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    Compositions and methods for treating pathologies that necessitate suppression of gastric acid secretion
    1.
    发明申请
    Compositions and methods for treating pathologies that necessitate suppression of gastric acid secretion 审中-公开
    用于治疗需要抑制胃酸分泌的病理的组合物和方法

    公开(公告)号：US20060135406A1

    公开(公告)日：2006-06-22

    申请号：US11351001

    申请日：2006-02-09

    申请人： Sabina Glozman ,  Ayelet David ,  Lada Paul

    发明人： Sabina Glozman ,  Ayelet David ,  Lada Paul

    IPC分类号： A61K38/54 ,  A61K31/4439

    CPC分类号： A61K38/2207 ,  A61K31/4439

    摘要： The present invention is related to novel oral compositions comprising an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor, pentagastrin (PG) or a PG analogue as an activator of parietal cells in the gastric lumen. In a preferred embodiment, the composition further comprises at least one agent that preserves the availability of PG in the gastric fluids, thus enabling PG to act locally in the stomach. Unexpectedly, the compositions of the present invention exhibit anti-acid activity locally in the stomach that is meal-independent, exhibit fast onset and prolonged inhibition of acid secretion.

    摘要翻译： 本发明涉及包含作为胃酸分泌抑制剂的不可逆胃H + / H + + / - ATP酶质粒泵抑制剂（PPI）的新型口服组合物，五加胃泌素（PG ）或PG类似物作为胃内腔壁细胞的激活剂。 在优选的实施方案中，组合物还包含至少一种保留胃液中PG的可用性的试剂，从而使PG能够局部地在胃中起作用。 意外地，本发明的组合物在胃中局部表现出与膳食无关的抗酸活性，表现出快速发作和延长的酸分泌抑制。

    Compositions and Methods for Inhibiting Gastric Acid Secretion
    3.
    发明申请
    Compositions and Methods for Inhibiting Gastric Acid Secretion 有权
    抑制胃酸分泌的组合物和方法

    公开(公告)号：US20100247634A1

    公开(公告)日：2010-09-30

    申请号：US12768375

    申请日：2010-04-27

    申请人： Aleksey Kostadinov ,  Ayelet David ,  Sabina Glozman

    发明人： Aleksey Kostadinov ,  Ayelet David ,  Sabina Glozman

    IPC分类号： A61K9/48 ,  A61K9/20 ,  A61K9/28 ,  A61K31/19 ,  A61K31/194

    CPC分类号： A61K31/19 ,  A61K9/2081 ,  A61K31/4439 ,  A61K47/12 ,  A61K2300/00

    摘要： The present invention is related to novel oral compositions comprising an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor and one or more small carboxylic acid molecules as parietal cell activators in the gastric lumen. Unexpectedly, the compositions of the present invention are capable of enhancing the anti-acid activity of PPI in the stomach. The present invention further relates to a method of using such compositions to reduce gastric acid secretion in a mammal.

    摘要翻译： 本发明涉及包含作为胃酸分泌抑制剂的不可逆胃H + / K + -ATP酶质子泵抑制剂（PPI）和作为胃内腔壁细胞活化剂的一种或多种小羧酸分子的新型口服组合物。 意外地，本发明的组合物能够增强胃中PPI的抗酸活性。 本发明还涉及使用这种组合物以减少哺乳动物胃酸分泌的方法。

    Composition and methods for inhibiting gastric acid secretion
    5.
    发明授权
    Composition and methods for inhibiting gastric acid secretion 有权
    用于抑制胃酸分泌的组合物和方法

    公开(公告)号：US07803817B2

    公开(公告)日：2010-09-28

    申请号：US11191688

    申请日：2005-07-27

    申请人： Aleksey Kostadinov ,  Ayelet David ,  Sabina Glozman

    发明人： Aleksey Kostadinov ,  Ayelet David ,  Sabina Glozman

    IPC分类号： A61K31/4439 ,  A61K31/194

    CPC分类号： A61K31/19 ,  A61K9/2081 ,  A61K31/4439 ,  A61K47/12 ,  A61K2300/00

    摘要： The present invention is related to oral compositions comprising an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor and succinc acid as a parietal cell activator in the gastric lumen. The compositions of the present invention are capable of enhancing the anti-acid activity of PPI in the stomach. The present invention further relates to a method of using such compositions to reduce gastric acid secretion in a mammal.

    摘要翻译： 本发明涉及含有作为胃酸分泌抑制剂的不可逆胃H + / K + -ATP酶质子泵抑制剂（PPI）和胃肠腔中作为壁细胞活化剂的琥珀酸的口服组合物。 本发明的组合物能够增强胃中PPI的抗酸活性。 本发明还涉及使用这种组合物以减少哺乳动物胃酸分泌的方法。

    TARGETED DELIVERY SYSTEMS FOR DIAGNOSTIC APPLICATIONS
    6.
    发明申请
    TARGETED DELIVERY SYSTEMS FOR DIAGNOSTIC APPLICATIONS 审中-公开
    用于诊断应用的目标交付系统

    公开(公告)号：US20130142734A1

    公开(公告)日：2013-06-06

    申请号：US13521345

    申请日：2011-01-11

    申请人： Ayelet David

    发明人： Ayelet David

    IPC分类号： A61K49/00

    CPC分类号： A61K49/0054 ,  A61K47/65 ,  A61K49/0032 ,  A61K49/0034

    摘要： Targeting of imaging probes specifically to diseased tissues such as cancer is attractive because it potentially allows the improvement of tumor detection. One of the problems associated with conventional, low molecular weight imaging probes is the limited tumor:background ratio. To circumvent this, imaging probes may be conjugated to polymeric carriers to target solid tumors by either passive accumulation of macromolecules into tumor tissues due to the “enhanced permeability and retention” effect (EPR effect) or active targeting through the incorporation of cell-specific recognition ligands that mediate binding to cancer-specific antigens. This invention describes an innovative targeting strategy for the selective delivery of diagnostic agents into solid tumors by means of polymer-NIR fluorochrome conjugates modified with targeting ligands that bind to antigens or receptors that are uniquely expressed or over-expressed on the target cells relative to normal tissues.

