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    NOVEL SINGLE CHEMICAL ENTITIES AND METHODS FOR DELIVERY OF OLIGONUCLEOTIDES
    2.
    发明公开
    NOVEL SINGLE CHEMICAL ENTITIES AND METHODS FOR DELIVERY OF OLIGONUCLEOTIDES 审中-公开
    用于递送寡核苷酸的新型单一化学实体和方法

    公开(公告)号：EP2611927A1

    公开(公告)日：2013-07-10

    申请号：EP11822416.1

    申请日：2011-08-29

    申请人： Merck Sharp & Dohme Corp.

    发明人： COLLETTI, Steven, L. ,  GOSSELIN, Francis ,  JADHAV, Vasant, R. ,  SHAW, Anthony, W. ,  TELLERS, David, M. ,  TUCKER, Thomas, J. ,  YUAN, Yu ,  ZEWGE, Daniel

    IPC分类号： C12P21/06

    CPC分类号： C12N15/113 ,  A61K47/64 ,  C12N15/111 ,  C12N15/87 ,  C12N2310/14 ,  C12N2310/3513 ,  C12N2310/3515 ,  C12N2320/32

    摘要： In an embodiment the instant invention discloses a modular composition comprising 1) an oligonueleotide; 2) one or more linkers, which may be the same or different, selected from Table 1, wherein the linkers are attached to the oligonucleotide at the 2'-position of the ribose rings and/or the terminal 3'- and/or 5'-positions of the oligonucleotide; 3) optionally, one or more peptides, which may be the same or different, selected from SEQ ID NOs: 1-59, wherein the peptides are attached to the linkers; and optionally one or more lipids, solubilizing groups and/or targeting ligands attached to the oligonucleotide.

    摘要翻译： 在一个实施方案中，本发明公开了一种模块化组合物，其包含1）寡核苷酸; 2）选自表1的一个或多个接头，其可以是相同或不同的，其中所述接头在核糖环的2'-位置和/或末端3'-和/或5'-位置与寡核苷酸连接 寡核苷酸的'位置; 3）任选地，选自SEQ ID NO：1-59的一种或多种可相同或不同的肽，其中所述肽连接于所述接头; 和任选地与寡核苷酸连接的一种或多种脂质，增溶基团和/或靶向配体。

    CGRP RECEPTOR ANTAGONISTS
    4.
    发明授权
    CGRP RECEPTOR ANTAGONISTS 有权
    CGRP受体拮抗剂

    公开(公告)号：EP1615914B1

    公开(公告)日：2010-05-05

    申请号：EP04750028.5

    申请日：2004-04-09

    申请人： Merck Sharp & Dohme Corp.

    发明人： BURGEY, Christopher, S. ,  PAONE, Daniel, V. ,  SHAW, Anthony, W. ,  WILLIAMS, Theresa, M.

    IPC分类号： C07D413/14 ,  C07D405/14 ,  A61K31/4545 ,  C07D401/14 ,  A61P25/06

    CPC分类号： C07D401/14 ,  C07D413/14

    摘要： The present invention is directed to compounds of Formula I and Formula II: (where variables R1, R2, R3, R4, R6, A, B, G, J, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

    摘要翻译： 本发明涉及用作CGRP拮抗剂的式I和式II化合物（其中变量R 1，R 2，R 3，R 4，R 6，A，B，G，J，W，X和Y如本文所定义） 受体，并可用于治疗或预防与CGRP有关的疾病，例如头痛，偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的此类疾病中的用途。

    CGRP RECEPTOR ANTAGONISTS
    6.
    发明授权
    CGRP RECEPTOR ANTAGONISTS 有权
    CGRP受体拮抗剂

    公开(公告)号：EP1802372B1

    公开(公告)日：2011-05-04

    申请号：EP05803913.2

    申请日：2005-10-12

    申请人： Merck Sharp & Dohme Corp.

    发明人： PAONE, Daniel, V. ,  SHAW, Anthony, W. ,  POTTEIGER, Craig, M.

    IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D401/00 ,  C07D487/00

    CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

    摘要： Compounds of Formula (I) and Formula (II) (where variables R1, R2, R4, A, B, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

    摘要翻译： 式（I）和式（II）化合物（其中变量R 1，R 2，R 4，A，B，W，X，Y和Z如本文所定义）可用作CGRP受体的拮抗剂并可用于治疗或预防 涉及CGRP的疾病，如头痛，偏头痛和丛集性头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的此类疾病中的用途。