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    • 30. 发明申请
    • COFERONS AND METHODS OF MAKING AND USING THEM
    • 制作和使用它们的公司及方法
    • WO2009126290A2
    • 2009-10-15
    • PCT/US2009/002223
    • 2009-04-09
    • CORNELL UNIVERSITYPURDUE RESEARCH FOUNDATIONBARANY, FrancisPINGLE, ManeeshBERGSTROM, DonaldGARDINA, Sarah, Filippa
    • BARANY, FrancisPINGLE, ManeeshBERGSTROM, DonaldGARDINA, Sarah, Filippa
    • C12Q1/68
    • A61K47/545A61K31/69C07D233/64C07D307/92C07D309/30C07D319/24C07D493/22C07F5/02C07H7/02C07H9/02C40B30/04
    • The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes a diversity element which potentially binds to a target molecule with a dissociation constant of less than 300 μM and a linker element connected to the diversity element. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to said diversity element, and is capable of forming a reversible covalent bond or non-covalent interaction with a binding partner of the linker element. The monomers canbe covalently or non-covalently linked together to form a therapeutic multimer or a precursor thereof. Also disclosed is a method of screening for therapeutic multimer precursors which bind to a target molecule associated with a condition and a method of screening for linker elements capable of binding to one another. The present invention additionally relates to a therapeutic multimer, which includes a plurality of covalently or non-covalently linked monomers, therapeutic monomers, and uses of such dimers and monomers.
    • 本发明涉及可用于制备治疗化合物的单体。 所述单体包括潜在地结合具有小于300μM的解离常数的靶分子的多样性元件和连接到所述分集元件的连接体元件。 连接体元件具有小于500道尔顿的分子量,通过连接器直接或间接连接到所述多样性元件上,并且能够与连接体元件的结合配偶体形成可逆共价键或非共价相互作用。 单体可以共价或非共价连接在一起以形成治疗性多聚体或其前体。 还公开了筛选结合与条件相关的靶分子的治疗性多聚体前体的方法和筛选能够彼此结合的连接子元件的方法。 本发明另外涉及治疗性多聚体,其包括多个共价或非共价连接的单体,治疗性单体,以及这些二聚体和单体的用途。