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    LIPOPHILIC DIESTERS OF CHELATING AGENT FOR INHIBITION OF ENZYME ACTIVITY
    1.
    发明申请
    LIPOPHILIC DIESTERS OF CHELATING AGENT FOR INHIBITION OF ENZYME ACTIVITY 审中-公开
    用于抑制酶活性的螯合剂的锂离子电池

    公开(公告)号：WO2004028443A2

    公开(公告)日：2004-04-08

    申请号：PCT/IL2003/000225

    申请日：2003-03-16

    Applicant: D-PHARM LTD. ,  STRIEM, Sarina ,  FRIEDMAN, Jonathan, Eduard ,  REZNITSKY-COHEN, Dalia ,  KOZAK, Alexander

    Inventor： STRIEM, Sarina ,  FRIEDMAN, Jonathan, Eduard ,  REZNITSKY-COHEN, Dalia ,  KOZAK, Alexander

    IPC: A61K

    CPC classification number: A61K31/225

    Abstract: The present invention relates to the use of lipophilic diesters of the chelating agent 1,2-bis(2 aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA) for inhibition of proteolytic activities of certain metalloproteinases and of calpain. The invention further relates to methods for preventing, treating or managing MMP-related and calpain-related diseases or disorders in mammals comprising administering to a mammal in need thereof, a pharmaceutical composition comprising a therapeutically effective amount of said lipophilic diesters of the chelating agent BAPTA.

    Abstract translation: 本发明涉及螯合剂1,2-双（2-氨基苯氧基）乙烷-N，N，N'，N'-四乙酸（BAPTA）的亲脂性二酯用于抑制某些金属蛋白酶的蛋白水解活性和 钙蛋白酶。 本发明还涉及用于预防，治疗或管理哺乳动物中MMP-相关和钙蛋白酶相关疾病或病症的方法，其包括向有需要的哺乳动物施用包含治疗有效量的螯合剂BAPTA的所述亲脂性二酯的药物组合物 。

    COMPOSITIONS AND METHODS FOR REVERSIBLY INCREASING PERMEABILITY OF BIOMEMBRANES
    2.
    发明申请
    COMPOSITIONS AND METHODS FOR REVERSIBLY INCREASING PERMEABILITY OF BIOMEMBRANES 审中-公开
    可逆地提高生物膜渗透性的组合物和方法

    公开(公告)号：WO9902120A2

    公开(公告)日：1999-01-21

    申请号：PCT/IL9800317

    申请日：1998-07-07

    Applicant: DPHARM LTD ,  KOZAK ALEXANDER ,  VINIKOVA MARINA ,  SHAPIRO ISRAEL

    Inventor： VINIKOVA MARINA ,  SHAPIRO ISRAEL ,  KOZAK ALEXANDER

    IPC: A61K47/12 ,  A61K47/14 ,  A61K47/16 ,  A61K49/00 ,  C07C51/38 ,  C07C53/128 ,  A61K

    CPC classification number: C07C53/128

    Abstract: The present invention provides a family of branched fatty acids and their derivatives, which improve and enable the penetration and absorption of active ingredients through biomembranes, such as the blood brain barrier. The invention further provides pharmaceutical compositions comprising these branched fatty acids and methods of using these compositions to permeabilize biological membranes thereby improving the administration of bioactive or therapeutic substances to cells or organs. According to a more preferred embodiment of this invention the methods are particularly useful to treat certain kinds of CNS lesions and diseases including tumors, infections, abscesses and degenerative and behavioral disorders.

    Abstract translation: 本发明提供了一类支链脂肪酸及其衍生物，其通过生物膜如血脑屏障改善并使得活性成分能够渗透和吸收。 本发明进一步提供了包含这些支链脂肪酸的药物组合物以及使用这些组合物使生物膜透化从而改善生物活性或治疗性物质向细胞或器官的施用的方法。 根据本发明更优选的实施方案，所述方法特别适用于治疗某些种类的CNS损伤和疾病，包括肿瘤，感染，脓肿以及退行性和行为障碍。

    COMPOSITIONS AND METHODS FOR REVERSIBLY INCREASING PERMEABILITY OF BIOMEMBRANES
    4.
    发明申请
    COMPOSITIONS AND METHODS FOR REVERSIBLY INCREASING PERMEABILITY OF BIOMEMBRANES 审中-公开
    反应性增加生物膜渗透性的组合物和方法

    公开(公告)号：WO9902120A8

    公开(公告)日：2002-06-06

    申请号：PCT/IL9800317

    申请日：1998-07-07

    Applicant: DPHARM LTD ,  VINIKOVA MARINA ,  SHAPIRO ISRAEL ,  KOZAK ALEXANDER

    Inventor： VINIKOVA MARINA ,  SHAPIRO ISRAEL ,  KOZAK ALEXANDER

    IPC: A61K47/12 ,  A61K47/14 ,  A61K47/16 ,  A61K49/00 ,  C07C51/38 ,  C07C53/128 ,  C07C233/00 ,  C07F9/02

    CPC classification number: C07C53/128

    Abstract: The present invention provides a family of branched fatty acids and their derivatives, which improve and enable the penetration and absorption of active ingredients through biomembranes, such as the blood brain barrier. The invention further provides pharmaceutical compositions comprising these branched fatty acids and methods of using these compositions to permeabilize biological membranes thereby improving the administration of bioactive or therapeutic substances to cells or organs. According to a more preferred embodiment of this invention the methods are particularly useful to treat certain kinds of CNS lesions and diseases including tumors, infections, abscesses and degenerative and behavioral disorders.

