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    USE OF INTRACELLULAR ENZYMES FOR THE RELEASE OF COVALENTLY LINKED BIOACTIVES
    1.
    发明申请
    USE OF INTRACELLULAR ENZYMES FOR THE RELEASE OF COVALENTLY LINKED BIOACTIVES 审中-公开
    用于释放共连接生物活性的细胞内酶的使用

    公开(公告)号：WO2012129112A2

    公开(公告)日：2012-09-27

    申请号：PCT/US2012029504

    申请日：2012-03-16

    申请人： CATABASIS PHARMACEUTICALS INC ,  JIROUSEK MICHAEL R ,  MILNE JILL C ,  CARNEY DAVID ,  BEMIS JEAN E ,  VU CHI B

    发明人： JIROUSEK MICHAEL R ,  MILNE JILL C ,  CARNEY DAVID ,  BEMIS JEAN E ,  VU CHI B

    IPC分类号： A61K31/455

    CPC分类号： A61K47/48338 ,  A61K31/194 ,  A61K31/198 ,  A61K31/202 ,  A61K31/455 ,  A61K31/60 ,  A61K31/618 ,  A61K45/06 ,  A61K47/542 ,  A61K47/55 ,  A61K47/65 ,  A61K2300/00

    摘要： The present invention relates to targeting an intracellular enzyme for release of covalently linked bioactives which results in a synergistic effect between the bioactives. The present invention relates to the use of bioactives that are directly connected covalently or through a covalent molecular linker which have increased therapeutic activity when released as the free bioactives by intracellular enzymes as compared to when the bioactives are administered individually (i.e. not covalently linked). Further, methods are described of administering to patients in need thereof, bioactives as linked bioactives having increased therapeutic activity. Accordingly, this invention also relates to methods of treating patients for certain diseases.

    摘要翻译： 本发明涉及靶向细胞内酶以释放共价连接的生物活性物质，其导致生物活性物之间的协同作用。 本发明涉及当与单独施用生物活性（即不共价连接）相比时，通过共价直接连接或通过共价分子接头直接连接的生物活性物质，其通过细胞内酶释放作为游离生物活性时具有增加的治疗活性。 此外，描述了向有需要的患者施用作为具有增加的治疗活性的相关生物活性物的生物活性物质的方法。 因此，本发明还涉及治疗患者某些疾病的方法。

    SIRTUIN MODULATING COMPOUNDS
    4.
    发明申请
    SIRTUIN MODULATING COMPOUNDS 审中-公开
    SIRTUIN调节化合物

    公开(公告)号：WO2008156869A2

    公开(公告)日：2008-12-24

    申请号：PCT/US2008/007776

    申请日：2008-06-20

    申请人： SIRTRIS PHARMACEUTICALS, INC. ,  BEMIS, Jean ,  DISCH, Jeremy, S. ,  NG, Pui, Yee ,  OALMANN, Christopher ,  PERNI, Robert, B. ,  VU, Chi, B.

    发明人： BEMIS, Jean ,  DISCH, Jeremy, S. ,  NG, Pui, Yee ,  OALMANN, Christopher ,  PERNI, Robert, B. ,  VU, Chi, B.

    IPC分类号： C07D513/04 ,  A61K31/437 ,  A61P3/10

    CPC分类号： C07D513/04

    摘要： Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin- modulating compound in combination with another therapeutic agent.

    摘要翻译： 本文提供了新的沉默调节蛋白的调节化合物及其使用方法。 沉默调节蛋白的调节化合物可用于增加细胞的寿命，以及治疗和/或预防各种各样的疾病和病症，包括例如与老化或紧张相关的疾病或病症，糖尿病，肥胖症，神经变性疾病， 心血管疾病，血液凝固障碍，炎症，癌症和/或潮红以及将受益于增加的线粒体活性的疾病或病症。 还提供了包含沉默调节蛋白的调节性化合物与另一种治疗剂组合的组合物。

    AMIDE DERIVATIVES OF 16-MEMBERED RING ANTIBIOTIC MACROLIDES
    7.
    发明申请
    AMIDE DERIVATIVES OF 16-MEMBERED RING ANTIBIOTIC MACROLIDES 审中-公开
    16成环抗生素的酰胺衍生物

    公开(公告)号：WO1995002594A1

    公开(公告)日：1995-01-26

    申请号：PCT/IB1994000199

    申请日：1994-07-04

    申请人： PFIZER INC. ,  LUNDY, Kristin, Marie ,  VU, Chi, B.

    发明人： PFIZER INC.

    IPC分类号： C07D407/12

    CPC分类号： C07H17/08

    摘要： The present invention relates to amide derivatives of formula (I) or (II) of 19-carboxy-19-deformyl 16-membered ring macrolide antibiotics rosaramicin, repromicin, tylosin, 5-O-mycaminosyltylonolide, 4-deoxy-O-mycaminosyltylonolide, desmycosin, lactenocin, O-demethyllactenocin, cirramycin A1, and 23-deoxymycaminosyltylonolide, which are useful against bacterial and mycoplasmic pathogens in aminals. Also claimed are a pharmaceutical composition of such derivatives and their use in treating bacterial and mycoplasmic infections in animals.

    摘要翻译： 本发明涉及19-羧基-19-变形的16-元环大环内酯类抗生素罗曲霉素，repromicin，泰乐菌素，5-O-碳霉糖基太乐内酯，4-脱氧-O-碳霉糖基太乐内酯， 脱敏霉素，乳内聚合素，O-去甲基乳杆菌素，西拉霉素A1和23-脱氧霉素基太乐内酯，其可用于胰腺中的细菌和支原体病原体。 还要求保护这些衍生物的药物组合物及其在治疗动物细菌和支原体感染中的用途。