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    Methods and Compositions for Treating and Diagnosing Kidney Disease
    2.
    发明申请
    Methods and Compositions for Treating and Diagnosing Kidney Disease 有权
    治疗和诊断肾脏疾病的方法和组成

    公开(公告)号：US20120270791A1

    公开(公告)日：2012-10-25

    申请号：US13440641

    申请日：2012-04-05

    申请人： Christopher Paul Leamon ,  Iontcho Radoslavov Vlahov

    发明人： Christopher Paul Leamon ,  Iontcho Radoslavov Vlahov

    IPC分类号： A61K38/08 ,  A61P13/12 ,  C07K7/06

    CPC分类号： A61K51/04 ,  A61K47/551 ,  A61K47/552 ,  A61K49/0002 ,  A61K51/00 ,  C07D475/04 ,  C07D519/00 ,  C07K7/02

    摘要： The invention relates to a method for diagnosing a kidney disease state. The method comprises the steps of administering to a patient a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises a diagnostic marker, and diagnosing the kidney disease state. The invention also relates to a method for treating a kidney disease state. The method comprises the steps of administering to a patient suffering from the disease state an effective amount of a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises an antigen, a cytotoxin, or a cell growth inhibitor, and eliminating the disease state.

    摘要翻译： 本发明涉及诊断肾脏疾病状态的方法。 该方法包括以下步骤：向患者施用包含通式VLD的缀合物或复合物的组合物，其中组V包含结合肾近端小管细胞的维生素受体结合配体，D组包括诊断标记物，并诊断 肾脏疾病状态。 本发明还涉及治疗肾脏疾病状态的方法。 该方法包括以下步骤：向患有疾病状态的患者施用有效量的包含通式VLD的缀合物或复合物的组合物，其中组V包含结合肾近端小管细胞的维生素受体结合配体， D组包含抗原，细胞毒素或细胞生长抑制剂，并消除疾病状态。

    FOLATE-TARGETED DIAGNOSTICS AND TREATMENT
    3.
    发明申请
    FOLATE-TARGETED DIAGNOSTICS AND TREATMENT 审中-公开
    FOLATE-TARGETED诊断和治疗

    公开(公告)号：US20120128587A1

    公开(公告)日：2012-05-24

    申请号：US13388184

    申请日：2010-07-30

    申请人： Christopher Paul Leamon ,  Richard Messmann ,  David Morgenstern

    发明人： Christopher Paul Leamon ,  Richard Messmann ,  David Morgenstern

    IPC分类号： A61K51/08 ,  A61P35/04 ,  A61P35/00 ,  A61K38/08 ,  A61K9/127

    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。

    METHOD OF ADMINISTERING CONJUGATES
    7.
    发明申请
    METHOD OF ADMINISTERING CONJUGATES 审中-公开
    管理方法

    公开(公告)号：US20100272675A1

    公开(公告)日：2010-10-28

    申请号：US12743191

    申请日：2008-11-14

    申请人： Christopher Paul Leamon ,  P. Ronald Ellis

    发明人： Christopher Paul Leamon ,  P. Ronald Ellis

    IPC分类号： A61K38/20 ,  A61K47/00 ,  A61K38/21

    CPC分类号： A61K38/2013 ,  A61K38/208 ,  A61K47/646

    摘要： The invention relates to a method of treating a host animal to eliminate pathogenic cells. The method comprises the steps of administering to the host animal a hapten-carrier conjugate, administering to the host animal a TH-I biasing adjuvant, and administering to said host animal a ligand conjugated to a hapten herein the ligand-hapten conjugate is administered during the first cycle of therapy with the hapten-carrier conjugate. The invention also relates to the same method wherein the ratio of the hapten-carrier conjugate to the TH-I biasing adjuvant on a weight to weight basis ranges from about 1:10 to about 1:1.

