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1. 发明申请

WO2003092742A1 VITAMIN-TARGETED IMAGING AGENTS 审中-公开
标题翻译：维生素靶向成像剂
公开(公告)号：WO2003092742A1
公开(公告)日：2003-11-13
申请号：PCT/US2003/014379
申请日：2003-05-06
申请人： ENDOCYTE, INC. , LEAMON, Christopher, Paul , PARKER, Matthew, A.
发明人： LEAMON, Christopher, Paul , PARKER, Matthew, A.
IPC分类号： A61K49/00
CPC分类号： A61K51/08 , A61K47/54 , A61K47/551 , A61K51/025 , A61K51/0402 , A61K51/0459 , A61K51/0497 , A61K51/088
摘要： The invention relates to compounds and methods for targeting radionuclide-based imaging agents to cells having receptors for a vitamin, or vitamin receptor binding derivative or analog thereof, by using such a vitamin as the targeting ligand for the imaging agent. The invention provides a compound of the formula (I) or (II) for use in such methods. In the compound, V is a vitamin that is a substrate for receptor-mediated transmembrane transport in vivo, or a vitamin receptor binding derivative or analog thereof, L is a divalent linker, R is a side chair of an amino acid of the formula H 2 NCHRCOOH, M is a cation of a radionuclide, n is 1 or 0, K is 1 or 0, and the compound can be in a pharmaceutically acceptable carrier therefor. The vitamin-based compounds can be used to target radionuclides to cells, such as a variety of tumor cell types, for use in diagnostic imaging of the targeted cells.
摘要翻译：本发明涉及通过使用这样的维生素作为成像剂的靶向配体，将基于放射性核素的成像剂靶向具有维生素或维生素受体结合衍生物或其类似物的受体的细胞的化合物和方法。本发明提供了用于这些方法的式（I）或（II）化合物。在化合物中，V是作为体内受体介导的跨膜转运的底物的维生素或维生素受体结合衍生物或其类似物，L是二价连接基，R是式H2NCHRCOOH的氨基酸的侧椅 M是放射性核素的阳离子，n为1或0，K为1或0，该化合物可以是药学上可接受的载体。基于维生素的化合物可用于将放射性核素靶向细胞，例如各种肿瘤细胞类型，用于靶向细胞的诊断成像。

2. 发明申请

WO2004069159A3 VITAMIN RECEPTOR BINDING DRUG DELIVERY CONJUGATES 审中-公开
标题翻译：维生素B受体结合药物联合用药
公开(公告)号：WO2004069159A3
公开(公告)日：2005-06-16
申请号：PCT/US2004002070
申请日：2004-01-27
申请人： ENDOCYTE INC , VLAHOV IONTCHO RADOSLAVOV , LEAMON CHRISTOPHER PAUL , PARKER MATTHEW A , HOWARD STEPHEN J , SANTHAPURAM HARI KRISHNA , SATYAM APPARAO , REDDY JOSEPH ANAND
发明人： VLAHOV IONTCHO RADOSLAVOV , LEAMON CHRISTOPHER PAUL , PARKER MATTHEW A , HOWARD STEPHEN J , SANTHAPURAM HARI KRISHNA , SATYAM APPARAO , REDDY JOSEPH ANAND
IPC分类号： A61K20060101 , A61K39/395 , A61K51/00 , A61K51/08 , A61M36/14 , C07K16/46
CPC分类号： A61K47/48569 , A61K47/48384 , A61K47/484 , A61K47/48715 , A61K47/551 , A61K47/65 , A61K47/6803 , A61K47/6807 , A61K47/6851 , A61K47/6889 , C07K16/30 , C07K2317/55
摘要： The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety is a vitamin, or a vitamin receptor binding analog or a derivative thereof, and the drug includes analogs or derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) comprises one or more spacer linkers, releasable linkers, and heteroatom linkers. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
摘要翻译：本发明描述了维生素受体结合药物递送缀合物及其制备方法。药物递送缀合物由维生素受体结合部分，二价连接体（L）和药物组成。维生素受体结合部分是维生素或维生素受体结合类似物或其衍生物，并且该药物包括其类似物或衍生物。维生素受体结合部分与二价连接体共价连接，并且药物或其类似物或衍生物与二价连接体共价连接，其中二价连接体（L）包含一个或多个间隔基连接体，可释放接头，和杂原子接头。还描述了使用药物递送缀合物消除致病细胞群的方法和药物组合物。

3. 发明申请

WO2004069159A2 VITAMIN RECEPTOR BINDING DRUG DELIVERY CONJUGATES 审中-公开
标题翻译：维生素B受体结合药物联合用药
公开(公告)号：WO2004069159A2
公开(公告)日：2004-08-19
申请号：PCT/US2004/002070
申请日：2004-01-27
申请人： ENDOCYTE, INC. , VLAHOV, Iontcho, Radoslavov , LEAMON, Christopher, Paul , PARKER, Matthew, A. , HOWARD, Stephen, J. , SANTHAPURAM, Hari, Krishna , SATYAM, Apparao , REDDY, Joseph, Anand
发明人： VLAHOV, Iontcho, Radoslavov , LEAMON, Christopher, Paul , PARKER, Matthew, A. , HOWARD, Stephen, J. , SANTHAPURAM, Hari, Krishna , SATYAM, Apparao , REDDY, Joseph, Anand
IPC分类号： A61K
CPC分类号： A61K47/48569 , A61K47/48384 , A61K47/484 , A61K47/48715 , A61K47/551 , A61K47/65 , A61K47/6803 , A61K47/6807 , A61K47/6851 , A61K47/6889 , C07K16/30 , C07K2317/55
摘要： The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety is a vitamin, or a vitamin receptor binding analog or a derivative thereof, and the drug includes analogs or derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) comprises one or more spacer linkers, releasable linkers, and heteroatom linkers. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
摘要翻译：本发明描述了维生素受体结合药物递送缀合物及其制备方法。药物递送缀合物由维生素受体结合部分，二价连接体（L）和药物组成。维生素受体结合部分是维生素或维生素受体结合类似物或其衍生物，并且该药物包括其类似物或衍生物。维生素受体结合部分与二价连接体共价连接，并且药物或其类似物或衍生物与二价连接体共价连接，其中二价连接体（L）包含一个或多个间隔基连接体，可释放接头，和杂原子接头。还描述了使用药物递送缀合物消除致病细胞群的方法和药物组合物。

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