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    SYNTHETIC PLATELETS
    2.
    发明申请
    SYNTHETIC PLATELETS 审中-公开
    合成胶片

    公开(公告)号：US20080213369A1

    公开(公告)日：2008-09-04

    申请号：US11851718

    申请日：2007-09-07

    申请人： Maria I.C. Gyongyossy-Issa ,  Jayachandran N. Kizhakkedathu ,  Iren Constantinescu ,  William Campbell ,  Carlos A. Del Carpio Munoz

    发明人： Maria I.C. Gyongyossy-Issa ,  Jayachandran N. Kizhakkedathu ,  Iren Constantinescu ,  William Campbell ,  Carlos A. Del Carpio Munoz

    IPC分类号： A61K9/14 ,  A61K38/00 ,  A61P9/00

    CPC分类号： A61K9/1271 ,  A61K9/1277 ,  A61K35/19 ,  A61K47/6911

    摘要： A synthetic platelet substitute that interacts with platelets and the (sub)endothelium, comprising: (a) a carrier molecule comprising lipidic particles with a cross-linked surface mesh, the lipidic particles comprising: an inner lipidic particle of pharmaceutically acceptable particle-forming lipids; hydrophilic polymer chains linked to the surface of the lipidic particle, the hydrophilic polymer chains comprising a crosslinkable end group at free ends thereof; and cross-linker groups linking the end groups of the hydrophilic polymer chains to form the cross-linked surface mesh; and (b) at least one receptor molecule attached to the surface of the carrier molecule. The receptor molecule can be a peptide moiety specific for ligands involved in platelet function.

    摘要翻译： 一种与血小板和（亚）内皮相互作用的合成血小板替代物，其包含：（a）包含具有交联表面网的脂质颗粒的载体分子，所述脂质颗粒包含：药学上可接受的形成颗粒的脂质的内脂质颗粒 ; 亲水性聚合物链与脂质颗粒的表面连接，亲水性聚合物链在其自由端包含可交联端基; 和连接亲水性聚合物链的端基以形成交联表面网的交联剂基团; 和（b）至少一个连接于载体分子表面的受体分子。 受体分子可以是特异于参与血小板功能的配体的肽部分。

    Peptide mimotopes that inhibits interaction between a platelet receptor and a platelet receptor ligand
    4.
    发明授权
    Peptide mimotopes that inhibits interaction between a platelet receptor and a platelet receptor ligand 有权
    抑制血小板受体和血小板受体配体之间相互作用的肽模拟表位

    公开(公告)号：US07919465B2

    公开(公告)日：2011-04-05

    申请号：US12546811

    申请日：2009-08-25

    申请人： Maria I. C. Gyongyossy-Issa ,  Dana V. Devine ,  Iren Constantinescu ,  William Campbell ,  Carlos A. Del Carpio Munoz

    发明人： Maria I. C. Gyongyossy-Issa ,  Dana V. Devine ,  Iren Constantinescu ,  William Campbell ,  Carlos A. Del Carpio Munoz

    IPC分类号： A61K38/10

    CPC分类号： C07K14/705 ,  A61K38/00 ,  A61K47/60

    摘要： It is provided mimotope receptors and inhibitors that employ peptide mimics that mimic the shape and function of natural receptors and ligands, thus providing synthetic binding sites for ligands and receptors. Receptor mimics can be attached to carriers, such as liposomes, to act as synthetic platelets, for example, by providing multiple binding sites for binding to other (natural or synthetic) platelets or to the endothelium. Synthetic platelets would have virtually limitless shelf life and would not require disease screening prior to transfusion, thereby providing a solution to the perpetual platelet shortages, as well as the safety and storage issues associated with natural blood platelets.

    摘要翻译： 提供了模拟表位受体和抑制剂，其使用模拟天然受体和配体的形状和功能的肽模拟物，从而提供配体和受体的合成结合位点。 受体模拟物可以与载体例如脂质体连接起作为合成血小板，例如通过提供与其它（天然或合成的）血小板或内皮结合的多个结合位点。 合成血小板将具有几乎无限的保质期，并且在输血之前不需要疾病筛查，从而提供对永久血小板缺乏症以及与天然血小板相关的安全和储存问题的解决方案。

    Mimotope receptors and inhibitors for platelet-platelet and platelet-endothelium interactions
    6.
    发明申请
    Mimotope receptors and inhibitors for platelet-platelet and platelet-endothelium interactions 审中-公开
    用于血小板 - 血小板和血小板 - 内皮相互作用的模拟表位受体和抑制剂

