一和第二反应性基团反应的分子; 使所述支架与至少一个分子接触以在偶联反应中在所述支架和所述至少一个分子之间形成至少两个键，其中所述连接的形成加速连续键的形成，优选地其中所述偶联反应在 溶液，更优选在水溶液中。 此外，提供了选择候选药物化合物的方法，其包括提供本文化合物文库并确定靶分子与化合物的结合。

公开(公告)号：US20140296478A1

公开(公告)日：2014-10-02

申请号：US14201593

申请日：2014-03-07

Applicant: PEPSCAN SYSTEMS B.V.

Inventor： Peter TIMMERMAN ,  Joris BELD ,  Robbert H. MELOEN ,  Wouter C. PUIJK

IPC: C07K17/02

CPC classification number: G01N33/54306 ,  C07K17/02 ,  C40B30/04 ,  G01N33/54353

Abstract: The disclosure relates to the field of candidate drug testing and drug development. Described are methods for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, the method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule able to react with the at least first and second reactive group; and contacting the scaffold with at least one molecule to form at least two linkages between the scaffold and the molecule in a coupling reaction, wherein the formation of a linkage accelerates the formation of a consecutive linkage. The coupling reaction may be performed in solution, such as an aqueous solution. Furthermore, described is a method for selecting a candidate drug compound comprising providing a library of the compounds and determining the binding of a target molecule to the compounds.

Abstract translation: 本公开涉及候选药物检测和药物开发领域。 描述了提供由至少一个分子通过至少两个键连接到分子支架上的化合物的方法，所述方法包括提供包含至少第一和第二反应性基团的支架; 提供至少一个能够与所述至少第一和第二反应性基团反应的分子; 以及使所述支架与至少一个分子接触以在偶联反应中在所述支架和所述分子之间形成至少两个连接，其中所述连接的形成加速连续连接的形成。 偶联反应可以在溶液中进行，例如水溶液。 此外，描述了选择候选药物化合物的方法，包括提供化合物文库并确定靶分子与化合物的结合。