    摘要翻译： 本发明涉及一种治疗宿主动物以消除致病细胞的方法。 该方法包括以下步骤：向宿主动物施用半抗原 - 载体缀合物，向宿主动物施用TH-1偏置佐剂，并向所述宿主动物施用与本文中的半抗原结合的配体 - 配偶体缀合物的配体， 用半抗原载体缀合物的第一个疗程循环。 本发明还涉及相同的方法，其中重量/体重基础上的半抗原 - 载体缀合物与TH-1偏置佐剂的比例范围为约1:10至约1:1。

    Fusogenic lipids and vesicles
    8.
    发明授权
    Fusogenic lipids and vesicles 失效
    融合脂质和囊泡

    公开(公告)号：US06858226B2

    公开(公告)日：2005-02-22

    申请号：US10081463

    申请日：2002-02-22

    申请人： Christopher Paul Leamon

    发明人： Christopher Paul Leamon

    IPC分类号： A61K9/127 ,  A61K47/28 ,  A61K48/00 ,  C07C323/52 ,  C07C323/60 ,  C07F9/10 ,  C07J9/00 ,  C12N15/113 ,  C12N15/88

    CPC分类号： C12N15/1135 ,  A61K9/1271 ,  A61K48/00 ,  C12N15/88 ,  C12N2310/315 ,  C12N2310/321 ,  C12N2310/3341 ,  C12N2310/346 ,  Y10S977/907 ,  C12N2310/3525

    摘要： Novel lipid compounds are provided that may be termed “pro-cationic” in that they are neutral or negatively charged until they are either brought into contact with cellular membranes or are internalized by cells. The lipids have a hydrophobic tail group and a hydrophilic head group, the head group incorporating both a positively and negatively charged region at physiological pH. The hydrophobic tail group is stably connected to the positive region of the head group which in turn is connected to the negative region by a disulfide bond that is susceptible to cleavage by membrane-bound and intracellular factors. Cleavage of the disulfide bond removes the negatively charged region from the head group resulting in a lipid that is cationic and therefor fusogenic with negatively charged cell membranes. Consequently, lipids of the invention are useful as components of liposomes that serve as vehicles for delivering pharmaceutical agents into cells with reduced toxicity.

    摘要翻译： 提供了可以称为“阳离子阳离子”的新型脂质化合物，因为它们是中性的或带负电荷的，直到它们与细胞膜接触或被细胞内化。 脂质具有疏水性尾巴基团和亲水性头部基团，头部基团在生理pH下既带有带正电荷又带负电荷的区域。 疏水性尾基稳定地连接到头基的正区域，该基团又通过易受膜结合和胞内因子切割的二硫键连接到负区。 二硫键的切割从头部基团中除去带负电荷的区域，导致一种阳离子脂质，并带有带负电荷的细胞膜。 因此，本发明的脂质可用作脂质体的组分，其作为用于将药剂递送到具有降低的毒性的细胞中的载体。

    Tubulysins and processes for preparing
    9.
    发明授权
    Tubulysins and processes for preparing 有权
    管状体和制备方法

    公开(公告)号：US09187521B2

    公开(公告)日：2015-11-17

    申请号：US12739579

    申请日：2008-10-23

    申请人： Iontcho Radoslavov Vlahov ,  Christopher Paul Leamon ,  Yu Wang

    发明人： Iontcho Radoslavov Vlahov ,  Christopher Paul Leamon ,  Yu Wang

    IPC分类号： A61K31/445 ,  C07K5/02

    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。

    Binding ligand linked drug delivery conjugates of tubulysins
    10.
    发明申请
    Binding ligand linked drug delivery conjugates of tubulysins 审中-公开
    肾上腺素的结合配体连接的药物递送共轭物

    公开(公告)号：US20130116195A1

    公开(公告)日：2013-05-09

    申请号：US13507076

    申请日：2012-06-01

    申请人： Christopher Paul Leamon ,  Iontcho Radoslavov Vlahov

    发明人： Christopher Paul Leamon ,  Iontcho Radoslavov Vlahov

    IPC分类号： A61K38/08

    CPC分类号： A61K38/08 ,  A61K47/551 ,  A61K47/595

    摘要： Described herein are compounds, pharmaceutical compositions, and methods for treating pathogenic cell populations. Kits including the compounds or pharmaceutical compositions are described. The compounds described herein include conjugates of tubulysins and folates. The conjugates also include a releasable bivalent linker.

    摘要翻译： 本文描述了用于治疗致病细胞群体的化合物，药物组合物和方法。 描述了包括化合物或药物组合物的试剂盒。 本文所述的化合物包括肾上腺素和叶酸盐的缀合物。 缀合物还包括可释放的二价连接体。