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    PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY
    4.
    发明公开
    PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY 审中-公开

    公开(公告)号：EP3334744A1

    公开(公告)日：2018-06-20

    申请号：EP16835928.9

    申请日：2016-08-11

    申请人： Galera Labs, LLC

    发明人： KEENE, Jeffery L. ,  SCHALL, Otto F. ,  RILEY, Dennis P.

    IPC分类号： C07F13/00 ,  C07F15/02 ,  C07F15/04 ,  C07F1/08

    CPC分类号： C07F13/005 ,  A61K9/0019 ,  A61K9/2866 ,  A61K9/4816 ,  A61K31/28 ,  A61K31/555 ,  A61K47/14 ,  A61K47/38 ,  A61K47/44

    摘要： Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands having the formula -OC(O)X1. (Formula A) each of the two axial ligands has the formula -OC(=O)X1 wherein each X1 is independently substituted or unsubstituted phenyl or -C(-X2)(-X3)(-X4); each X2 is independently substituted or unsubstituted phenyl, or substituted or unsubstituted alkyl; each X3 is independently hydrogen, hydroxyl, alkyl, amino, -X5C(=O)R13 where X5 is NH or O, and R13 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or -OR14, where R14 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or together with X4 is (=O); and each X4 is independenly hydrogen or together with X3 is (=O).

    Aqueous solutions of radiometal complexes with tridentate ligends
    5.
    发明授权
    Aqueous solutions of radiometal complexes with tridentate ligends 有权

    公开(公告)号：EP2708547B1

    公开(公告)日：2018-06-20

    申请号：EP13185433.3

    申请日：2009-03-10

    申请人： Universität Zürich

    发明人： Alberto, Roger ,  Braband, Henrik

    IPC分类号： C07F13/00 ,  A61K51/00

    CPC分类号： A61K51/0482 ,  C07F13/005

    摘要： A complex having the formula: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ [L 3 MO 3 ] n wherein L 3 represents a tridentate ligand, M represents a metal selected from Tc and Re, and n is a charge from -2 to +1, provided that L 3 is not di-1H-pyrazol-1-ylacetate, bis(3,5-dimethyl-1H-pyrazol-1-yl)acetate, 1,1,1-methanetriyltris(1H-pyrazole), 1,1,1-methanetriyltris(3,5-dimethyl-1H-pyrazole), 1,4,7-triazacyclononane, 1,4,7-trimethyltriazacyclononane, 1,4,7-trithiacyclononane, hydrotris(1-pyrazolyl)borate or [(· 5 -C 5 H 5 )Co{P(OR) 2 (=O)} 3 ] - , where R is methyl or ethyl; or a complex having the formula: [L 3 MO 3 ] n wherein L 3 represents a tridentate ligand bearing one or more functional groups suitable for facilitating the attachment of a targeting moiety, or bearing one or more linker groups capable of bearing such a functional groups, M represents a metal selected from Tc and Re, and n is a charge from -2 to +1, provide that, when L 3 bears one or more linker groups, none of which bears a functional group suitable for the attachment of a targeting moiety, at least one of the linker groups contains at least three carbon atoms, pharmaceutical compositions thereof, and dialato derivatives of [L 3 MO 3 ] n and methods for their synthesis.

    CONJUGATES DERIVED FROM NON-STEROIDAL ANTI-INFLAMMATORY DRUGS AND METHODS OF USE THEREOF IN IMAGING
    8.
    发明公开
    CONJUGATES DERIVED FROM NON-STEROIDAL ANTI-INFLAMMATORY DRUGS AND METHODS OF USE THEREOF IN IMAGING 审中-公开
    非甾体抑制剂及其方法利用影像学结合物

    公开(公告)号：EP3160514A1

    公开(公告)日：2017-05-03

    申请号：EP15812491.7

    申请日：2015-06-22

    申请人： Reiley Pharmaceuticals, Inc.

    发明人： REILEY, Mark A. ,  SILBER, B. Michael ,  MEDINA, Julio ,  KAYSER, Frank ,  SHRADER, William D.

    IPC分类号： A61K47/50

    CPC分类号： C07B59/004 ,  A61K51/0402 ,  A61K51/0478 ,  A61K51/0487 ,  A61K51/0497 ,  C07F13/00 ,  C07F13/005

    摘要： Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.

    摘要翻译： 从非甾体类抗炎药（NSAIDs）和它们的游离缺失盘的使用方法，对于有用的，除其他外，识别和定位病理学和/或炎症的负责疼痛的患者中的感觉的部位衍生缀合物; 用于鉴定伯，仲，良性或恶性肿瘤的部位; 以及用于诊断感染或确定或排除疑似感染。 基于NSAID偶联物包含在成像部分。 缀合物在集中增加环加氧酶表达的位点，从而揭示出其与疼痛和炎症相关，与肿瘤的存在和/或位置相关的增加的前列腺素产生的位点，所有。 COX增加哪些领域表现因此可以帮助筛选的感染。