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    ACYLOXYALKYL CARBAMATE PRODRUGS OF TRANEXAMIC ACID, METHODS OF SYNTHESIS AND USE
    2.
    发明公开
    ACYLOXYALKYL CARBAMATE PRODRUGS OF TRANEXAMIC ACID, METHODS OF SYNTHESIS AND USE 有权
    ACYLOXYALKYLCARBAMAT-PRODRUGS VONTRANEXANSÄUREUND ANWENDUNG

    公开(公告)号：EP1919859A2

    公开(公告)日：2008-05-14

    申请号：EP06785134.5

    申请日：2006-06-20

    申请人： Xenoport, Inc.

    发明人： JANDELEIT, Bernd ,  LI, Yunxiao ,  ZERANGUE, Noa ,  GALLOP, Mark, A.

    IPC分类号： C07C271/22

    CPC分类号： C07C271/22 ,  C07B2200/07 ,  C07C2601/14

    摘要： Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)- cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)- cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.

    摘要翻译： 反式-4-（氨基甲基） - 环己烷羧酸的氨基甲酸烷氧基烷基酯前药，其药物组合物，制备反式-4-（氨基甲基） - 环己烷羧酸前体药物的方法，以及使用反式-4-（氨基甲基） - 环己烷羧酸及其药物组合物，用于治疗或预防各种疾病或病症。 还公开了反式-4-（氨基甲基） - 环己烷羧酸的氨基甲酸烷氧基烷基酯前药及其适用于口服和局部给药以及使用缓释剂型的给药的药物组合物。

    ENGINEERING ABSORPTION OF THERAPEUTIC COMPOUNDS VIA COLONIC TRANSPORTERS
    3.
    发明公开
    ENGINEERING ABSORPTION OF THERAPEUTIC COMPOUNDS VIA COLONIC TRANSPORTERS 审中-公开
    工程吸收KOLONTRANSPORTER的治疗性化合物

    公开(公告)号：EP1575494A2

    公开(公告)日：2005-09-21

    申请号：EP03737554.0

    申请日：2003-01-24

    申请人： Xenoport, Inc.

    发明人： ZERANGUE, Noa ,  CUNDY, Kenneth, C. ,  GALLOP, Mark, A.

    IPC分类号： A61K6/00

    CPC分类号： A61K47/64

    摘要： Methods of modifying therapeutic compounds such as drugs to be substrates for active transporters expressed in epithelial cells lining the lumen of the human colon are disclosed. The transporters expressed in the human colon include the sodium dependent multi-vitamin transporter (SMVT), and monocarboxylate transporters 1 and 4 (MCT 1 and MCT 4). The modified compounds can themselves be pharmacologically active, or upon cleavage of a chemical moiety after uptake from the colon, can be metabolized to form a compound that is pharmacologically active (e.g., a prodrug). The modified compounds disclosed herein are suitable for use in extended release oral dosage forms, particularly those that release drug over periods of greater than about 2-4 hours following administration.

    ADMINISTRATION OF AGENTS VIA THE PEPT-2 TRANSPORTER
    6.
    发明公开
    ADMINISTRATION OF AGENTS VIA THE PEPT-2 TRANSPORTER 审中-公开
    VERABREICHUNG VON MITTELNÜBERDEN PEPT-2-TRANSPORTER

    公开(公告)号：EP1406493A1

    公开(公告)日：2004-04-14

    申请号：EP02746512.9

    申请日：2002-06-11

    申请人： Xenoport, Inc.

    发明人： ZERANGUE, Noa ,  DIAS, Tracy ,  DOWER, William, J.

    IPC分类号： A01N37/18 ,  A61K38/00 ,  C07K1/00 ,  C07K14/00 ,  C07K16/00 ,  C07K17/00

    CPC分类号： C07D233/64 ,  A61K38/00 ,  A61K47/64 ,  C07C237/12 ,  C07C237/20 ,  C07C317/50 ,  C07C323/59 ,  C07C323/60 ,  C07C2601/14 ,  C07D207/16 ,  C07K5/0205 ,  G01N33/566

    摘要： The invention provides methods of screening agents, conjugates or conjugate moieties, linked or linkable to agents, for capacity to be transported as substrates through the PEPT2 transporter. The invention also provides methods of treatment involving delivery of agents that either alone, or as a result of linkage to a conjugate moiety, are substrates of the PEPT2 transporter. The invention also provides conjugates comprising a pharmaceutical agent which is linked to a conjugate moiety that is a substrate for a PEPT2 transporter.

    摘要翻译： 本发明提供了筛选能够通过PEPT2转运蛋白作为底物转运的能力的筛选试剂，缀合物或缀合物部分的方法，所述试剂，缀合物或缀合物部分与试剂连接或连接。 本发明还提供涉及递送药物的方法，所述药物单独或作为与缀合物部分连接的结果是PEPT2转运蛋白的底物。 本发明还提供了包含与作为PEPT2转运蛋白的底物的缀合物部分连接的药剂的缀合物。