    Abstract translation: 本发明提供了一种支链脂肪酸及其衍生物，其改善并且能够通过生物膜如血脑屏障渗透和吸收活性成分。 本发明进一步提供包含这些支链脂肪酸的药物组合物和使用这些组合物使生物膜透化从而改善对细胞或器官的生物活性或治疗物质的给药的方法。 根据本发明的一个更优选的实施方案，该方法特别适用于治疗某些种类的CNS病变和疾病，包括肿瘤，感染，脓肿和退行性和行为障碍。

    PRODRUGS WITH ENHANCED PENETRATION INTO CELLS
    5.
    发明申请
    PRODRUGS WITH ENHANCED PENETRATION INTO CELLS 审中-公开
    具有增强渗透入细胞的产品

    公开(公告)号：WO9422483A3

    公开(公告)日：1994-12-22

    申请号：PCT/GB9400669

    申请日：1994-03-30

    Applicant: KOSM GERALD EMMANUEL ,  DPHARM LTD ,  KOZAK ALEXANDER

    Inventor： KOZAK ALEXANDER

    IPC: C12P17/18 ,  A61K31/19 ,  A61K31/215 ,  A61K31/47 ,  A61K31/66 ,  A61K31/70 ,  A61K38/00 ,  A61K45/00 ,  A61K47/48 ,  A61P43/00 ,  C07F9/10 ,  C07F9/62 ,  C07F9/6558 ,  C07F9/6561

    CPC classification number: C07F9/10 ,  A61K47/54 ,  A61K47/542 ,  A61K47/544

    Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a human related to supranormal intracellular enzyme (.e.g. phospholipase and/or esterase) activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound accumulates selectively within cells having such supranormal intracellular enzyme activity. Exemplary conjugates are esters of the carboxylic function in the formula, with e.g. heptanoyl-sn-3-glycerophosphoryl-choline or octanoyl-sn-3-glycerophosphoryl-choline.

    Abstract translation: 本发明涉及药学上可接受的前体药物，其是药理学活性化合物和细胞内运输佐剂的共价缀合物，其特征在于存在对细胞内酶活性具有断裂敏感性的共价键。 前药可用于治疗与超细胞内酶（“磷脂酶和/或酯酶”）活动相关的人的病症或疾病的技术，由此在将其施用于具有这种病症或疾病的人时，该结合被破坏 响应于这种活性，并且药理活性化合物选择性地在具有这种超常规细胞内酶活性的细胞内积累。 共轭物是式中羧基官能团的酯， 庚酰基-sn-3-甘油磷酰胆碱或辛酰基-sn-3-甘油磷酰胆碱。

    PRODRUGS WITH ENHANCED PENETRATION INTO CELLS
    6.
    发明申请
    PRODRUGS WITH ENHANCED PENETRATION INTO CELLS 审中-公开
    具有增强渗透入细胞的产品

    公开(公告)号：WO1994022483A2

    公开(公告)日：1994-10-13

    申请号：PCT/GB1994000669

    申请日：1994-03-30

    Applicant: KOSMIN, Gerald, Emmanuel ,  D-PHARM, LTD. ,  KOZAK, Alexander

    Inventor： KOSMIN, Gerald, Emmanuel ,  D-PHARM, LTD.

    IPC: A61K47/48

    CPC classification number: C07F9/10 ,  A61K47/54 ,  A61K47/542 ,  A61K47/544

    Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a human related to supranormal intracellular enzyme (e.g. phospholipase and/or esterase) activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound accumulates selectively within cells having such supranormal intracellular enzyme activity. Exemplary conjugates are esters of the carboxylic function in the formula, with e.g. heptanoyl-sn-3-glycerophosphoryl-choline or octanoyl-sn-3-glycerophosphoryl-choline.

    Abstract translation: 本发明涉及药学上可接受的前体药物，其是药理学活性化合物和细胞内运输佐剂的共价缀合物，其特征在于存在对细胞内酶活性具有断裂敏感性的共价键。 该前体药物可用于治疗与超细胞内酶（例如磷脂酶和/或酯酶）活性相关的人的病症或疾病的技术，由此在将其施用于具有这种病症或疾病的人时，该结合被破坏 对这种活性的反应，并且药理活性化合物选择性地在具有这种超常规细胞内酶活性的细胞内积累。 共轭物是式中羧基官能团的酯， 庚酰基-sn-3-甘油磷酰胆碱或辛酰基-sn-3-甘油磷酰胆碱。

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