    摘要翻译： 成像探针特异性靶向患病组织如癌症是有吸引力的，因为它有可能改善肿瘤检测。 与传统的低分子量成像探针相关的问题之一是有限的肿瘤：背景比。 为了避免这种情况，由于“增强的通透性和保留”效应（EPR效应）或通过结合细胞特异性识别的主动靶向，成像探针可以通过被大量分子被动积累到肿瘤组织中而与聚合物载体缀合以靶向实体瘤 介导与癌症特异性抗原结合的配体。 本发明描述了一种创新的靶向策略，用于通过聚合物-NIR荧光染料缀合物将诊断剂选择性递送到实体瘤中，所述聚合物 - NIR荧光染料缀合物与靶向配体相结合，靶向配体与靶细胞相对于正常的单独表达或过表达的抗原或受体结合 组织。

    CAGED CELL PENETRATING PEPTIDE-POLYMER CONJUGATES FOR DIAGNOSTIC AND THERAPEUTIC APPLICATIONS
    7.
    发明申请
    CAGED CELL PENETRATING PEPTIDE-POLYMER CONJUGATES FOR DIAGNOSTIC AND THERAPEUTIC APPLICATIONS 审中-公开
    用于诊断和治疗应用的CAGED细胞渗透肽聚合物

    公开(公告)号：US20140017169A1

    公开(公告)日：2014-01-16

    申请号：US13700847

    申请日：2011-05-26

    申请人： Ayelet David ,  Gonen Ashkenasy ,  Yossi Shamay

    发明人： Ayelet David ,  Gonen Ashkenasy ,  Yossi Shamay

    IPC分类号： C07K9/00 ,  A61K47/32 ,  A61K49/00

    CPC分类号： C07K9/001 ,  A61K47/32 ,  A61K47/64 ,  A61K49/0002 ,  A61K49/0056

    摘要： The caged cell-penetrating peptide (cCPP) conjugates of this invention are ideal for intracellular delivery of a broad variety of cargoes including various nanoparticulate pharmaceutical carriers (liposomes, micelles, microparticles, nanoparticles, polymer-conjugates). The conjugates comprise a detectable agent or a therapeutic agent, and the conjugates provide a novel strategy for site-specific delivery of the same to appropriate tissues in the subject. Versatile application of the conjugates in diagnostics and imaging is described.

    摘要翻译： 本发明的笼状细胞穿透肽（cCPP）缀合物对于包括各种纳米颗粒药物载体（脂质体，胶束，微粒，纳米颗粒，聚合物共轭物）的多种货物的细胞内递送是理想的。 缀合物包含可检测的试剂或治疗剂，并且缀合物提供了将其相对于受试者的适当组织的位点特异性递送的新策略。 描述了共轭物在诊断和成像中的多用途应用。

    Vascular delivery systems
    9.
    发明授权
    Vascular delivery systems 有权
    血管输送系统

    公开(公告)号：US08840874B2

    公开(公告)日：2014-09-23

    申请号：US12954109

    申请日：2010-11-24

    申请人： Ayelet David ,  Gonen Ashkensy ,  Yosi Shamay

    发明人： Ayelet David ,  Gonen Ashkensy ,  Yosi Shamay

    IPC分类号： A61K31/785 ,  A61K38/10 ,  A61P35/00 ,  A61P35/04 ,  A61K47/48 ,  A61K49/00

    CPC分类号： A61K47/64 ,  A61K31/704 ,  A61K47/549 ,  A61K47/58 ,  A61K47/59 ,  A61K47/62 ,  A61K47/65 ,  A61K49/0017 ,  G01N33/5091

    摘要： The site-specific expression of selectins on endothelial cells of blood vessels during angiogenesis provides an opportunity to target anti-cancer drugs to the vascular endothelium to extend the range of the therapeutic effect. This invention describes an innovative drug targeting strategy for the selective delivery of the anticancer drugs to endothelial cells by means of polymer-drug conjugates modified with a carbohydrate ligand for the vascular selectins. A model chemotherapeutic drug, doxorubicin, and the E-selectin ligand, sLex, are attached to a biocompatible polymer (HPMA). The selective binding, cellular uptake, intracellular fate, and cell cytotoxicity of the polymer-bound drug are investigated in human endothelial cells.

    摘要翻译： 在血管生成期间，血管内皮细胞上的选择素的位点特异性表达提供了将抗癌药物靶向血管内皮的机会，以扩大治疗效果的范围。 本发明描述了通过用用于血管选择素的碳水化合物配体修饰的聚合物 - 药物缀合物选择性递送抗癌药物到内皮细胞的创新的药物靶向策略。 模型化疗药物多柔比星和E-选择蛋白配体sLex连接到生物相容性聚合物（HPMA）上。 在人内皮细胞中研究了聚合物结合药物的选择性结合，细胞摄取，细胞内命运和细胞毒性。