    公开(公告)号：US20080015145A1

    公开(公告)日：2008-01-17

    申请号：US11484364

    申请日：2006-07-11

    申请人： Maria Gyongyossy-Issa ,  Dana V. Devine ,  Iren Constantinescu ,  William Campbell ,  Carlos del Carpio Munoz

    发明人： Maria Gyongyossy-Issa ,  Dana V. Devine ,  Iren Constantinescu ,  William Campbell ,  Carlos del Carpio Munoz

    IPC分类号： A61K38/17 ,  C07K14/705

    CPC分类号： C07K14/705 ,  A61K38/00 ,  A61K47/60

    摘要： Mimotope receptors and inhibitors employ peptide mimics that mimic the shape and function of natural receptors and ligands, thus providing synthetic binding sites for ligands and receptors. Receptor mimics can be attached to carriers, such as liposomes, to act as synthetic platelets, for example, by providing binding sites for binding to other (natural or synthetic) platelets or to the endothelium. Synthetic platelets would have virtually limitless shelf life and would not require disease screening prior to transfusion, thereby providing a solution to the perpetual platelet shortages, as well as the safety and storage issues associated with natural blood platelets. Mimotope inhibitors (either free-molecule receptors or ligands) can act as antithrombotics by inhibiting platelet-platelet or platelet-endothelium interactions. Ligand mimics are preferably D-peptides that resist proteolytic degradation. Furthermore, these ligand mimics can also be attached to carriers for resisting excretion, thus forming the basis for a new class of antithrombotic drugs.

    摘要翻译： 模拟表位受体和抑制剂使用模仿天然受体和配体的形状和功能的肽模拟物，从而为配体和受体提供合成结合位点。 受体模拟物可以连接到载体，例如脂质体，以作为合成血小板，例如通过提供与其他（天然或合成的）血小板或内皮结合的结合位点。 合成血小板将具有几乎无限的保质期，并且在输血之前不需要疾病筛查，从而提供对永久血小板缺乏症以及与天然血小板相关的安全和储存问题的解决方案。 模拟表位抑制剂（自由分子受体或配体）可以通过抑制血小板 - 血小板或血小板 - 内皮相互作用而作为抗血栓形成。 配体模拟物优选是抵抗蛋白水解降解的D肽。 此外，这些配体模拟物也可以连接到载体以抵抗排泄，从而形成新类型抗血栓药物的基础。

    SURFACE CROSS-LINKED LIPIDIC PARTICLES, METHODS OF PRODUCTION AND USES THEREFOR
    7.
    发明申请
    SURFACE CROSS-LINKED LIPIDIC PARTICLES, METHODS OF PRODUCTION AND USES THEREFOR 审中-公开
    表面交联的亲脂粒子，其生产方法及其用途

    公开(公告)号：US20080063621A1

    公开(公告)日：2008-03-13

    申请号：US11851671

    申请日：2007-09-07

    申请人： Maria Gyongyossy-Issa ,  Jayachandran Kizhakkedathu ,  Iren Constantinescu

    发明人： Maria Gyongyossy-Issa ,  Jayachandran Kizhakkedathu ,  Iren Constantinescu

    IPC分类号： A61K31/01 ,  A61K31/74 ,  A61P43/00

    CPC分类号： A61K9/1271 ,  A61K9/1277 ,  A61K35/19 ,  A61K47/6911

    摘要： A method for producing a composition of lipidic particles coated with a cross-linked surface mesh, the method comprising the steps of: (i) preparing lipidic particles comprising pharmaceutically acceptable lipids, (ii) binding hydrophilic polymer chains to the surface of the lipidic particles, and (iii) cross-linking the hydrophilic polymer chains to form the cross-linked surface mesh. Pharmaceutical compositions comprising surface modified lipidic particles prepared according to this method are also described. The lipidic particles resist fusion with red blood cells and platelets in vitro, and are amenable to further derivatization by targeting molecules for controlled release of component and contents, thus providing a new generation of drug carrier systems.

    摘要翻译： 一种制备涂覆有交联表面网的脂质颗粒的组合物的方法，所述方法包括以下步骤：（i）制备包含药学上可接受的脂质的脂质颗粒，（ii）将亲水性聚合物链结合到脂质颗粒的表面 ，和（iii）交联亲水性聚合物链以形成交联表面网。 还描述了包含根据该方法制备的表面改性脂质颗粒的药物组合物。 脂质颗粒体外抵抗与红细胞和血小板的融合，并且适于通过靶向分子进一步衍生化以控制组分和内容物的释放，从而提供新一代的药物载体体系。