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121. 发明申请

US20160108085A1 TUBULYSINS AND PROCESSES FOR PREPARING 审中-公开
标题翻译：用于制备的管状体和方法
公开(公告)号：US20160108085A1
公开(公告)日：2016-04-21
申请号：US14921196
申请日：2015-10-23
申请人： ENDOCYTE, INC.
发明人： Iontcho Radoslavov Vlahov , Christopher Paul Leamon , Kevin Yu Wang
IPC分类号： C07K5/02 , C07K5/078
CPC分类号： C07K5/021 , C07K5/06139
摘要： Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations.
摘要翻译：描述了制备肾上腺素的方法。这些方法可用于制备预混合的肾上腺素的混合物，由tubulininins混合物制备单一的tubulinins，并将一种tubulyin转化成不同的tubulysin。本文所述的管状体素可用于治疗包括致病细胞群体的疾病和疾病状态。

122. 发明申请

US20160002167A1 BIVALENT LINKERS AND CONJUGATES THEREOF 审中-公开
公开(公告)号：US20160002167A1
公开(公告)日：2016-01-07
申请号：US14746075
申请日：2015-06-22
申请人： Endocyte, Inc.
发明人： Iontcho R. Vlahov , Christopher P. Leamon , Apparao Satyam , Stephen J. Howard
IPC分类号： C07D213/71
CPC分类号： C07D213/71 , A61K47/551 , A61K47/6803 , A61K49/0002 , C07D401/12 , C07D475/04
摘要： Bivalent linkers to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described.

123. 发明授权

US08834842B2 Vitamin-targeted imaging agents 有权
标题翻译：维生素靶向成像剂
公开(公告)号：US08834842B2
公开(公告)日：2014-09-16
申请号：US13793624
申请日：2013-03-11
申请人： Endocyte, Inc.
发明人： Christopher P. Leamon , Matthew A. Parker
IPC分类号： A61K49/00 , A61K51/08 , A61K47/48 , A61K51/04 , A61K51/02
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 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。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。

124. 发明申请

US20140140925A1 FOLATE-TARGETED DIAGNOSTICS AND TREATMENT 审中-公开
标题翻译： FOLATE-TARGETED诊断和治疗
公开(公告)号：US20140140925A1
公开(公告)日：2014-05-22
申请号：US13800309
申请日：2013-03-13
申请人： ENDOCYTE, INC.
发明人： Christopher P. LEAMON , Richard MESSMANN , David MORGENSTERN
IPC分类号： C07K5/113 , A61K51/08
CPC分类号： C07K5/1021 , A61K51/0459 , A61K51/088 , G01N33/57423 , G01N33/57449 , G01N33/94 , G01N2800/52
摘要： Methods of detecting and assessing functionally active folate receptors on tumors and treatment associated with those tumors are described. Also described are methods of selecting ovarian and lung cancer patients for therapy with a folate-vinca conjugate by identifying functionally active folate receptors on the tumors of the patient. Also described are methods and compositions for treating folate receptor expressing epithelial tumors with a folate-vinca conjugate in combination with doxorubicin such as pegylated liposomal doxorubicin in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum sensitive ovarian tumors. Also described are methods of treating platinum-resistant ovarian cancer using a folate-targeted drug, in the absence or presence of selecting the patient by identifying functionally active folate receptors on the tumors of the patient.
摘要翻译：描述了检测和评估肿瘤上的功能活性叶酸受体和与这些肿瘤相关的治疗的方法。还描述了通过鉴定患者肿瘤上的功能活性叶酸受体来选择卵巢和肺癌患者用叶酸 - 长春花碱缀合物治疗的方法。还描述了用叶酸 - 长春花碱缀合物与多柔比星联合治疗叶酸受体表达上皮肿瘤的方法和组合物，所述多柔比星例如聚乙二醇化脂质体多柔比星，其中肿瘤包括卵巢，子宫内膜或非小细胞肺癌肿瘤，包括耐铂性卵巢肿瘤和铂敏感性卵巢肿瘤。还描述了在没有或存在通过鉴定患者肿瘤上的功能活性叶酸受体来选择患者的情况下使用叶酸盐靶向药物治疗铂抗性卵巢癌的方法。

125. 发明申请

US20140073761A1 CONJUGATES CONTAINING HYDROPHILIC SPACER LINKERS 审中-公开
标题翻译：含有疏水间隔物的连接物
公开(公告)号：US20140073761A1
公开(公告)日：2014-03-13
申请号：US13785542
申请日：2013-03-05
申请人： ENDOCYTE, INC.
发明人： Christopher P. LEAMON , Iontcho R. Vlahov , Hari Krishna R. Santhapuram , Paul J. Kleindl , Kevin Yu Wang , Fei You
IPC分类号： A61K47/48
CPC分类号： C07K9/003 , A61K47/545 , A61K47/60 , A61K47/65 , C07H15/24
摘要： Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.
摘要翻译：本文描述了使用含有用于成像，诊断和/或治疗由致病细胞群体引起的疾病和疾病状态的亲水性间隔物接头的细胞受体结合药物递送缀合物用于靶向药物递送的组合物和方法。

126. 发明申请

US20140065068A1 VITAMIN-TARGETED IMAGING AGENTS 有权
标题翻译：维生素靶向成像剂
公开(公告)号：US20140065068A1
公开(公告)日：2014-03-06
申请号：US13793624
申请日：2013-03-11
申请人： ENDOCYTE, INC.
发明人： Christopher P. LEAMON , Matthew A. PARKER
IPC分类号： A61K51/08 , A61K51/02 , A61K51/04
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 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。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。

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